Invention Grant
- Patent Title: Degradation of cyclin-dependent kinase 9 (CDK9) by conjugation of CDK9 inhibitors with E3 ligase ligand and methods of use
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Application No.: US16094102Application Date: 2017-04-21
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Publication No.: US10532103B2Publication Date: 2020-01-14
- Inventor: Nathanael S. Gray , Tinghu Zhang , Calla M. Olson , Yanke Liang , Nicholas Kwiatkowski
- Applicant: Dana-Farber Cancer Institute, Inc.
- Applicant Address: US MA Boston
- Assignee: Dana-Farber Cancer Institute, Inc.
- Current Assignee: Dana-Farber Cancer Institute, Inc.
- Current Assignee Address: US MA Boston
- Agency: Cooley LLP
- Agent Heidi A. Erlacher; Chen Chen
- International Application: PCT/US2017/028924 WO 20170421
- International Announcement: WO2017/185023 WO 20171026
- Main IPC: A61K47/55
- IPC: A61K47/55 ; A61K31/427 ; A61K31/4523 ; C07D417/14

Abstract:
The present application provides bifunctional compounds of Formula (I): or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof, which act as protein degradation inducing moieties for cyclin-dependent kinase 9 (CDK9), the present application also relates to methods for the targeted degradation of CDK9 through the use of the bifunctional compounds that link a ubiquitin ligase-binding moiety to a ligand that is capable of binding to CDK9 which can be utilized in the treatment of disorders modulated by CDK9.
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