Genentech, Inc.

Constellation Pharmaceuticals, Inc.

D.e. Shaw Research, LLC

Relay Therapeutics, Inc.

Yong Tang

Christopher G Nasveschuk

Steven R Magnuson

Alexander M Taylor

Terry Crawford

Brian K Albrecht

F Anthony Romero

Vickie Hsiao-Wei Tsui

Shumei Wang

Daniel J Burdick

Alexandre Cote

Yves LeBlanc

Michael Charles Hewitt

Steven F Bellon

Les A Dakin

Martin Duplessis

Mark Andrew Murcko

Lucian V DiPietro

André Lescarbeau

Fabrizio Giordanetto

Sathesh P Bhat

Elizabeth Helen Kelley

W Patrick Walters

Eric Therrien

Markus Kristofer Dahlgren

Kelley C Shortsleeves

Paul Maragakis

Andrew Charles Good

Jack Benjamin Greisman

Marc Adler

Anthony F Romero

Levi Charles Thomas Pierce

Markus Kristofer Dahlgeren

The present disclosure relates to compounds of formula (I) and pharmaceutical compositions thereof and methods for inhibiting the activity of SHP2 phosphatase with the compounds and compositions of the disclosure. The present disclosure further relates to, but is not limited to, methods for treating disorders associated with SHP2 deregulation with the compounds and compositions of the disclosure. 

Substituted pyrazolo[3,4-b]pyrazines as SHP2 phosphatase inhibitors

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.

Therapeutic compounds and uses thereof

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 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.

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Cambridge, MA, United States of America

Yong Tang