701977-22-2Relevant academic research and scientific papers
SUBSTITUTED ESTERS AS CANNABINOID-1 RECEPTOR MODULATORS
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Page/Page column 58-59, (2008/06/13)
Novel compounds of the structural formula (I) are antagonists and/or inverse agonists of the Cannabinoid-1 (CB1) receptor and are useful in the treatment, prevention and suppression of diseases mediated by the CB1 receptor. The compounds of the present in
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.
