Genentech, Inc.

Array Biopharma Inc.

Newlink Genetics Corporation

Genetech, Inc.

F. Hoffmann-La Roche Ag

Curis, Inc.

Lewis J Gazzard

John A Flygare

Bryan K Chan

Timothy Heffron

Frederick Cohen

Vickie Hsiao-Wei Tsui

Emanuela Gancia

Rohan V Mendonca

Huifen Chen

Andrew Madin

Jun Liang

Eileen Mary Seward

Michael Siu

Sushant Malhotra

Michael Lainchbury

Yonghan Hu

Joy Drobnick

John Tellis

Joseph P Lyssikatos

BinQing Wei

Binqing Wei

Samuel S Kintz

Jacob Bradley Schwarz

Weiru Wang

Craig Stivala

Kin Chiu Fong

Matthew W Cartwright

David Favor

Andrew Good

James F Blake

David A Moreno

Graham Elgin Jones

Peter J Mohr

Aihe Zhou

Naomi S Rajapaksa

Kurt Deshayes

Adam Wade Cook

Li Ren

John Joseph Gaudino

Zhonghua Pei

Hazel Joan Dyke

Bainian Feng

Andrew T Metcalf

Kevin W Hunt

Richard Pastor

Wayne J Fairbrother

Brad Newhouse

Simon Charles Goodacre

Indrani W Gunawardana

Calum MacLeod

Karen Williams

Michael Lyon

Charles Ellwood

Jane Schmidt

Brendan Parr

Peter Scott Dragovich

Mark Joseph Chicarelli

Thomas Pillow

Tony P Tang

Steven T Staben

Po-Wai Yuen

Firoz Jaipuri

Emily J Hanan

Sanjeev Kumar

Guosheng Wu

Michael F T Koehler

Aijun Lu

Allen A Thomas

Malcolm Huestis

Baihua Hu

Blake Daniels

Hans Purkey

Hima Potturi

Lan Wang

Jesse Waldo

Thomas E Rawson

Calum Macleod

Wendy Liu

Xingyu Lin

Eli M Wallace

Steven Huy Do

Chudi Obioma Ndubaku

Kirk D Robarge

Erik James Hicken

David Y Jackson

Elisia Villemure

Nicole Blaquiere

Terry Kellar

Rustam Ferdinand Garrey

Robert J Kaus

Edward HyungSuk Ha

Benjamin Douglas Sellers

Christopher Stephen Siedem

Jim Blake

Jianfeng Xin

Robert Anthony Blake

Samantha Alyson Green

Yanyan Chu

Pete Mohr

Jason Demeese

3-Carbonylaminoisoquinoline compounds of formula (I): variations thereof, 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 3-carbonylaminoisoquinoline compounds.

Isoquinoline compounds for the treatment of cancer

Isoquinoline compounds of formula (I): variations thereof, 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.

Isoquinoline compounds and uses thereof

Provided herein are aza-tetracyclic oxazepinyl compounds useful in the treatment of cancers.

Aza-tetracyclic oxazepine compounds and uses thereof

Naphthyridine compounds and uses thereof

The present disclosure relates to compounds and salts thereof that are useful for inhibiting target polypeptides and proteins, in particular, bromodomain (e.g., BRD4) proteins. Also disclosed are pharmaceutical compositions comprising the compounds, or a salt (e.g., a pharmaceutically acceptable salt) thereof, and methods of using such compounds and salts in the treatment of various bromodomain-mediated diseases or disorders.

Tert-butyl (s)-2-(4-(phenyl)-6H-thieno[3, 2-f][1, 2, 4]triazolo[4, 3-a] [1,4]diazepin-6-yl) acetate derivatives and related compounds as bromodomain BRD4 inhibitors for treating cancer

Novel inhibitors of IAP that are useful as therapeutic agents for treating malignancies and have the general formula I: wherein R, R, R, R, Rand Rare as described herein.

Inhibitors of IAP

Azaindole 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 azaindole compounds.

Azaindoles as inhibitors of HPK1

Presently provided are inhibitors of TD02 and IDO1 and pharmaceutical compositions thereof, useful for modulating an activity of tryptophan 2,3 dioxygenase and indoleamine 2,3-dioxygenase 1; treating immunosuppression; treating a medical conditions that benefit from the inhibition of tryptophan degradation; enhancing the effectiveness of an anti-cancer treatment comprising administering an anti-cancer agent; and treating tumor-specific immunosuppression associated with cancer.

TDO2 and IDO1 inhibitors

3-Carbonylamino-8-aminoisoquinoline compounds of formula (I): variations thereof, 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 3-carbonylamino-8-aminoisoquinoline compounds.

8-aminoisoquinoline compounds and uses thereof

Presently provided are inhibitors of cellularly expressed TD02 and IDO1, and pharmaceutical compositions thereof, useful for modulating an activity of tryptophan 2,3 dioxygenase and indoleamine 2,3-dioxygenase 1; treating immunosuppression; treating a medical conditions that benefit from the inhibition of tryptophan degradation; enhancing the effectiveness of an anti-cancer treatment comprising administering an anti-cancer agent; and treating tumor-specific immunosuppression associated with cancer. 

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

The present disclosure relates to bifunctional compounds, which can be used as modulators of targeted ubiquitination. In particular, the present disclosure is directed to compounds which contain on one end a VHL ligand moiety, which binds to the VHL E3 ubiquitin ligase, and on the other end a moiety that binds a target protein such that degradation of the target protein/polypeptide is effectuated. Also disclosed are VHL ligands.

(4-hydroxypyrrolidin-2-yl)-heterocyclic compounds and methods of use thereof

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

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Belmont, CA, United States of America

Lewis J Gazzard