851728-60-4

Basic information

• Product Name: PF 514273
• Synonyms: PF 514273;2-(2-Chlorophenyl)-3-(4-chlorophenyl)-7-(2,2-difluoropropyl)-6,7-dihydro-2H-pyrazolo[3,4-f][1,4]oxazepin-8(5H)-one;2H-Pyrazolo[3,4-f][1,4]oxazepin-8(5H)-one, 2-(2-chlorophenyl)-3-(4-chlorophenyl)-7-(2,2-difluoropropyl)-6,7-dihydro-;2-(2-chlorophenyl)-3-(4-chlorophenyl)-7-(2,2-difluoropropyl)-5,6-dihydropyrazolo[3,4-f][1,4]oxazepin-8-one
• CAS NO: 851728-60-4
• Molecular Formula: C21H17Cl2F2N3O2
• Molecular Weight: 452.2813864
• Product Categories: Pfizer Compounds;Amines;Aromatics;Heterocycles;Inhibitors;Intermediates & Fine Chemicals;Pharmaceuticals
• Mol File: 851728-60-4.mol
• Article Data: 3

Chemical Properties

• Melting Point: 158-160°C
• Appearance: white to beige/
• Storage Temp.: Store at +4°C
• Solubility: DMSO: >5mg/mL (warmed)
• CAS DataBase Reference: PF 514273(CAS DataBase Reference)
• NIST Chemistry Reference: PF 514273(851728-60-4)
• EPA Substance Registry System: PF 514273(851728-60-4)

Safety Data

• WGK Germany: 3
• Hazardous Substances Data: 851728-60-4(Hazardous Substances Data)

Usage

Chemical Properties

White Solid

Uses

A novel, bicyclic lactam-based cannabinoid-1 receptor antagonist for the treatment of obesity.

Upstream product

• 851728-92-2 1-(2-chlorophenyl)-5-(4-chlorophenyl)-4-hydroxy-1H-pyrazole-3-carboxylic acid (2,2-difluoropropyl)-(2-hydroxy-ethyl)amide 

Relevant articles and documents

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

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.

Bicyclic pyrazolyl and imidazolyl compounds and uses thereof

Compounds of Formula (I) are described herein. The compounds have been shown to act as cannabinoid receptor ligands and are therefore useful in the treatment of diseases linked to the mediation of the cannabinoid receptors in animals.