Genentech, Inc.

Constellation Pharmaceuticals, Inc.

F. Hoffmann-la Roche Ag

Curis, Inc.

Vickie Hsiao-Wei Tsui

Steven R Magnuson

John A Flygare

Frederick Cohen

F Anthony Romero

Lewis J Gazzard

Brian K Albrecht

Alexander M Taylor

Christopher G Nasveschuk

Terry Crawford

Alexandre Cote

Daniel J Burdick

Kwong Wah Lai

Fei Wang

Jun Liang

Michael Charles Hewitt

Steven F Bellon

Wayne J Fairbrother

Shumei Wang

Sarah Bronner

Yong Tang

Patrick Cyr

Bainian Feng

Victor S Gehling

Kevin X Chen

Birong Zhang

Richard Pastor

Les A Dakin

Yves LeBlanc

Kurt Deshayes

John Wai

Jeremy M Murray

Yves Leblanc

Cuong Q Ly

James Richard Jr Kiefer

Marc Adler

Bing-Yan Zhu

Jean-Christophe P Harmange

Steven Huy Do

Aleksandr Kolesnikov

Xiaojing Wang

Wendy Lee

Martin Duplessis

Kirk D Robarge

Simon Charles Goodacre

Mark S Stanley

Karen Williams

Aihe Zhou

Michael F T Koehler

Alexandre Côté

Steven Elliot Kauder

Zhaoyang Wen

James Richard Kiefer, Jr

Yingjie Lai

Huiyong Hu

Jiangpeng Liao

Anthony F Romero

Jackson G Egen

Christopher G Nasveschuck

Stephen Franz Keteltas

Jackson Egen

Kevin Chen

Novel inhibitors of IAP that are useful as therapeutic agents for treating malignancies and have the general formula I: wherein R, R, R, R, Rand Rare as described herein.

Inhibitors of IAP

The present invention relates to a compound formula (I): and to salts thereof, wherein R, RX, and Y have any of the values defined herein, and compositions and uses thereof. The compounds are useful as inhibitors of CBP and/or EP300. 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 CBP and/or EP300-mediated disorders.

Therapeutic compounds and uses thereof

The present invention relates to compounds of formula (I) and formula (II): and to salts thereof, wherein R-Rof formula (I) and R-Rof formula (II) have any of the values defined herein, and compositions and uses thereof. The compounds are useful as inhibitors of CBP and/or EP300. Also included are pharmaceutical compositions comprising a compound of formula (I) of formula (II), or a pharmaceutically acceptable salt thereof, and methods of using such compounds and salts in the treatment of various CBP and/or EP300-mediated disorders.

The present invention relates to compounds useful as inhibitors of one or more histone demethylses, such as KDM2b. The invention also provides pharmaceutically acceptable compositions comprising compounds of the present invention and methods of using said compositions in the treatment of various disorders.

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.

The present invention relates to compounds of formula (I): and to salts thereof, wherein A has any of the values defined in the specification, and compositions and uses thereof. The compounds are useful as inhibitors of CBP and/or EP300. 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 CBP and/or EP300-mediated disorders.

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.

Pyrazolo[3,4-c]pyridine compounds of Formula I, including stereoisomers, geometric isomers, tautomers, and pharmaceutically acceptable salts thereof, wherein Rand Rare as defined herein, are useful for inhibiting Pim kinase, and for treating disorders such as cancer mediated by Pim kinase. 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. 

Pyrazolo[3,4-c]pyridine compounds and methods of use

The present invention relates to compounds of formula (I) or formula (II): and to salts thereof, wherein R-Rof formula (I) and R-Rof formula (II) have any of the values defined herein, and compositions and uses thereof. The compounds are useful as inhibitors of CBP and/or EP300. Also included are pharmaceutical compositions comprising a compound of formula (I) of formula (II) or a pharmaceutically acceptable salt thereof, and methods of using such compounds and salts in the treatment of various CBP and/or EP300-mediated disorders.

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South San Francisco, CA, United States of America

Vickie Hsiao-Wei Tsui