Benzoxepin PI3K inhibitor compounds and methods of use

US8673952B2 · kind B2 · utility

Assignee

• F. Hoffmann-La Roche AG · CH

Inventors

• Nicole Blaquiere · South San Francisco, US
• Steven Do · San Jose, US
• Danette Dudley · Ann Arbor, US
• Adrian Folkes · Slough, GB
• Richard Goldsmith · Belmont, US
• Robert Heald · Harlow, GB
• Timothy Heffron · Burlingame, US
• 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
• BinQing Wei · Belmont, US

Key dates

• Filing date: Aug 7, 2012
• Grant date: Mar 18, 2014
• Expiry date: Aug 7, 2032

Classification

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

Abstract

Benzoxepin compounds of Formula I, and including stereoisomers, geometric isomers, tautomers, 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 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.