2. Academic Validation
  3. 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

  • J Med Chem. 2009 May 14;52(9):2652-5. doi: 10.1021/jm900255t.
Robert L Dow 1,  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
Affiliations

Affiliation

  • 1 Department of Cardiovascular, Metabolic and Endocrine Diseases, Pfizer Global Research and Development, Groton, Connecticut 06340, USA. robert.l.dow@pfizer.com
PMID: 19351113 DOI: 10.1021/jm900255t
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.

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