Millennium Pharmaceuticals Limited

Genentech, Inc.

Cor Therapeutics, Inc.

F. Hoffmann-La Roche Ag

Hoffmann-La Roche Inc.

Portola Pharmaceuticals, Inc.

Piramed Limited

Constellation Pharmaceuticals, Inc.

Hoffman-Laroche, Inc. (US Only)

F. Hoffman-Laroche, Ag (Ex-US)

Bing-Yan Zhu

Robert M Scarborough

Yonghong Song

Wenrong Huang

Daniel P Sutherlin

Alan G Olivero

Adrian Folkes

Penglie Zhang

Tim Heffron

Erick A Goldman

Richard A Goldsmith

Zhaozhong Jon Jia

Georgette M Castanedo

Charles K Marlowe

Lingyan Wang

Irina Chuckowree

Nan Chi Wan

Simon Mathieu

Wenhao Li

Tracy Bayliss

Jingmei Zuckett

Steven T Staben

Shumei Wang

Janet Gunzner

Sally Oxenford

Michael Siu

Steven R Magnuson

Shawn M Bauer

Richard Pastor

Jennafer Dotson

Ting Su

Joseph P Lyssikatos

Jun Liang

Steven Huy Do

Aleksandr Kolesnikov

Uma Sinha

Gary D Probst

Kimberly Malesky

Alan M Laibelman

Wendy Liu

Yanchen Zhang

Paul Goldsmith

Neil Pegg

James P Kanter

Vickie H Tsui

Thomas E Rawson

Aihe Zhou

Jason R Zbieg

Kim A Kane-Maguire

Zheng Jifu

Xu Xing

Zhao Junping

Lisa Marie Barton

He Haiying

Xiao Yisong

Christian Wiesmann

Christopher Hurley

Emily J Hanan

Paul Gibbons

Vishal Verma

Stephen Joseph Shuttleworth

Ramsay Beveridge

Terry Crawford

Alexandre Cote

Tim Hancox

Stephen Shuttleworth

Marie Anne Evangelista

Paul Powell Beroza

Lane Clizbe

Samir Bouayad-Gervais

Russell Tyler Smith

Anwesha Dey

Willy Teng

Fei Wang

Brian K Albrecht

Brian Salvatore Safina

F Anthony Romero

Xiaojing Wang

Kevin X Chen

Timothy Heffron

Alexander M Taylor

Vickie Hsiao-Wei Tsui

Birong Zhang

Mark Edward Zak

Matthias Rueth

Rohan V Mendonca

Kwong Wah Lai

Jun M Li

Alexandre Côté

Robin Larouche-Gauthier

Steven Elliot Kauder

Malcolm Huestis

Sarah Bronner

Ignacio Aliagas-Martin

Patrick Cyr

Jeremy M Murray

Jiangpeng Liao

Jason S Halladay

Liang Zhao

Marc Adler

This disclosure relates to compounds and methods of using said compounds, as well as pharmaceutical compositions containing such compounds, for treating diseases and conditions mediated by TEAD, such as cancer.

Therapeutic compounds and methods of use

A compound, of formula (I): suitable for treating a cancer wherein the cancer is susceptible to inhibition of Cbl-B.

Lactams as CBL-B inhibitors selective over C-CBL

Pyrazolo compounds and methods of use thereof

Novel benzamide compounds including their pharmaceutically acceptable isomers, salts, hydrates, solvates and prodrug derivatives having activity against mammalian factor Xa are described. Compositions containing such compounds are also described. The compounds and compositions are useful in vitro or in vivo for preventing or treating coagulation disorders.

Benzamides and related inhibitors of factor Xa

Compounds of Formulae Ia, and stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting lipid kinases including PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formula Ia for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed. 

Pharmaceutical compounds

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.

Therapeutic compounds and uses thereof

Benzamides and related inhibitors of factor XA

Compounds of Formulas Ia-d where X is S or O, mor is a morpholine group, and Ris a monocyclic heteroaryl group, and including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for modulating the activity of lipid kinases including PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formula Ia-d for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed. 

Phosphoinositide 3-kinase inhibitor compounds and methods of use

A compound of Formula I, enantiomers, diasteriomers, tautomers or pharmaceutically acceptable salts thereof, wherein R, R, R, Rand Rare defined herein, are useful as JAK kinase inhibitors. A pharmaceutical composition that includes a compound of Formula I and a pharmaceutically acceptable carrier, adjuvant or vehicle, and methods of treating or lessening the severity of a disease or condition responsive to the inhibition of JAK kinase activity in a patient are disclosed. 

Triazolopyridine JAK inhibitor compounds and methods

Benzopyran and benzoxepin compounds of Formulas I and II, and including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting lipid kinases including p110 alpha and other isoforms of PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formulas I and II for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed. 

Benzopyran and benzoxepin PI3K inhibitor compounds and methods of use

A compound of Formula I, enantiomers, diasteriomers, tautomers or pharmaceutically acceptable salts thereof, wherein R, Rand Rare defined herein, are useful as inhibitors of one or more Janus kinases. A pharmaceutical composition that includes a compound of Formula I and a pharmaceutically acceptable carrier, adjuvant or vehicle, and methods of treating or lessening the severity of a disease or condition responsive to the inhibition of a Janus kinase activity in a patient are disclosed. 

Pyrazolopyrimidine JAK inhibitor compounds and methods

Compounds of Formula I, and including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting lipid kinases including p110 alpha and other isoforms of PI3K, and for treating disorders such as cancer mediated by lipid kinases. 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. 

Pyrazolopyrimidine PI3K inhibitor compounds and methods of use

Growing community of inventors

Palo Alto, CA, United States of America

Bing-Yan Zhu