Genentech, Inc.

F. Hoffmann-la Roche Ag

Piramed Limited

Hoffman-laroche, Inc. (us Only)

F. Hoffman-laroche, Ag (ex-us)

Jennafer Dotson

Alan G Olivero

Bing-Yan Zhu

Daniel P Sutherlin

Adrian Folkes

Timothy Heffron

Shumei Wang

Tim Heffron

Robert Andrew Heald

Georgette M Castanedo

Irina Chuckowree

Richard A Goldsmith

Nan Chi Wan

Vickie H Tsui

Simon Mathieu

Janet Gunzner

Tracy Bayliss

Bryan K Chan

Steven T Staben

Christian Wiesmann

Chudi Obioma Ndubaku

Graham Elgin Jones

Lan Wang

Sally Oxenford

Kimberly Malesky

Tim Hancox

Neville James McLean

Laurent Salphati

Sussie Lerche Krintel

Joseph P Lyssikatos

Zachary Kevin Sweeney

Anthony A Estrada

Jun Liang

Brian Salvatore Safina

Eileen Mary Seward

BinQing Wei

Charles Baker-Glenn

Birong Zhang

Emily J Hanan

Matthias Rueth

Michael Lainchbury

Thomas E Rawson

Aihe Zhou

Binqing Wei

Stephen Joseph Shuttleworth

Jun M Li

Marian C Bryan

Ignacio Aliagas-Martin

Stephen Shuttleworth

Jason S Halladay

Francois Diederich

Frederick Brookfield

Michael Prime

BinQuing Wei

Adrian J Folkes

Irina S Chuckowree

Christian Weismann

Neville James Mclean

Joseph Lyssikatos

Chudi Ndubaku

This invention relates to novel compounds which are inhibitors of T790M containing EGFR mutants, to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy for the prevention or treatment of cancer.

Azaindazole compounds as inhibitors of T790M containing EGFR mutants

Tricyclic PI3k inhibitor compounds of Formula I with anti-cancer activity, anti-inflammatory activity, or immunoregulatory properties, and more specifically with PI3 kinase modulating or inhibitory activity are described. Methods are described for using the tricyclic PI3K inhibitor compounds of Formula I for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, organisms, or associated pathological conditions.  Formula I compounds include stereoisomers, geometric isomers, tautomers, and pharmaceutically acceptable salts thereof. The dashed lines indicate an optional double bond, and at least one dashed line is a double bond. The substituents are as described.

Tricyclic 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

Bicyclic pyrazole LRRK2 small molecule inhibitors

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

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 or inflammation 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. 

Pyrazolopyridine PI3K inhibitor compounds and methods of use

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. 

Compounds of Formulas Ia and Ib, and including 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. 

The invention provides novel kinase inhibitors that are useful as therapeutic agents for example in the treatment malignancies where the compounds have the general formula I wherein A, X, Y, Z, Ra, Rb, Rc, R, R, Rand m are defined herein.

Pentacyclic kinase inhibitors

Growing community of inventors

Belmont, CA, United States of America

Jennafer Dotson