Constellation Pharmaceuticals, Inc.

Genentech, Inc.

Genetech, Inc.

Alexandre Cote

James E Audia

Fei Wang

Brian K Albrecht

Alexander M Taylor

Christopher G Nasveschuk

Steven R Magnuson

F Anthony Romero

Terry Crawford

Yves LeBlanc

Vickie Hsiao-Wei Tsui

Martin Duplessis

Daniel J Burdick

Michael Charles Hewitt

Richard Pastor

Yong Tang

Andrew Charles Good

Victor S Gehling

Steven F Bellon

Shumei Wang

Les A Dakin

Jean-Christophe P Harmange

Jun Liang

Anthony F Romero

James Richard Jr Kiefer

Yves Leblanc

Kevin X Chen

Birong Zhang

Rishi G Vaswani

Kwong Wah Lai

Sarah Bronner

James Richard Kiefer, Jr

Patrick Cyr

Jeremy M Murray

Jiangpeng Liao

Marc Adler

Christopher G Nasveschuck

Jackson Egen

James Edmund Audia

Christopher G Naveschuk

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.

Provided herein are compounds of formula I: and salts thereof and compositions and uses thereof. The compounds are useful as inhibitors of LSD1. 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 LSD1-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 invention relates to compounds of formula (I) and salts thereof: wherein R-Rhave any of the values defined in the specification. The compounds and salts are useful for treating PCAF mediated disorders and/or GCN5 mediated disorders. The invention also provides pharmaceutical compositions comprising a compound of formula (I), or a pharmaceutically acceptable salt thereof, as well as and methods of using said compounds, salts, or compositions in the treatment of various 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, 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 present invention relates to compounds useful as inhibitors of bromodomain-containing proteins. 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.

Bromodomain inhibitors and uses thereof

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Cambridge, MA, United States of America

Alexandre Cote