2-Methyl-1-phenylpropan-2-amine (Phentermine)

Reaxys

PubChem

eMolecules

Reactions (281)

Substances (3)

Structure

Citations (440)

Structure/Compound Data Chemical Name: Phentermin Reaxys Registry Number: 970319

CAS Registry Number: 122-09-8 Type of Substance: isocyclic Molecular Formula: C10H15N Linear Structure Formula: C10H15N Molecular Weight: 149.236 InChI Key: DHHVAGZRUROJKS-UHFFFAOYSA-N

1

N° of preparations All Preps | All Reactions 31 prep out of 237 reactions.

Available Data

N° of ref.

Identification Physical Data (23) Spectra (20) Bioactivity (47) Other Data (380)

390

Synthesize | Hide Details Find similar Chemical Names and Synonyms Phentermin, Phentermine Identification Substance Label (15) Label

Reference

D

Yuan, Ming; Chen, Li; Wang, Junwei; Chen, Shenjie; Wang, Kongchao; Xue, Yongbo; Yao, Guangmin; Luo, Zengwei; Zhang, Yonghui

Organic Letters, 2015 , vol. 17, # 2 p. 346 - 349 Title/Abstract Full Text View citing articles Show Details

Formula 1

Institute of Pharmacology and Toxicology Academy of Military Medical Sciences P.L.A. China; LI, Song; GAO, Chunsheng; ZHONG, Wu; WANG, Yuli; YANG, Meiyan; SHAN, Li; ZHOU, Xinbo; ZHENG, Zhibing; WANG, Xiaokui

Patent: EP2829266 A1, 2015 ; Title/Abstract Full Text Show Details

Institute of Pharmacology and Toxicology Academy of Military Medical Sciences P.L.A. China; LI, Song; Gao, Chunseng; Zhong, Wu; Wang, Yuli;

Yang, Meiyan; Shan, Li; Zhou, Xinbo; Zheng, Zhibing; Wang, Xiaokui

Patent: US2015/44295 A1, 2015 ; Title/Abstract Full Text Show Details

1d

Tanaka; Yamamura; Nakane; Kitamura

Chemical Communications, 2015 , vol. 51, # 66 p. 13110 - 13112 Title/Abstract Full Text View citing articles Show Details

2d

Tanaka, Shinji; Saburi, Hajime; Murase, Takanori; Yoshimura, Masahiro; Kitamura, Masato

Journal of Organic Chemistry, 2006 , vol. 71, # 12 p. 4682 - 4684 Title/Abstract Full Text View citing articles Show Details

Rodrguez, Aleix; Albert, Joan; Ariza, Xavier; Garcia, Jordi; Granell, Jaume; Farrs, Jaume; La Mela, Andrea; Nicols, Ernesto

Journal of Organic Chemistry, 2014 , vol. 79, # 20 p. 9578 - 9585 Title/Abstract Full Text View citing articles Show Details

3k

Albert, Joan; Ariza, Xavier; Calvet, Teresa; Font-Bardia, Merce; Garcia, Jordi; Granell, Jaume; Lamela, Andrea; Lopez, Blanca; Martinez, Manuel; Ortega, Laura; Rodriguez, Aleix; Santos, David

Organometallics, 2013 , vol. 32, # 2 p. 649 - 659 Title/Abstract Full Text View citing articles Show Details

15

Huang, Xianhai; Palani, Anandan; Xiao, Dong; Aslanian, Robert; Shih, Neng-Yang

Organic Letters, 2004 , vol. 6, # 25 p. 4795 - 4798 Title/Abstract Full Text View citing articles Show Details

Ito, Nobuhiro; Watahiki, Tsutomu; Maesawa, Tsuneaki; Maegawa, Tomohiro; Sajiki, Hironao

Synthesis, 2008 , # 9 art. no. F03608SS, p. 1467 - 1478 Title/Abstract Full Text View citing articles Show Details

49

Lewin, Anita H.; Navarro, Hernan A.; Wayne Mascarella

Bioorganic and Medicinal Chemistry, 2008 , vol. 16, # 15 p. 7415 - 7423 Title/Abstract Full Text View citing articles Show Details

12

Lee, Peter J.; Chen, Weibin; Gebler, John C.

Analytical Chemistry, 2004 , vol. 76, # 16 p. 4888 - 4893 Title/Abstract Full Text View citing articles Show Details

phen

Tao, Rui; Fray, Anne; Aspley, Sue; Brammer, Richard; Heal, David; Auerbach, Sidney

European Journal of Pharmacology, 2002 , vol. 445, # 1-2 p. 69 - 81 Title/Abstract Full Text View citing articles Show Details

9b

Gai; Grigg; Collard; Muir

Chemical Communications, 2001 , # 18 p. 1712 - 1713 Title/Abstract Full Text View citing articles Show Details

3d (free base)

Jirgensons; Kauss; Kalvinsh; Gold

Synthesis, 2000 , # 12 p. 1709 - 1712 Title/Abstract Full Text View citing articles Show Details

8

Adams, Mortimer H.; Ameer, Farouk; Green, Ivan R.; Syce, James A.

Synthetic Communications, 1999 , vol. 29, # 14 p. 2419 - 2430 Title/Abstract Full Text View citing articles Show Details

Merck 7415

Wojnicki, Francis H. E.; Rothman, Richard B.; Rice, Kenner C.; Glowa, John R.

Journal of Pharmacology and Experimental Therapeutics, 1999 , vol. 288, # 2 p. 550 - 560 Title/Abstract Full Text View citing articles Show Details

amine a

Deyrup; Nowicki; Richards; Otero; Harrison; Baker

Naunyn-Schmiedeberg's Archives of Pharmacology, 1999 , vol. 359, # 3 p. 168 - 177 Title/Abstract Full Text View citing articles Show Details

PTM

Nakahara, Yuji; Kikura, Ruri

Archives of Toxicology, 1996 , vol. 70, # 12 p. 841 - 849 Title/Abstract Full Text View citing articles Show Details

Patent-Specific Data (5) Prophetic Compound

Related Markush Structure (RN)

Reference

22958454

Pathway Therapeutics Inc.

Patent: US2012/252802 A1, 2012 ; Title/Abstract Full Text Show Details

18464592

SUN PHARMA ADVANCED RESEARCH COMPANY LTD

Patent: WO2008/111096 A2, 2008 ;

Title/Abstract Full Text Show Details

Caron, Marc G.; Sotnikova, Tatyana D.; Gainetdinov, Raul R.

Patent: US2007/27208 A1, 2007 ;

11337200

Title/Abstract Full Text Show Details

AstraZeneca AB

Patent: US6369064 B1, 2002 ;

20826382

Title/Abstract Full Text Show Details

prophetic product

University of Florida

Patent: US4771059 A1, 1988 ;

Title/Abstract Full Text Show Details

Derivative (7) Derivative

Comment (Derivative)

Reference

phentermine hydrochloride

Jirgensons; Kauss; Kalvinsh; Gold

Synthesis, 2000 , # 12 p. 1709 - 1712 Title/Abstract Full Text View citing articles Show Details

Hydrochlorid: F: 200grad; IR, NMR

Marquardt; Edwards

The Journal of organic chemistry, 1972 , vol. 37, # 11 p. 1861 - 1863 Title/Abstract Full Text View citing articles Show Details

Hydrochlorid: IR

Mesley; Evans

Journal of Pharmacy and Pharmacology, 1970 , vol. 22, p. 321,325-329 Full Text Show Details

Hydrochlorid C10H15N*HCl. Duennschichtchromatogra. Verh. u.

Nachweisreaktionen

Palitzsch et al.

Pharmazie, 1968 , vol. 23, p. 246,248 Full Text Show Details

Hydrochlorid = Wilpo

New Drugs

American Journal of Pharmacy and the Sciences Supporting Public Health (19371978), 1962 , vol. 134, p. 6,21 Full Text Show Details

Hydrochlorid. F:200-201grad(Thomas-Hoover-Apparat; unkorr.)

Shetty

Journal of Organic Chemistry, 1961 , vol. 26, p. 3002 Full Text View citing articles Show Details

Pikrat. F:109-110grad(Thomas-Hoover-Apparat;unkorr.)

Shetty

Journal of Organic Chemistry, 1961 , vol. 26, p. 3002 Full Text View citing articles Show Details

Physical Data Boiling Point (7) Boiling Point

Pressure (Boiling Point)

Reference

68 °C

7.5 Torr

Wannagat, U.; Damrath, V.; Harder, U.

Monatshefte fuer Chemie, 1994 , vol. 125, # 11 p. 1159 - 1170 Title/Abstract Full Text View citing articles Show Details

110 °C

20 Torr

Christol et al.

Bulletin de la Societe Chimique de France, 1961 , p. 2317 Full Text Show Details

106.5 - 107 °C

31 Torr

Girault-Vexlearschi

Bulletin de la Societe Chimique de France, 1956 , p. 589,596 Full Text Show Details

86 - 88 °C

13 Torr

Moed et al.

Recueil des Travaux Chimiques des Pays-Bas, 1955 , vol. 74, p. 919,922 Full Text Show Details

94 °C

15 Torr

Kornblum; Iffland

Journal of the American Chemical Society, 1949 , vol. 71, p. 2137,2138,2140 Full Text View citing articles Show Details

89 - 90 °C

10 Torr

Zenitz; Macks; Moore

Journal of the American Chemical Society, 1948 , vol. 70, p. 955 Full Text View citing articles Show Details

203 - 205 °C

760 Torr

Mentzer

Comptes Rendus Hebdomadaires des Seances de l'Academie des Sciences, vol. 213>1941>581, p. 583 Full Text Show Details

Refractive Index (3) Refractive Index

Wavelength (Refractive Index)

Temperature (Refractive Index)

Reference

1.5125

589 nm

20 °C

Wannagat, U.; Damrath, V.; Harder, U.

Monatshefte fuer Chemie, 1994 , vol. 125, # 11 p. 1159 - 1170 Title/Abstract Full Text View citing articles Show Details

1.5132

589 nm

20 °C

Kornblum; Iffland

Journal of the American Chemical Society, 1949 , vol. 71, p. 2137,2138,2140 Full Text View citing articles Show Details

1.513

589 nm

20 °C

Zenitz; Macks; Moore

Journal of the American Chemical Society, 1948 , vol. 70, p. 955 Full Text View citing articles Show Details

Chromatographic Data (3) Chromatographic data

Reference

HPLC (High performance liquid chromatography)

Paíga, Paula; Rodrigues, Manuela J.E.; Correia, Manuela; Amaral, Joana S.; Oliveira, M. Beatriz P.P.; Delerue-Matos, Cristina

European Journal of Pharmaceutical Sciences, 2017 , vol. 99, p. 219 - 227 Title/Abstract Full Text Show Details

LC (Liquid chromatography)

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

UPLC (Ultra performance liquid chromatography)

Lin, Huei-Ru; Liao, Chao-Chuan; Lin, Tzu-Chieh

Rapid Communications in Mass Spectrometry, 2014 , vol. 28, # 19 p. 2043 - 2053 Title/Abstract Full Text View citing articles Show Details

Crystal Property Description (1) Colour & Other Properties yellow

Location

Reference

supporting information

Albert, Joan; Ariza, Xavier; Calvet, Teresa; Font-Bardia, Merce; Garcia, Jordi; Granell, Jaume; Lamela, Andrea; Lopez, Blanca; Martinez, Manuel; Ortega, Laura; Rodriguez, Aleix; Santos, David

Organometallics, 2013 , vol. 32, # 2 p. 649 - 659 Title/Abstract Full Text View citing articles Show Details

Dissociation Exponent (2) Dissociation Exponent (pK)

Temperature (Dissociation Exponent)

Solvent (Dissociation Exponent)

Method (Dissociation Exponent)

Type (Dissociation Exponent)

Comment (Dissociation Exponent)

9.33 - 10.12

26 °C

methanol H2O

a1/apparent

Ratio of solvents: 10 to 80 percent v/v MeOH

Canals; Valko; Bosch; Hill; Roses

Analytical Chemistry, 2001 , vol. 73, # 20 p. 4937 - 4945 Title/Abstract Full Text View citing articles Show Details

10.13

20 °C

H2O

potentiometric

a/thermodynamic

Girault-Vexlearschi

Bulletin de la Societe Chimique de France, 1956 , p. 589,596 Full Text Show Details

Reference

Enthalpies of Other Phase Transitions (1) Comment (Enthalpies of Other Phase Transitions)

Reference

Enthalpies of other phase transition(s) given

Gobble, Chase; Rath, Nigam; Chickos, James

Journal of Chemical and Engineering Data, 2013 , vol. 58, # 9 p. 2600 - 2609 Title/Abstract Full Text View citing articles Show Details

Further Information (5) Description (Further Information)

Reference

Further information

Cartoni et al.

Bollettino Chimico Farmaceutico, 1976 , vol. 115, p. 347,350 Full Text Show Details

Further information

Reisch; Alfes; Moellmann

Die Pharmazie, 1968 , vol. 23, # 5 p. 245 - 246 Title/Abstract Full Text View citing articles Show Details

Further information

Palitzsch et al.

Pharmazie, 1968 , vol. 23, p. 246,248 Full Text Show Details

Further information

New Drugs

American Journal of Pharmacy and the Sciences Supporting Public Health (1937-1978), 1962 , vol. 134, p. 6,21 Full Text Show Details

Further information

Shetty

Journal of Organic Chemistry, 1961 , vol. 26, p. 3002 Full Text View citing articles Show Details

Liquid/Liquid Systems (MCS) (1) Description (Liquid/Liquid Systems (MCS))

Reference

Distribution between solvent 1 + 2

Mihailova; Testa

European Journal of Medicinal Chemistry, 1978 , vol. 13, # 1 p. 49 - 52 Title/Abstract Full Text View citing articles Show Details

Spectra NMR Spectroscopy (7) Description (NMR Spectroscopy)

Nucleus (NMR Spectroscopy)

Solvents (NMR Spectroscopy)

Temperature (NMR Spectroscopy)

Frequency (NMR Spectroscopy)

Chemical shifts

1H

chloroform-d1

Chemical shifts

13C

chloroform-d1

Chemical shifts Spectrum

1H

Chemical shifts Spectrum

Chemical shifts

Location

Reference

400 MHz

supporting information

Albert, Joan; Ariza, Xavier; Calvet, Teresa; Font-Bardia, Merce; Garcia, Jordi; Granell, Jaume; Lamela, Andrea; Lopez, Blanca; Martinez, Manuel; Ortega, Laura; Rodriguez, Aleix; Santos, David

Organometallics, 2013 , vol. 32, # 2 p. 649 - 659 Title/Abstract Full Text View citing articles Show Details

101 MHz

supporting information

Albert, Joan; Ariza, Xavier; Calvet, Teresa; Font-Bardia, Merce; Garcia, Jordi; Granell, Jaume; Lamela, Andrea; Lopez, Blanca; Martinez, Manuel; Ortega, Laura; Rodriguez, Aleix; Santos, David

Organometallics, 2013 , vol. 32, # 2 p. 649 - 659 Title/Abstract Full Text View citing articles Show Details

chloroform-d1

24.94 °C

400 MHz

supporting information

Gildner, Peter G.; Gietter, Amber A. S.; Cui, Di; Watson, Donald A.

Journal of the American Chemical Society, 2012 , vol. 134, # 24 p. 9942 - 9945 Title/Abstract Full Text View citing articles Show Details

13C

chloroform-d1

24.94 °C

101 MHz

supporting information

Gildner, Peter G.; Gietter, Amber A. S.; Cui, Di; Watson, Donald A.

Journal of the American Chemical Society, 2012 , vol. 134, # 24 p. 9942 - 9945 Title/Abstract Full Text View citing articles Show Details

1H

CDCl3

600 MHz

Tanaka, Shinji; Saburi, Hajime; Murase, Takanori; Yoshimura, Masahiro; Kitamura, Masato

Journal of Organic Chemistry, 2006 , vol. 71, # 12 p. 4682 4684 Title/Abstract Full Text View citing articles Show Details

Spectrum

1H

CDCl3

600 MHz

Tanaka, Shinji; Saburi, Hajime; Murase, Takanori; Yoshimura, Masahiro; Kitamura, Masato

Journal of Organic Chemistry, 2006 , vol. 71, # 12 p. 4682 4684 Title/Abstract Full Text View citing articles Show Details

Chemical shifts

1H

CCl4

Wannagat, U.; Damrath, V.; Harder, U.

Monatshefte fuer Chemie, 1994 , vol. 125, # 11 p. 1159 - 1170 Title/Abstract Full Text View citing articles Show Details

IR Spectroscopy (3) Description (IR Spectroscopy)

Solvent (IR Spectroscopy)

Location

Comment (IR Spectroscopy)

Reference

ATR (attenuated total reflectance) Bands

neat (no solvent, solid phase)

supporting information

Albert, Joan; Ariza, Xavier; Calvet, Teresa; Font-Bardia, Merce; Garcia, Jordi; Granell, Jaume; Lamela, Andrea; Lopez, Blanca; Martinez, Manuel; Ortega, Laura; Rodriguez, Aleix; Santos, David

Organometallics, 2013 , vol. 32, # 2 p. 649 - 659 Title/Abstract Full Text View citing articles Show Details

Bands

supporting information

film

Gildner, Peter G.; Gietter, Amber A. S.; Cui, Di; Watson, Donald A.

Journal of the American Chemical Society, 2012 , vol. 134, # 24 p. 9942 - 9945 Title/Abstract Full Text View citing articles Show Details

IR

Mesley; Evans

Journal of Pharmacy and Pharmacology, 1970 , vol. 22, p. 321,325-329 Full Text Show Details

Mass Spectrometry (10) Location

Comment (Mass Spectrometry)

electrospray ionisation (ESI) spectrum

Jeong, Eun Sook; Kim, So-Hee; Cha, Eun-Ju; Lee, Kang Mi; Kim, Ho Jun; Lee, Sang-Won; Kwon, OhSeung; Lee, Jaeick

Rapid Communications in Mass Spectrometry, 2015 , vol. 29, # 4 p. 367 - 384 Title/Abstract Full Text View citing articles Show Details

Paíga, Paula; Rodrigues, Manuela J.E.; Correia, Manuela; Amaral, Joana S.; Oliveira, M. Beatriz P.P.; Delerue-Matos, Cristina

European Journal of Pharmaceutical Sciences, 2017 , vol. 99, p. 219 - 227 Title/Abstract Full Text Show Details

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, OhSeung; Lee, Jaeick

Rapid Communications in Mass Spectrometry, 2015 , vol. 29, # 4 p. 367 - 384 Title/Abstract Full Text Show Details

liquid chromatography mass spectrometry (LCMS) CID (collision-induced dissociation) spectrum

Lin, Huei-Ru; Liao, Chao-Chuan; Lin, Tzu-Chieh

Rapid Communications in Mass Spectrometry, 2014 , vol. 28, # 19 p. 2043 - 2053 Title/Abstract Full Text View citing articles Show Details

electrospray ionisation (ESI) high resolution mass spectrometry (HRMS) spectrum

supporting information

Albert, Joan; Ariza, Xavier; Calvet, Teresa; Font-Bardia, Merce; Garcia, Jordi; Granell, Jaume; Lamela, Andrea; Lopez, Blanca; Martinez, Manuel; Ortega, Laura; Rodriguez, Aleix; Santos, David

Organometallics, 2013 , vol. 32, # 2 p. 649 - 659 Title/Abstract Full Text View citing articles Show Details

IT (ion trap) CID (collision-induced dissociation) Spectrum

Oberacher, Herbert; Pitterl, Florian; Siapi, Eleni; Steele, Barry R.; Letzel, Thomas; Grosse, Sylvia; Poschner, Bernhard; Tagliaro, Franco; Gottardo, Rossella; Chacko, Silvi A.; Josephs, Jonathan L.

Journal of Mass Spectrometry, 2012 , vol. 47, # 2 p. 263 - 270 Title/Abstract Full Text View citing articles Show Details

HRMS (High resolution mass spectrometry) Spectrum

supporting information

Gildner, Peter G.; Gietter, Amber A. S.; Cui, Di; Watson, Donald A.

Journal of the American Chemical Society, 2012 , vol. 134, # 24 p. 9942 - 9945 Title/Abstract Full Text View citing articles Show Details

Description (Mass Spectrometry)

Reference

ESI (Electrospray ionisation) Spectrum

supporting information

Gildner, Peter G.; Gietter, Amber A. S.; Cui, Di; Watson, Donald A.

Journal of the American Chemical Society, 2012 , vol. 134, # 24 p. 9942 - 9945 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

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

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

Reisch et al.

Journal of Pharmacy and Pharmacology, 1968 , vol. 20, p. 81,85 Full Text Show Details

Cartoni et al.

Bollettino Chimico Farmaceutico, 1976 , vol. 115, p. 347,350 Full Text Show Details

Bioactivity Pharmacological Data (47) 1 of 47

Comment (Pharmacological Data)

Bioactivities present

Reference

Continental Pharma

Patent: US3954871 A1, 1976 ; Title/Abstract Full Text Show Details

Sterling Drug Inc.

Patent: US4374149 A1, 1983 ; Title/Abstract Full Text Show Details

Aktiebolaget Hassle

Patent: US4244969 A1, 1981 ; Title/Abstract Full Text Show Details

Beecham Group Limited

Patent: US4478849 A1, 1984 ; Title/Abstract Full Text Show Details

Santilli,A.A. et al.

Journal of Medicinal Chemistry, 1964 , vol. 7, p. 68 - 72 Full Text View citing articles Show Details

Howe; Crowther; Stephenson; Rao; Smith

Journal of medicinal chemistry, 1968 , vol. 11, # 5 p. 1000 - 1008 Title/Abstract Full Text View citing articles Show Details

Mazur,R.H. et al.

Journal of Medicinal Chemistry, 1970 , vol. 13, p. 1217 - 1221 Full Text View citing articles Show Details

Johnston; McCaleb; Opliger; Laster; Montgomery

Journal of medicinal chemistry, 1971 , vol. 14, # 17 p. 600 - 614 Title/Abstract Full Text View citing articles Show Details

Reisch; Alfes; Kommert; Jantos; Moellmann; Clasing

Die Pharmazie, 1970 , vol. 25, # 5 p. 331 - 334 Title/Abstract Full Text View citing articles Show Details

Hoechst Marion Roussell, Inc.

Patent: US5808071 A1, 1998 ; Title/Abstract Full Text Show Details

Ohno,A. et al.

Bulletin of the Chemical Society of Japan, 1971 , vol. 44, # 2 p. 463 - 467 Full Text View citing articles Show Details

Thuong,N.T.; Chabrier,P.

Bulletin de la Societe Chimique de France, 1975 , p. 2083 - 2088 Full Text View citing articles Show Details

Sankyo Company, Limited

Patent: US5536714 A1, 1996 ;

Title/Abstract Full Text Show Details

Ibanez; Roig; Ruiz; et al.

European Journal of Medicinal Chemistry, 1977 , vol. 12, # 5 p. 459 - 462 Title/Abstract Full Text View citing articles Show Details

Arya,V.P.

Indian Journal of Chemistry, 1975 , vol. 13, p. 1262 - 1266 Full Text View citing articles Show Details

Greene,F.D. et al.

Journal of Organic Chemistry, 1969 , vol. 34, # 8 p. 2263 - 2269 Full Text View citing articles Show Details

Reinecke,M.G.; Daubert,R.G.

Journal of Organic Chemistry, 1973 , vol. 38, p. 3281 - 3287 Full Text View citing articles Show Details

Chugai Seiyaku Kabushiki Kaisha

Patent: US6534546 B1, 2003 ; Title/Abstract Full Text Show Details

NOVARTIS AG; NOVARTIS PHARMA GMBH

Patent: WO2004/16601 A1, 2004 ; Title/Abstract Full Text Show Details

Matin; Rowland

Journal of pharmaceutical sciences, 1972 , vol. 61, # 8 p. 1235 - 1240 Title/Abstract Full Text View citing articles Show Details

2 of 47

Comment (Pharmacological Data)

Bioactivities present

Reference

Schaeffer; Cho; Fischer

Journal of Pharmaceutical Sciences, 1976 , vol. 65, # 1 p. 122 - 126 Title/Abstract Full Text View citing articles Show Details

Beckett; Belanger

Journal of Pharmacy and Pharmacology, 1975 , vol. 27, # 12 p. 928 - 936 Title/Abstract Full Text View citing articles Show Details

NOVARTIS AG; NOVARTIS PHARMA GMBH

Patent: WO2005/49088 A2, 2005 ; Title/Abstract Full Text Show Details

PFIZER PRODUCTS INC.

Patent: WO2005/61506 A1, 2005 ; Title/Abstract Full Text Show Details

PFIZER PRODUCTS INC.

Patent: WO2005/61507 A1, 2005 ; Title/Abstract Full Text Show Details

BLM Group, Inc.

Patent: US2005/222040 A1, 2005 ; Title/Abstract Full Text Show Details

Boehringer Ingelheim International GmbH

Patent: US2005/245500 A1, 2005 ; Title/Abstract Full Text Show Details

Bhanot, Sanjay; Dobie, Kenneth W.

Patent: US2005/261233 A1, 2005 ; Title/Abstract Full Text Show Details

IRM LLC

Patent: WO2005/113506 A1, 2005 ; Title/Abstract Full Text Show Details

Novo Nordisk, A/S

Patent: US6972294 B1, 2005 ; Title/Abstract Full Text Show Details

OREXIGEN THERAPEUTICS, INC.

Patent: WO2006/17504 A1, 2006 ; Title/Abstract Full Text Show Details

Essentialis, Inc.

Patent: US2006/51418 A1, 2006 ; Title/Abstract Full Text Show Details

Yancopoulos, George D.; Wiegand, Stanley J.; Sleeman, Mark W.; Koehler-Stec, Ellen-Marie

Patent: US2006/58224 A1, 2006 ; Title/Abstract Full Text Show Details

Higuchi, John; Li, S. Kevin; Higuchi, William I.; Hastings, Matthew S.

Patent: US2006/88515 A1, 2006 ; Title/Abstract Full Text Show Details

PHARMACOPEIA DRUG DISCOVERY, INC.

Patent: WO2006/44293 A2, 2006 ;

Title/Abstract Full Text Show Details

Kirk, Randal J.

Patent: US2006/100136 A1, 2006 ; Title/Abstract Full Text Show Details

Sterling Drug Inc.

Patent: DE2728641 , 1978 ; Chem.Abstr., 1979 , vol. 90, # 137468 Full Text Show Details

Yamanouchi Pharm.

Patent: FR2299855DE2603417 , 19761976 ; Chem.Abstr., 1976 , vol. 85, # 159632 Full Text Show Details

JOHN I. HASS, INC.

Patent: WO2006/55985 A1, 2006 ; Title/Abstract Full Text Show Details

Elan Corporation, plc

Patent: US2006/121112 A1, 2006 ; Title/Abstract Full Text Show Details

3 of 47

Comment (Pharmacological Data)

Bioactivities present

Reference

ASTRAZENECA AB; ASTRAZENECA UK LIMITED

Patent: WO2006/67428 A2, 2006 ; Title/Abstract Full Text Show Details

Meng, Wei; Hamann, Lawrence G.; Brigance, Robert

Patent: US2006/142576 A1, 2006 ; Title/Abstract Full Text Show Details

BRISTOL-MYERS SQUIBB COMPANY

Patent: WO2006/71752 A1, 2006 ; Title/Abstract Full Text Show Details

PFIZER PRODUCTS INC.

Patent: WO2006/90250 A1, 2006 ; Title/Abstract Full Text Show Details

PROTEMIX CORPORATION LIMITED

Patent: WO2006/104397 A1, 2006 ; Title/Abstract Full Text Show Details

MERCK and CO., INC.

Patent: WO2006/127530 A2, 2006 ; Title/Abstract Full Text Show Details

LABORATORIOS DEL DR. ESTEVE, S.A.

Patent: EP1743636 A1, 2007 ; Title/Abstract Full Text Show Details

AMYLIN PHARMACEUTICALS, INC.

Patent: WO2006/105527 A3, 2006 ; Title/Abstract Full Text Show Details

Caron, Marc G.; Sotnikova, Tatyana D.; Gainetdinov, Raul R.

Patent: US2007/27208 A1, 2007 ; Title/Abstract Full Text Show Details

LABORATORIOS DEL DR.ESTEVE, S.A

Patent: WO2007/9693 A1, 2007 ; Title/Abstract Full Text Show Details

ASTRAZENECA AB; ASTRAZENECA UK LIMITED

Patent: WO2007/10222 A2, 2007 ; Title/Abstract Full Text Show Details

OREXIGEN THERAPEUTICS, INC.

Patent: WO2007/16108 A1, 2007 ; Title/Abstract Full Text Show Details

MELIOR DISCOVERY, INC.

Patent: WO2007/24863 A2, 2007 ; Title/Abstract Full Text Show Details

Schering Corporation

Patent: US2007/66644 A1, 2007 ; Title/Abstract Full Text Show Details

ASTRAZENECA AB; ASTRAZENECA UK LIMITED

Patent: WO2007/39740 A2, 2007 ;

Title/Abstract Full Text Show Details

NOVARTIS AG; NOVARTIS PHARMA GmbH

Patent: WO2007/41366 A1, 2007 ; Title/Abstract Full Text Show Details

Bristol-Myers Squibb Company

Patent: US2007/99913 A1, 2007 ; Title/Abstract Full Text Show Details

AMYLIN PHARMACEUTICALS, INC.

Patent: WO2007/55728 A1, 2007 ; Title/Abstract Full Text Show Details

AMYLIN PHARMACEUTICALS, INC.

Patent: WO2007/55743 A2, 2007 ; Title/Abstract Full Text Show Details

Mallinckrodt Inc.

Patent: US2007/129444 A1, 2007 ; Title/Abstract Full Text Show Details

4 of 47

Comment (Pharmacological Data)

Bioactivities present

Reference

ASTRAZENECA AB

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IRM LLC

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IRM LLC

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GELESIS, INC.

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MERCK FROSST CANADA LTD.

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Comment (Pharmacological Data)

Bioactivities present

Reference

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New Drugs

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Manufactures J.R.Bottu

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Wallace and Tiesnan

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Richey, Herman G.; Cabre, Socorro

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Comment (Pharmacological

Bioactivities present

Data)

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Mohrle; Scharf; Ruhman; Schmid

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Kusachi, Shozo; Thompson, Robert D.; Bugni, William J.; Yamada, Nobuyuki; Olsson, R. A.

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Leclerc; Decker; Schwartz

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Thavonekham, Bounkham

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Comment (Pharmacological Data)

Bioactivities present

Reference

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Mathvink; Barritta; Candelore; Cascieri; Deng; Tota; Strader; Wyvratt; Fisher; Weber

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Wojnicki, Francis H. E.; Rothman, Richard B.; Rice, Kenner C.; Glowa, John R.

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Balcioglu, Aygul; Wurtman, Richard J.

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Canals; Valko; Bosch; Hill; Roses

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Deyrup; Nowicki; Richards; Otero; Harrison; Baker

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El Hadri; Nicolle, Edwige; Leclerc; Pietri-Rouxel; Strosberg; Archimbault

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Villhauer, Edwin B.; Brinkman, John A.; Naderi, Goli B.; Burkey, Bryan F.; Dunning, Beth E.; Prasad, Kapa; Mangold, Bonnie L.; Russell, Mary E.; Hughes, Thomas E.

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Lebsack, Alec D.; Gunzner, Janet; Wang, Bowei; Pracitto, Richard; Schaffhauser, Herve; Santini, Angelina; Aiyar, Jayashree; Bezverkov, Robert; Munoz, Benito; Liu, Wensheng; Venkatraman, Shankar

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Schechter, Martin D.; McBurney, Denise

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Ferrer-Lorente, Raquel; Cabot, Cristina; Fernandez-Lopez, Jose-Antonio; Remesar, Xavier; Alemany, Maria

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Butera, John A.; Jenkins, Douglas J.; Lennox, Joseph R.; Sheldon, Jeffrey H.; Norton, N. Wesley; Warga, Dawn; Argentieri, Thomas M.

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Huang, Xianhai; Palani, Anandan; Xiao, Dong; Aslanian, Robert; Shih, Neng-Yang

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Lee, Peter J.; Chen, Weibin; Gebler, John C.

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8 of 47

Comment (Pharmacological Data)

Bioactivities present

Reference

Tanaka, Shinji; Saburi, Hajime; Murase, Takanori; Yoshimura, Masahiro; Kitamura, Masato

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Bunzow; Sonders; Arttamangkul; Harrison; Zhang; Quigley; Darland; Suchland; Pasumamula; Kennedy; Olson; Magenis; Amara; Grandy

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Tao, Rui; Fray, Anne; Aspley, Sue; Brammer, Richard; Heal, David; Auerbach, Sidney

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Coumar, Mohane Selvaraj; Chang, Chung-Nien; Chen, Chiung-Tong; Chen, Xin; Chien, Chia-Hui; Tsai, Ting-Yueh; Cheng, JaiHong; Wu, Hsin-Yi; Han, Chia-Hung; Wu, Ssu-Hui; Huang, Yu-Wen; Hsu, Tsu; Hsu, Li-Jen; Chao, Yu-Sheng; Hsieh, HsingPang; Jiaang, Weir-Torn

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Sterling Drug Inc.

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University of Florida

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American Home Products Corporation

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Mead Johnson and Company

Patent: US4055658 A1, 1977 ; Title/Abstract Full Text Show Details

NPS Pharmaceuticals, Inc.

Patent: US6429207 B1, 2002 ; Title/Abstract Full Text Show Details

NPS Pharmaceuticals, Inc.; SmithKline Beecham, Corp.; SmithKline Beecham, PLC

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Orexigen Therapeutics, Inc

Patent: US2008/113026 A1, 2008 ; Title/Abstract Full Text Show Details

Bristol-Myers Squibb

Patent: US2008/234366 A1, 2008 ; Title/Abstract Full Text Show Details

BRISTOL-MYERS SQUIBB

Patent: US2008/234367 A1, 2008 ; Title/Abstract Full Text Show Details

SUN PHARMA ADVANCED RESEARCH COMPANY LTD

Patent: WO2008/111096 A2, 2008 ; Title/Abstract Full Text Show Details

ALPEX PHARMA S.A.

Patent: US2008/206327 A1, 2008 ; Title/Abstract Full Text Show Details

Ito, Nobuhiro; Watahiki, Tsutomu; Maesawa, Tsuneaki; Maegawa, Tomohiro; Sajiki, Hironao

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Barak, Larry S.; Salahpour, Ali; Zhang, Xiaodong; Masri, Bernard; Sotnikova, Tatyana D.; Ramsey, Amy J.; Violin, Jonathan D.; Lefkowitz, Robert J.; Caron, Marc G.; Gainetdinov, Raul R.

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Lewin, Anita H.; Navarro, Hernan A.; Wayne Mascarella

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Sattigeri, Jitendra A.; Andappan, Murugaiah M.S.; Kishore, Kaushal; Sethi, Sachin; Kandalkar, Sachin Ramesh; Pal, Chanchal Kumar; Mahajan, Dipak C.; Ahmed, Shahadat; Parkale, Santhosh Sadashiv; Srinivasan, T.; Sharma, Lalima; Bansal, Vinay S.; Chugh, Anita; Davis, Joseph Alexanand

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9 of 47

Comment (Pharmacological Data)

Bioactivities present

Reference

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Marquis, Robert W.; Lago, Amparo M.; Callahan, James F.; Lee Trout, Robert E.; Gowen, Maxine; DelMar, Eric G.; Van Wagenen, Bradford C.; Logan, Sarah; Shimizu, Scott; Fox, John; Nemeth, Edward F.; Yang, Zheng; Roethke, Theresa; Smith, Brian R.; Ward, Keith W.; Lee, John; Keenan, Richard M.; Bhatnagar, Pradip

Journal of Medicinal Chemistry, 2009 , vol. 52, # 13 p. 3982 - 3993 Title/Abstract Full Text View citing articles Show Details

BOEHRINGER INGELHEIM PHARMA GMBH and CO. KG

Patent: WO2004/33412 A1, 2004 ; Title/Abstract Full Text Show Details

MERCK and CO., INC.

Patent: WO2003/87037 A1, 2003 ; Title/Abstract Full Text Show Details

Aventis Pharmaceuticals Inc.

Patent: EP929527 B1, 2004 ; Title/Abstract Full Text Show Details

NOVARTIS AG; NOVARTIS PHARMA GMBH

Patent: WO2005/74924 A1, 2005 ; Title/Abstract Full Text Show Details

ASTRAZENECA AB; ASTRAZENECA UK LIMITED

Patent: WO2005/95354 A1, 2005 ; Title/Abstract Full Text Show Details

ASTELLAS PHARMA INC.

Patent: WO2005/110981 A1, 2005 ; Title/Abstract Full Text Show Details

IRM LLC

Patent: WO2005/113519 A1, 2005 ; Title/Abstract Full Text Show Details

AUSPEX PHARMACEUTICAL, INC.; GANT, Thomas, G.; SHAHBAZ, Manoucherhr

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Hoenke, Christoph; Bouyssou, Thierry; Tautermann, Christofer S.; Rudolf, Klaus; Schnapp, Andreas; Konetzki, Ingo

Bioorganic and Medicinal Chemistry Letters, 2009 , vol. 19, # 23 p. 6640 - 6644 Title/Abstract Full Text View citing articles Show Details

Pasternak, Alexander; Goble, Stephen D.; deJesus, Reynalda K.; Hreniuk, Donna L.; Chung, Christine C.; Tota, Michael R.; Mazur, Paul; Feighner, Scott D.; Howard, Andrew D.; Mills, Sander G.; Yang, Lihu

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Bouyssou, Thierry; Hoenke, Christoph; Rudolf, Klaus; Lustenberger, Philipp; Pestel, Sabine; Sieger, Peter; Lotz, Ralf; Heine, Claudia; Buettner, Frank H.; Schnapp, Andreas; Konetzki, Ingo

Bioorganic and Medicinal Chemistry Letters, 2010 , vol. 20, # 4 p. 1410 - 1414 Title/Abstract Full Text View citing articles Show Details

Ishibashi, Yoshitaka; Miyata, Kengo; Kitamura, Masato

European Journal of Organic Chemistry, 2010 , # 22 p. 4201 - 4204 Title/Abstract Full Text View citing articles Show Details

Beattie, David; Bradley, Michelle; Brearley, Andrew; Charlton, Steven J.; Cuenoud, Bernard M.; Fairhurst, Robin A.; Gedeck, Peter; Gosling, Martin; Janus, Diana; Jones, Darryl; Lewis, Christine; McCarthy, Clive; Oakman, Helen; Stringer, Rowan; Taylor, Roger J.; Tuffnell, Andrew

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CENGENT THERAPEUTICS, INC.

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Andersen, Denise Lyn; Chang, Catherine H.; Falsey, James R.; Frohn, Michael J.; Hong, Fang-Tsao; Liao, Hongyu; Liu, Longbin; Lopez, Patricia; Retz, Daniel Martin; Rishton, Gilbert M.; Rzasa, Robert M.; Siegmund, Aaron; Tadesse, Seifu; Tamayo, Nuria; Tegley, Christopher M.

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PFIZER PRODUCTS INC.

Patent: WO2006/33001 A1, 2006 ; Title/Abstract Full Text Show Details

NOVARTIS AG; NOVARTIS PHARMA GMBH

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ASTRAZENECA AB

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10 of 47

Comment (Pharmacological Data)

Bioactivities present

Reference

KARO BIO AB

Patent: WO2007/39125 A2, 2007 ; Title/Abstract Full Text Show Details

NOVARTIS AG; NOVARTIS PHARMA GmbH

Patent: WO2007/67613 A1, 2007 ; Title/Abstract Full Text Show Details

NOVARTIS AG; NOVARTIS PHARMA GmbH

Patent: WO2007/67615 A2, 2007 ; Title/Abstract Full Text Show Details

Bristol-Myers Squibb Company

Patent: US2008/9534 A1, 2008 ; Title/Abstract Full Text Show Details

AstraZeneca AB

Patent: US6369064 B1, 2002 ; Title/Abstract Full Text Show Details

Lopez, Blanca; Rodriguez, Aleix; Santos, David; Albert, Joan; Ariza, Xavier; Garcia, Jordi; Granell, Jaume

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Sasmal, Pradip K.; Reddy, D. Srinivasa; Talwar, Rashmi; Venkatesham; Balasubrahmanyam; Kannan; Srinivas; Kumar, K. Shiva; Devi, B. Neelima; Jadhav, Vikram P.; Khan, Sanjoy K.; Mohan, Priya; Chaudhury, Hira; Bhuniya, Debnath; Iqbal, Javed; Chakrabarti, Ranjan

Bioorganic and Medicinal Chemistry Letters, 2011 , vol. 21, # 1 p. 562 - 568 Title/Abstract Full Text View citing articles Show Details

Vonaparti; Lyris; Angelis; Panderi; Koupparis; Tsantili-Kakoulidou; Peters; Nielen; Georgakopoulos

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Jacobsen, John R.; Choi, Seok Ki; Combs, Jesse; Fournier, Eric J.L.; Klein, Uwe; Pfeiffer, Juergen W.; Thomas, G. Roger; Yu, Cecile; Moran, Edmund J.

Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 2 p. 1213 - 1218 Title/Abstract Full Text View citing articles Show Details

Hamada, Yoshio; Tagad, Harichandra D.; Nishimura, Yoshinori; Ishiura, Shoichi; Kiso, Yoshiaki

Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 2 p. 1130 - 1135 Title/Abstract Full Text View citing articles Show Details

Miyakoshi, Hitoshi; Miyahara, Seiji; Yokogawa, Tatsushi; Chong, Khoon Tee; Taguchi, Junko; Endoh, Kanji; Yano, Wakako; Wakasa, Takeshi; Ueno, Hiroyuki; Takao, Yayoi; Nomura, Makoto; Shuto, Satoshi; Nagasawa, Hideko; Fukuoka, Masayoshi

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Oberacher, Herbert; Pitterl, Florian; Siapi, Eleni; Steele, Barry R.; Letzel, Thomas; Grosse, Sylvia; Poschner, Bernhard; Tagliaro, Franco; Gottardo, Rossella; Chacko, Silvi A.; Josephs, Jonathan L.

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Gildner, Peter G.; Gietter, Amber A. S.; Cui, Di; Watson, Donald A.

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Pathway Therapeutics Inc.

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Demory, Emilien; Farran, Daniel; Chavant, Pierre Y.; Blandin, Veronique; Baptiste, Benoit

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Sotnikova, Tatyana D; Beaulieu, Jean-Martin; Gainetdinov, Raul R; Caron, Marc G

CNS and neurological disorders drug targets, 2006 , vol. 5, # 1 p. 45 - 56 Title/Abstract Full Text Show Details

Rothman, Richard B.; Baumann, Michael H.

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Rothman, Richard B.; Blough, Bruce E.; Baumann, Michael H.

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Maeda, Akiko; Golczak, Marcin; Chen, Yu; Okano, Kiichiro; Kohno, Hideo; Shiose, Satomi; Ishikawa, Kaede; Harte, William; Palczewska, Grazyna; Maeda, Tadao; Palczewski, Krzysztof

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Albert, Joan; Ariza, Xavier; Calvet, Teresa; Font-Bardia, Merce; Garcia, Jordi; Granell, Jaume; Lamela, Andrea; Lopez, Blanca; Martinez, Manuel; Ortega, Laura; Rodriguez, Aleix; Santos, David

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11 of 47

Comment (Pharmacological Data)

Bioactivities present

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Comment (Pharmacological Data)

Bioactivities present

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Comment (Pharmacological Data)

Bioactivities present

Reference

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Comment (Pharmacological Data)

Bioactivities present

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Comment (Pharmacological Data)

Bioactivities present

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Comment (Pharmacological Data)

Bioactivities present

Reference

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Expert Review of Endocrinology and Metabolism, 2016 , vol. 11, # 5 p. 373 - 378 Title/Abstract Full Text Show Details

Amariles, Pedro; Cifuentes, Laura

Current Clinical Pharmacology, 2016 , vol. 11, # 2 p. 95 - 109 Title/Abstract Full Text Show Details

Black, Robin L.; Higbea, Ashley M.; Duval, Courtney; Chastain, Lisa M.

Expert Review of Endocrinology and Metabolism, 2016 , vol. 11, # 5 p. 415 - 423 Title/Abstract Full Text Show Details

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Current Issues in Pharmacy and Medical Sciences, 2016 , vol. 29, # 2 p. 57 - 60 Title/Abstract Full Text Show Details

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Journal of the Korean Society of Food Science and Nutrition, 2016 , vol. 45, # 8 p. 1202 - 1207 Title/Abstract Full Text Show Details

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Comment (Pharmacological Data)

Bioactivities present

Reference

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Beijing Ruidu Pharmaceutical Co., Ltd.; Guan, Wenzhen; Wang, Haiwen; Zhang, Lixian

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American Journal of Health-System Pharmacy, 2016 , vol. 73, # 19 p. 1493 - 1507 Title/Abstract Full Text Show Details

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Annals of Gastroenterology, 2016 , vol. 29, # 4 p. 424 - 438 Title/Abstract Full Text Show Details

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American Journal of Medicine, 2016 , vol. 129, # 8 p. 1 - 6,879 Title/Abstract Full Text Show Details

Vorsanger, Matthew H.; Subramanyam, Pritha; Weintraub, Howard S.; Lamm, Steven H.; Underberg, James A.; Gianos, Eugenia; Goldberg, Ira J.; Schwartzbard, Arthur Z.

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Srikanth, Sundararajan; Deedwania, Prakash

Current Hypertension Reports, 2016 , vol. 18, # 10 art. no. 76 Title/Abstract Full Text Show Details

Balaji, Meriga; Ganjayi, Muni Swamy; Hanuma Kumar, Gali E.N.; Parim, Brahma Naidu; Mopuri, Ramgopal; Dasari, Sreenivasulu

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Saunders, Katherine H.; Igel, Leon I.; Aronne, Louis J.

Expert Opinion on Pharmacotherapy, 2016 , vol. 17, # 16 p. 2235 - 2242 Title/Abstract Full Text Show Details

Kim, Jae Dong; Jung, Youn Jae; Woo, Chang Hee; Choi, Young Chan; Choi, Ji Suk; Cho, Yong Woo

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Tiscione, Nicholas B.; Miller, Russell; Shan, Xiaoqin; Sprague, Jessica; Yeatman, Dustin Tate

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Journal of Chromatography B: Analytical Technologies in the Biomedical and Life Sciences, 2016 , vol. 1038, p. 19 - 25 Title/Abstract Full Text Show Details

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19 of 47

Comment (Pharmacological Data)

Bioactivities present

Reference

Saunders, Katherine H.; Shukla, Alpana P.; Igel, Leon I.; Kumar, Rekha B.; Aronne, Louis J.

Endocrinology and Metabolism Clinics of North America, 2016 , vol. 45, # 3 p. 521 - 538 Title/Abstract Full Text Show Details

Malin, Steven K.; Kashyap, Sangeeta R.

Endocrinology and Metabolism Clinics of North America, 2016 , vol. 45, # 3 p. 553 - 564 Title/Abstract Full Text Show Details

Ben-Shlomo, Anat; Fleseriu, Maria

Endocrinology and Metabolism Clinics of North America, 2016 , vol. 45, # 3 p. xv Title/Abstract Full Text Show Details

Aagaard; Hallgreen; Hansen

International Journal of Obesity, 2016 , vol. 40, # 11 p. 1742 - 1747 Title/Abstract Full Text Show Details

Journal of Adolescent Health, 2016 , vol. 59, # 5 p. 602 - 606 Title/Abstract Full Text Show Details

Keith, Jeanette N.

Gastroenterology Clinics of North America, 2016 , vol. 45, # 4 p. 663 - 672 Title/Abstract Full Text Show Details

Bluth, Martin H.; Pincus, Matthew R.

Clinics in Laboratory Medicine, 2016 , vol. 36, # 4 p. 603 - 634 Title/Abstract Full Text Show Details

Morikawa, Yoshifumi; Shibata, Akinobu; Okumura, Naoko; Ikari, Akira; Sasajima, Yasuhide; Suenami, Koichi; Sato, Kiyohito; Takekoshi, Yuji; El-Kabbani, Ossama; Matsunaga, Toshiyuki

Toxicology and Applied Pharmacology, 2017 , vol. 314, p. 1 - 11 Title/Abstract Full Text Show Details

Zhang, Yan Victoria; Wei, Bin; Zhu, Yu; Zhang, Yanhua; Bluth, Martin H.

Clinics in Laboratory Medicine, 2016 , vol. 36, # 4 p. 635 - 661 Title/Abstract Full Text Show Details

Clark, Glenn T.; Ram, Saravanan

Oral and Maxillofacial Surgery Clinics of North America, 2016 , vol. 28, # 3 p. 397 - 407 Title/Abstract Full Text Show Details

Srinivas, Nuggehally R.

American Journal of Therapeutics, 2016 , vol. 23, # 6 p. e1826 - e1838 Title/Abstract Full Text Show Details

Casolin, Armand

Journal of Analytical Toxicology, 2016 , vol. 40, # 7 art. no. BKW055, p. 479 - 485 Title/Abstract Full Text Show Details

Peng, Po-Jui; Ho, Pei-Shen; Tsai, Chia-Kuang; Huang, San-Yuan; Liang, Chih-Sung

Clinical Neuropharmacology, 2016 , vol. 39, # 6 p. 306 - 310 Title/Abstract Full Text Show Details

Zheng, Xirong; Deng, Jing; Zhang, Ting; Yao, Jianzhuang; Zheng, Fang; Zhan, Chang-Guo

Chemico-Biological Interactions, 2016 , vol. 259, p. 99 - 103 Title/Abstract Full Text Show Details

Truter, Ilse

South African Journal of Clinical Nutrition, 2016 , vol. 29, # 4 p. 139 - 144 Title/Abstract Full Text Show Details

Onakpoya, Igho J.; Heneghan, Carl J.; Aronson, Jeffrey K.

BMC Medicine, 2016 , vol. 14, # 1 art. no. 191 Title/Abstract Full Text Show Details

Akiyama, Yoshitaka; Morita, Tomoko; Matsuda, Masafumi

Journal of the Japan Diabetes Society, 2016 , vol. 59, # 11 p. 734 - 735 Title/Abstract Full Text Show Details

Buhler, Amber V.K.; Huynh, Pearl; Low, Pauline; Von, Mary

Journal of Oral and Maxillofacial Surgery, 2016 , vol. 74, # 12 p. 2447 - 2452 Title/Abstract Full Text Show Details

Bodnar Willard, Melissa A.; McGuffin, Victoria L.; Smith, Ruth Waddell

Forensic Science International, 2017 , vol. 270, p. 111 - 120 Title/Abstract Full Text Show Details

McShea, Shannon

Physician Assistant Clinics, 2017 , vol. 2, # 1 p. 87 - 106 Title/Abstract Full Text Show Details

Comment (Pharmacological Data)

Bioactivities present

Reference

Harper, Claudia; Pattinson, Andrea L.; Fernando, Hamish A.; Zibellini, Jessica; Seimon, Radhika V.; Sainsbury, Amanda

Hormone Molecular Biology and Clinical Investigation, 2016 , vol. 28, # 3 p. 133 - 149 Title/Abstract Full Text Show Details

Burcelin; Gourdy

Obesity Reviews, 2017 , vol. 18, # 1 p. 86 - 98 Title/Abstract Full Text Show Details

Bozkurt, Biykem; Aguilar, David; Deswal, Anita; Dunbar, Sandra B.; Francis, Gary S.; Horwich, Tamara; Jessup, Mariell; Kosiborod, Mikhail; Pritchett, Allison M.; Ramasubbu, Kumudha; Rosendorff, Clive; Yancy, Clyde

Circulation, 2016 , vol. 134, # 23 p. e535 - e578 Title/Abstract Full Text Show Details

King, Rhodri J.; Ajjan, Ramzi A.

Diabetes and Vascular Disease Research, 2016 , vol. 14, # 1 p. 2 - 13

Title/Abstract Full Text Show Details

Landecho, Manuel F.; Moncada, Rafael; Valentí, Víctor; Frühbeck, Gema

Current Pharmaceutical Design, 2016 , vol. 22, # 37 p. 5687 - 5697 Title/Abstract Full Text Show Details

Kalathiya, Umesh; Padariya; Baginski

Biotechnology and Applied Biochemistry, 2016 , vol. 63, # 6 p. 765 - 778 Title/Abstract Full Text Show Details

DiNicolantonio, James J.; Chatterjee, Subhankar; O'Keefe, James H.; Meier, Pascal

Open Heart, 2014 , vol. 1, # 1 art. no. E000173 Title/Abstract Full Text Show Details

Westover, Arthur N.; Nakonezny, Paul A.; Adinoff, Bryon; Brown, Edson Sherwood; Halm, Ethan A.

Journal of Child and Adolescent Psychopharmacology, 2016 , vol. 26, # 10 p. 889 - 899 Title/Abstract Full Text Show Details

Cnubben, Nicole H.P.; Tel, Shanti L.; Hemmes, Marleen A.; Langenkamp-Brand, Astrid; Grossouw, Dimitri; Jansen, Harm T.; de Bie, Bert T.H.J.

BMC Obesity, 2016 , vol. 3, # 1 art. no. 18 Title/Abstract Full Text Show Details

Paíga, Paula; Rodrigues, Manuela J.E.; Correia, Manuela; Amaral, Joana S.; Oliveira, M. Beatriz P.P.; Delerue-Matos, Cristina European Journal of Pharmaceutical Sciences, 2017 , vol. 99, p. 219 - 227 Title/Abstract Full Text Show Details

Goldfine, Allison B.; Shoelson, Steven E.

Journal of Clinical Investigation, 2017 , vol. 127, # 1 p. 83 - 93 Title/Abstract Full Text Show Details

Ryder; Kaizer; Rudser; Gross; Kelly; Fox

International Journal of Obesity, 2017 , vol. 41, # 1 p. 90 - 93 Title/Abstract Full Text Show Details

Fu, Chuhan; Jiang, Yao; Guo, Jiao; Su, Zhengquan

Journal of Agricultural and Food Chemistry, 2016 , vol. 64, # 51 p. 9571 - 9585 Title/Abstract Full Text Show Details

Roller, Nichole B.

Journal of Pediatric Surgical Nursing, 2015 , vol. 4, # 3 p. 103 - 111 Title/Abstract Full Text Show Details

Lendoiro, Elena; Jiménez-Morigosa, Cristian; Cruz, Angelines; Páramo, Mario; López-Rivadulla, Manuel; de Castro, Ana

Drug Testing and Analysis, 2017 , vol. 9, # 1 p. 96 - 105 Title/Abstract Full Text Show Details

Merrilees, Mervyn J.; Falk, Ben A.; Zuo, Ning; Dickinson, Michelle E.; May, Barnaby C. H.; Wight, Thomas N.

Journal of Tissue Engineering and Regenerative Medicine, 2017 , vol. 11, # 1 p. 295 - 305 Title/Abstract Full Text Show Details

Kwon, Nam Ji; Han, Eunyoung

International Journal of Pharmacology, 2017 , vol. 13, # 2 p. 218 - 226 Title/Abstract Full Text Show Details

Schoonjans; Paelinck; Marchau; Gunning; Gammaitoni; Galer; Lagae; Ceulemans

European Journal of Neurology, 2017 , vol. 24, # 2 p. 309 - 314 Title/Abstract Full Text Show Details

Narayanaswami, Vidya; Dwoskin, Linda P.

Pharmacology and Therapeutics, 2017 , vol. 170, p. 116 - 147 Title/Abstract Full Text Show Details

Alshagga, Mustafa Ahmed; Alshawsh, Mohammed Abdullah; Seyedan, Atefehalsadat; Alsalahi, Abdulsamad; Pan, Yan; Mohankumar, Suresh Kumar; Alkebsi, Abdolgodose; Kassim, Saba; Mohamed, Zahurin

Annals of Nutrition and Metabolism, 2017 , vol. 69, # 3-4 p. 200 - 211 Title/Abstract Full Text Show Details

20 of 47

Comment (Pharmacological Data)

Bioactivities present

Reference

Carey, Jennifer L.; Nader, Nathalie; Chai, Peter R.; Carreiro, Stephanie; Griswold, Matthew K.; Boyle, Katherine L.

Clinical Therapeutics, 2017 , vol. 39, # 1 p. 10 - 22 Title/Abstract Full Text Show Details

Kameshwar, Vivek Hamse; Kumar; Priya, Babu S.; Swamy, S. Nanjunda

Molecular and Cellular Biochemistry, 2017 , vol. 426, # 1-2 p. 161 - 175 Title/Abstract Full Text Show Details

Bialer, Meir; Johannessen, Svein I.; Levy, René H.; Perucca, Emilio; Tomson, Torbjörn; White, H. Steve

Epilepsia, 2017 , vol. 58, # 2 p. 181 - 221 Title/Abstract Full Text Show Details

Garvey, W. Timothy; Mechanick, Jeffrey I.; Brett, Elise M.; Garber, Alan J.; Hurley, Daniel L.; Jastreboff, Ania M.; Nadolsky, Karl; Pessah-Pollack, Rachel; Plodkowski, Raymond

Endocrine Practice, 2016 , vol. 22, p. 1 - 203 Title/Abstract Full Text Show Details

Krentz; Fujioka; Hompesch

Diabetes, Obesity and Metabolism, 2016 , vol. 18, # 6 p. 558 - 570 Title/Abstract Full Text Show Details

Pratt, Wayne E.; Lin, Peagan; Pierce-Messick, Zachary; Ilesanmi, Adeolu O.; Clissold, Kara A.

Behavioural Brain Research, 2017 , vol. 323, p. 15 - 23 Title/Abstract Full Text Show Details

Mameli, Chiara; Zuccotti, Gian Vincenzo; Carnovale, Carla; Galli, Erica; Nannini, Pilar; Cervia, Davide; Perrotta, Cristiana

Pharmacological Research, 2017 , vol. 119, p. 99 - 117 Title/Abstract Full Text Show Details

Sukhdev, Singh; Bhupender, Sharma; Singh, Kanwar Shamsher

Mini-Reviews in Medicinal Chemistry, 2017 , vol. 17, # 4 p. 371 - 379 Title/Abstract Full Text Show Details

Elzanfaly, Eman S.; Amer, Enas A.; Galal, Sara A.; Zaazaa, Hala E.

Der Pharma Chemica, 2016 , vol. 8, # 22 p. 32 - 37 Title/Abstract Full Text Show Details

Kong, Tae Yeon; Kim, Ju Hyun; Kim, Jin Young; In, Moon Kyo; Choi, Kyung Ho; Kim, Hee Seung; Lee, Hye Suk

Archives of Pharmacal Research, 2017 , vol. 40, # 2 p. 180 - 196 Title/Abstract Full Text Show Details

Show next 20

21 of 47

Hide facts

Comment (Pharmacological Data)

physiological behaviour discussed

Reference

Vivus, Inc.; Najarian, Thomas; Tam, Peter Y.; Wilson, Leland F.

Patent: US2016/22630 A1, 2016 ; Title/Abstract Full Text Show Details

22 of 47

Comment (Pharmacological Data)

physiological behaviour discussed

Reference

PROXIMAGEN LIMITED; RICHARDSON, Peter; CAMPBELL, Bruce

Patent: WO2015/1359 A1, 2015 ; Title/Abstract Full Text Show Details

23 of 47

Comment (Pharmacological Data)

physiological behaviour discussed

Reference

Randox Laboratories Ltd.; Benchik, Elouard; Fitzgerald, Peter; Lowry, Philip; McConnell, Ivan

Patent: EP2950104 A1, 2015 ; Title/Abstract Full Text Show Details

24 of 47

25 of 47

26 of 47

Comment (Pharmacological Data)

physiological behaviour discussed

Reference

Röhrig, Ute F.; Majjigapu, Somi Reddy; Chambon, Marc; Bron, Sylvian; Pilotte, Luc; Colau, Didier; Van Den Eynde, Benoît J.; Turcatti, Gerardo; Vogel, Pierre; Zoete, Vincent; Michielin, Olivier

European Journal of Medicinal Chemistry, 2014 , vol. 84, p. 284 - 301 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

agonist

Species or TestSystem (Pharmacological Data)

RD-HGA16 cells expressing human TAAR 1 receptor

Method (Pharmacological Data)

hTAAR1 activation assay; title comp. incubated with test cells in presence of Calcium 3 dye as fluorescent substrate (HAM's F-12 medium, 10percent FBS, 5percent CO2/95percent air, 37 deg C, 1 h); title comp. effect on internal calcium mobilization assessed; fluorimetry

Further Details (Pharmacological Data)

hTAAR1: human trace amine receptor 1; Emax: maximal title comp. efficacy

Type (Pharmacological Data)

EC50

Value of Type (Pharmacological Data)

920 nmol/l

Results

title comp. exhibited Emax 68percent

Reference

Lewin, Anita H.; Navarro, Hernan A.; Wayne Mascarella

Bioorganic and Medicinal Chemistry, 2008 , vol. 16, # 15 p. 7415 - 7423 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

locomotor behaviors; effect on

Species or TestSystem (Pharmacological Data)

DAT-KO mouse

Sex

male and female

Method (Pharmacological

Experimental We report here that the pharmacologic inhibition of the rate-limiting enzyme of DA synthesis, TH, almost immediately depletes brain DA to undetectable levels in DAT-KO mice and induces a transient recapitulation of essentially all PD symptoms for up to 16

Data)

h. DA-deficient DAT-KO mice (DDD mice) thus represent an acute PD model that is useful for studying the efficacy of compounds that potentially can restore control of locomotion in the absence of any contribution of the dopaminergic system. By using this approach, we found that several amphetamine derivatives can counteract the behavioral manifestations of severe DA deficiency, suggesting that, in addition to well-known DA-mediated effects, amphetamine-like compounds can also affect motor functions in a DA- and DAT-independent manner. Materials and Methods Animals. DAT-KO mice were generated as previously described [11]. Animal care was in accordance with the Guide for Care and Use of Laboratory Animals (National Institutes of Health publication No.865-23, Bethesda, Md., United States) with an approved protocol from the Duke University Institutional Animal Care and Use Committee. C57BL/6J3129Sv/J hybrid WT and DAT-KO mice, 3-5 mo old, of both sexes were used. None of animals used in these studies had the neurodegenerative phenotype sporadically observed in DAT-KO mice [60]. Drugs. Drugs or saline (0.9percent NaCl) were administered intraperitoneally (IP) or subcutaneously (SC) in a volume of 10 ml/kg. The drags were either from Sigma (St. Louis, Mo., United States) or supplied by the National Institute of Drug Abuse (NIDA).

Drugs provided by the NIDA Drug Supply Program included: (+/-)-MDMA, (+)-MDMA, (+/-)-6-OH-MDA, (+/-)-MDA, (+/-)-MDE, (+)-MDE, ()-MDE, and AFT (alpha-ethyl-tryptamine acetate). Neurochemical assessments. Striatal tissue contents of DA and frontal cortical tissue levels of NE were assessed using HPLC-EC (high performance liquid chromatography with electrochemical detection) as described [8]. In vivo microdialysis measurements of striatal extracellular DA levels in freely moving mice were performed at least 24 h after implantation of a microdialysis probe as described previously [50]. Dialysate samples were assayed for DA using HPLC-EC. Behavioral methods. Locomotor activity of littermate WT and DATKO mice was measured in an Omnitech CCDigiscan (Accuscan Instruments, Columbus, Ohio United States) activity monitor under bright illumination [83]. All behavioral experiments were performed between 10:00 AM and 5:00 PM. Activity was measured at 5-min intervals, To evaluate the effects of drugs on motor behaviors, mice were placed into activity monitor chambers (20.x.20 cm) for 30 min and then treated with αMT (250 mg/kg IP). A drug or combination of drugs were injected 1 h after αMT administration, and various parameters of locomotor activity were monitored for up to 3 h. In cumulative dosing experiments, animals were treated with increasing doses of drugs after a 1-h interval. For the akinesia test, the mouse is held by the tail so that it is standing on forelimbs only and moving on its own. The number of steps taken with both forelimbs was recorded during a 30-s trial [57]. The presence of catalepsy was determined and measured by placing the animal's forepaws on a horizontal wooden bar (0.7 cm in diameter), 4 cm above the tabletop. The time until the mouse removed both forepaws from the bar was recorded, with a maximum cut-off time of 3 min [53]. In the grasping test of muscular rigidity, the mouse is suspended by its forelimbs on a metal rod (diameter: 0.25 cm) positioned approximately 20 cm above the table. The time the animal remains on the rod (maximum 1 min) was noted [58]. To assess rigidity in a bracing task, the number of steps taken with each forelimb when the mouse is pushed sideways over a distance of 50 cm was recorded [57]. Tremor was scored visually in mice using the rating scale [54]: 0, no tremor; 1, occasional isolated twi

Results

Akinesia test: ~10-40 number of steps; at Catalepsy test: ~30-180sec; at Grasping test: ~10-30 seconds time spent on the rod of the title compound administered after 1h of αMT treatment; figure is given

Location

Page/Page column 3; 12-15; sheet 9

Reference

Caron, Marc G.; Sotnikova, Tatyana D.; Gainetdinov, Raul R.

Patent: US2007/27208 A1, 2007 ; Title/Abstract Full Text Show Details

27 of 47

Effect (Pharmacological Data)

body weight; effect on

Species or TestSystem (Pharmacological Data)

DIO (Levin) rat

Sex

male

Route of Application

peroral

Method (Pharmacological Data)

EXAMPLE 4[00268] To demonstrate effects of the combination of amylin and a serotonergic/noradrenergic reuptake inhibitor on changes in body weight and body composition, DIO male rats were fattened and divided into four treatment groups, as described in Example 2. Rat amylin was dissolved in 50percent DMSO in sterile water and sibutramine was dissolved in sterile water. Each group was implanted with subcutaneous osmotic mini-pumps designed to deliver vehicle, sibutramine (3 mg/kg/day) or amylin (100 μg/kg/day) for a 14 day period.

Body weight and food intake were recorded daily. Body composition was measured prior to and after drag treatment using NMR (Echo Medical Systems, Houston, TX). For body composition measurements, rats were briefly placed (~1 min) in a well-ventilated plexiglass tube that was then inserted into a specialized rodent NMR machine. Rats were scanned prior to pump implantation and on the final day of the experiment. This enabled the calculation of changes in actual grams of fat and dry lean tissue (e.g., grams of body fat after treatment grams of body fat at baseline = change in grams of body fat) and changes in percent body composition for fat and dry lean tissue (e.g., percent body fat after treatment -percent body fat at baseline = change in percent body fat).[00269] The graph in Figure 1OA depicts vehicle-corrected changes in percent body weight of the treatment groups over the two weeks of treatment. Sibutramine administration alone and amylin administration alone resulted in about a 6percent decease in body weight. The percent decrease in body weight in response to administration of a combination of amylin and sibutramine was about 12percent. Figures 1OB and 1OC depict changes in body fat and changes in body protein, respectively, produced after the two weeks of treatment. Fat mass loss was evident with the treatment of either amylin alone or sibutramine alone, and a synergistic effect was obtained when both amylin and sibutramine were administered in combination (Fig. 10B). Administration of amylin alone resulted in an increase in lean (protein) mass. Lean (protein) mass was relatively unchanged when sibutramine was administered alone or in combination with amylin (Fig. 10C). These results support a metabolic effect of the combination of agents as well as a weight reducing effect.[00270] The combination of amylin and catecholaminergic agonist, phentermine, were also tested for effects on changes in body weight and body composition. Phentermine is classically referred to as a catecholaminergic agonist as it actually hits NA/5-HT receptors. DIO male rats were fattened and divided into four treatment groups, as described above. Each group was implanted with subcutaneous osmotic mini-pumps and/or inserted with an oral gavage, designed to deliver vehicle, phentermine (10 mg/kg/day), amylin (100 μg/kg/day) or phentermine (10 mg/kg/day) + amylin (100 μg/kg/day) for a 14 day period. The mini-pump contained either vehicle (50percent DMSO in water) or amylin while the oral gavage administered either sterile water or phentermine. Body weight was recorded daily and body composition was measured prior to and after drag treatment using NMR. [00271] The graph in Figure 1 IA depicts vehicle-corrected changes in percent body weight of the treatment groups over the two weeks of treatment. Phentermine administration alone resulted in about a 5 percent decrease in body weight and amylin administration alone resulted in about a 7 percent decease in body weight. The percent decrease in body weight in response to administration of a combination of amylin and phentermine was about 12percent. Figures 1 IB and 11C depict changes in body fat and changes in body protein, respectively, produced after the two weeks of treatment. A modest amount of fat mass loss was evident with the treatment of phentermine alone and a greater amount of fat mass loss was evident with the treatment of amylin alone. When amylin and phentermine were administered in combination, a synergi

Results

title compound at 10 mg/kg/day produced ~5percent decrease in body weight at ~0-2w treatment; administration with amylin produced ~12percent decrease in body weight; figure is given

Location

Page/Page column 7; 76-78; 7/15

Reference

AMYLIN PHARMACEUTICALS, INC.

Patent: WO2007/55728 A1, 2007 ; Title/Abstract Full Text Show Details

28 of 47

Effect (Pharmacological Data)

fat mass; effect on

Species or TestSystem (Pharmacological Data)

DIO (Levin) rat

Sex

male

Route of Application

peroral

Method (Pharmacological Data)

EXAMPLE 4[00268] To demonstrate effects of the combination of amylin and a serotonergic/noradrenergic reuptake inhibitor on changes in body weight and body composition, DIO male rats were fattened and divided into four treatment groups, as described in Example 2. Rat amylin was dissolved in 50percent DMSO in sterile water and sibutramine was dissolved in sterile water. Each group was implanted with subcutaneous osmotic mini-pumps designed to deliver vehicle, sibutramine (3 mg/kg/day) or amylin (100 μg/kg/day) for a 14 day period.

Body weight and food intake were recorded daily. Body composition was measured prior to and after drag treatment using NMR (Echo Medical Systems, Houston, TX). For body composition measurements, rats were briefly placed (~1 min) in a well-ventilated plexiglass tube that was then inserted into a specialized rodent NMR machine. Rats were scanned prior to pump implantation and on the final day of the experiment. This enabled the calculation of changes in actual grams of fat and dry lean tissue (e.g., grams of body fat after treatment grams of body fat at baseline = change in grams of body fat) and changes in percent body composition for fat and dry lean tissue (e.g., percent body fat after treatment -percent body fat at baseline = change in percent body fat).[00269] The graph in Figure 1OA depicts vehicle-corrected changes in percent body weight of the treatment groups over the two weeks of treatment. Sibutramine administration alone and amylin administration alone resulted in about a 6percent decease in body weight. The percent decrease in body weight in response to administration of a combination of amylin and sibutramine was about 12percent. Figures 1OB and 1OC depict changes in body fat and changes in body protein, respectively, produced after the two weeks of treatment. Fat mass loss was evident with the treatment of either amylin alone or sibutramine alone, and a synergistic effect was obtained when both amylin and sibutramine were administered in combination (Fig. 10B). Administration of amylin alone resulted in an increase in lean (protein) mass. Lean (protein) mass was relatively unchanged when sibutramine was administered alone or in combination with amylin (Fig. 10C). These results support a metabolic effect of the combination of agents as well as a weight reducing effect.[00270] The combination of amylin and catecholaminergic agonist, phentermine, were also tested for effects on changes in body weight and body composition. Phentermine is classically referred to as a catecholaminergic agonist as it actually hits NA/5-HT receptors. DIO male rats were fattened and divided into four treatment groups, as described above. Each group was implanted with subcutaneous osmotic mini-pumps and/or inserted with an oral gavage, designed to deliver vehicle, phentermine (10 mg/kg/day), amylin (100 μg/kg/day) or phentermine (10 mg/kg/day) + amylin (100 μg/kg/day) for a 14 day period. The mini-pump contained either vehicle (50percent DMSO in water) or amylin while the oral gavage administered either sterile water or phentermine. Body weight was recorded daily and body composition was measured prior to and after drag treatment using NMR. [00271] The graph in Figure 1 IA depicts vehicle-corrected changes in percent body weight of the treatment groups over the two weeks of treatment. Phentermine administration alone resulted in about a 5 percent decrease in body weight and amylin administration alone resulted in about a 7 percent decease in body weight. The percent decrease in body weight in response to administration of a combination of amylin and phentermine was about 12percent. Figures 1 IB and 11C depict changes in body fat and changes in body protein, respectively, produced after the two weeks of treatment. A modest amount of fat mass loss was evident with the treatment of phentermine alone and a greater amount of fat mass loss was evident with the treatment of amylin alone. When amylin and phentermine were administered in combination, a synergi

Results

title compound at 10 mg/kg/day produced the fat mass loss to be ~-5 grams at ~0-2w treatment; synergistic effect at ~-40 grams was observed when the compound was administered with amylin; figure is given

Location

Page/Page column 7; 76-78; 7/15

Reference

AMYLIN PHARMACEUTICALS, INC.

Patent: WO2007/55728 A1, 2007 ; Title/Abstract Full Text Show Details

29 of 47

Effect (Pharmacological Data)

lean (protein) mass; effect on

Species or TestSystem (Pharmacological Data)

DIO (Levin) rat

Sex

male

Route of Application

peroral

Method (Pharmacological Data)

EXAMPLE 4[00268] To demonstrate effects of the combination of amylin and a serotonergic/noradrenergic reuptake inhibitor on changes in body weight and body composition, DIO male rats were fattened and divided into four treatment groups, as described in Example 2. Rat amylin was dissolved in 50percent DMSO in sterile water and sibutramine was dissolved in sterile water. Each group was implanted with subcutaneous osmotic mini-pumps designed to deliver vehicle, sibutramine (3 mg/kg/day) or amylin (100 μg/kg/day) for a 14 day period.

Body weight and food intake were recorded daily. Body composition was measured prior to and after drag treatment using NMR (Echo Medical Systems, Houston, TX). For body composition measurements, rats were briefly placed (~1 min) in a well-ventilated plexiglass tube that was then inserted into a specialized rodent NMR machine. Rats were scanned prior to pump implantation and on the final day of the experiment. This enabled the calculation of changes in actual grams of fat and dry lean tissue (e.g., grams of body fat after treatment grams of body fat at baseline = change in grams of body fat) and changes in percent body composition for fat and dry lean tissue (e.g., percent body fat after treatment -percent body fat at baseline = change in percent body fat).[00269] The graph in Figure 1OA depicts

vehicle-corrected changes in percent body weight of the treatment groups over the two weeks of treatment. Sibutramine administration alone and amylin administration alone resulted in about a 6percent decease in body weight. The percent decrease in body weight in response to administration of a combination of amylin and sibutramine was about 12percent. Figures 1OB and 1OC depict changes in body fat and changes in body protein, respectively, produced after the two weeks of treatment. Fat mass loss was evident with the treatment of either amylin alone or sibutramine alone, and a synergistic effect was obtained when both amylin and sibutramine were administered in combination (Fig. 10B). Administration of amylin alone resulted in an increase in lean (protein) mass. Lean (protein) mass was relatively unchanged when sibutramine was administered alone or in combination with amylin (Fig. 10C). These results support a metabolic effect of the combination of agents as well as a weight reducing effect.[00270] The combination of amylin and catecholaminergic agonist, phentermine, were also tested for effects on changes in body weight and body composition. Phentermine is classically referred to as a catecholaminergic agonist as it actually hits NA/5-HT receptors. DIO male rats were fattened and divided into four treatment groups, as described above. Each group was implanted with subcutaneous osmotic mini-pumps and/or inserted with an oral gavage, designed to deliver vehicle, phentermine (10 mg/kg/day), amylin (100 μg/kg/day) or phentermine (10 mg/kg/day) + amylin (100 μg/kg/day) for a 14 day period. The mini-pump contained either vehicle (50percent DMSO in water) or amylin while the oral gavage administered either sterile water or phentermine. Body weight was recorded daily and body composition was measured prior to and after drag treatment using NMR. [00271] The graph in Figure 1 IA depicts vehicle-corrected changes in percent body weight of the treatment groups over the two weeks of treatment. Phentermine administration alone resulted in about a 5 percent decrease in body weight and amylin administration alone resulted in about a 7 percent decease in body weight. The percent decrease in body weight in response to administration of a combination of amylin and phentermine was about 12percent. Figures 1 IB and 11C depict changes in body fat and changes in body protein, respectively, produced after the two weeks of treatment. A modest amount of fat mass loss was evident with the treatment of phentermine alone and a greater amount of fat mass loss was evident with the treatment of amylin alone. When amylin and phentermine were administered in combination, a synergi Results

title compound at 10mg/kg/day did not change the lean (protein) mass at ~0-2w treatment; title compound administered with amylin tended to have the greatest increase in the lean (protein) mass at ~6 grams; figure is given

Location

Page/Page column 7; 76-78; 7/15

Reference

AMYLIN PHARMACEUTICALS, INC.

Patent: WO2007/55728 A1, 2007 ; Title/Abstract Full Text Show Details

30 of 47

Effect (Pharmacological Data)

body fat; effect on

Species or TestSystem (Pharmacological Data)

Diet-induced obesity (DIO) rat

Sex

male

Method (Pharmacological Data)

EXAMPLE 4[00270] To demonstrate effects of the combination of amylin and a serotonergic/noradrenergic reuptake inhibitor on changes in body weight and body composition, DIO male rats were fattened and divided into four treatment groups, as described in Example 2. Rat amylin was dissolved in 50percent DMSO in sterile water and sibutramine was dissolved in sterile water. Each group was implanted with subcutaneous osmotic mini-pumps designed to deliver vehicle, sibutramine (3 mg/kg/day) or amylin (100 μg/kg/day) for a 14 day period.

Body weight and food intake were recorded daily. Body composition was measured prior to and after drag treatment using NMR (Echo Medical Systems, Houston, TX). For body composition measurements, rats were briefly placed (~1 min) in a well-ventilated plexiglass tube that was then inserted into a specialized rodent NMR machine. Rats were scanned prior to pump implantation and on the final day of the experiment. This enabled the calculation of changes in actual grams of fat and dry lean tissue (e.g., grams of body fat after treatment grams of body fat at baseline = change in grams of body fat) and changes in percent body composition for fat and dry lean tissue (e.g., percent body fat after treatment -percent body fat at baseline = change in percent body fat).[00271] The graph in Figure 1OA depicts vehicle-corrected changes in percent body weight of the treatment groups over the two weeks of treatment. Sibutramine administration alone and amylin administration alone resulted in about a 6percent decease in body weight. The percent decrease in body weight in response to administration of a combination of amylin and sibutramine was about 12percent. Figures 1OB and 1OC depict changes in body fat and changes in body protein, respectively, produced after the two weeks of treatment. Fat mass loss was evident with the treatment of either amylin alone or sibutramine alone, and a synergistic effect was obtained when both amylin and sibutramine were administered in combination (Fig. 10B). Administration of amylin alone resulted in an increase in lean (protein) mass. Lean (protein) mass was relatively unchanged when sibutramine was administered alone or in combination with amylin (Fig. 10C). These results support a metabolic effect of the combination of agents as well as a weight reducing effect.[00272] The combination of amylin and catecholaminergic agonist, phentermine, were also tested for effects on changes in body weight and body composition. Phentermine is classically referred to as a catecholaminergic agonist as it actually hits NA/5-HT receptors. DIO male rats were fattened and divided into four treatment groups, as described above. Each group was implanted with subcutaneous osmotic mini-pumps and/or inserted with an oral gavage, designed to deliver vehicle, phentermine (10 mg/kg/day), amylin (100 μg/kg/day) or phentermine (10 mg/kg/day) + amylin (100 μg/kg/day) for a 14 day period. The mini-pump contained either vehicle (50percent DMSO in water) or amylin while the oral gavage administered either sterile water or phentermine. Body weight was recorded daily and body composition was measured prior to and after drug treatment using NMR. [00273] The graph in Figure 1 IA depicts vehicle-corrected changes in percent body weight of the treatment groups over the two weeks of treatment. Phentermine administration alone resulted in about a 5 percent decrease in body weight and amylin administration alone resulted in about a 7 percent decease in body weight. The percent decrease in body weight in response to administration of a combination of amylin and phentermine was about 12percent. Figures 11 B and 11 C depict changes in body fat and changes in body protein, respectively, produced after the two weeks of treatment. A modest amount of fat mass loss was evident with the treatment of phentermine alone and a greater amount of fat mass loss was evident with the treatment of amylin alone. When amylin and phentermine were administered in combination, a synergistic effe

Results

modest amount of fat loss was evident with title compound treatment; figure is given

Location

Page/Page column 9; 79-80; 7/15

Reference

AMYLIN PHARMACEUTICALS, INC.

Patent: WO2007/55743 A2, 2007 ; Title/Abstract Full Text Show Details

31 of 47

Effect (Pharmacological Data)

body protein; effect on

Species or TestSystem (Pharmacological Data)

Diet-induced obesity (DIO) rat

Sex

male

Method (Pharmacological Data)

EXAMPLE 4[00270] To demonstrate effects of the combination of amylin and a serotonergic/noradrenergic reuptake inhibitor on changes in body weight and body composition, DIO male rats were fattened and divided into four treatment groups, as described in Example 2. Rat amylin was dissolved in 50percent DMSO in sterile water and sibutramine was dissolved in sterile water. Each group was implanted with subcutaneous osmotic mini-pumps designed to deliver vehicle, sibutramine (3 mg/kg/day) or amylin (100 μg/kg/day) for a 14 day period.

Body weight and food intake were recorded daily. Body composition was measured prior to and after drag treatment using NMR (Echo Medical Systems, Houston, TX). For body composition measurements, rats were briefly placed (~1 min) in a well-ventilated plexiglass tube that was then inserted into a specialized rodent NMR machine. Rats were scanned prior to pump implantation and on the final day of the experiment. This enabled the calculation of changes in actual grams of fat and dry lean tissue (e.g., grams of body fat after treatment grams of body fat at baseline = change in grams of body fat) and changes in percent body composition for fat and dry lean tissue (e.g., percent body fat after treatment -percent body fat at baseline = change in percent body fat).[00271] The graph in Figure 1OA depicts vehicle-corrected changes in percent body weight of the treatment groups over the two weeks of treatment. Sibutramine administration alone and amylin administration alone resulted in about a 6percent decease in body weight. The percent decrease in body weight in response to administration of a combination of amylin and sibutramine was about 12percent. Figures 1OB and 1OC depict changes in body fat and changes in body protein, respectively, produced after the two weeks of treatment. Fat mass loss was evident with the treatment of either amylin alone or sibutramine alone, and a synergistic effect was obtained when both amylin and sibutramine were administered in combination (Fig. 10B). Administration of amylin alone resulted in an increase in lean (protein) mass. Lean (protein) mass was relatively unchanged when sibutramine was administered alone or in combination with amylin (Fig. 10C). These results support a metabolic effect of the combination of agents as well as a weight reducing effect.[00272] The combination of amylin and catecholaminergic agonist, phentermine, were also tested for effects on changes in body weight and body composition. Phentermine is classically referred to as a catecholaminergic agonist as it actually hits NA/5-HT receptors. DIO male rats were fattened and divided into four treatment groups, as described above. Each group was implanted with subcutaneous osmotic mini-pumps and/or inserted with an oral gavage, designed to deliver vehicle, phentermine (10 mg/kg/day), amylin (100 μg/kg/day) or phentermine (10 mg/kg/day) + amylin (100 μg/kg/day) for a 14 day period. The mini-pump contained either vehicle (50percent DMSO in water) or amylin while the oral gavage administered either sterile water or phentermine. Body weight was recorded daily and body composition was measured prior to and after drug treatment using NMR. [00273] The graph in Figure 1 IA depicts vehicle-corrected changes in percent body weight of the treatment groups over the two weeks of treatment. Phentermine administration alone resulted in about a 5 percent decrease in body weight and amylin administration alone resulted in about a 7 percent decease in body weight. The percent decrease in body weight in response to administration of a combination of amylin and phentermine was about 12percent. Figures 11 B and 11 C depict changes in body fat and changes in body protein, respectively, produced after the two weeks of treatment. A modest amount of fat mass loss was evident with the treatment of phentermine alone and a greater amount of fat mass loss was evident with the treatment of amylin alone. When amylin and phentermine were administered in combination, a synergistic effe

Location

Page/Page column 9; 79-80; 7/15

Comment (Pharmacological Data)

No effect

Reference

AMYLIN PHARMACEUTICALS, INC.

Patent: WO2007/55743 A2, 2007 ; Title/Abstract Full Text Show Details

32 of 47

Effect (Pharmacological Data)

body weight; effect on

Species or TestSystem (Pharmacological Data)

Diet-induced obesity (DIO) rat

Sex

male

Method (Pharmacological Data)

EXAMPLE 4[00270] To demonstrate effects of the combination of amylin and a serotonergic/noradrenergic reuptake inhibitor on changes in body weight and body composition, DIO male rats were fattened and divided into four treatment groups, as described in Example 2. Rat amylin was dissolved in 50percent DMSO in sterile water and sibutramine was dissolved in sterile water. Each group was implanted with subcutaneous osmotic mini-pumps designed to deliver vehicle, sibutramine (3 mg/kg/day) or amylin (100 μg/kg/day) for a 14 day period.

Body weight and food intake were recorded daily. Body composition was measured prior to and after drag treatment using NMR (Echo Medical Systems, Houston, TX). For body composition measurements, rats were briefly placed (~1 min) in a well-ventilated plexiglass tube that was then inserted into a specialized rodent NMR machine. Rats were scanned prior to pump implantation and on the final day of the experiment. This enabled the calculation of changes in actual grams of fat and dry lean tissue (e.g., grams of body fat after treatment grams of body fat at baseline = change in grams of body fat) and changes in percent body composition for fat and dry lean tissue (e.g., percent body fat after treatment -percent body fat at baseline = change in percent body fat).[00271] The graph in Figure 1OA depicts vehicle-corrected changes in percent body weight of the treatment groups over the two weeks of treatment. Sibutramine administration alone and amylin administration alone resulted in about a 6percent decease in body weight. The percent decrease in body weight in response to administration of a combination of amylin and sibutramine was about 12percent. Figures 1OB and 1OC depict changes in body fat and changes in body protein, respectively, produced after the two weeks of treatment. Fat mass loss was evident with the treatment of either amylin alone or sibutramine alone, and a synergistic effect was obtained when both amylin and sibutramine were administered in combination (Fig. 10B). Administration of amylin alone resulted in an increase in lean (protein) mass. Lean (protein) mass was relatively unchanged when sibutramine was administered alone or in combination with amylin (Fig. 10C). These results support a metabolic effect of the combination of agents as well as a weight reducing effect.[00272] The combination of amylin and catecholaminergic agonist, phentermine, were also tested for effects on changes in body weight and body composition. Phentermine is classically referred to as a catecholaminergic agonist as it actually hits NA/5-HT receptors. DIO male rats were fattened and divided into four treatment groups, as described above. Each group was implanted with subcutaneous osmotic mini-pumps and/or inserted with an oral gavage, designed to deliver vehicle, phentermine (10 mg/kg/day), amylin (100 μg/kg/day) or phentermine (10 mg/kg/day) + amylin (100 μg/kg/day) for a 14 day period. The mini-pump contained either vehicle (50percent DMSO in water) or amylin while the oral gavage administered either sterile water or phentermine. Body weight was recorded daily and body composition was measured prior to and after drug treatment using NMR. [00273] The graph in Figure 1 IA depicts vehicle-corrected changes in percent body weight of the treatment groups over the two weeks of treatment. Phentermine administration alone resulted in about a 5 percent decrease in body weight and amylin administration alone resulted

in about a 7 percent decease in body weight. The percent decrease in body weight in response to administration of a combination of amylin and phentermine was about 12percent. Figures 11 B and 11 C depict changes in body fat and changes in body protein, respectively, produced after the two weeks of treatment. A modest amount of fat mass loss was evident with the treatment of phentermine alone and a greater amount of fat mass loss was evident with the treatment of amylin alone. When amylin and phentermine were administered in combination, a synergistic effe Results

title compound resulted in about a 5percent decrease in body weight; figure is given

Location

Page/Page column 9; 79-80; 7/15

Reference

AMYLIN PHARMACEUTICALS, INC.

Patent: WO2007/55743 A2, 2007 ; Title/Abstract Full Text Show Details

33 of 47

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Effect (Pharmacological Data)

monoamine transporter; interaction with

Species or TestSystem (Pharmacological Data)

rat caudate putamen crude vesicular fraction

Method (Pharmacological Data)

vesicular fraction incubated with title comp. and 2 nmol/l <3H>DHTBZ for 4 h at 25 deg C; rapid filtration; liquid scintillation counting

Further Details (Pharmacological Data)

DHTBZ: dihydrotetrabenazine; VMAT2: vesicular monoamine transporter type 2; IC50 for title comp. inhibition of <3H>DHTBZ binding

Type (Pharmacological Data)

IC50

Value of Type (Pharmacological Data)

> 100 μmol/l

Reference

Partilla, John S.; Dempsey, Allison G.; Nagpal, Ameet S.; Blough, Bruce E.; Baumann, Michael H.; Rothman, Richard B.

Journal of Pharmacology and Experimental Therapeutics, 2006 , vol. 319, # 1 p. 237 - 246 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

monoamine transporter; interaction with

Species or TestSystem (Pharmacological Data)

rat caudate putamen crude vesicular fraction

Method (Pharmacological Data)

vesicular fraction incubated with title comp. and 60 nmol/l <3H>dopamine for 5 min at 25 deg C; rapid filtration; liquid scintillation counting

Further Details (Pharmacological Data)

DHTBZ: dihydrotetrabenazine; VMAT2: vesicular monoamine transporter type 2; IC50 for title comp. inhibition of <3H>dopamine uptake

Type (Pharmacological Data)

IC50

Value of Type (Pharmacological Data)

> 100 μmol/l

Reference

Partilla, John S.; Dempsey, Allison G.; Nagpal, Ameet S.; Blough, Bruce E.; Baumann, Michael H.; Rothman, Richard B.

Journal of Pharmacology and Experimental Therapeutics, 2006 , vol. 319, # 1 p. 237 - 246 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

transmitter releasing

Species or TestSystem (Pharmacological Data)

rat caudate putamen crude vesicular fraction

Method (Pharmacological Data)

vesicular fraction preloaded with 60 nmol/l <3H>tyramine for 20 min at 25 deg C, incubated with title comp. for 2 min at 25 deg C; rapid filtration; liquid scintillation counting; <3H>tyramine release evaluated

Further Details

EC50 for title comp. inhibition of <3H>tyramine release

(Pharmacological Data)

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Type (Pharmacological Data)

EC50

Value of Type (Pharmacological Data)

> 100 μmol/l

Reference

Partilla, John S.; Dempsey, Allison G.; Nagpal, Ameet S.; Blough, Bruce E.; Baumann, Michael H.; Rothman, Richard B.

Journal of Pharmacology and Experimental Therapeutics, 2006 , vol. 319, # 1 p. 237 - 246 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

transmitter releasing

Species or TestSystem (Pharmacological Data)

rat caudate putamen crude vesicular fraction

Method (Pharmacological Data)

vesicular fraction preloaded with 60 nmol/l <3H>dopamine for 20 min at 25 deg C, incubated with title comp. for 10 min at 25 deg C; rapid filtration; liquid scintillation counting; <3H>dopamine release evaluated

Further Details (Pharmacological Data)

EC50 for title comp. inhibition of <3H>dopamine release

Type (Pharmacological Data)

EC50

Value of Type (Pharmacological Data)

> 100 μmol/l

Reference

Partilla, John S.; Dempsey, Allison G.; Nagpal, Ameet S.; Blough, Bruce E.; Baumann, Michael H.; Rothman, Richard B.

Journal of Pharmacology and Experimental Therapeutics, 2006 , vol. 319, # 1 p. 237 - 246 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

Body weight and food intake; effect on

Species or TestSystem (Pharmacological Data)

Diet-Induced Obesity; AKR/J mouse

Route of Application

intraperitoneal

Method (Pharmacological Data)

A study was conducted to determine the effect of the combination of phentermine and Axokine.(TM). on body weight and food intake in a mouse model of obesity. 30 DIO (Diet-Induced Obesity; AKR/J mice fed a high fat diet) mice were divided into 5 equal groups (n=6 per group). Four groups were treated daily in the afternoon starting on Day 0 as follows: Group A (control): 0.9percent NaCl (4 μl/g, intraperitoneal (IP) injection) and placebo (4 μl/g subcutaneous (SC) injection); Group B: Axokine.(TM). (0.03 mg/kg, SC); Group C: phentermine (10.0 mg/kg, IP); Group D: Axokine.(TM). (0.03 mg/kg, SC)+phentermine (10.0 mg/kg, IP). The sixth group, Group E was pair fed to Group B; each animal in this group received the average amount of food the Axokine.(TM). treated animals consumed the previous day. This treatment paradigm continued until Day 21 (last injection on Day 20). As illustrated in FIG. 1, daily administration of Axokine.(TM). or phentermine resulted in a significant decrease in body weight relative to control animals. After 21 days of treatment, animals receiving Axokine.(TM). lost approximately 19percent of their starting body weight; phentermine-treated mice lost about 15percent, while control animals had a decrease of 2percent. DIO mice receiving daily administration of Axokine.(TM).+phentermine lost approximately 26percent of their starting body weight, an amount that was significantly greater than either Axokine.(TM). alone or phentermine alone. Animals who were pair-fed to the Axokine.(TM). group, lost weight at a rate similar to that of the Axokine.(TM). group up to Day 11 of the study. After this time, their weight loss reached a plateau. Despite receiving less food than controls and the same amount as the Axokine.(TM). group, they did not lose any additional weight. In terms of 24 h food intake (FIG. 2), all treatment groups had a decrease in food intake over the first 2 days of the study (Day 0 to Day 2) relative to their pre-study intake (Day -1). After the second day of the study, control animals resumed their typical eating pattern, consuming approximately 4 g of food a day. Animals who received Axokine.(TM). or were pair-fed, maintained this decreased food intake of about 2.75 g per day until Day 12 when they began to consume more food (3.5 g at the end of the study). Phentermine treated mice also had decreased food intake relative to control but the overall pattern was more variable. As expected, the combination of Axokine.(TM). and phentermine also resulted in a decreased food consumption that was noticeably different than either compound alone, starting around Day 9 of the study. Taken together, the results of the study demonstrate that the combination of Axokine.

(TM). and phentermine can cause a greater degree of weight loss than either agent by itself and this is due in part to a reduction in food intake.

Results

After 21 days of treatment, animals receiving test compound lost approximately 15percent of their starting body weight, while control animals had a decrease of 2percent. Test compound treated mice also had decreased food intake relative to control but the overall pattern was more variable; figures are given.

Location

Page/Page column 3-4

Reference

Yancopoulos, George D.; Wiegand, Stanley J.; Sleeman, Mark W.; Koehler-Stec, Ellen-Marie

Patent: US2006/58224 A1, 2006 ;

Title/Abstract Full Text Show Details

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Effect (Pharmacological Data)

anti-obesity

Species or TestSystem (Pharmacological Data)

Wistar rat

Sex

male

Route of Application

peroral

Concentration (Pharmacological Data)

5 mg/kg

Kind of Dosing (Pharmacological Data)

title comp. administered by gavage for 10 days

Method (Pharmacological Data)

title comp. administered; body weight and food intake recorded; rats were killed; body composition (energy, lipid) determined using bomb calorimeter; serum TG, TC, insulin, glucose, AST, ALT, 3-hydroxybutyrate levels, HOMA score measured

Further Details (Pharmacological Data)

overweight rats were used; TG: total triacylglycerol; TC: total cholesterol; AST and ALT: aspartate and alanine transaminase; HOMA: homeostasis model assessment; untreated control

Results

title comp. did not significantly affect body weight and energy, food intake; title comp. did not reduce glucose, 3-hydroxybutyrate, AST but induced increase in ALT levels (diagram, table)

Reference

Ferrer-Lorente, Raquel; Cabot, Cristina; Fernandez-Lopez, Jose-Antonio; Remesar, Xavier; Alemany, Maria

European Journal of Pharmacology, 2005 , vol. 513, # 3 p. 243 - 248 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

transmitter releasing

Species or TestSystem (Pharmacological Data)

Sprague-Dawley rat

Sex

male

Route of Application

intraperitoneal

Concentration (Pharmacological Data)

1 - 10 mg/kg

Method (Pharmacological Data)

title comp. administered; microdialysis of hypothalamus performed; dialysate samples collected every 30 min and analyzed for 5-HT by high-performance liquid chromatography

Further Details (Pharmacological Data)

title comp. administered with 5-HT1A receptor agonist, 8-OH-DPAT (0.1 mg/kg, s.c.), fluoxetine (10 mg/kg), or D-fenfluramine (1 mg/kg); title comp. administered locally into hypothalamus followed by systemic title comp. injection; 5-HT: serotonin

Results

title comp. produced dose-dependent increases in extracellular 5-HT in hypothalamus; fluoxetine attenuated increase in 5-HT induced by title comp.; effect of title comp. increased in presence of D-fenfluramine

Reference

Tao, Rui; Fray, Anne; Aspley, Sue; Brammer, Richard; Heal, David; Auerbach, Sidney

European Journal of Pharmacology, 2002 , vol. 445, # 1-2 p. 69 - 81 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

potassium channel; inhibition of

Species or TestSystem (Pharmacological Data)

Chinese hamster ovary cells

Concentration (Pharmacological Data)

Ca. 30 - 300 μmol/l

Method (Pharmacological Data)

potassium outward current measured at 23-25 deg C, in whole cell configuration of patch-clamp technique; voltage-clamp protocols applied; amplitude of current assessed at end of 250-ms command pulse voltages applied every 15 s from -70 to +50 mV

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Further Details (Pharmacological Data)

cells expressing human Kv1.5 voltage-gated potassium channel; further studies on voltage-dependence

Results

title comp. dose-dependently inhibited potassium current, at 300 μmol/l 21 percent of current blocked

Reference

Perchenet, Loic; Hilfiger, Laurence; Mizrahi, Jacques; Clement-Chomienne, Odile

Journal of Pharmacology and Experimental Therapeutics, 2001 , vol. 298, # 3 p. 1108 - 1119 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

agonist

Species or TestSystem (Pharmacological Data)

HEK293 cells expressing rTAR1

Concentration (Pharmacological Data)

1 μmol/l

Method (Pharmacological Data)

cells incubated in KRH with 100 μmol/l 3-isobutyl-1-methylxanthine and title comp. for 1 h at 37 deg C; cAMP content measured using competitive binding of <3H>cAMP to a cAMP-binding protein

Further Details (Pharmacological Data)

HEK: human embryonic kidney; rTAR1: rat trace amine receptor 1; reference comp.: forskolin; KRH: Krebs-Ringer-HEPES buffer

Results

title comp. induced cAMP production acting as agonist (diagram)

Reference

Bunzow; Sonders; Arttamangkul; Harrison; Zhang; Quigley; Darland; Suchland; Pasumamula; Kennedy; Olson; Magenis; Amara; Grandy

Molecular Pharmacology, 2001 , vol. 60, # 6 p. 1181 - 1188 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

antagonist

Species or TestSystem (Pharmacological Data)

adult rhesus monkeys (Macaca mulatta)

Sex

male

Route of Application

intravenous

Concentration (Pharmacological Data)

0.1 - 10 mg/kg

Method (Pharmacological Data)

monkeys trained to sit in a chair, examined in an operant chamber; i.v. jugular catheter and vascular-access port inplanted; various light effects connected with various actions; effect of title comp. on cocaine abuse examined

Further Details (Pharmacological Data)

acute treatment (0.3-10 mg/kg) with 10-100 μg/kg cocaine; subacute treatment (3 or 5.6 mg/kg); assessement with GBR 12909maiintained responding (30 μg/kg)

Results

acute treatment with title comp. decreased cocaine maintained responding; subacute treatment also decreased cocaine-maintained responding more than food.maintained responding; decreased responding mainitained by GBR 12909 (30 μg/kg)

Reference

Wojnicki, Francis H. E.; Rothman, Richard B.; Rice, Kenner C.; Glowa, John R.

Journal of Pharmacology and Experimental Therapeutics, 1999 , vol. 288, # 2 p. 550 - 560 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

neuroregulatoric

Species or TestSystem (Pharmacological Data)

Sprague Dawley rat

Sex

male

Route of Application

intraperitoneal

Concentration (Pharmacological

20 mg/kg

Data)

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Method (Pharmacological Data)

rats perfused, title comp. added, samples collected from striatal dialysis, dopamine (DA) and serotonin (5-HT) measured with HPLC

Results

title comp. increased striatal DA concentrations (148 +/- 17 percent) without affecting those of 5-HT

Reference

Balcioglu, Aygul; Wurtman, Richard J.

Journal of Pharmacology and Experimental Therapeutics, 1998 , vol. 284, # 3 p. 991 - 997 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

incorporation into hair

Species or TestSystem (Pharmacological Data)

Dark-Agouti rats

Sex

male

Route of Application

intraperitoneal

Concentration (Pharmacological Data)

5 mg/kg

Exposure Period (Pharmacological Data)

10 d

Method (Pharmacological Data)

rats of 95-105 g, 5 wks old; back hair of rats shaved; hair collected; blood collected 5, 15, 30, 60, 120, 360 min after dosing; plasma prepared; areas under conc. vs. time curve (AUCs) calculated; incorporated rates (ICRs) determination

Results

AUC, 211.4 μg*min/ml; 35.55 ng/mg conc. in hair; ICR, 0.17

Reference

Nakahara, Yuji; Kikura, Ruri

Archives of Toxicology, 1996 , vol. 70, # 12 p. 841 - 849 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

modulation of discriminative effect of cocaine

Species or TestSystem (Pharmacological Data)

Sprague-Dawley rat

Sex

male

Route of Application

intraperitoneal

Concentration (Pharmacological Data)

1.25 - 5 mg/kg

Method (Pharmacological Data)

lever-responding drug discrimination test; rats trained to discriminate i.p. injected 10.0 mg/kg cocaine from saline; substitution test of title comp. at 20 min pre-session; percentage of rats making cocaine-lever selections counted

Type (Pharmacological Data)

ED50

Value of Type (Pharmacological Data)

2.356 mg/kg

Results

title comp. at doses of 1.25, 2.5 and 5.0 mg/kg produced 20, 58.3 and 80 percent, respectively, cocaine-lever selection (diagram)

Reference

Schechter, Martin D.; McBurney, Denise

Life Sciences, 1996 , vol. 59, # 20 p. PL303-PL308 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

modulation of discriminative effect of cocaine

Species or TestSystem (Pharmacological Data)

Sprague-Dawley rat

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Sex

male

Route of Application

intraperitoneal

Concentration (Pharmacological Data)

1.25 - 5 mg/kg

Method (Pharmacological Data)

lever-responding drug discrimination test; rats trained to discriminate 10.0 mg/kg cocaine from saline; substitution test of title comp. in combination with fenfluramine at 20 min pre-session; percentage of rats making cocaine-lever selections counted

Further Details (Pharmacological Data)

fenfluramine coadministered at 2 mg/kg

Type (Pharmacological Data)

ED50

Value of Type (Pharmacological Data)

2.356 mg/kg

Results

title comp. at doses of 1.25, 2.5 and 5.0 mg/kg produced 20, 58.3 and 80 percent, respectively, cocaine-lever selection, co-administration of title comp. with fenfluramine produced 40, 50 and 91.7 percent responding with ED50 1.817 mg/kg (diagram)

Reference

Schechter, Martin D.; McBurney, Denise

Life Sciences, 1996 , vol. 59, # 20 p. PL303-PL308 Title/Abstract Full Text View citing articles Show Details

Comment (Pharmacological Data)

inhibition of rat pancreatic lipase

Reference

Comai; Sullivan

Journal of Pharmaceutical Sciences, 1982 , vol. 71, # 4 p. 418 - 421 Title/Abstract Full Text View citing articles Show Details

Other Data Use (379) Use Pattern

Location

Reference

Pharmaceuticals

Page/Page column 22

Institute of Pharmacology and Toxicology Academy of Military Medical Sciences P.L.A. China; LI, Song; GAO, Chunsheng; ZHONG, Wu; WANG, Yuli; YANG, Meiyan; SHAN, Li; ZHOU, Xinbo; ZHENG, Zhibing; WANG, Xiaokui

Patent: EP2829266 A1, 2015 ; Title/Abstract Full Text Show Details

lowering blood pressure

Page/Page column 22

Institute of Pharmacology and Toxicology Academy of Military Medical Sciences P.L.A. China; LI, Song; GAO, Chunsheng; ZHONG, Wu; WANG, Yuli; YANG, Meiyan; SHAN, Li; ZHOU, Xinbo; ZHENG, Zhibing; WANG, Xiaokui

Patent: EP2829266 A1, 2015 ; Title/Abstract Full Text Show Details

manufacture of a medicament for reducing body weight

Page/Page column 22

Institute of Pharmacology and Toxicology Academy of Military Medical Sciences P.L.A. China; LI, Song; GAO, Chunsheng; ZHONG, Wu; WANG, Yuli; YANG, Meiyan; SHAN, Li; ZHOU, Xinbo; ZHENG, Zhibing; WANG, Xiaokui

Patent: EP2829266 A1, 2015 ; Title/Abstract Full Text Show Details

manufacture of a medicament for treatment of coronary heart disease

Page/Page column 22

manufacture of a medicament for treatment of diabetes

Page/Page column 22

Institute of Pharmacology and Toxicology Academy of Military Medical Sciences P.L.A. China; LI, Song; GAO, Chunsheng; ZHONG, Wu; WANG, Yuli; YANG, Meiyan; SHAN, Li; ZHOU, Xinbo; ZHENG, Zhibing; WANG, Xiaokui

Patent: EP2829266 A1, 2015 ; Title/Abstract Full Text Show Details

Institute of Pharmacology and Toxicology Academy of Military Medical Sciences P.L.A. China; LI, Song; GAO, Chunsheng; ZHONG, Wu; WANG, Yuli; YANG, Meiyan; SHAN, Li; ZHOU, Xinbo; ZHENG, Zhibing; WANG, Xiaokui

Patent: EP2829266 A1, 2015 ; Title/Abstract Full Text Show Details

manufacture of a medicament for treatment of hyperlipidemia

Page/Page column 22

Institute of Pharmacology and Toxicology Academy of Military Medical Sciences P.L.A. China; LI, Song; GAO, Chunsheng; ZHONG, Wu; WANG, Yuli; YANG, Meiyan; SHAN, Li; ZHOU, Xinbo; ZHENG, Zhibing; WANG, Xiaokui

Patent: EP2829266 A1, 2015 ; Title/Abstract Full Text Show Details

manufacture of a medicament for treatment of hypertension

Page/Page column 22

Institute of Pharmacology and Toxicology Academy of Military Medical Sciences P.L.A. China; LI, Song; GAO, Chunsheng; ZHONG, Wu; WANG, Yuli; YANG, Meiyan; SHAN, Li; ZHOU, Xinbo; ZHENG, Zhibing; WANG, Xiaokui

Patent: EP2829266 A1, 2015 ; Title/Abstract Full Text Show Details

realizing antihypertension

Page/Page column 22

Institute of Pharmacology and Toxicology Academy of Military Medical Sciences P.L.A. China; LI, Song; GAO, Chunsheng; ZHONG, Wu; WANG, Yuli; YANG, Meiyan; SHAN, Li; ZHOU, Xinbo; ZHENG, Zhibing; WANG, Xiaokui

Patent: EP2829266 A1, 2015 ; Title/Abstract Full Text Show Details

realizing blood fat reduction

Page/Page column 22

Institute of Pharmacology and Toxicology Academy of Military Medical Sciences P.L.A. China; LI, Song; GAO, Chunsheng; ZHONG, Wu; WANG, Yuli; YANG, Meiyan; SHAN, Li; ZHOU, Xinbo; ZHENG, Zhibing; WANG, Xiaokui

Patent: EP2829266 A1, 2015 ; Title/Abstract Full Text Show Details

realizing weight loss

Page/Page column 22

Institute of Pharmacology and Toxicology Academy of Military Medical Sciences P.L.A. China; LI, Song; GAO, Chunsheng; ZHONG, Wu; WANG, Yuli; YANG, Meiyan; SHAN, Li; ZHOU, Xinbo; ZHENG, Zhibing; WANG, Xiaokui

Patent: EP2829266 A1, 2015 ; Title/Abstract Full Text Show Details

reducing blood fat

Page/Page column 22

Institute of Pharmacology and Toxicology Academy of Military Medical Sciences P.L.A. China; LI, Song; GAO, Chunsheng; ZHONG, Wu; WANG, Yuli; YANG, Meiyan; SHAN, Li; ZHOU, Xinbo; ZHENG, Zhibing; WANG, Xiaokui

Patent: EP2829266 A1, 2015 ; Title/Abstract Full Text Show Details

treatment of mental or nervous diseases

Page/Page column 22

Institute of Pharmacology and Toxicology Academy of Military Medical Sciences P.L.A. China; LI, Song; GAO, Chunsheng; ZHONG, Wu; WANG, Yuli; YANG, Meiyan; SHAN, Li; ZHOU, Xinbo; ZHENG, Zhibing; WANG, Xiaokui

Patent: EP2829266 A1, 2015 ; Title/Abstract Full Text Show Details

Anti-obesity agent

Appetite-regulating agent

Obesity

dopamine reuptake inhibitor

Page/Page column 55

AUSPEX PHARMACEUTICAL, INC.; GANT, Thomas, G.; SHAHBAZ, Manoucherhr

Patent: WO2010/48358 A2, 2010 ;

Page/Page column 55

AUSPEX PHARMACEUTICAL, INC.; GANT, Thomas, G.; SHAHBAZ, Manoucherhr

Patent: WO2010/48358 A2, 2010 ;

Page/Page column 55

AUSPEX PHARMACEUTICAL, INC.; GANT, Thomas, G.; SHAHBAZ, Manoucherhr

Patent: WO2010/48358 A2, 2010 ;

OREXIGEN THERAPEUTICS, INC.

Patent: WO2006/17504 A1, 2006 ;

Title/Abstract Full Text Show Details

Title/Abstract Full Text Show Details

Title/Abstract Full Text Show Details

Title/Abstract Full Text Show Details

Orexigen Therapeutics, Inc

Patent: US2008/113026 A1, 2008 ; Title/Abstract Full Text Show Details

Weight loss

OREXIGEN THERAPEUTICS, INC.

Patent: WO2007/16108 A1, 2007 ; Title/Abstract Full Text Show Details

Orexigen Therapeutics, Inc

Patent: US2008/113026 A1, 2008 ; Title/Abstract Full Text Show Details

Suppressing appetite

Orexigen Therapeutics, Inc

Patent: US2008/113026 A1, 2008 ; Title/Abstract Full Text Show Details

Obesity-related conditions

Orexigen Therapeutics, Inc

Patent: US2008/113026 A1, 2008 ; Title/Abstract Full Text Show Details

in combination with dapagliflozin or its propylene glycol hydrate

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Bristol-Myers Squibb

Patent: US2008/234366 A1, 2008 ; Title/Abstract Full Text Show Details

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antiobesity agent

PHARMACOPEIA DRUG DISCOVERY, INC.

Patent: WO2006/44293 A2, 2006 ; Title/Abstract Full Text Show Details

Avestha Gengraine Technologies Pvt. Ltd.

Patent: US2008/20971 A1, 2008 ; Title/Abstract Full Text Show Details

Bristol-Myers Squibb

Patent: US2008/234366 A1, 2008 ; Title/Abstract Full Text Show Details

in combination with SGLT2 inhibitor

BRISTOL-MYERS SQUIBB

Patent: US2008/234367 A1, 2008 ; Title/Abstract Full Text Show Details

obesity

OREXIGEN THERAPEUTICS, INC.

Patent: WO2006/17504 A1, 2006 ; Title/Abstract Full Text Show Details

GELESIS, INC.

Patent: WO2007/112436 A2, 2007 ; Title/Abstract Full Text Show Details

BRISTOL-MYERS SQUIBB

Patent: US2008/234367 A1, 2008 ; Title/Abstract Full Text Show Details

anti-obesity agent

BRISTOL-MYERS SQUIBB

Patent: US2008/234367 A1, 2008 ; Title/Abstract Full Text Show Details

anorectic agent

PHARMACOPEIA DRUG DISCOVERY, INC.

Patent: WO2006/44293 A2, 2006 ; Title/Abstract Full Text Show Details

Bristol-Myers Squibb

Patent: US2008/234366 A1, 2008 ; Title/Abstract Full Text Show Details

BRISTOL-MYERS SQUIBB

Patent: US2008/234367 A1, 2008 ; Title/Abstract Full Text Show Details

Weight control

ALPEX PHARMA S.A.

Patent: US2008/206327 A1, 2008 ; Title/Abstract Full Text Show Details

epilepsy

LABORATORIOS DEL DR.ESTEVE, S.A

Patent: WO2007/9693 A1, 2007 ; Title/Abstract Full Text Show Details

Tam, Peter Y.; Wilson, Leland F.

Patent: US2008/103179 A1, 2008 ; Title/Abstract Full Text Show Details

diabetes

Tam, Peter Y.; Wilson, Leland F.

Patent: US2008/103179 A1, 2008 ; Title/Abstract Full Text Show Details

hypertension

Yancopoulos, George D.; Wiegand, Stanley J.; Sleeman, Mark W.; Koehler-Stec, Ellen-Marie

Patent: US2006/58224 A1, 2006 ;

Title/Abstract Full Text Show Details

Tam, Peter Y.; Wilson, Leland F.

Patent: US2008/103179 A1, 2008 ; Title/Abstract Full Text Show Details

pulmonary hypertension

Tam, Peter Y.; Wilson, Leland F.

Patent: US2008/103179 A1, 2008 ; Title/Abstract Full Text Show Details

migraine

LABORATORIOS DEL DR.ESTEVE, S.A

Patent: WO2007/9693 A1, 2007 ; Title/Abstract Full Text Show Details

Tam, Peter Y.; Wilson, Leland F.

Patent: US2008/103179 A1, 2008 ; Title/Abstract Full Text Show Details

sleep apnea

Tam, Peter Y.; Wilson, Leland F.

Patent: US2008/103179 A1, 2008 ; Title/Abstract Full Text Show Details

depression

LABORATORIOS DEL DR.ESTEVE, S.A

Patent: WO2007/9693 A1, 2007 ; Title/Abstract Full Text Show Details

Tam, Peter Y.; Wilson, Leland F.

Patent: US2008/103179 A1, 2008 ; Title/Abstract Full Text Show Details

impulse control disorders

Tam, Peter Y.; Wilson, Leland F.

Patent: US2008/103179 A1, 2008 ; Title/Abstract Full Text Show Details

alcohol addiction

Tam, Peter Y.; Wilson, Leland F.

Patent: US2008/103179 A1, 2008 ; Title/Abstract Full Text Show Details

sympathomimetic agent

Tam, Peter Y.; Wilson, Leland F.

Patent: US2008/103179 A1, 2008 ; Title/Abstract Full Text Show Details

second agent of the composition with antiepileptic agent

Tam, Peter Y.; Wilson, Leland F.

Patent: US2008/103179 A1, 2008 ; Title/Abstract Full Text Show Details

second agent of the composition with anticonvulsant sulfamate or sulfonylurea compound

Tam, Peter Y.; Wilson, Leland F.

Patent: US2008/103179 A1, 2008 ; Title/Abstract Full Text Show Details

Antiobesity

Sattigeri, Jitendra A.; Andappan, Murugaiah M.S.; Kishore, Kaushal; Sethi, Sachin; Kandalkar, Sachin Ramesh; Pal, Chanchal Kumar; Mahajan, Dipak C.; Ahmed, Shahadat; Parkale, Santhosh Sadashiv; Srinivasan, T.; Sharma, Lalima; Bansal, Vinay S.; Chugh, Anita; Davis, Joseph Alexanand

Patent: US2008/300251 A1, 2008 ; Title/Abstract Full Text Show Details

Anti-obesity agent

Bhanot, Sanjay; Dobie, Kenneth W.

Patent: US2005/261233 A1, 2005 ; Title/Abstract Full Text Show Details

IRM LLC

Patent: WO2005/113506 A1, 2005 ; Title/Abstract Full Text Show Details

JOHN I. HASS, INC.

Patent: WO2006/55985 A1, 2006 ;

Title/Abstract Full Text Show Details

BRISTOL-MYERS SQUIBB COMPANY

Patent: WO2006/71752 A1, 2006 ; Title/Abstract Full Text Show Details

PROTEMIX CORPORATION LIMITED

Patent: WO2006/104397 A1, 2006 ; Title/Abstract Full Text Show Details

NOVARTIS AG; NOVARTIS PHARMA GmbH

Patent: WO2007/41366 A1, 2007 ; Title/Abstract Full Text Show Details

Bristol-Myers Squibb Company

Patent: US2007/99913 A1, 2007 ; Title/Abstract Full Text Show Details

AMYLIN PHARMACEUTICALS, INC.

Patent: WO2007/55728 A1, 2007 ; Title/Abstract Full Text Show Details

IRM LLC

Patent: WO2007/89557 A2, 2007 ; Title/Abstract Full Text Show Details

IRM LLC

Patent: WO2007/89667 A1, 2007 ; Title/Abstract Full Text Show Details

Bristol-Myers Squibb Company

Patent: US2008/9533 A1, 2008 ; Title/Abstract Full Text Show Details

IRM LLC

Patent: WO2005/113519 A1, 2005 ; Title/Abstract Full Text Show Details

anti-diabetic agent

Anorectic agent

Insulin resistance

Page/Page column 10; 32

Page/Page column 10; 32

Bristol-Myers Squibb Company

Patent: US2008/9534 A1, 2008 ; Title/Abstract Full Text Show Details

Bristol-Myers Squibb Company

Patent: US2008/9534 A1, 2008 ; Title/Abstract Full Text Show Details

NOVARTIS AG; NOVARTIS PHARMA GMBH

Patent: WO2005/49088 A2, 2005 ; Title/Abstract Full Text Show Details

LABORATORIOS DEL DR.ESTEVE, S.A

Patent: WO2007/9693 A1, 2007 ; Title/Abstract Full Text Show Details

Antiobesity agent

Novo Nordisk, A/S

Patent: US6972294 B1, 2005 ; Title/Abstract Full Text Show Details

NOVO NORDISK A/S

Patent: WO2007/144394 A2, 2007 ; Title/Abstract Full Text Show Details

Appetite suppressant

Bhanot, Sanjay; Dobie, Kenneth W.

Patent: US2005/261233 A1, 2005 ; Title/Abstract Full Text Show Details

POMYTKIN, Igor Anatolievich; SOLOVIEV, Sergey Pavlovich

Patent: WO2007/69932 A1, 2007 ; Title/Abstract Full Text Show Details

metabolic syndrome

Yancopoulos, George D.; Wiegand, Stanley J.; Sleeman, Mark W.; Koehler-Stec, Ellen-Marie

Patent: US2006/58224 A1, 2006 ; Title/Abstract Full Text Show Details

LABORATORIOS DEL DR.ESTEVE, S.A

Patent: WO2007/9693 A1, 2007 ;

Title/Abstract Full Text Show Details

Anti-obesity compound

ASTRAZENECA AB; ASTRAZENECA UK LIMITED

Patent: WO2006/67428 A2, 2006 ; Title/Abstract Full Text Show Details

PFIZER PRODUCTS INC.

Patent: WO2006/90250 A1, 2006 ; Title/Abstract Full Text Show Details

ASTRAZENECA AB

Patent: WO2007/64272 A1, 2007 ; Title/Abstract Full Text Show Details

food-related disorders

LABORATORIOS DEL DR. ESTEVE, S.A.

Patent: EP1743636 A1, 2007 ; Title/Abstract Full Text Show Details

Antiobesity compound

MERCK and CO., INC.

Patent: WO2006/127530 A2, 2006 ; Title/Abstract Full Text Show Details

MERCK FROSST CANADA LTD.

Patent: WO2007/134457 A1, 2007 ; Title/Abstract Full Text Show Details

cannabinoid 1 (CB1) receptor modulator; lipase inhibitor

LABORATORIOS DEL DR.ESTEVE, S.A

Patent: WO2007/9693 A1, 2007 ; Title/Abstract Full Text Show Details

Food-related disorders

LABORATORIOS DEL DR.ESTEVE, S.A

Patent: WO2007/9693 A1, 2007 ; Title/Abstract Full Text Show Details

Digestive metabolism

LABORATORIOS DEL DR.ESTEVE, S.A

Patent: WO2007/9693 A1, 2007 ; Title/Abstract Full Text Show Details

Regulate food intake

LABORATORIOS DEL DR.ESTEVE, S.A

Patent: WO2007/9693 A1, 2007 ; Title/Abstract Full Text Show Details

Modulate energy expenditure

LABORATORIOS DEL DR.ESTEVE, S.A

Patent: WO2007/9693 A1, 2007 ; Title/Abstract Full Text Show Details

Reduce central anorexigenic effects

LABORATORIOS DEL DR.ESTEVE, S.A

Patent: WO2007/9693 A1, 2007 ; Title/Abstract Full Text Show Details

Reduce peripheral anorexigenic effects

LABORATORIOS DEL DR.ESTEVE, S.A

Patent: WO2007/9693 A1, 2007 ; Title/Abstract Full Text Show Details

bulimia

LABORATORIOS DEL DR.ESTEVE, S.A

Patent: WO2007/9693 A1, 2007 ; Title/Abstract Full Text Show Details

anorexia

LABORATORIOS DEL DR.ESTEVE, S.A

Patent: WO2007/9693 A1, 2007 ; Title/Abstract Full Text Show Details

cachexia

LABORATORIOS DEL DR.ESTEVE, S.A

Patent: WO2007/9693 A1, 2007 ; Title/Abstract Full Text Show Details

drug-induced obesity

LABORATORIOS DEL DR.ESTEVE, S.A

Patent: WO2007/9693 A1, 2007 ; Title/Abstract Full Text Show Details

appetence disorder

LABORATORIOS DEL DR.ESTEVE, S.A

Patent: WO2007/9693 A1, 2007 ; Title/Abstract Full Text Show Details

appetite disorders

LABORATORIOS DEL DR.ESTEVE, S.A

Patent: WO2007/9693 A1, 2007 ; Title/Abstract Full Text Show Details

eating disorders associated with excessive food intake

LABORATORIOS DEL DR.ESTEVE, S.A

Patent: WO2007/9693 A1, 2007 ; Title/Abstract Full Text Show Details

type Il diabetus mellitus

LABORATORIOS DEL DR.ESTEVE, S.A

Patent: WO2007/9693 A1, 2007 ; Title/Abstract Full Text Show Details

non-insuline dependent diabetes mellitus

LABORATORIOS DEL DR.ESTEVE, S.A

Patent: WO2007/9693 A1, 2007 ; Title/Abstract Full Text Show Details

Improve cardiovascular

LABORATORIOS DEL DR.ESTEVE, S.A

Patent: WO2007/9693 A1, 2007 ; Title/Abstract Full Text Show Details

Improve metabolic risk factor

LABORATORIOS DEL DR.ESTEVE, S.A

Patent: WO2007/9693 A1, 2007 ; Title/Abstract Full Text Show Details

Elevated triglycerides

LABORATORIOS DEL DR.ESTEVE, S.A

Patent: WO2007/9693 A1, 2007 ; Title/Abstract Full Text Show Details

Lower HDL cholesterol

LABORATORIOS DEL DR.ESTEVE, S.A

Patent: WO2007/9693 A1, 2007 ; Title/Abstract Full Text Show Details

Impaired fasting glucose

LABORATORIOS DEL DR.ESTEVE, S.A

Patent: WO2007/9693 A1, 2007 ; Title/Abstract Full Text Show Details

Dyslipidemia

LABORATORIOS DEL DR.ESTEVE, S.A

Patent: WO2007/9693 A1, 2007 ; Title/Abstract Full Text Show Details

weight independent aspects of metabolic syndrome

LABORATORIOS DEL DR.ESTEVE, S.A

Patent: WO2007/9693 A1, 2007 ; Title/Abstract Full Text Show Details

Restenosis

LABORATORIOS DEL DR.ESTEVE, S.A

Patent: WO2007/9693 A1, 2007 ; Title/Abstract Full Text Show Details

Psychosis

LABORATORIOS DEL DR.ESTEVE, S.A

Patent: WO2007/9693 A1, 2007 ; Title/Abstract Full Text Show Details

alcohol abuse

LABORATORIOS DEL DR.ESTEVE, S.A

Patent: WO2007/9693 A1, 2007 ;

Title/Abstract Full Text Show Details

nicotine abuse

LABORATORIOS DEL DR.ESTEVE, S.A

Patent: WO2007/9693 A1, 2007 ; Title/Abstract Full Text Show Details

drug abuse

LABORATORIOS DEL DR.ESTEVE, S.A

Patent: WO2007/9693 A1, 2007 ; Title/Abstract Full Text Show Details

medicament abuse

LABORATORIOS DEL DR.ESTEVE, S.A

Patent: WO2007/9693 A1, 2007 ; Title/Abstract Full Text Show Details

schizophrenia

LABORATORIOS DEL DR.ESTEVE, S.A

Patent: WO2007/9693 A1, 2007 ; Title/Abstract Full Text Show Details

anxiety

LABORATORIOS DEL DR.ESTEVE, S.A

Patent: WO2007/9693 A1, 2007 ; Title/Abstract Full Text Show Details

neurodegenerative disorders

LABORATORIOS DEL DR.ESTEVE, S.A

Patent: WO2007/9693 A1, 2007 ; Title/Abstract Full Text Show Details

Morbus Parkinson

LABORATORIOS DEL DR.ESTEVE, S.A

Patent: WO2007/9693 A1, 2007 ; Title/Abstract Full Text Show Details

Morbus Huntington

LABORATORIOS DEL DR.ESTEVE, S.A

Patent: WO2007/9693 A1, 2007 ; Title/Abstract Full Text Show Details

Morbus Alzheimer

LABORATORIOS DEL DR.ESTEVE, S.A

Patent: WO2007/9693 A1, 2007 ; Title/Abstract Full Text Show Details

Multiple Sclerosis

LABORATORIOS DEL DR.ESTEVE, S.A

Patent: WO2007/9693 A1, 2007 ; Title/Abstract Full Text Show Details

cerebellar disorders

LABORATORIOS DEL DR.ESTEVE, S.A

Patent: WO2007/9693 A1, 2007 ; Title/Abstract Full Text Show Details

spinocerebellar disorders

LABORATORIOS DEL DR.ESTEVE, S.A

Patent: WO2007/9693 A1, 2007 ; Title/Abstract Full Text Show Details

cognitive disorders

LABORATORIOS DEL DR.ESTEVE, S.A

Patent: WO2007/9693 A1, 2007 ; Title/Abstract Full Text Show Details

cranial trauma

LABORATORIOS DEL DR.ESTEVE, S.A

Patent: WO2007/9693 A1, 2007 ; Title/Abstract Full Text Show Details

panic attacks

LABORATORIOS DEL DR.ESTEVE, S.A

Patent: WO2007/9693 A1, 2007 ;

Title/Abstract Full Text Show Details

peripheric neuropathy

LABORATORIOS DEL DR.ESTEVE, S.A

Patent: WO2007/9693 A1, 2007 ; Title/Abstract Full Text Show Details

glaucoma

LABORATORIOS DEL DR.ESTEVE, S.A

Patent: WO2007/9693 A1, 2007 ; Title/Abstract Full Text Show Details

Raynaud's disease

LABORATORIOS DEL DR.ESTEVE, S.A

Patent: WO2007/9693 A1, 2007 ; Title/Abstract Full Text Show Details

tremblement disorders

LABORATORIOS DEL DR.ESTEVE, S.A

Patent: WO2007/9693 A1, 2007 ; Title/Abstract Full Text Show Details

compulsive disorders

LABORATORIOS DEL DR.ESTEVE, S.A

Patent: WO2007/9693 A1, 2007 ; Title/Abstract Full Text Show Details

senile dementia

LABORATORIOS DEL DR.ESTEVE, S.A

Patent: WO2007/9693 A1, 2007 ; Title/Abstract Full Text Show Details

thymic disorders

LABORATORIOS DEL DR.ESTEVE, S.A

Patent: WO2007/9693 A1, 2007 ; Title/Abstract Full Text Show Details

tardive dyskinesia

LABORATORIOS DEL DR.ESTEVE, S.A

Patent: WO2007/9693 A1, 2007 ; Title/Abstract Full Text Show Details

bone disorders

LABORATORIOS DEL DR.ESTEVE, S.A

Patent: WO2007/9693 A1, 2007 ; Title/Abstract Full Text Show Details

osteoporosis

LABORATORIOS DEL DR.ESTEVE, S.A

Patent: WO2007/9693 A1, 2007 ; Title/Abstract Full Text Show Details

Paget's disease of bone

LABORATORIOS DEL DR.ESTEVE, S.A

Patent: WO2007/9693 A1, 2007 ; Title/Abstract Full Text Show Details

cancer

LABORATORIOS DEL DR.ESTEVE, S.A

Patent: WO2007/9693 A1, 2007 ; Title/Abstract Full Text Show Details

brain cancer

LABORATORIOS DEL DR.ESTEVE, S.A

Patent: WO2007/9693 A1, 2007 ; Title/Abstract Full Text Show Details

bone cancer

LABORATORIOS DEL DR.ESTEVE, S.A

Patent: WO2007/9693 A1, 2007 ; Title/Abstract Full Text Show Details

lip cancer

LABORATORIOS DEL DR.ESTEVE, S.A

Patent: WO2007/9693 A1, 2007 ; Title/Abstract Full Text Show Details

mouth cancer

LABORATORIOS DEL DR.ESTEVE, S.A

Patent: WO2007/9693 A1, 2007 ; Title/Abstract Full Text Show Details

esophageal cancer

LABORATORIOS DEL DR.ESTEVE, S.A

Patent: WO2007/9693 A1, 2007 ; Title/Abstract Full Text Show Details

stomach cancer

LABORATORIOS DEL DR.ESTEVE, S.A

Patent: WO2007/9693 A1, 2007 ; Title/Abstract Full Text Show Details

liver cancer

LABORATORIOS DEL DR.ESTEVE, S.A

Patent: WO2007/9693 A1, 2007 ; Title/Abstract Full Text Show Details

bladder cancer

LABORATORIOS DEL DR.ESTEVE, S.A

Patent: WO2007/9693 A1, 2007 ; Title/Abstract Full Text Show Details

pancreas cancer

LABORATORIOS DEL DR.ESTEVE, S.A

Patent: WO2007/9693 A1, 2007 ; Title/Abstract Full Text Show Details

ovary cancer

LABORATORIOS DEL DR.ESTEVE, S.A

Patent: WO2007/9693 A1, 2007 ; Title/Abstract Full Text Show Details

cervical cancer

LABORATORIOS DEL DR.ESTEVE, S.A

Patent: WO2007/9693 A1, 2007 ; Title/Abstract Full Text Show Details

lung cancer

LABORATORIOS DEL DR.ESTEVE, S.A

Patent: WO2007/9693 A1, 2007 ; Title/Abstract Full Text Show Details

breast cancer

LABORATORIOS DEL DR.ESTEVE, S.A

Patent: WO2007/9693 A1, 2007 ; Title/Abstract Full Text Show Details

skin cancer

LABORATORIOS DEL DR.ESTEVE, S.A

Patent: WO2007/9693 A1, 2007 ; Title/Abstract Full Text Show Details

colon cancer

LABORATORIOS DEL DR.ESTEVE, S.A

Patent: WO2007/9693 A1, 2007 ; Title/Abstract Full Text Show Details

bowl cancer

LABORATORIOS DEL DR.ESTEVE, S.A

Patent: WO2007/9693 A1, 2007 ; Title/Abstract Full Text Show Details

prostate cancer

LABORATORIOS DEL DR.ESTEVE, S.A

Patent: WO2007/9693 A1, 2007 ; Title/Abstract Full Text Show Details

colcon cancer

LABORATORIOS DEL DR.ESTEVE, S.A

Patent: WO2007/9693 A1, 2007 ; Title/Abstract Full Text Show Details

bowel cancer

LABORATORIOS DEL DR.ESTEVE, S.A

Patent: WO2007/9693 A1, 2007 ;

Title/Abstract Full Text Show Details

medicament-induced movement disorders

LABORATORIOS DEL DR.ESTEVE, S.A

Patent: WO2007/9693 A1, 2007 ; Title/Abstract Full Text Show Details

dystonia

LABORATORIOS DEL DR.ESTEVE, S.A

Patent: WO2007/9693 A1, 2007 ; Title/Abstract Full Text Show Details

endotoxemic shock

LABORATORIOS DEL DR.ESTEVE, S.A

Patent: WO2007/9693 A1, 2007 ; Title/Abstract Full Text Show Details

stroke

LABORATORIOS DEL DR.ESTEVE, S.A

Patent: WO2007/9693 A1, 2007 ; Title/Abstract Full Text Show Details

hemorrhagic shock

LABORATORIOS DEL DR.ESTEVE, S.A

Patent: WO2007/9693 A1, 2007 ; Title/Abstract Full Text Show Details

hypotension

LABORATORIOS DEL DR.ESTEVE, S.A

Patent: WO2007/9693 A1, 2007 ; Title/Abstract Full Text Show Details

insomnia

LABORATORIOS DEL DR.ESTEVE, S.A

Patent: WO2007/9693 A1, 2007 ; Title/Abstract Full Text Show Details

immunologic disorders

LABORATORIOS DEL DR.ESTEVE, S.A

Patent: WO2007/9693 A1, 2007 ; Title/Abstract Full Text Show Details

sclerotic plaques

LABORATORIOS DEL DR.ESTEVE, S.A

Patent: WO2007/9693 A1, 2007 ; Title/Abstract Full Text Show Details

diarrhea

LABORATORIOS DEL DR.ESTEVE, S.A

Patent: WO2007/9693 A1, 2007 ; Title/Abstract Full Text Show Details

asthma

LABORATORIOS DEL DR.ESTEVE, S.A

Patent: WO2007/9693 A1, 2007 ; Title/Abstract Full Text Show Details

memory disorders

LABORATORIOS DEL DR.ESTEVE, S.A

Patent: WO2007/9693 A1, 2007 ; Title/Abstract Full Text Show Details

pruritus

LABORATORIOS DEL DR.ESTEVE, S.A

Patent: WO2007/9693 A1, 2007 ; Title/Abstract Full Text Show Details

pain

LABORATORIOS DEL DR.ESTEVE, S.A

Patent: WO2007/9693 A1, 2007 ; Title/Abstract Full Text Show Details

potentiation of the analgesic effect of narcotic

LABORATORIOS DEL DR.ESTEVE, S.A

Patent: WO2007/9693 A1, 2007 ; Title/Abstract Full Text Show Details

influencing intestinal transit

LABORATORIOS DEL DR.ESTEVE, S.A

Patent: WO2007/9693 A1, 2007 ; Title/Abstract Full Text Show Details

potentiation of the non-narcotic analgesics effect of narcotic

LABORATORIOS DEL DR.ESTEVE, S.A

Patent: WO2007/9693 A1, 2007 ; Title/Abstract Full Text Show Details

dementia

LABORATORIOS DEL DR.ESTEVE, S.A

Patent: WO2007/9693 A1, 2007 ; Title/Abstract Full Text Show Details

memory loss

LABORATORIOS DEL DR.ESTEVE, S.A

Patent: WO2007/9693 A1, 2007 ; Title/Abstract Full Text Show Details

vascular dementia

LABORATORIOS DEL DR.ESTEVE, S.A

Patent: WO2007/9693 A1, 2007 ; Title/Abstract Full Text Show Details

mild cognitive impairment

LABORATORIOS DEL DR.ESTEVE, S.A

Patent: WO2007/9693 A1, 2007 ; Title/Abstract Full Text Show Details

frontotemporal dementia

LABORATORIOS DEL DR.ESTEVE, S.A

Patent: WO2007/9693 A1, 2007 ; Title/Abstract Full Text Show Details

Pick's disease

LABORATORIOS DEL DR.ESTEVE, S.A

Patent: WO2007/9693 A1, 2007 ; Title/Abstract Full Text Show Details

binge eating disorders

LABORATORIOS DEL DR.ESTEVE, S.A

Patent: WO2007/9693 A1, 2007 ; Title/Abstract Full Text Show Details

juvenile obesity

LABORATORIOS DEL DR.ESTEVE, S.A

Patent: WO2007/9693 A1, 2007 ; Title/Abstract Full Text Show Details

drug induced obesity

LABORATORIOS DEL DR.ESTEVE, S.A

Patent: WO2007/9693 A1, 2007 ; Title/Abstract Full Text Show Details

atypical depression

LABORATORIOS DEL DR.ESTEVE, S.A

Patent: WO2007/9693 A1, 2007 ; Title/Abstract Full Text Show Details

behavioural addictions

LABORATORIOS DEL DR.ESTEVE, S.A

Patent: WO2007/9693 A1, 2007 ; Title/Abstract Full Text Show Details

attention deficit disorders

LABORATORIOS DEL DR.ESTEVE, S.A

Patent: WO2007/9693 A1, 2007 ; Title/Abstract Full Text Show Details

Tourette's syndrome

LABORATORIOS DEL DR.ESTEVE, S.A

Patent: WO2007/9693 A1, 2007 ; Title/Abstract Full Text Show Details

suppression of reward- related behaviours

LABORATORIOS DEL DR.ESTEVE, S.A

Patent: WO2007/9693 A1, 2007 ;

Title/Abstract Full Text Show Details

conditioned place avoidance

LABORATORIOS DEL DR.ESTEVE, S.A

Patent: WO2007/9693 A1, 2007 ; Title/Abstract Full Text Show Details

suppression of cocaine-induced conditioned place preference

LABORATORIOS DEL DR.ESTEVE, S.A

Patent: WO2007/9693 A1, 2007 ; Title/Abstract Full Text Show Details

suppression of morphine-induced conditioned place preference

LABORATORIOS DEL DR.ESTEVE, S.A

Patent: WO2007/9693 A1, 2007 ; Title/Abstract Full Text Show Details

impulsivity

LABORATORIOS DEL DR.ESTEVE, S.A

Patent: WO2007/9693 A1, 2007 ; Title/Abstract Full Text Show Details

sexual dysfunction

LABORATORIOS DEL DR.ESTEVE, S.A

Patent: WO2007/9693 A1, 2007 ; Title/Abstract Full Text Show Details

erectile difficulty

LABORATORIOS DEL DR.ESTEVE, S.A

Patent: WO2007/9693 A1, 2007 ; Title/Abstract Full Text Show Details

female sexual dysfunction

LABORATORIOS DEL DR.ESTEVE, S.A

Patent: WO2007/9693 A1, 2007 ; Title/Abstract Full Text Show Details

seizure disorders

LABORATORIOS DEL DR.ESTEVE, S.A

Patent: WO2007/9693 A1, 2007 ; Title/Abstract Full Text Show Details

nausea

LABORATORIOS DEL DR.ESTEVE, S.A

Patent: WO2007/9693 A1, 2007 ; Title/Abstract Full Text Show Details

emesis

LABORATORIOS DEL DR.ESTEVE, S.A

Patent: WO2007/9693 A1, 2007 ; Title/Abstract Full Text Show Details

neuroinflammatory disease

LABORATORIOS DEL DR.ESTEVE, S.A

Patent: WO2007/9693 A1, 2007 ; Title/Abstract Full Text Show Details

demyelinisation related disorders

LABORATORIOS DEL DR.ESTEVE, S.A

Patent: WO2007/9693 A1, 2007 ; Title/Abstract Full Text Show Details

Guillan-Barre syndrome

LABORATORIOS DEL DR.ESTEVE, S.A

Patent: WO2007/9693 A1, 2007 ; Title/Abstract Full Text Show Details

viral encephalitis

LABORATORIOS DEL DR.ESTEVE, S.A

Patent: WO2007/9693 A1, 2007 ; Title/Abstract Full Text Show Details

cerebrovascular accidents

LABORATORIOS DEL DR.ESTEVE, S.A

Patent: WO2007/9693 A1, 2007 ; Title/Abstract Full Text Show Details

Neurological disorder

LABORATORIOS DEL DR.ESTEVE, S.A

Patent: WO2007/9693 A1, 2007 ; Title/Abstract Full Text Show Details

muscle spasticity

LABORATORIOS DEL DR.ESTEVE, S.A

Patent: WO2007/9693 A1, 2007 ; Title/Abstract Full Text Show Details

traumatic brain injury

LABORATORIOS DEL DR.ESTEVE, S.A

Patent: WO2007/9693 A1, 2007 ; Title/Abstract Full Text Show Details

spinal cord injury

LABORATORIOS DEL DR.ESTEVE, S.A

Patent: WO2007/9693 A1, 2007 ; Title/Abstract Full Text Show Details

inflammation

LABORATORIOS DEL DR.ESTEVE, S.A

Patent: WO2007/9693 A1, 2007 ; Title/Abstract Full Text Show Details

immunomodulatory disorders

LABORATORIOS DEL DR.ESTEVE, S.A

Patent: WO2007/9693 A1, 2007 ; Title/Abstract Full Text Show Details

cutaneous T-cell lymphoma

LABORATORIOS DEL DR.ESTEVE, S.A

Patent: WO2007/9693 A1, 2007 ; Title/Abstract Full Text Show Details

rheumatoid arthritis

LABORATORIOS DEL DR.ESTEVE, S.A

Patent: WO2007/9693 A1, 2007 ; Title/Abstract Full Text Show Details

systemic lupus erythematosus

LABORATORIOS DEL DR.ESTEVE, S.A

Patent: WO2007/9693 A1, 2007 ; Title/Abstract Full Text Show Details

sepsis

LABORATORIOS DEL DR.ESTEVE, S.A

Patent: WO2007/9693 A1, 2007 ; Title/Abstract Full Text Show Details

sarcoidosis

LABORATORIOS DEL DR.ESTEVE, S.A

Patent: WO2007/9693 A1, 2007 ; Title/Abstract Full Text Show Details

idiopathic pulmonary fibrosis

LABORATORIOS DEL DR.ESTEVE, S.A

Patent: WO2007/9693 A1, 2007 ; Title/Abstract Full Text Show Details

bronchopulmonary dysplasia

LABORATORIOS DEL DR.ESTEVE, S.A

Patent: WO2007/9693 A1, 2007 ; Title/Abstract Full Text Show Details

retinal disease

LABORATORIOS DEL DR.ESTEVE, S.A

Patent: WO2007/9693 A1, 2007 ; Title/Abstract Full Text Show Details

Scleroderma

LABORATORIOS DEL DR.ESTEVE, S.A

Patent: WO2007/9693 A1, 2007 ; Title/Abstract Full Text Show Details

renal ischemia

LABORATORIOS DEL DR.ESTEVE, S.A

Patent: WO2007/9693 A1, 2007 ;

Title/Abstract Full Text Show Details

mycocardial infarction

LABORATORIOS DEL DR.ESTEVE, S.A

Patent: WO2007/9693 A1, 2007 ; Title/Abstract Full Text Show Details

cerebral ischemia

LABORATORIOS DEL DR.ESTEVE, S.A

Patent: WO2007/9693 A1, 2007 ; Title/Abstract Full Text Show Details

nephritis

LABORATORIOS DEL DR.ESTEVE, S.A

Patent: WO2007/9693 A1, 2007 ; Title/Abstract Full Text Show Details

hepatitis

LABORATORIOS DEL DR.ESTEVE, S.A

Patent: WO2007/9693 A1, 2007 ; Title/Abstract Full Text Show Details

glomerulonephritis

LABORATORIOS DEL DR.ESTEVE, S.A

Patent: WO2007/9693 A1, 2007 ; Title/Abstract Full Text Show Details

cryptogenic fibrosing aveolitis

LABORATORIOS DEL DR.ESTEVE, S.A

Patent: WO2007/9693 A1, 2007 ; Title/Abstract Full Text Show Details

psoriasis

LABORATORIOS DEL DR.ESTEVE, S.A

Patent: WO2007/9693 A1, 2007 ; Title/Abstract Full Text Show Details

transplant rejection

LABORATORIOS DEL DR.ESTEVE, S.A

Patent: WO2007/9693 A1, 2007 ; Title/Abstract Full Text Show Details

atopic dermatitis

LABORATORIOS DEL DR.ESTEVE, S.A

Patent: WO2007/9693 A1, 2007 ; Title/Abstract Full Text Show Details

vasculitis

LABORATORIOS DEL DR.ESTEVE, S.A

Patent: WO2007/9693 A1, 2007 ; Title/Abstract Full Text Show Details

allergy

LABORATORIOS DEL DR.ESTEVE, S.A

Patent: WO2007/9693 A1, 2007 ; Title/Abstract Full Text Show Details

Seasonal allergic rhinitis

LABORATORIOS DEL DR.ESTEVE, S.A

Patent: WO2007/9693 A1, 2007 ; Title/Abstract Full Text Show Details

Crohn's disease

LABORATORIOS DEL DR.ESTEVE, S.A

Patent: WO2007/9693 A1, 2007 ; Title/Abstract Full Text Show Details

inflammatory bowel disease

LABORATORIOS DEL DR.ESTEVE, S.A

Patent: WO2007/9693 A1, 2007 ; Title/Abstract Full Text Show Details

reversible airway obstruction

LABORATORIOS DEL DR.ESTEVE, S.A

Patent: WO2007/9693 A1, 2007 ; Title/Abstract Full Text Show Details

adult respiratory distress syndrome

LABORATORIOS DEL DR.ESTEVE, S.A

Patent: WO2007/9693 A1, 2007 ; Title/Abstract Full Text Show Details

chronic obstructive pulmonary disease

LABORATORIOS DEL DR.ESTEVE, S.A

Patent: WO2007/9693 A1, 2007 ; Title/Abstract Full Text Show Details

bronchitis

LABORATORIOS DEL DR.ESTEVE, S.A

Patent: WO2007/9693 A1, 2007 ; Title/Abstract Full Text Show Details

cerebral apoplexy

LABORATORIOS DEL DR.ESTEVE, S.A

Patent: WO2007/9693 A1, 2007 ; Title/Abstract Full Text Show Details

craniocerebral trauma

LABORATORIOS DEL DR.ESTEVE, S.A

Patent: WO2007/9693 A1, 2007 ; Title/Abstract Full Text Show Details

neuropathic pain disorders

LABORATORIOS DEL DR.ESTEVE, S.A

Patent: WO2007/9693 A1, 2007 ; Title/Abstract Full Text Show Details

gastric ulcers

LABORATORIOS DEL DR.ESTEVE, S.A

Patent: WO2007/9693 A1, 2007 ; Title/Abstract Full Text Show Details

atheriosclerosis

LABORATORIOS DEL DR.ESTEVE, S.A

Patent: WO2007/9693 A1, 2007 ; Title/Abstract Full Text Show Details

liver cirrhosis

LABORATORIOS DEL DR.ESTEVE, S.A

Patent: WO2007/9693 A1, 2007 ; Title/Abstract Full Text Show Details

Acute health problems

LABORATORIOS DEL DR.ESTEVE, S.A

Patent: WO2007/9693 A1, 2007 ; Title/Abstract Full Text Show Details

melanocortin 3 receptor (MC3-R) agonist; (MC4-R) agonist; α-melanocyte stimulating hormone (αMSH) activity enhancer; POMC neuron activity promoter; selective serotonin reuptake inhibitor (SSRI); serotonin 2C agonist; serotonin 1B agonist; agouti-related protein (AgRP) inhibitor; neruopeptide Y (NPY) inhibitor; γ-amino butyric acid (GABA) inhibitor; GABA receptor antagonist; GABA channel antagonist; dopamine agonist; dopamine reuptake inhibitor; norepinephrine agonist

Anti-obesity

OREXIGEN THERAPEUTICS, INC.

Patent: WO2007/16108 A1, 2007 ; Title/Abstract Full Text Show Details

ASTRAZENECA AB; ASTRAZENECA UK LIMITED

Patent: WO2007/10222 A2, 2007 ; Title/Abstract Full Text Show Details

ASTRAZENECA AB; ASTRAZENECA UK LIMITED

Patent: WO2007/39740 A2, 2007 ; Title/Abstract Full Text Show Details

weight loss agent

Schering Corporation

Patent: US2007/66644 A1, 2007 ; Title/Abstract Full Text Show Details

β-adrenergic receptor agonist, preferably β-3 receptor agonist

MELIOR DISCOVERY, INC.

Patent: WO2007/24863 A2, 2007 ; Title/Abstract Full Text Show Details

anti-obesity drug

MELIOR DISCOVERY, INC.

Patent: WO2007/24863 A2, 2007 ;

Title/Abstract Full Text Show Details

selective serotonin reuptalce inhibitor

AMYLIN PHARMACEUTICALS, INC.

Patent: WO2007/55728 A1, 2007 ; Title/Abstract Full Text Show Details

Obesity-related disorder

AMYLIN PHARMACEUTICALS, INC.

Patent: WO2007/55728 A1, 2007 ; Title/Abstract Full Text Show Details

Insulin-resistance syndrome

AMYLIN PHARMACEUTICALS, INC.

Patent: WO2007/55728 A1, 2007 ; Title/Abstract Full Text Show Details

AMYLIN PHARMACEUTICALS, INC.

Patent: WO2007/55743 A2, 2007 ; Title/Abstract Full Text Show Details

Lipodystrophy

AMYLIN PHARMACEUTICALS, INC.

Patent: WO2007/55728 A1, 2007 ; Title/Abstract Full Text Show Details

AMYLIN PHARMACEUTICALS, INC.

Patent: WO2007/55743 A2, 2007 ; Title/Abstract Full Text Show Details

Nonalcoholic steatohepatitis

AMYLIN PHARMACEUTICALS, INC.

Patent: WO2007/55728 A1, 2007 ; Title/Abstract Full Text Show Details

Cardiovascular disease

AMYLIN PHARMACEUTICALS, INC.

Patent: WO2007/55728 A1, 2007 ; Title/Abstract Full Text Show Details

AMYLIN PHARMACEUTICALS, INC.

Patent: WO2007/55743 A2, 2007 ; Title/Abstract Full Text Show Details

Obesity related disorders

AMYLIN PHARMACEUTICALS, INC.

Patent: WO2007/55743 A2, 2007 ; Title/Abstract Full Text Show Details

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Nonalcoholic steatohepatitis (NASH)

AMYLIN PHARMACEUTICALS, INC.

Patent: WO2007/55743 A2, 2007 ; Title/Abstract Full Text Show Details

Desire to lose body weight

AMYLIN PHARMACEUTICALS, INC.

Patent: WO2007/55743 A2, 2007 ; Title/Abstract Full Text Show Details

Metabolic conditions

AMYLIN PHARMACEUTICALS, INC.

Patent: WO2007/55743 A2, 2007 ; Title/Abstract Full Text Show Details

Type 2 dependent diabetes

AMYLIN PHARMACEUTICALS, INC.

Patent: WO2007/55743 A2,

2007 ; Title/Abstract Full Text Show Details

Non-insulin dependent diabetes

AMYLIN PHARMACEUTICALS, INC.

Patent: WO2007/55743 A2, 2007 ; Title/Abstract Full Text Show Details

gestational diabetes

AMYLIN PHARMACEUTICALS, INC.

Patent: WO2007/55743 A2, 2007 ; Title/Abstract Full Text Show Details

Eating disorders

AMYLIN PHARMACEUTICALS, INC.

Patent: WO2007/55743 A2, 2007 ; Title/Abstract Full Text Show Details

Therapeutic agent

Mallinckrodt Inc.

Patent: US2007/129444 A1, 2007 ; Title/Abstract Full Text Show Details

Diabetes

Essentialis, Inc.

Patent: US2006/51418 A1, 2006 ; Title/Abstract Full Text Show Details

AMYLIN PHARMACEUTICALS, INC.

Patent: WO2007/55728 A1, 2007 ; Title/Abstract Full Text Show Details

AMYLIN PHARMACEUTICALS, INC.

Patent: WO2007/55743 A2, 2007 ; Title/Abstract Full Text Show Details

Hypertension

Essentialis, Inc.

Patent: US2006/51418 A1, 2006 ; Title/Abstract Full Text Show Details

LABORATORIOS DEL DR.ESTEVE, S.A

Patent: WO2007/9693 A1, 2007 ; Title/Abstract Full Text Show Details

Metabolic syndrome

Essentialis, Inc.

Patent: US2006/51418 A1, 2006 ; Title/Abstract Full Text Show Details

AMYLIN PHARMACEUTICALS, INC.

Patent: WO2007/55728 A1, 2007 ;

Title/Abstract Full Text Show Details

AMYLIN PHARMACEUTICALS, INC.

Patent: WO2007/55743 A2, 2007 ; Title/Abstract Full Text Show Details

Polycystic ovary syndrome

Essentialis, Inc.

Patent: US2006/51418 A1, 2006 ; Title/Abstract Full Text Show Details

AMYLIN PHARMACEUTICALS, INC.

Patent: WO2007/55728 A1, 2007 ; Title/Abstract Full Text Show Details

AMYLIN PHARMACEUTICALS, INC.

Patent: WO2007/55743 A2, 2007 ; Title/Abstract Full Text Show Details

Type 1 diabetes

Essentialis, Inc.

Patent: US2006/51418 A1, 2006 ; Title/Abstract Full Text Show Details

AMYLIN PHARMACEUTICALS, INC.

Patent: WO2007/55743 A2, 2007 ; Title/Abstract Full Text Show Details

vomiting

Essentialis, Inc.

Patent: US2006/51418 A1, 2006 ; Title/Abstract Full Text Show Details

LABORATORIOS DEL DR.ESTEVE, S.A

Patent: WO2007/9693 A1, 2007 ; Title/Abstract Full Text Show Details

Appetite regulating agent

IRM LLC

Patent: WO2007/89557 A2, 2007 ; Title/Abstract Full Text Show Details

IRM LLC

Patent: WO2007/89667 A1, 2007 ; Title/Abstract Full Text Show Details

bipolar disorders

OREXIGEN THERAPEUTICS, INC.

Patent: WO2006/17504 A1, 2006 ; Title/Abstract Full Text Show Details

LABORATORIOS DEL DR.ESTEVE, S.A

Patent: WO2007/9693 A1, 2007 ;

Title/Abstract Full Text Show Details

appetite suppresant; antiobesity agent

GELESIS, INC.

Patent: WO2007/112436 A2, 2007 ; Title/Abstract Full Text Show Details

enhancing gastric retention

GELESIS, INC.

Patent: WO2007/112436 A2, 2007 ; Title/Abstract Full Text Show Details

controlled drug delivery

GELESIS, INC.

Patent: WO2007/112436 A2, 2007 ; Title/Abstract Full Text Show Details

inducing weight loss

GELESIS, INC.

Patent: WO2007/112436 A2, 2007 ; Title/Abstract Full Text Show Details

gastrointestinal disorders

GELESIS, INC.

Patent: WO2007/112436 A2, 2007 ; Title/Abstract Full Text Show Details

Obesity

NOVARTIS AG; NOVARTIS PHARMA GMBH

Patent: WO2005/49088 A2, 2005 ; Title/Abstract Full Text Show Details

Essentialis, Inc.

Patent: US2006/51418 A1, 2006 ; Title/Abstract Full Text Show Details

LABORATORIOS DEL DR.ESTEVE, S.A

Patent: WO2007/9693 A1, 2007 ; Title/Abstract Full Text Show Details

AMYLIN PHARMACEUTICALS, INC.

Patent: WO2007/55743 A2, 2007 ; Title/Abstract Full Text Show Details

ASTRAZENECA AB; ASTRAZENECA UK LIMITED

Patent: WO2005/95354 A1, 2005 ; Title/Abstract Full Text Show Details

anti-obesity compound

Page/Page column 26

ASTRAZENECA AB

Patent: WO2007/18460 A1, 2007 ; Title/Abstract Full Text Show Details

Anorectic agent

Page/Page

KARO BIO AB

column 13

Patent: WO2007/39125 A2, 2007 ; Title/Abstract Full Text Show Details

Anti-obesity drug

Page/Page column 31

NOVARTIS AG; NOVARTIS PHARMA GmbH

Patent: WO2007/67613 A1, 2007 ; Title/Abstract Full Text Show Details

Anti-obesity agent

Page/Page column 36

NOVARTIS AG; NOVARTIS PHARMA GmbH

Patent: WO2007/67615 A2, 2007 ; Title/Abstract Full Text Show Details

Syndrome X

NOVARTIS AG; NOVARTIS PHARMA GMBH

Patent: WO2005/49088 A2, 2005 ; Title/Abstract Full Text Show Details

Essentialis, Inc.

Patent: US2006/51418 A1, 2006 ; Title/Abstract Full Text Show Details

Stroke

NOVARTIS AG; NOVARTIS PHARMA GMBH

Patent: WO2005/49088 A2, 2005 ; Title/Abstract Full Text Show Details

Essentialis, Inc.

Patent: US2006/51418 A1, 2006 ; Title/Abstract Full Text Show Details

Hyperlipidemia

NOVARTIS AG; NOVARTIS PHARMA GMBH

Patent: WO2005/49088 A2, 2005 ; Title/Abstract Full Text Show Details

Essentialis, Inc.

Patent: US2006/51418 A1, 2006 ; Title/Abstract Full Text Show Details

A component of composition for treatment of obesity or an obesity-related condition

Yancopoulos, George D.; Wiegand, Stanley J.; Sleeman, Mark W.; KoehlerStec, Ellen-Marie

Patent: US2006/58224 A1, 2006 ; Title/Abstract Full Text Show Details

reduction in body weight

Yancopoulos, George D.; Wiegand, Stanley J.; Sleeman, Mark W.; KoehlerStec, Ellen-Marie

Patent: US2006/58224 A1, 2006 ; Title/Abstract Full Text

Show Details

improvement in diabetic parameters

Yancopoulos, George D.; Wiegand, Stanley J.; Sleeman, Mark W.; KoehlerStec, Ellen-Marie

Patent: US2006/58224 A1, 2006 ; Title/Abstract Full Text Show Details

liver steatosis

Yancopoulos, George D.; Wiegand, Stanley J.; Sleeman, Mark W.; KoehlerStec, Ellen-Marie

Patent: US2006/58224 A1, 2006 ; Title/Abstract Full Text Show Details

fasting glucose and insulin levels

Yancopoulos, George D.; Wiegand, Stanley J.; Sleeman, Mark W.; KoehlerStec, Ellen-Marie

Patent: US2006/58224 A1, 2006 ; Title/Abstract Full Text Show Details

oral glucose tolerance, triglycerides and non-esterified free-fatty acids

Yancopoulos, George D.; Wiegand, Stanley J.; Sleeman, Mark W.; KoehlerStec, Ellen-Marie

Patent: US2006/58224 A1, 2006 ; Title/Abstract Full Text Show Details

type II diabetes

Yancopoulos, George D.; Wiegand, Stanley J.; Sleeman, Mark W.; KoehlerStec, Ellen-Marie

Patent: US2006/58224 A1, 2006 ; Title/Abstract Full Text Show Details

therapeutic agent

Yancopoulos, George D.; Wiegand, Stanley J.; Sleeman, Mark W.; KoehlerStec, Ellen-Marie

Patent: US2006/58224 A1, 2006 ; Title/Abstract Full Text Show Details

vasoconstricting agent

Higuchi, John; Li, S. Kevin; Higuchi, William I.; Hastings, Matthew S.

Patent: US2006/88515 A1, 2006 ; Title/Abstract Full Text Show Details

sympathomimetic

Higuchi, John; Li, S. Kevin; Higuchi, William I.; Hastings, Matthew S.

Patent: US2006/88515 A1, 2006 ; Title/Abstract Full Text Show Details

Anti-obezity agent

Meng, Wei; Hamann,

Lawrence G.; Brigance, Robert

Patent: US2006/142576 A1, 2006 ;

Title/Abstract Full Text Show Details

stimulant

Kirk, Randal J.

Patent: US2006/100136 A1, 2006 ; Title/Abstract Full Text Show Details

Anti-diabetic agent

JOHN I. HASS, INC.

Patent: WO2006/55985 A1, 2006 ; Title/Abstract Full Text Show Details

sympathomimetic agent of controlled-release pharmaceutical composition which is capable of delivering therapeutic amounts of active agent to specific region of gastrointestinal tract

Elan Corporation, plc

Patent: US2006/121112 A1, 2006 ; Title/Abstract Full Text Show Details

in combination with topiramate

Elan Corporation, plc

Patent: US2006/121112 A1, 2006 ; Title/Abstract Full Text Show Details

partial seizures with or without secondarily generalized seizures

Elan Corporation, plc

Patent: US2006/121112 A1, 2006 ; Title/Abstract Full Text Show Details

primary generalized tonic-clonic seizures

Elan Corporation, plc

Patent: US2006/121112 A1, 2006 ; Title/Abstract Full Text Show Details

seizures associated with Lennox Gastaut Syndrome

Elan Corporation, plc

Patent: US2006/121112 A1, 2006 ; Title/Abstract Full Text Show Details

migraines

Elan Corporation, plc

Patent: US2006/121112 A1, 2006 ; Title/Abstract Full Text Show Details

potassium ATP (KATP) channel opener; inhibition of fasting insulin secretion; inhibition of stimulated insulin secretion; elevation of energy expenditure; elevation of beta oxidation of fat; Reduced glyceraldehyde phosphate dehydrogenase activity of adipocytes; Reduced expression of fatty acid synthase by adipocytes; Enhanced lipolysis by adipocytes; Reduced production of lipoprotein lipase by adipocytes; enhanced expression of β3 Adrenergic Receptor (β3AR)

Disease involving KATP channels

Essentialis, Inc.

Patent: US2006/51418 A1, 2006 ; Title/Abstract Full Text Show Details

Essentialis, Inc.

Patent: US2006/51418 A1, 2006 ; Title/Abstract Full Text Show Details

Hyperphagia

Essentialis, Inc.

Patent: US2006/51418 A1,

2006 ; Title/Abstract Full Text Show Details

Hypoglycemia

Essentialis, Inc.

Patent: US2006/51418 A1, 2006 ; Title/Abstract Full Text Show Details

Obesity associated co-morbidities

Essentialis, Inc.

Patent: US2006/51418 A1, 2006 ; Title/Abstract Full Text Show Details

weight loss

Essentialis, Inc.

Patent: US2006/51418 A1, 2006 ; Title/Abstract Full Text Show Details

Reducing visceral fat

Essentialis, Inc.

Patent: US2006/51418 A1, 2006 ; Title/Abstract Full Text Show Details

Restore normal glucose tolerance

Essentialis, Inc.

Patent: US2006/51418 A1, 2006 ; Title/Abstract Full Text Show Details

weight gain

Essentialis, Inc.

Patent: US2006/51418 A1, 2006 ; Title/Abstract Full Text Show Details

Impaired glucose tolerance

Essentialis, Inc.

Patent: US2006/51418 A1, 2006 ; Title/Abstract Full Text Show Details

Dyslipidemia associated with the use of the anti-psychotics

Essentialis, Inc.

Patent: US2006/51418 A1, 2006 ; Title/Abstract Full Text Show Details

Prader-Willi Syndrome

Essentialis, Inc.

Patent: US2006/51418 A1, 2006 ; Title/Abstract Full Text Show Details

Froelich's Syndrome

Essentialis, Inc.

Patent: US2006/51418 A1, 2006 ; Title/Abstract Full Text Show Details

Cohen Syndrome

Essentialis, Inc.

Patent: US2006/51418 A1, 2006 ; Title/Abstract Full Text

Show Details

Summit Syndrome

Essentialis, Inc.

Patent: US2006/51418 A1, 2006 ; Title/Abstract Full Text Show Details

Alstrom Syndrome

Essentialis, Inc.

Patent: US2006/51418 A1, 2006 ; Title/Abstract Full Text Show Details

Borjeson Syndrome

Essentialis, Inc.

Patent: US2006/51418 A1, 2006 ; Title/Abstract Full Text Show Details

Bardet-Biedl Syndrome

Essentialis, Inc.

Patent: US2006/51418 A1, 2006 ; Title/Abstract Full Text Show Details

Hyperlipoproteinemia type I

Essentialis, Inc.

Patent: US2006/51418 A1, 2006 ; Title/Abstract Full Text Show Details

Hyperlipoproteinemia type II

Essentialis, Inc.

Patent: US2006/51418 A1, 2006 ; Title/Abstract Full Text Show Details

Hyperlipoproteinemia type III

Essentialis, Inc.

Patent: US2006/51418 A1, 2006 ; Title/Abstract Full Text Show Details

Hyperlipoproteinemia type IV

Essentialis, Inc.

Patent: US2006/51418 A1, 2006 ; Title/Abstract Full Text Show Details

Reducing the incidence of adverse effects

Essentialis, Inc.

Patent: US2006/51418 A1, 2006 ; Title/Abstract Full Text Show Details

Prediabetes

Essentialis, Inc.

Patent: US2006/51418 A1, 2006 ; Title/Abstract Full Text Show Details

Type 2 diabetes

Essentialis, Inc.

Patent: US2006/51418 A1, 2006 ; Title/Abstract Full Text Show Details

Osteoarthritis

Essentialis, Inc.

Patent: US2006/51418 A1, 2006 ; Title/Abstract Full Text Show Details

Cardiovascular condition

Essentialis, Inc.

Patent: US2006/51418 A1, 2006 ; Title/Abstract Full Text Show Details

Metabolic disease

Essentialis, Inc.

Patent: US2006/51418 A1, 2006 ; Title/Abstract Full Text Show Details

Hyperinsulemia

Essentialis, Inc.

Patent: US2006/51418 A1, 2006 ; Title/Abstract Full Text Show Details

Hyperinsulinism

Essentialis, Inc.

Patent: US2006/51418 A1, 2006 ; Title/Abstract Full Text Show Details

Preservation of pancreatic function in type 1 diabetics

Essentialis, Inc.

Patent: US2006/51418 A1, 2006 ; Title/Abstract Full Text Show Details

Prevention of the transition from prediabetes to diabetes

Essentialis, Inc.

Patent: US2006/51418 A1, 2006 ; Title/Abstract Full Text Show Details

Correction of the defects in insulin secretion contributing to prediabetes

Essentialis, Inc.

Patent: US2006/51418 A1, 2006 ; Title/Abstract Full Text Show Details

Correction of the defects in insulin secretion contributing to type II diabetes

Essentialis, Inc.

Patent: US2006/51418 A1, 2006 ; Title/Abstract Full Text Show Details

Correction of the defects in insulin sensitivity contributing to prediabetes

Essentialis, Inc.

Patent: US2006/51418 A1, 2006 ; Title/Abstract Full Text Show Details

Correction of the defects in insulin sensitivity contributing to type II diabetes

Essentialis, Inc.

Patent: US2006/51418 A1, 2006 ; Title/Abstract Full Text Show Details

Ischemic injury

Essentialis, Inc.

Patent: US2006/51418 A1, 2006 ;

Title/Abstract Full Text Show Details

Reperfusion injury

Essentialis, Inc.

Patent: US2006/51418 A1, 2006 ; Title/Abstract Full Text Show Details

Provide beta cell rest

Essentialis, Inc.

Patent: US2006/51418 A1, 2006 ; Title/Abstract Full Text Show Details

Beta cell failure

Essentialis, Inc.

Patent: US2006/51418 A1, 2006 ; Title/Abstract Full Text Show Details

Improved glycemic control

Essentialis, Inc.

Patent: US2006/51418 A1, 2006 ; Title/Abstract Full Text Show Details

Reduction in blood pressure

Essentialis, Inc.

Patent: US2006/51418 A1, 2006 ; Title/Abstract Full Text Show Details

Myocardial infarct

Essentialis, Inc.

Patent: US2006/51418 A1, 2006 ; Title/Abstract Full Text Show Details

Edema

Essentialis, Inc.

Patent: US2006/51418 A1, 2006 ; Title/Abstract Full Text Show Details

Fluid retention

Essentialis, Inc.

Patent: US2006/51418 A1, 2006 ; Title/Abstract Full Text Show Details

Reduced rates of excretion of sodium

Essentialis, Inc.

Patent: US2006/51418 A1, 2006 ; Title/Abstract Full Text Show Details

Reduced rates of excretion of chloride

Essentialis, Inc.

Patent: US2006/51418 A1, 2006 ; Title/Abstract Full Text Show Details

Reduced rates of excretion of uric acid

Essentialis, Inc.

Patent: US2006/51418 A1, 2006 ; Title/Abstract Full Text Show Details

ketoacidosis

Essentialis, Inc.

Patent: US2006/51418 A1, 2006 ; Title/Abstract Full Text Show Details

Nausea

Essentialis, Inc.

Patent: US2006/51418 A1, 2006 ; Title/Abstract Full Text Show Details

Dyspepsia

Essentialis, Inc.

Patent: US2006/51418 A1, 2006 ; Title/Abstract Full Text Show Details

Ileus

Essentialis, Inc.

Patent: US2006/51418 A1, 2006 ; Title/Abstract Full Text Show Details

Headaches

Essentialis, Inc.

Patent: US2006/51418 A1, 2006 ; Title/Abstract Full Text Show Details

compositions for affecting weight loss

OREXIGEN THERAPEUTICS, INC.

Patent: WO2006/17504 A1, 2006 ; Title/Abstract Full Text Show Details

increasing energy expenditure

OREXIGEN THERAPEUTICS, INC.

Patent: WO2006/17504 A1, 2006 ; Title/Abstract Full Text Show Details

increasing satiety

OREXIGEN THERAPEUTICS, INC.

Patent: WO2006/17504 A1, 2006 ; Title/Abstract Full Text Show Details

suppressing the appetite of an individual

OREXIGEN THERAPEUTICS, INC.

Patent: WO2006/17504 A1, 2006 ; Title/Abstract Full Text Show Details

Composition for the treating, preventing, or ameliorating one or more symptoms of a protein tyrosine phosphatase mediated disease

Page/Page column 53; 96

CENGENT THERAPEUTICS, INC.

Patent: WO2006/28970 A1, 2006 ; Title/Abstract Full Text Show Details

Anti-obesity agent

Page/Page column 30

PFIZER PRODUCTS INC.

Patent: WO2006/33001 A1, 2006 ;

Title/Abstract Full Text Show Details

modulating central norepinephrine and dopamine receptors through the promotion of catecholamine release

PFIZER PRODUCTS INC.

Patent: WO2005/61506 A1, 2005 ; Title/Abstract Full Text Show Details

PFIZER PRODUCTS INC.

Patent: WO2005/61507 A1, 2005 ; Title/Abstract Full Text Show Details

Adrenergic agent

PFIZER PRODUCTS INC.

Patent: WO2005/61506 A1, 2005 ; Title/Abstract Full Text Show Details

PFIZER PRODUCTS INC.

Patent: WO2005/61507 A1, 2005 ; Title/Abstract Full Text Show Details

Type 2 diabetes mellitus

NOVARTIS AG; NOVARTIS PHARMA GMBH

Patent: WO2005/49088 A2, 2005 ; Title/Abstract Full Text Show Details

Hypertension including hypertension in the elderly

NOVARTIS AG; NOVARTIS PHARMA GMBH

Patent: WO2005/49088 A2, 2005 ; Title/Abstract Full Text Show Details

Familial dyslipidemic hypertension

NOVARTIS AG; NOVARTIS PHARMA GMBH

Patent: WO2005/49088 A2, 2005 ; Title/Abstract Full Text Show Details

Isolated systolic hypertension(ISH)

NOVARTIS AG; NOVARTIS PHARMA GMBH

Patent: WO2005/49088 A2, 2005 ; Title/Abstract Full Text Show Details

Increased collagen formation

NOVARTIS AG; NOVARTIS PHARMA GMBH

Patent: WO2005/49088 A2, 2005 ; Title/Abstract Full Text Show Details

Fibrosis

NOVARTIS AG; NOVARTIS PHARMA GMBH

Patent: WO2005/49088 A2, 2005 ; Title/Abstract Full Text Show Details

Remodeling following hypertension

NOVARTIS AG; NOVARTIS PHARMA GMBH

Patent: WO2005/49088 A2, 2005 ;

Title/Abstract Full Text Show Details

Erectile dysfunction

NOVARTIS AG; NOVARTIS PHARMA GMBH

Patent: WO2005/49088 A2, 2005 ; Title/Abstract Full Text Show Details

Impaired vascular compliance

NOVARTIS AG; NOVARTIS PHARMA GMBH

Patent: WO2005/49088 A2, 2005 ; Title/Abstract Full Text Show Details

Congestive heart failure

NOVARTIS AG; NOVARTIS PHARMA GMBH

Patent: WO2005/49088 A2, 2005 ; Title/Abstract Full Text Show Details

Left ventricular hypertrophy

NOVARTIS AG; NOVARTIS PHARMA GMBH

Patent: WO2005/49088 A2, 2005 ; Title/Abstract Full Text Show Details

Survival post myocardial infarction(MI)

NOVARTIS AG; NOVARTIS PHARMA GMBH

Patent: WO2005/49088 A2, 2005 ; Title/Abstract Full Text Show Details

Coronary artery diseases

NOVARTIS AG; NOVARTIS PHARMA GMBH

Patent: WO2005/49088 A2, 2005 ; Title/Abstract Full Text Show Details

Atherosclerosis

NOVARTIS AG; NOVARTIS PHARMA GMBH

Patent: WO2005/49088 A2, 2005 ; Title/Abstract Full Text Show Details

Angina pectoris

NOVARTIS AG; NOVARTIS PHARMA GMBH

Patent: WO2005/49088 A2, 2005 ; Title/Abstract Full Text Show Details

Thrombosis

NOVARTIS AG; NOVARTIS PHARMA GMBH

Patent: WO2005/49088 A2, 2005 ; Title/Abstract Full Text Show Details

Renal failure

NOVARTIS AG; NOVARTIS PHARMA GMBH

Patent: WO2005/49088 A2, 2005 ;

Title/Abstract Full Text Show Details

Chronic renal failure

NOVARTIS AG; NOVARTIS PHARMA GMBH

Patent: WO2005/49088 A2, 2005 ; Title/Abstract Full Text Show Details

Glomerulosclerosis

NOVARTIS AG; NOVARTIS PHARMA GMBH

Patent: WO2005/49088 A2, 2005 ; Title/Abstract Full Text Show Details

Nephropathy

NOVARTIS AG; NOVARTIS PHARMA GMBH

Patent: WO2005/49088 A2, 2005 ; Title/Abstract Full Text Show Details

Hypothyroidism

NOVARTIS AG; NOVARTIS PHARMA GMBH

Patent: WO2005/49088 A2, 2005 ; Title/Abstract Full Text Show Details

Endothelial dysfunction with or without hypertension

NOVARTIS AG; NOVARTIS PHARMA GMBH

Patent: WO2005/49088 A2, 2005 ; Title/Abstract Full Text Show Details

Hyperlipoproteinemia

NOVARTIS AG; NOVARTIS PHARMA GMBH

Patent: WO2005/49088 A2, 2005 ; Title/Abstract Full Text Show Details

Hypertryglyceridemia

NOVARTIS AG; NOVARTIS PHARMA GMBH

Patent: WO2005/49088 A2, 2005 ; Title/Abstract Full Text Show Details

Hypercholesterolemia

NOVARTIS AG; NOVARTIS PHARMA GMBH

Patent: WO2005/49088 A2, 2005 ; Title/Abstract Full Text Show Details

Macular degeneration

NOVARTIS AG; NOVARTIS PHARMA GMBH

Patent: WO2005/49088 A2, 2005 ; Title/Abstract Full Text Show Details

Cataract

NOVARTIS AG; NOVARTIS PHARMA GMBH

Patent: WO2005/49088 A2, 2005 ;

Title/Abstract Full Text Show Details

Glaucoma

NOVARTIS AG; NOVARTIS PHARMA GMBH

Patent: WO2005/49088 A2, 2005 ; Title/Abstract Full Text Show Details

Skin and connective tissue disorders

NOVARTIS AG; NOVARTIS PHARMA GMBH

Patent: WO2005/49088 A2, 2005 ; Title/Abstract Full Text Show Details

Restenosis after percutaneous transluminal angioplasty

NOVARTIS AG; NOVARTIS PHARMA GMBH

Patent: WO2005/49088 A2, 2005 ; Title/Abstract Full Text Show Details

Restenosis after coronary artery bypass surgery

NOVARTIS AG; NOVARTIS PHARMA GMBH

Patent: WO2005/49088 A2, 2005 ; Title/Abstract Full Text Show Details

Peripheral vascular disease

NOVARTIS AG; NOVARTIS PHARMA GMBH

Patent: WO2005/49088 A2, 2005 ; Title/Abstract Full Text Show Details

Reproductive disorders

NOVARTIS AG; NOVARTIS PHARMA GMBH

Patent: WO2005/49088 A2, 2005 ; Title/Abstract Full Text Show Details

Pulmonary disease

NOVARTIS AG; NOVARTIS PHARMA GMBH

Patent: WO2005/49088 A2, 2005 ; Title/Abstract Full Text Show Details

Gallstones

NOVARTIS AG; NOVARTIS PHARMA GMBH

Patent: WO2005/49088 A2, 2005 ; Title/Abstract Full Text Show Details

Fasting-inducedcholecystitis

NOVARTIS AG; NOVARTIS PHARMA GMBH

Patent: WO2005/49088 A2, 2005 ; Title/Abstract Full Text Show Details

Cancers

NOVARTIS AG; NOVARTIS PHARMA GMBH

Patent: WO2005/49088 A2, 2005 ;

Title/Abstract Full Text Show Details

Cutaneous disease

NOVARTIS AG; NOVARTIS PHARMA GMBH

Patent: WO2005/49088 A2, 2005 ; Title/Abstract Full Text Show Details

Cushing's syndrome

NOVARTIS AG; NOVARTIS PHARMA GMBH

Patent: WO2005/49088 A2, 2005 ; Title/Abstract Full Text Show Details

Insulinoma

NOVARTIS AG; NOVARTIS PHARMA GMBH

Patent: WO2005/49088 A2, 2005 ; Title/Abstract Full Text Show Details

Craniopharyngioma

NOVARTIS AG; NOVARTIS PHARMA GMBH

Patent: WO2005/49088 A2, 2005 ; Title/Abstract Full Text Show Details

Premenstrual syndrome

NOVARTIS AG; NOVARTIS PHARMA GMBH

Patent: WO2005/49088 A2, 2005 ; Title/Abstract Full Text Show Details

anorectic

Boehringer Ingelheim International GmbH

Patent: US2005/245500 A1, 2005 ; Title/Abstract Full Text Show Details

appetite suppressant

BLM Group, Inc.

Patent: US2005/222040 A1, 2005 ; Title/Abstract Full Text Show Details

weight loss promotor

BLM Group, Inc.

Patent: US2005/222040 A1, 2005 ; Title/Abstract Full Text Show Details

noradrenergic agent

BLM Group, Inc.

Patent: US2005/222040 A1, 2005 ; Title/Abstract Full Text Show Details

pharmaceutical composition

BLM Group, Inc.

Patent: US2005/222040 A1, 2005 ; Title/Abstract Full Text Show Details

combination therapy

BLM Group, Inc.

Patent: US2005/222040 A1, 2005 ;

Title/Abstract Full Text Show Details

Appetite-regulating agent

IRM LLC

Patent: WO2005/113506 A1, 2005 ; Title/Abstract Full Text Show Details

IRM LLC

Patent: WO2005/113519 A1, 2005 ; Title/Abstract Full Text Show Details

Anorectic agent

MERCK and CO., INC.

Patent: WO2003/87037 A1, 2003 ; Title/Abstract Full Text Show Details

Isolation from Natural Product (1) Isolation from Natural Product

Reference

Rabbit liver

Beckett; Belanger

Journal of Pharmacy and Pharmacology, 1975 , vol. 27, # 12 p. 928 - 936 Title/Abstract Full Text View citing articles Show Details

Chemical Name: phentermine hydrochloride Reaxys Registry Number: 3912379

CAS Registry Number: 1197-21-3 Type of Substance: isocyclic Molecular Formula: C10H16N*Cl Linear Structure Formula: C6H5CH2C(CH3)2NH3(1+)*Cl(1-

2

12 prep out of 46 reactions.

Identification Physical Data (12) Spectra (8) Bioactivity (21) Other Data (1)

65

)=C H CH C(CH )2NH Cl 6 5 2 3 3

Molecular Weight: 185.697 InChI Key: NCAIGTHBQTXTLR-UHFFFAOYSA-N

Synthesize | Hide Details Find similar Chemical Names and Synonyms phentermine hydrochloride, α,α-dimethylphenethylamine hydrochloride, Phentermine hydrochloride, 1,1-dimethyl-2-phenylethylamine HCl, phentermine HCl, α,α-dimethylphenethylamine hydrochloride, 1,1-dimethyl-2-phenyl-ethylamine hydrochloride Identification Substance Label (7) Label

Reference

Intermediate 75

GLAXOSMITHKLINE LLC; AXTEN, Jeffrey, Michael; BLACKLEDGE, Charles, William; BRADY, Gerald, Patrick; FENG, Yanhoug, G.; GRANT, Seth, W.; MEDINA, Jesus, Rahul; MILLER, William, H.; ROMERIL, Stuart, P.

Patent: WO2010/59658 A1, 2010 ; Title/Abstract Full Text Show Details

Phent

Li, Su-Min; Campbell, Bettye L.; Katz, Jonathan L.

Journal of Pharmacology and Experimental Therapeutics, 2006 , vol. 317, # 3 p. 1088 - 1096 Title/Abstract Full Text View citing articles Show Details

14

Shao, Ning; Wang, Cheng; Huang, Xianhai; Xiao, Dong; Palani, Anandan; Aslanian, Robert; Shih, Neng-Yang

Tetrahedron Letters, 2006 , vol. 47, # 38 p. 6743 - 6746 Title/Abstract Full Text View citing articles Show Details

phen

Zolkowska, Dorota; Rothman, Richard B.; Baumann, Michael H.

Journal of Pharmacology and Experimental Therapeutics, 2006 , vol. 318, # 2 p. 604 - 610 Title/Abstract Full Text View citing articles Show Details

13

Katritzky, Alan R.; Cui, Xilin; Long, Qiuhe; Yang, Baozhen; Wilcox, Allan L.; Zhang, Yong-Kang

Organic Preparations and Procedures International, 2000 , vol. 32, # 2 p. 175 - 183 Title/Abstract Full Text View citing articles Show Details

3d

Jirgensons; Kauss; Kalvinsh; Gold

Synthesis, 2000 , # 12 p. 1709 - 1712 Title/Abstract Full Text View citing articles Show Details

2e

Gajda; Koziara; Napieraj; Sikora; Zwierzak

Polish Journal of Chemistry, 2000 , vol. 74, # 10 p. 1385 - 1387 Title/Abstract Full Text View citing articles Show Details

Patent-Specific Data (3)

Related Markush Structure (RN)

Location in Patent

Reference

Page/Page column

King, Clifford Riley; Bristol, David W.; English, Michael L.

Patent: US2014/178480 A1, 2014 ; Title/Abstract Full Text Show Details

Claim

Louisiana State University Medical Center Foundation

Patent: US5795880 A1, 1998 ; Title/Abstract Full Text Show Details

General Mills, Inc.

Patent: US2002/44968 A1, 2002 ; Title/Abstract Full Text Show Details

The Procter and Gamble Company

Patent: US5614178 A1, 1997 ; Title/Abstract Full Text Show Details

19814331

G.D. Searle and Co.

Patent: US6337398 B1, 2002 ;

Title/Abstract Full Text Show Details

Physical Data Melting Point (5) Melting Point

Solvent (Melting Point)

Comment (Melting Point)

Reference

196 - 200 °C

Jirgensons; Kauss; Kalvinsh; Gold

Synthesis, 2000 , # 12 p. 1709 - 1712 Title/Abstract Full Text View citing articles Show Details

200 - 202 °C

Dube, Michael F.; Timberlake, Jack W.

Tetrahedron, 1980 , vol. 36, p. 1753 - 1756 Title/Abstract Full Text View citing articles Show Details

203 °C

Decomposition.

Girault-Vexlearschi

Bulletin de la Societe Chimique de France, 1956 , p. 589,596 Full Text Show Details

199 - 200 °C

propan-2-ol diisopropyl ether

Zenitz; Macks; Moore

Journal of the American Chemical Society, 1948 , vol. 70, p. 955 Full Text View citing articles Show Details

198 - 198.5 °C

Ritter; Kalish

Journal of the American Chemical Society, 1948 , vol. 70, p. 4048 Organic Syntheses, 1964 , vol. 44, p. 44,45 Full Text View citing articles Show Details

Crystal Phase (1) Description (Crystal Phase)

Reference

Crystal habit

Jordan

Journal of Pharmaceutical Sciences, 1993 , vol. 82, # 12 p. 1269 - 1271 Title/Abstract Full Text View citing articles Show Details

Crystal Property Description (3)

Colour & Other Properties white

white

white

Location

Reference

Page/Page column 158

GLAXOSMITHKLINE LLC; AXTEN, Jeffrey, Michael; BLACKLEDGE, Charles, William; BRADY, Gerald, Patrick; FENG, Yanhoug, G.; GRANT, Seth, W.; MEDINA, Jesus, Rahul; MILLER, William, H.; ROMERIL, Stuart, P.

Patent: WO2010/59658 A1, 2010 ;

Page/Page column 115

GLAXOSMITHKLINE LLC; AXTEN, Jeffrey, Michael; BRADY, Gerald, Patrick, Jr.; GALLAGHER, Timothy, Francis; HEERDING, Dirk, A.; MEDINA, Jesus, Raul; ROMERIL, Stuart, Paul

Patent: WO2010/120854 A1, 2010 ;

Page/Page column 16

Andersen, Denise Lyn; Chang, Catherine H.; Falsey, James R.; Frohn, Michael J.; Hong, Fang-Tsao; Liao, Hongyu; Liu, Longbin; Lopez, Patricia; Retz, Daniel Martin; Rishton, Gilbert M.; Rzasa, Robert M.; Siegmund, Aaron; Tadesse, Seifu; Tamayo, Nuria; Tegley, Christopher M.

Patent: US2006/69110 A1, 2006 ;

Title/Abstract Full Text Show Details

Title/Abstract Full Text Show Details

Title/Abstract Full Text Show Details

Optics (2) Description (Optics)

Reference

Crystal refractive indices

Jordan

Journal of Pharmaceutical Sciences, 1993 , vol. 82, # 12 p. 1269 - 1271 Title/Abstract Full Text View citing articles Show Details

Natural birefringence

Jordan

Journal of Pharmaceutical Sciences, 1993 , vol. 82, # 12 p. 1269 - 1271 Title/Abstract Full Text View citing articles Show Details

Solubility (MCS) (1) Location

Comment (Solubility (MCS))

Reference

Paragraph 0212-0218

phentermine hydrochloride was completely soluble at pH 4.5 and pH 7.0

King, Clifford Riley; Bristol, David W.; English, Michael L.

Patent: US2014/178480 A1, 2014 ; Title/Abstract Full Text Show Details

Spectra NMR Spectroscopy (4) Description (NMR Spectroscopy)

Nucleus (NMR Spectroscopy)

Solvents (NMR Spectroscopy)

Frequency (NMR Spectroscopy)

Chemical shifts

1H

CDCl3

200 MHz

Jirgensons; Kauss; Kalvinsh; Gold

Synthesis, 2000 , # 12 p. 1709 - 1712 Title/Abstract Full Text View citing articles Show Details

Chemical shifts

13C

CDCl3

50 MHz

Jirgensons; Kauss; Kalvinsh; Gold

Synthesis, 2000 , # 12 p. 1709 - 1712 Title/Abstract Full Text View citing articles Show Details

Chemical shifts

1H

D2O

250 MHz

Gajda; Koziara; Napieraj; Sikora; Zwierzak

Polish Journal of Chemistry, 2000 , vol. 74, # 10 p. 1385 - 1387 Title/Abstract Full Text View citing articles Show Details

Chemical shifts

1H

D2O

Koziara, Anna; Osowska-Pacewicka, Krystyna; Zawadzki, Stefan; Zwierzak, Andrzej

Synthesis, 1987 , # 5 p. 487 - 489 Title/Abstract Full Text Show Details

IR Spectroscopy (2)

Reference

Description (IR Spectroscopy)

Solvent (IR Spectroscopy)

Comment (IR Spectroscopy)

Bands

KBr

Gajda; Koziara; Napieraj; Sikora; Zwierzak

Polish Journal of Chemistry, 2000 , vol. 74, # 10 p. 1385 - 1387 Title/Abstract Full Text View citing articles Show Details

Bands

KBr

2960 - 990 cm**(-1)

Koziara, Anna; Osowska-Pacewicka, Krystyna; Zawadzki, Stefan; Zwierzak, Andrzej

Synthesis, 1987 , # 5 p. 487 - 489 Title/Abstract Full Text Show Details

Reference

Mass Spectrometry (2) Description (Mass Spectrometry)

Location

Reference

LCMS (Liquid chromatography mass spectrometry) ESI (Electrospray ionisation)

Page/Page column 158

GLAXOSMITHKLINE LLC; AXTEN, Jeffrey, Michael; BLACKLEDGE, Charles, William; BRADY, Gerald, Patrick; FENG, Yanhoug, G.; GRANT, Seth, W.; MEDINA, Jesus, Rahul; MILLER, William, H.; ROMERIL, Stuart, P.

Patent: WO2010/59658 A1, 2010 ;

LCMS (Liquid chromatography mass spectrometry) ESI (Electrospray ionisation)

Page/Page column 115

Title/Abstract Full Text Show Details

GLAXOSMITHKLINE LLC; AXTEN, Jeffrey, Michael; BRADY, Gerald, Patrick, Jr.; GALLAGHER, Timothy, Francis; HEERDING, Dirk, A.; MEDINA, Jesus, Raul; ROMERIL, Stuart, Paul

Patent: WO2010/120854 A1, 2010 ; Title/Abstract Full Text Show Details

Bioactivity Pharmacological Data (21) 1 of 21

Comment (Pharmacological Data)

Bioactivities present

Reference

Louisiana State University Medical Center Foundation

Patent: US5795880 A1, 1998 ; Title/Abstract Full Text Show Details

General Mills, Inc.

Patent: US2002/44968 A1, 2002 ; Title/Abstract Full Text Show Details

Warner-Lambert Company

Patent: US4018825 A1, 1977 ; Title/Abstract Full Text Show Details

Theravance, Inc.

Patent: US2005/159448 A1, 2005 ; Title/Abstract Full Text Show Details

Beiersdorf

Patent: DE1913199 , 1970 ; Chem.Abstr., 1971 , vol. 74, # 13005 Full Text Show Details

Girault-Vexlearschi

Bulletin de la Societe Chimique de France, 1956 , p. 589,596 Full Text Show Details

Zenitz; Macks; Moore

Journal of the American Chemical Society, 1948 , vol. 70, p. 955 Full Text View citing articles Show Details

Ritter; Kalish

Journal of the American Chemical Society, 1948 , vol. 70, p. 4048 Organic Syntheses, 1964 , vol. 44, p. 44,45 Full Text View citing articles Show Details

Buchowiecki, Wieslaw; Grosman-Zjawiona, Zofia; Zjawiony, Jordan

Tetrahedron Letters, 1985 , vol. 26, # 9 p. 1245 - 1248 Title/Abstract Full Text View citing articles Show Details

Dube, Michael F.; Timberlake, Jack W.

Tetrahedron, 1980 , vol. 36, p. 1753 - 1756 Title/Abstract Full Text View citing articles Show Details

Koziara, Anna; Osowska-Pacewicka, Krystyna; Zawadzki, Stefan; Zwierzak, Andrzej

Synthesis, 1987 , # 5 p. 487 - 489 Title/Abstract Full Text Show Details

Milecki, Jan; Baker, Stephen P.; Standifer, Kelly M.; Ishizu, Takashi; Chida, Yasuhiro; et al.

Journal of Medicinal Chemistry, 1987 , vol. 30, # 9 p. 1563 - 1566 Title/Abstract Full Text View citing articles Show Details

Baldwin, Jack E.; Adlington, Robert M.; Newington, Ian M.

Journal of the Chemical Society, Chemical Communications, 1986 , # 2 p. 176 - 178

Title/Abstract Full Text View citing articles Show Details

Jordan

Journal of Pharmaceutical Sciences, 1993 , vol. 82, # 12 p. 1269 - 1271 Title/Abstract Full Text View citing articles Show Details

Delbeke; Debackere

Arzneimittel-Forschung/Drug Research, 1986 , vol. 36, # 1 p. 134 - 137 Title/Abstract Full Text View citing articles Show Details

McNamara; Dobrusin; Leonard; Shuler; Kaltenbronn; Quin 3rd.; Bur; Thomas; Doherty; Scholten; Zimmerman; Gibbs; Gowan; Latash; Leopold; Przybranowski; Sebolt-Leopold

Journal of medicinal chemistry, 1997 , vol. 40, # 21 p. 3319 - 3322 Title/Abstract Full Text View citing articles Show Details

Watson

Journal of Organic Chemistry, 1998 , vol. 63, # 2 p. 406 - 407 Title/Abstract Full Text View citing articles Show Details

Katritzky, Alan R.; Cui, Xilin; Long, Qiuhe; Yang, Baozhen; Wilcox, Allan L.; Zhang, Yong-Kang

Organic Preparations and Procedures International, 2000 , vol. 32, # 2 p. 175 - 183 Title/Abstract Full Text View citing articles Show Details

Jirgensons; Kauss; Kalvinsh; Gold

Synthesis, 2000 , # 12 p. 1709 - 1712 Title/Abstract Full Text View citing articles Show Details

Gajda; Koziara; Napieraj; Sikora; Zwierzak

Polish Journal of Chemistry, 2000 , vol. 74, # 10 p. 1385 - 1387 Title/Abstract Full Text View citing articles Show Details

2 of 21

Comment (Pharmacological Data)

Bioactivities present

Reference

Nandigama, Ravi K.; Newton-Vinson, Paige; Edmondson, Dale E.

Biochemical Pharmacology, 2002 , vol. 63, # 5 p. 865 - 869 Title/Abstract Full Text View citing articles Show Details

Li, Su-Min; Campbell, Bettye L.; Katz, Jonathan L.

Journal of Pharmacology and Experimental Therapeutics, 2006 , vol. 317, # 3 p. 1088 - 1096 Title/Abstract Full Text View citing articles Show Details

Zhi, Jianguo; Moore, Rema; Kanitra, Linda; Mulligan, Thomas E

Journal of clinical pharmacology, 2002 , vol. 42, # 9 p. 1011 - 1019 Title/Abstract Full Text View citing articles Show Details

Shao, Ning; Wang, Cheng; Huang, Xianhai; Xiao, Dong; Palani, Anandan; Aslanian, Robert; Shih, Neng-Yang

Tetrahedron Letters, 2006 , vol. 47, # 38 p. 6743 - 6746 Title/Abstract Full Text View citing articles Show Details

Ulus, Ismail H.; Maher, Timothy J.; Wurtman, Richard J.

Biochemical Pharmacology, 2000 , vol. 59, # 12 p. 1611 - 1621 Title/Abstract Full Text View citing articles Show Details

Zolkowska, Dorota; Rothman, Richard B.; Baumann, Michael H.

Journal of Pharmacology and Experimental Therapeutics, 2006 , vol. 318, # 2 p. 604 - 610 Title/Abstract Full Text View citing articles Show Details

Day, Robert F.; Lafontaine, Jennifer A.

Patent: US2002/52392 A1, 2002 ; Title/Abstract Full Text Show Details

The Procter and Gamble Company

Patent: US5614178 A1, 1997 ; Title/Abstract Full Text Show Details

Vicente, Jose; Saura-Llamas, Isabel; Bautista, Delia

Organometallics, 2005 , vol. 24, # 24 p. 6001 - 6004 Title/Abstract Full Text View citing articles Show Details

ALPEX PHARMA S.A.

Patent: US2008/206327 A1, 2008 ; Title/Abstract Full Text Show Details

Lewin, Anita H.; Navarro, Hernan A.; Wayne Mascarella

Bioorganic and Medicinal Chemistry, 2008 , vol. 16, # 15 p. 7415 - 7423 Title/Abstract Full Text View citing articles Show Details

Bristol, David William; King, Clifford Riley; Mitchener, JR., Joseph Pike; Audia, Vicki Haynes

Patent: US2008/293695 A1, 2008 ; Title/Abstract Full Text Show Details

G.D. Searle and Co.

Patent: US6337398 B1, 2002 ; Title/Abstract Full Text Show Details

GLAXOSMITHKLINE LLC; AXTEN, Jeffrey, Michael; BLACKLEDGE, Charles, William; BRADY, Gerald, Patrick; FENG, Yanhoug, G.; GRANT, Seth, W.; MEDINA, Jesus, Rahul; MILLER, William, H.; ROMERIL, Stuart, P.

Patent: WO2010/59658 A1, 2010 ; Title/Abstract Full Text Show Details

Andersen, Denise Lyn; Chang, Catherine H.; Falsey, James R.; Frohn, Michael J.; Hong, Fang-Tsao; Liao, Hongyu; Liu, Longbin; Lopez, Patricia; Retz, Daniel Martin; Rishton, Gilbert M.; Rzasa, Robert M.; Siegmund, Aaron; Tadesse, Seifu; Tamayo, Nuria; Tegley, Christopher M.

Patent: US2006/69110 A1, 2006 ; Title/Abstract Full Text Show Details

GLAXOSMITHKLINE LLC; AXTEN, Jeffrey, Michael; BRADY, Gerald, Patrick, Jr.; GALLAGHER, Timothy, Francis; HEERDING, Dirk, A.; MEDINA, Jesus, Raul; ROMERIL, Stuart, Paul

Patent: WO2010/120854 A1, 2010 ;

Title/Abstract Full Text Show Details

Addy, Carol; Jumes, Patricia; Rosko, Kimberly; Li, Susie; Li, Hankun; Maes, Andrea; Johnson-Levonas, Amy O.; Chodakewitz, Jeffrey; Stoch, S. Aubrey; Wagner, John A.

Journal of Clinical Pharmacology, 2009 , vol. 49, # 10 p. 1228 - 1238 Title/Abstract Full Text View citing articles Show Details

Takacs, Peter; Zhang, Yanping; Yavagal, Sujata; Candiotti, Keith; Chakhtoura, Nahida; Medina, Carlos A.

International Urogynecology Journal, 2012 , vol. 23, # 3 p. 357 - 363 Title/Abstract Full Text View citing articles Show Details

Daly; Creveling; Witkop

Journal of medicinal chemistry, 1966 , vol. 9, # 3 p. 273 - 280 Title/Abstract Full Text Show Details

Anderson Jr.; Santi

Journal of Medicinal Chemistry, 1976 , vol. 19, # 11 p. 1270 - 1275 Title/Abstract Full Text Show Details

3 of 21

Comment (Pharmacological Data)

Bioactivities present

Reference

LaPidus; Patil; LaPidus; Tye

Title/Abstract Full Text Show Details

Type: Review, Lab: EFF_071212, Owner: EFFECT, Number: 000, Revision: 07.12.2012 00:00:00 2012 Full Text Show Details

HOLM; HUUS; KOPF; MOLLER NIELSEN; PETERSEN

Acta pharmacologica et toxicologica, 1960 , vol. 17, p. 121 - 136 Title/Abstract Full Text Show Details

M. R. WARREN; D. G. MARSH; C. R. THOMPSON; R. S. SHELTON; T. J. BECKER

The Journal of pharmacology and experimental therapeutics, 1943 , vol. 79, p. 187 Full Text Show Details

Clarke's Analysis of Drugs and Poisons Full Text Show Details

BECKER

Toxicology and applied pharmacology, 1961 , vol. 3, p. 256 - 259 Title/Abstract Full Text Show Details

http://www.medsafe.govt.nz/Profs/datasheet/d/durominecap.htm Full Text Show Details

http://www.acnp.org/g4/GN401000156/CH152.html Full Text Show Details

http://www.pharmgkb.org/do/serve?objId=PA164748099&objCls=Drug Full Text Show Details

King, Clifford Riley; Bristol, David W.; English, Michael L.

Patent: US2014/178480 A1, 2014 ; Title/Abstract Full Text Show Details

Kim, Eun Ji; Choi, Ji Suk; Kim, Jun Sung; Choi, Young Chan; Cho, Yong Woo

Biomacromolecules, 2016 , vol. 17, # 1 p. 4 - 11 Title/Abstract Full Text View citing articles Show Details

Acosta, Andres; Camilleri, Michael; Linker-Nord, Sara; Busciglio, Irene; Iturrino, Johanna; Szarka, Lawrence A.; Zinsmeister, Alan R.

Journal of Neurogastroenterology and Motility, 2016 , vol. 22, # 1 p. 69 - 77 Title/Abstract Full Text View citing articles Show Details

Afzal, Mohadese Unesi

Research Journal of Pharmaceutical, Biological and Chemical Sciences, 2016 , vol. 7, # 1 p. 336 - 339 Title/Abstract Full Text View citing articles Show Details

McKay, Mary Pat; Groff, Loren

Accident Analysis and Prevention, 2016 , vol. 90, p. 108 - 117 Title/Abstract Full Text View citing articles Show Details

Yang, Mei; Peng, Songxu; Li, Wei; Wan, Zhihua; Fan, Linlin; Du, Yukai

Scientific Reports, 2016 , vol. 6, art. no. 23948 Title/Abstract Full Text View citing articles Show Details

Ahmad, Nadia N.; Butsch, Winfield Scott; Aidarous, Sabina

Obstetrics and Gynecology Clinics of North America, 2016 , vol. 43, # 2 p. 201 - 230 Title/Abstract Full Text View citing articles Show Details

Bahmani, Mahmoud; Eftekhari, Zohreh; Saki, Kourosh; Fazeli-Moghadam, Ezatollah; Jelodari, Mahyar; Rafieian-Kopaei, Mahmoud

Journal of Evidence-Based Complementary and Alternative Medicine, 2015 , vol. 21, # 3 p. 228 - 234 Title/Abstract Full Text View citing articles Show Details

Venkataraman, Lavanya; Sivaraman, Balakrishnan; Vaidya, Pratik; Ramamurthi, Anand

Journal of Tissue Engineering and Regenerative Medicine, 2016 , vol. 10, # 12 p. 1041 - 1056 Title/Abstract Full Text Show Details

Carney, Bonnie C.; Liu, Zekun; Alkhalil, Abdulnaser; Travis, Taryn E.; Ramella-Roman, Jessica; Moffatt, Lauren T.; Shupp, Jeffrey W.

Journal of Burn Care and Research, 2017 , vol. 38, # 1 p. 28 - 35 Title/Abstract Full Text Show Details

Merrilees, Mervyn J.; Falk, Ben A.; Zuo, Ning; Dickinson, Michelle E.; May, Barnaby C. H.; Wight, Thomas N.

Journal of Tissue Engineering and Regenerative Medicine, 2017 , vol. 11, # 1 p. 295 - 305 Title/Abstract Full Text Show Details

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Comment (Pharmacological Data)

Bioactivities present

Reference

Narayanaswami, Vidya; Dwoskin, Linda P.

Pharmacology and Therapeutics, 2017 , vol. 170, p. 116 - 147 Title/Abstract Full Text Show Details

Wu, Lian; Zhang, Jing; Qu, Jie Ming; Bai, Chun-Xue; Merrilees, Mervyn J.

International Journal of COPD, 2017 , vol. 12, p. 267 - 273 Title/Abstract Full Text Show Details

Garvey, W. Timothy; Mechanick, Jeffrey I.; Brett, Elise M.; Garber, Alan J.; Hurley, Daniel L.; Jastreboff, Ania M.; Nadolsky, Karl; Pessah-Pollack, Rachel; Plodkowski, Raymond

Endocrine Practice, 2016 , vol. 22, p. 1 - 203 Title/Abstract Full Text Show Details

Lin, Heng An; Chong, Keen Wai; Yeo, William

Journal of Orthopaedic Surgery, 2014 , vol. 22, # 1 p. 56 - 59 Title/Abstract Full Text Show Details

Butler, Colin R.; Hynds, Robert E.; Crowley, Claire; Gowers, Kate H.C.; Partington, Leanne; Hamilton, Nicholas J.; Carvalho, Carla; Platé, Manuela; Samuel, Edward R.; Burns, Alan J.; Urbani, Luca; Birchall, Martin A.; Lowdell, Mark W.; De Coppi, Paolo; Janes, Sam M.

Biomaterials, 2017 , vol. 124, p. 95 - 105 Title/Abstract Full Text Show Details

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Effect (Pharmacological Data)

drug interaction

Species or TestSystem (Pharmacological Data)

Sprague-Dawley rat

Sex

male

Route of Application

intraperitoneal

Concentration (Pharmacological Data)

Ca. 2 - 30 μmol/kg

Method (Pharmacological Data)

rats trained to discriminate cocaine (29.4 μmol/kg, i.p.) from saline treated with title comp.; 5 or 15 min after rats tested in two-lever operant-conditioning chambers

Further Details (Pharmacological Data)

further studies: title comp. dosed with cocaine (ca. 3-30 μmol/kg)

Type (Pharmacological Data)

ED50

Value of Type (Pharmacological Data)

7.09 μmol/kg

Results

title comp. engendered dose-related increases in percent of responses on cocaine-appropriate lever; title comp. in combination with cocaine produced sign. greater effect

Reference

Li, Su-Min; Campbell, Bettye L.; Katz, Jonathan L.

Journal of Pharmacology and Experimental Therapeutics, 2006 , vol. 317, # 3 p. 1088 - 1096 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

transmitter releasing

Species or TestSystem (Pharmacological Data)

Sprague-Dawley rat

Sex

male

Route of Application

intravenous

Concentration (Pharmacological Data)

1 - 3 mg/kg

Kind of Dosing (Pharmacological Data)

title comp. dissolved in saline and administered as bolus injection

Method (Pharmacological Data)

rats administered with title comp.; blood collected every 15 min pre-dosing and at 15-min intervals for 90 min post-dosing; dialyzed; dialysates assayed for 5-hydroxytryptamine and 5-hydroxyindoleacetic acid using HPLC with electrochemical detection

Further Details (Pharmacological Data)

control: saline; ref.: fluoxetine

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Results

title comp. had very weak effect on 5-hydroxytryptamine levels; title comp. treatment did not affect plasma 5-hydroxyindoleacetic acid levels; diagram

Reference

Zolkowska, Dorota; Rothman, Richard B.; Baumann, Michael H.

Journal of Pharmacology and Experimental Therapeutics, 2006 , vol. 318, # 2 p. 604 - 610 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

transmitter releasing

Species or TestSystem (Pharmacological Data)

Sprague-Dawley rat blood

Sex

male

Concentration (Pharmacological Data)

0.3 - 33 μmol/l

Kind of Dosing (Pharmacological Data)

title comp. dissolved in saline

Method (Pharmacological Data)

title comp. added to blood samples; microdialysis probes placed into blood samples; dialysate efflux collected for 15 min; assayed for 5hydroxytryptamine levels

Further Details (Pharmacological Data)

control: saline; ref.: fluoxetine

Results

title comp. significantly increased plasma 5-hydroxytryptamine levels only at 33 μmol/l; diagram

Reference

Zolkowska, Dorota; Rothman, Richard B.; Baumann, Michael H.

Journal of Pharmacology and Experimental Therapeutics, 2006 , vol. 318, # 2 p. 604 - 610 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

enzyme; inhib. of

Species or TestSystem (Pharmacological Data)

human liver monoamine oxidase A

Concentration (Pharmacological Data)

1000 - 3500 μmol/l

Method (Pharmacological Data)

recombinant human liver MAO A incubated in 50 mmol/l potassium phosphate, pH 7.5, 0.5 percent (w/v) Triton X-100 at 25 deg C in presence of title comp.; MAO A-catalyzed oxidation of p-CF3-benzylamine was determined; spectrophotometric assay

Further Details (Pharmacological Data)

MAO A: monoamine oxidase A; oxidation was monitored at 243 nm; further investigations using preincubation with title comp. for >= 15 min before addition of MAO A

Type (Pharmacological Data)

Ki

Value of Type (Pharmacological Data)

498 μmol/l

Results

title comp. competitively inhibited human MAO A; association and dissociation with title comp. occurred very rapidly (figure)

Reference

Nandigama, Ravi K.; Newton-Vinson, Paige; Edmondson, Dale E.

Biochemical Pharmacology, 2002 , vol. 63, # 5 p. 865 - 869 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

enzyme; inhib. of

Species or TestSystem (Pharmacological Data)

human liver monoamine oxidase B

Concentration (Pharmacological Data)

1000 - 3000 μmol/l

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11 of 21

Method (Pharmacological Data)

recombinant human liver MAO B was incubated in 50 mmol/l potassium phosphate pH 7.5, 0.5 percent (w/v) Triton X-100 at 25 deg C in presence of title comp.; MAO B-catalyzed oxidation of benzylamine was determined; spectrophotometric assay

Further Details (Pharmacological Data)

MAO B: monoamine oxidase B; oxidation was monitored at 250 nm; further investigations using preincubation with title comp. for >= 15 min before addition of MAO B

Type (Pharmacological Data)

Ki

Value of Type (Pharmacological Data)

375 μmol/l

Results

title comp. competitively inhibited human MAO B; association and dissociation with title comp. occurred very rapidly (figure)

Reference

Nandigama, Ravi K.; Newton-Vinson, Paige; Edmondson, Dale E.

Biochemical Pharmacology, 2002 , vol. 63, # 5 p. 865 - 869 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

enzyme; inhib. of

Species or TestSystem (Pharmacological Data)

Sprague-Dawley rat lung homogenate

Sex

male

Concentration (Pharmacological Data)

10 - 10000 μmol/l

Method (Pharmacological Data)

homogenates preincubated with title comp. (20 min, 37 deg C); reaction started by <14C>serotonin; incubated (5 or 10 min); reaction stopped by 3 N HCl; serotonin deaminated metabolites extracted; radioactivity measured with LSS; MAO-A activity detd.

Further Details (Pharmacological Data)

LSS: liquid scintillation spectrometry; MAO-A: monoamine oxidase-A

Type (Pharmacological Data)

Ki

Value of Type (Pharmacological Data)

85 μmol/l

Results

title comp. inhibited the ability of MAO-A to deaminate serotonin and the inhibition was concentration-dependent; table, figure

Reference

Ulus, Ismail H.; Maher, Timothy J.; Wurtman, Richard J.

Biochemical Pharmacology, 2000 , vol. 59, # 12 p. 1611 - 1621 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

enzyme; inhib. of

Species or TestSystem (Pharmacological Data)

Sprague-Dawley rat lung homogenate

Sex

male

Concentration (Pharmacological Data)

10 - 32000 μmol/l

Method (Pharmacological Data)

homogenates preincubated with title comp. (20 min, 37 deg C); reaction started by <14C>β-phenylethylamine; incubated (2 min); reaction stopped by 3 N HCl; deaminated metabolites extracted; radioactivity detd. by LSS; MAO-B activity detd.

Further Details (Pharmacological Data)

LSS: liquid scintillation spectrometry; MAO-B: monoamine oxidase-B

Type (Pharmacological Data)

Ki

Value of Type (Pharmacological

326 μmol/l

Data)

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Results

title comp. inhibited the ability of MAO-B to deaminate β-phenylethylamine and the inhibition was concentration-dependent; table, figure

Reference

Ulus, Ismail H.; Maher, Timothy J.; Wurtman, Richard J.

Biochemical Pharmacology, 2000 , vol. 59, # 12 p. 1611 - 1621 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

enzyme; inhib. of

Species or TestSystem (Pharmacological Data)

Sprague-Dawley rat liver homogenate

Sex

male

Concentration (Pharmacological Data)

10 - 10000 μmol/l

Method (Pharmacological Data)

homogenates preincubated with title comp. (20 min, 37 deg C); reaction started by <14C>serotonin; incubated (5 or 10 min); reaction stopped by 3 N HCl; serotonin deaminated metabolites extracted; radioactivity measured with LSS; MAO-A activity detd.

Further Details (Pharmacological Data)

LSS: liquid scintillation spectrometry; MAO-A: monoamine oxidase-A; further study: reversibility of MAO-A by title comp. was studied using dilution method

Type (Pharmacological Data)

Ki

Value of Type (Pharmacological Data)

85 μmol/l

Results

title comp. inhibited ability of MAO-A to deaminate serotonin and the inhibition was conc.-dependent; diluting the samples 50-fold resulted in total recovery of MAO-A activity indicating that title comp. inhibited MAO-A reversibly; table, fig.

Reference

Ulus, Ismail H.; Maher, Timothy J.; Wurtman, Richard J.

Biochemical Pharmacology, 2000 , vol. 59, # 12 p. 1611 - 1621 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

enzyme; inhib. of

Species or TestSystem (Pharmacological Data)

Sprague-Dawley rat liver homogenate

Sex

male

Concentration (Pharmacological Data)

10 - 32000 μmol/l

Method (Pharmacological Data)

homogenates preincubated with title comp. (20 min, 37 deg C); reaction started by <14C>β-phenylethylamine; incubated (2 min); reaction stopped by 3 N HCl; deaminated metabolites extracted; radioactivity detd. by LSS; MAO-B activity detd.

Further Details (Pharmacological Data)

LSS: liquid scintillation spectrometry; MAO-B: monoamine oxidase-B; further study: reversibility of MAO-B by title comp. was studied using dilution method

Type (Pharmacological Data)

Ki

Value of Type (Pharmacological Data)

416 μmol/l

Results

title comp. inhibited ability of MAO-B to deaminate β-phenylethylamine and the inhibition was conc.-dependent; diluting the samples 50fold resulted in total recovery of MAO-B activity indicating that title comp. inhibited MAO-B reversibly; table, fig.

Reference

Ulus, Ismail H.; Maher, Timothy J.; Wurtman, Richard J.

Biochemical Pharmacology, 2000 , vol. 59, # 12 p. 1611 - 1621 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

enzyme; inhib. of

15 of 21

16 of 21

Species or TestSystem (Pharmacological Data)

Sprague-Dawley rat brain homogenate

Sex

male

Concentration (Pharmacological Data)

10 - 10000 μmol/l

Method (Pharmacological Data)

homogenates preincubated with title comp. (20 min, 37 deg C); reaction started by <14C>serotonin; incubated (5 or 10 min); reaction stopped by 3 N HCl; serotonin deaminated metabolites extracted; radioactivity measured with LSS; MAO-A activity detd.

Further Details (Pharmacological Data)

LSS: liquid scintillation spectrometry; MAO-A: monoamine oxidase-A

Type (Pharmacological Data)

Ki

Value of Type (Pharmacological Data)

88 μmol/l

Results

title comp. inhibited ability of MAO-A to deaminate serotonin and the inhibition was concentration-dependent and competitive; table, fig.

Reference

Ulus, Ismail H.; Maher, Timothy J.; Wurtman, Richard J.

Biochemical Pharmacology, 2000 , vol. 59, # 12 p. 1611 - 1621 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

enzyme; inhib. of

Species or TestSystem (Pharmacological Data)

Sprague-Dawley rat brain homogenate

Sex

male

Concentration (Pharmacological Data)

10 - 32000 μmol/l

Method (Pharmacological Data)

homogenates preincubated with title comp. (20 min, 37 deg C); reaction started by <14C>β-phenylethylamine; incubated (2 min); reaction stopped by 3 N HCl; deaminated metabolites extracted; radioactivity measured with LSS; MAO-B activity detd.

Further Details (Pharmacological Data)

LSS: liquid scintillation spectrometry; MAO-B: monoamine oxidase-B

Type (Pharmacological Data)

Ki

Value of Type (Pharmacological Data)

310 μmol/l

Results

title comp. inhibited ability of MAO-B to deaminate β-phenylethylamine and the inhibition was concentration-dependent; table, fig.

Reference

Ulus, Ismail H.; Maher, Timothy J.; Wurtman, Richard J.

Biochemical Pharmacology, 2000 , vol. 59, # 12 p. 1611 - 1621 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

enzyme; inhib. of

Species or TestSystem (Pharmacological Data)

Sprague-Dawley rat lung homogenate

Sex

male

Concentration (Pharmacological Data)

100 μmol/l

Method (Pharmacological Data)

homogenates preincubated with title comp. at 37 deg C for 5-40 min; reaction started by <14C>serotonin; incubated for 5 min; reaction stopped by 3 N HCl; serotonin deaminated metabolites extracted; radioactivity measured with LSS; MAO-A activity detd.

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19 of 21

Further Details (Pharmacological Data)

LSS: liquid scintillation spectrometry; MAO-A: monoamine oxidase-A

Results

title comp. inhibited the ability of MAO-A to deaminate serotonin; title comp. inhibition of serotonin metabolism was enhanced by preincubation and was maximal and stable after 5 min of preincubation; figure

Reference

Ulus, Ismail H.; Maher, Timothy J.; Wurtman, Richard J.

Biochemical Pharmacology, 2000 , vol. 59, # 12 p. 1611 - 1621 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

enzyme; inhib. of

Species or TestSystem (Pharmacological Data)

Sprague-Dawley rat liver homogenate

Sex

male

Concentration (Pharmacological Data)

100 μmol/l

Method (Pharmacological Data)

homogenates preincubated with title comp. at 37 deg C for 5-40 min; reaction started by <14C>serotonin; incubated for 5 min; reaction stopped by 3 N HCl; serotonin deaminated metabolites extracted; radioactivity measured with LSS; MAO-A activity detd.

Further Details (Pharmacological Data)

LSS: liquid scintillation spectrometry; MAO-A: monoamine oxidase-A

Results

title comp. inhibited the ability of MAO-A to deaminate serotonin; title comp. inhibition of serotonin metabolism was enhanced by preincubation and was maximal and stable after 5 min of preincubation; figure

Reference

Ulus, Ismail H.; Maher, Timothy J.; Wurtman, Richard J.

Biochemical Pharmacology, 2000 , vol. 59, # 12 p. 1611 - 1621 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

enzyme; inhib. of

Species or TestSystem (Pharmacological Data)

Sprague-Dawley rat brain homogenate

Sex

male

Concentration (Pharmacological Data)

100 μmol/l

Method (Pharmacological Data)

homogenates preincubated with title comp. at 37 deg C for 5-40 min; reaction started by <14C>serotonin; incubated for 5 min; reaction stopped by 3 N HCl; serotonin deaminated metabolites extracted; radioactivity measured with LSS; MAO-A activity detd.

Further Details (Pharmacological Data)

LSS: liquid scintillation spectrometry; MAO-A: monoamine oxidase-A

Results

title comp. inhibited the ability of MAO-A to deaminate serotonin; title comp. inhibition of serotonin metabolism was enhanced by preincubation and was maximal and stable after 5 min of preincubation; figure

Reference

Ulus, Ismail H.; Maher, Timothy J.; Wurtman, Richard J.

Biochemical Pharmacology, 2000 , vol. 59, # 12 p. 1611 - 1621 Title/Abstract Full Text View citing articles Show Details

Effect (Pharmacological Data)

enzyme; inhib. of

Species or TestSystem (Pharmacological Data)

Sprague-Dawley rat liver homogenate

Sex

male

Concentration (Pharmacological Data)

130 μmol/l

Method (Pharmacological

homogenates preincubated with title comp. alone or with other MAO inhibitors (20 min, 37 deg C); incubated with <14C>serotonin (5 or 10 min); reaction stopped by 3 N HCl; deaminated metabolites extracted; radioactivity detd. by LSS; MAO activity detd.

Data)

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Further Details (Pharmacological Data)

MAO: monoamine oxidase; LSS: liquid scintillation spectrometry; MAO inhibitors: l-pseudoephedrine, d-pseudoephedrine, l-ephedrine, dephedrine, d,l-norephedrine, estradiol benzoate

Results

title comp. alone caused 22 percent inhibition of MAO activity; title comp. + MAO inhibitors caused considerably greater inhibition; title comp. + d-pseudoephedrine + d-ephedrine with/without estradiol benzoate or d,l-norephedrine showed additive effect; table

Reference

Ulus, Ismail H.; Maher, Timothy J.; Wurtman, Richard J.

Biochemical Pharmacology, 2000 , vol. 59, # 12 p. 1611 - 1621 Title/Abstract Full Text View citing articles Show Details

Comment (Pharmacological Data)

clinical pharmacokinetics: elimination half-life after the intake of the retard preparation Jonamine 15: 11.0-13.3 h, 12.45 mg/kg p.o., human

Reference

Delbeke; Debackere

Arzneimittel-Forschung/Drug Research, 1986 , vol. 36, # 1 p. 134 - 137 Title/Abstract Full Text View citing articles Show Details

Comment (Pharmacological Data)

clinical pharmacokinetics: urinary excretion during a 72-h period under normal conditions (excretion peak 4 h after administration), elimination half-life: 13.6-19.3 h, after acetazolamide: 10.4-16.5 h or furosemide: 11.4-17.3 h, 12.45 mg/kg p.o.,human

Reference

Delbeke; Debackere

Arzneimittel-Forschung/Drug Research, 1986 , vol. 36, # 1 p. 134 - 137 Title/Abstract Full Text View citing articles Show Details

Other Data Use (1) Use Pattern

Reference

weight-control

ALPEX PHARMA S.A.

Patent: US2008/206327 A1, 2008 ; Title/Abstract Full Text Show Details

Reaxys Registry Number: 18581811

CAS Registry Number: 1039678-74-4 Molecular Formula: C10H15N Linear Structure Formula: C10H2(2)H13N

Molecular Weight: 162.133 InChI Key: DHHVAGZRUROJKS-BEKAVNSESA-N

3

Synthesize | Hide Details Find similar

Identification Substance Label (1) Label

Reference

15-d

Ito, Nobuhiro; Watahiki, Tsutomu; Maesawa, Tsuneaki; Maegawa, Tomohiro; Sajiki, Hironao

Synthesis, 2008 , # 9 art. no. F03608SS, p. 1467 - 1478 Title/Abstract Full Text View citing articles Show Details

1 prep out of 1 reactions.

Identification

1