Benzopyran and benzoxepin PI3K inhibitor compounds and methods of use

US8846762B2 · kind B2 · utility

Assignees

• Genentech, Inc. · US
• F. Hoffmann-La Roche AG · CH

Inventors

• Steven Do · San Jose, US
• Richard Goldsmith · Belmont, US
• Tim Heffron · San Francisco, US
• Aleksandr Kolesnikov · Mill Valley, US
• Steven Staben · South San Francisco, US
• Alan G. Olivero · South San Francisco, US
• Michael Siu · Burlingame, US
• Daniel P. Sutherlin · Redwood City, US
• Bing-Yan Zhu · South San Francisco, US
• Paul Goldsmith · Basel, CH
• Tracy Bayliss · Basel, CH
• Adrian Folkes · Slough, GB
• Neil Anthony Pegg · Stevenage, GB

Key dates

• Filing date: Jan 10, 2013
• Grant date: Sep 30, 2014
• Expiry date: Jan 10, 2033

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D513/14
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

Benzopyran and benzoxepin compounds of Formulas I and II, and including stereoisomers, geometric isomers, tautomer solvates, metabolites and pharmaceutically acceptable salts thereof, 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 Formulas I and II for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.