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Discovery of 2-(2-chlorophenyl)-3-(4-chlorophenyl)-7-(2,2-difluoropropyl)-6,7-dihydro-2H-pyrazolo[3,4-f][1,4]oxazepin-8(5H)-one (PF-514273), a Novel, Bicyclic Lactam-Based cannabinoid-1 Receptor Antagonist for the Treatment of Obesity

Discovery of 2-(2-chlorophenyl)-3-(4-chlorophenyl)-7-(2,2-difluoropropyl)-6,7-dihydro-2H-pyrazolo[3,4-f][1,4]oxazepin-8(5H)-one (PF-514273), a Novel, Bicyclic Lactam-Based cannabinoid-1 Receptor Antagonist for the Treatment of Obesity

Robert L Dow, Philip A Carpino, John R Hadcock, Shawn C Black, Philip A Iredale, Paul DaSilva-Jardine, Steven R Schneider, Ernest S Paight, David A Griffith, Dennis O Scott, Rebecca E O'Connor, Chudy I Nduaka

J Med Chem. 2009 May 14;52(9):2652-5.

PMID: 19351113

Abstract:

We report the design, synthesis, and structure-activity relationships of novel bicyclic lactam-based cannabinoid type 1 (CB(1)) receptor antagonists. Members of these series are potent, selective antagonists in in vitro/in vivo efficacy models of CB(1) antagonism and exhibit robust oral activity in rodent models of food intake. These efforts led to the identification of 19d, which has been advanced to human clinical trials for weight management.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP851728604	PF-514273		851728-60-4	Price

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