Dana-farber-cancer Institute Inc.

Jie Jiang

Tinghu Zhang

Nathanael Schiander Gray

Nicholas Paul Kwiatkowski

Nathanael S Gray

Eric S Fischer

Zhixiang He

Guangyan Du

Katherine Donovan

Mingfeng Hao

Mingxing Teng

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

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

The present disclosure provides compounds of Formula (I), and pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled derivatives, and prodrugs thereof. The compounds of the present disclosure are inhibitors of kinases (e.g., a cyclin-dependent kinase (CDK) (e.g., CDK7)). The compounds may be selective for inhibiting the activity of a kinase (e.g., CDK7) over certain other kinases (e.g., CDK2, CDK9, CDK12). Also provided are pharmaceutical compositions, kits, methods of use, and uses that involve the compounds. The compounds may be useful in inhibiting the activity of a kinase, down-regulating the transcription of MYC or MCL-1, inhibiting the growth of a cell, inducing apoptosis of a cell, treating a disease, and/or preventing a disease (e.g., proliferative disease, cystic fibrosis).

Inhibitors of cyclin-dependent kinase 7 and uses thereof

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Brookline, MA, United States of America

Jie Jiang