Benzoxazepin PI3K inhibitor compounds and methods of use

US9546178B2 · kind B2 · utility

Assignee

• Genentech, Inc. · US

Inventors

• Nicole Blaquiere · South San Francisco, US
• Steven Do · San Jose, US
• Danette Dudley · Ann Arbor, US
• Adrian Folkes · Slough, GB
• Robert Heald · Harlow, GB
• Timothy Heffron · Burlingame, US
• Mark Jones · Harlow, GB
• Aleksandr Kolesnikov · Mill Valley, US
• Chudi Ndubaku · Oakland, US
• Alan G. Olivero · South San Francisco, US
• Stephen Price · Harlow, GB
• Steven Staben · South San Francisco, US
• Lan Wang · Foster City, US

Key dates

• Filing date: Nov 3, 2015
• Grant date: Jan 17, 2017
• Expiry date: Nov 3, 2035

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D519/00
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

Benzoxazepin compounds of Formula I, including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, wherein: Z1 is CR1 or N; Z2 is CR2 or N; Z3 is CR3 or N; Z4 is CR4 or N; and B is a pyrazolyl, imidazolyl, or triazolyl ring fused to the benzoxepin ring, are useful for inhibiting lipid kinases including p110 alpha and other isoforms of PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.