851728-87-5Relevant academic research and scientific papers
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
Dow, Robert L.,Carpino, Philip A.,Hadcock, John R.,Black, Shawn C.,Iredale, Philip A.,DaSilva-Jardine, Paul,Schneider, Steven R.,Paight, Ernest S.,Griffith, David A.,Scott, Dennis O.,O'Connor, Rebecca E.,Nduaka, Chudy I.
supporting information; experimental part, p. 2652 - 2655 (2010/03/03)
We report the design, synthesis, and structure-activity relationships of novel bicyclic lactam-based cannabinoid type 1 (CB1) receptor antagonists. Members of these series are potent, selective antagonists in in vitro/in vivo efficacy models of CB1 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.
PYRAZOLE COMPOUNDS HAVING CANNABINOID RECEPTOR (CB1) ANTAGONIZING ACTIVITY
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Page/Page column 111, (2008/06/13)
The present invention relates to a pyrazole compound having potent CB1-antagonizing activity, having the following formula [I]: wherein R1 and R2 are the same or different and an optionally substituted aryl group etc., R3 is an alkyl group etc., E is one of the following groups of the formula (i) to (iv): Q1 is a single bond, an alkylene group or a group of the formula: -N(R7)-, R7 is a hydrogen atom or an alkyl group, Q2 is a single bond, an oxygen atom or an alkylene group, R4 is a cycloalkyl group, a group of the formula: -N(R5)(R6) etc., one of R5 and R6 is a hydrogen atom or an alkyl group and the other is an alkyl group, a group of the formula: -N(R8)(R9) etc., D is an oxygen atom etc., RA1 is an amino group etc., RA2 is an optionally substituted aliphatic heterocyclic group, R is an alkyl group optionally substituted by one to three halogen atom(s) etc., one of R8 and R9 is a hydrogen atom or an alkyl group and the other is an alkyl group etc., or a pharmaceutically acceptable salt thereof.
