Dana-farber-cancer Institute Inc.

Cornell University

The University of Texas System

Children's Medical Center Corporation

Guangyan Du

Tinghu Zhang

Nathanael Schiander Gray

Eric S Fischer

Katherine Donovan

Zhixiang He

Radoslaw Nowak

Jing Ting Christine Yuan

Nathanael S Gray

Alyssa Verano

John M Hatcher

David A Scott

Ari Matthew Melnick

Lorena Fontan Gabas

Nathaniel Henning

Nicholas Paul Kwiatkowski

Kenneth Dale Westover

Jie Jiang

Hao Wu

Hu Liu

Qi Qiao

Suman Rao

Deepak Gurbani

Nozhat Safaee

Spandan Chennamadhavuni

Disclosed are bispecific compounds (degraders) that target CDK7 for degradation. Also disclosed are pharmaceutical compositions containing the degraders and methods of using the compounds to treat disease.

Degraders of cyclin-dependent kinase 7 (CDK7) and uses thereof

Disclosed are bifunctional compounds, pharmaceutical compositions containing them, and methods of making and using them to treat diseases and disorders characterized by aberrant protein activity wherein the protein is targeted for degradation by KEAP1 and the Cul3-based E3-ubiquitin ligase complex.

Degraders that target proteins via KEAP1

Disclosed herein are compounds of Formula (I) and pharmaceutically acceptable salts thereof. Also disclosed herein are methods of using the compounds of Formula (I) in the treatment of certain diseases (e.g., cancer).

Small molecule inhibitors of SRC tyrosine kinase

Disclosed are immunomodulatory compounds, pharmaceutical compositions containing them, and methods of making and using the compounds to treat diseases and disorders characterized by aberrant protein activity that can be targeted by cereblon.

Immunomodulatory compounds

Disclosed are compounds with immunomodulatory activity, methods of making the compounds, pharmaceutical compositions containing the compounds, and methods of using the compounds to treat diseases or disorders characterized or mediated by dysfunctional protein activity.

Ligands to cereblon (CRBN)

Disclosed are degraders, pharmaceutical compositions containing them, and methods of making and using the degraders to treat diseases and disorders characterized by aberrant protein activity that can be targeted by cereblon.

Bispecific degraders

Disclosed are degraders, pharmaceutical compositions containing them, and methods of making and using the degraders to treat diseases and disorders characterized by dysregulated or dysfunctional protein activity that can be targeted by cereblon.

CRBN modulators

Provided herein are compounds of Formula (I) and pharmaceutical compositions thereof, which may be useful as MALT1 inhibitors. Also provided are for the treatment of proliferative disorders (e.g., cancer (e.g., non-Hodgkin's lymphoma, diffuse large B-cell lymphoma, MALT lymphoma), benign neoplasm, a disease associated with angiogenesis, an autoimmune disease, an inflammatory disease, an autoinflammatory disease) by administering a compound of Formula (I). 

MALT1 inhibitors and uses thereof

Provided herein are bifunctional compounds that inhibit MALT1 and/or promote targeted ubiquitination for the degradation of MALT1. In particular, provided are compounds that can bind MALT1, a protein whose activity is responsible for constitutive NF-KB signaling in certain cancers (e.g., activated B-cell diffuse large B-cell lymphoma (ABC-DLBCL)), and can assist in its degradation by recruiting an E3 ubiquitin ligase (e.g., Cereblon, VHL), which can ubiquitinate MALT1, marking it for proteasome degradation. Also provided are pharmaceutical compositions comprising the bifunctional compounds, methods of treating cancer with the bifunctional compounds, methods of promoting the degradation of MALT1, and methods of binding E3 ubiquitin ligase activity in a subject by administering a compound or composition described herein.

Compounds for MALT1 degredation

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Jamaica Plain, MA, United States of America

Guangyan Du