Genentech, Inc.

F. Hoffmann-la Roche Ag

Piramed Limited

Hoffmann-la Roche Inc.

Genetech, Inc.

Xenova Limited

Adrian Folkes

Alan G Olivero

Irina Chuckowree

Steven T Staben

Daniel P Sutherlin

Nan Chi Wan

Bing-Yan Zhu

Richard A Goldsmith

Steven Huy Do

Aleksandr Kolesnikov

Tim Heffron

Timothy Heffron

Georgette M Castanedo

Stephen Colin Price

Robert Andrew Heald

Chudi Obioma Ndubaku

Nicole Blaquiere

Danette Dudley

Simon Mathieu

Stephen Joseph Shuttleworth

Tracy Bayliss

Janet Gunzner

Sally Oxenford

Shumei Wang

Lan Wang

Timothy Colin Hancox

Mark Jones

Stewart James Baker

Sukhjit Sohal

Tim Hancox

Mohammed A Latif

Jennafer Dotson

Stephen Shuttleworth

Michael Siu

Kimberly Malesky

Paul Goldsmith

Neil Pegg

Vickie H Tsui

Christian Wiesmann

BinQing Wei

Binqing Wei

William Alexander Denny

Nigel Vicker

Paul John Goldsmith

John Milton

Janet Gunzer-Toste

Shouming Wang

Irina Cchuckowree

Janet Gunzer

Bing-Yang Zhu

Compounds of Formulae Ia, and stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting lipid kinases including PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formula Ia for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed. 

Pharmaceutical compounds

Benzoxazepin compounds of Formula I, including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, wherein: Zis CRor N; Zis CRor N; Zis CRor N; Zis CRor 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. 

Benzoxazepin PI3K inhibitor compounds and methods of use

Compounds of Formulas Ia-d where X is S or O, mor is a morpholine group, and Ris a monocyclic heteroaryl group, and including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for modulating the activity of lipid kinases including PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formula Ia-d for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed. 

Phosphoinositide 3-kinase inhibitor compounds and methods of use

Benzopyran and benzoxepin compounds of Formulas I and II, 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 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. 

Benzopyran and benzoxepin PI3K inhibitor compounds and methods of use

Benzoxepin compounds of Formula I, and including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, wherein: Zis CRor N; Zis CRor N; Zis CRor N; Zis CRor N; and where (i) Xis N and Xis S, (ii) Xis S and Xis N, (iii) Xis CRand Xis S, (iv) Xis S and Xis CR; (v) Xis NRand Xis N, (vi) Xis N and Xis NR, (vii) Xis CRand Xis O, (viii) Xis O and Xis CR, (ix) Xis CRand Xis C(R), (x) Xis C(R)and Xis CR; (xi) Xis N and Xis O, or (xii) Xis O and Xis N, 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. 

Benzoxepin PI3K inhibitor compounds and methods of use

Provided herein is a pharmaceutical composition that comprises a pharmaceutically acceptable carrier or diluent and, as an active ingredient, the compound 2-(1H-indazol-4-yl)-6-(4-methanesulfonyl-piperazin-1-ylmethyl)-4-morpholin-4-yl-thieno[3,2-d]pyrimidine bismesylate.

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. 

Pyrazolopyrimidine PI3K inhibitor compounds and methods of use

Fused pyrimidines of formula (I): wherein R-R, A and n have any of the values described in the specification; and pharmaceutically acceptable salts thereof; have activity as inhibitors of PI3K and may thus be used to treat diseases and disorders arising from abnormal cell growth, function or behaviour associated with PI3 kinase such as cancer, immune disorders, cardiovascular disease, viral infection, inflammation, metabolism/endocrine disorders and neurological disorders. Processes for synthesizing the compounds are also described.

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. 

Compounds of Formulae Ia and Ib, and stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting lipid kinases including PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formula Ia and Ib for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed. 

Growing community of inventors

Basel, Switzerland

Adrian Folkes