Dana-Farber-Cancer Institute Inc.

Eric S Fischer

Nathanael Schiander Gray

Tinghu Zhang

Radoslaw Nowak

Katherine Donovan

Guangyan Du

Zhixiang He

Jing Ting Christine Yuan

Alyssa Verano

Hojong Yoon

Tyler Faust

Hu Liu

Nicholas Paul Kwiatkowski

Nathanael S Gray

David A Scott

Calla M Olson

Jie Jiang

Yao Liu

Brian Groendyke

Nathaniel Henning

Eric Wang

Quan Cai

Shourya Sonkar Roy Burman

Mingxing Teng

Zhengnian Li

Benika J Pinch

Nozhat Safaee

The present invention relates to bifunctional compounds, compositions, and methods for treating diseases or conditions mediated by dysfunctional cyclin-dependent kinase 2 (CDK2) and CDK5 activity.

CDK2/5 degraders and uses thereof

Described herein are compositions and methods for modulating protein abundance in a target-specific manner via degron tags.

Protein tag to induce ligand dependent degradation of protein/protein-fusions

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 are bifunctional compounds (degraders) that target Wee1 tyrosine kinase for degradation. Also disclosed are pharmaceutical compositions containing the degraders and methods of using the compounds to treat disease.

Degraders of WEE1 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 and pharmaceutically acceptable salts and stereoisomers thereof that may cause degradation of various proteins e.g., IKZF2 (Helios). Also disclosed are pharmaceutical compositions containing same, and methods of making and using the compounds to treat diseases and disorders characterized or mediated by aberrant protein activity.

Small molecule degraders of Helios and methods of use

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

DCAF15 is a substrate recognition (adaptor) protein of E3 ubiquitin ligase. Disclosed herein are compounds that recruit ubiquitin ligase CRL4, to a target RNA recognition motif (RRM), causing its degradation. Also disclosed herein are compositions and methods of use in treating associated disorders and diseases.

Sulfonamide derivatives for protein degradation

The present invention relates to compounds, compositions and methods for treating diseases or conditions mediated by proteins of the SWI/SNF chromatin-remodeling complex, including PB1.

Small molecule degraders of polybromo-1 (PBRM1)

Disclosed are heterobifunctional compounds that effectuate selective degradation of a target protein, and which include a targeting ligand that binds a target protein and at least one other protein, a ligand that binds an E3 ubiquitin ligase or a component of E3 ubiquitin ligase, and a specificity modulating linker that links the first ligand and the second ligand. Pharmaceutical compositions containing the compounds, and methods of using and making the compounds are also disclosed.

Growing community of inventors

Newton, MA, United States of America

Eric S Fischer