Merck & Company, Inc.

Merck Sharp & Dohme Corporation

Cornell University

Cyteir Therapeutics, Inc.

Cortexyme, Inc.

Yissum Research Development Company of the Hebrew University of Jerusalem Ltd.

Biotheryx, Inc.

Merck + Co., Inc.

Kronos Bio, Inc.

Tabomedex Biosciences, LLC

Other

The Scripps Research Institute

Merck Sharp + Dohme Corp.

Istituto Di Ricerche Di Biologia Molecolare P. Angeletti S.r.l.

Aquinnah Pharmaceuticals, Inc.

Joseph P Vacca

Craig Alan Coburn

Dansu Li

Sarah Bettigole

Casey Cameron McComas

Bruce D Dorsey

Randall W Hungate

Joel R Huff

M Katharine Holloway

Nigel J Liverton

John A McCauley

Shawn J Stachel

David Brian Olsen

John J Baldwin

Alfredo C Castro

Andrei William Konradi

Michael T Rudd

William C Lumma, Jr

Thomas Joseph Tucker

Steven D Young

Philip E Sanderson

Stephen F Brady

Steven W Ludmerer

Harold G Selnick

Mark E Fraley

John S Wai

Ian W Davies

Terry A Lyle

Linda S Payne

Andrew William Stamford

F George Njoroge

Ian M Bell

Qun Dang

Frank W Bennett

Stephane L Bogen

Jinlong Jiang

Daniel Vincent Paone

Christopher S Burgey

Philippe G Nantermet

Fa-Xiang Ding

Dmitri A Pissarnitski

Vinay M Girijavallabhan

Shuzhi Dong

Takao Suzuki

Vishal Verma

Diem N Nguyen

Roger M Freidinger

Linghang Zhuang

Andrew Stewart Tasker

Alexander Pasternak

Melissa S Egbertson

Ashok Arasappan

Craig A Stump

James C Barrow

Laurie H Glimcher

Ying Huang

Shaun R Stauffer

Michael H Serrano-Wu

Jean-Marc Lapierre

Vincenzo Summa

C Blair Zartman

Xin Gu

Steven N Gallicchio

Cory R Theberge

Mark W Embrey

Dong-Mei Feng

Latha G Nair

Charles J McIntyre

Hemaka Anthony Rajapakse

Zhengwu James Deng

Thorsten E Fisher

Julio Cesar Medina

Matthew G Stanton

Gerald S Ponticello

Hao Wu

Theresa M Williams

Robert W Sullivan

Kun Liu

Bin Hu

Kyle W H Chan

Frank Mercurio

Juan Carlos Jaen

S Jane deSolms

Paul E Erdman

Maria Emilia Di Francesco

Huw M Nash

Leah M Fung

Peter D Williams

Anthony W Shaw

Fei Sun

Wayne J Thompson

Richard Soll

Jose Alexander

Donnette D Staas

Jules A Shafer

Jian Zhu

Matthew D Disney

David Louis Clark

Joseph J Romano

David Allen Annis

Provided herein are small molecule inhibitors for the targeting or IRE1 protein family members. Binding may be direct or indirect. Further provided herein are methods of using IRE1 small molecule inhibitors for use in treating or ameliorating cancer in a subject. Moreover, IRE1 small molecule inhibitors described herein are for the treatment of cancer, where the cancer is a solid or hematologic cancer.

IRE1 small molecule inhibitors

Provided herein are heteroaryl compounds, for example, a compound of Formula I or IA, and pharmaceutical compositions thereof. Also provided herein are methods of their use for treating, ameliorating, or preventing one or more symptoms of a disorder, disease, or condition mediated by a casein kinase 1 (CK1), an interleukin-1 receptor associated kinase (IRAK1), or a cyclin-dependent kinase 9 (CDK9).

Heteroaryl compounds, pharmaceutical compositions thereof, and their therapeutic use

This application is directed to inhibitors of RAD51 represented by the following structural formula, and methods for their use, such as to treat pancreatic cancer.

Methods of using RAD51 inhibitors for treatment of pancreatic cancer

The present invention provides pyrazole derivatives, e.g., a compound of Formula (I), and their uses in methods of treating malignant disease and disorders and methods for treating inflammatory diseases and disorders.

Pyrazole compounds and uses thereof

This application is directed to inhibitors of RAD51 represented by the following structural formula, and methods for their use, such as to treat cancer, autoimmune diseases, immune deficiencies, or neurodegenerative diseases.

RAD51 inhibitors

The present invention provides pyrazole pyrimidine derivatives which inhibit Casein kinase I (CKI) and/or Interleukin-1 receptor-associated kinase 1 (IRAKI) and methods of their manufacture, compositions comprising them and uses thereof in methods of treating malignant disease and disorders and methods for treating inflammatory diseases and disorders.

Pyrazole pyrimidine derivative and uses thereof

Inhibitors of CDK9 that are pyrazolo[1,5-a]pyrimidine derivatives and salts thereof, corresponding to formula (I):

Substituted pyrazolo[1,5-a]pyrimidines for modulating CDK9 activity

This application is directed to inhibitors of RAD51 represented by the following structural formula: in combination with a PARP inhibitor, and methods for their use, such as to treat cancer, autoimmune diseases, immune deficiencies, or neurodegenerative diseases.

Combinations of RAD51 and PARP inhibitors

Herein, compounds, compositions and methods for modulating inclusion formation and stress granules in cells related to the onset of neurodegenerative diseases, musculoskeletal diseases, cancer, ophthalmological diseases, and viral infections are described.

Compounds, compositions and methods of use

The present invention relates generally to therapeutics targeting the bacterium, including its protease Lysine gingipain (Kgp), and their use for the treatment of disorders associated withinfection, including brain disorders such as Alzheimer's disease. In certain embodiments, the invention provides compounds according to Formula I, as described herein, and pharmaceutically acceptable salts thereof. 

Inhibitors of lysine gingipain

Growing community of inventors

Telford, PA, United States of America

Joseph P Vacca