701977-09-5Relevant articles and documents
LIQUID PHARMACEUTICAL COMPOSITIONS FOR PARENTERAL ADMINISTRATION OF A SUBSTITUTED AMIDE
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Page/Page column 12-13, (2009/05/28)
A liquid pharmaceutical composition comprising N-[1S,2S]-3-[(4-chlorophenyl)-2-(3-cyanophenyl)-1-methylpropyl]-2-methyl-2-{[(5-trifluoromethyl)pyridine-2-yl]oxy}propanamide is disclosed, together with processes of preparing the liquid pharmaceutical compo
Catalytic, enantioselective synthesis of taranabant, a novel, acyclic cannabinoid-1 receptor inverse agonist for the treatment of obesity
Chen, G-Yi,Frey, Lisa F.,Shultz, Scott,Wallace, Debra J.,Marcantonio, Karen,Payack, Joeseph F.,Vazquez, Enrique,Springfield, Shawn A.,Zhou, George,Liu, Ping,Kieczykowski, Gerard R.,Chen, Alex M.,Phenix, Brian D.,Singh, Utpal,Strine, Jeff,Izzo, Brianne,Krska, Shane W.
, p. 616 - 623 (2012/12/31)
Chiral amide 1 (MK-0364, taranabant) is a potent, selective, and orally bioavailable cannabinoid-1 receptor (CB-1R) inverse agonist indicated for the treatment of obesity. An asymmetric synthesis featuring a dynamic kinetic resolution via hydrogenation fo
Discovery of N-[(1S,2S)-3-(4-chlorophenyl)-2-(3-cyanophenyl)-1- methylpropyl]-2-methyl-2-{[5-(trifluoromethyl)pyridin-2-yl]oxy}propanamide (MK-0364), a novel, acyclic cannabinoid-1 receptor inverse agonist for the treatment of obesity
Lin, Linus S.,Lanza Jr., Thomas J.,Jewell, James P.,Liu, Fing,Shah, Shrenik K.,Qi, Hongbo,Tong, Xinchun,Wang, Junying,Xu, Suoyu S.,Fong, Tung M.,Shen, Chun-Pyn,Lao, Julie,Xiao, Jing Chen,Shearman, Lauren P.,Stribling, D. Sloan,Rosko, Kimberly,Strack, Alison,Marsh, Donald J.,Feng, Yue,Kumar, Sanjeev,Samuel, Koppara,Yin, Wenji,Van Der Ploeg, Lex H. T.,Goulet, Mark T.,Hagmann, William K.
, p. 7584 - 7587 (2007/10/03)
The discovery of novel acyclic amide cannabinoid-1 receptor inverse agonists is described. They are potent, selective, orally bioavailable, and active in rodent models of food intake and body weight reduction. A major focus of the optimization process was to increase in vivo efficacy and to reduce the potential for formation of reactive metabolites. These efforts led to the identification of compound 48 for development as a clinical candidate for the treatment of obesity.