Reaxys
PubChem
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Reactions (68)
Substances (47)
Structure
Citations (508)
Structure/Compound Data Chemical Name: Modafinil Reaxys Registry Number: 1978970
CAS Registry Number: 112111-43-0, 112111-47-4, 112111-49-6, 68693-11-8 Type of Substance: isocyclic Molecular Formula: C15H15NO2S Linear Structure Formula: C15H15NO2S Molecular Weight: 273.356
InChI Key: YFGHCGITMMYXAQ-UHFFFAOYSA-N
1
N° of preparations All Preps | All Reactions 20 prep out of 23 reactions.
Available Data
N° of ref.
Identification Physical Data (14) Spectra (21) Bioactivity (150) Other Data (327)
469
Synthesize | Hide Details Find similar Chemical Names and Synonyms Modafinil Identification Substance Label (21) Label
Reference
2
Jung, Jae-Chul; Lee, Yeonju; Son, Jee-Young; Lim, Eunyoung; Jung, Mankil; Oh, Seikwan
Molecules, 2012 , vol. 17, # 9 p. 10446 - 10458 Title/Abstract Full Text View citing articles Show Details
Cao, Jianjing; Slack, Rachel D.; Bakare, Oluyomi M.; Burzynski, Caitlin; Rais, Rana; Slusher, Barbara S.; Kopajtic, Theresa; Bonifazi, Alessandro; Ellenberger, Michael P.; Yano, Hideaki; He, Yi; Bi, Guo-Hua; Xi, Zheng-Xiong; Loland, Claus J.; Newman, Amy Hauck
Journal of Medicinal Chemistry, 2016 , vol. 59, # 23 p. 10676 - 10691 Title/Abstract Full Text View citing articles Show Details
RAC-MOD
Krasulova, Kristyna; Siller, Michal; Holas, Ondrej; Dvorak, Zdenek; Anzenbacher, Pavel
Xenobiotica, 2016 , vol. 46, # 4 p. 315 - 324
Title/Abstract Full Text View citing articles Show Details
3o
Neveselý, Tomáš; Svobodová, Eva; Chudoba, Josef; Sikorski, Marek; Cibulka, Radek
Advanced Synthesis and Catalysis, 2016 , vol. 358, # 10 p. 1654 - 1663 Title/Abstract Full Text View citing articles Show Details
5
KANDULA, Mahesh
Patent: WO2013/179153 A1, 2013 ; Title/Abstract Full Text Show Details
Kandula, Mahesh
Patent: US2015/141513 A1, 2015 ; Title/Abstract Full Text Show Details
10l
Šturala, Jiří; Boháčová, Soňa; Chudoba, Josef; Metelková, Radka; Cibulka, Radek
Journal of Organic Chemistry, 2015 , vol. 80, # 5 p. 2676 - 2699 Title/Abstract Full Text View citing articles Show Details
9h
Hartman, Tomáš; Šturala, Jiří; Cibulka, Radek
Advanced Synthesis and Catalysis, 2015 , vol. 357, # 16-17 p. 3573 - 3586 Title/Abstract Full Text View citing articles Show Details
(±)-1
Okunola-Bakare, Oluyomi M.; Cao, Jianjing; Kopajtic, Theresa; Katz, Jonathan L.; Loland, Claus J.; Shi, Lei; Newman, Amy Hauck
Journal of Medicinal Chemistry, 2014 , vol. 57, # 3 p. 1000 - 1013 Title/Abstract Full Text View citing articles Show Details
1
Lesur, Brigitte; Lin, Yin G.; Marcy, Val R.; Aimone, Lisa D.; Gruner, John; Bacon, Edward R.; Chatterjee, Sankar
Chemical Biology and Drug Design, 2013 , vol. 81, # 3 p. 429 - 432 Title/Abstract Full Text View citing articles Show Details
I
GENERICS [UK] LIMITED; MYLAN DEVELOPMENT CENTRE PRIVATE LIMITED
Patent: WO2008/149141 A2, 2008 ; Title/Abstract Full Text Show Details
200
MALLINCKRODT INC.
Patent: WO2007/70238 A2, 2007 ; Title/Abstract Full Text Show Details
(+/-)-3
Prisinzano, Thomas; Podobinski, John; Tidgewell, Kevin; Luo, Min; Swenson, Dale
Tetrahedron Asymmetry, 2004 , vol. 15, # 6 p. 1053 - 1058 Title/Abstract Full Text View citing articles Show Details
Negwer8 5346
Taneja, Indu; Bruehl, Stephen; Robertson, David
Journal of Clinical Pharmacology, 2004 , vol. 44, # 12 p. 1425 - 1427 Title/Abstract Full Text View citing articles Show Details
CRL 40476-[f I]
CEPHALON FRANCE; ORGANISATION DE SYNTHESE MONDIALE ORSYMONDE
Patent: WO2004/14846 A1, 2004 ; Title/Abstract Full Text Show Details
CRL 40476-[f III]
CEPHALON FRANCE; ORGANISATION DE SYNTHESE MONDIALE ORSYMONDE
Patent: WO2004/14846 A1, 2004 ;
CRL 40476-[f IV]
CEPHALON FRANCE; ORGANISATION DE SYNTHESE MONDIALE ORSYMONDE
Patent: WO2004/14846 A1, 2004 ;
CRL 40476-[f VII]
CEPHALON FRANCE; ORGANISATION DE SYNTHESE MONDIALE ORSYMONDE
Patent: WO2004/14846 A1, 2004 ;
CRL 40476-[f VI]
CEPHALON FRANCE; ORGANISATION DE SYNTHESE MONDIALE ORSYMONDE
Patent: WO2004/14846 A1, 2004 ;
CRL 40476-[f V]
CEPHALON FRANCE; ORGANISATION DE SYNTHESE MONDIALE ORSYMONDE
Patent: WO2004/14846 A1, 2004 ;
Title/Abstract Full Text Show Details
Title/Abstract Full Text Show Details
Title/Abstract Full Text Show Details
Title/Abstract Full Text Show Details
Title/Abstract Full Text Show Details
M12: 6311
Wong, Y. Nancy; King, S. Peter; Laughton, Watson B.; McCormick, George C.; Grebow, Peter E.
Journal of Clinical Pharmacology, 1998 , vol. 38, # 3 p. 276 - 282 Title/Abstract Full Text View citing articles Show Details
MODA
Vezin; Daveloose; Debouzy; Fauvelle; Roussel; Viret
Bollettino Chimico Farmaceutico, 1994 , vol. 133, # 7 p. 476 - 481 Title/Abstract Full Text View citing articles Show Details
Label
Reference
CRL 40476
Lab. Lafon
Patent: DE2809625US4177290 , 19781979 ; Chem.Abstr., vol. 93, # 7872 Full Text Show Details
Patent-Specific Data (4) Related Markush Structure (RN)
Reference FECHTER, Cary Erwin
Patent: WO2016/209765 A1, 2016 ;
30987469
Title/Abstract Full Text Show Details
27378387; 27378388
THE UNITED STATES OF AMERICA, AS REPRESENTED BY THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICES; NEWMAN, Amy Hauck; OKUNOLABAKARE, Oluyomi M.; CAO, Jianjing
Patent: WO2014/138518 A2, 2014 ; Title/Abstract Full Text Show Details
The Board of Trustees of the University of Arkansas
Patent: US2008/221216 A1, 2008 ;
18499450
Title/Abstract Full Text Show Details
MALLINCKRODT INC.
Patent: WO2007/70238 A2, 2007 ;
11339069
Title/Abstract Full Text Show Details
Physical Data Melting Point (6) Melting Point
Solvent (Melting Point)
159 160 °C
Location
Reference
Paragraph 0112
Kandula, Mahesh
Patent: US2015/141513 A1, 2015 ; Title/Abstract Full Text Show Details
161 162 °C
methanol
Paragraph 0112
Kandula, Mahesh
Patent: US2015/141513 A1, 2015 ; Title/Abstract Full Text Show Details
120 122 °C
161 162 °C
methanol
supporting information
Bogolubsky, Andrey V.; Moroz, Yurii S.; Mykhailiuk, Pavel K.; Ostapchuk, Eugeniy N.; Rudnichenko, Alexander V.; Dmytriv, Yurii V.; Bondar, Anna N.; Zaporozhets, Olga A.; Pipko, Sergey E.; Doroschuk, Roman A.; Babichenko, Liudmyla N.; Konovets, Anzhelika I.; Tolmachev, Andrey
ACS Combinatorial Science, 2015 , vol. 17, # 6 p. 348 - 354 Title/Abstract Full Text View citing articles Show Details
Paragraph 00101
KANDULA, Mahesh
Patent: WO2013/179153 A1, 2013 ; Title/Abstract Full Text Show Details
164 165 °C
isopropyl alcohol N,Ndimethyl-
Bicherov; Akopova; Spiglazov; Morkovnik
Russian Chemical Bulletin, 2010 , vol. 59, # 1 p. 91 - 101 Title/Abstract Full Text View citing articles Show Details
formamide SEPRACOR INC.
Patent: WO2005/63248 A1, 2005 ;
163 165 °C
Title/Abstract Full Text Show Details
Chromatographic Data (3) Chromatographic data
Original string
Location
Reference Jeong, Eun Sook; Kim, So-Hee; Cha, Eun-Ju; Lee, Kang Mi; Kim, Ho Jun; Lee, Sang-Won; Kwon, Oh-Seung; Lee, Jaeick
Rapid Communications in Mass Spectrometry, 2015 , vol. 29, # 4 p. 367 - 384 Title/Abstract Full Text View citing articles Show Details
Jeong, Eun Sook; Kim, So-Hee; Cha, Eun-Ju; Lee, Kang Mi; Kim, Ho Jun; Lee, Sang-Won; Kwon, Oh-Seung; Lee, Jaeick
Rapid Communications in Mass Spectrometry, 2015 , vol. 29, # 4 p. 367 - 384 Title/Abstract Full Text Show Details
LC (Liquid chromatography)
TLC (Thin layer chromatography)
R&f %0.6
Kandula, Mahesh
Patent: US2015/141513 A1, 2015 ;
Paragraph 0112
Title/Abstract Full Text Show Details
TLC (Thin layer chromatography)
R&f% 0.6
Paragraph 00101
KANDULA, Mahesh
Patent: WO2013/179153 A1, 2013 ; Title/Abstract Full Text Show Details
Crystal Property Description (4) Colour & Other Properties white
Location
Reference
Paragraph 0112
Kandula, Mahesh
Patent: US2015/141513 A1, 2015 ; Title/Abstract Full Text Show Details
white
supporting information
Bogolubsky, Andrey V.; Moroz, Yurii S.; Mykhailiuk, Pavel K.; Ostapchuk, Eugeniy N.; Rudnichenko, Alexander V.; Dmytriv, Yurii V.; Bondar, Anna N.; Zaporozhets, Olga A.; Pipko, Sergey E.; Doroschuk, Roman A.; Babichenko, Liudmyla N.; Konovets, Anzhelika I.; Tolmachev, Andrey
ACS Combinatorial Science, 2015 , vol. 17, # 6 p. 348 - 354 Title/Abstract Full Text View citing articles Show Details
white
Paragraph 00101
KANDULA, Mahesh
Patent: WO2013/179153 A1, 2013 ; Title/Abstract Full Text Show Details
MALLINCKRODT INC.
Patent: WO2007/70238 A2, 2007 ;
white
Title/Abstract Full Text Show Details
TEVA PHARMACEUTICAL INDUSTRIES LTD.; TEVA PHARMACEUTICALS USA, INC.
Patent: WO2007/103221 A2, 2007 ; Title/Abstract Full Text Show Details
Solubility (MCS) (1) Solubility
Saturation
Temperature (Solubility (MCS))
Solvent (Solubility (MCS))
0.136678 g·l-1
in solution
25 °C
phosphate buffer
Reference Alelyunas, Yun W.; Empfield, James R.; McCarthy, Dennis; Spreen, Russell C.; Bui, Khanh; Pelosi-Kilby, Luciana; Shen, Cindy
Bioorganic and Medicinal Chemistry Letters, 2010 , vol. 20, # 24 p. 7312 - 7316 Title/Abstract Full Text View citing articles Show Details
Spectra NMR Spectroscopy (15) Description (NMR Spectroscopy)
Nucleus (NMR Spectroscopy)
Coupling Nuclei
Solvents (NMR Spectroscopy)
Temperature (NMR Spectroscopy)
Frequency (NMR Spectroscopy)
Original Text (NMR Spectroscopy)
Location
Comment (NMR Spectroscopy)
Reference
Chemical shifts Spectrum
1H
chloroform-d1
300 MHz
supporting information
Neveselý, Tomáš; Svobodová, Eva; Chudoba, Josef; Sikorski, Marek; Cibulka, Radek
Advanced Synthesis and Catalysis, 2016 , vol. 358, # 10 p. 1654 - 1663 Title/Abstract Full Text View citing articles Show Details
Chemical shifts Spectrum
13C
chloroform-d1
101 MHz
supporting information
Neveselý, Tomáš; Svobodová, Eva; Chudoba, Josef; Sikorski, Marek; Cibulka, Radek
Advanced Synthesis and Catalysis, 2016 , vol. 358, # 10 p. 1654 - 1663 Title/Abstract Full Text View citing articles Show Details
Spectrum
1H
supporting information
Šturala, Jiří; Boháčová, Soňa; Chudoba, Josef; Metelková, Radka; Cibulka, Radek
Journal of Organic Chemistry, 2015 , vol. 80, # 5 p. 2676 - 2699 Title/Abstract Full Text View citing articles Show Details
Chemical shifts Spectrum
1H
dimethylsulfoxided6
500 MHz
supporting information
Bogolubsky, Andrey V.; Moroz, Yurii S.; Mykhailiuk, Pavel K.; Ostapchuk, Eugeniy N.; Rudnichenko, Alexander V.; Dmytriv, Yurii V.; Bondar, Anna N.; Zaporozhets, Olga A.; Pipko, Sergey E.; Doroschuk, Roman A.; Babichenko, Liudmyla N.; Konovets, Anzhelika I.; Tolmachev, Andrey
ACS Combinatorial Science, 2015 , vol. 17, # 6 p. 348 - 354 Title/Abstract Full Text View citing articles Show Details
Chemical shifts Spectrum
13C
dimethylsulfoxided6
125.7 MHz
supporting information
Bogolubsky, Andrey V.; Moroz, Yurii S.; Mykhailiuk, Pavel K.; Ostapchuk, Eugeniy N.; Rudnichenko, Alexander V.; Dmytriv, Yurii V.; Bondar, Anna N.; Zaporozhets, Olga A.; Pipko, Sergey E.; Doroschuk, Roman A.; Babichenko, Liudmyla N.; Konovets, Anzhelika I.; Tolmachev, Andrey
ACS Combinatorial Science, 2015 , vol. 17, # 6 p. 348 - 354 Title/Abstract Full Text View citing articles Show Details
Chemical shifts Spectrum
1H
dimethylsulfoxided6
24.84 °C
399.9 MHz
supporting information
Hartman, Tomáš; Šturala, Jiří; Cibulka, Radek
Advanced Synthesis and Catalysis, 2015 , vol. 357, # 16-17 p. 3573 - 3586 Title/Abstract Full Text View citing articles Show Details
Chemical shifts Spectrum
13C
dimethylsulfoxided6
24.84 °C
supporting information
Hartman, Tomáš; Šturala, Jiří; Cibulka, Radek
Advanced Synthesis and Catalysis, 2015 , vol. 357, # 16-17 p. 3573 - 3586 Title/Abstract Full Text View citing articles Show Details
Chemical shifts
1H
chloroform-d1
Chemical shifts
1H
dimethylsulfoxided6
Vezin; Daveloose; Debouzy; Fauvelle; Roussel; Viret
Bollettino Chimico Farmaceutico, 1994 , vol. 133, # 7 p. 476 - 481 Title/Abstract Full Text View citing articles Show Details
Prisinzano, Thomas; Podobinski, John; Tidgewell, Kevin; Luo, Min; Swenson, Dale
Tetrahedron Asymmetry, 2004 , vol. 15, # 6 p. 1053 - 1058 Title/Abstract Full Text View citing articles Show Details
Chemical shifts
13C
dimethylsulfoxided6
Vezin; Daveloose; Debouzy; Fauvelle; Roussel; Viret
Bollettino Chimico Farmaceutico, 1994 , vol. 133,
300 MHz
Bicherov; Akopova; Spiglazov; Morkovnik
Russian Chemical Bulletin, 2010 , vol. 59, # 1 p. 91 - 101 Title/Abstract Full Text View citing articles Show Details
# 7 p. 476 - 481 Title/Abstract Full Text View citing articles Show Details
Prisinzano, Thomas; Podobinski, John; Tidgewell, Kevin; Luo, Min; Swenson, Dale
Tetrahedron Asymmetry, 2004 , vol. 15, # 6 p. 1053 - 1058 Title/Abstract Full Text View citing articles Show Details 1H
1H
1H
chloroform-d1
1H
chloroform-d1
1H
chloroform-d1
Spin-spin coupling constants
Prisinzano, Thomas; Podobinski, John; Tidgewell, Kevin; Luo, Min; Swenson, Dale
Tetrahedron Asymmetry, 2004 , vol. 15, # 6 p. 1053 - 1058 Title/Abstract Full Text View citing articles Show Details
dimethylsulfoxided6
1H NMR (CDCl3): 3.223.27 ppm, d, 1H, (S(O)CH2); 3.63-3.68 ppm, d, 1H, (J=12.5 Hz), (S(O)CH2); 5.32 ppm, s, 1H, (S(O)CHPh2); 7.38 - 7.5 ppm, m, 10H, (Aromatic).
Signals given
3.22 -3.27 ppm d 1H S(O)CH2 3.63 -3.68 ppm d 1H (J = 12.5 Hz) S(O)CH2 5.32 ppm s 1H S(O)CHPh2 7.38 - 7.5 ppm m 10H Aromatic
Signals given
H-NMR (CDC13, 5 ppm): 3. 223. 27 (d, 1H); 3. 63-3. 68 (d, 1H) (J = 12 Hz); 5. 32 (s, 1H) ; 7. 38 7. 49 (m, 10 H).
Signals given
dimethylsulfoxided6
Dipharma S.p.A.
Patent: EP1466897 A1, 2004 ; Title/Abstract Full Text Show Details
DINAMITE DIPHARMA S.P.A. abbreviated DIPHARMA S.P.A.
Patent: US2004/192929 A1, 2004 ; Title/Abstract Full Text Show Details
DINAMITE DIPHARMA S.P.A., in abbreviated form DIPHARMA S.P.A.
Patent: WO2003/95423 A1, 2003 ; Title/Abstract Full Text Show Details
1H-1H
Vezin; Daveloose; Debouzy; Fauvelle; Roussel; Viret
Bollettino Chimico Farmaceutico, 1994 , vol. 133, # 7 p. 476 - 481 Title/Abstract Full Text View citing articles Show Details
IR Spectroscopy (1) Description (IR Spectroscopy)
Comment (IR Spectroscopy)
Reference
Bands
neat (no solvent, solid phase)
Bicherov; Akopova; Spiglazov; Morkovnik
Russian Chemical Bulletin, 2010 , vol. 59, # 1 p. 91 - 101 Title/Abstract Full Text View citing articles Show Details
Mass Spectrometry (5) Description (Mass Spectrometry)
Location
Comment (Mass Spectrometry)
Reference
liquid chromatography mass spectrometry (LCMS) electrospray ionisation (ESI) spectrum
Jeong, Eun Sook; Kim, So-Hee; Cha, Eun-Ju; Lee, Kang Mi; Kim, Ho Jun; Lee, Sang-Won; Kwon, Oh-Seung; Lee, Jaeick
Rapid Communications in Mass Spectrometry, 2015 , vol. 29, # 4 p. 367 - 384 Title/Abstract Full Text Show Details
electrospray ionisation
Jeong, Eun Sook; Kim, So-Hee; Cha, Eun-Ju; Lee, Kang Mi; Kim, Ho Jun; Lee, Sang-Won; Kwon, Oh-Seung; Lee, Jaeick
(ESI) spectrum
Rapid Communications in Mass Spectrometry, 2015 , vol. 29, # 4 p. 367 - 384 Title/Abstract Full Text View citing articles Show Details
APCI (atmospheric pressure chemical ionization) spectrum
Bogolubsky, Andrey V.; Moroz, Yurii S.; Mykhailiuk, Pavel K.; Ostapchuk, Eugeniy N.; Rudnichenko, Alexander V.; Dmytriv, Yurii V.; Bondar, Anna N.; Zaporozhets, Olga A.; Pipko, Sergey E.; Doroschuk, Roman A.; Babichenko, Liudmyla N.; Konovets, Anzhelika I.; Tolmachev, Andrey
ACS Combinatorial Science, 2015 , vol. 17, # 6 p. 348 - 354 Title/Abstract Full Text View citing articles Show Details
supporting information
Vonaparti; Lyris; Angelis; Panderi; Koupparis; Tsantili-Kakoulidou; Peters; Nielen; Georgakopoulos
Rapid Communications in Mass Spectrometry, 2010 , vol. 24, # 11 p. 1595 - 1609 Title/Abstract Full Text View citing articles Show Details
HRMS (High resolution mass spectrometry) TOFMS (Time of flight mass spectrum) ESI (Electrospray ionisation) LCMS (Liquid chromatography mass spectrometry) Spectrum LCMS (Liquid chromatography mass spectrometry) ESI (Electrospray ionisation) Tandem mass spectrometry Spectrum
mol peak
Thoerngren, John-Olof; Oestervall, Fredrik; Garle, Mats
Journal of Mass Spectrometry, 2008 , vol. 43, # 7 p. 980 - 992 Title/Abstract Full Text View citing articles Show Details
Bioactivity Pharmacological Data (150) 1 of 150
Comment (Pharmacological Data)
Bioactivities present
Reference
Laboratoire L. Lafon
Patent: US4177290 A1, 1979 ; Title/Abstract Full Text Show Details
CHEMAGIS LTD.
Patent: US2002/183552 A1, 2002 ; Title/Abstract Full Text Show Details
CEPHALON, INC.
Patent: WO2003/99774 A1, 2003 ; Title/Abstract Full Text Show Details
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CEPHALON FRANCE; ORGANISATION DE SYNTHESE MONDIALE ORSYMONDE
Patent: WO2004/14846 A1, 2004 ; Title/Abstract Full Text Show Details
DINAMITE DIPHARMA S.P.A., in abbreviated form DIPHARMA S.P.A.
Patent: WO2003/95423 A1, 2003 ; Title/Abstract Full Text Show Details
DINAMITE DIPHARMA S.P.A. abbreviated DIPHARMA S.P.A.
Patent: US2004/192929 A1, 2004 ; Title/Abstract Full Text Show Details
Dipharma S.p.A.
Patent: EP1466897 A1, 2004 ; Title/Abstract Full Text Show Details
Orsymonde (Organisation de synthese Mondiale)
Patent: EP1477476 A1, 2004 ; Title/Abstract Full Text Show Details
PediaMed Pharmaceuticals, Inc.
Patent: US2004/259809 A1, 2004 ; Title/Abstract Full Text Show Details
Ray, Anup Kumar; Nandi, Indranil; Palaniswamy, Suresh; Davila, Pablo; Vora, Aakanksha Harshad
Patent: US2005/8704 A1, 2005 ; Title/Abstract Full Text Show Details
Ayala, William J.
Patent: US2005/31688 A1, 2005 ;
Title/Abstract Full Text Show Details
CEPHALON, INC.
Patent: WO2005/27890 A1, 2005 ; Title/Abstract Full Text Show Details
MALLINCKRODT INC.?
Patent: WO2005/42479 A1, 2005 ; Title/Abstract Full Text Show Details
BECTON, DICKINSON and COMPANY
Patent: WO2005/46701 A1, 2005 ; Title/Abstract Full Text Show Details
Barbera, Gary; Doshi, Chetan Chhabildas; Patel, Mahendra R.; Davila, Pablo; Patel, Satishkumar Ambalal
Patent: US2005/249814 A1, 2005 ; Title/Abstract Full Text Show Details
Cypress Bioscience, Inc.
Patent: US2006/39866 A1, 2006 ; Title/Abstract Full Text Show Details
Melker, Richard J.; Gold, Mark S.
Patent: US2006/62734 A1, 2006 ; Title/Abstract Full Text Show Details
CEPHALON INC.
Patent: WO2006/30278 A1, 2006 ; Title/Abstract Full Text Show Details
CENTRE FOR ADDICTION AND MENTAL HEALTH
Patent: WO2006/32146 A1, 2006 ; Title/Abstract Full Text Show Details
2 of 150
Comment (Pharmacological Data)
Bioactivities present
Reference
Feuerstein, Seth; Coric, Vladimir
Patent: US2006/167068 A1, 2006 ; Title/Abstract Full Text Show Details
Carter, Andrew
Patent: US2006/222627 A1, 2006 ; Title/Abstract Full Text Show Details
Mutual Pharmaceutical Company, Inc.
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MICELL TECHNOLOGIES, INC.
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NEUROHEALING PHARMACEUTICALS, INC.
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Cypress Bioscience, Inc.
Patent: US2007/72946 A1, 2007 ; Title/Abstract Full Text Show Details
Mallinckrodt Inc.
Patent: US2007/129444 A1, 2007 ; Title/Abstract Full Text Show Details
MALLINCKRODT INC.
Patent: WO2007/70238 A2, 2007 ; Title/Abstract Full Text Show Details
BOEHRINGER INGELHEIM INTERNATIONAL GMBH; BOEHRINGER INGELHEIM PHARMA GMBH and CO. KG
Patent: WO2007/93624 A2, 2007 ; Title/Abstract Full Text Show Details
TEVA PHARMACEUTICAL INDUSTRIES LTD.; TEVA PHARMACEUTICALS USA, INC.
Patent: WO2007/103221 A2, 2007 ; Title/Abstract Full Text Show Details
Cephalon France
Patent: US2006/24370 A1, 2006 ; Title/Abstract Full Text Show Details
BrainCells, Inc.
Patent: US2007/270449 A1, 2007 ; Title/Abstract Full Text Show Details
HIKMA PHARMACEUTICALS
Patent: US2007/275057 A1, 2007 ; Title/Abstract Full Text Show Details
QUESTCOR PHARMACEUTICALS, INC.
Patent: WO2008/3093 A2, 2008 ; Title/Abstract Full Text Show Details
NEUROHEALING PHARMACEUTICALS, INC.
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CYPRESS BIOSCIENCE, INC.
Patent: WO2008/21932 A2, 2008 ; Title/Abstract Full Text Show Details
BrainCells, Inc.
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THERAQUEST BIOSCIENCES, INC.
Patent: WO2008/33351 A2, 2008 ; Title/Abstract Full Text Show Details
BRAINCELLS, INC.
Patent: WO2008/39863 A2, 2008 ; Title/Abstract Full Text Show Details
BrainCells, Inc.
Patent: US2008/103165 A1, 2008 ; Title/Abstract Full Text Show Details
3 of 150
Comment (Pharmacological Data)
Bioactivities present
Reference
HAAS, Magali
Patent: US2008/103199 A1, 2008 ; Title/Abstract Full Text Show Details
Lab. L. Lafon S.A.
Patent: DE2809625 , 1978 ; Chem.Abstr., vol. 90, # 22644 Full Text Show Details
Lab. Lafon
Patent: DE2809625US4177290 , 19781979 ; Chem.Abstr., vol. 93, # 7872 Full Text Show Details
Saletu; Frey; Krupka; Anderer; Grunberger; Barbanoj
Arzneimittel-Forschung/Drug Research, 1989 , vol. 39, # 10 p. 1268 - 1273 Title/Abstract Full Text View citing articles Show Details
Vezin; Daveloose; Debouzy; Fauvelle; Roussel; Viret
Bollettino Chimico Farmaceutico, 1994 , vol. 133, # 7 p. 476 - 481 Title/Abstract Full Text View citing articles Show Details
Tanganelli; de la Mora; Ferraro; Mendez-Franco; Beani; Rambert; Fuxe
European Journal of Pharmacology, 1995 , vol. 273, # 1-2 p. 63 - 71 Title/Abstract Full Text View citing articles Show Details
Ferraro, Luca; Tanganelli, Sergio; O'Connor, William Thomas; Antonelli, Tiziana; Rambert, Francis; Fuxe, Kjell
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Robertson Jr., Philmore; Hellriegel, Edward T.; Arora, Sanjay; Nelson, Michael
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Prisinzano, Thomas; Podobinski, John; Tidgewell, Kevin; Luo, Min; Swenson, Dale
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Harvanová, Marianna; Gondová, Taťána
Journal of Pharmaceutical and Biomedical Analysis, 2017 , vol. 138, p. 267 - 271 Title/Abstract Full Text View citing articles Show Details
Newsome, Scott D.; Aliotta, Philip J.; Bainbridge, Jacquelyn; Bennett, Susan E.; Cutter, Gary; Fenton, Kaylan; Lublin, Fred; Northrop, Dorothy; Rintell, David; Walker, Bryan D.; Weigel, Megan; Zackowski, Kathleen; Jones, David E.
International Journal of MS Care, 2017 , vol. 19, # 1 p. 42 - 56 Title/Abstract Full Text View citing articles Show Details
Touitou, Yvan; Reinberg, Alain; Touitou, David
Life Sciences, 2017 , vol. 173, p. 94 - 106 Title/Abstract Full Text View citing articles Show Details
Franke, Andreas G.; Gränsmark, Patrik; Agricola, Alexandra; Schühle, Kai; Rommel, Thilo; Sebastian, Alexandra; Balló, Harald E.; Gorbulev, Stanislav; Gerdes, Christer; Frank, Björn; Ruckes, Christian; Tüscher, Oliver; Lieb, Klaus
European Neuropsychopharmacology, 2017 , vol. 27, # 3 p. 248 - 260 Title/Abstract Full Text View citing articles Show Details
Nardone, Raffaele; Orioli, Andrea; Golaszewski, Stefan; Brigo, Francesco; Sebastianelli, Luca; Höller, Yvonne; Frey, Vanessa; Trinka, Eugen
Journal of Spinal Cord Medicine, 2017 , vol. 40, # 1 p. 8 - 16 Title/Abstract Full Text View citing articles Show Details
Jang, Sung Ho; Seo, Jeong Pyo
Medicine (United States), 2017 , vol. 96, # 7 art. no. E6103 Title/Abstract Full Text View citing articles Show Details
Ballester, Javier; Valentine, Gerald; Sofuoglu, Mehmet
Expert Review of Clinical Pharmacology, 2017 , vol. 10, # 3 p. 305 - 314 Title/Abstract Full Text View citing articles Show Details
Lopez, Régis; Barateau, Lucie; Evangelista, Elisa; Chenini, Sofiene; Robert, Philippe; Jaussent, Isabelle; Dauvilliers, Yves
Sleep, 2017 , vol. 40, # 1 Title/Abstract Full Text Show Details
Kaser, Muzaffer; Deakin, Julia B.; Michael, Albert; Zapata, Camilo; Bansal, Rachna; Ryan, Dragana; Cormack, Francesca; Rowe, James B.; Sahakian, Barbara J.
Biological Psychiatry: Cognitive Neuroscience and Neuroimaging, 2017 , vol. 2, # 2 p. 115 - 122 Title/Abstract Full Text View citing articles Show Details
Khalili-Mahani, Najmeh; Rombouts, Serge A. R. B.; van Osch, Matthias J. P.; Duff, Eugene P.; Carbonell, Felix; Nickerson, Lisa D.; Becerra, Lino; Dahan, Albert; Evans, Alan C; Soucy, Jean-Paul; Wise, Richard; Zijdenbos, Alex P.; van Gerven, Joop M.
Human Brain Mapping, 2017 , vol. 38, # 4 p. 2276 - 2325 Title/Abstract Full Text View citing articles Show Details
Krähenbüh, Stephan
Therapeutische Umschau, 2016 , vol. 73, # 11 p. 701 - 706 Title/Abstract Full Text Show Details
Rottoli, Mariarosa; La Gioia, Sara; Frigeni, Barbara; Barcella, Valeria
Expert Review of Neurotherapeutics, 2017 , vol. 17, # 4 p. 373 - 379 Title/Abstract Full Text Show Details
Kollb-Sielecka, Marta; Demolis, Pierre; Emmerich, Joseph; Markey, Greg; Salmonson, Tomas; Haas, Manuel
Sleep Medicine, 2017 , vol. 33, p. 125 - 129 Title/Abstract Full Text Show Details
Coulon, Philippe; Landisman, Carole E.
Neuron, 2017 , vol. 93, # 6 p. 1275 - 1295 Title/Abstract Full Text Show Details
Bennett, Trevor; Holloway, Katy
International Journal of Drug Policy, 2017 , vol. 44, p. 12 - 22 Title/Abstract Full Text Show Details
Nicholson, Paul J.; Wilson, Nigel
British Journal of General Practice, 2017 , vol. 67, # 656 p. 100 - 101 Title/Abstract Full Text Show Details
Liu, Feng; Wang, Xuefeng
Expert Review of Neurotherapeutics, 2017 , vol. 17, # 5 p. 475 - 485 Title/Abstract Full Text Show Details
Gan, Shaoyan; Yin, Junjie; Yao, Yuan; Liu, Yang; Chang, Denghu; Zhu, Dan; Shi, Lei
Organic and Biomolecular Chemistry, 2017 , vol. 15, # 12 p. 2647 - 2654 Title/Abstract Full Text Show Details
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Comment (Pharmacological Data)
Bioactivities present
Reference
Dowling, Geraldine; Kavanagh, Pierce V.; Talbot, Brian; O’Brien, John; Hessman, Gary; McLaughlin, Gavin; Twamley, Brendan; Brandt, Simon D.
Drug Testing and Analysis, 2017 , vol. 9, # 3 p. 518 - 528 Title/Abstract Full Text Show Details
Brandt, Simon D.; Kavanagh, Pierce V.
Drug Testing and Analysis, 2017 , vol. 9, # 3 p. 342 - 346 Title/Abstract Full Text Show Details
Kolderová, Natalie; Neveselý, Tomáš; Šturala, Jiří; Kuchař, Martin; Holakovský, Roman; Kohout, Michal
Chromatographia, 2017 , vol. 80, # 4 p. 547 - 557 Title/Abstract Full Text Show Details
Heersmink, Richard
Phenomenology and the Cognitive Sciences, 2017 , vol. 16, # 1 p. 17 - 32 Title/Abstract Full Text Show Details
Matoulek, Martin; Tuka, Vladimír; Fialová, Magdalena; Nevšímalová, Soňa; Šonka, Karel
Sleep Medicine, 2017 , vol. 34, p. 7 - 12 Title/Abstract Full Text Show Details
Johnson, Adrian; Hamilton, Trevor James
PeerJ, 2017 , vol. 2017, # 2 art. no. E2994 Title/Abstract Full Text Show Details
Inamoto, Yoshihiro; Lee, Stephanie J.
Haematologica, 2017 , vol. 102, # 4 p. 614 - 625 Title/Abstract Full Text Show Details
FECHTER, Cary Erwin
Patent: WO2016/209765 A1, 2016 ; Title/Abstract Full Text Show Details
Weiergräber, Marco; Ehninger, Dan; Broich, Karl
Medizinische Monatsschrift fur Pharmazeuten, 2017 , vol. 40, # 4 p. 154 - 166 Title/Abstract Full Text Show Details
Sim, Juhyun; Kim, Eunmi; Yang, Wonkyung; Woo, Sanghee; In, Sangwhan
Forensic Science International, 2017 , vol. 274, p. 91 - 98 Title/Abstract Full Text Show Details
Hodges, Sarah E.; Pittman, Brian; Morgan, Peter T.
Sleep, 2017 , vol. 40, # 3 art. no. ZSW069 Title/Abstract Full Text Show Details
Shin, Eun-Joo; Dang, Duy-Khanh; Tran, The-Vinh; Tran, Hai-Quyen; Jeong, Ji Hoon; Nah, Seung-Yeol; Jang, Choon-Gon; Yamada, Kiyofumi; Nabeshima, Toshitaka; Kim, Hyoung-Chun
Archives of Pharmacal Research, 2017 , vol. 40, # 4 p. 403 - 428 Title/Abstract Full Text Show Details
Kahn, René S.; Sommer, Iris E.; Murray, Robin M.; Meyer-Lindenberg, Andreas; Weinberger, Daniel R.; Cannon, Tyrone D.; O'Donovan, Michael; Correll, Christoph U.; Kane, John M.; Van Os, Jim; Insel, Thomas R.
Nature Reviews Disease Primers, 2015 , vol. 1, art. no. 15067 Title/Abstract Full Text Show Details
Sergeeva, Olga A.; De Luca, Roberto; Mazur, Karolina; Chepkova, Aissa N.; Haas, Helmut L.; Bauer, Andreas
Neuropharmacology, 2017 , vol. 119, p. 111 - 122 Title/Abstract Full Text Show Details
Hoffmann, Anika; Müller, Hermann L.
Minerva Endocrinologica, 2017 , vol. 42, # 2 p. 132 - 144 Title/Abstract Full Text Show Details
Wolf, Carl E.; Poklis, Justin L.; Cumpston, Kirk; Moss, Michael; Poklis, Alphonse
Drug Testing and Analysis, 2017 , vol. 9, # 4 p. 657 - 659 Title/Abstract Full Text Show Details
Punzi, Miriam; Gili, Tommaso; Petrosini, Laura; Caltagirone, Carlo; Spalletta, Gianfranco; Sensi, Stefano L.
Frontiers in Aging Neuroscience, 2017 , vol. 9, # MAR art. no. 85 Title/Abstract Full Text Show Details
Fayette; Gahérová; Móciková; Marková; Kozák; Horáček
Klinicka Onkologie, 2017 , vol. 30, # 2 p. 93 - 99 Title/Abstract Full Text Show Details
Drugs and Therapy Perspectives, 2017 , vol. 33, # 5 p. 222 - 226 Title/Abstract Full Text Show Details
Lashch; Boiko
Nevrologiya, Neiropsikhiatriya, Psikhosomatika, 2016 , vol. 8, # 1 p. 82 - 85 Title/Abstract Full Text Show Details
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Comment (Pharmacological Data)
Bioactivities present
Reference
Mohammed, Zeid; Grunze, Heinz
Neuropsychiatry, 2016 , vol. 6, # 3 p. 96 - 111 Title/Abstract Full Text Show Details
Black, Sarah Wurts; Yamanaka, Akihiro; Kilduff, Thomas S.
Progress in Neurobiology, 2017 , vol. 152, p. 89 - 113 Title/Abstract Full Text Show Details
Grabb, Margaret C.; Gobburu, Jogarao V.S.
Progress in Neurobiology, 2017 , vol. 152, p. 38 - 57 Title/Abstract Full Text Show Details
Lazuras, Lambros; Ypsilanti, Antonia; Lamprou, Efthymios; Kontogiorgis, Christos
Substance Use and Misuse, 2017 , vol. 52, # 7 p. 950 - 958 Title/Abstract Full Text Show Details
Everts, Sarah
Chemical and Engineering News, 2017 , vol. 95, # 12 p. 25 - 26 Title/Abstract Full Text Show Details
Morley, Kirsten C.; Cornish, Jennifer L.; Faingold, Alon; Wood, Katie; Haber, Paul S.
Expert Opinion on Investigational Drugs, 2017 , vol. 26, # 5 p. 563 - 578 Title/Abstract Full Text Show Details
West, Caroline; Konjaria, Mari-Luiza; Shashviashvili, Natia; Lemasson, Elise; Bonnet, Pascal; Kakava, Rusudan; Volonterio, Alessandro; Chankvetadze, Bezhan
Journal of Chromatography A, 2017 , vol. 1499, p. 174 - 182 Title/Abstract Full Text Show Details
Lu, Cong; Shi, Zhe; Dong, Liming; Lv, Jingwei; Xu, Pan; Li, Yinghui; Qu, Lina; Liu, Xinmin
Phytotherapy Research, 2017 , vol. 31, # 5 p. 763 - 770 Title/Abstract Full Text Show Details
Bivard, Andrew; Lillicrap, Thomas; Krishnamurthy, Venkatesh; Holliday, Elizabeth; Attia, John; Pagram, Heather; Nilsson, Michael; Parsons, Mark; Levi, Christopher R.
Stroke, 2017 , vol. 48, # 5 p. 1293 - 1298 Title/Abstract Full Text Show Details
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Comment (Pharmacological Data)
physiological behaviour discussed
Reference
Krasulova, Kristyna; Siller, Michal; Holas, Ondrej; Dvorak, Zdenek; Anzenbacher, Pavel
Xenobiotica, 2016 , vol. 46, # 4 p. 315 - 324 Title/Abstract Full Text View citing articles Show Details
Comment (Pharmacological Data)
physiological behaviour discussed
Reference
Saroja, Sivaprakasam R.; Aher, Yogesh D.; Kalaba, Predrag; Aher, Nilima Y.; Zehl, Martin; Korz, Volker; Subramaniyan, Saraswathi; Miklosi, Andras G.; Zanon, Lisa; Neuhaus, Winfried; Höger, Harald; Langer, Thierry; Urban, Ernst; Leban, Johann; Lubec, Gert
Behavioural Brain Research, 2016 , vol. 312, p. 127 - 137 Title/Abstract Full Text View citing articles Show Details
Comment (Pharmacological Data)
physiological behaviour discussed
Reference
Martínez-Guerrero, Lucy J.; Morales, Mark; Ekins, Sean; Wright, Stephen H.
Molecular Pharmacology, 2016 , vol. 90, # 3 p. 254 - 264 Title/Abstract Full Text View citing articles Show Details
Comment (Pharmacological Data)
physiological behaviour discussed
Reference
SK Biopharmaceuticals Co., Ltd.; Khayrallah, Moise A.; Bream, Gary; Butts, Stephen E.; Melnick, Susan Marie; Taylor, Duncan
Patent: US9464041 B2, 2016 ; Title/Abstract Full Text Show Details
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Comment (Pharmacological Data)
physiological behaviour discussed
Reference
Cao, Jianjing; Slack, Rachel D.; Bakare, Oluyomi M.; Burzynski, Caitlin; Rais, Rana; Slusher, Barbara S.; Kopajtic, Theresa; Bonifazi, Alessandro; Ellenberger, Michael P.; Yano, Hideaki; He, Yi; Bi, Guo-Hua; Xi, Zheng-Xiong; Loland, Claus J.; Newman, Amy Hauck
Journal of Medicinal Chemistry, 2016 , vol. 59, # 23 p. 10676 - 10691 Title/Abstract Full Text View citing articles Show Details
Location
Paragraph
Comment (Pharmacological Data)
physiological behaviour discussed
Reference
FECHTER, Cary Erwin
Patent: WO2016/209765 A1, 2016 ; Title/Abstract Full Text Show Details
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Location
Page/Page column
Comment (Pharmacological Data)
physiological behaviour discussed
Reference
COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES; MOUTHON, Franck; CHARVERIAT, Mathieu
Patent: WO2015/11246 A1, 2015 ; Title/Abstract Full Text Show Details
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Comment (Pharmacological Data)
physiological behaviour discussed
Reference
Zolkowska, Dorota; Andres-Mach, Marta; Prisinzano, Thomas E.; Baumann, Michael H.; Luszczki, Jarogniew J.
Psychopharmacology, 2015 , vol. 232, # 14 art. no. 3884, p. 2463 - 2479 Title/Abstract Full Text View citing articles Show Details
Comment (Pharmacological Data)
physiological behaviour discussed
Reference
Okunola-Bakare, Oluyomi M.; Cao, Jianjing; Kopajtic, Theresa; Katz, Jonathan L.; Loland, Claus J.; Shi, Lei; Newman, Amy Hauck
Journal of Medicinal Chemistry, 2014 , vol. 57, # 3 p. 1000 - 1013 Title/Abstract Full Text View citing articles Show Details
Comment (Pharmacological Data)
physiological behaviour discussed
Reference
THE UNITED STATES OF AMERICA, AS REPRESENTED BY THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICES; NEWMAN, Amy Hauck; OKUNOLA-BAKARE, Oluyomi M.; CAO, Jianjing
Patent: WO2014/138518 A2, 2014 ; Title/Abstract Full Text Show Details
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Comment (Pharmacological Data)
physiological behaviour discussed
Reference
EWHA UNIVERSITY-INDUSTRY COLLABORATION FOUNDATION; Suh, Suk Hyo; Jung, Jae Chul; Oh, Sei Kwan
Patent: US2014/296333 A1, 2014 ; Title/Abstract Full Text Show Details
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Comment (Pharmacological Data)
physiological behaviour discussed
Reference
Gonzlez, Betina; Raineri, Mariana; Cadet, Jean Lud; Garca-Rill, Edgar; Urbano, Francisco J.; Bisagno, Veronica
Neuropharmacology, 2014 , vol. 87, p. 188 - 197 Title/Abstract Full Text View citing articles Show Details
Effect (Pharmacological Data)
pharmacokinetics
Species or Test-System (Pharmacological Data)
rat
Route of Application
intraperitoneal
Type (Pharmacological Data)
wake 3 h AUC
Value of Type (Pharmacological Data)
117 min
Reference
Lesur, Brigitte; Lin, Yin G.; Marcy, Val R.; Aimone, Lisa D.; Gruner, John; Bacon, Edward R.; Chatterjee, Sankar
Chemical Biology and Drug Design, 2013 , vol. 81, # 3 p. 429 - 432 Title/Abstract Full Text View citing articles Show Details
Effect (Pharmacological Data)
pharmacokinetics
Species or Test-System (Pharmacological Data)
rat
Route of Application
intraperitoneal
Type (Pharmacological Data)
wake 4 h AUC
Value of Type (Pharmacological Data)
117 min
Reference
Lesur, Brigitte; Lin, Yin G.; Marcy, Val R.; Aimone, Lisa D.; Gruner, John; Bacon, Edward R.; Chatterjee, Sankar
Chemical Biology and Drug Design, 2013 , vol. 81, # 3 p. 429 - 432 Title/Abstract Full Text View citing articles Show Details
Effect (Pharmacological Data)
transporter binding
Species or Test-System (Pharmacological Data)
not explicitly stated by authors
Further Details (Pharmacological Data)
inhibitory concentration (IC); IC50 related to: dopamine transporter
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Type (Pharmacological Data)
IC50
Value of Type (Pharmacological Data)
3.7 μmol/l
Reference
Lesur, Brigitte; Lin, Yin G.; Marcy, Val R.; Aimone, Lisa D.; Gruner, John; Bacon, Edward R.; Chatterjee, Sankar
Chemical Biology and Drug Design, 2013 , vol. 81, # 3 p. 429 - 432 Title/Abstract Full Text View citing articles Show Details
Effect (Pharmacological Data)
transporter binding
Species or Test-System (Pharmacological Data)
not explicitly stated by authors
Results
molecular target: dopamine transporter; species of target: rat
Reference
Lesur, Brigitte; Lin, Yin G.; Marcy, Val R.; Aimone, Lisa D.; Gruner, John; Bacon, Edward R.; Chatterjee, Sankar
Chemical Biology and Drug Design, 2013 , vol. 81, # 3 p. 429 - 432 Title/Abstract Full Text View citing articles Show Details
Comment (Pharmacological Data)
physiological behaviour discussed
Reference
De Bruyn, Tom; Van Westen, Gerard J.P.; IJzerman, Adriaan P.; Stieger, Bruno; De Witte, Peter; Augustijns, Patrick F.; Annaert, Pieter P.
Molecular Pharmacology, 2013 , vol. 83, # 6 p. 1257 - 1267 Title/Abstract Full Text View citing articles Show Details
Effect (Pharmacological Data)
pharmacokinetics
Species or Test-System (Pharmacological Data)
rat
Route of Application
intraperitoneal
Concentration (Pharmacological Data)
100 mg/kg
Kind of Dosing (Pharmacological Data)
title compound administered for 4h
Further Details (Pharmacological Data)
wake promotion assay
Type (Pharmacological Data)
AUC
Value of Type (Pharmacological Data)
117 min
Reference
Dunn, Derek; Hostetler, Greg; Iqbal, Mohamed; Messina-Mclaughlin, Patricia; Reiboldt, Alyssa; Lin, Yin Guo; Gruner, John; Bacon, Edward R.; Ator, Mark A.; Chatterjee, Sankar
Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 6 p. 2315 - 2317 Title/Abstract Full Text View citing articles Show Details
Effect (Pharmacological Data)
enzyme activity; inhibition of
Species or Test-System (Pharmacological Data)
not explicitly stated by authors
Concentration (Pharmacological Data)
10 μmol/l
Further Details (Pharmacological Data)
inhibition rate related to: CYP 2D6
Type (Pharmacological Data)
inhibition rate
Value of Type (Pharmacological Data)
< 10 percent
Reference
Dunn, Derek; Hostetler, Greg; Iqbal, Mohamed; Messina-Mclaughlin, Patricia; Reiboldt, Alyssa; Lin, Yin Guo; Gruner, John; Bacon, Edward R.; Ator, Mark A.; Chatterjee, Sankar
Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 6 p. 2312 - 2314 Title/Abstract Full Text View citing articles Show Details
Effect (Pharmacological Data)
enzyme activity; inhibition of
Species or Test-System (Pharmacological Data)
not explicitly stated by authors
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Concentration (Pharmacological Data)
10 μmol/l
Further Details (Pharmacological Data)
inhibition rate related to: CYP 3A4
Type (Pharmacological Data)
inhibition rate
Value of Type (Pharmacological Data)
< 10 percent
Reference
Dunn, Derek; Hostetler, Greg; Iqbal, Mohamed; Messina-Mclaughlin, Patricia; Reiboldt, Alyssa; Lin, Yin Guo; Gruner, John; Bacon, Edward R.; Ator, Mark A.; Chatterjee, Sankar
Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 6 p. 2312 - 2314 Title/Abstract Full Text View citing articles Show Details
Effect (Pharmacological Data)
enzyme activity; inhibition of
Species or Test-System (Pharmacological Data)
not explicitly stated by authors
Further Details (Pharmacological Data)
IC50 related to: CYP 2C19
Type (Pharmacological Data)
IC50
Value of Type (Pharmacological Data)
11 μmol/l
Reference
Dunn, Derek; Hostetler, Greg; Iqbal, Mohamed; Messina-Mclaughlin, Patricia; Reiboldt, Alyssa; Lin, Yin Guo; Gruner, John; Bacon, Edward R.; Ator, Mark A.; Chatterjee, Sankar
Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 6 p. 2312 - 2314 Title/Abstract Full Text View citing articles Show Details
Effect (Pharmacological Data)
enzyme activity; inhibition of
Species or Test-System (Pharmacological Data)
not explicitly stated by authors
Results
molecular target: CYP 2C19
Reference
Dunn, Derek; Hostetler, Greg; Iqbal, Mohamed; Messina-Mclaughlin, Patricia; Reiboldt, Alyssa; Lin, Yin Guo; Gruner, John; Bacon, Edward R.; Ator, Mark A.; Chatterjee, Sankar
Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 6 p. 2312 - 2314 Title/Abstract Full Text View citing articles Show Details
Effect (Pharmacological Data)
pharmacokinetics
Species or Test-System (Pharmacological Data)
Sprague-Dawley rat
Sex
male
Route of Application
intraperitoneal
Concentration (Pharmacological Data)
100 mg/kg
Kind of Dosing (Pharmacological Data)
title comp. in 0.5percent methylcellulose/0.2percent tween-80 in distilled water
Further Details (Pharmacological Data)
rat wake promotion assay; PDP value observed 3h after dosing
Type (Pharmacological Data)
AUC
Value of Type (Pharmacological Data)
117 min
Reference
Dunn, Derek; Hostetler, Greg; Iqbal, Mohamed; Messina-Mclaughlin, Patricia; Reiboldt, Alyssa; Lin, Yin Guo; Gruner, John; Bacon, Edward R.; Ator, Mark A.; Chatterjee, Sankar
Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 6 p. 2312 - 2314 Title/Abstract Full Text View citing articles Show Details
Effect (Pharmacological Data)
pharmacokinetics
Species or Test-System (Pharmacological Data)
liver of human
Further Details
human liver S9 metabolism assay; PDP value observed at 2h; parent remaining related to: liver
(Pharmacological Data)
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Type (Pharmacological Data)
parent remaining
Value of Type (Pharmacological Data)
77 percent
Reference
Dunn, Derek; Hostetler, Greg; Iqbal, Mohamed; Messina-Mclaughlin, Patricia; Reiboldt, Alyssa; Lin, Yin Guo; Gruner, John; Bacon, Edward R.; Ator, Mark A.; Chatterjee, Sankar
Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 6 p. 2312 - 2314 Title/Abstract Full Text View citing articles Show Details
Effect (Pharmacological Data)
protein binding affinity
Species or Test-System (Pharmacological Data)
not explicitly stated by authors
Further Details (Pharmacological Data)
IC50 related to: rat dopamine transporter
Type (Pharmacological Data)
IC50
Value of Type (Pharmacological Data)
3.7 μmol/l
Reference
Dunn, Derek; Hostetler, Greg; Iqbal, Mohamed; Messina-Mclaughlin, Patricia; Reiboldt, Alyssa; Lin, Yin Guo; Gruner, John; Bacon, Edward R.; Ator, Mark A.; Chatterjee, Sankar
Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 6 p. 2312 - 2314 Title/Abstract Full Text View citing articles Show Details
Effect (Pharmacological Data)
protein binding affinity
Species or Test-System (Pharmacological Data)
not explicitly stated by authors
Results
molecular target: rat dopamine transporter
Reference
Dunn, Derek; Hostetler, Greg; Iqbal, Mohamed; Messina-Mclaughlin, Patricia; Reiboldt, Alyssa; Lin, Yin Guo; Gruner, John; Bacon, Edward R.; Ator, Mark A.; Chatterjee, Sankar
Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 6 p. 2312 - 2314 Title/Abstract Full Text View citing articles Show Details
Effect (Pharmacological Data)
protein uptake; inhibition of
Species or Test-System (Pharmacological Data)
not explicitly stated by authors
Further Details (Pharmacological Data)
IC50 related to: SERT
Type (Pharmacological Data)
IC50
Value of Type (Pharmacological Data)
> 300 μmol/l
Reference
Dunn, Derek; Hostetler, Greg; Iqbal, Mohamed; Messina-Mclaughlin, Patricia; Reiboldt, Alyssa; Lin, Yin Guo; Gruner, John; Bacon, Edward R.; Ator, Mark A.; Chatterjee, Sankar
Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 6 p. 2312 - 2314 Title/Abstract Full Text View citing articles Show Details
Effect (Pharmacological Data)
protein uptake; inhibition of
Species or Test-System (Pharmacological Data)
not explicitly stated by authors
Further Details (Pharmacological Data)
IC50 related to: rat dopamine transporter
Type (Pharmacological Data)
IC50
Value of Type (Pharmacological Data)
4.3 μmol/l
Reference
Dunn, Derek; Hostetler, Greg; Iqbal, Mohamed; Messina-Mclaughlin, Patricia; Reiboldt, Alyssa; Lin, Yin Guo; Gruner, John; Bacon, Edward R.; Ator, Mark A.; Chatterjee, Sankar
Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 6 p. 2312 - 2314 Title/Abstract Full Text View citing articles Show Details
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Effect (Pharmacological Data)
protein uptake; inhibition of
Species or Test-System (Pharmacological Data)
not explicitly stated by authors
Further Details (Pharmacological Data)
IC50 related to: rat norepinephrine transporter
Type (Pharmacological Data)
IC50
Value of Type (Pharmacological Data)
63.9 μmol/l
Reference
Dunn, Derek; Hostetler, Greg; Iqbal, Mohamed; Messina-Mclaughlin, Patricia; Reiboldt, Alyssa; Lin, Yin Guo; Gruner, John; Bacon, Edward R.; Ator, Mark A.; Chatterjee, Sankar
Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 6 p. 2312 - 2314 Title/Abstract Full Text View citing articles Show Details
Effect (Pharmacological Data)
protein uptake; inhibition of
Species or Test-System (Pharmacological Data)
not explicitly stated by authors
Results
molecular target: rat dopamine transporter
Reference
Dunn, Derek; Hostetler, Greg; Iqbal, Mohamed; Messina-Mclaughlin, Patricia; Reiboldt, Alyssa; Lin, Yin Guo; Gruner, John; Bacon, Edward R.; Ator, Mark A.; Chatterjee, Sankar
Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 6 p. 2312 - 2314 Title/Abstract Full Text View citing articles Show Details
Effect (Pharmacological Data)
protein uptake; inhibition of
Species or Test-System (Pharmacological Data)
not explicitly stated by authors
Results
molecular target: rat norepinephrine transporter
Reference
Dunn, Derek; Hostetler, Greg; Iqbal, Mohamed; Messina-Mclaughlin, Patricia; Reiboldt, Alyssa; Lin, Yin Guo; Gruner, John; Bacon, Edward R.; Ator, Mark A.; Chatterjee, Sankar
Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 6 p. 2312 - 2314 Title/Abstract Full Text View citing articles Show Details
Effect (Pharmacological Data)
enzyme activity; inhibition of
Species or Test-System (Pharmacological Data)
not explicitly stated by authors
Further Details (Pharmacological Data)
IC50 related to: CYP2C19
Type (Pharmacological Data)
IC50
Value of Type (Pharmacological Data)
11 μmol/l
Reference
Dunn, Derek; Hostetler, Greg; Iqbal, Mohamed; Marcy, Val R.; Lin, Yin Guo; Jones, Bruce; Aimone, Lisa D.; Gruner, John; Ator, Mark A.; Bacon, Edward R.; Chatterjee, Sankar
Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 11 p. 3751 - 3753 Title/Abstract Full Text View citing articles Show Details
Effect (Pharmacological Data)
enzyme activity; inhibition of
Species or Test-System (Pharmacological Data)
not explicitly stated by authors
Results
molecular target: CYP2C19
Reference
Dunn, Derek; Hostetler, Greg; Iqbal, Mohamed; Marcy, Val R.; Lin, Yin Guo; Jones, Bruce; Aimone, Lisa D.; Gruner, John; Ator, Mark A.; Bacon, Edward R.; Chatterjee, Sankar
Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 11 p. 3751 - 3753 Title/Abstract Full Text View citing articles Show Details
Effect (Pharmacological Data)
pharmacokinetics
Species or Test-System (Pharmacological Data)
rat
Route of Application
intraperitoneal
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60 of 150
61 of 150
62 of 150
Concentration (Pharmacological Data)
100 mg/kg
Further Details (Pharmacological Data)
wake-promoting activity over 3 h was measured; wake promotion assay
Type (Pharmacological Data)
AUC
Value of Type (Pharmacological Data)
117 min
Reference
Dunn, Derek; Hostetler, Greg; Iqbal, Mohamed; Marcy, Val R.; Lin, Yin Guo; Jones, Bruce; Aimone, Lisa D.; Gruner, John; Ator, Mark A.; Bacon, Edward R.; Chatterjee, Sankar
Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 11 p. 3751 - 3753 Title/Abstract Full Text View citing articles Show Details
Effect (Pharmacological Data)
protein binding affinity
Species or Test-System (Pharmacological Data)
striata of rat
Further Details (Pharmacological Data)
DAT binding assay; DAT: dopamine transporter
Results
molecular target: dopamine transporter
Reference
Dunn, Derek; Hostetler, Greg; Iqbal, Mohamed; Marcy, Val R.; Lin, Yin Guo; Jones, Bruce; Aimone, Lisa D.; Gruner, John; Ator, Mark A.; Bacon, Edward R.; Chatterjee, Sankar
Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 11 p. 3751 - 3753 Title/Abstract Full Text View citing articles Show Details
Effect (Pharmacological Data)
protein binding affinity
Species or Test-System (Pharmacological Data)
striata of rat
Further Details (Pharmacological Data)
DAT binding assay; DAT: dopamine transporter; IC50 related to: dopamine transporter
Type (Pharmacological Data)
IC50
Value of Type (Pharmacological Data)
3.7 μmol/l
Reference
Dunn, Derek; Hostetler, Greg; Iqbal, Mohamed; Marcy, Val R.; Lin, Yin Guo; Jones, Bruce; Aimone, Lisa D.; Gruner, John; Ator, Mark A.; Bacon, Edward R.; Chatterjee, Sankar
Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 11 p. 3751 - 3753 Title/Abstract Full Text View citing articles Show Details
Effect (Pharmacological Data)
wake-promoting
Species or Test-System (Pharmacological Data)
rat
Route of Application
intraperitoneal
Concentration (Pharmacological Data)
100 mg/kg
Further Details (Pharmacological Data)
for control total awake time over 3 h was 65 min
Type (Pharmacological Data)
total awake time over 3 h (AUC)
Value of Type (Pharmacological Data)
117 min
Reference
Louvet, Philippe; Schweizer, Dominique; Gourdel, Marie-Edith; Riguet, Eric; Yue, Christoph; Marcy, Val R.; Lin, Yin Guo; Gruner, John; Lesur, Brigitte; Bacon, Edward R.; Chatterjee, Sankar
European Journal of Medicinal Chemistry, 2012 , vol. 54, p. 949 - 951 Title/Abstract Full Text View citing articles Show Details
Effect (Pharmacological Data)
wake-promoting
Species or Test-System (Pharmacological Data)
rat
Route of Application
intraperitoneal
Concentration
100 mg/kg
(Pharmacological Data)
63 of 150
64 of 150
65 of 150
66 of 150
67 of 150
Further Details (Pharmacological Data)
for control total awake time over 3 h was 79.2 min
Type (Pharmacological Data)
total awake time over 3 h (AUC)
Value of Type (Pharmacological Data)
117 min
Reference
Louvet, Philippe; Schweizer, Dominique; Gourdel, Marie-Edith; Riguet, Eric; Yue, Christoph; Marcy, Val R.; Lin, Yin Guo; Gruner, John; Lesur, Brigitte; Bacon, Edward R.; Chatterjee, Sankar
European Journal of Medicinal Chemistry, 2012 , vol. 54, p. 949 - 951 Title/Abstract Full Text View citing articles Show Details
Effect (Pharmacological Data)
monoamine transporter binding affinity
Species or Test-System (Pharmacological Data)
brain membranes of rat
Further Details (Pharmacological Data)
Ki related to: dopamine transporter
Type (Pharmacological Data)
Ki
Value of Type (Pharmacological Data)
2520 nmol/l
Reference
Cao, Jianjing; Prisinzano, Thomas E.; Okunola, Oluyomi M.; Kopajtic, Theresa; Shook, Matthew; Katz, Jonathan L.; Newman, Amy Hauck
ACS Medicinal Chemistry Letters, 2011 , vol. 2, # 1 p. 48 - 52 Title/Abstract Full Text View citing articles Show Details
Effect (Pharmacological Data)
monoamine transporter binding affinity
Species or Test-System (Pharmacological Data)
brain membranes of rat
Results
molecular target: dopamine transporter
Reference
Cao, Jianjing; Prisinzano, Thomas E.; Okunola, Oluyomi M.; Kopajtic, Theresa; Shook, Matthew; Katz, Jonathan L.; Newman, Amy Hauck
ACS Medicinal Chemistry Letters, 2011 , vol. 2, # 1 p. 48 - 52 Title/Abstract Full Text View citing articles Show Details
Effect (Pharmacological Data)
locomotor activity; effect on
Species or Test-System (Pharmacological Data)
mouse
Concentration (Pharmacological Data)
100 - 560 mg/kg
Type (Pharmacological Data)
maximal locomotor activity
Value of Type (Pharmacological Data)
500 counts/min
Reference
Cao, Jianjing; Prisinzano, Thomas E.; Okunola, Oluyomi M.; Kopajtic, Theresa; Shook, Matthew; Katz, Jonathan L.; Newman, Amy Hauck
ACS Medicinal Chemistry Letters, 2011 , vol. 2, # 1 p. 48 - 52 Title/Abstract Full Text View citing articles Show Details
Effect (Pharmacological Data)
locomotor activity; effect on
Species or Test-System (Pharmacological Data)
mouse
Concentration (Pharmacological Data)
100 - 560 mg/kg
Type (Pharmacological Data)
dose for maximal activity
Value of Type (Pharmacological Data)
300 mg/kg
Reference
Cao, Jianjing; Prisinzano, Thomas E.; Okunola, Oluyomi M.; Kopajtic, Theresa; Shook, Matthew; Katz, Jonathan L.; Newman, Amy Hauck
ACS Medicinal Chemistry Letters, 2011 , vol. 2, # 1 p. 48 - 52 Title/Abstract Full Text View citing articles Show Details
Effect (Pharmacological
locomotor activity; effect on
Data)
68 of 150
69 of 150
70 of 150
Species or Test-System (Pharmacological Data)
mouse
Concentration (Pharmacological Data)
100 - 560 mg/kg
Type (Pharmacological Data)
time for maximal activity
Value of Type (Pharmacological Data)
1 h
Reference
Cao, Jianjing; Prisinzano, Thomas E.; Okunola, Oluyomi M.; Kopajtic, Theresa; Shook, Matthew; Katz, Jonathan L.; Newman, Amy Hauck
ACS Medicinal Chemistry Letters, 2011 , vol. 2, # 1 p. 48 - 52 Title/Abstract Full Text View citing articles Show Details
Effect (Pharmacological Data)
transporter; inhibition of
Species or Test-System (Pharmacological Data)
HEK293-Flp-In cells; genetically modified/infected with: human OCT2
Concentration (Pharmacological Data)
20 μmol/l
Kind of Dosing (Pharmacological Data)
title comp. dissolved in DMSO
Further Details (Pharmacological Data)
OCT2: organic cation transporter 2 (solute carrier 22A2); HEK: human embryonic kidney; fluorescent probe substrate: 4-(4-(dimethylamino)styryl)-N-methyl-pyridinium (ASP+) (5 μmol/l); high-throughput assay; fluorimetry; inhibition rate related to: OCT2
Type (Pharmacological Data)
inhibition rate
Value of Type (Pharmacological Data)
18.3 percent
Location
supporting information
Reference
Kido, Yasuto; Matsson, Paer; Giacomini, Kathleen M.
Journal of Medicinal Chemistry, 2011 , vol. 54, # 13 p. 4548 - 4558 Title/Abstract Full Text View citing articles Show Details
Effect (Pharmacological Data)
transporter; inhibition of
Species or Test-System (Pharmacological Data)
HEK293-Flp-In cells; genetically modified/infected with: human OCT2
Concentration (Pharmacological Data)
20 μmol/l
Kind of Dosing (Pharmacological Data)
title comp. dissolved in DMSO
Further Details (Pharmacological Data)
OCT2: organic cation transporter 2 (solute carrier 22A2); HEK: human embryonic kidney; fluorescent probe substrate: 4-(4-(dimethylamino)styryl)-N-methyl-pyridinium (ASP+) (5 μmol/l); high-throughput assay; fluorimetry
Results
molecular target: human OCT2
Location
supporting information
Reference
Kido, Yasuto; Matsson, Paer; Giacomini, Kathleen M.
Journal of Medicinal Chemistry, 2011 , vol. 54, # 13 p. 4548 - 4558 Title/Abstract Full Text View citing articles Show Details
Effect (Pharmacological Data)
cocaine substitution
Species or Test-System (Pharmacological Data)
Sprague-Dawley rat
Sex
male
Route of Application
intraperitoneal
Concentration (Pharmacological Data)
<= 300 mg/kg
Kind of Dosing (Pharmacological Data)
title comp. dissolved in 5percent arabic gum solution; admin. as salt
Further Details (Pharmacological Data)
title comp. engenders cocaine-appropriate responding with 90.2percent substitution at 300 mg/kg; effective dose (ED)
Type (Pharmacological Data)
ED50
71 of 150
72 of 150
73 of 150
Value of Type (Pharmacological Data)
95.96 mg/kg
Reference
Paterson, Neil E.; Fedolak, Allison; Olivier, Berend; Hanania, Taleen; Ghavami, Afshin; Caldarone, Barbara
Pharmacology Biochemistry and Behavior, 2010 , vol. 95, # 4 p. 449 - 456 Title/Abstract Full Text View citing articles Show Details
Effect (Pharmacological Data)
enzyme activity; inhibition of
Species or Test-System (Pharmacological Data)
fatty acid amide hydrolase of human
Concentration (Pharmacological Data)
1 μmol/l
Type (Pharmacological Data)
percent inhibition
Value of Type (Pharmacological Data)
-1.68 percent
Location
supporting information
Reference
Vincent, Fabien; Nguyen, Margaret T.; Emerling, Daniel E.; Kelly, Michael G.; Duncton, Matthew A.J.
Bioorganic and Medicinal Chemistry Letters, 2009 , vol. 19, # 23 p. 6793 - 6796 Title/Abstract Full Text View citing articles Show Details
Effect (Pharmacological Data)
enzyme activity; inhibition of
Species or Test-System (Pharmacological Data)
fatty acid amide hydrolase of human
Concentration (Pharmacological Data)
1 μmol/l
Results
molecular target: fatty acid amide hydrolase
Location
supporting information
Reference
Vincent, Fabien; Nguyen, Margaret T.; Emerling, Daniel E.; Kelly, Michael G.; Duncton, Matthew A.J.
Bioorganic and Medicinal Chemistry Letters, 2009 , vol. 19, # 23 p. 6793 - 6796 Title/Abstract Full Text View citing articles Show Details
Effect (Pharmacological Data)
delayed ejaculation; effect on
Species or Test-System (Pharmacological Data)
human
Route of Application
peroral
Method (Pharmacological Data)
Example 1. Delayed ejaculation with sublingually administered d-modafinil.The synthesis of (d)-(+)-modafinil has been described in the literature (see, e.g., Prisinzano et al., Tetrahedron Asymmetry, 15: 1053-1058 (2004); US Patent No. 4,927,855 ("Lafon synthesis"))- In accordance with the Lafon synthesis, the intermediate carboxylic acid was converted to the diastereomic salt mixture with (+) alpha-methylbenzylamine. The diastereomers were separated, and the appropriate chiral acid liberated from the salt form. The acid was converted to the methyl ester via esterification and reacted with ammonia/methanol solution to yield d-modafinil. The enantiomeric purity was in excess of 98percent-99percent.Initial formulation tests of modafinil (racemate) and pure d-modafinil revealed a bitter taste. Therefore, the pharmaceutical formulation included one or more taste-masking ingredients. The d-modafinil was mixed with various taste-masking agents, including pulverized mints, breath fresheners, and natural and artificial flavorings. The synthesized d-modafinil was compounded into a composition containing sugar, spearmint flavor, cinnamon flavor, gum arabic, gelatin, corn syrup, and dyes that could be administered sublingually. Formulations containing 100 mg of d-modafinil were prepared. Subject 1 took the above-described formulation of d-modafinil sublingually at 9:00 pm in the course of testing a composition containing d-modafinil for a different effect unrelated to sexual activity. Subject 1 reported that unexpectedly the time to ejaculate during sexual activity was significantly longer than usual by a factor of about two to three times. A week later, Subject 1 took the formulation sublingually for a second time and, again, reported that the time to ejaculate during sexual intercourse was significantly delayed by a factor of approximately two to three times.The data demonstrate that sublingual administration of d-modafinil can provide a desirable delay of ejaculation during sexual activity, that the effect is drug-dependent, and that the effect is reversible.
Results
delay in ejaculation during sexual activity was experienced by patients treated with 200 mg of the title compound
Location
Page/Page column 19-20
Reference
NEUROHEALING PHARMACEUTICALS, INC.
Patent: WO2008/21341 A2, 2008 ; Title/Abstract Full Text Show Details
74 of 150
Effect (Pharmacological Data)
transmitter releasing
Species or Test-System (Pharmacological Data)
Wistar rat
Sex
male
Route of Application
intraperitoneal
Concentration
75 - 150 mg/kg
(Pharmacological Data)
75 of 150
76 of 150
77 of 150
Kind of Dosing (Pharmacological Data)
suspended in 0.3percent carboxymethylcellulose (CMC) in saline
Method (Pharmacological Data)
hypothalamic histamine release in freely moving rats examined using in vivo microdialysis; dialysate samples collected every 20 min for 3 h after title comp. injection and assayed for histamine by high performance chromatography-fluometric method
Further Details (Pharmacological Data)
control: 0.3percent CMC; reference comp.: methylphenidate (3 mg/kg, i.p.)
Results
title comp. increased histamine release immediately after administration with gradual reduction within 1 h and 2 h at low and high doses, respectively; methylphenidate had no effect; fig.
Reference
Ishizuka, Tomoko; Murakami, Masahiro; Yamatodani, Atsushi
European Journal of Pharmacology, 2008 , vol. 578, # 2-3 p. 209 - 215 Title/Abstract Full Text View citing articles Show Details
Effect (Pharmacological Data)
behavioural symptoms
Species or Test-System (Pharmacological Data)
Wistar rat
Sex
male
Route of Application
intraperitoneal
Concentration (Pharmacological Data)
75 - 150 mg/kg
Kind of Dosing (Pharmacological Data)
suspended in 0.3percent carboxymethylcellulose (CMC) in saline
Method (Pharmacological Data)
locomotor activity counts automatically recorded in 20-min bins by infrared sensor for 3 h after title comp. administration
Further Details (Pharmacological Data)
control: 0.3percent CMC; reference comp.: methylphenidate (3 mg/kg, i.p.)
Results
title comp. increased locomotor activity immediately after administration to 300percent and 600percent at low and high doses, respectively; at high dose effect was similar to methylphenidate; fig.
Reference
Ishizuka, Tomoko; Murakami, Masahiro; Yamatodani, Atsushi
European Journal of Pharmacology, 2008 , vol. 578, # 2-3 p. 209 - 215 Title/Abstract Full Text View citing articles Show Details
Effect (Pharmacological Data)
behavioural symptoms
Species or Test-System (Pharmacological Data)
C57BL mouse
Sex
male
Route of Application
intraperitoneal
Concentration (Pharmacological Data)
150 mg/kg
Kind of Dosing (Pharmacological Data)
suspended in 0.3percent carboxymethylcellulose (CMC) in saline
Method (Pharmacological Data)
locomotor activity counts automatically recorded every 20 min by infrared sensor until 4 h after title comp. administration; testing carried out during the light phase
Further Details (Pharmacological Data)
further investigation on mechanism of action using depletion of neuronal histamine through pretreatment with α-fluoromethylhistidine; control: 0.3percent CMC; reference comp.: methylphenidate (20 mg/kg, i.p.)
Results
title comp. increased locomotor activity similarly to methylphenidate; mechanism of action of title comp. (but not methylphenidate) involved activation of central histaminergic system; fig.
Reference
Ishizuka, Tomoko; Murakami, Masahiro; Yamatodani, Atsushi
European Journal of Pharmacology, 2008 , vol. 578, # 2-3 p. 209 - 215 Title/Abstract Full Text View citing articles Show Details
Effect (Pharmacological Data)
behavioural symptoms
Species or Test-System (Pharmacological Data)
C57BL mouse
Sex
male
Route of Application
intraperitoneal
Concentration (Pharmacological Data)
150 mg/kg
Kind of Dosing
suspended in 0.3percent carboxymethylcellulose (CMC) in saline
(Pharmacological Data)
78 of 150
Method (Pharmacological Data)
cumulative counts of locomotor activity automatically recorded by infrared sensor during 2 h after title comp. administration at 00:00 the active period of mice (dark phase) or at the light phase
Further Details (Pharmacological Data)
control: 0.3percent CMC; reference comp.: methylphenidate (20 mg/kg, i.p.)
Results
title comp. increased locomotor activity similarly to methylphenidate after administration at the light phase; after treatment at dark phase title comp. was less potent than methylphenidate; fig.
Reference
Ishizuka, Tomoko; Murakami, Masahiro; Yamatodani, Atsushi
European Journal of Pharmacology, 2008 , vol. 578, # 2-3 p. 209 - 215 Title/Abstract Full Text View citing articles Show Details
Effect (Pharmacological Data)
sleep movement disorders; effect on
Species or Test-System (Pharmacological Data)
non-obese with periodic limb movement disorder (PLMD), restless leg syndrome (RLS) without apnea and primary snoring of human
Sex
female
Route of Application
peroral
Method (Pharmacological Data)
Example 2. Subject Administered 50 mg of ModafinilA 53 year old non-obese female, 61 kg, with sleep study diagnosed PLMD with RLS without apnea, and Primary snoring, took modafinil 50 mg by mouth between 8 am and noon. No urge to move legs in the evenings occurred and no leg jerks during sleep were observed by her partner. The patient noted increased restfulness and her partner noticed an absence of .imb movements and snoring while asleep. Example 3. Subject Administered 100 mg of ModafinilA 53 year old non-obese female, 61 kg, with sleep study diagnosed PLMD with RLS without apnea and Primary snoring, took modafinil 100 mg by mouth in the morning. No urge to move legs in the evenings occurred and no leg jerks during sleep were observed by her partner. The patient noted increased restfulness and her partner noticed an absence of limb movements and snoring while asleep.Example 4. Continuous use evening dosageA 54 year old non-obese female, 61 kg, with sleep study diagnosedPLMD with RLS without apnea and Primary snoring, took modafinil 50 mg by mouth 1-3 hours prior to bedtime. Limb movements and the urge to move the limb and associated sensations while awake were greatly reduced after approximately 90 minutes. The patient then took 25 mg of modafiniS as needed and noted that symptoms were either completely relieved or greatly diminished. Chronic use every day for periods of 5 to 7 days produced periods free from RLS and PLMD symptoms, which returned immediately after stopping the drug.
Results
title compound treatment at 50 and 100 mg between 8 am and noon and in the morning, respectively, showed no urge to move legs in the evenings occurred and no leg jerks during sleep were observed by her partner; increased restfulness was noted by the patient and her partner noticed an absence of limb movements and snoring while asleep; treatment with 50 mg title compound 1-3 hours prior to bedtime showed great reduction of limb movement, the urge to move the limb and associated (comment)
Location
Page/Page column 8-9
Reference
LAVIN, Thomas, N.
Patent: WO2008/77127 A2, 2008 ; Title/Abstract Full Text Show Details
79 of 150
Effect (Pharmacological Data)
sleep movement disorders; effect on
Species or Test-System (Pharmacological Data)
non-obese with periodic limb movement disorder (PLMD), restless leg syndrome (RLS) with apnea and primary snoring of human
Sex
female
Route of Application
peroral
Method (Pharmacological Data)
Example 5. Continuous use morning dosage A 53 year old non-obese female, 61 kg, with sleep study diagnosedPLMD with RLS with apnea and Primary snoring, took modafinil 50 mg or 25 mg by mouth in the morning. Limb movements and the urge to move the limb and associated sensations while awake were greatly reduced. The lower dosage of 25 mg failed to entirely remove symptoms. Either 50 mg or 25 mg was used intermittently for a period of 14 months. Chronic use every day for periods of up to 11 days produced periods free from RLS and PLMD symptoms, which returned immediately after stopping the drug. The sleep partner noted a marked decrease in snoring.
Results
title compound treatment at 50 mg and 25 mg in the morning showed great reduction in limb movements, the urge to move the limb and associated sensations while awake; lower dosage of 25 mg title compound failed to entirely remove symptoms; chronic use every day for periods up to 11 days produced periods free from RLS and PLMD symptoms, which returned immediately after stopping the drug; decrease in snoring was observed by the sleeping partner
Location
Page/Page column 9
Reference
LAVIN, Thomas, N.
Patent: WO2008/77127 A2, 2008 ; Title/Abstract Full Text Show Details
80 of 150
Effect (Pharmacological Data)
sleep movement disorders; effect on
Species or Test-System (Pharmacological Data)
non-obese with restless leg syndrome (RLS), periodic limb movement in sleep (PLMS) and primary snoring of human
Sex
female
Route of Application
peroral
Method (Pharmacological Data)
Example 6. Sleep Study Results, evening dosageA non-obese female subject with no outstanding medical history other than restless leg syndrome and PLMS of 6 years duration, and Primary snoring, age 54, 60 kg, was entered into an overnight sleep study in a specialist hospital sleep disorder center. Subject was monitored by polysomnography recording method identifying sleep stages and their durations, detection and measurements of apneas, detection and measurement of PLM (periodic limb movements, snoring and measurement of pψ2, heart rate and arterial pressure. Sleep stages were identified using electroencephalograph^ and electromyographic recording. Oxygen saturation was measured by transcutaneous oximetric measurement and revealed no apnea. Baseline studies without drug administration showed that
the subject exhibited multiple PLMs during sleep and significant snoring episodes. After oral administration of 50 mg modafinil in the evening PLMs were not detected during sleep as illustrated in Drawing 1. Snoring as represented by the Snore Index was reduced 70percent Results
title compound tretament at 50 mg reduced snoring by 70percent as represented by the snore index score, however, periodic limb movements (PLMs) were not detected; figure is given
Location
Page/Page column title page; 4; 9; 1/1
Reference
LAVIN, Thomas, N.
Patent: WO2008/77127 A2, 2008 ; Title/Abstract Full Text Show Details
81 of 150
Effect (Pharmacological Data)
H-reflex frequency dependent depression; restoration of
Species or Test-System (Pharmacological Data)
Sprague-Dawley rat
Sex
female
Route of Application
peroral
Method (Pharmacological Data)
Section 3Modafinil Restored Frequency Dependent Depression of the H-Reflex in Spinally Transected RatsMethods:Rats were spinally transected as in Section 1 of this Example. One group of rats received no exercise after transection. A second group of rats was treated with passive exercise using the motorized bicycle exercise trainer, as in Section 1. Passive exercise was begun within 7 days of transection. A third group of transected rats were not exercised but were given 3 mg/Kg modafinil per day. A 100 mg modafinil pill was ground by mortar and pestle and mixed with 9 ml of syrup and 1 ml of water. The dose to the animal was 0.1 ml p.o. daily (3 mg/Kg/day). Modafinil was started between 48 hours and 7 days after transection. A fourth group of rats was untransected normal controls. Each group contained 9 to 12 rats.At 30 days after transection, the H-reflex of each rat was measured as in Section 1.Results:The H-reflex of the four groups of rats was measured at 30 days after transection at stimulation frequencies from 0.2 to 10 Hz. The four groups of rats were normal controls (control), transected and untreated for 30 days after transection (Tx-30), transected and treated solely with 3 mg/Kg/day modafinil p.o. for 30 days (Mod), and transected and treated solely with passive exercise for 30 days (MBET 30). The results are shown in FIG. D1.FIG. 6 shows that as you increase the stimulation for 0.2 to 10 Hz, the H-reflex amplitude in intact rats (control) decreases markedly. In rats that were transected and tested 30 days after surgery (Tx-30), the amplitude of the reflex did not habituate-that is, there was hyper-reflexia. In rats that were transected and MBET begun within 7 days after surgery and exercised for 30 days (MBET 30), the reflex amplitude decreased as in intact animals, indicating that passive exercise led to a normalization of the hyper-reflexia. In animals that were transected and not exercised but given daily doses of modafinil beginning 7 days after surgery (Mod), the reflexes were normalized, indicating that modafinil also alleviated hyper-reflexia.Hyper-reflexia is a component of spasticity, so that normalization of hyper-reflexia indicates a reduction or elimination of spasticity. These studies demonstrated that oral administration of modafinil, which is used to promote waking in narcoleptic subjects, was effective in reducing hyper-reflexia after spinal transection
Results
title compound administration at 3 mg/kg/day normalized the reflexes of the transected mouse; figure is given
Location
Page/Page column 2; 6-7; Sheet 6
Reference
The Board of Trustees of the University of Arkansas
Patent: US2008/221216 A1, 2008 ; Title/Abstract Full Text Show Details
82 of 150
Effect (Pharmacological Data)
neuronal differentiation; stimulation of
Species or Test-System (Pharmacological Data)
neural stem cells (hNSCs) of human
Method (Pharmacological Data)
FIG. 9 is a dose-response curve showing effect of the neurogenic agents MKC-231 and modafinil (adrenergic agonist) in combination on neuronal differentiation of human neural stem cells compared to the effect of either agent alone. When run independently, each compound was tested in a concentration response curve ranging from 0.01 μM to 31.6 μM. In combination, the compounds were combined at equal concentrations at each point (for example, the first point in the combined curve consisted of a test of 0.01 μM MKC-231 and 0.01 μM modafinil). Data is presented as the percentage of the neuronal positive control, with basal media values subtracted. When used alone, EC50 was observed at an MKC-231 concentration of 8.6 μM or a modafinil concentration estimated to be 83 μM (based on extrapolation of the observed data). When used in combination, neurogenesis is greatly enhanced: EC50 was observed at a combination of MKC-231 and modafinil at concentrations of 1.1 μM each, resulting in a synergistic combination index of 0.14.; Example 8Effects of Modafinil in Combination with the MKC-231 on Differentiation of Human Neural Stem CellsHuman neural stem cells (hNSCs) were isolated and grown in monolayer culture, plated, treated with varying concentrations of MKC-231 in the presence or absence of modafinil, and stained with TUJ-1 antibody for the detection of neuronal differentiation as described in above. Mitogen-free test media with a positive control for neuronal differentiation was used along with basal media without growth factors as a negative control.Results are shown in FIG. 9, which shows concentration response curves of neuronal differentiation after background media values are subtracted. The concentration response curves of the combination of MKC-231 with modafinil are shown with the concentration response curves either agent alone. The data is presented as a percent of neuronal positive control. The data indicate that the combination of MKC-231 with modafinil resulted in synergistically enhanced neuronal differentiation relative to that that produced by either agent alone.
Type (Pharmacological Data)
EC50
Value of Type (Pharmacological Data)
83 μmol/l
Results
title compound dose-dependently increases neuronal differentiation at concentration from 0.01 to 31.6 μM; figure is given
Location
Page/Page column 3; 40-41; sheet 9
Reference
BrainCells, Inc.
Patent: US2008/64671 A1, 2008 ; Title/Abstract Full Text Show Details
83 of 150
Effect (Pharmacological Data)
neuroregulatoric
Species or Test-System (Pharmacological Data)
129Sv mouse
84 of 150
85 of 150
86 of 150
Route of Application
intraperitoneal
Concentration (Pharmacological Data)
32 mg/kg
Kind of Dosing (Pharmacological Data)
title comp. dissolved in 20percent dimethylsulfoxide
Method (Pharmacological Data)
title comp. administered; polygraphic records performed within 14 h and scored by 30-s epochs for W, SWS and PS; W, SWS and PS amount as well as latencies to SWS and PS determined
Further Details (Pharmacological Data)
further investigation using HDC knockout mice; W: wakefulness; SWS: slow wave sleep; PS: paradoxical sleep; HDC: histidine decarboxylase
Results
title comp. increased W and decreased SWS and PS; this effect did not depend on HDC
Reference
Parmentier; Anaclet; Guhennec; Brousseau; Bricout; Giboulot; Bozyczko-Coyne; Spiegel; Ohtsu; Williams; Lin
Biochemical Pharmacology, 2007 , vol. 73, # 8 p. 1157 - 1171 Title/Abstract Full Text View citing articles Show Details
Effect (Pharmacological Data)
neuroregulatoric
Species or Test-System (Pharmacological Data)
129Sv mouse
Route of Application
intraperitoneal
Concentration (Pharmacological Data)
32 mg/kg
Kind of Dosing (Pharmacological Data)
title comp. dissolved in 20percent dimethylsulfoxide
Method (Pharmacological Data)
title comp. administered; polygraphic records performed within 14 h and EEG power spectra recorded
Further Details (Pharmacological Data)
further investigation using HDC knockout mice; EEG: electroencephalogram; HDC: histidine decarboxylase
Results
title comp. suppressed cortical slow activity (δ and slow ψ); this effect did not depend on HDC
Reference
Parmentier; Anaclet; Guhennec; Brousseau; Bricout; Giboulot; Bozyczko-Coyne; Spiegel; Ohtsu; Williams; Lin
Biochemical Pharmacology, 2007 , vol. 73, # 8 p. 1157 - 1171 Title/Abstract Full Text View citing articles Show Details
Effect (Pharmacological Data)
behavioural symptoms
Species or Test-System (Pharmacological Data)
Sprague-Dawley rat
Sex
male
Route of Application
peroral
Concentration (Pharmacological Data)
32 - 128 mg/kg
Kind of Dosing (Pharmacological Data)
title comp. (Provigil, Alertec and Vigiler) dissolved in water containing 0.1percent DMSO and adminisered via gavage at a volume of 1 ml/kg
Method (Pharmacological Data)
rats trained to discriminate cocaine/amphetamine from saline injection for delivery of food pellet; admin. with title comp.; response rates determined after 10-240 min delay
Further Details (Pharmacological Data)
control: vehicle
Results
title comp. at 64 and 128 mg/kg induced higher response rates than at 32 mg/kg; title comp. partially substituted for cocaine/amphetamine discriminative stimulus with substitution being time-dependent and most pronounced at 60-120 min; diagrams
Reference
Dopheide, Marsha M.; Morgan, Russell E.; Rodvelt, Kelli R.; Schachtman, Todd R.; Miller, Dennis K.
European Journal of Pharmacology, 2007 , vol. 568, # 1-3 p. 112 - 123 Title/Abstract Full Text View citing articles Show Details
Effect (Pharmacological Data)
behavioural symptoms
Species or Test-System (Pharmacological Data)
Sprague-Dawley rat
Sex
male
Route of Application
peroral
Concentration (Pharmacological Data)
32 mg/kg
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Kind of Dosing (Pharmacological Data)
title comp. (Provigil, Alertec and Vigiler) dissolved in water vehicle containing 0.1percent DMSO and adminisered via gavage at a volume of 1 ml solution/kg
Method (Pharmacological Data)
rats trained to discriminate cocaine/amphetamine from saline injection for delivery of food pellet; administered with title comp.; 50 min later, cocaine/amphetamine administered; response rates determined after 10 min delay
Further Details (Pharmacological Data)
control: vehicle
Results
title comp. augmented the discriminative stimulus of cocaine and amphetamine; diagram
Reference
Dopheide, Marsha M.; Morgan, Russell E.; Rodvelt, Kelli R.; Schachtman, Todd R.; Miller, Dennis K.
European Journal of Pharmacology, 2007 , vol. 568, # 1-3 p. 112 - 123 Title/Abstract Full Text View citing articles Show Details
Effect (Pharmacological Data)
transmitter releasing
Species or Test-System (Pharmacological Data)
striatal slices of Sprague-Dawley rat
Sex
male
Concentration (Pharmacological Data)
0.01 - 300 μmol/l
Kind of Dosing (Pharmacological Data)
title comp. (Provigil, Alertec and Vigiler) used
Method (Pharmacological Data)
test system preloaded with <3H>dopamine; superfused with buffer containing title comp. for 6 min followed by buffer without title comp. for 20 min; filtered; radioactivity determined by liquid scintillation spectroscopy
Further Details (Pharmacological Data)
control: without title comp.; reference compounds: amphetamine, nicotine; further study: effect of nomifensine, mecamylamine on activity of title comp.
Results
title comp. at 100 and 300 μM increased the <3H>overflow in a concentration-dependent manner compared to control; at 0.01-30 μM, no effect was observed; title comp. effect attenuated by nomifensine but not by mecamylamine; diagrams, table
Reference
Dopheide, Marsha M.; Morgan, Russell E.; Rodvelt, Kelli R.; Schachtman, Todd R.; Miller, Dennis K.
European Journal of Pharmacology, 2007 , vol. 568, # 1-3 p. 112 - 123 Title/Abstract Full Text View citing articles Show Details
Effect (Pharmacological Data)
transmitter releasing
Species or Test-System (Pharmacological Data)
striatal slices of Sprague-Dawley rat
Sex
male
Concentration (Pharmacological Data)
0.01 - 30 μmol/l
Kind of Dosing (Pharmacological Data)
title comp. (Provigil, Alertec and Vigiler) used
Method (Pharmacological Data)
test system preloaded with <3H>dopamine; superfused with buffer containing title comp. for 10 min followed by amphetamine (1/3 μmol/l) for 6 min; filtered; radioactivity determined by liquid scintillation spectroscopy
Further Details (Pharmacological Data)
control: without title comp.
Results
title comp. signif. diminished <3H>overflow evoked by 1 μmol/l amphetamine but only 30 μmol/l diminished <3H>overflow evoked by 3 μmol/l amphetamine; diagram
Reference
Dopheide, Marsha M.; Morgan, Russell E.; Rodvelt, Kelli R.; Schachtman, Todd R.; Miller, Dennis K.
European Journal of Pharmacology, 2007 , vol. 568, # 1-3 p. 112 - 123 Title/Abstract Full Text View citing articles Show Details
Effect (Pharmacological Data)
transmitter releasing
Species or Test-System (Pharmacological Data)
striatal slices of Sprague-Dawley rat
Sex
male
Concentration (Pharmacological Data)
0.01 - 30 μmol/l
Kind of Dosing (Pharmacological Data)
title comp. (Provigil, Alertec and Vigiler) used
Method (Pharmacological Data)
test system preloaded with <3H>dopamine; superfused with buffer containing title comp. for 10 min followed by nicotine for 6 min; filtered; radioactivity determined by liquid scintillation spectroscopy
Further Details (Pharmacological Data)
control: without title comp.
Comment
No effect
(Pharmacological Data)
90 of 150
Reference
Dopheide, Marsha M.; Morgan, Russell E.; Rodvelt, Kelli R.; Schachtman, Todd R.; Miller, Dennis K.
European Journal of Pharmacology, 2007 , vol. 568, # 1-3 p. 112 - 123 Title/Abstract Full Text View citing articles Show Details
Effect (Pharmacological Data)
wakefulness; effect on
Species or Test-System (Pharmacological Data)
human
Route of Application
sublingual
Method (Pharmacological Data)
Double blind study of sub-lingual d-modafinil composition in a normal human volunteer.The goal of this test was to confirm the suitability of the sublingual formulation and to ascertain if the purported short acting d-modafinil test article, under conditions of being very tired near to bedtime, had an affect on wakefulness.The test subject was given three vials: one vial containing the base formulation (as in Example 1) to test the taste and delivery means, and two coded vials. One of the coded vials contained 100 mg of d-modafinil formulation, and the second coded vial contained placebo (an equivalent amount of formulation).The subject was instructed to place the contents of the test formulation under the tongue, to allow the formulation to dissolve over two minutes, and to rinse any residual material with some water. ResultsSubject reported that the taste of the base formulation was pronounced, but tolerable. At 11 : 15 p.m. in the evening, the contents of one coded vial was placed under the tongue, allowed to dissolve over two minutes, and any residual was rinsed with some water. A strong taste remained for some time. The test subject then reported reading in bed, dozing on and off for EPO approximately 1.5 hours. After the room was darkened, the subject reported sleeping lighter, and awakening at least once at 3:15 a.m. during the night.On a following evening at 11 : 15 p.m., the contents of the second coded vial was similarly placed under the tongue, allowed to dissolve over two minutes under the tongue and rinsed. The test subject reported reading in bed until 12:50 a.m., then darkening the room and sleeping undisturbed all night until the morning.At both evenings the test subject reported being equally very tired. Approximately one week before these tests, the same subject took 200 mg racemic modafinil (Provigil.(R).) at 10 p.m. and reported a very pronounced effect, essentially being keep awake through the night to 5 a.m. Before unblinding the test articles, the subject recorded that one of the test articles was active, but neither test substance kept him awake as strongly or as long as the 200 mg racemic modafinil. After unblinding the test articles, it was confirmed that the coded vial with the reported activity contained 100 mg d-modafnil.
Results
approximately one week before these tests, the same subject took 200 mg test compound and reported a very pronounced effect
Location
Page/Page column 20; 21
Reference
NEUROHEALING PHARMACEUTICALS, INC.
Patent: WO2007/13962 A2, 2007 ; Title/Abstract Full Text Show Details
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Effect (Pharmacological Data)
neuronal differentiation; effect on
Species or Test-System (Pharmacological Data)
human neural stem cells (hNSCs)
Method (Pharmacological Data)
Example 21 Effects of the 5-HT1a Agonist Buspirone in Combination with Modafinil on Differentiation of Human Neural Stem Cells Human neural stem cells (hNSCs) were isolated and grown in monolayer culture, plated, treated with varying concentrations of buspirone in the presence or absence of modafinil, and stained with TUJ-1 antibody for the detection of neuronal differentiation or GFAP antibody for the detection of astrocyte differentiation, as described above. Mitogen-free test media with a positive control for neuronal differentiation was used along with basal media without growth factors as a negative control. Results are shown in FIGS. 39 and 40, which show concentration response curves of neuronal and astrocyte differentiation respectively, after background media values are subtracted. The concentration response curves of the combination of buspirone with modafinil are shown with the concentration response curves of buspirone or modafinil alone. The data is presented as a percent of neuronal or astrocyte positive control. The data indicate that the combination of buspirone with modafinil resulted in consistent neuronal differentiation with a simultaneous decrease in astrocyte differentiation relative to that produced by buspirone alone.
Type (Pharmacological Data)
EC50
Value of Type (Pharmacological Data)
12.5 μmol/l
Results
Figure is given.
Location
Page/Page column 6; 45; sheet 39
Reference
BrainCells, Inc.
Patent: US2007/270449 A1, 2007 ; Title/Abstract Full Text Show Details
92 of 150
Effect (Pharmacological Data)
astrocyte differentiation; effect on
Species or Test-System (Pharmacological Data)
human neural stem cells (hNSCs)
Method (Pharmacological Data)
Example 21 Effects of the 5-HT1a Agonist Buspirone in Combination with Modafinil on Differentiation of Human Neural Stem Cells Human neural stem cells (hNSCs) were isolated and grown in monolayer culture, plated, treated with varying concentrations of buspirone in the presence or absence of modafinil, and stained with TUJ-1 antibody for the detection of neuronal differentiation or GFAP antibody for the detection of astrocyte differentiation, as described above. Mitogen-free test media with a positive control for neuronal differentiation was used along with basal media without growth factors as a negative control. Results are shown in FIGS. 39 and 40, which show concentration response curves of neuronal and astrocyte differentiation respectively, after background media values are subtracted. The concentration response curves of the combination of buspirone with modafinil are shown with the concentration response curves of buspirone or modafinil alone. The data is presented as a percent of neuronal or astrocyte positive control. The data indicate that the combination of buspirone with modafinil resulted in consistent neuronal differentiation with a simultaneous decrease in astrocyte differentiation relative to that produced by buspirone alone.
Type (Pharmacological Data)
EC50
Value of Type (Pharmacological Data)
> 31.6 μmol/l
Results
Figure is given.
Location
Page/Page column 6; 45; sheet 40
Reference
BrainCells, Inc.
Patent: US2007/270449 A1, 2007 ; Title/Abstract Full Text Show Details
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Effect (Pharmacological Data)
behavioural symptoms
Species or Test-System (Pharmacological Data)
Syrian hamster
Sex
male
Route of Application
intraperitoneal
Concentration (Pharmacological Data)
100 - 300 mg/kg
Kind of Dosing (Pharmacological Data)
suspended in 0.25 percent carboxymethylcellulose
Method (Pharmacological Data)
hamsters were kept under 14-/10-h LD cycle and implanted with s.c. electrodes into the scull and nuchal muscle; 7 days later they were treated with title comp. at ZT 6 and EEG was recorded for 12 h, behavioral state was scored
Further Details (Pharmacological Data)
control: vehicle; LD: light-dark; ZT: zeitgeber time; EEG: electroencephalogram; ZT 6 is 6 h before lights off
Results
title comp. dose-dependently increased wakefulness at the expense of slow-wave and paradoxical sleep; at 300 mg/kg title comp. produced almost completely wakefulness for 6 h, paradoxical sleep was almost completely suppressed during 12 h
Reference
Webb, Ian C.; Pollock, Michael S.; Mistlberger, Ralph E.
Journal of Pharmacology and Experimental Therapeutics, 2006 , vol. 317, # 2 p. 882 - 889 Title/Abstract Full Text View citing articles Show Details
Effect (Pharmacological Data)
behavioural symptoms
Species or Test-System (Pharmacological Data)
Syrian hamster
Sex
male
Route of Application
intraperitoneal
Concentration (Pharmacological Data)
300 mg/kg
Kind of Dosing (Pharmacological Data)
suspended in 0.25 percent carboxymethylcellulose
Method (Pharmacological Data)
hamsters were kept under 14-/10-h LD cycle and treated with title comp. at ZT 6; they were videotaped in home cages for 3 h and the amount of time spent in various behaviors was analyzed
Further Details (Pharmacological Data)
control: vehicle; LD: light-dark; ZT: zeitgeber time; ZT 6 is 6 h before lights off; behaviors: active wake, quiet wake, behavioral sleep, grooming, feeding and drinking
Results
title comp. increased the percentage of total wakefulness and quiet wakefulness and significantly decreased the percentage of behavioral sleep and grooming
Reference
Webb, Ian C.; Pollock, Michael S.; Mistlberger, Ralph E.
Journal of Pharmacology and Experimental Therapeutics, 2006 , vol. 317, # 2 p. 882 - 889 Title/Abstract Full Text View citing articles Show Details
Effect (Pharmacological Data)
behavioural symptoms
Species or Test-System (Pharmacological Data)
Syrian hamster
Sex
male
Route of Application
intraperitoneal
Concentration (Pharmacological Data)
150 - 300 mg/kg
Kind of Dosing (Pharmacological Data)
suspended in 0.25 percent carboxymethylcellulose
Method (Pharmacological Data)
hamsters were kept under 14-/10-h LD cycle and treated with title comp. at ZT 6; the lights were then turned off and left off for 4 days, phase shifts were measured
Further Details (Pharmacological Data)
control: vehicle; LD: light-dark; ZT: zeitgeber time; phase shifts were measured by comparing the time of the onset of spontaneous activity (main period of daily wheel running) before and after treatment
Comment
No effect
(Pharmacological Data)
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Reference
Webb, Ian C.; Pollock, Michael S.; Mistlberger, Ralph E.
Journal of Pharmacology and Experimental Therapeutics, 2006 , vol. 317, # 2 p. 882 - 889 Title/Abstract Full Text View citing articles Show Details
Effect (Pharmacological Data)
behavioural symptoms
Species or Test-System (Pharmacological Data)
Syrian hamster
Sex
male
Route of Application
intraperitoneal
Concentration (Pharmacological Data)
300 mg/kg
Kind of Dosing (Pharmacological Data)
suspended in 0.25 percent carboxymethylcellulose
Method (Pharmacological Data)
hamsters were kept under 14-/10-h LD cycle and subjected to 1 night of LL; after that they were treated with title comp. at ZT 4, the lights were turned off at ZT 6 and left off for 4 days; phase shifts were measured
Further Details (Pharmacological Data)
control: vehicle; LD: light-dark; LL: constant light; ZT: zeitgeber time; phase shifts were measured by comparing the time of the onset of spontaneous activity (main period of daily wheel running) before and after treatment
Comment (Pharmacological Data)
No effect
Reference
Webb, Ian C.; Pollock, Michael S.; Mistlberger, Ralph E.
Journal of Pharmacology and Experimental Therapeutics, 2006 , vol. 317, # 2 p. 882 - 889 Title/Abstract Full Text View citing articles Show Details
Effect (Pharmacological Data)
behavioural symptoms
Species or Test-System (Pharmacological Data)
Syrian hamster
Sex
male
Route of Application
intraperitoneal
Concentration (Pharmacological Data)
300 mg/kg
Kind of Dosing (Pharmacological Data)
suspended in 0.25 percent carboxymethylcellulose
Method (Pharmacological Data)
hamsters were kept under 14-/10-h LD cycle and treated with title comp. at ZT 6 or ZT 12; lights were turned off at ZT 12 and left off for 4-7 days; the effect on phase shifts induced by 15-min light pulse (ca. 190 lx) at ZT 13 of treatment day measured
Further Details (Pharmacological Data)
control: vehicle; LD: light-dark; ZT: zeitgeber time; phase shifts were measured by comparing the time of the onset of spontaneous activity (main period of daily wheel running) during 3 days before treatment and on days 2, 3 and 6 after
Comment (Pharmacological Data)
No effect
Reference
Webb, Ian C.; Pollock, Michael S.; Mistlberger, Ralph E.
Journal of Pharmacology and Experimental Therapeutics, 2006 , vol. 317, # 2 p. 882 - 889 Title/Abstract Full Text View citing articles Show Details
Effect (Pharmacological Data)
behavioural symptoms
Species or Test-System (Pharmacological Data)
Syrian hamster
Sex
male
Route of Application
intraperitoneal
Concentration (Pharmacological Data)
300 mg/kg
Kind of Dosing (Pharmacological Data)
suspended in 0.25 percent carboxymethylcellulose
Method (Pharmacological Data)
hamsters were kept under 14-/10-h LD cycle, lights were turned off at ZT 12; at ZT 17 animals were treated with title comp. and the effect on phase shifts induced by 15-min light pulse (ca. 190 lx) at ZT 18 was measured; lights remained off for 4-7 days
Further Details (Pharmacological Data)
control: vehicle; LD: light-dark; ZT: zeitgeber time; phase shifts were measured by comparing the time of the onset of spontaneous activity (main period of daily wheel running) during 3 days before treatment and on days 2, 3 and 6 after
Comment (Pharmacological Data)
No effect
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Reference
Webb, Ian C.; Pollock, Michael S.; Mistlberger, Ralph E.
Journal of Pharmacology and Experimental Therapeutics, 2006 , vol. 317, # 2 p. 882 - 889 Title/Abstract Full Text View citing articles Show Details
Effect (Pharmacological Data)
behavioural symptoms
Species or Test-System (Pharmacological Data)
Syrian hamster
Sex
male
Route of Application
intraperitoneal
Concentration (Pharmacological Data)
300 mg/kg
Kind of Dosing (Pharmacological Data)
suspended in 0.25 percent carboxymethylcellulose
Method (Pharmacological Data)
hamsters kept under 14-/10-h LD cycle were subjected to 1 night of LL; then they were treated with title comp. at ZT 4 and confined to a new wheel at ZT 6; the lights were turned off during confinement and left off for 4 days; phase shifts were measured
Further Details (Pharmacological Data)
control: vehicle; LD: light-dark; LL: constant light; ZT: zeitgeber time; phase shifts were measured by comparing the time of the onset of spontaneous activity (main period of daily wheel running) before and after treatment
Comment (Pharmacological Data)
No effect
Reference
Webb, Ian C.; Pollock, Michael S.; Mistlberger, Ralph E.
Journal of Pharmacology and Experimental Therapeutics, 2006 , vol. 317, # 2 p. 882 - 889 Title/Abstract Full Text View citing articles Show Details
Effect (Pharmacological Data)
behavioural symptoms
Species or Test-System (Pharmacological Data)
Syrian hamster
Sex
male
Route of Application
intraperitoneal
Concentration (Pharmacological Data)
300 mg/kg
Kind of Dosing (Pharmacological Data)
suspended in 0.25 percent carboxymethylcellulose
Method (Pharmacological Data)
hamsters kept under 14-/10-h LD cycle were subjected to 1 night of LL; then they were treated with title comp. at ZT 4 and confined to a new wheel at ZT 6 (for 3 h); lights turned off at ZT 6 and the effect on wheel running activity analyzed for 18 h
Further Details (Pharmacological Data)
control: vehicle; LD: light-dark; LL: constant light; ZT: zeitgeber time
Results
title comp. decreased the number of 18-h cumulative wheel revolutions by 55.4 percent; the number of wheel revolutions during wheel confinement was decreased by 53.3 percent
Reference
Webb, Ian C.; Pollock, Michael S.; Mistlberger, Ralph E.
Journal of Pharmacology and Experimental Therapeutics, 2006 , vol. 317, # 2 p. 882 - 889 Title/Abstract Full Text View citing articles Show Details
Effect (Pharmacological Data)
behavioural symptoms
Species or Test-System (Pharmacological Data)
Syrian hamster
Sex
male
Route of Application
intraperitoneal
Concentration (Pharmacological Data)
300 mg/kg
Kind of Dosing (Pharmacological Data)
suspended in 0.25 percent carboxymethylcellulose
Method (Pharmacological Data)
hamsters kept under 14-/10-h LD cycle were subjected to 1 night of LL; then they were treated with title comp. at ZT 4 and the lights were turned off at ZT 6; the effect on wheel running activity was analyzed for 18 h
Further Details (Pharmacological Data)
control: vehicle; LD: light-dark; LL: constant light; ZT: zeitgeber time
Results
title comp. decreased the number of 18-h cumulative wheel revolutions by 51.5 percent
Reference
Webb, Ian C.; Pollock, Michael S.; Mistlberger, Ralph E.
Journal of Pharmacology and Experimental Therapeutics, 2006 , vol. 317, # 2 p. 882 - 889 Title/Abstract Full Text View citing articles Show Details
102 of 150
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105 of 150
Effect (Pharmacological Data)
receptor; binding activity
Species or Test-System (Pharmacological Data)
Macaca mulatta, rhesus monkey
Sex
male and female
Route of Application
intravenous
Concentration (Pharmacological Data)
2 - 8 mg/kg
Method (Pharmacological Data)
title comp. administered; after 1 h <11C>CFT or <11C>altropane injected i.v.; DAT or NET, resp., occupancy measured using positron emission tomography imagine
Further Details (Pharmacological Data)
CFT: 2β-carbomethoxy-3β-4-(fluorophenyl)tropane; DAT: dopamine transporter; NET: norepinephrine transporter; methylphenidate used as reference comp.
Results
title comp. occupied 35percent and 53percent of DAT sites in striatum at 5 and 8 mg/kg, resp., when <11C>CFT probe was used; at 8 mg/kg decreased <11C>altropane binding by 67percent; effect comparable to that of methylphenidate; no effect at 2 mg/kg (table, figures)
Reference
Madras, Bertha K.; Xie, Zhihua; Lin, Zhicheng; Jassen, Amy; Panas, Helen; Lynch, Laurie; Johnson, Ryan; Livni, Eli; Spencer, Thomas J.; Bonab, Ali A.; Miller, Gregory M.; Fischman, Alan J.
Journal of Pharmacology and Experimental Therapeutics, 2006 , vol. 319, # 2 p. 561 - 569 Title/Abstract Full Text View citing articles Show Details
Effect (Pharmacological Data)
receptor; binding activity
Species or Test-System (Pharmacological Data)
HEK293 cells
Method (Pharmacological Data)
radioligand binding assay performed; cells transfected with DAT incubated with <3H>DA in presence of title comp.; radioactivity measured using scintillation fluid
Further Details (Pharmacological Data)
DAT: dopamine transporter
Type (Pharmacological Data)
IC50
Value of Type (Pharmacological Data)
4360 nmol/l
Reference
Madras, Bertha K.; Xie, Zhihua; Lin, Zhicheng; Jassen, Amy; Panas, Helen; Lynch, Laurie; Johnson, Ryan; Livni, Eli; Spencer, Thomas J.; Bonab, Ali A.; Miller, Gregory M.; Fischman, Alan J.
Journal of Pharmacology and Experimental Therapeutics, 2006 , vol. 319, # 2 p. 561 - 569 Title/Abstract Full Text View citing articles Show Details
Effect (Pharmacological Data)
receptor; binding activity
Species or Test-System (Pharmacological Data)
HEK293 cells
Method (Pharmacological Data)
transport assay performed; cells transfected with DAT pretreated with title comp.; incubated with <3H>DA at 25 deg C for 10 min in darkness; radioactivity measured using scintillation fluid
Further Details (Pharmacological Data)
DAT: dopamine transporter; reference comp. (IC50, nmol/l): methylphenidate (25.4), benztropine (213), bupropion (1088)
Type (Pharmacological Data)
IC50
Value of Type (Pharmacological Data)
6390 nmol/l
Reference
Madras, Bertha K.; Xie, Zhihua; Lin, Zhicheng; Jassen, Amy; Panas, Helen; Lynch, Laurie; Johnson, Ryan; Livni, Eli; Spencer, Thomas J.; Bonab, Ali A.; Miller, Gregory M.; Fischman, Alan J.
Journal of Pharmacology and Experimental Therapeutics, 2006 , vol. 319, # 2 p. 561 - 569 Title/Abstract Full Text View citing articles Show Details
Effect (Pharmacological Data)
receptor; binding activity
Species or Test-System (Pharmacological Data)
HEK293 cells
Method (Pharmacological Data)
transport assay performed; cells transfected with NET pretreated with title comp.; incubated with <3H>norepinephrine at 25 deg C for 10 min in darkness; radioactivity measured using scintillation fluid
Further Details (Pharmacological Data)
NET: norepinephrine transporter; reference comp. (IC50, nmol/l): methylphenidate (26.5), benztropine (667)
Type (Pharmacological Data)
IC50
106 of 150
107 of 150
108 of 150
109 of 150
Value of Type (Pharmacological Data)
35600 nmol/l
Reference
Madras, Bertha K.; Xie, Zhihua; Lin, Zhicheng; Jassen, Amy; Panas, Helen; Lynch, Laurie; Johnson, Ryan; Livni, Eli; Spencer, Thomas J.; Bonab, Ali A.; Miller, Gregory M.; Fischman, Alan J.
Journal of Pharmacology and Experimental Therapeutics, 2006 , vol. 319, # 2 p. 561 - 569 Title/Abstract Full Text View citing articles Show Details
Effect (Pharmacological Data)
receptor; binding activity
Species or Test-System (Pharmacological Data)
HEK293 cells
Method (Pharmacological Data)
transport assay performed; cells transfected with NET pretreated with title comp.; incubated with <3H>dopamine at 25 deg C for 10 min in darkness; radioactivity measured using scintillation fluid
Further Details (Pharmacological Data)
NET: norepinephrine transporter
Type (Pharmacological Data)
IC50
Value of Type (Pharmacological Data)
170000 nmol/l
Reference
Madras, Bertha K.; Xie, Zhihua; Lin, Zhicheng; Jassen, Amy; Panas, Helen; Lynch, Laurie; Johnson, Ryan; Livni, Eli; Spencer, Thomas J.; Bonab, Ali A.; Miller, Gregory M.; Fischman, Alan J.
Journal of Pharmacology and Experimental Therapeutics, 2006 , vol. 319, # 2 p. 561 - 569 Title/Abstract Full Text View citing articles Show Details
Effect (Pharmacological Data)
receptor; binding activity
Species or Test-System (Pharmacological Data)
HEK293 cells
Method (Pharmacological Data)
transport assay performed; cells transfected with SERT pretreated with title comp.; incubated with <3H>serotonin at 25 deg C for 10 min in darkness; radioactivity measured using scintillation fluid
Further Details (Pharmacological Data)
SERT: serotonin transporter; reference comp.: benztropine (IC50 = 21660 nmol/l)
Type (Pharmacological Data)
IC50
Value of Type (Pharmacological Data)
> 500 μmol/l
Reference
Madras, Bertha K.; Xie, Zhihua; Lin, Zhicheng; Jassen, Amy; Panas, Helen; Lynch, Laurie; Johnson, Ryan; Livni, Eli; Spencer, Thomas J.; Bonab, Ali A.; Miller, Gregory M.; Fischman, Alan J.
Journal of Pharmacology and Experimental Therapeutics, 2006 , vol. 319, # 2 p. 561 - 569 Title/Abstract Full Text View citing articles Show Details
Effect (Pharmacological Data)
receptor; binding activity
Species or Test-System (Pharmacological Data)
Macaca mulatta, rhesus monkey
Sex
male and female
Route of Application
intravenous
Concentration (Pharmacological Data)
2 - 8 mg/kg
Method (Pharmacological Data)
title comp. administered; after 1 h <11C>MeNER injected i.v.; NET occupancy measured using positron emission tomography imagine
Further Details (Pharmacological Data)
MeNER: (S,S)-2-(α-(2-methoxyphenoxy)benzyl)morpholine; NET: norepinephrine transporter
Results
title comp. occupied 16percent and 44percent of NET sites in thalamus at 5 and 8 mg/kg, resp.; no effect at 2 mg/kg (table, figures)
Reference
Madras, Bertha K.; Xie, Zhihua; Lin, Zhicheng; Jassen, Amy; Panas, Helen; Lynch, Laurie; Johnson, Ryan; Livni, Eli; Spencer, Thomas J.; Bonab, Ali A.; Miller, Gregory M.; Fischman, Alan J.
Journal of Pharmacology and Experimental Therapeutics, 2006 , vol. 319, # 2 p. 561 - 569 Title/Abstract Full Text View citing articles Show Details
Effect (Pharmacological Data)
receptor; binding activity
Species or Test-System (Pharmacological Data)
HEK293 cells
Concentration
Ca. 1E-09 - 0.0001 mol/l
(Pharmacological Data)
110 of 150
Method (Pharmacological Data)
cells expressing or not human DAT, NET or SERT transfected with TA1 and CRE-luc reporter system; treated with title comp. alone or in presence of PEA for 18 h; lysed; TA1 activation determined by measuring luciferase conc.
Further Details (Pharmacological Data)
DAT: dopamine transporter; NET: norepinephrine transporter; SERT: serotonin transporter; TA1: trace amine receptor; CRE: cAMP response element; PEA: phenethylamine
Results
title comp. sign. increased TA1 activity in presence of DAT at 100 μmol/l; no effect on TA1 activity alone or in presence of NET or SERT; at 10 μmol/l in presence of PEA sign. activated TA1 in presence of DAT or NET, but not SERT (figure)
Reference
Madras, Bertha K.; Xie, Zhihua; Lin, Zhicheng; Jassen, Amy; Panas, Helen; Lynch, Laurie; Johnson, Ryan; Livni, Eli; Spencer, Thomas J.; Bonab, Ali A.; Miller, Gregory M.; Fischman, Alan J.
Journal of Pharmacology and Experimental Therapeutics, 2006 , vol. 319, # 2 p. 561 - 569 Title/Abstract Full Text View citing articles Show Details
Effect (Pharmacological Data)
self-injurious behavior; effect on
Species or Test-System (Pharmacological Data)
human
Sex
female
Method (Pharmacological Data)
Example 2; Treatment of a 45-Year-Old Female with Self-Injurious Behavior Using Riluzole; Patient 2 was a 45-year-old woman with a long history of borderline personality disorder, major depression, obsessive-compulsive disorder and generalized anxiety disorder. She had a several year history of engaging in self-injurious behavior such as hitting herself until she bruised, banging her head, and cutting herself. These self-injurious behaviors and the cravings to cut worsened under times of stress. She was previously treated with intensive psychotherapy, cognitive behavioral therapy, and pharmacotherapy. Medication management included treatment trials, either alone or in combination, of the following medications: EFFEXOR, ZOLOFT (sertaline HCl), TOPAMAX (topirimate), ATIVAN (lorazepam), trazodone, ABILIFY AND NEURONTIN (gabapentin). Riluzole, a glutamate modulating agent, was added to her medication regimen which consisted of ZOLOFT 200 mg each day, RISPERDAL (risperidone) 2 mg at bedtime, KLONOPIN 1 mg three times per day and PROVIGIL (modafinil) 200 mg a day. Riluzole was dosed at 50 mg twice a day. She reported a marked attenuation and ultimately, complete cessation of the desire to engage in self-injurious behaviors. Similar to the first case, the cessation in self-injurious behaviors occurred between week 2 and 3 of treatment with riluzole. Patient 2 has not engaged in any self-injurious behaviors in over six months, which represents the longest period of time that she has not engaged in self-injurious behavior over the last several years.
Results
treatment with title compound (200 mg once daily) in combination with zoloft (200 mg once daily), risperidone (2 mg once daily), klonopin (1 mg, 3 times per day) and riluzole (50 mg twice a day) caused a marked attenuation and ultimately, complete cessation of the desire to engage in self-injurious behaviors
Location
Page/Page column 7
Reference
Feuerstein, Seth; Coric, Vladimir
Patent: US2006/167068 A1, 2006 ; Title/Abstract Full Text Show Details
111 of 150
Effect (Pharmacological Data)
blood pressure; effect on
Species or Test-System (Pharmacological Data)
human
Sex
male and female
Route of Application
peroral
Method (Pharmacological Data)
RESEARCH DESIGNType of Design and Sub-Groups of Problem Gamblers. We assessed the effects of a 200-mg oral dose of modafinil in a placebo-controlled, fully counterbalanced, double blind, between-within design. The within-subjects factor was Treatment: drug vs. placebo. The between-subjects factor was Sequence of Treatment: Half of the subjects received modafinil on test session 1 and placebo on test session 2; the other half received the treatments in reverse order.Subjects Subjects were 6 problem gamblers as defined by scores > 5 on the South Oaks Gambling Screen (SOGS; Lesieur Blume, 1987) and on the DSM-IV (APA, 1994).Each subject underwent two procedurally identical (except for drug treatment) test sessions. On each session, subjects received their assigned drug treatment and underwent a 15-minute gambling episode on a slot-machine version Electronic Gaming Device (EGD). Subjective, cognitive, and behavioral indices were assessed at multiple time points throughout each session (see details below).General Reliability and Validity of Tasks and Dependent Measures.Modified visual analogue scales Modified Visual Analogue Scales (m-VAS; 0-10) measure (a) Desire to Gamble, (b) Confidence to Refrain from Gambling. M-VAS ratings are widely used tools for assessing drug effects (Fischman Foltin, 1991), and their sensitivity to drug effects in problem gamblers has been validated in our two previous drug studies (Zack Poulos, 2004; Zack, Poulos Desmond, 2004). M-VAS ratings also assess the subjective pleasurable or rewarding effects of the gambling episode (i.e., Enjoyment, Excitement, and perceived 'High'). M- VAS measures of gambling reward have been validated in previous published studies (Loba, Stewart, Klein, Blackburn, 2001), as well as in our recent haloperidol study (Zack, Poulos Desmond, 2004).M-VAS Measure of Interest in Everyday Activities To assess the effects of modafinil on subjective (i.e., state) boredom proneness during the test sessions, we used an m-VAS scale (0-10) to rate agreement with the following statement: "Right now, I could find interest in any one of a variety of everyday activities."Addiction Research Center Inventory (ARCI) Relevant sub-scales of the ARCI (Haertzen, 1965) assess responses to the drug treatment at several points within each test session (see Session Timeline below). The ARCI is a standardized index of drug effects that measures a range of EPO subjective, mental, emotional and physical responses to psychoactive drugs. The ARCI has been used to assess the modulating effects of modafnil on subjective responses to cocaine (Dackis et al., 2003).Stop Signal Task We use the most recent version of the Stop-Signal Task, which employs an algorithm to compute mean inhibitory latency to the stop signal (also known as Stop SignalReaction Time; SSRT). This task provides a behavioral index of inhibitory control: The faster the SSRT, the better is the inhibitory control. Performance on this task has been shown to correlate positively with scores on the Eysenck Impulsiveness Scale in heterogeneous samples (Logan, Schachar, Tannock, 1997). The task has been widely validated in terms of its sensitivity to drug effects, including modafinil, as well as in clinical populations (e.g., ADHD patients; For details, see Turner et al. 2004).Gambling/Slot Machine Episode As in previous laboratory gambling studies (Loba et al., 2001), subjects are given cash credits with which to bet. They are required to play for 15 minutes. Play stops if a subject exhausts all credits. To increase validity and provide an incentive to do well on the slot machine, subjects are advised that they will receive a monetary bonus at the end of the study proportional to the number of credits they win on each session. This is also noted in the consent form. For ethical reasons, all subjects in fact receive an identical bonus of USD80 (USD40 x 2 sessions) in addition to their participation fee. We use an El
Results
there was only minor fluctuation in blood pressure due to the game under modafinil (figure is given)
Location
Page/Page column 5; 8; 12; 18; sheet 4
Reference
CENTRE FOR ADDICTION AND MENTAL HEALTH
Patent: WO2006/32146 A1, 2006 ; Title/Abstract Full Text Show Details
112 of 150
113 of 150
Effect (Pharmacological Data)
analgesic, other
Species or Test-System (Pharmacological Data)
human
Sex
male and female
Route of Application
peroral
Concentration (Pharmacological Data)
400 mg
Kind of Dosing (Pharmacological Data)
daily for 2 days
Method (Pharmacological Data)
12 healthy subjects in randomized, double-blind crossover study; 2 h after the second dose responses in acute pain tests assessed (finger pressure pain task using Forgione-Barber pain stimulator, 10 min rest, then forearm ischemic pain task)
Further Details (Pharmacological Data)
both acute pain tests evaluated using verbal numeric rating scale and by completing McGill Pain Questionnaire
Comment (Pharmacological Data)
No effect
Reference
Taneja, Indu; Bruehl, Stephen; Robertson, David
Journal of Clinical Pharmacology, 2004 , vol. 44, # 12 p. 1425 - 1427 Title/Abstract Full Text View citing articles Show Details
Effect (Pharmacological Data)
pharmacokinetics
Species or Test-System (Pharmacological Data)
beagle dog
Sex
male
Route of Application
peroral
Method (Pharmacological Data)
polymorphic forms of title comp. racemate administered as single dose; blood samples collected predose and 0.5 to 24 h post-dose; plasma title comp. concentrations determined by validated high-pressure liquid chromatography
Results
title comp. Cmax = 18.60 μg/ml, C4h = 15.37 μg/ml, AUC0-24h = 164.80 h*μg/ml
Location
Page 44-46
Reference
CEPHALON FRANCE; ORGANISATION DE SYNTHESE MONDIALE ORSYMONDE
Patent: WO2004/14846 A1, 2004 ; Title/Abstract Full Text Show Details
114 of 150
Effect (Pharmacological Data)
pharmacokinetics
Species or Test-System (Pharmacological Data)
beagle dog
Sex
male
Route of Application
peroral
Method (Pharmacological Data)
polymorphic forms of title comp. racemate administered as single dose; blood samples collected predose and 0.5 to 24 h post-dose; plasma title comp. concentrations determined by validated high-pressure liquid chromatography
Results
title comp. conc. increased in time-dependent manner with Cmax = 18.60 μg/ml , Tmax = 3.00 h
Location
Page 44; 46-47
Reference
CEPHALON FRANCE; ORGANISATION DE SYNTHESE MONDIALE ORSYMONDE
Patent: WO2004/14846 A1, 2004 ; Title/Abstract Full Text Show Details
115 of 150
Effect (Pharmacological Data)
pharmacokinetics
Species or Test-System (Pharmacological Data)
beagle dog
Sex
male
Route of Application
peroral
Method (Pharmacological Data)
polymorphic forms of title comp. racemate administered as single dose; blood samples collected predose and 0.5 to 24 h post-dose; plasma title comp. concentrations determined by validated high-pressure liquid chromatography
Results
title comp. Cmax = 24.98 μg/ml, C4h = 21.23 μg/ml, AUC0-24h = 200.69 h*μg/ml Page 44-46
Location Reference
CEPHALON FRANCE; ORGANISATION DE SYNTHESE MONDIALE ORSYMONDE
Patent: WO2004/14846 A1, 2004 ; Title/Abstract Full Text Show Details
116 of 150
Effect (Pharmacological Data)
pharmacokinetics
Species or Test-System (Pharmacological Data)
beagle dog
Sex
male
Route of Application
peroral
Method (Pharmacological Data)
polymorphic forms of title comp. racemate administered as single dose; blood samples collected predose and 0.5 to 24 h post-dose; plasma title comp. concentrations determined by validated high-pressure liquid chromatography
Results
title comp. conc. increased in time-dependent manner with Cmax = 18.72 μg/ml, Tmax = 1.67 h
Location
Page 44; 46-47
Reference
CEPHALON FRANCE; ORGANISATION DE SYNTHESE MONDIALE ORSYMONDE
Patent: WO2004/14846 A1, 2004 ; Title/Abstract Full Text Show Details
117 of 150
118 of 150
Effect (Pharmacological Data)
drug interaction
Species or Test-System (Pharmacological Data)
human
Sex
female
Route of Application
peroral
Kind of Dosing (Pharmacological Data)
200 mg once daily for 7 d from day 6 - 8 of 28-d menstrual cycle 2, followed by 400 mg once daily for two last weeks of cycle 2 and 1-st week of cycle 3; given with 240 ml of water
Method (Pharmacological Data)
Ortho Tri-Cyclen given throughout cycles 1, 2, and 1-st wk of cycle 3; 24-h blood sampled on cycle 2 day 5 - 7 and last treatment day; ethinyl estradiol plasma conc. measured by HPLC with ultraviolet detection
Further Details (Pharmacological Data)
Ortho Tri-Cyclen: 0.035 mg ethinyl estradiol with 0.180 - 0.250 progestin norgestimate, p.o.; AUC(0-τ): area under conc.-time curve; Cmax/Ctrough: maximum/minimum plasma conc., resp.; tmax: time to Cmax:; t1/2: half-life; placebo control
Results
in title comp. group ethinyl estradiol AUC(0-τ) was significantly decreased from cycle 2 to cycle 3 by 18 percent, Cmax by 11 percent, and tmax by 0.3 h; no significant difference in t1/2, Ctrough, and terminal elimination rate constant
Reference
Robertson Jr., Philmore; Hellriegel, Edward T.; Arora, Sanjay; Nelson, Michael
Clinical Pharmacology and Therapeutics, 2002 , vol. 71, # 1 p. 46 - 56 Title/Abstract Full Text View citing articles Show Details
Effect (Pharmacological Data)
pharmacokinetics
Species or Test-System (Pharmacological Data)
human
Sex
female
Route of Application
peroral
Kind of Dosing (Pharmacological Data)
200 mg once daily for 7 d from day 6 - 8 of 28-d menstrual cycle 2, followed by 400 mg once daily for two last weeks of cycle 2 and 1-st week of cycle 3; given with 240 ml of water
Method (Pharmacological Data)
title comp. given with Ortho Tri-Cyclen and triazolam (0.125 mg added on days 5 - 7 of cycles 2 and 3); 24-h blood sampled at last treatment day; title comp. and metabolites 1/2 (title comp. acid/sulfone, resp.) plasma conc. measured by HPLC
Further Details (Pharmacological Data)
Ortho Tri-Cyclen: 0.035 mg ethinyl estradiol with 0.180 - 0.250 progestin norgestimate, p.o., for cycles 1, 2, 1-st wk of cycle 3; AUC(0-τ): area under curve; Cmax/trough: max/minimum plasma conc., resp.; tmax: time to Cmax:; t1/2: half-life
Half-life Time (Pharmacological Data)
11.4 h
Results
title comp./metabolite 1/2 AUC(0-τ) = 131/51/105 μg*h/ml, Cmax = 13.4/6.1/5.2 μg/ml, Ctrough = 2.4/0.4/4.3 μg/ml, tmax = 1.8/2.8/4.8 h, terminal rate constant for elimination from plasma = 0.062/0.128/- (resp.); metabolite 1/2 t1/2 = 5.5/- h
Metabolite (Pharmacological Data)
modafinil acid [Reaxys RN: 6650982] ; Modafinil sulfone [Reaxys RN: 9199801]
Reference
Robertson Jr., Philmore; Hellriegel, Edward T.; Arora, Sanjay; Nelson, Michael
Clinical Pharmacology and Therapeutics, 2002 , vol. 71, # 1 p. 46 - 56 Title/Abstract Full Text View citing articles Show Details
119 of 150
120 of 150
121 of 150
122 of 150
Effect (Pharmacological Data)
releasing hormones
Species or Test-System (Pharmacological Data)
human
Sex
female
Route of Application
peroral
Kind of Dosing (Pharmacological Data)
200 mg once daily for 7 d from day 6 - 8 of 28-d menstrual cycle 2, followed by 400 mg once daily for two last weeks of cycle 2 and 1-st week of cycle 3; given with 240 ml of water
Method (Pharmacological Data)
title comp. given with Ortho Tri-Cyclen and triazolam (0.125 mg added on days 5 - 7 of cycles 2 and 3, p.o.); 24-h blood sampled on day 5 - 7 of cycle 2 and on last treatment day; FSH and LH plasma conc. determined
Further Details (Pharmacological Data)
Ortho Tri-Cyclen: 0.035 mg ethinyl estradiol with 0.180 - 0.250 progestin norgestimate, p.o., for cycles 1, 2, and 1-st wk of cycle 3; FSH: follicle-stimulating hormone; LH: luteinizing hormone; placebo control
Results
no significant differences in title comp./placebo groups in mean changes from cycle 2 to 3 in FSH, LH plasma conc.; title comp./placebo mean change in plasma FSH conc. increased by 0.4/0.1 mIU/L, mean LH plasma conc. increased by 0.4/0.2 mIU/L (resp.)
Reference
Robertson Jr., Philmore; Hellriegel, Edward T.; Arora, Sanjay; Nelson, Michael
Clinical Pharmacology and Therapeutics, 2002 , vol. 71, # 1 p. 46 - 56 Title/Abstract Full Text View citing articles Show Details
Effect (Pharmacological Data)
toxicity
Species or Test-System (Pharmacological Data)
human
Sex
female
Route of Application
peroral
Kind of Dosing (Pharmacological Data)
200 mg once daily for 7 d from day 6 - 8 of 28-d menstrual cycle 2, followed by 400 mg once daily for two last weeks of cycle 2 and 1-st week of cycle 3; given with 240 ml of water
Method (Pharmacological Data)
title comp. (group A) given with Ortho Tri-Cyclen and triazolam (0.125 mg added on days 5 - 7 of cycles 2 and 3, p.o.); blood and urine sampled at screening visit, and on last treatment day; adverse events recorded
Further Details (Pharmacological Data)
Ortho Tri-Cyclen: 0.035 mg ethinyl estradiol with 0.180 - 0.250 progestin norgestimate, p.o., for cycles 1, 2, and 1-st wk of cycle 3; placebo control (group B)
Results
adverse events were mild or moderate; in groups A and B most frequent were headache/asthenia/nausea/dizziness/metrorrhagia/pain/dysmenorrhea/anorexia in 72/50/33/28/22/17/17/17 and 53/58/11/11/5/5/5/0 percent, resp.
Reference
Robertson Jr., Philmore; Hellriegel, Edward T.; Arora, Sanjay; Nelson, Michael
Clinical Pharmacology and Therapeutics, 2002 , vol. 71, # 1 p. 46 - 56 Title/Abstract Full Text View citing articles Show Details
Effect (Pharmacological Data)
enzyme; induction of
Species or Test-System (Pharmacological Data)
human
Sex
female
Route of Application
peroral
Concentration (Pharmacological Data)
200 mg
Kind of Dosing (Pharmacological Data)
200 mg once daily for 7 d from day 6 - 8 of 28-d menstrual cycle 2, followed by 400 mg once daily for two last weeks of cycle 2 and 1-st week of cycle 3; given with 240 ml of water
Method (Pharmacological Data)
title comp. (group A) given with Ortho Tri-Cyclen and triazolam (0.125 mg added on days 5 - 7 of cycles 2 and 3, p.o.); blood and urine sampled at screening visit and on last treatment day; alkaline phosphatase levels determined
Further Details (Pharmacological Data)
Ortho Tri-Cyclen: 0.035 mg ethinyl estradiol + 0.180 - 0.250 progestin norgestimate, for cycle 1, 2, and 1-st wk of cycle 3; placebo control (group B)
Results
statistically significant increase observed in mean change from baseline for alkaline phosphatase, greater in group A vs group B, without clinically significant abnormal alkaline phosphatase levels for any subject
Reference
Robertson Jr., Philmore; Hellriegel, Edward T.; Arora, Sanjay; Nelson, Michael
Clinical Pharmacology and Therapeutics, 2002 , vol. 71, # 1 p. 46 - 56 Title/Abstract Full Text View citing articles Show Details
Effect (Pharmacological Data)
drug interaction
Species or Test-System (Pharmacological Data)
human
Sex
female peroral
Route of Application
123 of 150
124 of 150
125 of 150
Kind of Dosing (Pharmacological Data)
200 mg once daily for 7 d from day 6 - 8 of 28-d menstrual cycle 2, followed by 400 mg once daily for two last weeks of cycle 2 and 1-st week of cycle 3; given with 240 ml of water
Method (Pharmacological Data)
Ortho Tri-Cyclen given for cycle 1, 2, and 1-st wk of cycle 3, p.o.; 0.125 mg triazolam added on days 5 - 7 of cycles 2 and 3, p.o.; 24-h blood sampled on cycle 2 days 5 - 7 and on last day of treatment; triazolam plasma conc. measured by HPLC
Further Details (Pharmacological Data)
Ortho Tri-Cyclen: 0.035 mg ethinyl estradiol with 0.180-0.250 progestin norgestimate; AUC(0-τ): area under curve; Cmax/trough: max/minimum plasma conc., resp.; tmax: time to Cmax:; t1/2: half-life; λ: elimination rate constant; placebo control
Results
in title comp. group triazolam AUC(0-τ) significantly changed from cycle 2 to cycle 3 by -59 percent, Cmax by -42 percent, λ by 51 percent, t1/2 by -35 percent
Reference
Robertson Jr., Philmore; Hellriegel, Edward T.; Arora, Sanjay; Nelson, Michael
Clinical Pharmacology and Therapeutics, 2002 , vol. 71, # 1 p. 46 - 56 Title/Abstract Full Text View citing articles Show Details
Effect (Pharmacological Data)
pharmacokinetics
Species or Test-System (Pharmacological Data)
human
Sex
male and female
Route of Application
peroral
Concentration (Pharmacological Data)
200 - 400 mg
Kind of Dosing (Pharmacological Data)
title comp. (100 mg TB) admin. once-daily, early morning (200 mg on days 1-7; 400 mg on days 8-28) alone/in combination with once-daily, MAD of Dex (20 mg on days 22-28)
Method (Pharmacological Data)
open-label, randomized, single-period, parallel-group, single-center study; healthy subjects (13 Caucasians, 2 others) in groups (GPs) received title comp. with/without Dex; blood collected pre- and post-dosing (day 21, 28) upto 24 h; PK detd. by HPLC
Further Details (Pharmacological Data)
control: placebo; group 1: title comp.+dextroamphetamine (Dex); group 2: title comp. alone; safety and tolerability also studied; TB: tablets; MAD: mid-afternoon doses
Results
mean changes in PK parameters for title comp. and its two circulating metabolites between group 1 and 2 were not statistically signif. different, except Cmax for modafinil acid; mild to moderate adverse events reported; tables, diagram
Reference
Hellriegel, Edward T.; Arora, Sanjay; Nelson, Michael; Robertson Jr., Philmore
Journal of Clinical Pharmacology, 2002 , vol. 42, # 4 p. 450 - 460 Title/Abstract Full Text View citing articles Show Details
Effect (Pharmacological Data)
biotransformation
Species or Test-System (Pharmacological Data)
human
Sex
male and female
Route of Application
peroral
Concentration (Pharmacological Data)
200 - 400 mg
Kind of Dosing (Pharmacological Data)
title comp. (100 mg tablets) admin. once-daily, early morning (200 mg on d 1-7; 400 mg on d 8-28) alone/in combination with once-daily, mid-afternoon doses of Dex (20 mg on d 22-28)
Method (Pharmacological Data)
open-label, randomized, single-period, parallel-group, single-center study; healthy subjects (13 Caucasians, 2 others) in groups (GPs) received title comp. with/without Dex; blood collected pre- and post-dosing (d 21 and 28) upto 24 h; PK detd. by HPLC
Further Details (Pharmacological Data)
control: placebo; group (GP) 1: title comp.+dextroamphetamine (DEX); GP 2: title comp. alone; MTPC: mean trough plasma conc.; MC: mean changes; PK: pharmacokinetic parameters
Results
MTPC of metabolites on d 19-21 and 26-28 was similar within treatment GPs; MTPC of acid was similar between GPs but sulfone was higher in GP 1 than GP 2; MC in PK between GPs were not signif. different except Cmax for acid metabolite; diagrams, tables
Metabolite (Pharmacological Data)
modafinil acid [Reaxys RN: 6650982] ; Modafinil sulfone [Reaxys RN: 9199801]
Reference
Hellriegel, Edward T.; Arora, Sanjay; Nelson, Michael; Robertson Jr., Philmore
Journal of Clinical Pharmacology, 2002 , vol. 42, # 4 p. 450 - 460 Title/Abstract Full Text View citing articles Show Details
Effect (Pharmacological Data)
pharmacokinetics
Species or Test-System (Pharmacological Data)
human
Sex
male and female
Route of Application
peroral
Concentration
200 mg
(Pharmacological Data)
126 of 150
127 of 150
128 of 150
Kind of Dosing (Pharmacological Data)
200 mg title comp. (PROVIGIL(R)) was admin. on days 1-7 and 400 mg on days 8-28; title comp. (PROVIGIL(R)) was admin. as a single dose with 240 ml of water
Method (Pharmacological Data)
open-label, randomized, single period study; healthy subjects received title comp.; methylphenidate was administered on days 22-28; blood sampled at pre- and 24 h post dosing; plasma concentration of title comp. was determined by HPLC; PK calculated
Further Details (Pharmacological Data)
PK: pharmacokinetic parameters
Half-life Time (Pharmacological Data)
11 - 11.5 h
Results
mean trough plasma concentrations (μg/ml) of title comp. was ranged from 2.1 to 2.5; AUC0-24 (μg*h/ml), Cmax (μg/ml), tmax (h), t1/2 (h) of title comp., on day 21/day 28 were 143.8/139.4, 13.5/13.3, 1.9/2.1, 11.5/11.0, respectively; table, fig.
Reference
Hellriegel; Arora; Nelson; Robertson P.
Journal of Clinical Pharmacology, 2001 , vol. 41, # 8 p. 895 - 904 Title/Abstract Full Text View citing articles Show Details
Effect (Pharmacological Data)
pharmacokinetics
Species or Test-System (Pharmacological Data)
human
Sex
male and female
Route of Application
peroral
Concentration (Pharmacological Data)
200 mg
Kind of Dosing (Pharmacological Data)
200 mg title comp. (PROVIGIL(R)) was admin. on days 1-7 and 400 mg on days 8-28; title comp. (PROVIGIL(R)) was admin. as a single dose with 240 ml of water
Method (Pharmacological Data)
open-label, randomized, single period study; healthy subjects received title comp.; blood sampled at pre- and 24 h post dosing; plasma concentration of title comp. was determined by HPLC; pharmacokinetic parameters calculated
Half-life Time (Pharmacological Data)
12.6 - 14.2 h
Results
mean trough plasma concentrations (μg/ml) of title comp. was ranged from 2.5 to 4.4; AUC0-24 (μg*h/ml), Cmax (μg/ml), tmax (h), t1/2 (h) of title comp., on day 21/day 28 were 151.8/147.7, 13.5/14.3, 2.1/2.3, 14.2/12.6, respectively; table, fig.
Reference
Hellriegel; Arora; Nelson; Robertson P.
Journal of Clinical Pharmacology, 2001 , vol. 41, # 8 p. 895 - 904 Title/Abstract Full Text View citing articles Show Details
Effect (Pharmacological Data)
biotransformation
Species or Test-System (Pharmacological Data)
human
Sex
male and female
Route of Application
peroral
Concentration (Pharmacological Data)
200 mg
Kind of Dosing (Pharmacological Data)
200 mg title comp. (PROVIGIL(R)) was admin. on days 1-7 and 400 mg on days 8-28; title comp. (PROVIGIL(R)) was admin. as a single dose with 240 ml of water
Method (Pharmacological Data)
open-label, randomized, single period study; healthy subjects received title comp.; blood sampled at pre- and 24 h post dosing; plasma concentration of title comp. metabolites were determined by HPLC; pharmacokinetic parameters calculated
Further Details (Pharmacological Data)
title comp. metabolites: title comp. acid and title comp. sulfone
Results
AUC0-24, Cmax and tmax of title comp. acid/title comp. sulfone on day 21 were 49.1/138.9 μg*h/ml, 4.8/7.1 μg/ml and 2.9/10.3 h, respectively; table, fig.
Metabolite (Pharmacological Data)
modafinil acid [Reaxys RN: 6650982] ; Modafinil sulfone [Reaxys RN: 9199801]
Reference
Hellriegel; Arora; Nelson; Robertson P.
Journal of Clinical Pharmacology, 2001 , vol. 41, # 8 p. 895 - 904 Title/Abstract Full Text View citing articles Show Details
Effect (Pharmacological Data)
adverse effect
Species or Test-System (Pharmacological Data)
human
Sex
male and female
129 of 150
130 of 150
131 of 150
Route of Application
peroral
Concentration (Pharmacological Data)
200 mg
Kind of Dosing (Pharmacological Data)
200 mg title comp. (PROVIGIL(R)) was admin. on days 1-7 and 400 mg on days 8-28; title comp. (PROVIGIL(R)) was admin. as a single dose with 240 ml of water
Method (Pharmacological Data)
open-label, randomized, single period study; healthy subjects were treated with title comp.; adverse events were observed
Results
adverse events were observed in 47 and 77 percent of subjects administered with 200 and 400 mg title comp., respectively; most commonly reported adverse event was headache (69 percent of subjects); tables
Reference
Hellriegel; Arora; Nelson; Robertson P.
Journal of Clinical Pharmacology, 2001 , vol. 41, # 8 p. 895 - 904 Title/Abstract Full Text View citing articles Show Details
Effect (Pharmacological Data)
pharmacokinetics
Species or Test-System (Pharmacological Data)
human
Sex
male
Route of Application
peroral
Concentration (Pharmacological Data)
200 - 800 mg
Kind of Dosing (Pharmacological Data)
200, 400, 600 or 800 mg once daily for 7 d
Method (Pharmacological Data)
single-center, randomized, double-blind, placebo-controlled, ascending-dose trial in normal, healthy volunteers; levels of title comp., its l and d enantiomers, and metabolites in blood and urine (HPLC); Cmax. Tmax, AUC, VD, OC, PC and RC
Further Details (Pharmacological Data)
safety and tolerability determined; oral, plasma and renal clearance (OC, PC and RC, resp.); VD = volume of distribution
Half-life Time (Pharmacological Data)
Ca. 15 h
Results
title comp. had a rapid oral absorption rate; eliminated primarily by metabolism with dose- and time-independent pharmacokinetics; d-enantiomer eliminated 3-fold faster than l; 200-600 mg generally well tolerated; PC ca. 50 ml/min, VD ca. 0.8 l/kg
Reference
Wong, Y. Nancy; Simcoe, Donna; Hartman, Linda N.; Laughton, Watson B.; King, S. Peter; McCormick, George C.; Grebow, Peter E.
Journal of Clinical Pharmacology, 1999 , vol. 39, # 1 p. 30 - 40 Title/Abstract Full Text View citing articles Show Details
Effect (Pharmacological Data)
biotransformation
Species or Test-System (Pharmacological Data)
human
Sex
male
Route of Application
peroral
Concentration (Pharmacological Data)
200 - 800 mg
Kind of Dosing (Pharmacological Data)
200, 400, 600 or 800 mg once daily for 7 d
Method (Pharmacological Data)
single-center, randomized, double-blind, placebo-controlled, ascending-dose trial in normal, healthy volunteers; levels of title comp., its l and d enantiomers, and metabolites in blood and urine (HPLC)
Half-life Time (Pharmacological Data)
Ca. 15 h
Results
title comp. eliminated primarily by metabolism
Metabolite (Pharmacological Data)
modafinil acid [Reaxys RN: 6650982] ; Modafinil sulfone [Reaxys RN: 9199801]
Reference
Wong, Y. Nancy; Simcoe, Donna; Hartman, Linda N.; Laughton, Watson B.; King, S. Peter; McCormick, George C.; Grebow, Peter E.
Journal of Clinical Pharmacology, 1999 , vol. 39, # 1 p. 30 - 40 Title/Abstract Full Text View citing articles Show Details
Effect (Pharmacological Data)
cardiotonic
Species or Test-System (Pharmacological Data)
human
Sex
male
132 of 150
133 of 150
134 of 150
Route of Application
peroral
Kind of Dosing (Pharmacological Data)
200 mg in the morning and 100 mg at midday for 2 d
Method (Pharmacological Data)
systolic/diastolic blood pressure (SBP/DBP) and HR measured before and for up to 24 h after 1-st title comp. dose (including vigilance, psychometry, ergometry, total daytime, NREM/REM, total sleep) by continuous intraarterial blood pressure monitoring
Further Details (Pharmacological Data)
26 healthy men aged 20 - 60 with mild-moderate obstructive sleep apnea; HR: heart rate; NREM/REM: nonrapid/rapid eye movement, resp.; time-weighted mean arterial pressure (MAP), MAP values and heart rate for different periods calculated; placebo control
Results
title comp. had no significant effect on time-weighted MAP, MAP and HR at nocturnal sleep and under resting conditions in daytime, caused significant increase in SBP at ergometric and psychometric tests and in DBP at ergometric test (table, figure)
Reference
Heitmann, Joerg; Cassel, Werner; Grote, Ludger; Bickel, Ulrich; Hartlaub, Udo; Penzel, Thomas; Peter, Joerg Hermann
Clinical Pharmacology and Therapeutics, 1999 , vol. 65, # 3 p. 328 - 335 Title/Abstract Full Text View citing articles Show Details
Effect (Pharmacological Data)
psychotonic
Species or Test-System (Pharmacological Data)
human
Sex
male
Route of Application
peroral
Kind of Dosing (Pharmacological Data)
200 mg in the morning and 100 mg at midday
Method (Pharmacological Data)
daytime sleepiness determined by Multiple Sleep Latency Test (MSLT) and vigilance test performed; sleep latency for MSLT and reaction time for vigilance test measured
Further Details (Pharmacological Data)
26 healthy subjects aged 20 - 60 with mild to moderate obstructive sleep apnea; placebo control
Results
title comp. significantly shortened mean reaction time for vigilance test (to 1.23 s vs. control 1.46 s, resp.), significantly prolonged mean sleep latency (to 14.71 min vs. control 9.09 min), improving both from clear pathologic to ca. normal values
Reference
Heitmann, Joerg; Cassel, Werner; Grote, Ludger; Bickel, Ulrich; Hartlaub, Udo; Penzel, Thomas; Peter, Joerg Hermann
Clinical Pharmacology and Therapeutics, 1999 , vol. 65, # 3 p. 328 - 335 Title/Abstract Full Text View citing articles Show Details
Effect (Pharmacological Data)
breath stimulant
Species or Test-System (Pharmacological Data)
human
Sex
male
Route of Application
peroral
Kind of Dosing (Pharmacological Data)
200 mg in the morning and 100 mg at midday for 2 d
Method (Pharmacological Data)
respiration monitored by thermistor (oronasal airflow), thoracic and abdominal bands (uncalibrated inductive respiratory plethysmography), and oxygen saturation (pulse oximetry)
Further Details (Pharmacological Data)
26 healthy subjects aged 20 - 60 with mild to moderate obstructive sleep apnea; respiratory disturbance index (number of apneas and hypopneas) calculated; placebo control
Results
title comp. insignificantly decreased respiratory disturbance index to 32.5 events/h vs. 33.9 events/h in control
Reference
Heitmann, Joerg; Cassel, Werner; Grote, Ludger; Bickel, Ulrich; Hartlaub, Udo; Penzel, Thomas; Peter, Joerg Hermann
Clinical Pharmacology and Therapeutics, 1999 , vol. 65, # 3 p. 328 - 335 Title/Abstract Full Text View citing articles Show Details
Effect (Pharmacological Data)
toxicity
Species or Test-System (Pharmacological Data)
human
Sex
male
Route of Application
peroral
Kind of Dosing (Pharmacological Data)
200 mg given in the morning and 100 mg at midday for 2 d
Method (Pharmacological Data)
subjects were assessed for adverse events; routine laboratory tests performed
Further Details (Pharmacological Data)
26 healthy subjects aged 20 - 60 with mild to moderate obstructive sleep apnea; placebo control
Results
title comp. caused total of 7 adverse events; one adverse event (supraventricular tachycardia) was serious; routine laboratory tests showed no clinically relevant
changes
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Reference
Heitmann, Joerg; Cassel, Werner; Grote, Ludger; Bickel, Ulrich; Hartlaub, Udo; Penzel, Thomas; Peter, Joerg Hermann
Clinical Pharmacology and Therapeutics, 1999 , vol. 65, # 3 p. 328 - 335 Title/Abstract Full Text View citing articles Show Details
Effect (Pharmacological Data)
pharmacokinetics
Species or Test-System (Pharmacological Data)
human
Sex
male and female
Route of Application
peroral
Concentration (Pharmacological Data)
200 mg
Kind of Dosing (Pharmacological Data)
two 100 mg tablets of title comp. administered with 240 mL of water
Method (Pharmacological Data)
blood and urine samples collected at timed intervals up to 72 h postdose; title comp. and its metabolites conc. determined in plasma and urine by HPLC
Further Details (Pharmacological Data)
young males and females (26-29 years) and elderly males (63 years) were treated; Cmax: maximum plasma conc.; tmax: time to Cmax; CL/F: plasma oral clearance; V/D: apparent volume of distribution; CLrenal: renal clearance
Half-life Time (Pharmacological Data)
10.5 - 14.4 h
Results
title comp. Cmax = 5.20, 4.81, 4.21 μg/ml, tmax = 1.7, 2.0, 1.7 h, AUC = 61.3, 67.7, 57.0 μg*h/ml and CL/F = 0.88, 0.63, 0.72 ml/min/kg for young females, elderly males and young males, respectively; no difference in CLrenal and V/F
Reference
Wong, Y. Nancy; King, S. Peter; Simcoe, Donna; Gorman, Steve; Laughton, Watson; McCormick, George C.; Grebow, Peter
Journal of Clinical Pharmacology, 1999 , vol. 39, # 3 p. 281 - 288 Title/Abstract Full Text View citing articles Show Details
Effect (Pharmacological Data)
pharmacokinetics
Species or Test-System (Pharmacological Data)
human
Sex
male and female
Route of Application
peroral
Concentration (Pharmacological Data)
200 mg
Kind of Dosing (Pharmacological Data)
two 100 mg tablets of title comp. administered with 240 mL of water
Method (Pharmacological Data)
blood and urine samples collected at timed intervals up to 72 h postdose; title comp. and its metabolites conc. determined in plasma and urine by HPLC
Further Details (Pharmacological Data)
young males and females (26-29 years) and elderly males (63 years) were treated; MRTpo: mean residence time
Results
title comp. exhibited stereospecific pharmacokinetics: d-/l-title comp. enantiomers MRTpo (hr) values of 5.72/16.8, 4.83/14.2, 5.90/20.5 for young males, young females and elderly males, respectively (table)
Comment (Pharmacological Data)
Further metabolite(s)
Reference
Wong, Y. Nancy; King, S. Peter; Simcoe, Donna; Gorman, Steve; Laughton, Watson; McCormick, George C.; Grebow, Peter
Journal of Clinical Pharmacology, 1999 , vol. 39, # 3 p. 281 - 288 Title/Abstract Full Text View citing articles Show Details
Effect (Pharmacological Data)
biotransformation
Species or Test-System (Pharmacological Data)
human
Sex
male and female
Route of Application
peroral
Concentration (Pharmacological Data)
200 mg
Kind of Dosing (Pharmacological Data)
two 100 mg tablets of title comp. administered with 240 mL of water
Method (Pharmacological Data)
blood and urine samples collected at timed intervals up to 72 h postdose; title comp. and its metabolites conc. determined in plasma and urine by HPLC
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Further Details (Pharmacological Data)
young males and females (26-29 years) and elderly males (63 years) were treated
Results
modafinil acid was the major urinary metabolite; percent of title comp. dose excreted in urine as modafinil acid = 35, 60 , 51 for young females, elderly males and young males, respectively
Metabolite (Pharmacological Data)
modafinil acid [Reaxys RN: 6650982] ; Modafinil sulfone [Reaxys RN: 9199801]
Comment (Pharmacological Data)
Further metabolite(s)
Reference
Wong, Y. Nancy; King, S. Peter; Simcoe, Donna; Gorman, Steve; Laughton, Watson; McCormick, George C.; Grebow, Peter
Journal of Clinical Pharmacology, 1999 , vol. 39, # 3 p. 281 - 288 Title/Abstract Full Text View citing articles Show Details
Effect (Pharmacological Data)
biotransformation
Species or Test-System (Pharmacological Data)
human
Sex
male and female
Route of Application
peroral
Concentration (Pharmacological Data)
200 mg
Kind of Dosing (Pharmacological Data)
two 100 mg tablets of title comp. administered with 240 mL of water
Method (Pharmacological Data)
blood and urine samples collected at timed intervals up to 72 h postdose; title comp. and its metabolites conc. determined in plasma and urine by HPLC
Further Details (Pharmacological Data)
young males and females (26-29 years) and elderly males (63 years) were treated
Metabolite (Pharmacological Data)
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d-modafinil [Reaxys RN: 10016759] ; l-modafinil [Reaxys RN: 10018841]
Reference
Wong, Y. Nancy; King, S. Peter; Simcoe, Donna; Gorman, Steve; Laughton, Watson; McCormick, George C.; Grebow, Peter
Journal of Clinical Pharmacology, 1999 , vol. 39, # 3 p. 281 - 288 Title/Abstract Full Text View citing articles Show Details
Effect (Pharmacological Data)
pharmacokinetics; modulation of
Species or Test-System (Pharmacological Data)
human
Sex
male
Route of Application
peroral
Concentration (Pharmacological Data)
200 mg
Method (Pharmacological Data)
title comp. given in combination with dextroamphetamine (10 mg); blood samples collected up to 48 h; plasma dextroamphetamine conc. measured by LC/MS/MS, its pharmacokinetic parameters calculated
Further Details (Pharmacological Data)
control: dextroamphetamine alone
Comment (Pharmacological Data)
No effect
Reference
Wong, Y. Nancy; Wang, Lixia; Hartman, Linda; Simcoe, Donna; Chen, Yusong; Laughton, Watson; Eldon, Richard; Markland, Colin; Grebow, Peter
Journal of Clinical Pharmacology, 1998 , vol. 38, # 10 p. 971 - 978 Title/Abstract Full Text View citing articles Show Details
Effect (Pharmacological Data)
pharmacokinetics
Species or Test-System (Pharmacological Data)
human
Sex
male
Route of Application
peroral
Concentration (Pharmacological Data)
200 mg
Method (Pharmacological Data)
title comp. administered, blood samples collected up to 48 h; plasma title comp. and metabolites conc. measured by HPLC, pharmacokinetic parameters calculated
Further Details (Pharmacological Data)
AUC: area under serum conc.-time curve; Cmax: maximum serum conc.; tmax: time to Cmax; Cl/F: apparent oral clearance
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Half-life Time (Pharmacological Data)
11.3 h
Results
Cmax = 4.83 μg/ml; tmax = 1.8 h; AUC = 60.1 μg*h/ml; Cl/F = 0.81 ml/min/kg (table)
Metabolite (Pharmacological Data)
modafinil acid [Reaxys RN: 6650982] ; Modafinil sulfone [Reaxys RN: 9199801]
Reference
Wong, Y. Nancy; Wang, Lixia; Hartman, Linda; Simcoe, Donna; Chen, Yusong; Laughton, Watson; Eldon, Richard; Markland, Colin; Grebow, Peter
Journal of Clinical Pharmacology, 1998 , vol. 38, # 10 p. 971 - 978 Title/Abstract Full Text View citing articles Show Details
Effect (Pharmacological Data)
drug interaction
Species or Test-System (Pharmacological Data)
human
Sex
male
Route of Application
peroral
Concentration (Pharmacological Data)
200 mg
Kind of Dosing (Pharmacological Data)
single dose, two 100-mg tablets
Method (Pharmacological Data)
pharmacokinetic interaction with 40 mg threo-methylphenidate studied in 21 healthy men (27.6 +/- 6.2 years, 74.7 +/- 9.0 kg); title comp. and metabolites determined in plasma by HPLC from blood sampled up to 48 h postdose; adverse events recorded
Further Details (Pharmacological Data)
open-label 3 * 3 Latin square, randomized, single-dose, crossover study; threo-methylphenidate enantiomers determined in plasma by LC/MS/MS from blood sampled up to 18 h postdose
Half-life Time (Pharmacological Data)
12.3 h
Results
significant increases in tmax for title comp. (from 0.5-3.0 h to 1.0-6.0 h) and modafinil acid (from 1.0-4.0 h to 2.0-6.0 h); no effect on pharmacokinetic parameters of threo-methylphenidate enantiomers; no serious adverse events; graphs, tables
Metabolite (Pharmacological Data)
modafinil acid [Reaxys RN: 6650982] ; Modafinil sulfone [Reaxys RN: 9199801]
Reference
Wong, Y. Nancy; King, S. Peter; Laughton, Watson B.; McCormick, George C.; Grebow, Peter E.
Journal of Clinical Pharmacology, 1998 , vol. 38, # 3 p. 276 - 282 Title/Abstract Full Text View citing articles Show Details
Effect (Pharmacological Data)
pharmacokinetics
Species or Test-System (Pharmacological Data)
human
Sex
male
Route of Application
peroral
Concentration (Pharmacological Data)
200 mg
Kind of Dosing (Pharmacological Data)
single dose, two 100-mg tablets
Method (Pharmacological Data)
pharmacokinetics studied in 21 healthy men (27.6 +/- 6.2 years, 74.7 +/- 9.0 kg); title comp. and metabolites determined in plasma by HPLC from blood sampled up to 48 h postdose
Further Details (Pharmacological Data)
open-label study
Half-life Time (Pharmacological Data)
12.2 h
Results
parameters for title comp. / modafinil acid: Cmax 4.10 / 1.91 μg/ml, tmax 2.0 (0.5-3.0) / 3.0(1.0-4.0) h, AUC0-infinity 56.9 / 22.6 γ*h/ml, total systemic plasma clearance of title comp. 62.0 ml/min; graphs, table
Metabolite (Pharmacological Data)
modafinil acid [Reaxys RN: 6650982] ; Modafinil sulfone [Reaxys RN: 9199801]
Reference
Wong, Y. Nancy; King, S. Peter; Laughton, Watson B.; McCormick, George C.; Grebow, Peter E.
Journal of Clinical Pharmacology, 1998 , vol. 38, # 3 p. 276 - 282 Title/Abstract Full Text View citing articles Show Details
Effect (Pharmacological Data)
antisedative
Species or Test-System (Pharmacological Data)
Wistar rat
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Sex
male
Route of Application
intraperitoneal
Concentration (Pharmacological Data)
30 - 300 mg/kg
Kind of Dosing (Pharmacological Data)
title comp. suspended in sterile 0.25 percent methylcellulose
Method (Pharmacological Data)
rats treated with title comp. 5 h after lights on; LMA (every 10 s) and Tb (every min) monitored via i.p. telemetry; sleep-wakefulness determined by EEG every 10 s
Further Details (Pharmacological Data)
control: vehicle; reference comp.: METH (methamphetamine); LMA: locomotor activity; Tb: body temperature; EEG: electroencephalogram
Results
during the first 3 h posttreatment, title comp. dose-dependently increased wake time (diagram); title comp. did not produce rebound hypersomnolence and increased LMA less than METH
Reference
Edgar, Dale M.; Seidel, Wesley F.
Journal of Pharmacology and Experimental Therapeutics, 1997 , vol. 283, # 2 p. 757 - 769 Title/Abstract Full Text View citing articles Show Details
Effect (Pharmacological Data)
increase of dopamine release
Species or Test-System (Pharmacological Data)
Sprague-Dawley rat
Sex
male
Route of Application
subcutaneous
Concentration (Pharmacological Data)
30 - 300 mg/kg
Kind of Dosing (Pharmacological Data)
doses in 0.5 percent arabic gum solution
Method (Pharmacological Data)
rat weight 300-350 g; 5-7 rats/group; halothane-anaesthesia; microdialysis probe implantation into intermediate nucleus accumbens; title comp. injection; perfusate collected every 20 min for 120 min; reverse-phase HPLC-ED
Further Details (Pharmacological Data)
time - dopamine release curve
Results
title comp. dose-dependently increased accumbens dopamine release, reaching peak effect at 40 min after injection from 100 to 300 mg/kg, but not at 30 mg/kg (diagram given)
Reference
Ferraro, Luca; Tanganelli, Sergio; O'Connor, William Thomas; Antonelli, Tiziana; Rambert, Francis; Fuxe, Kjell
European Journal of Pharmacology, 1996 , vol. 306, # 1-3 p. 33 - 39 Title/Abstract Full Text View citing articles Show Details
Effect (Pharmacological Data)
decrease of GABA release
Species or Test-System (Pharmacological Data)
Sprague-Dawley rat
Sex
male
Route of Application
subcutaneous
Concentration (Pharmacological Data)
30 - 300 mg/kg
Kind of Dosing (Pharmacological Data)
doses in 0.5 percent arabic gum solution
Method (Pharmacological Data)
rat weight 300-350 g; 7 rats/group; halothane-anaesthesia; microdialysis probe implantation into intermediate nucleus accumbens; title comp. injection; perfusate collected every 20 min for 120 min; reverse-phase HPLC-ED
Further Details (Pharmacological Data)
time - γ-aminobutyric acid (GABA) release curve
Results
title comp. dose-dependently decreased accumbens GABA release from 100 to 300 mg/kg, but not at 30 mg/kg (diagram given)
Reference
Ferraro, Luca; Tanganelli, Sergio; O'Connor, William Thomas; Antonelli, Tiziana; Rambert, Francis; Fuxe, Kjell
European Journal of Pharmacology, 1996 , vol. 306, # 1-3 p. 33 - 39 Title/Abstract Full Text View citing articles Show Details
Effect (Pharmacological Data)
antagonist
Species or Test-System (Pharmacological Data)
guinea pig
Sex
male and female
Route of Application
subcutaneous
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Concentration (Pharmacological Data)
30 mg/kg
Method (Pharmacological Data)
γ-aminobutyric acid outfow (AAO, mass-fragmentography) from parietal cortex with or without pretreatment with 125 μg i.c.v. 5,7-dihydroxytriptamine (5,7-DHT, 7 d befor exp.); dopamine (D) and noradrenaline (N) levels in the cortex (HPLC)
Results
rapid and long-lasting inhibition of AAO; 5,7-DHT pretreatment caused slight increase, instead of decrease, in AAO; D not affected; N enhanced significantly
Reference
Tanganelli; de la Mora; Ferraro; Mendez-Franco; Beani; Rambert; Fuxe
European Journal of Pharmacology, 1995 , vol. 273, # 1-2 p. 63 - 71 Title/Abstract Full Text View citing articles Show Details
Effect (Pharmacological Data)
antagonist
Species or Test-System (Pharmacological Data)
Wistar rat
Sex
male
Route of Application
subcutaneous
Concentration (Pharmacological Data)
30 mg/kg
Method (Pharmacological Data)
γ-aminobutyric acid outfow (AAO) from parietal cortex (mass-fragmentography)
Results
rapid and long-lasting inhibition of AAO
Reference
Tanganelli; de la Mora; Ferraro; Mendez-Franco; Beani; Rambert; Fuxe
European Journal of Pharmacology, 1995 , vol. 273, # 1-2 p. 63 - 71 Title/Abstract Full Text View citing articles Show Details
Effect (Pharmacological Data)
antagonist
Species or Test-System (Pharmacological Data)
guinea pig
Sex
male and female
Route of Application
subcutaneous
Concentration (Pharmacological Data)
30 mg/kg/d
Exposure Period (Pharmacological Data)
8 d
Method (Pharmacological Data)
γ-aminobutyric acid outfow (AAO, mass-fragmentography) from parietal cortex with or without pretreatment with 125 μg i.c.v. 5,7-dihydroxytriptamine (5,7-DHT, 7 d befor exp.) or 35.8 ng/kg i.p. prazosin (P, 30 min befor admin. of title comp.)
Further Details (Pharmacological Data)
noradrenalin (N), 5-hydroxytriptamine (5-HT) and dopamine (D) levels (HPLC)
Results
significantly inhibited AAO; 5,7-DHT pretreatment caused consistent and prolonged enhancement in AAO; D not affected; N enhanced significantly; counter-acted 5,7DHT-induced reduction on 5-HT level; treatment with P completely prevented increase of AAO
Reference
Tanganelli; de la Mora; Ferraro; Mendez-Franco; Beani; Rambert; Fuxe
European Journal of Pharmacology, 1995 , vol. 273, # 1-2 p. 63 - 71 Title/Abstract Full Text View citing articles Show Details
Effect (Pharmacological Data)
agonist
Species or Test-System (Pharmacological Data)
Wistar rat brain
Sex
male
Concentration (Pharmacological Data)
1 - 1000 μmol/l
Method (Pharmacological Data)
brain slices of patogen-free rats incubated in Krebs-Ringer medium containing 1 μM <3H>-γ-aminobutyric acid (<3H>GABA); <3H>GABA uptake and release (scintillation spectrometry); glutamic acid decarboxylase activity
Comment (Pharmacological Data)
No effect
Reference
Tanganelli; de la Mora; Ferraro; Mendez-Franco; Beani; Rambert; Fuxe
European Journal of Pharmacology, 1995 , vol. 273, # 1-2 p. 63 - 71 Title/Abstract Full Text View citing articles Show Details
Comment (Pharmacological Data)
effect on sleep architecture, sleep and awakening quality in elderlies
Reference
Saletu; Frey; Krupka; Anderer; Grunberger; Barbanoj
Arzneimittel-Forschung/Drug Research, 1989 , vol. 39, # 10 p. 1268 - 1273 Title/Abstract Full Text View citing articles Show Details
Other Data Use (327) Use Pattern
Location
Reference
Pharmaceuticals
Page/Page column title page; 62-67
HSU, John
Patent: WO2017/15309 A1, 2017 ; Title/Abstract Full Text Show Details
acute pain in combination with analgesic
Page/Page column title page; 62-67
HSU, John
Patent: WO2017/15309 A1, 2017 ; Title/Abstract Full Text Show Details
acute pain in combination with antihistamine
Page/Page column title page; 62-67
HSU, John
Patent: WO2017/15309 A1, 2017 ; Title/Abstract Full Text Show Details
acute pain in combination with barbiturate
Page/Page column title page; 62-67
HSU, John
Patent: WO2017/15309 A1, 2017 ; Title/Abstract Full Text Show Details
acute pain in combination with benzodiazepine
Page/Page column title page; 62-67
HSU, John
Patent: WO2017/15309 A1, 2017 ; Title/Abstract Full Text Show Details
acute pain in combination with kappa receptor agonist
Page/Page column title page; 62-67
HSU, John
Patent: WO2017/15309 A1, 2017 ; Title/Abstract Full Text Show Details
acute pain in combination with non-steroidal anti-inflammatory agent
Page/Page column title page; 62-67
HSU, John
Patent: WO2017/15309 A1, 2017 ; Title/Abstract Full Text Show Details
acute pain in combination with opioid mu receptor agonist
Page/Page column title page; 62-67
HSU, John
Patent: WO2017/15309 A1, 2017 ; Title/Abstract Full Text Show Details
acute pain in combination with opioid receptor agonist
Page/Page column title page; 62-67
HSU, John
Patent: WO2017/15309 A1, 2017 ; Title/Abstract Full Text Show Details
anethesia in combination with analgesic
Page/Page column title page; 62-67
HSU, John
Patent: WO2017/15309 A1, 2017 ; Title/Abstract Full Text Show Details
anethesia in combination with antihistamine
Page/Page column title page; 62-67
HSU, John
Patent: WO2017/15309 A1, 2017 ; Title/Abstract Full Text Show Details
anethesia in combination with barbiturate
Page/Page column title page; 62-67
HSU, John
Patent: WO2017/15309 A1, 2017 ; Title/Abstract Full Text Show Details
anethesia in combination with benzodiazepine
Page/Page column title page; 62-67
HSU, John
Patent: WO2017/15309 A1, 2017 ; Title/Abstract Full Text Show Details
anethesia in combination with kappa receptor agonist
Page/Page column title page; 62-67
HSU, John
Patent: WO2017/15309 A1, 2017 ; Title/Abstract Full Text Show Details
anethesia in combination with non-steroidal anti-inflammatory agent
HSU, John
Patent: WO2017/15309 A1, 2017 ;
Page/Page column title page; 62-67
Title/Abstract Full Text Show Details
anethesia in combination with opioid mu receptor agonist
HSU, John
Patent: WO2017/15309 A1, 2017 ;
Page/Page column title page; 62-67
Title/Abstract Full Text Show Details
anethesia in combination with opioid receptor agonist
HSU, John
Patent: WO2017/15309 A1, 2017 ;
Page/Page column title page; 62-67
Title/Abstract Full Text Show Details
chronic pain in combination with analgesic
HSU, John
Patent: WO2017/15309 A1, 2017 ;
Page/Page column title page; 62-67
Title/Abstract Full Text Show Details
chronic pain in combination with antihistamine
HSU, John
Patent: WO2017/15309 A1, 2017 ;
Page/Page column title page; 62-67
Title/Abstract Full Text Show Details
chronic pain in combination with barbiturate
HSU, John
Patent: WO2017/15309 A1, 2017 ;
Page/Page column title page; 62-67
Title/Abstract Full Text Show Details
Use Pattern
Location
Reference
chronic pain in combination with benzodiazepine
Page/Page column title page; 62-67
HSU, John
Patent: WO2017/15309 A1, 2017 ;
Page/Page column title page; 62-67
HSU, John
Patent: WO2017/15309 A1, 2017 ;
Page/Page column title page; 62-67
HSU, John
Patent: WO2017/15309 A1, 2017 ;
Page/Page column title page; 62-67
HSU, John
Patent: WO2017/15309 A1, 2017 ;
Page/Page column title page; 62-67
HSU, John
Patent: WO2017/15309 A1, 2017 ;
Page/Page column title page; 62-67
HSU, John
Patent: WO2017/15309 A1, 2017 ;
Page/Page column title page; 62-67
HSU, John
Patent: WO2017/15309 A1, 2017 ;
Page/Page column title page; 62-67
HSU, John
Patent: WO2017/15309 A1, 2017 ;
Page/Page column title page; 62-67
HSU, John
Patent: WO2017/15309 A1, 2017 ;
chronic pain in combination with kappa receptor agonist
chronic pain in combination with non-steroidal anti-inflammatory agent
chronic pain in combination with opioid mu receptor agonist
chronic pain in combination with opioid receptor agonist
for treating drug abuse in combination with analgesic
for treating drug abuse in combination with antihistamine
for treating drug abuse in combination with barbiturate
for treating drug abuse in combination with benzodiazepine
Title/Abstract Full Text Show Details
Title/Abstract Full Text Show Details
Title/Abstract Full Text Show Details
Title/Abstract Full Text Show Details
Title/Abstract Full Text Show Details
Title/Abstract Full Text Show Details
Title/Abstract Full Text Show Details
Title/Abstract Full Text Show Details
Title/Abstract Full Text Show Details
for treating drug abuse in combination with kappa receptor agonist
for treating drug abuse in combination with non-steroidal anti-inflammatory agent
for treating drug abuse in combination with opioid mu receptor agonist
for treating drug abuse in combination with opioid receptor agonist
obstructive sleep apnea in combination with analgesic
obstructive sleep apnea in combination with antihistamine
obstructive sleep apnea in combination with barbiturate
obstructive sleep apnea in combination with benzodiazepine
obstructive sleep apnea in combination with kappa receptor
obstructive sleep apnea in combination with non-steroidal anti-inflammatory agent
obstructive sleep apnea in combination with opioid mu receptor agonist
obstructive sleep apnea in combination with opioid receptor agonist
preventing or deterring abuse of the therapeutic agent in combination with analgesic
preventing or deterring abuse of the therapeutic agent in combination with antihistamine
preventing or deterring abuse of the therapeutic agent in combination with barbiturate
Page/Page column title page; 62-67
HSU, John
Patent: WO2017/15309 A1, 2017 ;
Page/Page column title page; 62-67
HSU, John
Patent: WO2017/15309 A1, 2017 ;
Page/Page column title page; 62-67
HSU, John
Patent: WO2017/15309 A1, 2017 ;
Page/Page column title page; 62-67
HSU, John
Patent: WO2017/15309 A1, 2017 ;
Page/Page column title page; 62-67
HSU, John
Patent: WO2017/15309 A1, 2017 ;
Page/Page column title page; 62-67
HSU, John
Patent: WO2017/15309 A1, 2017 ;
Page/Page column title page; 62-67
HSU, John
Patent: WO2017/15309 A1, 2017 ;
Page/Page column title page; 62-67
HSU, John
Patent: WO2017/15309 A1, 2017 ;
Page/Page column title page; 62-67
HSU, John
Patent: WO2017/15309 A1, 2017 ;
Page/Page column title page; 62-67
HSU, John
Patent: WO2017/15309 A1, 2017 ;
Page/Page column title page; 62-67
HSU, John
Patent: WO2017/15309 A1, 2017 ;
Page/Page column title page; 62-67
HSU, John
Patent: WO2017/15309 A1, 2017 ;
Page/Page column title page; 62-67
HSU, John
Patent: WO2017/15309 A1, 2017 ;
Page/Page column title page; 62-67
HSU, John
Patent: WO2017/15309 A1, 2017 ;
Page/Page column title page; 62-67
HSU, John
Patent: WO2017/15309 A1, 2017 ;
Title/Abstract Full Text Show Details
Title/Abstract Full Text Show Details
Title/Abstract Full Text Show Details
Title/Abstract Full Text Show Details
Title/Abstract Full Text Show Details
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Title/Abstract Full Text Show Details
preventing or deterring abuse of the therapeutic agent in combination with benzodiazepine
preventing or deterring abuse of the therapeutic agent in combination with kappa receptor agonist
preventing or deterring abuse of the therapeutic agent in combination with non-steroidal anti-inflammatory agent
preventing or deterring abuse of the therapeutic agent in combination with opioid mu receptor agonist
preventing or deterring abuse of the therapeutic agent in combination with opioid receptor agonist
sleep apnea in combination with analgesic
sleep apnea in combination with antihistamine
sleep apnea in combination with barbiturate
sleep apnea in combination with benzodiazepine
sleep apnea in combination with kappa receptor agonist
sleep apnea in combination with non-steroidal anti-inflammatory agent
sleep apnea in combination with opioid mu receptor agonist
sleep apnea in combination with opioid receptor agonist
Pharmaceuticals
abuse deterrent in combination with an abuse deterrent active
Kleine-Levin syndrome
Page/Page column title page; 62-67
HSU, John
Patent: WO2017/15309 A1, 2017 ;
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HSU, John
Patent: WO2017/15309 A1, 2017 ;
Page/Page column title page; 62-67
HSU, John
Patent: WO2017/15309 A1, 2017 ;
Page/Page column title page; 62-67
HSU, John
Patent: WO2017/15309 A1, 2017 ;
Page/Page column title page; 62-67
HSU, John
Patent: WO2017/15309 A1, 2017 ;
Page/Page column title page; 62-67
HSU, John
Patent: WO2017/15309 A1, 2017 ;
Page/Page column title page; 62-67
HSU, John
Patent: WO2017/15309 A1, 2017 ;
Page/Page column title page; 62-67
HSU, John
Patent: WO2017/15309 A1, 2017 ;
Page/Page column title page; 62-67
HSU, John
Patent: WO2017/15309 A1, 2017 ;
Page/Page column title page; 62-67
HSU, John
Patent: WO2017/15309 A1, 2017 ;
Page/Page column title page; 62-67
HSU, John
Patent: WO2017/15309 A1, 2017 ;
Page/Page column title page; 62-67
HSU, John
Patent: WO2017/15309 A1, 2017 ;
Page/Page column title page; 62-67
HSU, John
Patent: WO2017/15309 A1, 2017 ;
Page/Page column title page; 32-34
SELA, Yoram; LAMENSDORF, Itschak
Patent: WO2016/181218 A1, 2016 ;
Page/Page column title page; 32-34
Page/Page column 41-42
Title/Abstract Full Text Show Details
Title/Abstract Full Text Show Details
Title/Abstract Full Text Show Details
Title/Abstract Full Text Show Details
Title/Abstract Full Text Show Details
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Title/Abstract Full Text Show Details
Title/Abstract Full Text Show Details
Title/Abstract Full Text Show Details
SELA, Yoram; LAMENSDORF, Itschak
Patent: WO2016/181218 A1, 2016 ; Title/Abstract Full Text Show Details
COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES; MOUTHON, Franck;
CHARVERIAT, Mathieu
Patent: WO2015/11246 A1, 2015 ; Title/Abstract Full Text Show Details
Parkinson disease
Page/Page column 41-42
COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES; MOUTHON, Franck; CHARVERIAT, Mathieu
Patent: WO2015/11246 A1, 2015 ; Title/Abstract Full Text Show Details
Periodic Lim Movement Disorders (PLMD)
Page/Page column 41-42
COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES; MOUTHON, Franck; CHARVERIAT, Mathieu
Patent: WO2015/11246 A1, 2015 ; Title/Abstract Full Text Show Details
Pharmaceuticals
Page/Page column 41-42
COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES; MOUTHON, Franck; CHARVERIAT, Mathieu
Patent: WO2015/11246 A1, 2015 ; Title/Abstract Full Text Show Details
alertness disorders
Page/Page column 41-42
COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES; MOUTHON, Franck; CHARVERIAT, Mathieu
Patent: WO2015/11246 A1, 2015 ; Title/Abstract Full Text Show Details
anxiety disorders
Page/Page column 41-42
COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES; MOUTHON, Franck; CHARVERIAT, Mathieu
Patent: WO2015/11246 A1, 2015 ; Title/Abstract Full Text Show Details
attention deficit hyperactivity disorder (ADHD)
Page/Page column 41-42
COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES; MOUTHON, Franck; CHARVERIAT, Mathieu
Patent: WO2015/11246 A1, 2015 ; Title/Abstract Full Text Show Details
attention disorders
Page/Page column 41-42
COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES; MOUTHON, Franck; CHARVERIAT, Mathieu
Patent: WO2015/11246 A1, 2015 ; Title/Abstract Full Text Show Details
bipolar disorder
Page/Page column 41-42
COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES; MOUTHON, Franck; CHARVERIAT, Mathieu
Patent: WO2015/11246 A1, 2015 ; Title/Abstract Full Text Show Details
breathing difficulty and fatigue, notably due to cancer, neurodegenerative disorders, menopause, traumatic brain injuries, viral infection or post-myelitis, or to fibromyalgia
Page/Page column 41-42
COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES; MOUTHON, Franck; CHARVERIAT, Mathieu
Patent: WO2015/11246 A1, 2015 ; Title/Abstract Full Text Show Details
cataplexy in narcoleptic patients
Page/Page column 41-42
COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES; MOUTHON, Franck; CHARVERIAT, Mathieu
Patent: WO2015/11246 A1, 2015 ; Title/Abstract Full Text Show Details
central sleep apnea
Page/Page column 41-42
COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES; MOUTHON, Franck; CHARVERIAT, Mathieu
Patent: WO2015/11246 A1, 2015 ;
Title/Abstract Full Text Show Details
chronic renal failure
Page/Page column 41-42
COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES; MOUTHON, Franck; CHARVERIAT, Mathieu
Patent: WO2015/11246 A1, 2015 ; Title/Abstract Full Text Show Details
circadian rhythm disorders
Page/Page column 41-42
COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES; MOUTHON, Franck; CHARVERIAT, Mathieu
Patent: WO2015/11246 A1, 2015 ; Title/Abstract Full Text Show Details
dementia
Page/Page column 41-42
COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES; MOUTHON, Franck; CHARVERIAT, Mathieu
Patent: WO2015/11246 A1, 2015 ; Title/Abstract Full Text Show Details
dependence or addiction (to games, drugs, alcohol, tobacco, etc.)
Page/Page column 41-42
COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES; MOUTHON, Franck; CHARVERIAT, Mathieu
Patent: WO2015/11246 A1, 2015 ; Title/Abstract Full Text Show Details
depression
Page/Page column 41-42
COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES; MOUTHON, Franck; CHARVERIAT, Mathieu
Patent: WO2015/11246 A1, 2015 ; Title/Abstract Full Text Show Details
disorders after sleep restriction or sleep deprivation
Page/Page column 41-42
COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES; MOUTHON, Franck; CHARVERIAT, Mathieu
Patent: WO2015/11246 A1, 2015 ; Title/Abstract Full Text Show Details
enhancing the memory
Page/Page column 41-42
COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES; MOUTHON, Franck; CHARVERIAT, Mathieu
Patent: WO2015/11246 A1, 2015 ; Title/Abstract Full Text Show Details
excessive daytime sleepiness (EDS)
Page/Page column 41-42
COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES; MOUTHON, Franck; CHARVERIAT, Mathieu
Patent: WO2015/11246 A1, 2015 ; Title/Abstract Full Text Show Details
fecal or urinary incontinence
Page/Page column 41-42
COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES; MOUTHON, Franck; CHARVERIAT, Mathieu
Patent: WO2015/11246 A1, 2015 ; Title/Abstract Full Text Show Details
hyperphagia
Page/Page column 41-42
COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES; MOUTHON, Franck; CHARVERIAT, Mathieu
Patent: WO2015/11246 A1, 2015 ; Title/Abstract Full Text Show Details
idiopathic hypersomnia
Page/Page column 41-42
COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES; MOUTHON, Franck; CHARVERIAT, Mathieu
Patent: WO2015/11246 A1, 2015 ; Title/Abstract Full Text Show Details
in combination with flecainide
Page/Page column 41-42
COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES; MOUTHON, Franck; CHARVERIAT, Mathieu
Patent: WO2015/11246 A1, 2015 ; Title/Abstract Full Text Show Details
insomnia
Page/Page column 41-42
COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES; MOUTHON, Franck; CHARVERIAT, Mathieu
Patent: WO2015/11246 A1, 2015 ; Title/Abstract Full Text Show Details
insufficient sleep time
Page/Page column 41-42
COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES; MOUTHON, Franck; CHARVERIAT, Mathieu
Patent: WO2015/11246 A1, 2015 ; Title/Abstract Full Text Show Details
jet-lag
Page/Page column 41-42
COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES; MOUTHON, Franck; CHARVERIAT, Mathieu
Patent: WO2015/11246 A1, 2015 ; Title/Abstract Full Text Show Details
liver failure
Page/Page column 41-42
COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES; MOUTHON, Franck; CHARVERIAT, Mathieu
Patent: WO2015/11246 A1, 2015 ; Title/Abstract Full Text Show Details
maintaining healthy subjects awake for long-lasting periods of time
Page/Page column 41-42
COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES; MOUTHON, Franck; CHARVERIAT, Mathieu
Patent: WO2015/11246 A1, 2015 ; Title/Abstract Full Text Show Details
malaise
Page/Page column 41-42
COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES; MOUTHON, Franck; CHARVERIAT, Mathieu
Patent: WO2015/11246 A1, 2015 ; Title/Abstract Full Text Show Details
manic episode
Page/Page column 41-42
COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES; MOUTHON, Franck; CHARVERIAT, Mathieu
Patent: WO2015/11246 A1, 2015 ; Title/Abstract Full Text Show Details
medication-induced somnolence (due to benzodiazepines, barbiturates, sleeping pills, antidepressants, anti-psychotics...)
Page/Page column 41-42
COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES; MOUTHON, Franck; CHARVERIAT, Mathieu
Patent: WO2015/11246 A1, 2015 ; Title/Abstract Full Text Show Details
mood disorders
Page/Page column 41-42
COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES; MOUTHON, Franck; CHARVERIAT, Mathieu
Patent: WO2015/11246 A1, 2015 ; Title/Abstract Full Text Show Details
multiple sclerosis
Page/Page column 41-42
COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES; MOUTHON, Franck; CHARVERIAT, Mathieu
Patent: WO2015/11246 A1, 2015 ; Title/Abstract Full Text Show Details
narcolepsy (with or without cataplexy)
Page/Page column 41-42
COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES; MOUTHON, Franck; CHARVERIAT, Mathieu
Patent: WO2015/11246 A1, 2015 ; Title/Abstract Full Text Show Details
neuromuscular disorders
Page/Page column 41-42
COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES; MOUTHON, Franck; CHARVERIAT, Mathieu
Patent: WO2015/11246 A1, 2015 ; Title/Abstract Full Text Show Details
obesity
Page/Page column 41-42
COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES; MOUTHON, Franck; CHARVERIAT, Mathieu
Patent: WO2015/11246 A1, 2015 ; Title/Abstract Full Text Show Details
obsessive-compulsive disorder
Page/Page column 41-42
COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES; MOUTHON, Franck; CHARVERIAT, Mathieu
Patent: WO2015/11246 A1, 2015 ; Title/Abstract Full Text Show Details
obstructive sleep apnea/hypopnea (SAHOS)
Page/Page column 41-42
COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES; MOUTHON, Franck; CHARVERIAT, Mathieu
Patent: WO2015/11246 A1, 2015 ; Title/Abstract Full Text Show Details
parasomnia
Page/Page column 41-42
COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES; MOUTHON, Franck; CHARVERIAT, Mathieu
Patent: WO2015/11246 A1, 2015 ; Title/Abstract Full Text Show Details
post-traumatic stress disorder (PTSD)
Page/Page column 41-42
COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES; MOUTHON, Franck; CHARVERIAT, Mathieu
Patent: WO2015/11246 A1, 2015 ; Title/Abstract Full Text Show Details
premature ejaculation
Page/Page column 41-42
COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES; MOUTHON, Franck; CHARVERIAT, Mathieu
Patent: WO2015/11246 A1, 2015 ; Title/Abstract Full Text Show Details
respiratory disorders
Page/Page column 41-42
COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES; MOUTHON, Franck; CHARVERIAT, Mathieu
Patent: WO2015/11246 A1, 2015 ; Title/Abstract Full Text Show Details
restless legs syndrome (RLS)
Page/Page column 41-42
COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES; MOUTHON, Franck; CHARVERIAT, Mathieu
Patent: WO2015/11246 A1, 2015 ; Title/Abstract Full Text Show Details
rheumatologic disorders
Page/Page column 41-42
COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES; MOUTHON, Franck; CHARVERIAT, Mathieu
Patent: WO2015/11246 A1, 2015 ; Title/Abstract Full Text Show Details
schizophrenia
Page/Page column 41-42
COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES; MOUTHON, Franck; CHARVERIAT, Mathieu
Patent: WO2015/11246 A1, 2015 ; Title/Abstract Full Text Show Details
senility
Page/Page column 41-42
COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES; MOUTHON, Franck; CHARVERIAT, Mathieu
Patent: WO2015/11246 A1, 2015 ; Title/Abstract Full Text Show Details
shift work sleep disorder
Page/Page column 41-42
COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES; MOUTHON, Franck; CHARVERIAT, Mathieu
Patent: WO2015/11246 A1, 2015 ; Title/Abstract Full Text Show Details
sleep disorders
Page/Page column 41-42
COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES; MOUTHON, Franck; CHARVERIAT, Mathieu
Patent: WO2015/11246 A1, 2015 ; Title/Abstract Full Text Show Details
sleepiness
Page/Page column 41-42
COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES; MOUTHON, Franck; CHARVERIAT, Mathieu
Patent: WO2015/11246 A1, 2015 ; Title/Abstract Full Text Show Details
stroke
Page/Page column 41-42
COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES; MOUTHON, Franck; CHARVERIAT, Mathieu
Patent: WO2015/11246 A1, 2015 ; Title/Abstract Full Text Show Details
structural brain disorders
Page/Page column 41-42
COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES; MOUTHON, Franck; CHARVERIAT, Mathieu
Patent: WO2015/11246 A1, 2015 ; Title/Abstract Full Text Show Details
tinnitus
Page/Page column 41-42
COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES; MOUTHON, Franck; CHARVERIAT, Mathieu
Patent: WO2015/11246 A1, 2015 ; Title/Abstract Full Text Show Details
psychostimulant
Ayala, William J.
Patent: US2005/31688 A1, 2005 ; Title/Abstract Full Text Show Details
H. LUNDBECK A/S Patent: WO2009/76961 A1, 2009 ; Title/Abstract Full Text Show Details
alpha1-adrenergic agonist
QUESTCOR PHARMACEUTICALS, INC.
Patent: WO2008/3093 A2, 2008 ; Title/Abstract Full Text Show Details
in combination with alpha2-adrenergic agonist or baclofen
QUESTCOR PHARMACEUTICALS, INC.
Patent: WO2008/3093 A2, 2008 ; Title/Abstract Full Text Show Details
somnolence
QUESTCOR PHARMACEUTICALS, INC.
Patent: WO2008/3093 A2, 2008 ; Title/Abstract Full Text Show Details
lethargy
QUESTCOR PHARMACEUTICALS, INC.
Patent: WO2008/3093 A2, 2008 ; Title/Abstract Full Text Show Details
dizziness
QUESTCOR PHARMACEUTICALS, INC.
Patent: WO2008/3093 A2, 2008 ; Title/Abstract Full Text Show Details
drowsiness
QUESTCOR PHARMACEUTICALS, INC.
Patent: WO2008/3093 A2, 2008 ; Title/Abstract Full Text Show Details
lightheadedness
QUESTCOR PHARMACEUTICALS, INC.
Patent: WO2008/3093 A2, 2008 ; Title/Abstract Full Text Show Details
increased weakness
QUESTCOR PHARMACEUTICALS, INC.
Patent: WO2008/3093 A2, 2008 ; Title/Abstract Full Text Show Details
confusion
QUESTCOR PHARMACEUTICALS, INC.
Patent: WO2008/3093 A2, 2008 ; Title/Abstract Full Text Show Details
unsteadiness
QUESTCOR PHARMACEUTICALS, INC.
Patent: WO2008/3093 A2, 2008 ; Title/Abstract Full Text Show Details
clumsiness
QUESTCOR PHARMACEUTICALS, INC.
Patent: WO2008/3093 A2, 2008 ; Title/Abstract Full Text Show Details
pain
QUESTCOR PHARMACEUTICALS, INC.
Patent: WO2008/3093 A2, 2008 ; Title/Abstract Full Text Show Details
attenuating muscle spasticity
QUESTCOR PHARMACEUTICALS, INC.
Patent: WO2008/3093 A2, 2008 ; Title/Abstract Full Text Show Details
Premature ejaculation (PE)
NEUROHEALING PHARMACEUTICALS, INC.
Patent: WO2008/21341 A2, 2008 ; Title/Abstract Full Text Show Details
Excessive daytime sleepiness (EDS)
NEUROHEALING PHARMACEUTICALS, INC.
Patent: WO2008/21341 A2, 2008 ; Title/Abstract Full Text Show Details
Cognitive dysfunction associated with fibromyalgia
CYPRESS BIOSCIENCE, INC.
Patent: WO2008/21932 A2, 2008 ; Title/Abstract Full Text Show Details
Cognitive dysfunction associated with fibromyalgia syndrome (FMS)
CYPRESS BIOSCIENCE, INC.
Patent: WO2008/21932 A2, 2008 ; Title/Abstract Full Text Show Details
Cognitive dysfunction
CYPRESS BIOSCIENCE, INC.
Patent: WO2008/21932 A2, 2008 ; Title/Abstract Full Text Show Details
fibromyalgia syndrome (FMS)
CYPRESS BIOSCIENCE, INC.
Patent: WO2008/21932 A2, 2008 ; Title/Abstract Full Text Show Details
Pain
CYPRESS BIOSCIENCE, INC.
Patent: WO2008/21932 A2, 2008 ;
Title/Abstract Full Text Show Details
Fatigue
CYPRESS BIOSCIENCE, INC.
Patent: WO2008/21932 A2, 2008 ; Title/Abstract Full Text Show Details
Symptoms of cognitive dysfunction
CYPRESS BIOSCIENCE, INC.
Patent: WO2008/21932 A2, 2008 ; Title/Abstract Full Text Show Details
Symptoms associated with fibromyalgia
CYPRESS BIOSCIENCE, INC.
Patent: WO2008/21932 A2, 2008 ; Title/Abstract Full Text Show Details
fibromyalgia
CYPRESS BIOSCIENCE, INC.
Patent: WO2008/21932 A2, 2008 ; Title/Abstract Full Text Show Details
quality of life
CYPRESS BIOSCIENCE, INC.
Patent: WO2008/21932 A2, 2008 ; Title/Abstract Full Text Show Details
Mood
CYPRESS BIOSCIENCE, INC.
Patent: WO2008/21932 A2, 2008 ; Title/Abstract Full Text Show Details
active ingredient of multimodal abuse resistant pharmaceutical composition
THERAQUEST BIOSCIENCES, INC.
Patent: WO2008/33351 A2, 2008 ; Title/Abstract Full Text Show Details
active ingredient of multimodal extended release pharmaceutical composition
THERAQUEST BIOSCIENCES, INC.
Patent: WO2008/33351 A2, 2008 ; Title/Abstract Full Text Show Details
active ingredient of multimodal extended release abuse resistant pharmaceutical composition
THERAQUEST BIOSCIENCES, INC.
Patent: WO2008/33351 A2, 2008 ; Title/Abstract Full Text Show Details
Neurogenic agent
BRAINCELLS, INC.
Patent: WO2008/39863 A2, 2008 ; Title/Abstract Full Text Show Details
sleepiness
CEPHALON FRANCE; ORGANISATION DE SYNTHESE MONDIALE ORSYMONDE
Patent: WO2004/14846 A1, 2004 ; Title/Abstract Full Text Show Details
CEPHALON, INC.
Patent: WO2005/27890 A1, 2005 ; Title/Abstract Full Text Show Details
Cephalon France
Patent: US2006/24370 A1, 2006 ; Title/Abstract Full Text Show Details
QUESTCOR PHARMACEUTICALS, INC.
Patent: WO2008/3093 A2, 2008 ; Title/Abstract Full Text Show Details
tiredness
CEPHALON FRANCE; ORGANISATION DE SYNTHESE MONDIALE ORSYMONDE
Patent: WO2004/14846 A1, 2004 ; Title/Abstract Full Text Show Details
QUESTCOR PHARMACEUTICALS, INC.
Patent: WO2008/3093 A2, 2008 ; Title/Abstract Full Text Show Details
Promote wakefulness
INTRA-CELLULAR THERAPIES, INC.
Patent: WO2008/63505 A1, 2008 ; Title/Abstract Full Text Show Details
Regulate sleep
INTRA-CELLULAR THERAPIES, INC.
Patent: WO2008/63505 A1, 2008 ; Title/Abstract Full Text Show Details
Restless leg syndrome (RLS)
LAVIN, Thomas, N.
Patent: WO2008/77127 A2, 2008 ; Title/Abstract Full Text Show Details
Periodic limb movement in sleep (PLMS)
LAVIN, Thomas, N.
Patent: WO2008/77127 A2, 2008 ; Title/Abstract Full Text Show Details
Snoring ICSD 780.53-1
LAVIN, Thomas, N.
Patent: WO2008/77127 A2, 2008 ; Title/Abstract Full Text Show Details
Snoring
LAVIN, Thomas, N.
Patent: WO2008/77127 A2, 2008 ; Title/Abstract Full Text Show Details
unpleasant leg sensations associated with unwanted leg movements
LAVIN, Thomas, N.
Patent: WO2008/77127 A2, 2008 ; Title/Abstract Full Text Show Details
unwanted involuntary leg movements at rest
LAVIN, Thomas, N.
Patent: WO2008/77127 A2, 2008 ; Title/Abstract Full Text Show Details
unwanted involuntary leg movements awake
LAVIN, Thomas, N.
Patent: WO2008/77127 A2, 2008 ; Title/Abstract Full Text Show Details
unwanted involuntary leg movements asleep
LAVIN, Thomas, N.
Patent: WO2008/77127 A2, 2008 ; Title/Abstract Full Text Show Details
Restless leg syndrome (RLS) symptoms
LAVIN, Thomas, N.
Patent: WO2008/77127 A2, 2008 ; Title/Abstract Full Text Show Details
Excessive sleepiness associated with narcolepsy
LAVIN, Thomas, N.
Patent: WO2008/77127 A2, 2008 ; Title/Abstract Full Text Show Details
Excessive sleepiness associated with obstructive sleep apnea/hypopnea syndrome (OSA/HS)
LAVIN, Thomas, N.
Patent: WO2008/77127 A2, 2008 ; Title/Abstract Full Text Show Details
Shift work sleep disorder (SWSD)
LAVIN, Thomas, N.
Patent: WO2008/77127 A2, 2008 ; Title/Abstract Full Text Show Details
Allows restful sleep
LAVIN, Thomas, N.
Patent: WO2008/77127 A2, 2008 ; Title/Abstract Full Text Show Details
unpleasant sensation to move the leg
LAVIN, Thomas, N.
Patent: WO2008/77127 A2, 2008 ; Title/Abstract Full Text Show Details
unpleasant urgency to move the leg
LAVIN, Thomas, N.
Patent: WO2008/77127 A2, 2008 ; Title/Abstract Full Text Show Details
undesired involuntary limb movements
LAVIN, Thomas, N.
Patent: WO2008/77127 A2, 2008 ; Title/Abstract Full Text Show Details
Primary snoring unrelated to sleep apnea
LAVIN, Thomas, N.
Patent: WO2008/77127 A2, 2008 ; Title/Abstract Full Text Show Details
Primary snoring
LAVIN, Thomas, N.
Patent: WO2008/77127 A2, 2008 ; Title/Abstract Full Text Show Details
Pharmaceutical composition for treating disease, disorder, or medical condition mediated by histamine H3 receptor activity
JANSSEN PHARMACEUTICA N.V.
Patent: WO2008/109336 A1, 2008 ; Title/Abstract Full Text Show Details
adrenergic agonist
BrainCells, Inc.
Patent: US2007/270449 A1, 2007 ; Title/Abstract Full Text Show Details
BrainCells, Inc.
Patent: US2008/64671 A1, 2008 ; Title/Abstract Full Text Show Details
diseases and conditions of the central and peripheral nervous system
BrainCells, Inc.
Patent: US2008/64671 A1, 2008 ; Title/Abstract Full Text Show Details
neurogenic agent
BrainCells, Inc.
Patent: US2007/270449 A1, 2007 ; Title/Abstract Full Text Show Details
BrainCells, Inc.
Patent: US2008/64671 A1, 2008 ; Title/Abstract Full Text Show Details
additional active ingredient of a composition comprising a neurogenic agent and suitable for treating nervous system disorders
BrainCells, Inc.
Patent: US2008/103165 A1, 2008 ; Title/Abstract Full Text Show Details
second neurogenic agent that enhances a neurogenic effect of the first neurogenic agent
BrainCells, Inc.
Patent: US2008/103165 A1, 2008 ; Title/Abstract Full Text Show Details
nerve cell trauma
BrainCells, Inc.
Patent: US2008/103165 A1, 2008 ; Title/Abstract Full Text Show Details
psychiatric condition
BrainCells, Inc.
Patent: US2008/103165 A1, 2008 ; Title/Abstract Full Text Show Details
neurologically related condition
BrainCells, Inc.
Patent: US2008/103165 A1, 2008 ; Title/Abstract Full Text Show Details
neural stem cell disorder
BrainCells, Inc.
Patent: US2008/103165 A1, 2008 ; Title/Abstract Full Text Show Details
neural progenitor cell disorder
BrainCells, Inc.
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narcolepsy
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GENERICS [UK] LIMITED; MYLAN DEVELOPMENT CENTRE PRIVATE LIMITED
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GENERICS [UK] LIMITED; MYLAN DEVELOPMENT CENTRE PRIVATE LIMITED
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NEUROHEALING PHARMACEUTICALS, INC.
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Use Pattern promoting or enhancing the state of wakefulness
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Title/Abstract Full Text Show Details
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Patent: WO2007/13962 A2, 2007 ; Title/Abstract Full Text Show Details
promoting or enhancing the state of alertness
NEUROHEALING PHARMACEUTICALS, INC.
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central nervous system stimulation
NEUROHEALING PHARMACEUTICALS, INC.
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excessive daytime sleepiness (EDS)
NEUROHEALING PHARMACEUTICALS, INC.
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individuals who suffer from narcolepsy
NEUROHEALING PHARMACEUTICALS, INC.
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promoting a patient's recovery from anesthesia
NEUROHEALING PHARMACEUTICALS, INC.
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attention deficit disorder (ADD)
NEUROHEALING PHARMACEUTICALS, INC.
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attention deficit hyperactivity disorder (ADHD)
NEUROHEALING PHARMACEUTICALS, INC.
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neurorehabilitation program
NEUROHEALING PHARMACEUTICALS, INC.
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NEUROHEALING PHARMACEUTICALS, INC.
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Attention Deficit Hyperactivity Disorder (ADHD)
BOEHRINGER INGELHEIM INTERNATIONAL GMBH; BOEHRINGER INGELHEIM PHARMA GMBH and CO. KG
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Attention Deficit Hyperactivity Disorder (ADHD) predominantly impulsivity type
BOEHRINGER INGELHEIM INTERNATIONAL GMBH; BOEHRINGER INGELHEIM PHARMA GMBH and CO. KG
Patent: WO2007/93624 A2, 2007 ; Title/Abstract Full Text Show Details
Attention Deficit Hyperactivity Disorder (ADHD) predominantly inattentive type
BOEHRINGER INGELHEIM INTERNATIONAL GMBH; BOEHRINGER INGELHEIM PHARMA GMBH and CO. KG
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Attention Deficit Hyperactivity Disorder (ADHD) predominantly hyperactive-impulsive type
BOEHRINGER INGELHEIM INTERNATIONAL GMBH; BOEHRINGER INGELHEIM PHARMA GMBH and CO. KG
Patent: WO2007/93624 A2, 2007 ; Title/Abstract Full Text Show Details
Attention Deficit Hyperactivity Disorder (ADHD) predominantly not otherwise specified
BOEHRINGER INGELHEIM INTERNATIONAL GMBH; BOEHRINGER INGELHEIM PHARMA GMBH and CO. KG
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Attention Deficit Disorder (ADD)
BOEHRINGER INGELHEIM INTERNATIONAL GMBH; BOEHRINGER INGELHEIM PHARMA GMBH and CO. KG
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Cypress Bioscience, Inc.
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Cypress Bioscience, Inc.
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sleep hypopnea
Cypress Bioscience, Inc.
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Carter, Andrew
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Restenosis
Carter, Andrew
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Carter, Andrew
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Carter, Andrew
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Mutual Pharmaceutical Company, Inc.
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Mutual Pharmaceutical Company, Inc.
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Impulse control disorders
CENTRE FOR ADDICTION AND MENTAL HEALTH
Patent: WO2006/32146 A1, 2006 ; Title/Abstract Full Text Show Details
promotion of wakefulness
Cephalon France
Patent: US2006/24370 A1, 2006 ; Title/Abstract Full Text Show Details
treatment of Parkinson's disease
Cephalon France
Patent: US2006/24370 A1, 2006 ; Title/Abstract Full Text Show Details
cerebral ischemia
Cephalon France
Patent: US2006/24370 A1, 2006 ; Title/Abstract Full Text Show Details
stroke
Cephalon France
Patent: US2006/24370 A1, 2006 ; Title/Abstract Full Text Show Details
eating disorders
Cephalon France
Patent: US2006/24370 A1, 2006 ; Title/Abstract Full Text Show Details
stimulation of appetite and weight gain
Cephalon France
Patent: US2006/24370 A1, 2006 ; Title/Abstract Full Text Show Details
treatment of attention deficit hyperactivity disorder
Cephalon France
Patent: US2006/24370 A1, 2006 ; Title/Abstract Full Text Show Details
treatment of attention deficit hyperactivity fatigue
Cephalon France
Patent: US2006/24370 A1, 2006 ; Title/Abstract Full Text Show Details
improvement of cognitive dysfunction
Cephalon France
Patent: US2006/24370 A1, 2006 ; Title/Abstract Full Text Show Details
CEPHALON FRANCE; ORGANISATION DE SYNTHESE MONDIALE ORSYMONDE
Patent: WO2004/14846 A1, 2004 ;
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Title/Abstract Full Text Show Details
Cephalon France
Patent: US2006/24370 A1, 2006 ; Title/Abstract Full Text Show Details
CEPHALON FRANCE; ORGANISATION DE SYNTHESE MONDIALE ORSYMONDE
Patent: WO2004/14846 A1, 2004 ;
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Title/Abstract Full Text Show Details
Cephalon France
Patent: US2006/24370 A1, 2006 ; Title/Abstract Full Text Show Details
CEPHALON FRANCE; ORGANISATION DE SYNTHESE MONDIALE ORSYMONDE
Patent: WO2004/14846 A1, 2004 ;
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Title/Abstract Full Text Show Details
Cephalon France
Patent: US2006/24370 A1, 2006 ; Title/Abstract Full Text Show Details
Neurotransmitter modulator
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JANSSEN PHARMACEUTICA, N.V.
Patent: WO2006/66197 A1, 2006 ; Title/Abstract Full Text Show Details
component of pharmaceutical compositions
Ray, Anup Kumar; Nandi, Indranil; Palaniswamy, Suresh; Davila, Pablo; Vora, Aakanksha Harshad
Patent: US2005/8704 A1, 2005 ; Title/Abstract Full Text Show Details
energizer
Ayala, William J.
Patent: US2005/31688 A1, 2005 ; Title/Abstract Full Text Show Details
invigorant
Ayala, William J.
Patent: US2005/31688 A1, 2005 ; Title/Abstract Full Text Show Details
nervous system stimulant
Ayala, William J.
Patent: US2005/31688 A1, 2005 ; Title/Abstract Full Text Show Details
altering the somnolent state of a mammal
CEPHALON, INC.
Patent: WO2005/27890 A1, 2005 ; Title/Abstract Full Text Show Details
disorders of sleep and wakefulness
CEPHALON, INC.
Patent: WO2005/27890 A1, 2005 ; Title/Abstract Full Text Show Details
excessive daytime sleepiness
CEPHALON, INC.
Patent: WO2005/27890 A1, 2005 ; Title/Abstract Full Text Show Details
urinary incontinence
CEPHALON, INC.
Patent: WO2005/27890 A1, 2005 ; Title/Abstract Full Text Show Details
multiple sclerosis fatigue
CEPHALON, INC.
Patent: WO2005/27890 A1, 2005 ;
Title/Abstract Full Text Show Details
ADHD
CEPHALON, INC.
Patent: WO2005/27890 A1, 2005 ; Title/Abstract Full Text Show Details
Alzheimer's disorder
CEPHALON, INC.
Patent: WO2005/27890 A1, 2005 ; Title/Abstract Full Text Show Details
ischemia
CEPHALON, INC.
Patent: WO2005/27890 A1, 2005 ; Title/Abstract Full Text Show Details
acute day-time sleepiness attack
BECTON, DICKINSON and COMPANY
Patent: WO2005/46701 A1, 2005 ; Title/Abstract Full Text Show Details
active component of composition having improved solubility of a hydrophobic drug and a compound having at least one carboxylic acid moiety for treating schizophrenia
Barbera, Gary; Doshi, Chetan Chhabildas; Patel, Mahendra R.; Davila, Pablo; Patel, Satishkumar Ambalal
Patent: US2005/249814 A1, 2005 ; Title/Abstract Full Text Show Details
excessive sleepiness
CEPHALON FRANCE; ORGANISATION DE SYNTHESE MONDIALE ORSYMONDE
Patent: WO2004/14846 A1, 2004 ; Title/Abstract Full Text Show Details
CEPHALON, INC.
Patent: WO2005/27890 A1, 2005 ; Title/Abstract Full Text Show Details
obstructive sleep apnea
CEPHALON FRANCE; ORGANISATION DE SYNTHESE MONDIALE ORSYMONDE
Patent: WO2004/14846 A1, 2004 ; Title/Abstract Full Text Show Details
CEPHALON, INC.
Patent: WO2005/27890 A1, 2005 ; Title/Abstract Full Text Show Details
Improving sleep quality
SEPRACOR INC.
Patent: WO2005/63248 A1, 2005 ; Title/Abstract Full Text Show Details
insomnia
SEPRACOR INC.
Patent: WO2005/63248 A1, 2005 ; Title/Abstract Full Text Show Details
transient insomnia
SEPRACOR INC.
Patent: WO2005/63248 A1, 2005 ; Title/Abstract Full Text Show Details
short-term insomnia
SEPRACOR INC.
Patent: WO2005/63248 A1, 2005 ; Title/Abstract Full Text Show Details
chronic insomnia
SEPRACOR INC.
Patent: WO2005/63248 A1, 2005 ; Title/Abstract Full Text Show Details
Parkinson's disease
CEPHALON FRANCE; ORGANISATION DE SYNTHESE MONDIALE ORSYMONDE
Patent: WO2004/14846 A1, 2004 ; Title/Abstract Full Text Show Details
CEPHALON, INC.
Patent: WO2005/27890 A1, 2005 ; Title/Abstract Full Text Show Details
SEPRACOR INC.
Patent: WO2005/63248 A1, 2005 ; Title/Abstract Full Text Show Details
cerebral tissue from ischemia
SEPRACOR INC.
Patent: WO2005/63248 A1, 2005 ; Title/Abstract Full Text Show Details
urinary and fecal incontinence
SEPRACOR INC.
Patent: WO2005/63248 A1, 2005 ; Title/Abstract Full Text Show Details
sleep apneas of central origin
SEPRACOR INC.
Patent: WO2005/63248 A1, 2005 ; Title/Abstract Full Text Show Details
Component of composition for treating allergic reactions and other histamine-mediated symptoms
PediaMed Pharmaceuticals, Inc.
Patent: US2004/259809 A1, 2004 ; Title/Abstract Full Text Show Details
To reduce or alleviate the sedation caused by the antihistamine
PediaMed Pharmaceuticals, Inc.
Patent: US2004/259809 A1, 2004 ; Title/Abstract Full Text Show Details
appetite stimulant
CEPHALON FRANCE; ORGANISATION DE SYNTHESE MONDIALE ORSYMONDE
Patent: WO2004/14846 A1, 2004 ; Title/Abstract Full Text Show Details
attention disorders
CEPHALON FRANCE; ORGANISATION DE SYNTHESE MONDIALE ORSYMONDE
Patent: WO2004/14846 A1, 2004 ; Title/Abstract Full Text Show Details
central nervous system disorders
CEPHALON FRANCE; ORGANISATION DE SYNTHESE MONDIALE ORSYMONDE
Patent: WO2004/14846 A1, 2004 ; Title/Abstract Full Text Show Details
depressive mood
CEPHALON FRANCE; ORGANISATION DE SYNTHESE MONDIALE ORSYMONDE
Patent: WO2004/14846 A1, 2004 ; Title/Abstract Full Text Show Details
excessive sleepiness associated with a disease
CEPHALON FRANCE; ORGANISATION DE SYNTHESE MONDIALE ORSYMONDE
Patent: WO2004/14846 A1, 2004 ; Title/Abstract Full Text Show Details
excessive sleepiness associated with narcolepsy
CEPHALON FRANCE; ORGANISATION DE SYNTHESE MONDIALE ORSYMONDE
Patent: WO2004/14846 A1, 2004 ; Title/Abstract Full Text Show Details
fatigue
CEPHALON FRANCE; ORGANISATION DE SYNTHESE MONDIALE ORSYMONDE
Patent: WO2004/14846 A1, 2004 ; Title/Abstract Full Text Show Details
food behavior disorders
CEPHALON FRANCE; ORGANISATION DE SYNTHESE MONDIALE ORSYMONDE
Patent: WO2004/14846 A1, 2004 ;
Title/Abstract Full Text Show Details
hyperactivity (ADHD)
CEPHALON FRANCE; ORGANISATION DE SYNTHESE MONDIALE ORSYMONDE
Patent: WO2004/14846 A1, 2004 ; Title/Abstract Full Text Show Details
hypersomnia in cancer patients
CEPHALON FRANCE; ORGANISATION DE SYNTHESE MONDIALE ORSYMONDE
Patent: WO2004/14846 A1, 2004 ; Title/Abstract Full Text Show Details
hypersomnia
CEPHALON FRANCE; ORGANISATION DE SYNTHESE MONDIALE ORSYMONDE
Patent: WO2004/14846 A1, 2004 ; Title/Abstract Full Text Show Details
idiopathic hypersomnia
CEPHALON FRANCE; ORGANISATION DE SYNTHESE MONDIALE ORSYMONDE
Patent: WO2004/14846 A1, 2004 ; Title/Abstract Full Text Show Details
jet lag
CEPHALON FRANCE; ORGANISATION DE SYNTHESE MONDIALE ORSYMONDE
Patent: WO2004/14846 A1, 2004 ; Title/Abstract Full Text Show Details
neurodegenerative diseases
CEPHALON FRANCE; ORGANISATION DE SYNTHESE MONDIALE ORSYMONDE
Patent: WO2004/14846 A1, 2004 ; Title/Abstract Full Text Show Details
particularly tiredness and fatigue associated with multiple sclerosis
CEPHALON FRANCE; ORGANISATION DE SYNTHESE MONDIALE ORSYMONDE
Patent: WO2004/14846 A1, 2004 ; Title/Abstract Full Text Show Details
protecting cerebral tissue from ischemia
CEPHALON FRANCE; ORGANISATION DE SYNTHESE MONDIALE ORSYMONDE
Patent: WO2004/14846 A1, 2004 ; Title/Abstract Full Text Show Details
relieve severe pain
CEPHALON FRANCE; ORGANISATION DE SYNTHESE MONDIALE ORSYMONDE
Patent: WO2004/14846 A1, 2004 ; Title/Abstract Full Text Show Details
stimulating cognitive functions
CEPHALON FRANCE; ORGANISATION DE SYNTHESE MONDIALE ORSYMONDE
Patent: WO2004/14846 A1, 2004 ; Title/Abstract Full Text Show Details
time lag
CEPHALON FRANCE; ORGANISATION DE SYNTHESE MONDIALE ORSYMONDE
Patent: WO2004/14846 A1, 2004 ; Title/Abstract Full Text Show Details
vigilance disorders associated with Steinert's disease
CEPHALON FRANCE; ORGANISATION DE SYNTHESE MONDIALE ORSYMONDE
Patent: WO2004/14846 A1, 2004 ; Title/Abstract Full Text Show Details
vigilance disorders
CEPHALON FRANCE; ORGANISATION DE SYNTHESE MONDIALE ORSYMONDE
Patent: WO2004/14846 A1, 2004 ; Title/Abstract Full Text Show Details
CEPHALON FRANCE; ORGANISATION DE SYNTHESE MONDIALE ORSYMONDE
Patent: WO2004/14846 A1, 2004 ;
weak sunlight (sundowning)
Title/Abstract Full Text Show Details
CHEMAGIS LTD.
Patent: EP1260501 A1, 2002 ;
treatment of narcolepsia
Title/Abstract Full Text Show Details
Chemical Name: Nuvigil Reaxys Registry Number: 9767970
CAS Registry Number: 112111-43-0 Type of Substance: isocyclic Molecular Formula: C15H15NO2S Linear Structure Formula: C15H15NO2S Molecular Weight: 273.356
InChI Key: YFGHCGITMMYXAQ-LJQANCHMSA-N
2
17 prep out of 21 reactions.
Identification Physical Data (10) Spectra (9) Bioactivity (17) Other Data (22)
Synthesize | Hide Details Find similar Chemical Names and Synonyms Nuvigil, (-)-Modafinil, Armodafinil, (-)-modafinil, armodafinil, l-modafinil, modafinil Identification Substance Label (7) Label
Reference
R-MOD
Krasulova, Kristyna; Siller, Michal; Holas, Ondrej; Dvorak, Zdenek; Anzenbacher, Pavel
Xenobiotica, 2016 , vol. 46, # 4 p. 315 - 324 Title/Abstract Full Text View citing articles Show Details
2a
CODEXIS, INC.; Ang, Ee Lui; Alvizo, Oscar; Behrouzian, Behnaz; Clay, Michael; Collier, Steven; Eberhard, Ellen; Fu, Fan Jaslyn; Song, Shiwei; Smith, Derek; Widegren, Magnus; Wilson, Robert; Xu, Junye; Zhu, Jun
Patent: US9267159 B2, 2016 ; Title/Abstract Full Text Show Details
(R)-2
Cao, Jianjing; Slack, Rachel D.; Bakare, Oluyomi M.; Burzynski, Caitlin; Rais, Rana; Slusher, Barbara S.; Kopajtic, Theresa; Bonifazi, Alessandro; Ellenberger, Michael P.; Yano, Hideaki; He, Yi; Bi, Guo-Hua; Xi, Zheng-Xiong; Loland, Claus J.; Newman, Amy Hauck
Journal of Medicinal Chemistry, 2016 , vol. 59, # 23 p. 10676 - 10691 Title/Abstract Full Text View citing articles Show Details
Formula I
Areveli, Srinivas; Singamsetty, Radha Krishna; Vujjni, Satish Kumar; Adla, Vijaya Kumar; Kandala, Sreenadha Charyulu; Varanasi, Ganesh; Peddireddy, Subbareddy; Baig, Mohammed Azeezulla
Patent: US2010/36164 A1, 2010 ; Title/Abstract Full Text Show Details
I(R)
ACTAVIS GROUP PTC EHF
Patent: WO2009/24863 A2, 2009 ; Title/Abstract Full Text Show Details
(R)-()-3
Prisinzano, Thomas; Podobinski, John; Tidgewell, Kevin; Luo, Min; Swenson, Dale
Tetrahedron Asymmetry, 2004 , vol. 15, # 6 p. 1053 - 1058 Title/Abstract Full Text View citing articles Show Details
(-)(R)-1
Osorio-Lozada, Antonio; Prisinzano, Thomas; Olivo, Horacio F.
Tetrahedron Asymmetry, 2004 , vol. 15, # 23 p. 3811 - 3815 Title/Abstract Full Text View citing articles Show Details
36
Patent-Specific Data (1) Related Markush Structure (RN)
Reference CODEXIS, INC.; Ang, Ee Lui; Alvizo, Oscar; Behrouzian, Behnaz; Clay, Michael; Collier, Steven; Eberhard, Ellen; Fu, Fan Jaslyn; Song, Shiwei; Smith, Derek; Widegren, Magnus; Wilson, Robert; Xu, Junye; Zhu, Jun
Patent: US9267159 B2, 2016 ;
29405677
Title/Abstract Full Text Show Details
Physical Data Melting Point (4) Melting Point
Solvent (Melting Point)
156 - 158 °C
di-isopropyl ether
153 - 154 °C
ethanol
Location
Reference
supporting information
Cao, Jianjing; Prisinzano, Thomas E.; Okunola, Oluyomi M.; Kopajtic, Theresa; Shook, Matthew; Katz, Jonathan L.; Newman, Amy Hauck
ACS Medicinal Chemistry Letters, 2011 , vol. 2, # 1 p. 48 - 52 Title/Abstract Full Text View citing articles Show Details
LUPIN LIMITED
Patent: WO2009/90663 A1, 2009 ; Title/Abstract Full Text Show Details
TEVA PHARMACEUTICAL INDUSTRIES LTD.; TEVA PHARMACEUTICALS USA, INC.
Patent: WO2007/98273 A2, 2007 ;
146 - 147 °C
Title/Abstract Full Text Show Details
Osorio-Lozada, Antonio; Prisinzano, Thomas; Olivo, Horacio F.
Tetrahedron Asymmetry, 2004 , vol. 15, # 23 p. 3811 - 3815 Title/Abstract Full Text View citing articles Show Details
158 - 159 °C
Crystal Property Description (2) Colour & Other Properties
Location
Reference
white
supporting information
Cao, Jianjing; Prisinzano, Thomas E.; Okunola, Oluyomi M.; Kopajtic, Theresa; Shook, Matthew; Katz, Jonathan L.; Newman, Amy Hauck
ACS Medicinal Chemistry Letters, 2011 , vol. 2, # 1 p. 48 - 52 Title/Abstract Full Text View citing articles Show Details
TEVA PHARMACEUTICAL INDUSTRIES LTD.; TEVA PHARMACEUTICALS USA, INC.
Patent: WO2007/103221 A2, 2007 ;
white
Title/Abstract Full Text Show Details
ACTAVIS GROUP PTC EHF
Patent: WO2009/24863 A2, 2009 ; Title/Abstract Full Text Show Details
Optical Rotatory Power (3) Type (Optical Rotatory Power)
Concentration (Optical Rotatory Power)
Enantiomeric excess
Solvent (Optical Rotatory Power)
Optical Rotatory Power
Wavelength (Optical Rotatory Power)
Temperature (Optical Rotatory Power)
[alpha]
1.02 g/100ml
100 %ee
chloroform
-83.4 deg
589 nm
25 °C
[alpha]
1.0 g/100ml
CHCl3
-76.6 deg
589 nm
22 °C
Prisinzano, Thomas; Podobinski, John; Tidgewell, Kevin; Luo, Min; Swenson, Dale
Tetrahedron Asymmetry, 2004 , vol. 15, # 6 p. 1053 - 1058 Title/Abstract Full Text View citing articles Show Details
[alpha]
1.0 g/100ml
CHCl3
-79 deg
589 nm
22 °C
Osorio-Lozada, Antonio; Prisinzano, Thomas; Olivo, Horacio F.
Tetrahedron Asymmetry, 2004 , vol. 15, # 23 p. 3811 - 3815 Title/Abstract Full Text View citing articles Show Details
Location
Reference
supporting information
Cao, Jianjing; Prisinzano, Thomas E.; Okunola, Oluyomi M.; Kopajtic, Theresa; Shook, Matthew; Katz, Jonathan L.; Newman, Amy Hauck
ACS Medicinal Chemistry Letters, 2011 , vol. 2, # 1 p. 48 - 52 Title/Abstract Full Text View citing articles Show Details
Partition octan-1-ol/water (MCS) (1) log POW
pH
Location
Comment (Partition octan-1-ol/water (MCS))
Reference
1.17
7.4
supporting information
aq.buffer
Gunaydin, Hakan
ACS Medicinal Chemistry Letters, 2016 , vol. 7, # 1 p. 89 - 93 Title/Abstract Full Text View citing articles Show Details
Spectra NMR Spectroscopy (8) Description (NMR Spectroscopy)
Nucleus (NMR Spectroscopy)
Chemical shifts
1H
Chemical shifts
Chemical shifts
Coupling Nuclei
Solvents (NMR Spectroscopy)
Frequency (NMR Spectroscopy)
Location
Reference
dimethylsulfoxided6
supporting information
Cao, Jianjing; Prisinzano, Thomas E.; Okunola, Oluyomi M.; Kopajtic, Theresa; Shook, Matthew; Katz, Jonathan L.; Newman, Amy Hauck
ACS Medicinal Chemistry Letters, 2011 , vol. 2, # 1 p. 48 - 52 Title/Abstract Full Text View citing articles Show Details
13C
dimethylsulfoxided6
supporting information
Cao, Jianjing; Prisinzano, Thomas E.; Okunola, Oluyomi M.; Kopajtic, Theresa; Shook, Matthew; Katz, Jonathan L.; Newman, Amy Hauck
ACS Medicinal Chemistry Letters, 2011 , vol. 2, # 1 p. 48 - 52 Title/Abstract Full Text View citing articles Show Details
1H
dimethylsulfoxided6
Prisinzano, Thomas; Podobinski, John; Tidgewell, Kevin; Luo, Min; Swenson, Dale
Tetrahedron Asymmetry, 2004 , vol. 15, # 6 p. 1053 - 1058 Title/Abstract Full Text View citing articles Show Details
dimethylsulfoxided6
Prisinzano, Thomas; Podobinski, John; Tidgewell, Kevin; Luo, Min; Swenson, Dale
Tetrahedron Asymmetry, 2004 , vol. 15, # 6 p. 1053 - 1058 Title/Abstract Full Text View citing articles Show Details
Prisinzano, Thomas; Podobinski, John; Tidgewell, Kevin; Luo, Min; Swenson, Dale
Tetrahedron Asymmetry, 2004 , vol. 15, # 6 p. 1053 - 1058 Title/Abstract Full Text View citing articles Show Details
1H
1H
Chemical shifts
13C
dimethylsulfoxided6
Chemical shifts
1H
CDCl3
Chemical shifts
13C
CDCl3
1H
1H
300 MHz
Osorio-Lozada, Antonio; Prisinzano, Thomas; Olivo, Horacio F.
Tetrahedron Asymmetry, 2004 , vol. 15, # 23 p. 3811 - 3815 Title/Abstract Full Text View citing articles Show Details
Osorio-Lozada, Antonio; Prisinzano, Thomas; Olivo, Horacio F.
Tetrahedron Asymmetry, 2004 , vol. 15, # 23 p. 3811 - 3815 Title/Abstract Full Text View citing articles Show Details
CDCl3
300 MHz
Osorio-Lozada, Antonio; Prisinzano, Thomas; Olivo, Horacio F.
Tetrahedron Asymmetry, 2004 , vol. 15, # 23 p. 3811 - 3815 Title/Abstract Full Text View citing articles Show Details
IR Spectroscopy (1) Description (IR Spectroscopy)
Reference
Bands
Osorio-Lozada, Antonio; Prisinzano, Thomas; Olivo, Horacio F.
Tetrahedron Asymmetry, 2004 , vol. 15, # 23 p. 3811 - 3815 Title/Abstract Full Text View citing articles Show Details
Bioactivity Pharmacological Data (17) 1 of 17
Comment (Pharmacological Data)
Bioactivities present
Reference
Cypress Bioscience, Inc.
Patent: US2006/39866 A1, 2006 ; Title/Abstract Full Text Show Details
TEVA PHARMACEUTICAL INDUSTRIES LTD.; TEVA PHARMACEUTICALS USA, INC.
Patent: WO2007/98273 A2, 2007 ; Title/Abstract Full Text Show Details
TEVA PHARMACEUTICAL INDUSTRIES LTD.; TEVA PHARMACEUTICALS USA, INC.
Patent: WO2007/103221 A2, 2007 ; Title/Abstract Full Text Show Details
NEUROHEALING PHARMACEUTICALS, INC.
Patent: WO2008/21341 A2, 2008 ; Title/Abstract Full Text Show Details
Prisinzano, Thomas; Podobinski, John; Tidgewell, Kevin; Luo, Min; Swenson, Dale
Tetrahedron Asymmetry, 2004 , vol. 15, # 6 p. 1053 - 1058 Title/Abstract Full Text View citing articles Show Details
Osorio-Lozada, Antonio; Prisinzano, Thomas; Olivo, Horacio F.
Tetrahedron Asymmetry, 2004 , vol. 15, # 23 p. 3811 - 3815 Title/Abstract Full Text View citing articles Show Details
Olivo, Horacio F.; Osorio-Lozada, Antonio; Peeples, Tonya L.
Tetrahedron Asymmetry, 2005 , vol. 16, # 21 p. 3507 - 3511 Title/Abstract Full Text View citing articles Show Details
Ternois, James; Guillen, Frederic; Plaquevent, Jean-Christophe; Coquerel, Gerard
Tetrahedron Asymmetry, 2007 , vol. 18, # 24 p. 2959 - 2964 Title/Abstract Full Text View citing articles Show Details
Zhu, Hao-Jie; Wang, Jun-Sheng; Donovan, Jennifer L.; Jiang, Yan; Gibson, Bryan B.; DeVane, C. Lindsay; Markowitz, John S.
European Journal of Pharmacology, 2008 , vol. 578, # 2-3 p. 148 - 158 Title/Abstract Full Text View citing articles Show Details
TEVA PHARMACEUTICAL INDUSTRIES LTD.; TEVA PHARMACEUTICALS USA, INC.
Patent: WO2008/70143 A1, 2008 ; Title/Abstract Full Text Show Details
Gome, Boaz
Patent: US2009/48464 A1, 2009 ; Title/Abstract Full Text Show Details
ACTAVIS GROUP PTC EHF
Patent: WO2009/24863 A2, 2009 ; Title/Abstract Full Text Show Details
Jegorov, Alexandr
Patent: US2009/105346 A1, 2009 ; Title/Abstract Full Text Show Details
LUPIN LIMITED
Patent: WO2009/90663 A1, 2009 ; Title/Abstract Full Text Show Details
Intra-Cellular Therapies, Inc.
Patent: WO2009/145900 A1, 2009 ; Title/Abstract Full Text Show Details
Areveli, Srinivas; Singamsetty, Radha Krishna; Vujjni, Satish Kumar; Adla, Vijaya Kumar; Kandala, Sreenadha Charyulu; Varanasi, Ganesh; Peddireddy, Subbareddy; Baig, Mohammed Azeezulla
Patent: US2010/36164 A1, 2010 ; Title/Abstract Full Text Show Details
Cao, Jianjing; Prisinzano, Thomas E.; Okunola, Oluyomi M.; Kopajtic, Theresa; Shook, Matthew; Katz, Jonathan L.; Newman, Amy Hauck
ACS Medicinal Chemistry Letters, 2011 , vol. 2, # 1 p. 48 - 52 Title/Abstract Full Text View citing articles Show Details
Stingl, Kerstin A.; Weiss, Katharina M.; Tsogoeva, Svetlana B.
Tetrahedron, 2012 , vol. 68, # 40 p. 8493 - 8501 Title/Abstract Full Text View citing articles Show Details
Darwish, Mona; Kirby, Mary; Robertson Jr., Philmore; Hellriegel, Edward T.
Clinical Pharmacokinetics, 2008 , vol. 47, # 1 p. 61 - 74 Title/Abstract Full Text View citing articles Show Details
Darwish, Mona; Kirby, Mary; Hellriegel, Edward T.; Yang, Ronghua; Robertson Jr., Philmore
Clinical Drug Investigation, 2009 , vol. 29, # 2 p. 87 - 100 Title/Abstract Full Text View citing articles Show Details
2 of 17
Comment (Pharmacological Data)
Bioactivities present
Reference
Darwish, Mona; Bond, Mary; Hellriegel, Edward T.; Youakim, James M.; Yang, Ronghua; Robertson, Philmore
Journal of Clinical Pharmacology, 2012 , vol. 52, # 9 p. 1399 - 1409 Title/Abstract Full Text View citing articles Show Details
Type: Review, Lab: EFF_071212, Owner: EFFECT, Number: 000, Revision: 07.12.2012 00:00:00 2012 Full Text Show Details
Sutradhar, Manas; Martins, Luísa M.D.R.S.; Guedes da Silva, M. Fátima C.; Pombeiro, Armando J.L.
Coordination Chemistry Reviews, 2015 , vol. 301-302, p. 200 - 239 Title/Abstract Full Text View citing articles Show Details
Smith, Lillian; Mosley, Juan F.; Ford, Megan; Barwick, Thomas; Brooks, David; Luckett, Wileta
U.S. Pharmacist, 2016 , vol. 41, # 1 p. 40 - 44 Title/Abstract Full Text View citing articles Show Details
Gunaydin, Hakan
ACS Medicinal Chemistry Letters, 2016 , vol. 7, # 1 p. 89 - 93 Title/Abstract Full Text View citing articles Show Details
Krasulova, Kristyna; Siller, Michal; Holas, Ondrej; Dvorak, Zdenek; Anzenbacher, Pavel
Xenobiotica, 2016 , vol. 46, # 4 p. 315 - 324 Title/Abstract Full Text View citing articles Show Details
CODEXIS, INC.; Ang, Ee Lui; Alvizo, Oscar; Behrouzian, Behnaz; Clay, Michael; Collier, Steven; Eberhard, Ellen; Fu, Fan Jaslyn; Song, Shiwei; Smith, Derek; Widegren, Magnus; Wilson, Robert; Xu, Junye; Zhu, Jun
Patent: US9267159 B2, 2016 ; Title/Abstract Full Text Show Details
Ellefsen, Kayla N.; Concheiro, Marta; Huestis, Marilyn A.
Drug Metabolism Reviews, 2016 , vol. 48, # 2 p. 237 - 265 Title/Abstract Full Text View citing articles Show Details
Schumock, Glen T.; Li, Edward C.; Suda, Katie J.; Wiest, Michelle D.; Stubbings, JoAnn; Matusiak, Linda M.; Hunkler, Robert J.; Vermeulen, Lee C.
American Journal of Health-System Pharmacy, 2016 , vol. 73, # 14 p. 1058 - 1075 Title/Abstract Full Text View citing articles Show Details
Mila
Drugs of the Future, 2016 , vol. 41, # 5 p. 325 - 329 Title/Abstract Full Text View citing articles Show Details
Ruoff, Chad; Swick , Todd J.; Doekel, Robert; Emsellem, Helene A.; Feldman, Neil T.; Rosenberg, Russell; Bream, Gary; Khayrallah, Moise A.; Lu , Yuan; Black, Jed
Sleep, 2016 , vol. 39, # 7 p. 1379 - 1387 Title/Abstract Full Text View citing articles Show Details
Zong, Lili; Wang, Chao; Moeljadi, Adhitya Mangala Putra; Ye, Xinyi; Ganguly, Rakesh; Li, Yongxin; Hirao, Hajime; Tan, Choon-Hong
Nature Communications, 2016 , vol. 7, art. no. 13455 Title/Abstract Full Text View citing articles Show Details
Cao, Jianjing; Slack, Rachel D.; Bakare, Oluyomi M.; Burzynski, Caitlin; Rais, Rana; Slusher, Barbara S.; Kopajtic, Theresa; Bonifazi, Alessandro; Ellenberger, Michael P.; Yano, Hideaki; He, Yi; Bi, Guo-Hua; Xi, Zheng-Xiong; Loland, Claus J.; Newman, Amy Hauck
Journal of Medicinal Chemistry, 2016 , vol. 59, # 23 p. 10676 - 10691 Title/Abstract Full Text View citing articles Show Details
Willavize, Susan; Fiedler-Kelly, Jill; Ludwig, Elizabeth; Guan, Lingling
Journal of Clinical Pharmacology, 2017 , vol. 57, # 2 p. 255 - 265 Title/Abstract Full Text View citing articles Show Details
Liu, Yan; Zhang, Yumei; Li, Xuejian; Yuan, Qipeng; Liang, Hao
Chemical Communications, 2017 , vol. 53, # 22 p. 3216 - 3219 Title/Abstract Full Text Show Details
Zong, Lili; Tan, Choon-Hong
Accounts of Chemical Research, 2017 , vol. 50, # 4 p. 842 - 856 Title/Abstract Full Text Show Details
3 of 17
4 of 17
5 of 17
6 of 17
7 of 17
8 of 17
Comment (Pharmacological Data)
physiological behaviour discussed
Reference
Willavize, Susan; Fiedler-Kelly, Jill; Ludwig, Elizabeth; Guan, Lingling
Journal of Clinical Pharmacology, 2017 , vol. 57, # 2 p. 255 - 265 Title/Abstract Full Text View citing articles Show Details
Comment (Pharmacological Data)
physiological behaviour discussed
Reference
Krasulova, Kristyna; Siller, Michal; Holas, Ondrej; Dvorak, Zdenek; Anzenbacher, Pavel
Xenobiotica, 2016 , vol. 46, # 4 p. 315 - 324 Title/Abstract Full Text View citing articles Show Details
Comment (Pharmacological Data)
physiological behaviour discussed
Reference
Cao, Jianjing; Slack, Rachel D.; Bakare, Oluyomi M.; Burzynski, Caitlin; Rais, Rana; Slusher, Barbara S.; Kopajtic, Theresa; Bonifazi, Alessandro; Ellenberger, Michael P.; Yano, Hideaki; He, Yi; Bi, Guo-Hua; Xi, Zheng-Xiong; Loland, Claus J.; Newman, Amy Hauck
Journal of Medicinal Chemistry, 2016 , vol. 59, # 23 p. 10676 - 10691 Title/Abstract Full Text View citing articles Show Details
Effect (Pharmacological Data)
monoamine transporter binding affinity
Species or Test-System (Pharmacological Data)
brain membranes of rat
Further Details (Pharmacological Data)
Ki related to: dopamine transporter
Type (Pharmacological Data)
Ki
Value of Type (Pharmacological Data)
3260 nmol/l
Reference
Cao, Jianjing; Prisinzano, Thomas E.; Okunola, Oluyomi M.; Kopajtic, Theresa; Shook, Matthew; Katz, Jonathan L.; Newman, Amy Hauck
ACS Medicinal Chemistry Letters, 2011 , vol. 2, # 1 p. 48 - 52 Title/Abstract Full Text View citing articles Show Details
Effect (Pharmacological Data)
monoamine transporter binding affinity
Species or Test-System (Pharmacological Data)
brain membranes of rat
Results
molecular target: dopamine transporter
Reference
Cao, Jianjing; Prisinzano, Thomas E.; Okunola, Oluyomi M.; Kopajtic, Theresa; Shook, Matthew; Katz, Jonathan L.; Newman, Amy Hauck
ACS Medicinal Chemistry Letters, 2011 , vol. 2, # 1 p. 48 - 52 Title/Abstract Full Text View citing articles Show Details
Effect (Pharmacological
monoamine transporter binding affinity
Data)
9 of 17
10 of 17
11 of 17
12 of 17
13 of 17
Species or Test-System (Pharmacological Data)
brain membranes of rat
Concentration (Pharmacological Data)
<= 10 μmol/l
Results
no effect (related to serotonin transporter)
Reference
Cao, Jianjing; Prisinzano, Thomas E.; Okunola, Oluyomi M.; Kopajtic, Theresa; Shook, Matthew; Katz, Jonathan L.; Newman, Amy Hauck
ACS Medicinal Chemistry Letters, 2011 , vol. 2, # 1 p. 48 - 52 Title/Abstract Full Text View citing articles Show Details
Effect (Pharmacological Data)
monoamine transporter binding affinity
Species or Test-System (Pharmacological Data)
brain membranes of rat
Concentration (Pharmacological Data)
<= 10 μmol/l
Results
no effect (related to norepinephrine transporter)
Reference
Cao, Jianjing; Prisinzano, Thomas E.; Okunola, Oluyomi M.; Kopajtic, Theresa; Shook, Matthew; Katz, Jonathan L.; Newman, Amy Hauck
ACS Medicinal Chemistry Letters, 2011 , vol. 2, # 1 p. 48 - 52 Title/Abstract Full Text View citing articles Show Details
Effect (Pharmacological Data)
locomotor activity; effect on
Species or Test-System (Pharmacological Data)
mouse
Concentration (Pharmacological Data)
30 - 300 mg/kg
Type (Pharmacological Data)
maximal locomotor activity
Value of Type (Pharmacological Data)
Ca. 500 counts/min
Reference
Cao, Jianjing; Prisinzano, Thomas E.; Okunola, Oluyomi M.; Kopajtic, Theresa; Shook, Matthew; Katz, Jonathan L.; Newman, Amy Hauck
ACS Medicinal Chemistry Letters, 2011 , vol. 2, # 1 p. 48 - 52 Title/Abstract Full Text View citing articles Show Details
Effect (Pharmacological Data)
locomotor activity; effect on
Species or Test-System (Pharmacological Data)
mouse
Concentration (Pharmacological Data)
30 - 300 mg/kg
Type (Pharmacological Data)
time for maximal activity
Value of Type (Pharmacological Data)
1 h
Reference
Cao, Jianjing; Prisinzano, Thomas E.; Okunola, Oluyomi M.; Kopajtic, Theresa; Shook, Matthew; Katz, Jonathan L.; Newman, Amy Hauck
ACS Medicinal Chemistry Letters, 2011 , vol. 2, # 1 p. 48 - 52 Title/Abstract Full Text View citing articles Show Details
Effect (Pharmacological Data)
locomotor activity; effect on
Species or Test-System (Pharmacological Data)
mouse
Concentration (Pharmacological Data)
30 - 300 mg/kg
Type (Pharmacological Data)
dose for maximal activity
Value of Type (Pharmacological Data)
100 mg/kg
Reference
Cao, Jianjing; Prisinzano, Thomas E.; Okunola, Oluyomi M.; Kopajtic, Theresa; Shook, Matthew; Katz, Jonathan L.; Newman, Amy Hauck
ACS Medicinal Chemistry Letters, 2011 , vol. 2, # 1 p. 48 - 52 Title/Abstract Full Text View citing articles Show Details
Effect (Pharmacological
delayed ejaculation; effect on
Data) Species or Test-System (Pharmacological Data)
human
Route of Application
sublingual
Method (Pharmacological Data)
Example 1. Delayed ejaculation with sublingually administered d-modafinil.The synthesis of (d)-(+)-modafinil has been described in the literature (see, e.g., Prisinzano et al., Tetrahedron Asymmetry, 15: 1053-1058 (2004); US Patent No. 4,927,855 ("Lafon synthesis"))- In accordance with the Lafon synthesis, the intermediate carboxylic acid was converted to the diastereomic salt mixture with (+) alpha-methylbenzylamine. The diastereomers were separated, and the appropriate chiral acid liberated from the salt form. The acid was converted to the methyl ester via esterification and reacted with ammonia/methanol solution to yield d-modafinil. The enantiomeric purity was in excess of 98percent-99percent.Initial formulation tests of modafinil (racemate) and pure d-modafinil revealed a bitter taste. Therefore, the pharmaceutical formulation included one or more taste-masking ingredients. The d-modafinil was mixed with various taste-masking agents, including pulverized mints, breath fresheners, and natural and artificial flavorings. The synthesized d-modafinil was compounded into a composition containing sugar, spearmint flavor, cinnamon flavor, gum arabic, gelatin, corn syrup, and dyes that could be administered sublingually. Formulations containing 100 mg of d-modafinil were prepared. Subject 1 took the above-described formulation of d-modafinil sublingually at 9:00 pm in the course of testing a composition containing d-modafinil for a different effect unrelated to sexual activity. Subject 1 reported that unexpectedly the time to ejaculate during sexual activity was significantly longer than usual by a factor of about two to three times. A week later, Subject 1 took the formulation sublingually for a second time and, again, reported that the time to ejaculate during sexual intercourse was significantly delayed by a factor of approximately two to three times.The data demonstrate that sublingual administration of d-modafinil can provide a desirable delay of ejaculation during sexual activity, that the effect is drug-dependent, and that the effect is reversible.
Results
treatment with the title compound showed the time to ejaculate during sexual intercourse was significantly delayed by a factor of approximately two to three times
Location
Page/Page column 19-20
Reference
NEUROHEALING PHARMACEUTICALS, INC.
Patent: WO2008/21341 A2, 2008 ; Title/Abstract Full Text Show Details
14 of 17
15 of 17
16 of 17
Effect (Pharmacological Data)
P-glycoprotein activity; inhibition of
Species or Test-System (Pharmacological Data)
LLC-PK1/MDR1 cells
Concentration (Pharmacological Data)
10 - 100 μmol/l
Method (Pharmacological Data)
human P-glycoprotein overexpressing porcine kidney epithelial LLC-PK1 cells; after incubation with doxorubicin in the presence of title comp. for 1 h intracellular conc. of doxorubicin analyzed by HPLC
Further Details (Pharmacological Data)
control: 0.5percent dimethyl sulfoxide; positive control: PSC833 (2 μM), quinine (200 μM); P-glycoprotein negative parental LLC-PK1 cells used as negative control; efficiency of PSC833 was defined as 100percent
Comment (Pharmacological Data)
No effect
Reference
Zhu, Hao-Jie; Wang, Jun-Sheng; Donovan, Jennifer L.; Jiang, Yan; Gibson, Bryan B.; DeVane, C. Lindsay; Markowitz, John S.
European Journal of Pharmacology, 2008 , vol. 578, # 2-3 p. 148 - 158 Title/Abstract Full Text View citing articles Show Details
Effect (Pharmacological Data)
P-glycoprotein activity; inhibition of
Species or Test-System (Pharmacological Data)
LLC-PK1/MDR1 cells
Concentration (Pharmacological Data)
10 - 100 μmol/l
Method (Pharmacological Data)
human P-glycoprotein overexpressing porcine kidney epithelial LLC-PK1 cells; after incubation with rhodamine123 in the presence of title comp. for 1 h intracellular conc. of rhodamine123 analyzed by HPLC
Further Details (Pharmacological Data)
control: 0.5percent dimethyl sulfoxide; positive control: PSC833 (2 μM), quinine (200 μM); P-glycoprotein negative parental LLC-PK1 cells used as negative control; efficiency of PSC833 was defined as 100percent
Comment (Pharmacological Data)
No effect
Reference
Zhu, Hao-Jie; Wang, Jun-Sheng; Donovan, Jennifer L.; Jiang, Yan; Gibson, Bryan B.; DeVane, C. Lindsay; Markowitz, John S.
European Journal of Pharmacology, 2008 , vol. 578, # 2-3 p. 148 - 158 Title/Abstract Full Text View citing articles Show Details
Effect (Pharmacological Data)
transport
Species or Test-System (Pharmacological Data)
LLC-PK1/MDR1 cell monolayers
Concentration (Pharmacological Data)
5 μmol/l
Method (Pharmacological Data)
human P-glycoprotein overexpressing porcine kidney epithelial LLC-PK1 cells; title comp. loaded into B or A side of monolayers; incubation in the presence or absence of PSC833 (2 μM); title comp. in receiver compartment analyzed by HPLC
Further Details (Pharmacological Data)
control: 0.5percent dimethyl sulfoxide; B: basolateral; A: apical; Papp B-A/Papp A-B: apparent permeability coefficient for B-A/A-B direction; PSC833: selective P-glycoprotein inhibitor; reference: rhodamine123 (Papp B-A-to-Papp A-B ratio = 11.11)
17 of 17
Results
Papp B-A-to-Papp A-B ratio was 1.17 in the absence and 0.91 in the presence of PSC833; fig.
Reference
Zhu, Hao-Jie; Wang, Jun-Sheng; Donovan, Jennifer L.; Jiang, Yan; Gibson, Bryan B.; DeVane, C. Lindsay; Markowitz, John S.
European Journal of Pharmacology, 2008 , vol. 578, # 2-3 p. 148 - 158 Title/Abstract Full Text View citing articles Show Details
Effect (Pharmacological Data)
transport
Species or Test-System (Pharmacological Data)
LLC-PK1/MDR1 cells
Concentration (Pharmacological Data)
20 μmol/l
Method (Pharmacological Data)
human P-glycoprotein overexpressing porcine kidney epithelial LLC-PK1 cells; after incubation with title comp. in the presence or absence of PSC833 (2 μM) for 1 h intracellular conc. of title comp. analyzed by HPLC
Further Details (Pharmacological Data)
control: 0.5percent dimethyl sulfoxide; positive control: doxorubicin, rhodamine123; P-glycoprotein negative parental LLC-PK1 cells used as negative control
Results
accumulation of title comp. in LLC-PK1 cells was higher than that in LLC-PK1/MDR1 cells; cotreatment with PSC833 increased (45.6percent) title comp. conc. in LLCPK1/MDR1 cells, suggesting that P-glycoprotein might play role in transport of title comp.; fig.
Reference
Zhu, Hao-Jie; Wang, Jun-Sheng; Donovan, Jennifer L.; Jiang, Yan; Gibson, Bryan B.; DeVane, C. Lindsay; Markowitz, John S.
European Journal of Pharmacology, 2008 , vol. 578, # 2-3 p. 148 - 158 Title/Abstract Full Text View citing articles Show Details
Other Data Use (22) Use Pattern
Location
Reference
excessive sleepiness associated with narcolepsy
Jegorov, Alexandr
Patent: US2009/105346 A1, 2009 ; Title/Abstract Full Text Show Details
shift work sleep disorder
Jegorov, Alexandr
Patent: US2009/105346 A1, 2009 ; Title/Abstract Full Text Show Details
obstructive sleep apnea/hypopnea syndrome
Jegorov, Alexandr
Patent: US2009/105346 A1, 2009 ; Title/Abstract Full Text Show Details
Page/Page column 40
Intra-Cellular Therapies, Inc.
Patent: WO2009/145900 A1, 2009 ;
Page/Page column 40
Intra-Cellular Therapies, Inc.
Patent: WO2009/145900 A1, 2009 ;
Page/Page column 40
Intra-Cellular Therapies, Inc.
Patent: WO2009/145900 A1, 2009 ;
Treatment of side effect of conventional antipsychotic drugs; in combination with substituted heterocycle fused γcarboline compounds
Page/Page column 40
Intra-Cellular Therapies, Inc.
Patent: WO2009/145900 A1, 2009 ;
Treatment of Parkinson's disease in combination with substituted heterocycle fused γ-carboline compounds
Page/Page column 40
Intra-Cellular Therapies, Inc.
Patent: WO2009/145900 A1, 2009 ;
Page/Page column 40
Intra-Cellular Therapies, Inc.
Patent: WO2009/145900 A1, 2009 ;
Page/Page
Intra-Cellular Therapies, Inc.
Treatment of psychosis in combination with substituted heterocycle fused γ-carboline compounds
Treatment of schizophrenia in combination with substituted heterocycle fused γ-carboline compounds
Treatment of depression in combination with substituted heterocycle fused γ-carboline compounds
Treatment of sleep disorder in combination with substituted heterocycle fused γ-carboline compounds
Treatment of dyskinesia in combination with substituted heterocycle fused γ-carboline compounds
Title/Abstract Full Text Show Details
Title/Abstract Full Text Show Details
Title/Abstract Full Text Show Details
Title/Abstract Full Text Show Details
Title/Abstract Full Text Show Details
Title/Abstract Full Text Show Details
Premature ejaculation (PE)
column 40
Patent: WO2009/145900 A1, 2009 ;
NEUROHEALING PHARMACEUTICALS, INC.
Patent: WO2008/21341 A2, 2008 ;
Title/Abstract Full Text Show Details
Title/Abstract Full Text Show Details
Excessive daytime sleepiness (EDS)
NEUROHEALING PHARMACEUTICALS, INC.
Patent: WO2008/21341 A2, 2008 ; Title/Abstract Full Text Show Details
Excessive sleepiness
TEVA PHARMACEUTICAL INDUSTRIES LTD.; TEVA PHARMACEUTICALS USA, INC.
Patent: WO2007/98273 A2, 2007 ; Title/Abstract Full Text Show Details
Excessive sleepiness associated with narcolepsy
TEVA PHARMACEUTICAL INDUSTRIES LTD.; TEVA PHARMACEUTICALS USA, INC.
Patent: WO2007/98273 A2, 2007 ; Title/Abstract Full Text Show Details
Shift work sleep disorder ("SWSD")
TEVA PHARMACEUTICAL INDUSTRIES LTD.; TEVA PHARMACEUTICALS USA, INC.
Patent: WO2007/98273 A2, 2007 ; Title/Abstract Full Text Show Details
Obstructive sleep apnea/hypopnea syndrome ("OSA/HS")
TEVA PHARMACEUTICAL INDUSTRIES LTD.; TEVA PHARMACEUTICALS USA, INC.
Patent: WO2007/98273 A2, 2007 ; Title/Abstract Full Text Show Details
sleep related breathing disorder
Cypress Bioscience, Inc.
Patent: US2006/39866 A1, 2006 ; Title/Abstract Full Text Show Details
therapy
Cypress Bioscience, Inc.
Patent: US2006/39866 A1, 2006 ; Title/Abstract Full Text Show Details
pharmaceutical composition
Cypress Bioscience, Inc.
Patent: US2006/39866 A1, 2006 ; Title/Abstract Full Text Show Details
sleep apnea
Cypress Bioscience, Inc.
Patent: US2006/39866 A1, 2006 ; Title/Abstract Full Text Show Details
Hide facts Use Pattern
Reference
combination therapy
Cypress Bioscience, Inc.
Patent: US2006/39866 A1, 2006 ; Title/Abstract Full Text Show Details
daytime drowsiness
Cypress Bioscience, Inc.
Patent: US2006/39866 A1, 2006 ; Title/Abstract Full Text Show Details
Chemical Name: (+)-Modafinil Reaxys Registry Number: 9767971
Type of Substance: isocyclic Molecular Formula: C H NO S
12 prep out of 13 reactions.
Identification Physical Data (12) Spectra (11) Bioactivity (14) Other Data (2)
15
15 15
2
Linear Structure Formula: C15H15NO2S Molecular Weight: 273.356
InChI Key: YFGHCGITMMYXAQ-IBGZPJMESA-N 3
Synthesize | Hide Details Find similar Chemical Names and Synonyms (+)-Modafinil, (+)-modafinil, (S)-modafinil, armodafinil, d-modafinil, modafinil, OMO1-020 Identification Substance Label (4) Label
Reference
SMOD
Krasulova, Kristyna; Siller, Michal; Holas, Ondrej; Dvorak, Zdenek; Anzenbacher, Pavel
Xenobiotica, 2016 , vol. 46, # 4 p. 315 - 324 Title/Abstract Full Text View citing articles Show Details
(S)-2
Cao, Jianjing; Slack, Rachel D.; Bakare, Oluyomi M.; Burzynski, Caitlin; Rais, Rana; Slusher, Barbara S.; Kopajtic, Theresa; Bonifazi, Alessandro; Ellenberger, Michael P.; Yano, Hideaki; He, Yi; Bi, Guo-Hua; Xi, Zheng-Xiong; Loland, Claus J.; Newman, Amy Hauck
Journal of Medicinal Chemistry, 2016 , vol. 59, # 23 p. 10676 - 10691 Title/Abstract Full Text View citing articles Show Details
(S)(+)-3
Prisinzano, Thomas; Podobinski, John; Tidgewell, Kevin; Luo, Min; Swenson, Dale
Tetrahedron Asymmetry, 2004 , vol. 15, # 6 p. 1053 - 1058 Title/Abstract Full Text View citing articles Show Details
(+)(S)-1
Osorio-Lozada, Antonio; Prisinzano, Thomas; Olivo, Horacio F.
Tetrahedron Asymmetry, 2004 , vol. 15, # 23 p. 3811 - 3815 Title/Abstract Full Text View citing articles Show Details
Physical Data Melting Point (2) Melting Point
Solvent (Melting Point)
152.5 154 °C
di-isopropyl ether
Location
Reference
supporting information
Cao, Jianjing; Prisinzano, Thomas E.; Okunola, Oluyomi M.; Kopajtic, Theresa; Shook, Matthew; Katz, Jonathan L.; Newman, Amy Hauck
ACS Medicinal Chemistry Letters, 2011 , vol. 2, # 1 p. 48 - 52 Title/Abstract Full Text View citing articles Show Details
Olivo, Horacio F.; Osorio-Lozada, Antonio; Peeples, Tonya L.
Tetrahedron Asymmetry, 2005 , vol. 16, # 21 p. 3507 - 3511 Title/Abstract Full Text View citing articles Show Details
158 - 159 °C
Density (1) Density
Measurement Temperature
Type (Density)
Reference
1.342 g·cm-3
19.85 °C
crystallographic
In, Yasuko; Tomoo, Koji; Ishida, Toshimasa; Sakamoto, Yasuhiko
Chemical and Pharmaceutical Bulletin, 2004 , vol. 52, # 10 p. 1186 - 1189 Title/Abstract Full Text View citing articles Show Details
Crystal Phase (1) Description (Crystal Phase)
Temperature (Crystal Phase)
Reference
Crystal structure determination
19.85 °C
In, Yasuko; Tomoo, Koji; Ishida, Toshimasa; Sakamoto, Yasuhiko
Chemical and Pharmaceutical Bulletin, 2004 , vol. 52, # 10 p. 1186 - 1189 Title/Abstract Full Text View citing articles Show Details
Crystal Property Description (1) Colour & Other Properties
Location
Reference
white
supporting information
Cao, Jianjing; Prisinzano, Thomas E.; Okunola, Oluyomi M.; Kopajtic, Theresa; Shook, Matthew; Katz, Jonathan L.; Newman, Amy Hauck
ACS Medicinal Chemistry Letters, 2011 , vol. 2, # 1 p. 48 - 52 Title/Abstract Full Text View citing articles Show Details
Crystal System (1) Crystal System
Reference
monoclinic
In, Yasuko; Tomoo, Koji; Ishida, Toshimasa; Sakamoto, Yasuhiko
Chemical and Pharmaceutical Bulletin, 2004 , vol. 52, # 10 p. 1186 - 1189 Title/Abstract Full Text View citing articles Show Details
Interatomic Distances and Angles (1) Description
Comment (Interatomic Distances and Angles)
Reference
Interatomic distances and angles
Method of determination: Single crystal X-ray diffraction
In, Yasuko; Tomoo, Koji; Ishida, Toshimasa; Sakamoto, Yasuhiko
Chemical and Pharmaceutical Bulletin, 2004 , vol. 52, # 10 p. 1186 - 1189 Title/Abstract Full Text View citing articles Show Details
Optical Rotatory Power (4) Type (Optical Rotatory Power)
Concentration (Optical Rotatory Power)
Enantiomeric excess
Solvent (Optical Rotatory Power)
Optical Rotatory Power
Wavelength (Optical Rotatory Power)
Temperature (Optical Rotatory Power)
[alpha]
1.032 g/100ml
100 %ee
chloroform
78.5 deg
589 nm
26 °C
[alpha]
1.0 g/100ml
CHCl3
79 deg
589 nm
22 °C
Olivo, Horacio F.; Osorio-Lozada, Antonio; Peeples, Tonya L.
Tetrahedron Asymmetry, 2005 , vol. 16, # 21 p. 3507 - 3511 Title/Abstract Full Text View citing articles Show Details
[alpha]
0.99 g/100ml
CHCl3
76.7 deg
589 nm
22 °C
Prisinzano, Thomas; Podobinski, John; Tidgewell, Kevin; Luo, Min; Swenson, Dale
Tetrahedron Asymmetry, 2004 , vol. 15, # 6 p. 1053 - 1058 Title/Abstract Full Text View citing articles Show Details
[alpha]
1.0 g/100ml
CHCl3
81 deg
589 nm
22 °C
Osorio-Lozada, Antonio; Prisinzano, Thomas; Olivo, Horacio F.
Tetrahedron Asymmetry, 2004 , vol. 15, # 23 p. 3811 - 3815 Title/Abstract Full Text View citing articles Show Details
Location
Reference
supporting information
Cao, Jianjing; Prisinzano, Thomas E.; Okunola, Oluyomi M.; Kopajtic, Theresa; Shook, Matthew; Katz, Jonathan L.; Newman, Amy Hauck
ACS Medicinal Chemistry Letters, 2011 , vol. 2, # 1 p. 48 - 52 Title/Abstract Full Text View citing articles Show Details
Space Group (1) Space Group
Reference
4
In, Yasuko; Tomoo, Koji; Ishida, Toshimasa; Sakamoto, Yasuhiko
Chemical and Pharmaceutical Bulletin, 2004 , vol. 52, # 10 p. 1186 - 1189 Title/Abstract Full Text View citing articles Show Details
Spectra NMR Spectroscopy (10) Description (NMR Spectroscopy)
Nucleus (NMR Spectroscopy)
Chemical shifts
1H
Coupling Nuclei
Solvents (NMR Spectroscopy) dimethylsulfoxided6
Frequency (NMR Spectroscopy)
Location
Reference
supporting information
Cao, Jianjing; Prisinzano, Thomas E.; Okunola, Oluyomi M.; Kopajtic, Theresa; Shook, Matthew; Katz, Jonathan L.; Newman, Amy Hauck
ACS Medicinal Chemistry Letters, 2011 , vol. 2, # 1 p. 48 - 52 Title/Abstract Full Text View citing articles Show Details
13C
dimethylsulfoxided6
Chemical shifts
1H
dimethylsulfoxided6
300 MHz
Ternois, James; Guillen, Frederic; Plaquevent, Jean-Christophe; Coquerel, Gerard
Tetrahedron Asymmetry, 2007 , vol. 18, # 24 p. 2959 - 2964 Title/Abstract Full Text View citing articles Show Details
Chemical shifts
13C
dimethylsulfoxided6
75 MHz
Ternois, James; Guillen, Frederic; Plaquevent, Jean-Christophe; Coquerel, Gerard
Tetrahedron Asymmetry, 2007 , vol. 18, # 24 p. 2959 - 2964 Title/Abstract Full Text View citing articles Show Details
Chemical shifts
1H
CDCl3
Olivo, Horacio F.; Osorio-Lozada, Antonio; Peeples, Tonya L.
Tetrahedron Asymmetry, 2005 , vol. 16, # 21 p. 3507 - 3511 Title/Abstract Full Text View citing articles Show Details
CDCl3
Olivo, Horacio F.; Osorio-Lozada, Antonio; Peeples, Tonya L.
Tetrahedron Asymmetry, 2005 , vol. 16, # 21 p. 3507 - 3511 Title/Abstract Full Text View citing articles Show Details
1H
1H
supporting information
Cao, Jianjing; Prisinzano, Thomas E.; Okunola, Oluyomi M.; Kopajtic, Theresa; Shook, Matthew; Katz, Jonathan L.; Newman, Amy Hauck
ACS Medicinal Chemistry Letters, 2011 , vol. 2, # 1 p. 48 - 52 Title/Abstract Full Text View citing articles Show Details
Chemical shifts
Chemical shifts
13C
CDCl3
Olivo, Horacio F.; Osorio-Lozada, Antonio; Peeples, Tonya L.
Tetrahedron Asymmetry, 2005 , vol. 16, # 21 p. 3507 - 3511 Title/Abstract Full Text View citing articles Show Details
Chemical shifts
1H
dimethylsulfoxided6
Prisinzano, Thomas; Podobinski, John; Tidgewell, Kevin; Luo, Min; Swenson, Dale
Tetrahedron Asymmetry, 2004 , vol. 15, # 6 p. 1053 - 1058 Title/Abstract Full Text View citing articles Show Details
dimethylsulfoxided6
Prisinzano, Thomas; Podobinski, John; Tidgewell, Kevin; Luo, Min; Swenson, Dale
Tetrahedron Asymmetry, 2004 , vol. 15, # 6 p. 1053 - 1058 Title/Abstract Full Text View citing articles Show Details
dimethylsulfoxided6
Prisinzano, Thomas; Podobinski, John; Tidgewell, Kevin; Luo, Min; Swenson, Dale
Tetrahedron Asymmetry, 2004 , vol. 15, # 6 p. 1053 - 1058 Title/Abstract Full Text View citing articles Show Details
1H
Chemical shifts
13C
1H
IR Spectroscopy (1) Description (IR Spectroscopy)
Reference
Bands
Olivo, Horacio F.; Osorio-Lozada, Antonio; Peeples, Tonya L.
Tetrahedron Asymmetry, 2005 , vol. 16, # 21 p. 3507 - 3511 Title/Abstract Full Text View citing articles Show Details
Bioactivity Pharmacological Data (14) 1 of 14
Comment (Pharmacological Data)
Bioactivities present
Reference
Prisinzano, Thomas; Podobinski, John; Tidgewell, Kevin; Luo, Min; Swenson, Dale
Tetrahedron Asymmetry, 2004 , vol. 15, # 6 p. 1053 - 1058 Title/Abstract Full Text View citing articles Show Details
Osorio-Lozada, Antonio; Prisinzano, Thomas; Olivo, Horacio F.
Tetrahedron Asymmetry, 2004 , vol. 15, # 23 p. 3811 - 3815 Title/Abstract Full Text View citing articles Show Details
In, Yasuko; Tomoo, Koji; Ishida, Toshimasa; Sakamoto, Yasuhiko
Chemical and Pharmaceutical Bulletin, 2004 , vol. 52, # 10 p. 1186 - 1189 Title/Abstract Full Text View citing articles Show Details
Olivo, Horacio F.; Osorio-Lozada, Antonio; Peeples, Tonya L.
Tetrahedron Asymmetry, 2005 , vol. 16, # 21 p. 3507 - 3511 Title/Abstract Full Text View citing articles Show Details
Ternois, James; Guillen, Frederic; Plaquevent, Jean-Christophe; Coquerel, Gerard
Tetrahedron Asymmetry, 2007 , vol. 18, # 24 p. 2959 - 2964 Title/Abstract Full Text View citing articles Show Details
Zhu, Hao-Jie; Wang, Jun-Sheng; Donovan, Jennifer L.; Jiang, Yan; Gibson, Bryan B.; DeVane, C. Lindsay; Markowitz, John S.
European Journal of Pharmacology, 2008 , vol. 578, # 2-3 p. 148 - 158 Title/Abstract Full Text View citing articles Show Details
TEVA PHARMACEUTICAL INDUSTRIES LTD.; TEVA PHARMACEUTICALS USA, INC.
Patent: WO2008/70143 A1, 2008 ; Title/Abstract Full Text Show Details
Gome, Boaz
Patent: US2009/48464 A1, 2009 ;
Title/Abstract Full Text Show Details
Cao, Jianjing; Prisinzano, Thomas E.; Okunola, Oluyomi M.; Kopajtic, Theresa; Shook, Matthew; Katz, Jonathan L.; Newman, Amy Hauck
ACS Medicinal Chemistry Letters, 2011 , vol. 2, # 1 p. 48 - 52 Title/Abstract Full Text View citing articles Show Details
Stingl, Kerstin A.; Weiss, Katharina M.; Tsogoeva, Svetlana B.
Tetrahedron, 2012 , vol. 68, # 40 p. 8493 - 8501 Title/Abstract Full Text View citing articles Show Details
Ternois, James; Guillen, Frederic; Piacenza, Guy; Rose, Sebastien; Plaquevent, Jean-Christophe; Coquerel, Gerard
Organic Process Research and Development, 2008 , vol. 12, # 4 p. 614 - 617 Title/Abstract Full Text View citing articles Show Details
DEBREGEAS ET ASSOCIES PHARMA; Suplie, Pascal; Vivet, Philippe
Patent: US2015/73055 A1, 2015 ; Title/Abstract Full Text Show Details
Krasulova, Kristyna; Siller, Michal; Holas, Ondrej; Dvorak, Zdenek; Anzenbacher, Pavel
Xenobiotica, 2016 , vol. 46, # 4 p. 315 - 324 Title/Abstract Full Text View citing articles Show Details
CODEXIS, INC.; Ang, Ee Lui; Alvizo, Oscar; Behrouzian, Behnaz; Clay, Michael; Collier, Steven; Eberhard, Ellen; Fu, Fan Jaslyn; Song, Shiwei; Smith, Derek; Widegren, Magnus; Wilson, Robert; Xu, Junye; Zhu, Jun
Patent: US9267159 B2, 2016 ; Title/Abstract Full Text Show Details
Cao, Jianjing; Slack, Rachel D.; Bakare, Oluyomi M.; Burzynski, Caitlin; Rais, Rana; Slusher, Barbara S.; Kopajtic, Theresa; Bonifazi, Alessandro; Ellenberger, Michael P.; Yano, Hideaki; He, Yi; Bi, Guo-Hua; Xi, Zheng-Xiong; Loland, Claus J.; Newman, Amy Hauck
Journal of Medicinal Chemistry, 2016 , vol. 59, # 23 p. 10676 - 10691 Title/Abstract Full Text View citing articles Show Details
2 of 14
3 of 14
4 of 14
5 of 14
6 of 14
Comment (Pharmacological Data)
physiological behaviour discussed
Reference
Krasulova, Kristyna; Siller, Michal; Holas, Ondrej; Dvorak, Zdenek; Anzenbacher, Pavel
Xenobiotica, 2016 , vol. 46, # 4 p. 315 - 324 Title/Abstract Full Text View citing articles Show Details
Comment (Pharmacological Data)
physiological behaviour discussed
Reference
Cao, Jianjing; Slack, Rachel D.; Bakare, Oluyomi M.; Burzynski, Caitlin; Rais, Rana; Slusher, Barbara S.; Kopajtic, Theresa; Bonifazi, Alessandro; Ellenberger, Michael P.; Yano, Hideaki; He, Yi; Bi, Guo-Hua; Xi, Zheng-Xiong; Loland, Claus J.; Newman, Amy Hauck
Journal of Medicinal Chemistry, 2016 , vol. 59, # 23 p. 10676 - 10691 Title/Abstract Full Text View citing articles Show Details
Effect (Pharmacological Data)
monoamine transporter binding affinity
Species or Test-System (Pharmacological Data)
brain membranes of rat
Further Details (Pharmacological Data)
Ki related to: dopamine transporter
Type (Pharmacological Data)
Ki
Value of Type (Pharmacological Data)
7640 nmol/l
Reference
Cao, Jianjing; Prisinzano, Thomas E.; Okunola, Oluyomi M.; Kopajtic, Theresa; Shook, Matthew; Katz, Jonathan L.; Newman, Amy Hauck
ACS Medicinal Chemistry Letters, 2011 , vol. 2, # 1 p. 48 - 52 Title/Abstract Full Text View citing articles Show Details
Effect (Pharmacological Data)
monoamine transporter binding affinity
Species or Test-System (Pharmacological Data)
brain membranes of rat
Results
molecular target: dopamine transporter
Reference
Cao, Jianjing; Prisinzano, Thomas E.; Okunola, Oluyomi M.; Kopajtic, Theresa; Shook, Matthew; Katz, Jonathan L.; Newman, Amy Hauck
ACS Medicinal Chemistry Letters, 2011 , vol. 2, # 1 p. 48 - 52 Title/Abstract Full Text View citing articles Show Details
Effect (Pharmacological Data)
monoamine transporter binding affinity
Species or Test-System (Pharmacological Data)
brain membranes of rat
Concentration (Pharmacological Data)
<= 10 μmol/l
Results
no effect (related to serotonin transporter)
Reference
Cao, Jianjing; Prisinzano, Thomas E.; Okunola, Oluyomi M.; Kopajtic, Theresa; Shook, Matthew; Katz, Jonathan L.; Newman, Amy Hauck
ACS Medicinal Chemistry Letters, 2011 , vol. 2, # 1 p. 48 - 52 Title/Abstract Full Text View citing articles Show Details
7 of 14
8 of 14
9 of 14
10 of 14
11 of 14
Effect (Pharmacological Data)
monoamine transporter binding affinity
Species or Test-System (Pharmacological Data)
brain membranes of rat
Concentration (Pharmacological Data)
<= 10 μmol/l
Results
no effect (related to norepinephrine transporter)
Reference
Cao, Jianjing; Prisinzano, Thomas E.; Okunola, Oluyomi M.; Kopajtic, Theresa; Shook, Matthew; Katz, Jonathan L.; Newman, Amy Hauck
ACS Medicinal Chemistry Letters, 2011 , vol. 2, # 1 p. 48 - 52 Title/Abstract Full Text View citing articles Show Details
Effect (Pharmacological Data)
locomotor activity; effect on
Species or Test-System (Pharmacological Data)
mouse
Concentration (Pharmacological Data)
30 - 300 mg/kg
Type (Pharmacological Data)
maximal locomotor activity
Value of Type (Pharmacological Data)
Ca. 450 counts/min
Reference
Cao, Jianjing; Prisinzano, Thomas E.; Okunola, Oluyomi M.; Kopajtic, Theresa; Shook, Matthew; Katz, Jonathan L.; Newman, Amy Hauck
ACS Medicinal Chemistry Letters, 2011 , vol. 2, # 1 p. 48 - 52 Title/Abstract Full Text View citing articles Show Details
Effect (Pharmacological Data)
locomotor activity; effect on
Species or Test-System (Pharmacological Data)
mouse
Concentration (Pharmacological Data)
30 - 300 mg/kg
Type (Pharmacological Data)
time for maximal activity
Value of Type (Pharmacological Data)
1 h
Reference
Cao, Jianjing; Prisinzano, Thomas E.; Okunola, Oluyomi M.; Kopajtic, Theresa; Shook, Matthew; Katz, Jonathan L.; Newman, Amy Hauck
ACS Medicinal Chemistry Letters, 2011 , vol. 2, # 1 p. 48 - 52 Title/Abstract Full Text View citing articles Show Details
Effect (Pharmacological Data)
locomotor activity; effect on
Species or Test-System (Pharmacological Data)
mouse
Concentration (Pharmacological Data)
30 - 300 mg/kg
Type (Pharmacological Data)
dose for maximal activity
Value of Type (Pharmacological Data)
100 mg/kg
Reference
Cao, Jianjing; Prisinzano, Thomas E.; Okunola, Oluyomi M.; Kopajtic, Theresa; Shook, Matthew; Katz, Jonathan L.; Newman, Amy Hauck
ACS Medicinal Chemistry Letters, 2011 , vol. 2, # 1 p. 48 - 52 Title/Abstract Full Text View citing articles Show Details
Effect (Pharmacological Data)
P-glycoprotein activity; inhibition of
Species or Test-System (Pharmacological Data)
LLC-PK1/MDR1 cells
Concentration (Pharmacological Data)
10 - 100 μmol/l
Method (Pharmacological Data)
human P-glycoprotein overexpressing porcine kidney epithelial LLC-PK1 cells; after incubation with doxorubicin in the presence of title comp. for 1 h intracellular conc. of doxorubicin analyzed by HPLC
12 of 14
13 of 14
14 of 14
Further Details (Pharmacological Data)
control: 0.5percent dimethyl sulfoxide; positive control: PSC833 (2 μM), quinine (200 μM); P-glycoprotein negative parental LLC-PK1 cells used as negative control; efficiency of PSC833 was defined as 100percent
Comment (Pharmacological Data)
No effect
Reference
Zhu, Hao-Jie; Wang, Jun-Sheng; Donovan, Jennifer L.; Jiang, Yan; Gibson, Bryan B.; DeVane, C. Lindsay; Markowitz, John S.
European Journal of Pharmacology, 2008 , vol. 578, # 2-3 p. 148 - 158 Title/Abstract Full Text View citing articles Show Details
Effect (Pharmacological Data)
P-glycoprotein activity; inhibition of
Species or Test-System (Pharmacological Data)
LLC-PK1/MDR1 cells
Concentration (Pharmacological Data)
10 - 100 μmol/l
Method (Pharmacological Data)
human P-glycoprotein overexpressing porcine kidney epithelial LLC-PK1 cells; after incubation with rhodamine123 in the presence of title comp. for 1 h intracellular conc. of rhodamine123 analyzed by HPLC
Further Details (Pharmacological Data)
control: 0.5percent dimethyl sulfoxide; positive control: PSC833 (2 μM), quinine (200 μM); P-glycoprotein negative parental LLC-PK1 cells used as negative control; efficiency of PSC833 was defined as 100percent
Comment (Pharmacological Data)
No effect
Reference
Zhu, Hao-Jie; Wang, Jun-Sheng; Donovan, Jennifer L.; Jiang, Yan; Gibson, Bryan B.; DeVane, C. Lindsay; Markowitz, John S.
European Journal of Pharmacology, 2008 , vol. 578, # 2-3 p. 148 - 158 Title/Abstract Full Text View citing articles Show Details
Effect (Pharmacological Data)
transport
Species or Test-System (Pharmacological Data)
LLC-PK1/MDR1 cells
Concentration (Pharmacological Data)
20 μmol/l
Method (Pharmacological Data)
human P-glycoprotein overexpressing porcine kidney epithelial LLC-PK1 cells; after incubation with title comp. in the presence or absence of PSC833 (2 μM) for 1 h intracellular conc. of title comp. analyzed by HPLC
Further Details (Pharmacological Data)
control: 0.5percent dimethyl sulfoxide; positive control: doxorubicin, rhodamine123; P-glycoprotein negative parental LLC-PK1 cells used as negative control
Results
accumulation of title comp. in LLC-PK1 cells was higher than that in LLC-PK1/MDR1 cells; cotreatment with PSC833 increased (52.9percent) title comp. conc. in LLCPK1/MDR1 cells, suggesting that P-glycoprotein might play role in transport of title comp.; fig.
Reference
Zhu, Hao-Jie; Wang, Jun-Sheng; Donovan, Jennifer L.; Jiang, Yan; Gibson, Bryan B.; DeVane, C. Lindsay; Markowitz, John S.
European Journal of Pharmacology, 2008 , vol. 578, # 2-3 p. 148 - 158 Title/Abstract Full Text View citing articles Show Details
Effect (Pharmacological Data)
transport
Species or Test-System (Pharmacological Data)
LLC-PK1/MDR1 cell monolayers
Concentration (Pharmacological Data)
5 μmol/l
Method (Pharmacological Data)
human P-glycoprotein overexpressing porcine kidney epithelial LLC-PK1 cells; title comp. loaded into B or A side of monolayers; incubation in the presence or absence of PSC833 (2 μM); title comp. in receiver compartment analyzed by HPLC
Further Details (Pharmacological Data)
control: 0.5percent dimethyl sulfoxide; B: basolateral; A: apical; Papp B-A/Papp A-B: apparent permeability coefficient for B-A/A-B direction; PSC833: selective P-glycoprotein inhibitor; reference: rhodamine123 (Papp B-A-to-Papp A-B ratio = 11.11)
Results
Papp B-A-to-Papp A-B ratio was 1.24 in the absence and 0.85 in the presence of PSC833; fig.
Reference
Zhu, Hao-Jie; Wang, Jun-Sheng; Donovan, Jennifer L.; Jiang, Yan; Gibson, Bryan B.; DeVane, C. Lindsay; Markowitz, John S.
European Journal of Pharmacology, 2008 , vol. 578, # 2-3 p. 148 - 158 Title/Abstract Full Text View citing articles Show Details
Other Data Use (2) Use Pattern
Location
Reference
Pharmaceuticals
Page/Page column 6
DEBREGEAS ET ASSOCIES PHARMA; Suplie, Pascal; Vivet, Philippe
Patent: US2015/73055 A1, 2015 ; Title/Abstract Full Text Show Details
substitution treatment of cocaine addicts
Page/Page column 6
DEBREGEAS ET ASSOCIES PHARMA; Suplie, Pascal; Vivet, Philippe
Patent: US2015/73055 A1, 2015 ; Title/Abstract Full Text Show Details
Chemical Name: d-modafinil Reaxys Registry Number: 10016759
Type of Substance: isocyclic Molecular Formula: C15H15NO2S Linear Structure Formula: C15H15NO2S Molecular Weight: 273.356
InChI Key: YFGHCGITMMYXAQ-UHFFFAOYSA-N
1 prep out of 1 reactions.
Identification
1
3 prep out of 3 reactions.
Identification
2
4 prep
Physical
2
4
Synthesize | Hide Details Find similar Chemical Names and Synonyms d-modafinil, (+)-2-(diphenylmethyl)sulphinylacetamide, (+)-2-(benzhydrylsulphinyl)acetamide, (+)-modafinil Identification Patent-Specific Data (1) Related Markush Structure (RN)
Reference
12205109
CEPHALON FRANCE
Patent: EP1516869 A1, 2005 ; Title/Abstract Full Text Show Details
Chemical Name: l-modafinil Reaxys Registry Number: 10018841
Type of Substance: isocyclic Molecular Formula: C15H15NO2S Linear Structure Formula: C15H15NO2S Molecular Weight: 273.356
InChI Key: YFGHCGITMMYXAQ-UHFFFAOYSA-N 5
Synthesize | Hide Details Find similar Chemical Names and Synonyms l-modafinil, (-)-2-(diphenylmethyl)sulphinylacetamide, (-)-benzhydrylsulfinylacetamide, (-)-2-(benzhydrylsulphinyl)acetamide, (-)-modafinil, armodafinil Identification Patent-Specific Data (1) Related Markush Structure (RN)
Reference
12205109
CEPHALON FRANCE
Patent: EP1516869 A1, 2005 ; Title/Abstract Full Text Show Details
Chemical Name:
out of 7 reactions.
(-)-benzhydrylsulphinylacetamide Reaxys Registry Number: 11334026
Molecular Formula: C15H15NO2S Linear Structure Formula: C15H15NO2S Molecular Weight: 273.356
InChI Key: YFGHCGITMMYXAQ-UHFFFAOYSA-N
Data (3) Other Data (29)
6
Synthesize | Hide Details Find similar Chemical Names and Synonyms (-)-benzhydrylsulphinylacetamide, l-modafinil, (-)-modafinil, CRL 40982 Physical Data Melting Point (1) Melting Point
Solvent (Melting Point)
Reference
163 °C
ethanol toluene
Cephalon France; Organisation De Synthese Mondiale Orsymonde
Patent: US2006/135621 A1, 2006 ; Title/Abstract Full Text Show Details
Crystal Property Description (1) Colour & Other Properties
Reference
white
Cephalon France; Organisation De Synthese Mondiale Orsymonde
Patent: US2006/135621 A1, 2006 ; Title/Abstract Full Text Show Details
Optical Rotatory Power (1) Type (Optical Rotatory Power)
Solvent (Optical Rotatory Power)
Optical Rotatory Power
Wavelength (Optical Rotatory Power)
[alpha]
methanol
-18.6 deg
589 nm
Reference Cephalon France; Organisation De Synthese Mondiale Orsymonde
Patent: US2006/135621 A1, 2006 ; Title/Abstract Full Text Show Details
Other Data Use (29) Use Pattern
Reference
promoting CNS stimulation as an adrenergic agonist; activates glutamatergic circuits while inhibiting GABA; inhibits of dopamine reuptake, indirect inhibits of noradrenalin reuptake in the VLPO and orexin activation; has partial alpha 1B-adrenergic agonist effects by directly stimulating the receptors
NEUROHEALING PHARMACEUTICALS, INC.
Patent: WO2007/13962 A2, 2007 ; Title/Abstract Full Text Show Details
promoting or enhancing the state of wakefulness
NEUROHEALING PHARMACEUTICALS, INC.
Patent: WO2007/13962 A2, 2007 ; Title/Abstract Full Text Show Details
promoting or enhancing the state of alertness
NEUROHEALING PHARMACEUTICALS, INC.
Patent: WO2007/13962 A2, 2007 ;
Title/Abstract Full Text Show Details
central nervous system stimulation
NEUROHEALING PHARMACEUTICALS, INC.
Patent: WO2007/13962 A2, 2007 ; Title/Abstract Full Text Show Details
excessive daytime sleepiness (EDS)
NEUROHEALING PHARMACEUTICALS, INC.
Patent: WO2007/13962 A2, 2007 ; Title/Abstract Full Text Show Details
individuals who suffer from narcolepsy
NEUROHEALING PHARMACEUTICALS, INC.
Patent: WO2007/13962 A2, 2007 ; Title/Abstract Full Text Show Details
promoting a patient's recovery from anesthesia
NEUROHEALING PHARMACEUTICALS, INC.
Patent: WO2007/13962 A2, 2007 ; Title/Abstract Full Text Show Details
attention deficit disorder (ADD)
NEUROHEALING PHARMACEUTICALS, INC.
Patent: WO2007/13962 A2, 2007 ; Title/Abstract Full Text Show Details
attention deficit hyperactivity disorder (ADHD)
NEUROHEALING PHARMACEUTICALS, INC.
Patent: WO2007/13962 A2, 2007 ; Title/Abstract Full Text Show Details
neurorehabilitation program
NEUROHEALING PHARMACEUTICALS, INC.
Patent: WO2007/13962 A2, 2007 ; Title/Abstract Full Text Show Details
treat an impaired neurological function
NEUROHEALING PHARMACEUTICALS, INC.
Patent: WO2007/13962 A2, 2007 ; Title/Abstract Full Text Show Details
Parkinson's disease
Cephalon France; Organisation De Synthese Mondiale Orsymonde
Patent: US2006/135621 A1, 2006 ; Title/Abstract Full Text Show Details
depression, the depressive condition associated with low exposure to sunlight, schizophrenia, rotating shift working, time shifts
Cephalon France; Organisation De Synthese Mondiale Orsymonde
Patent: US2006/135621 A1, 2006 ; Title/Abstract Full Text Show Details
disturbances of the central nervous system
Cephalon France; Organisation De Synthese Mondiale Orsymonde
Patent: US2006/135621 A1, 2006 ; Title/Abstract Full Text Show Details
Cephalon France; Organisation De Synthese Mondiale Orsymonde
Patent: US2006/135621 A1, 2006 ;
eating disturbances
Title/Abstract Full Text Show Details
Cephalon France; Organisation De Synthese Mondiale Orsymonde
Patent: US2006/135621 A1, 2006 ;
excessive somnolence associated with a disease
Title/Abstract Full Text Show Details
Cephalon France; Organisation De Synthese Mondiale Orsymonde
Patent: US2006/135621 A1, 2006 ;
excessive somnolence associated with narcolepsy
Title/Abstract Full Text Show Details
Cephalon France; Organisation De Synthese Mondiale Orsymonde
Patent: US2006/135621 A1, 2006 ;
excessive somnolence
Title/Abstract Full Text Show Details
Cephalon France; Organisation De Synthese Mondiale Orsymonde
Patent: US2006/135621 A1, 2006 ;
hypersomnia in patients affected by a cancer treated by morphine analgesics to relieve pain
Title/Abstract Full Text Show Details
Cephalon France; Organisation De Synthese Mondiale Orsymonde
Patent: US2006/135621 A1, 2006 ;
idiopathic hypersomnia
Title/Abstract Full Text Show Details
Use Pattern
Reference
narcolepsy
Cephalon France; Organisation De Synthese Mondiale Orsymonde
Patent: US2006/135621 A1, 2006 ; Title/Abstract Full Text Show Details
obstructive sleep apnoeas
Cephalon France; Organisation De Synthese Mondiale Orsymonde
Patent: US2006/135621 A1, 2006 ; Title/Abstract Full Text Show Details
protection of the cerebral tissue against alertness disturbances associated with Steinert's disease
Cephalon France; Organisation De Synthese Mondiale Orsymonde
Patent: US2006/135621 A1, 2006 ; Title/Abstract Full Text Show Details
protection of the cerebral tissue against alertness disturbances, associated with hyperactivity (ADHD)
Cephalon France; Organisation De Synthese Mondiale Orsymonde
Patent: US2006/135621 A1, 2006 ; Title/Abstract Full Text Show Details
protection of the cerebral tissue against alertness disturbances
Cephalon France; Organisation De Synthese Mondiale Orsymonde
Patent: US2006/135621 A1, 2006 ; Title/Abstract Full Text Show Details
protection of the cerebral tissue against ischaemia
Cephalon France; Organisation De Synthese Mondiale Orsymonde
Patent: US2006/135621 A1, 2006 ; Title/Abstract Full Text Show Details
sleep apnoeas
Cephalon France; Organisation De Synthese Mondiale Orsymonde
Patent: US2006/135621 A1, 2006 ;
Title/Abstract Full Text Show Details
Cephalon France; Organisation De Synthese Mondiale Orsymonde
Patent: US2006/135621 A1, 2006 ;
somnolence
Title/Abstract Full Text Show Details
the condition of fatigue, in particular that associated with multiple sclerosis and other degenerative diseases
Cephalon France; Organisation De Synthese Mondiale Orsymonde
Patent: US2006/135621 A1, 2006 ; Title/Abstract Full Text Show Details
Chemical Name: (d)-(+)-modafinil Reaxys Registry Number: 14566857
Molecular Formula: C15H15NO2S Linear Structure Formula: C15H15NO2S Molecular Weight: 273.356
InChI Key: YFGHCGITMMYXAQ-UHFFFAOYSA-N
3 prep out of 3 reactions.
7
Synthesize | Hide Details Find similar Chemical Names and Synonyms (d)-(+)-modafinil, (+)-benzhydrylsulphinylacetamide, (+)-modafinil, d-modafinil, CRL 40983 Bioactivity Pharmacological Data (4) 1 of 4
Comment (Pharmacological Data)
Bioactivities present
Reference
CEPHALON FRANCE; ORGANISATION DE SYNTHESE MONDIALE ORSYMONDE
Patent: WO2004/14846 A1, 2004 ; Title/Abstract Full Text Show Details
CENTRE FOR ADDICTION AND MENTAL HEALTH
Patent: WO2006/32146 A1, 2006 ; Title/Abstract Full Text Show Details
Cephalon France; Organisation De Synthese Mondiale Orsymonde
Patent: US2006/135621 A1, 2006 ; Title/Abstract Full Text Show Details
Feuerstein, Seth; Coric, Vladimir
Patent: US2006/167068 A1, 2006 ; Title/Abstract Full Text Show Details
NEUROHEALING PHARMACEUTICALS, INC.
Patent: WO2007/13962 A2, 2007 ; Title/Abstract Full Text Show Details
BrainCells, Inc.
Patent: US2007/270449 A1, 2007 ; Title/Abstract Full Text Show Details
NEUROHEALING PHARMACEUTICALS, INC.
Patent: WO2008/21341 A2, 2008 ; Title/Abstract Full Text Show Details
BrainCells, Inc.
Patent: US2008/64671 A1, 2008 ; Title/Abstract Full Text Show Details
Saletu; Frey; Krupka; Anderer; Grunberger; Barbanoj
Arzneimittel-Forschung/Drug Research, 1989 , vol. 39, # 10 p. 1268 - 1273 Title/Abstract Full Text View citing articles Show Details
Ferraro, Luca; Tanganelli, Sergio; O'Connor, William Thomas; Antonelli, Tiziana; Rambert, Francis; Fuxe, Kjell
European Journal of Pharmacology, 1996 , vol. 306, # 1-3 p. 33 - 39
Bioactivity (4) Other Data (29)
25
Title/Abstract Full Text View citing articles Show Details
Edgar, Dale M.; Seidel, Wesley F.
Journal of Pharmacology and Experimental Therapeutics, 1997 , vol. 283, # 2 p. 757 - 769 Title/Abstract Full Text View citing articles Show Details
Heitmann, Joerg; Cassel, Werner; Grote, Ludger; Bickel, Ulrich; Hartlaub, Udo; Penzel, Thomas; Peter, Joerg Hermann
Clinical Pharmacology and Therapeutics, 1999 , vol. 65, # 3 p. 328 - 335 Title/Abstract Full Text View citing articles Show Details
Taneja, Indu; Bruehl, Stephen; Robertson, David
Journal of Clinical Pharmacology, 2004 , vol. 44, # 12 p. 1425 - 1427 Title/Abstract Full Text View citing articles Show Details
Wong, Y. Nancy; King, S. Peter; Simcoe, Donna; Gorman, Steve; Laughton, Watson; McCormick, George C.; Grebow, Peter
Journal of Clinical Pharmacology, 1999 , vol. 39, # 3 p. 281 - 288 Title/Abstract Full Text View citing articles Show Details
Webb, Ian C.; Pollock, Michael S.; Mistlberger, Ralph E.
Journal of Pharmacology and Experimental Therapeutics, 2006 , vol. 317, # 2 p. 882 - 889 Title/Abstract Full Text View citing articles Show Details
Madras, Bertha K.; Xie, Zhihua; Lin, Zhicheng; Jassen, Amy; Panas, Helen; Lynch, Laurie; Johnson, Ryan; Livni, Eli; Spencer, Thomas J.; Bonab, Ali A.; Miller, Gregory M.; Fischman, Alan J.
Journal of Pharmacology and Experimental Therapeutics, 2006 , vol. 319, # 2 p. 561 - 569 Title/Abstract Full Text View citing articles Show Details
Parmentier; Anaclet; Guhennec; Brousseau; Bricout; Giboulot; Bozyczko-Coyne; Spiegel; Ohtsu; Williams; Lin
Biochemical Pharmacology, 2007 , vol. 73, # 8 p. 1157 - 1171 Title/Abstract Full Text View citing articles Show Details
Dopheide, Marsha M.; Morgan, Russell E.; Rodvelt, Kelli R.; Schachtman, Todd R.; Miller, Dennis K.
European Journal of Pharmacology, 2007 , vol. 568, # 1-3 p. 112 - 123 Title/Abstract Full Text View citing articles Show Details
Ishizuka, Tomoko; Murakami, Masahiro; Yamatodani, Atsushi
European Journal of Pharmacology, 2008 , vol. 578, # 2-3 p. 209 - 215 Title/Abstract Full Text View citing articles Show Details
LAVIN, Thomas, N.
Patent: WO2008/77127 A2, 2008 ; Title/Abstract Full Text Show Details
2 of 4
Comment (Pharmacological Data)
Bioactivities present
Reference
The Board of Trustees of the University of Arkansas
Patent: US2008/221216 A1, 2008 ; Title/Abstract Full Text Show Details
Vincent, Fabien; Nguyen, Margaret T.; Emerling, Daniel E.; Kelly, Michael G.; Duncton, Matthew A.J.
Bioorganic and Medicinal Chemistry Letters, 2009 , vol. 19, # 23 p. 6793 - 6796 Title/Abstract Full Text View citing articles Show Details
Paterson, Neil E.; Fedolak, Allison; Olivier, Berend; Hanania, Taleen; Ghavami, Afshin; Caldarone, Barbara
Pharmacology Biochemistry and Behavior, 2010 , vol. 95, # 4 p. 449 - 456 Title/Abstract Full Text View citing articles Show Details
Dunn, Derek; Hostetler, Greg; Iqbal, Mohamed; Marcy, Val R.; Lin, Yin Guo; Jones, Bruce; Aimone, Lisa D.; Gruner, John; Ator, Mark A.; Bacon, Edward R.; Chatterjee, Sankar
Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 11 p. 3751 - 3753 Title/Abstract Full Text View citing articles Show Details
Tanganelli; Perez de la Mora; Ferraro; Mendez-Franco; Beani; Rambert; Fuxe
European Journal of Pharmacology, 1995 , vol. 273, # 1-2 p. 63 - 71 Title/Abstract Full Text Show Details
3 of 4
Effect (Pharmacological Data)
wakefulness; effect on
Species or Test-System (Pharmacological Data)
human
Route of Application
sublingual
Method (Pharmacological Data)
Double blind study of sub-lingual d-modafinil composition in a normal human volunteer.The goal of this test was to confirm the suitability of the sublingual formulation and to ascertain if the purported short acting d-modafinil test article, under conditions of being very tired near to bedtime, had an affect on wakefulness.The test subject was given three vials: one vial containing the base formulation (as in Example 1) to test the taste and delivery means, and two coded vials. One of the coded vials contained 100 mg of d-modafinil formulation, and the second coded vial contained placebo (an equivalent amount of formulation).The subject was instructed to place the contents of the test formulation under the tongue, to allow the formulation to dissolve over two minutes, and to rinse any residual material with some water. ResultsSubject reported that the taste of the base formulation was pronounced, but tolerable. At 11 : 15 p.m. in the evening, the contents of one coded vial was placed under the tongue, allowed to dissolve over two minutes, and any residual was rinsed with some water. A strong taste remained for some time. The test subject then reported reading in bed, dozing on and off for EPO approximately 1.5 hours. After the room was darkened, the subject reported sleeping lighter, and awakening at least once at 3:15 a.m. during the night.On a following evening at 11 : 15 p.m., the contents of the second coded vial was similarly placed under the tongue, allowed to dissolve over two minutes under the tongue and rinsed. The test subject reported reading in bed until 12:50 a.m., then darkening the room and sleeping undisturbed all night until the morning.At both evenings the test subject reported being equally very tired. Approximately one week before these tests, the same subject took 200 mg racemic modafinil (Provigil.(R).) at 10 p.m. and reported a very pronounced effect, essentially being keep awake through the night to 5 a.m. Before unblinding the test articles, the subject recorded that one of the test articles was active, but neither test substance kept him awake as strongly or as long as the 200 mg racemic modafinil. After unblinding the test articles, it was confirmed that the coded vial with the reported activity contained 100 mg d-modafnil.
Results
subject recorded that 100 mg of test compound kept him awake as strongly or as long as the 200 mg racemic modafinil
Location
Page/Page column 20; 21
Reference
NEUROHEALING PHARMACEUTICALS, INC.
Patent: WO2007/13962 A2, 2007 ; Title/Abstract Full Text Show Details
4 of 4
Effect (Pharmacological Data)
fall asleep; effect on
Route of Application
sublingual
Method (Pharmacological Data)
Double blind crossover study of sub-lingual d-modafinil in normal human volunteers.Two subjects received a set of coded vials containing either 200 mg of d-modafinil formulated according to Example 1 or an equivalent placebo formulation.The subjects were given the following instructions:Start testing at approximately the same time every evening, one hour before bedtime. Randomly select one of the coded vials each day.Open the vials and place the powder under your tongue.Allow the powder to dissolve slowly for approximately 1-2 minutes.After the powder is fully dissolved, you may drink some water.Record observations in a Visual Analogue Scale (VAS) describing the difficulty to fall asleep.Visual Analog Scale (0 to 3)Normal Kept awake, ability to sleep difficult to fall asleep0 1 2 3 0: fell asleep as usual1: slight, noticeable change2: noticeable change3: extreme change (kept awake most of night)Results from Subject 1Observations from vial with code no. 33 (later described as placebo): VAS = 0. No effect noticed. Went to bed at usual time and fell asleep as usual. EPO Observations from the second coded vial (later described as containing 200 mg of dmodafinil): VAS = I. It took longer than usual to fall asleep. Subject awoke several times during the night and felt more awake. Results from Subject 2 Observations from one coded vial (later described as placebo): VAS = 0. No effect noticed. Subject went to bed at usual time and fell asleep as usual.Observations from the second coded vial (later described as containing 200 mg of d- modafinil): VAS = 2. Subject reported that it took longer than usual to fall asleep. Subject reported that he usually falls asleep within a few minutes of reclining, but was significantly more alert after taking the contents of this vial (later revealed as containing 200 mg d-modafinil). After falling asleep, subject awoke several times during the night and after awaking, subject reported that it took a long time to fall asleep again.
Results
in test compound treatment conditions sleep is slight, noticeable change (VAS = 1) or it is noticeable change (VAS = 2); for placebo no effect noticed
Location
Page/Page column 21; 22
Reference
NEUROHEALING PHARMACEUTICALS, INC.
Patent: WO2007/13962 A2, 2007 ; Title/Abstract Full Text Show Details
Other Data Use (29) Use Pattern
Reference
promoting CNS stimulation as an adrenergic agonist; activates glutamatergic circuits while inhibiting GABA; inhibits of dopamine reuptake, indirect inhibits of noradrenalin reuptake in the VLPO and orexin activation; has partial alpha 1B-adrenergic agonist effects by directly stimulating the receptors
NEUROHEALING PHARMACEUTICALS, INC.
Patent: WO2007/13962 A2, 2007 ; Title/Abstract Full Text Show Details
promoting or enhancing the state of wakefulness
NEUROHEALING PHARMACEUTICALS, INC.
Patent: WO2007/13962 A2, 2007 ; Title/Abstract Full Text Show Details
promoting or enhancing the state of alertness
NEUROHEALING PHARMACEUTICALS, INC.
Patent: WO2007/13962 A2, 2007 ; Title/Abstract Full Text Show Details
central nervous system stimulation
NEUROHEALING PHARMACEUTICALS, INC.
Patent: WO2007/13962 A2, 2007 ; Title/Abstract Full Text Show Details
excessive daytime sleepiness (EDS)
NEUROHEALING PHARMACEUTICALS, INC.
Patent: WO2007/13962 A2, 2007 ; Title/Abstract Full Text Show Details
individuals who suffer from narcolepsy
NEUROHEALING PHARMACEUTICALS, INC.
Patent: WO2007/13962 A2, 2007 ; Title/Abstract Full Text Show Details
promoting a patient's recovery from anesthesia
NEUROHEALING PHARMACEUTICALS, INC.
Patent: WO2007/13962 A2, 2007 ; Title/Abstract Full Text Show Details
attention deficit disorder (ADD)
NEUROHEALING PHARMACEUTICALS, INC.
Patent: WO2007/13962 A2, 2007 ; Title/Abstract Full Text Show Details
attention deficit hyperactivity disorder (ADHD)
NEUROHEALING PHARMACEUTICALS, INC.
Patent: WO2007/13962 A2, 2007 ; Title/Abstract Full Text Show Details
neurorehabilitation program
NEUROHEALING PHARMACEUTICALS, INC.
Patent: WO2007/13962 A2, 2007 ; Title/Abstract Full Text Show Details
treat an impaired neurological function
NEUROHEALING PHARMACEUTICALS, INC.
Patent: WO2007/13962 A2, 2007 ; Title/Abstract Full Text Show Details
Parkinson's disease
Cephalon France; Organisation De Synthese Mondiale Orsymonde
Patent: US2006/135621 A1, 2006 ; Title/Abstract Full Text Show Details
depression, the depressive condition associated with low exposure to sunlight, schizophrenia, rotating shift working, time shifts
Cephalon France; Organisation De Synthese Mondiale Orsymonde
Patent: US2006/135621 A1, 2006 ; Title/Abstract Full Text Show Details
disturbances of the central nervous system
Cephalon France; Organisation De Synthese Mondiale Orsymonde
Patent: US2006/135621 A1, 2006 ; Title/Abstract Full Text Show Details
eating disturbances
Cephalon France; Organisation De Synthese Mondiale Orsymonde
Patent: US2006/135621 A1, 2006 ; Title/Abstract Full Text Show Details
excessive somnolence associated with a disease
Cephalon France; Organisation De Synthese Mondiale Orsymonde
Patent: US2006/135621 A1, 2006 ; Title/Abstract Full Text Show Details
excessive somnolence associated with narcolepsy
Cephalon France; Organisation De Synthese Mondiale Orsymonde
Patent: US2006/135621 A1, 2006 ; Title/Abstract Full Text Show Details
excessive somnolence
Cephalon France; Organisation De Synthese Mondiale Orsymonde
Patent: US2006/135621 A1, 2006 ; Title/Abstract Full Text Show Details
hypersomnia in patients affected by a cancer treated by morphine analgesics to relieve pain
Cephalon France; Organisation De Synthese Mondiale Orsymonde
Patent: US2006/135621 A1, 2006 ;
Title/Abstract Full Text Show Details
Cephalon France; Organisation De Synthese Mondiale Orsymonde
Patent: US2006/135621 A1, 2006 ;
idiopathic hypersomnia
Title/Abstract Full Text Show Details
Use Pattern
Reference
narcolepsy
Cephalon France; Organisation De Synthese Mondiale Orsymonde
Patent: US2006/135621 A1, 2006 ; Title/Abstract Full Text Show Details
Cephalon France; Organisation De Synthese Mondiale Orsymonde
Patent: US2006/135621 A1, 2006 ;
obstructive sleep apnoeas
Title/Abstract Full Text Show Details
protection of the cerebral tissue against alertness disturbances associated with Steinert's disease
Cephalon France; Organisation De Synthese Mondiale Orsymonde
Patent: US2006/135621 A1, 2006 ; Title/Abstract Full Text Show Details
protection of the cerebral tissue against alertness disturbances, associated with hyperactivity (ADHD)
Cephalon France; Organisation De Synthese Mondiale Orsymonde
Patent: US2006/135621 A1, 2006 ; Title/Abstract Full Text Show Details
protection of the cerebral tissue against alertness disturbances
Cephalon France; Organisation De Synthese Mondiale Orsymonde
Patent: US2006/135621 A1, 2006 ; Title/Abstract Full Text Show Details
Cephalon France; Organisation De Synthese Mondiale Orsymonde
Patent: US2006/135621 A1, 2006 ;
protection of the cerebral tissue against ischaemia
Title/Abstract Full Text Show Details
Cephalon France; Organisation De Synthese Mondiale Orsymonde
Patent: US2006/135621 A1, 2006 ;
sleep apnoeas
Title/Abstract Full Text Show Details
Cephalon France; Organisation De Synthese Mondiale Orsymonde
Patent: US2006/135621 A1, 2006 ;
somnolence
Title/Abstract Full Text Show Details
the condition of fatigue, in particular that associated with multiple sclerosis and other degenerative diseases
Cephalon France; Organisation De Synthese Mondiale Orsymonde
Patent: US2006/135621 A1, 2006 ; Title/Abstract Full Text Show Details
Chemical Name: 2-benzhydrylsulfinylacetamide Reaxys Registry Number: 27373978
Molecular Formula: C15H15NO2S Linear Structure Formula: C15H15NO2S Molecular Weight: 273.356
InChI Key: YFGHCGITMMYXAQ-UHFFFAOYSA-N 8
Synthesize | Hide Details
no reactions.
Physical Data (5)
1
Find similar Chemical Names and Synonyms 2-benzhydrylsulfinylacetamide, (±)-modafinil, 2-((diphenylmethyl)sulfinyl)acetamide Physical Data Density (1) Density
Type (Density)
Reference
1.339 g·cm-3
crystallographic
Mahieux, Julien; Sanselme, Morgane; Coquerel, Gerard
Crystal Growth and Design, 2013 , vol. 13, # 2 p. 908 - 917 Title/Abstract Full Text View citing articles Show Details
Conformation (1) Object of Investigation
Reference
Conformation
Mahieux, Julien; Sanselme, Morgane; Coquerel, Gerard
Crystal Growth and Design, 2013 , vol. 13, # 2 p. 908 - 917 Title/Abstract Full Text View citing articles Show Details
Crystal Phase (1) Description (Crystal Phase)
Reference
Structure of the solid
Mahieux, Julien; Sanselme, Morgane; Coquerel, Gerard
Crystal Growth and Design, 2013 , vol. 13, # 2 p. 908 - 917 Title/Abstract Full Text View citing articles Show Details
Crystal System (1) Crystal System
Reference
Rhombic
Mahieux, Julien; Sanselme, Morgane; Coquerel, Gerard
Crystal Growth and Design, 2013 , vol. 13, # 2 p. 908 - 917 Title/Abstract Full Text View citing articles Show Details
Space Group (1) Space Group
Comment (Space Group)
Reference
43
a = 18.172 Å; b = 52.375 Å; c = 5.698 Å; Z = 16; Method = Single crystal X-ray diffraction
Mahieux, Julien; Sanselme, Morgane; Coquerel, Gerard
Crystal Growth and Design, 2013 , vol. 13, # 2 p. 908 - 917 Title/Abstract Full Text View citing articles Show Details
Reaxys Registry Number: 18954088
CAS Registry Number: 1134802-56-4 Molecular Formula: C15H15NO2S Linear Structure Formula: C15H14(2)HNO2S
Molecular Weight: 274.348
InChI Key: YFGHCGITMMYXAQ-QPHVJCBYSA-N
9
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Identification Substance Label (1) Label
Reference
no reactions.
Identification
1
PROTIA, LLC
Patent: US2009/82462 A1, 2009 ;
12
Title/Abstract Full Text Show Details
Patent-Specific Data (1) Prophetic Compound
Related Markush Structure (RN)
Location in Patent
Reference
prophetic product
18954085
Page/page column 6
PROTIA, LLC
Patent: US2009/82462 A1, 2009 ; Title/Abstract Full Text Show Details
Reaxys Registry Number: 18954081
Molecular Formula: C15H15NO2S Linear Structure Formula: C15H13(2)H2NO2S
no reactions.
Identification
1
Identification
1
Molecular Weight: 275.34
InChI Key: YFGHCGITMMYXAQ-ZSJDYOACSA-N
10
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Identification Substance Label (1) Label
Reference
7
PROTIA, LLC
Patent: US2009/82461 A1, 2009 ; Title/Abstract Full Text Show Details
Patent-Specific Data (1) Prophetic Compound
Related Markush Structure (RN)
Location in Patent
Reference
prophetic product
18954080
Page/page column 5
PROTIA, LLC
Patent: US2009/82461 A1, 2009 ; Title/Abstract Full Text Show Details
Reaxys Registry Number: 18954086
Molecular Formula: C15H15NO2S Linear Structure Formula: C15H13(2)H2NO2S
Molecular Weight: 275.34
InChI Key: YFGHCGITMMYXAQ-BVFGSHTCSA-N
11
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Identification
no reactions.
Substance Label (1) Label
Reference
9
PROTIA, LLC
Patent: US2009/82462 A1, 2009 ; Title/Abstract Full Text Show Details
Patent-Specific Data (1) Prophetic Compound
Related Markush Structure (RN)
Location in Patent
Reference
prophetic product
18954085
Page/page column 5
PROTIA, LLC
Patent: US2009/82462 A1, 2009 ; Title/Abstract Full Text Show Details
Reaxys Registry Number: 18954087
CAS Registry Number: 1134802-54-2 Molecular Formula: C15H15NO2S Linear Structure Formula: C15H13(2)H2NO2S
no reactions.
Identification
1
Identification
1
Molecular Weight: 275.34
InChI Key: YFGHCGITMMYXAQ-OMVVLXAOSA-N
12
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Reference
10
PROTIA, LLC
Patent: US2009/82462 A1, 2009 ; Title/Abstract Full Text Show Details
Patent-Specific Data (1) Prophetic Compound
Related Markush Structure (RN)
Location in Patent
Reference
prophetic product
18954085
Page/page column 5
PROTIA, LLC
Patent: US2009/82462 A1, 2009 ; Title/Abstract Full Text Show Details
Reaxys Registry Number: 18954082
CAS Registry Number: 1133712-37-4 Molecular Formula: C15H15NO2S Linear Structure Formula: C15H12(2)H3NO2S
Molecular Weight: 276.332
InChI Key: YFGHCGITMMYXAQ-WVYCSPNRSA-N
13
Synthesize | Hide Details
no reactions.
Find similar
Identification Substance Label (1) Label
Reference
8
PROTIA, LLC
Patent: US2009/82461 A1, 2009 ; Title/Abstract Full Text Show Details
Patent-Specific Data (1) Prophetic Compound
Related Markush Structure (RN)
Location in Patent
Reference
prophetic product
18954080
Page/page column 5
PROTIA, LLC
Patent: US2009/82461 A1, 2009 ; Title/Abstract Full Text Show Details
Reaxys Registry Number: 18954089
Molecular Formula: C15H15NO2S Linear Structure Formula: C15H11(2)H4NO2S
no reactions.
Identification
1
Identification
1
Molecular Weight: 277.324
InChI Key: YFGHCGITMMYXAQ-XIYWSUDRSA-N
14
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Reference
11
PROTIA, LLC
Patent: US2009/82462 A1, 2009 ; Title/Abstract Full Text Show Details
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prophetic product
18954085
Page/page column 6
PROTIA, LLC
Patent: US2009/82462 A1, 2009 ; Title/Abstract Full Text Show Details
Reaxys Registry Number: 18954083
CAS Registry Number: 1133712-38-5 Molecular Formula: C15H15NO2S Linear Structure Formula: C15H10(2)H5NO2S
Molecular Weight: 278.316
InChI Key: YFGHCGITMMYXAQ-DYVTXVBDSA-N
15
no reactions.
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Reference
9; 10
PROTIA, LLC
Patent: US2009/82461 A1, 2009 ; Title/Abstract Full Text Show Details
Patent-Specific Data (1) Prophetic Compound
Related Markush Structure (RN)
Location in Patent
Reference
prophetic product
18954080
Page/page column 5
PROTIA, LLC
Patent: US2009/82461 A1, 2009 ; Title/Abstract Full Text Show Details
Reaxys Registry Number: 18954090
CAS Registry Number: 1134802-57-5 Molecular Formula: C15H15NO2S Linear Structure Formula: C15H10(2)H5NO2S
no reactions.
Molecular Weight: 278.316
InChI Key: YFGHCGITMMYXAQ-AOLFJIHXSA-N
16
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Reference
13; 14
PROTIA, LLC
Patent: US2009/82462 A1, 2009 ; Title/Abstract Full Text Show Details
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prophetic product
18954085
Page/page column 6
PROTIA, LLC
Identification
1
Patent: US2009/82462 A1, 2009 ; Title/Abstract Full Text Show Details
Chemical Name: 2-[(R)-(diphenylmethyl)sulfinyl]acetamide hemihydrate Reaxys Registry Number: 15558297
Molecular Formula: C15H15NO2S*0H2O Linear Structure Formula: C15H15NO2S*0.5H2O Molecular Weight: 282.363
InChI Key: TVIKTWOEQIEYMH-FSRHSHDFSA-N
1 prep out of 1 reactions.
Other Data (4)
1
Identification
1
17
Synthesize | Hide Details Find similar Chemical Names and Synonyms 2-[(R)-(diphenylmethyl)sulfinyl]acetamide hemihydrate, Armondafinil hemihydrate Other Data Use (4) Use Pattern
Reference
Excessive sleepiness
TEVA PHARMACEUTICAL INDUSTRIES LTD.; TEVA PHARMACEUTICALS USA, INC.
Patent: WO2007/98273 A2, 2007 ; Title/Abstract Full Text Show Details
Excessive sleepiness associated with narcolepsy
TEVA PHARMACEUTICAL INDUSTRIES LTD.; TEVA PHARMACEUTICALS USA, INC.
Patent: WO2007/98273 A2, 2007 ; Title/Abstract Full Text Show Details
Shift work sleep disorder ("SWSD")
TEVA PHARMACEUTICAL INDUSTRIES LTD.; TEVA PHARMACEUTICALS USA, INC.
Patent: WO2007/98273 A2, 2007 ; Title/Abstract Full Text Show Details
Obstructive sleep apnea/hypopnea syndrome ("OSA/HS")
TEVA PHARMACEUTICAL INDUSTRIES LTD.; TEVA PHARMACEUTICALS USA, INC.
Patent: WO2007/98273 A2, 2007 ; Title/Abstract Full Text Show Details
Reaxys Registry Number: 18954084
Molecular Formula: C15H15NO2S Linear Structure Formula: C15(2)H15NO2S
Molecular Weight: 288.236
InChI Key: YFGHCGITMMYXAQ-FHSPSHLESA-N
18
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Identification Substance Label (1)
no reactions.
Label
Reference
1; 6
PROTIA, LLC
Patent: US2009/82461 A1, 2009 ; Title/Abstract Full Text Show Details
Patent-Specific Data (1) Prophetic Compound
Related Markush Structure (RN)
Location in Patent
Reference
prophetic product
18954080
Page/page column 5
PROTIA, LLC
Patent: US2009/82461 A1, 2009 ; Title/Abstract Full Text Show Details
Reaxys Registry Number: 18954091
Molecular Formula: C15H15NO2S Linear Structure Formula: C15(2)H15NO2S
no reactions.
Identification
1
Other Data (4)
1
Molecular Weight: 288.236
InChI Key: YFGHCGITMMYXAQ-FIVZWEIFSA-N
19
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Identification Substance Label (1) Label
Reference
1; 8
PROTIA, LLC
Patent: US2009/82462 A1, 2009 ; Title/Abstract Full Text Show Details
Patent-Specific Data (1) Prophetic Compound
Related Markush Structure (RN)
Location in Patent
Reference
prophetic product
18954085
Page/page column 5
PROTIA, LLC
Patent: US2009/82462 A1, 2009 ; Title/Abstract Full Text Show Details
Chemical Name: 2-[(R)-(diphenylmethyl)sulfinyl]acetamide monohydrate Reaxys Registry Number: 15558295
CAS Registry Number: 947318-12-9 Molecular Formula: C15H15NO2S*H2O Linear Structure Formula: C15H15NO2S*H2O Molecular Weight: 291.371
InChI Key: TVIKTWOEQIEYMH-FSRHSHDFSA-N 20
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1 prep out of 1 reactions.
Chemical Names and Synonyms 2-[(R)-(diphenylmethyl)sulfinyl]acetamide monohydrate, Armondafinil monohydrate Other Data Use (4) Use Pattern
Reference
Excessive sleepiness
TEVA PHARMACEUTICAL INDUSTRIES LTD.; TEVA PHARMACEUTICALS USA, INC.
Patent: WO2007/98273 A2, 2007 ; Title/Abstract Full Text Show Details
Excessive sleepiness associated with narcolepsy
TEVA PHARMACEUTICAL INDUSTRIES LTD.; TEVA PHARMACEUTICALS USA, INC.
Patent: WO2007/98273 A2, 2007 ; Title/Abstract Full Text Show Details
Shift work sleep disorder ("SWSD")
TEVA PHARMACEUTICAL INDUSTRIES LTD.; TEVA PHARMACEUTICALS USA, INC.
Patent: WO2007/98273 A2, 2007 ; Title/Abstract Full Text Show Details
Obstructive sleep apnea/hypopnea syndrome ("OSA/HS")
TEVA PHARMACEUTICAL INDUSTRIES LTD.; TEVA PHARMACEUTICALS USA, INC.
Patent: WO2007/98273 A2, 2007 ; Title/Abstract Full Text Show Details
Chemical Name: (-)-modafinil acetonitrile solvate Reaxys Registry Number: 14566865
Molecular Formula: C2H3N*C15H15NO2S Linear Structure Formula: C2H3N*C15H15NO2S Molecular Weight: 314.408
InChI Key: JCXVRAJKQXEWHI-UHFFFAOYSA-N
1 prep out of 2 reactions.
1
1 prep out of 2 reactions.
1
21
Synthesize | Hide Details Find similar Chemical Names and Synonyms (-)-modafinil acetonitrile solvate Chemical Name: (+)-modafinil acetonitrile solvate Reaxys Registry Number: 14566866
Molecular Formula: C2H3N*C15H15NO2S Linear Structure Formula: C2H3N*C15H15NO2S Molecular Weight: 314.408
InChI Key: JCXVRAJKQXEWHI-UHFFFAOYSA-N 22
Synthesize | Hide Details Find similar Chemical Names and Synonyms (+)-modafinil acetonitrile solvate
Chemical Name: (-)-modafinil acetic acid solvate Reaxys Registry Number: 14566867
Molecular Formula: C2H4O2*C15H15NO2S Linear Structure Formula: C2H4O2*C15H15NO2S Molecular Weight: 333.408
InChI Key: JIQSCEZLYJHZBC-UHFFFAOYSA-N
1 prep out of 2 reactions.
1
1 prep out of 1 reactions.
1
1 prep out of 2 reactions.
1
1 prep out of 2 reactions.
1
23
Synthesize | Hide Details Find similar Chemical Names and Synonyms (-)-modafinil acetic acid solvate Chemical Name: (+)-modafinil acetic acid solvate Reaxys Registry Number: 14566868
Molecular Formula: C2H4O2*C15H15NO2S Linear Structure Formula: C2H4O2*C15H15NO2S Molecular Weight: 333.408
InChI Key: JIQSCEZLYJHZBC-UHFFFAOYSA-N 24
Synthesize | Hide Details Find similar Chemical Names and Synonyms (+)-modafinil acetic acid solvate Chemical Name: (-)-modafinil dimethylcarbonate solvate Reaxys Registry Number: 14566869
Molecular Formula: C3H6O3*C15H15NO2S Linear Structure Formula: C3H6O3*C15H15NO2S Molecular Weight: 363.434
InChI Key: QAPFKNAFCAMEED-UHFFFAOYSA-N 25
Synthesize | Hide Details Find similar Chemical Names and Synonyms (-)-modafinil dimethylcarbonate solvate, monodimethyl carbonate solvate of (-)-modafinil Chemical Name: (+)-modafinil dimethylcarbonate solvate Reaxys Registry Number: 14566870
Molecular Formula: C3H6O3*C15H15NO2S Linear Structure Formula: C3H6O3*C15H15NO2S Molecular Weight: 363.434
InChI Key: QAPFKNAFCAMEED-UHFFFAOYSA-N
26
Synthesize | Hide Details Find similar Chemical Names and Synonyms (+)-modafinil dimethylcarbonate solvate Chemical Name: Modafinil Bromazepam
no reactions.
1
no reactions.
1
no reactions.
1
Reaxys Registry Number: 30852728
Molecular Formula: C14H10BrN3O*C15H15NO2S Linear Structure Formula: C14H10BrN3O*C15H15NO2S Molecular Weight: 589.513
InChI Key: LMNJRLPKWVIFCL-UHFFFAOYSA-N 27
Synthesize | Hide Details Find similar Chemical Names and Synonyms Modafinil Bromazepam Chemical Name: modafinil citalopram haloperidol Reaxys Registry Number: 30175545
Molecular Formula: C15H15NO2S*C20H21FN2O*C21H23ClFNO2
Linear Structure Formula: C15H15NO2S*C20H21FN2O*C21H23ClFNO2
Molecular Weight: 973.624
InChI Key: KKZDGCOJEBVDST-UHFFFAOYSA-N 28
Synthesize | Hide Details Find similar Chemical Names and Synonyms modafinil citalopram haloperidol Chemical Name: Atomoxetine Donepezil Galantamine Memantine Methylphenidate Modafinil Rivastigmine Reaxys Registry Number: 30584732
Molecular Formula: C12H21N*C14H19NO2*C14H22N2O2*C15H15NO2S*C17H21NO*C17H21NO3*C24H29NO3
Linear Structure Formula: C12H21N*C14H19NO2*C14H22N2O2*C15H15NO2S*C17H21NO*C17H21NO3*C24H29NO3
Molecular Weight: 1858.53
InChI Key: DANVQFIKUOQCKF-VPQJJESLSA-N
29
Synthesize | Hide Details Find similar Chemical Names and Synonyms Atomoxetine Donepezil Galantamine Memantine Methylphenidate Modafinil Rivastigmine
30
mixture (composition completely given) :
2-[(diphenylmethyl)sulfinyl]acetamide calcium silicate magnesium trisilicate galactosyl-β-(1-gt;4)-glucose pregelatinized starch Croscarmellose sodium magnesium stearate NF
Chemical Name: composition 1B
no reactions.
Reaxys Registry Number: 11369833 Type of Substance: mixture (composition completely given)
Hide Details Chemical Names and Synonyms composition 1B Composition galactosyl-β-(1-gt;4)-glucose (212.5 mg)
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pregelatinized starch (25.0 mg)
2-[(diphenylmethyl)sulfinyl]acetamide (200 mg)
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magnesium stearate NF (7.5 mg)
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calcium silicate (25.0 mg)
Bioactivity (2) Other Data (7)
1
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magnesium trisilicate (5.0 mg)
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Bioactivity Pharmacological Data (2) 1 of 2
Comment (Pharmacological Data)
Bioactivities present
Reference
Patel, Ashish Anilbhai; Barbera, Gary
Patent: US2005/137264 A1, 2005 ; Title/Abstract Full Text Show Details
2 of 2
Effect (Pharmacological Data)
pharmacokinetics
Species or Test-System (Pharmacological Data)
human
Route of Application
peroral
Method (Pharmacological Data)
Bioequivalency Comparison of Modafinil Compositions 1A and 1B Prepared in Example 1, as Compared to Provigil.(R).The area under the curve (AUC) and the maximum concentration of modafinil obtained in vivo (Cmax) was determined for Modafinil Composition 1A, Composition 1B and Provigil.(R).. The results for Composition 1A and Provigil.(R). are summarized in Table II. The results for Composition 1B and Provigil.(R). are summarized in Table III. The results in Table II and Table III show that the bioequivalency of Compositions 1A and 1B prepared according to the invention exhibit a comparable AUC and Cmax as compared to Provigil.(R)..
Results
title substances exhibited a comparable Modafinil AUC and Cmax as compared to Provigil.(R).
Location
Page/Page column 3-4
Reference
Patel, Ashish Anilbhai; Barbera, Gary
Patent: US2005/137264 A1, 2005 ; Title/Abstract Full Text Show Details
Other Data Use (7) Use Pattern
Reference
Sleepiness
Patel, Ashish Anilbhai; Barbera, Gary
Patent: US2005/137264 A1, 2005 ; Title/Abstract Full Text Show Details
Promotion of wakefulness
Patel, Ashish Anilbhai; Barbera, Gary
Patent: US2005/137264 A1, 2005 ; Title/Abstract Full Text Show Details
Parkinson's disease
Patel, Ashish Anilbhai; Barbera, Gary
Patent: US2005/137264 A1, 2005 ;
Title/Abstract Full Text Show Details
Patel, Ashish Anilbhai; Barbera, Gary
Patent: US2005/137264 A1, 2005 ;
Cerebral ischemia
Title/Abstract Full Text Show Details
Patel, Ashish Anilbhai; Barbera, Gary
Patent: US2005/137264 A1, 2005 ;
Eating disorders
Title/Abstract Full Text Show Details
Patel, Ashish Anilbhai; Barbera, Gary
Patent: US2005/137264 A1, 2005 ;
Stimulation of appetite and weight gain
Title/Abstract Full Text Show Details
Patel, Ashish Anilbhai; Barbera, Gary
Patent: US2005/137264 A1, 2005 ;
Attention deficit hyperactivity disorder
Title/Abstract Full Text Show Details
31
mixture (composition completely given) :
2-[(diphenylmethyl)sulfinyl]acetamide calcium silicate galactosyl-β-(1-gt;4)-glucose pregelatinized starch Croscarmellose sodium magnesium stearate NF
Chemical Name: composition 1A
no reactions.
Reaxys Registry Number: 11369834 Type of Substance: mixture (composition completely given)
Hide Details Chemical Names and Synonyms composition 1A Composition galactosyl-β-(1-gt;4)-glucose (217.5 mg)
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pregelatinized starch (25.0 mg)
2-[(diphenylmethyl)sulfinyl]acetamide (200 mg)
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magnesium stearate NF (7.5 mg)
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calcium silicate (25.0 mg)
Bioactivity (2) Other Data (7)
1
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Bioactivity Pharmacological Data (2) 1 of 2
Comment (Pharmacological Data)
Bioactivities present
Reference
Patel, Ashish Anilbhai; Barbera, Gary
Patent: US2005/137264 A1, 2005 ; Title/Abstract Full Text Show Details
2 of 2
Effect (Pharmacological Data)
pharmacokinetics
Species or Test-System (Pharmacological Data)
human
Route of Application
peroral
Method (Pharmacological Data)
Bioequivalency Comparison of Modafinil Compositions 1A and 1B Prepared in Example 1, as Compared to Provigil.(R).The area under the curve (AUC) and the maximum concentration of modafinil obtained in vivo (Cmax) was determined for Modafinil Composition 1A, Composition 1B and Provigil.(R).. The results for Composition 1A and Provigil.(R). are summarized in Table II. The results for Composition 1B and Provigil.(R). are summarized in Table III. The results in Table II and Table III show that the bioequivalency of Compositions 1A and 1B prepared according to the invention exhibit a comparable AUC and Cmax as compared to Provigil.(R)..
Results
title substances exhibited a comparable Modafinil AUC and Cmax as compared to Provigil.(R).
Location
Page/Page column 3-4
Reference
Patel, Ashish Anilbhai; Barbera, Gary
Patent: US2005/137264 A1, 2005 ; Title/Abstract Full Text Show Details
Other Data Use (7) Use Pattern
Reference
Sleepiness
Patel, Ashish Anilbhai; Barbera, Gary
Patent: US2005/137264 A1, 2005 ; Title/Abstract Full Text Show Details
Promotion of wakefulness
Patel, Ashish Anilbhai; Barbera, Gary
Patent: US2005/137264 A1, 2005 ; Title/Abstract Full Text Show Details
Parkinson's disease
Patel, Ashish Anilbhai; Barbera, Gary
Patent: US2005/137264 A1, 2005 ; Title/Abstract Full Text Show Details
Cerebral ischemia
Patel, Ashish Anilbhai; Barbera, Gary
Patent: US2005/137264 A1, 2005 ; Title/Abstract Full Text Show Details
Eating disorders
Patel, Ashish Anilbhai; Barbera, Gary
Patent: US2005/137264 A1, 2005 ; Title/Abstract Full Text Show Details
Stimulation of appetite and weight gain
Patel, Ashish Anilbhai; Barbera, Gary
Patent: US2005/137264 A1, 2005 ; Title/Abstract Full Text Show Details
Attention deficit hyperactivity disorder
Patel, Ashish Anilbhai; Barbera, Gary
Patent: US2005/137264 A1, 2005 ;
Title/Abstract Full Text Show Details
32
mixture (composition partially given) :
2-[(diphenylmethyl)sulfinyl]acetamide lactose crospovidone hydroxypropyl cellulose sodium lauryl sulfate stearyl sodium fumarate talcum
Chemical Name: crospovidone; lactose monohydrate; low substituted hydroxypropyl cellulose; modafinil; Na stearyl fumarate; pregelatinized starch; sodium lauryl sulphate; talc; mixture of
no reactions.
Reaxys Registry Number: 11369839 Type of Substance: mixture (composition partially given)
Hide Details Chemical Names and Synonyms crospovidone; lactose monohydrate; low substituted hydroxypropyl cellulose; modafinil; Na stearyl fumarate; pregelatinized starch; sodium lauryl sulphate; talc; mixture of Composition 2-[(diphenylmethyl)sulfinyl]acetamide (200 mg)
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lactose
sodium lauryl sulfate (9.375 mg)
stearyl sodium fumarate (6.62 mg)
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crospovidone (80 mg)
talcum (9.375 mg)
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Bioactivity (2) Other Data (1)
1
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Bioactivity Pharmacological Data (2) 1 of 2
Comment (Pharmacological Data)
Bioactivities present
Reference
HIKMA PHARMACEUTICALS
Patent: US2007/275057 A1, 2007 ; Title/Abstract Full Text Show Details
2 of 2
Effect (Pharmacological Data)
pharmacokinetics
Species or Test-System (Pharmacological Data)
human
Method (Pharmacological Data)
Bioequivalence Comparison of Modafinil Tablets of the Invention with PROVIGIL.(R). 200 The area under curve (AUC) and the maximum plasma concentration of Modafinil obtained in vivo (Cmax) were determined for Modafinil tablets of the invention and PROVIGIL.(R). 200. The average blood levels of 12 volunteers in ug/mL are given in Table 6. The results in Table 7 illustrates that the AUC and Cmax ratios for Modafinil tablets of the invention versus PROVIGIL.(R). 200 are well within the bioequivalence acceptance criteria.
Results
The AUC and Cmax ratios for title compound versus reference tablets (PROVIGIL.(R).) are well within the bioequivalence acceptance criteria: C max: 97.75; AUC 0-t: 98.41; AUC 0-.infin.: 99.96. The average blood levels of modafinil, μg/mL at 0 - 72 hours: 0.0 - 4.04 (title compound); 0.0 - 3.98 (reference tablets PROVIGIL.(R).); figure is given.
Location
Page/Page column 1; 6; sheet 2
Reference
HIKMA PHARMACEUTICALS
Patent: US2007/275057 A1, 2007 ; Title/Abstract Full Text Show Details
Other Data Use (1) Use Pattern
Reference
tablet formulation
HIKMA PHARMACEUTICALS
Patent: US2007/275057 A1, 2007 ; Title/Abstract Full Text Show Details
33
mixture (composition partially given) :
2-[(diphenylmethyl)sulfinyl]acetamide Hide Details
Chemical Names and Synonyms PROVIGIL.(R). Composition
Chemical Name: PROVIGIL.(R). Reaxys Registry Number: 11369854 Type of Substance: mixture (composition partially given)
no reactions.
Bioactivity (2)
1
2-[(diphenylmethyl)sulfinyl]acetamide (200 mg)
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Bioactivity Pharmacological Data (2) 1 of 2
Comment (Pharmacological Data)
Bioactivities present
Reference
HIKMA PHARMACEUTICALS
Patent: US2007/275057 A1, 2007 ; Title/Abstract Full Text Show Details
2 of 2
Effect (Pharmacological Data)
pharmacokinetics
Species or Test-System (Pharmacological Data)
human
Method (Pharmacological Data)
Bioequivalence Comparison of Modafinil Tablets of the Invention with PROVIGIL.(R). 200 The area under curve (AUC) and the maximum plasma concentration of Modafinil obtained in vivo (Cmax) were determined for Modafinil tablets of the invention and PROVIGIL.(R). 200. The average blood levels of 12 volunteers in ug/mL are given in Table 6. The results in Table 7 illustrates that the AUC and Cmax ratios for Modafinil tablets of the invention versus PROVIGIL.(R). 200 are well within the bioequivalence acceptance criteria.
Results
Pharmacokinetic parameters: C max: 97.75; AUC 0-t: 98.41; AUC 0-.infin.: 99.96. The average blood levels of modafinil, μg/mL at 0 - 72 hours: 0.0 - 3.98; figure is given.
Location
Page/Page column 1; 6; sheet 2
Reference
HIKMA PHARMACEUTICALS
Patent: US2007/275057 A1, 2007 ; Title/Abstract Full Text Show Details
34
mixture (composition partially given) :
2-[(diphenylmethyl)sulfinyl]acetamide hydroxypropyl methylcellulose sodium dioctyl sulfosuccinate [14C]-Sucrose sodium lauryl sulfate galactosyl-β-(1-gt;4)-glucose cellulose crospovidone magnesium stearate NF
Reaxys Registry Number: 11382686 Type of Substance: mixture (composition partially given)
no reactions.
Hide Details
Composition [14C]-Sucrose
galactosyl-β-(1-gt;4)-glucose
2-[(diphenylmethyl)sulfinyl]acetamide
Other Data (26)
1
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sodium lauryl sulfate
magnesium stearate NF
sodium dioctyl sulfosuccinate
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cellulose
hydroxypropyl methylcellulose
crospovidone
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Other Data Use (26) Use Pattern
Reference
Dyssomnias
ELAN CORPORATION, PLC
Patent: WO2008/8879 A2, 2008 ; Title/Abstract Full Text Show Details
Narcolepsy
ELAN CORPORATION, PLC
Patent: WO2008/8879 A2, 2008 ; Title/Abstract Full Text Show Details
Chronic fatigue
ELAN CORPORATION, PLC
Patent: WO2008/8879 A2, 2008 ; Title/Abstract Full Text Show Details
Eating disorder
ELAN CORPORATION, PLC
Patent: WO2008/8879 A2, 2008 ; Title/Abstract Full Text Show Details
Compulsive behaviors
ELAN CORPORATION, PLC
Patent: WO2008/8879 A2, 2008 ; Title/Abstract Full Text Show Details
ADHD
ELAN CORPORATION, PLC
Patent: WO2008/8879 A2, 2008 ; Title/Abstract Full Text Show Details
Addictions
ELAN CORPORATION, PLC
Patent: WO2008/8879 A2, 2008 ; Title/Abstract Full Text Show Details
Substance abuse
ELAN CORPORATION, PLC
Patent: WO2008/8879 A2, 2008 ; Title/Abstract Full Text Show Details
Sleepiness
ELAN CORPORATION, PLC
Patent: WO2008/8879 A2, 2008 ; Title/Abstract Full Text Show Details
Nervous system disease
ELAN CORPORATION, PLC
Patent: WO2008/8879 A2, 2008 ; Title/Abstract Full Text Show Details
Nervous system conditions
ELAN CORPORATION, PLC
Patent: WO2008/8879 A2, 2008 ; Title/Abstract Full Text Show Details
Nervous system syndromes
ELAN CORPORATION, PLC
Patent: WO2008/8879 A2, 2008 ; Title/Abstract Full Text Show Details
Nervous system symptoms
ELAN CORPORATION, PLC
Patent: WO2008/8879 A2, 2008 ; Title/Abstract Full Text Show Details
Symptoms of the central nervous system (CNS)
ELAN CORPORATION, PLC
Patent: WO2008/8879 A2, 2008 ; Title/Abstract Full Text Show Details
Syndromes of the central nervous system (CNS)
ELAN CORPORATION, PLC
Patent: WO2008/8879 A2, 2008 ; Title/Abstract Full Text Show Details
Conditions of the central nervous system (CNS)
ELAN CORPORATION, PLC
Patent: WO2008/8879 A2, 2008 ; Title/Abstract Full Text Show Details
Neurological disesas
ELAN CORPORATION, PLC
Patent: WO2008/8879 A2, 2008 ; Title/Abstract Full Text Show Details
Neurological disorders
ELAN CORPORATION, PLC
Patent: WO2008/8879 A2, 2008 ;
Title/Abstract Full Text Show Details
ELAN CORPORATION, PLC
Patent: WO2008/8879 A2, 2008 ;
Neurological syndromes
Title/Abstract Full Text Show Details
ELAN CORPORATION, PLC
Patent: WO2008/8879 A2, 2008 ;
Neurological symptoms
Title/Abstract Full Text Show Details
Hide facts Use Pattern
Reference
Nacrolepsy
ELAN CORPORATION, PLC
Patent: WO2008/8879 A2, 2008 ; Title/Abstract Full Text Show Details
ELAN CORPORATION, PLC
Patent: WO2008/8879 A2, 2008 ;
Obstructive sleep apnea syndrome
Title/Abstract Full Text Show Details
ELAN CORPORATION, PLC
Patent: WO2008/8879 A2, 2008 ;
Obstructive sleep hypopnea syndrome
Title/Abstract Full Text Show Details
ELAN CORPORATION, PLC
Patent: WO2008/8879 A2, 2008 ;
Shift worker sleep disorder
Title/Abstract Full Text Show Details
Improvement of wakefulness in patients with excessive daytime sleepiness associated with nacrolepsy
ELAN CORPORATION, PLC
Patent: WO2008/8879 A2, 2008 ; Title/Abstract Full Text Show Details
ELAN CORPORATION, PLC
Patent: WO2008/8879 A2, 2008 ;
Idiopathic hypersomnia
Title/Abstract Full Text Show Details
35
mixture (composition partially given) :
2-[(diphenylmethyl)sulfinyl]acetamide galactosyl-β-(1-gt;4)-glucose crospovidone polyvinylpyrrolidone
Reaxys Registry Number: 11382687 Type of Substance: mixture (composition partially given)
no reactions.
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Composition galactosyl-β-(1-gt;4)-glucose
2-[(diphenylmethyl)sulfinyl]acetamide
polyvinylpyrrolidone
Other Data (9)
1
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crospovidone
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Other Data Use (9) Use Pattern
Reference
idiopathic hypersomnia
Barr Laboratories, Inc.
Patent: US2004/253308 A1, 2004 ; Title/Abstract Full Text Show Details
narcolepsy
Barr Laboratories, Inc.
Patent: US2004/253308 A1, 2004 ; Title/Abstract Full Text Show Details
sleep disorders
Barr Laboratories, Inc.
Patent: US2004/253308 A1, 2004 ; Title/Abstract Full Text Show Details
Parkinson's disease
Barr Laboratories, Inc.
Patent: US2004/253308 A1, 2004 ; Title/Abstract Full Text Show Details
depression
Barr Laboratories, Inc.
Patent: US2004/253308 A1, 2004 ; Title/Abstract Full Text Show Details
hypersomnia
Barr Laboratories, Inc.
Patent: US2004/253308 A1, 2004 ; Title/Abstract Full Text Show Details
Alzheimer's disease
Barr Laboratories, Inc.
Patent: US2004/253308 A1, 2004 ; Title/Abstract Full Text Show Details
anti-ischemic disorders
Barr Laboratories, Inc.
Patent: US2004/253308 A1, 2004 ; Title/Abstract Full Text Show Details
urinary incontinence
Barr Laboratories, Inc.
Patent: US2004/253308 A1, 2004 ; Title/Abstract Full Text Show Details
36
mixture (composition partially given) :
8-[4-[4-(pyrimidine-2-yl)-piperazine-1-yl]-butyl]-8-azaspiro[4.5]decane-7,9-dione 2-[(diphenylmethyl)sulfinyl]acetamide
Reaxys Registry Number: 11382688 Type of Substance: mixture (composition partially given)
no reactions.
Bioactivity (3)
1
Hide Details
Composition 8-[4-[4-(pyrimidine-2-yl)-piperazine-1-yl]-butyl]-8-azaspiro[4.5]decane-7,9-dione
2-[(diphenylmethyl)sulfinyl]acetamide
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Bioactivity Pharmacological Data (3) 1 of 3
Comment (Pharmacological Data)
Bioactivities present
Reference
BrainCells, Inc.
Patent: US2007/270449 A1, 2007 ; Title/Abstract Full Text Show Details
2 of 3
Effect (Pharmacological Data)
neuronal differentiation; effect on
Species or Test-System (Pharmacological Data)
human neural stem cells (hNSCs)
Method (Pharmacological Data)
Example 21 Effects of the 5-HT1a Agonist Buspirone in Combination with Modafinil on Differentiation of Human Neural Stem Cells Human neural stem cells (hNSCs) were isolated and grown in monolayer culture, plated, treated with varying concentrations of buspirone in the presence or absence of modafinil, and stained with TUJ-1 antibody for the detection of neuronal differentiation or GFAP antibody for the detection of astrocyte differentiation, as described above. Mitogen-free test media with a positive control for neuronal differentiation was used along with basal media without growth factors as a negative control. Results are shown in FIGS. 39 and 40, which show concentration response curves of neuronal and astrocyte differentiation respectively, after background media values are subtracted. The concentration response curves of the combination of buspirone with modafinil are shown with the concentration response curves of buspirone or modafinil alone. The data is presented as a percent of neuronal or astrocyte positive control. The data indicate that the combination of buspirone with modafinil resulted in consistent neuronal differentiation with a simultaneous decrease in astrocyte differentiation relative to that produced by buspirone alone.
Type (Pharmacological Data)
EC50
Value of Type (Pharmacological Data)
4.5 μmol/l
Results
Test compound resulted in consistent neuronal differentiation; figure is given.
Location
Page/Page column 6; 45; sheet 39
Reference
BrainCells, Inc.
Patent: US2007/270449 A1, 2007 ; Title/Abstract Full Text Show Details
3 of 3
Effect (Pharmacological Data)
astrocyte differentiation; effect on
Species or Test-System (Pharmacological Data)
human neural stem cells (hNSCs)
Method (Pharmacological Data)
Example 21 Effects of the 5-HT1a Agonist Buspirone in Combination with Modafinil on Differentiation of Human Neural Stem Cells Human neural stem cells (hNSCs) were isolated and grown in monolayer culture, plated, treated with varying concentrations of buspirone in the presence or absence of modafinil, and stained with TUJ-1 antibody for the detection of neuronal differentiation or GFAP antibody for the detection of astrocyte differentiation, as described above. Mitogen-free test media with a positive control for neuronal differentiation was used along with basal media without growth factors as a negative control. Results are shown in FIGS. 39 and 40, which show concentration response curves of neuronal and astrocyte differentiation respectively, after background media values are subtracted. The concentration response curves of the combination of buspirone with modafinil are shown with the concentration response curves of buspirone or modafinil alone. The data is presented as a percent of neuronal or astrocyte positive control. The data indicate that the combination of buspirone with modafinil resulted in consistent neuronal differentiation with a simultaneous decrease in astrocyte differentiation relative to that produced by buspirone alone.
Results
Differentiation was reduced from a maximum of 60percent with buspirone alone to a maximum of 28percent with test combination; figure is given.
Location
Page/Page column 6; 45; sheet 40
Reference
BrainCells, Inc.
Patent: US2007/270449 A1, 2007 ; Title/Abstract Full Text Show Details
37
mixture (composition partially given) :
1 [n (2,3 dimethyl 5,6,7,8 tetrahydrofuro[2,3 b]quinolin 4 yl)carbamoylmethyl]pyrrolidin 2 one 2-[(diphenylmethyl)sulfinyl]acetamide
Reaxys Registry Number: 11382689 Type of Substance: mixture (composition partially given)
no reactions.
Bioactivity (2)
1
Hide Details
Composition 2-[(diphenylmethyl)sulfinyl]acetamide
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1 [n (2,3 dimethyl 5,6,7,8 tetrahydrofuro[2,3 b]quinolin 4 yl)carbamoylmethyl]pyrrolidin 2 one
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Bioactivity Pharmacological Data (2) 1 of 2
Comment (Pharmacological Data)
Bioactivities present
Reference
BrainCells, Inc.
Patent: US2008/64671 A1, 2008 ; Title/Abstract Full Text Show Details
2 of 2
Effect (Pharmacological Data)
neuronal differentiation; stimulation of
Species or Test-System (Pharmacological Data)
neural stem cells (hNSCs) of human
Method (Pharmacological Data)
FIG. 9 is a dose-response curve showing effect of the neurogenic agents MKC-231 and modafinil (adrenergic agonist) in combination on neuronal differentiation of human neural stem cells compared to the effect of either agent alone. When run independently, each compound was tested in a concentration response curve ranging from 0.01 μM to 31.6 μM. In combination, the compounds were combined at equal concentrations at each point (for example, the first point in the combined curve consisted of a test of 0.01 μM MKC-231 and 0.01 μM modafinil). Data is presented as the percentage of the neuronal positive control, with basal media values subtracted. When used alone, EC50 was observed at an MKC-231 concentration of 8.6 μM or a modafinil concentration estimated to be 83 μM (based on extrapolation of the observed data). When used in combination, neurogenesis is greatly enhanced: EC50 was observed at a combination of MKC-231 and modafinil at concentrations of 1.1 μM each, resulting in a synergistic combination index of 0.14.; Example 8Effects of Modafinil in Combination with the MKC-231 on Differentiation of Human Neural Stem CellsHuman neural stem cells (hNSCs) were isolated and grown in monolayer culture, plated, treated with varying concentrations of MKC-231 in the presence or absence of modafinil, and stained with TUJ-1 antibody for the detection of neuronal differentiation as described in above. Mitogen-free test media with a positive control for neuronal differentiation was used along with basal media without growth factors as a negative control.Results are shown in FIG. 9, which shows concentration response curves of neuronal differentiation
after background media values are subtracted. The concentration response curves of the combination of MKC-231 with modafinil are shown with the concentration response curves either agent alone. The data is presented as a percent of neuronal positive control. The data indicate that the combination of MKC-231 with modafinil resulted in synergistically enhanced neuronal differentiation relative to that that produced by either agent alone. Results
title compound enhanced neurogenesis with EC50 observed at 1.1 umol/l MKC-231 and 1.1 umol/l modafinil; synergistic effect was observed; figure is given
Location
Page/Page column 3; 40-41; sheet 9
Reference
BrainCells, Inc.
Patent: US2008/64671 A1, 2008 ; Title/Abstract Full Text Show Details
38
Chemical Name: NanoCrystalTM
mixture (composition partially given) :
2-[(diphenylmethyl)sulfinyl]acetamide
no reactions.
Bioactivity (2)
1
Reaxys Registry Number: 11382690 Type of Substance: mixture (composition partially given)
Hide Details
Chemical Names and Synonyms NanoCrystalTM Composition 2-[(diphenylmethyl)sulfinyl]acetamide
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Bioactivity Pharmacological Data (2) 1 of 2
Comment (Pharmacological Data)
Bioactivities present
Reference
ELAN CORPORATION, PLC
Patent: WO2008/8879 A2, 2008 ; Title/Abstract Full Text Show Details
2 of 2
Effect (Pharmacological Data)
pharmacokinetics
Species or Test-System (Pharmacological Data)
beagle dog
Sex
male
Route of Application
peroral
Method (Pharmacological Data)
Example 3The purpose of this example is to determine the pharmacokinetics of modafinil when administered orally as 200 mg NanoCrystalTM dispersions and as 200 mg Provigil.(R). to fasted male beagle dogs. This study was a single dose two way crossover study conducted in 6 beagle dogs. There was at least a 7 day washout between each treatment period. The test formulation was modafinil Nanocrystal.(R). (100 mg/g) (10percentw/w) NCD (Batch No: TESR-1148-009). The reference formulation was modafinil tablets (Provigil.(R).) (Batch No: BN 5E39).Blood samples were collected before dosing and at 15 minutes (+/-5 minutes), 30 minutes (+/-5 minutes), 45 minutes (+/-5 minutes), 1 hour (+/-5 minutes), 1.25 hours (+/-5 minutes), 1.5 (+/-5 minutes), 1.75 hours (+/-5 minutes), 2 hours (+/-5 minutes), 3 hours (+/-10 minutes), 4 hours (+/-10 minutes), 6 hours (+/-10 minutes) and 12 hours (+/-10 minutes) after dosing. On Study Day 0, following an overnight fast (14-18 hrs), each animal received 200mg modafinil administered as 2g NanoCrystalTM dispersion by oral gavage. On Study Day 8, following an overnight fast (14- 18 hrs), each animal received 200 mg modafinil administered as Provigil tablets by oral administration.Modafinil was measured in dog plasma samples by a validated LC MS/MS method incorporating a liquidliquid extraction method by BioClin Research Laboratories. The limit of quantitation of the modafinil plasma assay was lOOng/mL (assay range 100-5000ng/mL). The pharmacokinetic evaluation was conducted by PK Pharma Innovations Limited. The pharmacokinetic parameters were calculated using WinNonlin.(TM)., Version 4.0.1
(Pharsight Corporation, USA).The following pharmacokinetic parameters were derived from the plasma concentrations versus time data for modafinil, using noncompartmental methodology:- - AUCinf (AUCo-.infin.) - Area under the curve from time of dosing extrapolated to infinity asAUCo-t + Ciast/ lambda z, where AUCo-t is the area under the curve from time of dosing to the last evaluable concentration, Ciast is the last evaluable plasma concentration and lambda z is the elimination rate constant associated with the terminal portion of the curve. - AUCiast (AUCo-t) - Area under the curve from the time of dosing to the time of the last quantifiable concentration calculated using the linear trapezoidal rule where AUC (trt2) = δt * (c2+ci)/2.- Maximum plasma concentration (Cmax) and its corresponding time (tmax) were recorded from the observed plasma concentration-time profiles. - Relative bioavailability of the test treatment (Trt A) to the reference (Trt B) based onAUC (test/reference and expressed as a percentage).- Half Life (tm) was calculated as In2/ Lambda z. - Lambda z (Kel) - First order rate constant associated with the terminal (log-linear) portion of the curve estimated via linear regression of time vs. log concentration. For each regression analysis, an adjusted r was computed as follows: Adjusted r = 1 - ((1- r2)*(n-l)) / (n-2), where r2 is the square of the correlation coefficient and n is the number of points used in the regression. Linear regression analyses of time versus log plasma concentration was conducted using a manual iterative procedure including increasing numbers of samples from the last three quantifiable plasma concentrations up to and including Cmax. The regression with the largest adjusted r was selected to estimate lambda z as -1 times the estimated slope of the regression line.As there were no significant deviations from the amount of modafinil administered in each of the administrations or the actual sampling times at which blood draws were obtained, pharmacokinetic analysis was based on nominal amounts administered and nominal sampling times.The data was summarized using descriptive statistics. Arithmetic means, standard deviations, and coefficients of variation were calculated for the Results
200 mg title compound treatment resulted in a mean 29percent increase in the extent and a mean 40percent increase in the rate of absorption of modafinil compared with the oral adminstration of 200 mg modafinil in the form of provigil tablets; the relative bioavailability and the relative Cmax of the test was 129percent and 140percent, respectively; the extent of absorption as determined by AUC was 35.8 μg/mL.h; the maximum concentration determined was 8.7 μ/mL; figure is given
Location
Page/Page column 14; 56-59; 8/8
Reference
ELAN CORPORATION, PLC
Patent: WO2008/8879 A2, 2008 ; Title/Abstract Full Text Show Details
39
Reaxys Registry Number: 13079480 Type of Substance: mixture (composition partially given)
mixture (composition partially given) :
2-[(diphenylmethyl)sulfinyl]acetamide succinic acid (2E)-but-2-enedioic acid
no reactions.
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Composition (2E)-but-2-enedioic acid
succinic acid
2-[(diphenylmethyl)sulfinyl]acetamide
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Identification Patent-Specific Data (1) Related Markush Structure (RN)
Reference
13054372
Peterson, Matthew; Bourghol Hickey, Magali; Oliveira, Mark; Almarsson, Orn; Remenar, Julius
Patent: US2005/267209 A1, 2005 ; Title/Abstract Full Text Show Details
Physical Data Melting Point (1) Melting Point
Reference
152.58 - 160 °C
Peterson, Matthew; Bourghol Hickey, Magali; Oliveira, Mark; Almarsson, Orn; Remenar, Julius
Patent: US2005/267209 A1, 2005 ;
Identification Physical Data (1) Other Data (63)
1
Title/Abstract Full Text Show Details
Other Data Use (63) Use Pattern
Reference
excessive daytime sleepiness associated with narcolepsy
Peterson, Matthew; Bourghol Hickey, Magali; Oliveira, Mark; Almarsson, Orn; Remenar, Julius
Patent: US2005/267209 A1, 2005 ; Title/Abstract Full Text Show Details
multiple sclerosis related fatigue
Peterson, Matthew; Bourghol Hickey, Magali; Oliveira, Mark; Almarsson, Orn; Remenar, Julius
Patent: US2005/267209 A1, 2005 ; Title/Abstract Full Text Show Details
infertility
Peterson, Matthew; Bourghol Hickey, Magali; Oliveira, Mark; Almarsson, Orn; Remenar, Julius
Patent: US2005/267209 A1, 2005 ; Title/Abstract Full Text Show Details
eating disorders
Peterson, Matthew; Bourghol Hickey, Magali; Oliveira, Mark; Almarsson, Orn; Remenar, Julius
Patent: US2005/267209 A1, 2005 ; Title/Abstract Full Text Show Details
attention deficit hyperactivity disorder (ADHD)
Peterson, Matthew; Bourghol Hickey, Magali; Oliveira, Mark; Almarsson, Orn; Remenar, Julius
Patent: US2005/267209 A1, 2005 ; Title/Abstract Full Text Show Details
Parkinson's disease
Peterson, Matthew; Bourghol Hickey, Magali; Oliveira, Mark; Almarsson, Orn; Remenar, Julius
Patent: US2005/267209 A1, 2005 ; Title/Abstract Full Text Show Details
incontinence
Peterson, Matthew; Bourghol Hickey, Magali; Oliveira, Mark; Almarsson, Orn; Remenar, Julius
Patent: US2005/267209 A1, 2005 ; Title/Abstract Full Text Show Details
sleep apnea
Peterson, Matthew; Bourghol Hickey, Magali; Oliveira, Mark; Almarsson, Orn; Remenar, Julius
Patent: US2005/267209 A1, 2005 ; Title/Abstract Full Text Show Details
myopathies
Peterson, Matthew; Bourghol Hickey, Magali; Oliveira, Mark; Almarsson, Orn; Remenar, Julius
Patent: US2005/267209 A1, 2005 ; Title/Abstract Full Text Show Details
neoplasia
Peterson, Matthew; Bourghol Hickey, Magali; Oliveira, Mark; Almarsson, Orn; Remenar, Julius
Patent: US2005/267209 A1, 2005 ; Title/Abstract Full Text Show Details
cancer
Peterson, Matthew; Bourghol Hickey, Magali; Oliveira, Mark; Almarsson, Orn; Remenar, Julius
Patent: US2005/267209 A1, 2005 ; Title/Abstract Full Text Show Details
carcinoma
Peterson, Matthew; Bourghol Hickey, Magali; Oliveira, Mark; Almarsson, Orn; Remenar, Julius
Patent: US2005/267209 A1, 2005 ; Title/Abstract Full Text Show Details
cancer of the bladder
Peterson, Matthew; Bourghol Hickey, Magali; Oliveira, Mark; Almarsson, Orn; Remenar, Julius
Patent: US2005/267209 A1, 2005 ; Title/Abstract Full Text Show Details
Cancer of the breast
Peterson, Matthew; Bourghol Hickey, Magali; Oliveira, Mark; Almarsson, Orn; Remenar, Julius
Patent: US2005/267209 A1, 2005 ;
Title/Abstract Full Text Show Details
Peterson, Matthew; Bourghol Hickey, Magali; Oliveira, Mark; Almarsson, Orn; Remenar, Julius
Patent: US2005/267209 A1, 2005 ;
Cancer of the colon
Title/Abstract Full Text Show Details
Peterson, Matthew; Bourghol Hickey, Magali; Oliveira, Mark; Almarsson, Orn; Remenar, Julius
Patent: US2005/267209 A1, 2005 ;
Cancer of the kidney
Title/Abstract Full Text Show Details
Peterson, Matthew; Bourghol Hickey, Magali; Oliveira, Mark; Almarsson, Orn; Remenar, Julius
Patent: US2005/267209 A1, 2005 ;
Cancer of the liver
Title/Abstract Full Text Show Details
Peterson, Matthew; Bourghol Hickey, Magali; Oliveira, Mark; Almarsson, Orn; Remenar, Julius
Patent: US2005/267209 A1, 2005 ;
Cancer of the lung
Title/Abstract Full Text Show Details
Peterson, Matthew; Bourghol Hickey, Magali; Oliveira, Mark; Almarsson, Orn; Remenar, Julius
Patent: US2005/267209 A1, 2005 ;
small cell lung cancer
Title/Abstract Full Text Show Details
Peterson, Matthew; Bourghol Hickey, Magali; Oliveira, Mark; Almarsson, Orn; Remenar, Julius
Patent: US2005/267209 A1, 2005 ;
Cancer of the esophagus
Title/Abstract Full Text Show Details
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Use Pattern
Reference
Cancer of the gall-bladder
Peterson, Matthew; Bourghol Hickey, Magali; Oliveira, Mark; Almarsson, Orn; Remenar, Julius
Patent: US2005/267209 A1, 2005 ; Title/Abstract Full Text Show Details
Cancer of the ovary
Peterson, Matthew; Bourghol Hickey, Magali; Oliveira, Mark; Almarsson, Orn; Remenar, Julius
Patent: US2005/267209 A1, 2005 ; Title/Abstract Full Text Show Details
Cacner of the pancreas
Peterson, Matthew; Bourghol Hickey, Magali; Oliveira, Mark; Almarsson, Orn; Remenar, Julius
Patent: US2005/267209 A1, 2005 ; Title/Abstract Full Text Show Details
Cancer of the stomach
Peterson, Matthew; Bourghol Hickey, Magali; Oliveira, Mark; Almarsson, Orn; Remenar, Julius
Patent: US2005/267209 A1, 2005 ; Title/Abstract Full Text Show Details
Cacner of the cervix
Peterson, Matthew; Bourghol Hickey, Magali; Oliveira, Mark; Almarsson, Orn; Remenar, Julius
Patent: US2005/267209 A1, 2005 ; Title/Abstract Full Text Show Details
Cancer of the thyroid
Peterson, Matthew; Bourghol Hickey, Magali; Oliveira, Mark; Almarsson, Orn; Remenar, Julius
Patent: US2005/267209 A1, 2005 ; Title/Abstract Full Text Show Details
Cancer of the prostate
Peterson, Matthew; Bourghol Hickey, Magali; Oliveira, Mark; Almarsson, Orn; Remenar, Julius
Patent: US2005/267209 A1, 2005 ; Title/Abstract Full Text Show Details
Cacner of the skin
Peterson, Matthew; Bourghol Hickey, Magali; Oliveira, Mark; Almarsson, Orn; Remenar, Julius
Patent: US2005/267209 A1, 2005 ; Title/Abstract Full Text Show Details
squamous cell carcinoma
Peterson, Matthew; Bourghol Hickey, Magali; Oliveira, Mark; Almarsson, Orn; Remenar, Julius
Patent: US2005/267209 A1, 2005 ;
Title/Abstract Full Text Show Details
hematopoietic tumors of lymphoid lineage
Peterson, Matthew; Bourghol Hickey, Magali; Oliveira, Mark; Almarsson, Orn; Remenar, Julius
Patent: US2005/267209 A1, 2005 ; Title/Abstract Full Text Show Details
leukemia
Peterson, Matthew; Bourghol Hickey, Magali; Oliveira, Mark; Almarsson, Orn; Remenar, Julius
Patent: US2005/267209 A1, 2005 ; Title/Abstract Full Text Show Details
acute lymphocitic leukemia
Peterson, Matthew; Bourghol Hickey, Magali; Oliveira, Mark; Almarsson, Orn; Remenar, Julius
Patent: US2005/267209 A1, 2005 ; Title/Abstract Full Text Show Details
acute lymphoblastic leukemia
Peterson, Matthew; Bourghol Hickey, Magali; Oliveira, Mark; Almarsson, Orn; Remenar, Julius
Patent: US2005/267209 A1, 2005 ; Title/Abstract Full Text Show Details
B-cell lymphoma
Peterson, Matthew; Bourghol Hickey, Magali; Oliveira, Mark; Almarsson, Orn; Remenar, Julius
Patent: US2005/267209 A1, 2005 ; Title/Abstract Full Text Show Details
T-cell-Lymphoma
Peterson, Matthew; Bourghol Hickey, Magali; Oliveira, Mark; Almarsson, Orn; Remenar, Julius
Patent: US2005/267209 A1, 2005 ; Title/Abstract Full Text Show Details
Hodgkin's lymphoma
Peterson, Matthew; Bourghol Hickey, Magali; Oliveira, Mark; Almarsson, Orn; Remenar, Julius
Patent: US2005/267209 A1, 2005 ; Title/Abstract Full Text Show Details
non-Hodgkin's lymphoma
Peterson, Matthew; Bourghol Hickey, Magali; Oliveira, Mark; Almarsson, Orn; Remenar, Julius
Patent: US2005/267209 A1, 2005 ; Title/Abstract Full Text Show Details
hairy cell lymphoma
Peterson, Matthew; Bourghol Hickey, Magali; Oliveira, Mark; Almarsson, Orn; Remenar, Julius
Patent: US2005/267209 A1, 2005 ; Title/Abstract Full Text Show Details
Burkett's lymphoma
Peterson, Matthew; Bourghol Hickey, Magali; Oliveira, Mark; Almarsson, Orn; Remenar, Julius
Patent: US2005/267209 A1, 2005 ; Title/Abstract Full Text Show Details
hematopoietic tumors of myeloid lineage
Peterson, Matthew; Bourghol Hickey, Magali; Oliveira, Mark; Almarsson, Orn; Remenar, Julius
Patent: US2005/267209 A1, 2005 ; Title/Abstract Full Text Show Details
acute myelogenous leukemias
Peterson, Matthew; Bourghol Hickey, Magali; Oliveira, Mark; Almarsson, Orn; Remenar, Julius
Patent: US2005/267209 A1, 2005 ; Title/Abstract Full Text Show Details
chronic myelogenous leukemias
Peterson, Matthew; Bourghol Hickey, Magali; Oliveira, Mark; Almarsson, Orn; Remenar, Julius
Patent: US2005/267209 A1, 2005 ; Title/Abstract Full Text Show Details
myelodysplastic syndrome
Peterson, Matthew; Bourghol Hickey, Magali; Oliveira, Mark; Almarsson, Orn; Remenar, Julius
Patent: US2005/267209 A1, 2005 ; Title/Abstract Full Text Show Details
promyelocytic leukemia
Peterson, Matthew; Bourghol Hickey, Magali; Oliveira, Mark; Almarsson, Orn; Remenar, Julius
Patent: US2005/267209 A1, 2005 ; Title/Abstract Full Text Show Details
tumors of mesenchymal origin
Peterson, Matthew; Bourghol Hickey, Magali; Oliveira, Mark; Almarsson, Orn; Remenar, Julius
Patent: US2005/267209 A1, 2005 ; Title/Abstract Full Text Show Details
fibrosarcoma
Peterson, Matthew; Bourghol Hickey, Magali; Oliveira, Mark; Almarsson, Orn; Remenar, Julius
Patent: US2005/267209 A1, 2005 ; Title/Abstract Full Text Show Details
rhabdomyosarcoma
Peterson, Matthew; Bourghol Hickey, Magali; Oliveira, Mark; Almarsson, Orn; Remenar, Julius
Patent: US2005/267209 A1, 2005 ; Title/Abstract Full Text Show Details
soft tissue sarcoma
Peterson, Matthew; Bourghol Hickey, Magali; Oliveira, Mark; Almarsson, Orn; Remenar, Julius
Patent: US2005/267209 A1, 2005 ; Title/Abstract Full Text Show Details
bone sarcoma
Peterson, Matthew; Bourghol Hickey, Magali; Oliveira, Mark; Almarsson, Orn; Remenar, Julius
Patent: US2005/267209 A1, 2005 ; Title/Abstract Full Text Show Details
tumors of the central nervous system
Peterson, Matthew; Bourghol Hickey, Magali; Oliveira, Mark; Almarsson, Orn; Remenar, Julius
Patent: US2005/267209 A1, 2005 ; Title/Abstract Full Text Show Details
Tumors of the peripheral nervous system
Peterson, Matthew; Bourghol Hickey, Magali; Oliveira, Mark; Almarsson, Orn; Remenar, Julius
Patent: US2005/267209 A1, 2005 ; Title/Abstract Full Text Show Details
astrocytoma
Peterson, Matthew; Bourghol Hickey, Magali; Oliveira, Mark; Almarsson, Orn; Remenar, Julius
Patent: US2005/267209 A1, 2005 ; Title/Abstract Full Text Show Details
neuroblastoma
Peterson, Matthew; Bourghol Hickey, Magali; Oliveira, Mark; Almarsson, Orn; Remenar, Julius
Patent: US2005/267209 A1, 2005 ; Title/Abstract Full Text Show Details
glioma
Peterson, Matthew; Bourghol Hickey, Magali; Oliveira, Mark; Almarsson, Orn; Remenar, Julius
Patent: US2005/267209 A1, 2005 ; Title/Abstract Full Text Show Details
schwannomas
Peterson, Matthew; Bourghol Hickey, Magali; Oliveira, Mark; Almarsson, Orn; Remenar, Julius
Patent: US2005/267209 A1, 2005 ; Title/Abstract Full Text Show Details
melanoma
Peterson, Matthew; Bourghol Hickey, Magali; Oliveira, Mark; Almarsson, Orn; Remenar, Julius
Patent: US2005/267209 A1, 2005 ; Title/Abstract Full Text Show Details
seminoma
Peterson, Matthew; Bourghol Hickey, Magali; Oliveira, Mark; Almarsson, Orn; Remenar, Julius
Patent: US2005/267209 A1, 2005 ; Title/Abstract Full Text Show Details
teratocarcinoma
Peterson, Matthew; Bourghol Hickey, Magali; Oliveira, Mark; Almarsson, Orn; Remenar, Julius
Patent: US2005/267209 A1, 2005 ; Title/Abstract Full Text Show Details
osteosarcoma
Peterson, Matthew; Bourghol Hickey, Magali; Oliveira, Mark; Almarsson, Orn; Remenar, Julius
Patent: US2005/267209 A1, 2005 ; Title/Abstract Full Text Show Details
xenoderoma pigmentosum
Peterson, Matthew; Bourghol Hickey, Magali; Oliveira, Mark; Almarsson, Orn; Remenar, Julius
Patent: US2005/267209 A1, 2005 ;
Title/Abstract Full Text Show Details
Peterson, Matthew; Bourghol Hickey, Magali; Oliveira, Mark; Almarsson, Orn; Remenar, Julius
Patent: US2005/267209 A1, 2005 ;
keratoctanthoma
Title/Abstract Full Text Show Details
Peterson, Matthew; Bourghol Hickey, Magali; Oliveira, Mark; Almarsson, Orn; Remenar, Julius
Patent: US2005/267209 A1, 2005 ;
thyroid follicular cancer
Title/Abstract Full Text Show Details
Peterson, Matthew; Bourghol Hickey, Magali; Oliveira, Mark; Almarsson, Orn; Remenar, Julius
Patent: US2005/267209 A1, 2005 ;
Kaposi's sarcoma
Title/Abstract Full Text Show Details
40
mixture (composition completely given) :
(-)-Modafinil dibenzhydryl disulfide (+)-Modafinil
Reaxys Registry Number: 18793945 Type of Substance: mixture (composition completely given)
0 prep out of 3 reactions.
1
Bioactivity (1)
1
Hide Details
Composition dibenzhydryl disulfide (1.08 - 1.74 percent)
41
mixture (composition partially given) :
2-[(diphenylmethyl)sulfinyl]acetamide d-N,a-dimethylphenethylamine
(-)-Modafinil (96.9 - 97.7 percent)
(+)-Modafinil (0.04 - 0.06 percent)
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Reaxys Registry Number: 27703154 Type of Substance: mixture (composition partially given)
no reactions.
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Composition 2-[(diphenylmethyl)sulfinyl]acetamide
d-N,a-dimethylphenethylamine
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Bioactivity Pharmacological Data (1) 1 of 1
42
Comment (Pharmacological Data)
physiological behaviour discussed
Reference
Gonzlez, Betina; Raineri, Mariana; Cadet, Jean Lud; Garca-Rill, Edgar; Urbano, Francisco J.; Bisagno, Veronica
Neuropharmacology, 2014 , vol. 87, p. 188 - 197 Title/Abstract Full Text View citing articles Show Details
mixture (composition partially given) :
2,5-bis-(2,2,2-Trifluoroethoxy)-n-(2-piperidyl-methyl)benzamid 2-[(diphenylmethyl)sulfinyl]acetamide
Reaxys Registry Number: 27778049 Type of Substance: mixture (composition partially given)
no reactions.
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Composition 2,5-bis-(2,2,2-Trifluoroethoxy)-n-(2-piperidyl-methyl)-benzamid
2-[(diphenylmethyl)sulfinyl]acetamide
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Bioactivity Pharmacological Data (1) 1 of 1
Location
Page/Page column
Comment (Pharmacological Data)
physiological behaviour discussed
Reference
COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES; MOUTHON, Franck; CHARVERIAT, Mathieu
Patent: WO2015/11246 A1, 2015 ; Title/Abstract Full Text Show Details
Bioactivity (1) Other Data (52)
1
Other Data Use (52) Use Pattern
Location
Reference
Kleine-Levin syndrome
Page/Page column 41-42
COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES; MOUTHON, Franck; CHARVERIAT, Mathieu
Patent: WO2015/11246 A1, 2015 ; Title/Abstract Full Text Show Details
Parkinson disease
Page/Page column 41-42
COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES; MOUTHON, Franck; CHARVERIAT, Mathieu
Patent: WO2015/11246 A1, 2015 ; Title/Abstract Full Text Show Details
Periodic Lim Movement Disorders (PLMD)
Page/Page column 41-42
COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES; MOUTHON, Franck; CHARVERIAT, Mathieu
Patent: WO2015/11246 A1, 2015 ; Title/Abstract Full Text Show Details
Pharmaceuticals
Page/Page column 41-42
COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES; MOUTHON, Franck; CHARVERIAT, Mathieu
Patent: WO2015/11246 A1, 2015 ; Title/Abstract Full Text Show Details
alertness disorders
Page/Page column 41-42
COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES; MOUTHON, Franck; CHARVERIAT, Mathieu
Patent: WO2015/11246 A1, 2015 ; Title/Abstract Full Text Show Details
anxiety disorders
Page/Page column 41-42
COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES; MOUTHON, Franck; CHARVERIAT, Mathieu
Patent: WO2015/11246 A1, 2015 ; Title/Abstract Full Text Show Details
attention deficit hyperactivity disorder (ADHD)
Page/Page column 41-42
COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES; MOUTHON, Franck; CHARVERIAT, Mathieu
Patent: WO2015/11246 A1, 2015 ; Title/Abstract Full Text Show Details
attention disorders
Page/Page column 41-42
COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES; MOUTHON, Franck; CHARVERIAT, Mathieu
Patent: WO2015/11246 A1, 2015 ; Title/Abstract Full Text Show Details
bipolar disorder
Page/Page column 41-42
COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES; MOUTHON, Franck; CHARVERIAT, Mathieu
Patent: WO2015/11246 A1, 2015 ; Title/Abstract Full Text Show Details
breathing difficulty and fatigue, notably due to cancer, neurodegenerative disorders, menopause, traumatic brain injuries, viral infection or post-myelitis, or to fibromyalgia
Page/Page column 41-42
COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES; MOUTHON, Franck; CHARVERIAT, Mathieu
Patent: WO2015/11246 A1, 2015 ; Title/Abstract Full Text Show Details
cataplexy in narcoleptic patients
Page/Page column 41-42
COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES; MOUTHON, Franck; CHARVERIAT, Mathieu
Patent: WO2015/11246 A1, 2015 ; Title/Abstract Full Text Show Details
central sleep apnea
Page/Page column 41-42
COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES; MOUTHON, Franck; CHARVERIAT, Mathieu
Patent: WO2015/11246 A1, 2015 ; Title/Abstract Full Text Show Details
chronic renal failure
Page/Page column 41-42
COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES; MOUTHON, Franck; CHARVERIAT, Mathieu
Patent: WO2015/11246 A1, 2015 ; Title/Abstract Full Text Show Details
circadian rhythm disorders
Page/Page column 41-42
COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES; MOUTHON, Franck; CHARVERIAT, Mathieu
Patent: WO2015/11246 A1, 2015 ; Title/Abstract Full Text Show Details
dementia
Page/Page column 41-42
COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES; MOUTHON, Franck; CHARVERIAT, Mathieu
Patent: WO2015/11246 A1, 2015 ; Title/Abstract Full Text Show Details
dependence or addiction (to games, drugs, alcohol, tobacco, etc.)
Page/Page column 41-42
COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES; MOUTHON, Franck; CHARVERIAT, Mathieu
Patent: WO2015/11246 A1, 2015 ; Title/Abstract Full Text Show Details
depression
Page/Page column 41-42
COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES; MOUTHON, Franck; CHARVERIAT, Mathieu
Patent: WO2015/11246 A1, 2015 ; Title/Abstract Full Text Show Details
disorders after sleep restriction or sleep deprivation
Page/Page column 41-42
COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES; MOUTHON, Franck; CHARVERIAT, Mathieu
Patent: WO2015/11246 A1, 2015 ; Title/Abstract Full Text Show Details
enhancing the memory
Page/Page column 41-42
COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES; MOUTHON, Franck; CHARVERIAT, Mathieu
Patent: WO2015/11246 A1, 2015 ; Title/Abstract Full Text Show Details
excessive daytime sleepiness (EDS)
Page/Page column 41-42
COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES; MOUTHON, Franck; CHARVERIAT, Mathieu
Patent: WO2015/11246 A1, 2015 ; Title/Abstract Full Text Show Details
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fecal or urinary incontinence
Page/Page column 41-42
COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES; MOUTHON, Franck; CHARVERIAT, Mathieu
Patent: WO2015/11246 A1, 2015 ; Title/Abstract Full Text Show Details
hyperphagia
Page/Page column 41-42
COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES; MOUTHON, Franck; CHARVERIAT, Mathieu
Patent: WO2015/11246 A1, 2015 ; Title/Abstract Full Text Show Details
idiopathic hypersomnia
Page/Page column 41-42
COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES; MOUTHON, Franck; CHARVERIAT, Mathieu
Patent: WO2015/11246 A1, 2015 ; Title/Abstract Full Text Show Details
insomnia
Page/Page column 41-42
COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES; MOUTHON, Franck; CHARVERIAT, Mathieu
Patent: WO2015/11246 A1, 2015 ; Title/Abstract Full Text Show Details
insufficient sleep time
Page/Page column 41-42
COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES; MOUTHON, Franck; CHARVERIAT, Mathieu
Patent: WO2015/11246 A1, 2015 ;
Title/Abstract Full Text Show Details
jet-lag
Page/Page column 41-42
COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES; MOUTHON, Franck; CHARVERIAT, Mathieu
Patent: WO2015/11246 A1, 2015 ; Title/Abstract Full Text Show Details
liver failure
Page/Page column 41-42
COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES; MOUTHON, Franck; CHARVERIAT, Mathieu
Patent: WO2015/11246 A1, 2015 ; Title/Abstract Full Text Show Details
maintaining healthy subjects awake for long-lasting periods of time
Page/Page column 41-42
COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES; MOUTHON, Franck; CHARVERIAT, Mathieu
Patent: WO2015/11246 A1, 2015 ; Title/Abstract Full Text Show Details
malaise
Page/Page column 41-42
COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES; MOUTHON, Franck; CHARVERIAT, Mathieu
Patent: WO2015/11246 A1, 2015 ; Title/Abstract Full Text Show Details
manic episode
Page/Page column 41-42
COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES; MOUTHON, Franck; CHARVERIAT, Mathieu
Patent: WO2015/11246 A1, 2015 ; Title/Abstract Full Text Show Details
medication-induced somnolence (due to benzodiazepines, barbiturates, sleeping pills, antidepressants, anti-psychotics...)
Page/Page column 41-42
COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES; MOUTHON, Franck; CHARVERIAT, Mathieu
Patent: WO2015/11246 A1, 2015 ; Title/Abstract Full Text Show Details
mood disorders
Page/Page column 41-42
COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES; MOUTHON, Franck; CHARVERIAT, Mathieu
Patent: WO2015/11246 A1, 2015 ; Title/Abstract Full Text Show Details
multiple sclerosis
Page/Page column 41-42
COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES; MOUTHON, Franck; CHARVERIAT, Mathieu
Patent: WO2015/11246 A1, 2015 ; Title/Abstract Full Text Show Details
narcolepsy (with or without cataplexy)
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COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES; MOUTHON, Franck; CHARVERIAT, Mathieu
Patent: WO2015/11246 A1, 2015 ; Title/Abstract Full Text Show Details
neuromuscular disorders
Page/Page column 41-42
COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES; MOUTHON, Franck; CHARVERIAT, Mathieu
Patent: WO2015/11246 A1, 2015 ; Title/Abstract Full Text Show Details
obesity
Page/Page column 41-42
COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES; MOUTHON, Franck; CHARVERIAT, Mathieu
Patent: WO2015/11246 A1, 2015 ; Title/Abstract Full Text Show Details
obsessive-compulsive disorder
Page/Page column 41-42
COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES; MOUTHON, Franck; CHARVERIAT, Mathieu
Patent: WO2015/11246 A1, 2015 ; Title/Abstract Full Text Show Details
obstructive sleep apnea/hypopnea (SAHOS)
Page/Page column 41-42
COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES; MOUTHON, Franck; CHARVERIAT, Mathieu
Patent: WO2015/11246 A1, 2015 ;
Title/Abstract Full Text Show Details
parasomnia
Page/Page column 41-42
COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES; MOUTHON, Franck; CHARVERIAT, Mathieu
Patent: WO2015/11246 A1, 2015 ; Title/Abstract Full Text Show Details
post-traumatic stress disorder (PTSD)
Page/Page column 41-42
COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES; MOUTHON, Franck; CHARVERIAT, Mathieu
Patent: WO2015/11246 A1, 2015 ; Title/Abstract Full Text Show Details
premature ejaculation
Page/Page column 41-42
COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES; MOUTHON, Franck; CHARVERIAT, Mathieu
Patent: WO2015/11246 A1, 2015 ; Title/Abstract Full Text Show Details
respiratory disorders
Page/Page column 41-42
COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES; MOUTHON, Franck; CHARVERIAT, Mathieu
Patent: WO2015/11246 A1, 2015 ; Title/Abstract Full Text Show Details
restless legs syndrome (RLS)
Page/Page column 41-42
COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES; MOUTHON, Franck; CHARVERIAT, Mathieu
Patent: WO2015/11246 A1, 2015 ; Title/Abstract Full Text Show Details
rheumatologic disorders
Page/Page column 41-42
COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES; MOUTHON, Franck; CHARVERIAT, Mathieu
Patent: WO2015/11246 A1, 2015 ; Title/Abstract Full Text Show Details
schizophrenia
Page/Page column 41-42
COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES; MOUTHON, Franck; CHARVERIAT, Mathieu
Patent: WO2015/11246 A1, 2015 ; Title/Abstract Full Text Show Details
senility
Page/Page column 41-42
COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES; MOUTHON, Franck; CHARVERIAT, Mathieu
Patent: WO2015/11246 A1, 2015 ; Title/Abstract Full Text Show Details
shift work sleep disorder
Page/Page column 41-42
COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES; MOUTHON, Franck; CHARVERIAT, Mathieu
Patent: WO2015/11246 A1, 2015 ; Title/Abstract Full Text Show Details
sleep disorders
Page/Page column 41-42
COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES; MOUTHON, Franck; CHARVERIAT, Mathieu
Patent: WO2015/11246 A1, 2015 ; Title/Abstract Full Text Show Details
sleepiness
Page/Page column 41-42
COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES; MOUTHON, Franck; CHARVERIAT, Mathieu
Patent: WO2015/11246 A1, 2015 ; Title/Abstract Full Text Show Details
stroke
Page/Page column 41-42
COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES; MOUTHON, Franck; CHARVERIAT, Mathieu
Patent: WO2015/11246 A1, 2015 ; Title/Abstract Full Text Show Details
structural brain disorders
Page/Page column 41-42
COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES; MOUTHON, Franck; CHARVERIAT, Mathieu
Patent: WO2015/11246 A1, 2015 ; Title/Abstract Full Text Show Details
tinnitus
Page/Page column 41-42
COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES; MOUTHON, Franck; CHARVERIAT, Mathieu
Patent: WO2015/11246 A1, 2015 ; Title/Abstract Full Text Show Details
43
Reaxys Registry Number: 27778050 Type of Substance: mixture (composition partially given)
mixture (composition partially given) :
(-)-Flecainide 2-[(diphenylmethyl)sulfinyl]acetamide
no reactions.
Bioactivity (2)
1
Identification Bioactivity (1)
1
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Composition 2-[(diphenylmethyl)sulfinyl]acetamide
(-)-Flecainide
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Bioactivity Pharmacological Data (2) 1 of 2
Comment (Pharmacological Data)
Bioactivities present
Reference
COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES; MOUTHON, Franck; CHARVERIAT, Mathieu
Patent: WO2015/11246 A1, 2015 ; Title/Abstract Full Text Show Details
2 of 2
Location
Page/Page column
Comment (Pharmacological Data)
physiological behaviour discussed
Reference
COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES; MOUTHON, Franck; CHARVERIAT, Mathieu
Patent: WO2015/11246 A1, 2015 ; Title/Abstract Full Text Show Details
44
mixture (composition partially given) :
valproic acid diphenylmethylsulfinylacetamide Hide Details
Chemical Name: VPA+MOD
no reactions.
Reaxys Registry Number: 28534974 Type of Substance: mixture (composition partially given)
Chemical Names and Synonyms VPA+MOD Composition valproic acid
diphenylmethylsulfinylacetamide
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Reference
VPA+MOD
Zolkowska, Dorota; Andres-Mach, Marta; Prisinzano, Thomas E.; Baumann, Michael H.; Luszczki, Jarogniew J.
Psychopharmacology, 2015 , vol. 232, # 14 art. no. 3884, p. 2463 - 2479 Title/Abstract Full Text View citing articles Show Details
Bioactivity Pharmacological Data (1) 1 of 1
45
Comment (Pharmacological Data)
Bioactivities present
Reference
Zolkowska, Dorota; Andres-Mach, Marta; Prisinzano, Thomas E.; Baumann, Michael H.; Luszczki, Jarogniew J.
Psychopharmacology, 2015 , vol. 232, # 14 art. no. 3884, p. 2463 - 2479 Title/Abstract Full Text View citing articles Show Details
mixture (composition partially given) :
carbamazepine diphenylmethylsulfinylacetamide Hide Details
Chemical Name: CBZ+MOD
no reactions.
Reaxys Registry Number: 28534977 Type of Substance: mixture (composition partially given)
Chemical Names and Synonyms CBZ+MOD Composition diphenylmethylsulfinylacetamide
carbamazepine
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Identification Bioactivity (1)
1
Identification Substance Label (1) Label
Reference
CBZ+MOD
Zolkowska, Dorota; Andres-Mach, Marta; Prisinzano, Thomas E.; Baumann, Michael H.; Luszczki, Jarogniew J.
Psychopharmacology, 2015 , vol. 232, # 14 art. no. 3884, p. 2463 - 2479 Title/Abstract Full Text View citing articles Show Details
Bioactivity Pharmacological Data (1) 1 of 1
46
Comment (Pharmacological Data)
Bioactivities present
Reference
Zolkowska, Dorota; Andres-Mach, Marta; Prisinzano, Thomas E.; Baumann, Michael H.; Luszczki, Jarogniew J.
Psychopharmacology, 2015 , vol. 232, # 14 art. no. 3884, p. 2463 - 2479 Title/Abstract Full Text View citing articles Show Details
Chemical Name: PB+MOD
mixture (composition partially given) :
phenobarbital diphenylmethylsulfinylacetamide
no reactions.
Reaxys Registry Number: 28534978 Type of Substance: mixture (composition partially given)
Hide Details Chemical Names and Synonyms PB+MOD Composition
diphenylmethylsulfinylacetamide
phenobarbital
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Reference
PB+MOD
Zolkowska, Dorota; Andres-Mach, Marta; Prisinzano, Thomas E.; Baumann, Michael H.; Luszczki, Jarogniew J.
Psychopharmacology, 2015 , vol. 232, # 14 art. no. 3884, p. 2463 - 2479 Title/Abstract Full Text View citing articles Show Details
Bioactivity Pharmacological Data (1) 1 of 1
Comment (Pharmacological Data)
Bioactivities present
Reference
Zolkowska, Dorota; Andres-Mach, Marta; Prisinzano, Thomas E.; Baumann, Michael H.; Luszczki, Jarogniew J.
Identification Bioactivity (1)
1
Psychopharmacology, 2015 , vol. 232, # 14 art. no. 3884, p. 2463 - 2479 Title/Abstract Full Text View citing articles Show Details
47
mixture (composition partially given) :
5,5-diphenylimidazolidine-2,4-dione diphenylmethylsulfinylacetamide Hide Details
Chemical Name: PHT+MOD
no reactions.
Reaxys Registry Number: 28534979 Type of Substance: mixture (composition partially given)
Chemical Names and Synonyms PHT+MOD Composition 5,5-diphenylimidazolidine-2,4-dione
diphenylmethylsulfinylacetamide
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Identification Substance Label (1) Label
Reference
PHT+MOD
Zolkowska, Dorota; Andres-Mach, Marta; Prisinzano, Thomas E.; Baumann, Michael H.; Luszczki, Jarogniew J.
Psychopharmacology, 2015 , vol. 232, # 14 art. no. 3884, p. 2463 - 2479 Title/Abstract Full Text View citing articles Show Details
Bioactivity Pharmacological Data (1) 1 of 1
Comment (Pharmacological Data)
Bioactivities present
Reference
Zolkowska, Dorota; Andres-Mach, Marta; Prisinzano, Thomas E.; Baumann, Michael H.; Luszczki, Jarogniew J.
Psychopharmacology, 2015 , vol. 232, # 14 art. no. 3884, p. 2463 - 2479 Title/Abstract Full Text View citing articles Show Details
Identification Bioactivity (1)
1