Genentech, Inc.

F. Hoffmann-la Roche Ag

Constellation Pharmaceuticals, Inc.

Curis, Inc.

Portola Pharmaceuticals, Inc.

Piramed Limited

Shumei Wang

Daniel P Sutherlin

Bing-Yan Zhu

Georgette M Castanedo

Daniel J Burdick

Kimberly Malesky

Alan G Olivero

Adrian Folkes

Janet Gunzner

Irina Chuckowree

Nan Chi Wan

Simon Mathieu

Jennafer Dotson

Christopher G Nasveschuk

Huifen Chen

Steven R Magnuson

Vickie Hsiao-Wei Tsui

Mark E Reynolds

Mark S Stanley

Scott J Savage

Tim Heffron

Terry Crawford

Janet L Gunzner-Toste

Sally Oxenford

Michael S Dina

Yong Tang

Liang Bao

Rebecca L Lalonde

Zachary Kevin Sweeney

Anthony A Estrada

Brian K Albrecht

Bryan K Chan

Mark Stewart Chambers

F Anthony Romero

Michael Charles Hewitt

Alexander M Taylor

Charles Baker-Glenn

Steven F Bellon

Guiling Zhao

Richard A Goldsmith

Vickie H Tsui

Daniel Shore

Alexandre Cote

Michael F T Koehler

Les A Dakin

Tracy Bayliss

Yves LeBlanc

Robert M Scarborough

Yonghong Song

Steven T Staben

Christian Wiesmann

Tim Hancox

Shawn M Bauer

Mark A Reynolds

Martin Duplessis

Timothy Heffron

Weiru Wang

Stephen Joseph Shuttleworth

Stephen Shuttleworth

Marc Adler

Anthony F Romero

Scott Savage

Janet Gunzner-Tate

Chhaya Bhakta

Mark Stanley

Irina S Chuckowree

Adrian J Folkes

Daniel Jon Burdick

Janet Gunzner-Toste

Michael F Koehler

Christian Weismann

The present invention relates to compounds of formula (I): and to salts thereof, wherein R, R, R, and Rhave any of the values defined in the specification, and compositions and uses thereof. The compounds are useful as inhibitors of bromodomains. Also included are pharmaceutical compositions comprising a compound of formula (I) or a pharmaceutically acceptable salt thereof, and methods of using such compounds and salts in the treatment of various bromodomain-mediated disorders.

Therapeutic compounds and uses thereof

The present invention relates to compounds of formula (I): and to salts thereof, wherein R-Rhave any of the values defined in the specification, and compositions and uses thereof. The compounds are useful as inhibitors of TAF1. Also included are pharmaceutical compositions comprising a compound of formula (I) or a pharmaceutically acceptable salt thereof, and methods of using such compounds and salts in the treatment of various TAF1-mediated disorders.

The present invention relates to compounds of formula (I): and to salts thereof, wherein R, R, and Q have any of the values defined in the specification, and compositions and uses thereof. The compounds are useful as inhibitors of bromodomains. Also included are pharmaceutical compositions comprising a compound of formula (I) or a pharmaceutically acceptable salt thereof, and methods of using such compounds and salts in the treatment of various bromodomain-mediated disorders.

The invention provides novel inhibitors of hedgehog signaling that are useful as a therapeutic agents for treating malignancies where the compounds have the general formula I: wherein A, X, Y R, R, R, R, m and n are as described herein.

Pyridyl inhibitors of hedgehog signalling

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

Compounds having the formula I wherein Rand Rare as defined herein are inhibitors of ERK kinase. Also disclosed are compositions and methods for treating hyperproliferative disorders. 

Substituted pyrrolo[2,3-b]pyrazines as serine/threonine kinase 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

Aminopyrimidine derivatives as LRRK2 modulators

Compounds of the formula I: or pharmaceutically acceptable salts thereof,

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 the formula I: or pharmaceutically acceptable salts thereof,wherein m, n. X, R, R, R, R, Rand Rare as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of diseases associated with LRRK2 receptor, such as Parkinson's disease.

Aminopyrimidine derivatives as LRRK2 inhibitors

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Foster City, CA, United States of America

Shumei Wang