Genentech, Inc.

Array Biopharma Inc.

F. Hoffmann-la Roche Ag

Genetech, Inc.

Hoffman-laroche, Inc. (us Only)

F. Hoffman-laroche, Ag (ex-us)

Aihe Zhou

Kirk D Robarge

Huifen Chen

Jun Liang

Mark Joseph Chicarelli

John Joseph Gaudino

Jacob Bradley Schwarz

James F Blake

Li Ren

David A Moreno

Lewis J Gazzard

Richard Pastor

Peter J Mohr

Bing-Yan Zhu

Andrew Madin

Bryan K Chan

Steven R Magnuson

BinQing Wei

Timothy Heffron

Michael Siu

Sushant Malhotra

Emanuela Gancia

Craig Stivala

Joseph P Lyssikatos

Daniel P Sutherlin

John A Flygare

Alan G Olivero

Dean R Artis

Yan Zhu

Birong Zhang

Brian Salvatore Safina

Christopher Hurley

Thomas E Rawson

Rohan V Mendonca

Jonas Grina

Rustam Ferdinand Garrey

Michael Lainchbury

Weiru Wang

Kin Chiu Fong

Naomi S Rajapaksa

Matthew W Cartwright

John Tellis

Andrew Good

Ignacio Aliagas-Martin

David Favor

Aijun Lu

Regina A Munroe

Mark S Stanley

Binqing Wei

Joy Drobnick

Yonghan Hu

Graham Elgin Jones

Richard A Goldsmith

Emily J Hanan

Paul Gibbons

Malcolm Huestis

Blake Daniels

Baihua Hu

Michael S Dina

Kenneth J Weese

Vickie Hsiao-Wei Tsui

Mark Edward Zak

Simon Charles Goodacre

Karen Williams

Matthias Rueth

Jun M Li

Jennafer Dotson

Wendy Liu

Yingjie Lai

Jason S Halladay

Jim Blake

Pete Mohr

Michael Prime

Frederick Brookfield

Jeffrey Blaney

Sam Kintz

Paul A Gibbons

Naomi Rajapaksa

Isoquinoline compounds and their use as inhibitors of HPK1 (hematopoietic kinase 1) are described. The compounds are useful in treating HPK1-dependent disorders and enhancing an immune response. Also described are methods of inhibiting HPK1, methods of treating HPK1-dependent disorders, methods for enhancing an immune response, and methods for preparing the isoquinoline compounds.

Isoquinolines as inhibitors of HPK1

Naphthyridine compounds and their use as inhibitors of HPK1 are described. The compounds are useful in treating HPK1-dependent disorders and enhancing an immune response. Also described are methods of inhibiting HPK1, methods of treating HPK1-dependent disorders, methods for enhancing an immune response, and methods for preparing the naphthyridine compounds.

Naphthyridines as inhibitors of HPK1

Compounds of Formula I or a stereoisomer, tautomer, prodrug or pharmaceutically acceptable salt thereof are provided, which are useful for the treatment of hyperproliferative, pain and inflammatory diseases. Methods of using compounds of Formula I or a stereoisomer, tautomer, prodrug or pharmaceutically acceptable salt thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed. 

Serine/threonine kinase inhibitors

Compounds having the formula I wherein R, X and Z as defined herein are inhibitors of ERK kinase. Also disclosed are compositions and methods for treating hyperproliferative disorders. 

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

The invention provides JAK kinase inhibitors of Formula Ia, enantiomers, diasteriomers or pharmaceutically acceptable salts thereof, wherein R, R, Rand Z are defined herein, a pharmaceutical composition that includes a compound of Formula Ia 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 JAK kinase activity in a patient. 

The invention provides compounds of Formula I, stereoisomers or pharmaceutically acceptable salts thereof, wherein A, B, D, R, R, Rand Rare defined herein, a pharmaceutical composition that includes a compound of Formula I and methods of use thereof. 

Janus kinase inhibitor compounds and methods

The invention provides novel kinase inhibitors that are useful as therapeutic agents for example in the treatment malignancies where the compounds have the general formula I wherein A, X, Y, Z, Ra, Rb, Rc, R, R, Rand m are defined herein.

Pentacyclic kinase inhibitors

Compounds having the structure shown below are useful to inhibit serine protease enzymes, such as TF/factor VIIa, factor Xa, thrombin and kallikrein. These compounds may be used in methods of preventing and/or treating clotting disorders.

Serine protease inhibitors

Compounds having the structure shown below wherein A, B, N , N , X, Y, Q, R , R and R are as defined herein are useful to inhibit serine protease enzymes, such as TF/factor VIIa factor Xa, thrombin and kallikrein. These compounds may be used in methods of preventing and/or treating clotting disorders.

Growing community of inventors

San Jose, CA, United States of America

Aihe Zhou