Genentech, Inc.

Constellation Pharmaceuticals, Inc.

F. Hoffmann-la Roche Ag

Terry Crawford

Steven R Magnuson

Brian K Albrecht

Alexander M Taylor

Christopher G Nasveschuk

F Anthony Romero

Alexandre Cote

Vickie Hsiao-Wei Tsui

Yves LeBlanc

Daniel J Burdick

Yong Tang

Huifen Chen

Michael Charles Hewitt

Martin Duplessis

Richard Pastor

Shumei Wang

Lan Wang

Chudi Obioma Ndubaku

Steven F Bellon

Les A Dakin

Seth F Harris

Andrew Charles Good

Kevin X Chen

Kwong Wah Lai

Jeremy M Murray

Anthony F Romero

Marc Adler

Bing-Yan Zhu

Fei Wang

Yves Leblanc

Alexandre Côté

Steven Elliot Kauder

Sarah Bronner

Patrick Cyr

Jiangpeng Liao

Jackson G Egen

Chudi Nbdubaku

Christopher G Nasveschuck

Kevin Chen

The present invention relates to methods for treating PCAF mediated disorders using a compound of formula (I) or a pharmaceutically acceptable salt thereof: wherein R, R-R, X, and each Rhave any of the values defined in the specification. Also included are novel compounds of formula (I) and salts thereof, as well as pharmaceutical compositions comprising a compound of formula (I) or a pharmaceutically acceptable salt thereof.

Therapeutic compounds and uses thereof

The present invention relates to compounds of formula (I): and 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 BRG1, BRM and/or PB1. 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 BRG1-mediated disorders, BRM-mediated disorders and/or PB1-mediated 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.

The present invention relates to methods for treating PCAF and GCN5 mediated disorders using a compound of formula (I) or a pharmaceutically acceptable salt thereof: wherein ring A, R, R, R, R, and each Rhave any of the values defined in the specification. Also included are novel compounds of Formula (I) and salts thereof, as well as pharmaceutical compositions comprising a compound of formula (I) or a pharmaceutically acceptable salt thereof.

The invention provides a method of inhibiting angiogenesis in a patient by administering a compound of formula (I): 

Aminoquinazoline and pyridopyrimidine derivatives

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.

The invention provides a method of treating cancer in a patient by administering a compound of formula (I): 

The invention provides novel compounds having the general formula: wherein A, Rand Rare as described herein, compositions including the compounds and methods of using the compounds.

Isoquinoline and naphthyridine derivatives

The invention provides novel compounds having the general formula: 

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South San Francisco, CA, United States of America

Terry Crawford