Genentech, Inc.

Constellation Pharmaceuticals, Inc.

Bayer Pharmaceuticals Corporation

Bayer Healthcare LLC

F. Hoffmann-la Roche Ag

Other

Smithkline Beecham Corporation

Steven R Magnuson

Vickie Hsiao-Wei Tsui

Terry Crawford

F Anthony Romero

Brian K Albrecht

Alexander M Taylor

Richard Pastor

Christopher G Nasveschuk

Alexandre Cote

Jun Liang

Ning Qi

Barton W Phillips

William H Bullock

Julie A Dixon

Bing-Yan Zhu

Zhonghua Zhang

Brent Chandler

Yves LeBlanc

Stephen J O'Connor

Birong Zhang

Uday R Khire

Daniel J Burdick

Kwong Wah Lai

Yamin Wang

Harold C E Kluender

Qingjie Liu

Yong Tang

Joseph P Lyssikatos

Fei Wang

Ann-Marie Campbell

Huifen Chen

Michael Charles Hewitt

Martin Duplessis

Michael Siu

Kyle E Parcella

Steven F Bellon

Shumei Wang

Lan Wang

Jason S Newcom

Zhenqiu Hong

Sarah Bronner

Wendy Liu

Roger Astbury Smith

Jacques P Dumas

Victor S Gehling

Chudi Obioma Ndubaku

Kevin X Chen

Gaetan H Ladouceur

Zheng Liu

Simon Charles Goodacre

Karen Williams

Derek B Lowe

Sidney Xi Liang

Aihe Zhou

Quanrong Shen

Les A Dakin

Yingjie Lai

Yves Leblanc

Wendy Lee

Christopher Hurley

Benjamin Jones

Eric Mull

Jill E Wood

Tatiana Shelekhin

David Gunn

Emily J Hanan

Vickie H Tsui

Jianmei Fan

Paul Gibbons

Mark S Stanley

Calum MacLeod

Thomas E Rawson

Ning Miao Su

Martin Michels

Calum Macleod

Toby Jonathan Blench

Robert Dean Dally

Ming Wang

Holia Hatoum-Mokdad

Philip L Wickens

Joachim Rudolph

Libing Chen

Miao Dai

Samuel J Danishefsky

Dhanapalan Nagarathnam

Jean-Christophe P Harmange

Manoj Patel

Andreas Stolle

Mark Edward Zak

Xin Ma

Kirk D Robarge

Neal Rosen

Rohan V Mendonca

Laura Sepp-Lorenzino

James H Cook, Ii

Alexandre Côté

Steven Elliot Kauder

Dyuti Majumdar

Philip D G Coish

Ann-Marie Bullion

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 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.

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 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.

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.

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Dublin, CA, United States of America

Steven R Magnuson