Invention Grant
- Patent Title: Degradation of Bruton's tyrosine kinase (BTK) by conjugation of BTK inhibitors with E3 ligase ligand and methods of use
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Application No.: US16963993Application Date: 2019-01-29
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Publication No.: US11712458B2Publication Date: 2023-08-01
- Inventor: Nathanael S. Gray , Jinhua Wang , Dennis Dobrovolsky
- 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: Burns & Levinson, LLP
- Agent Daniel W. Clarke; Shawn P. Foley
- International Application: PCT/US2019/015505 2019.01.29
- International Announcement: WO2019/148150A 2019.08.01
- Date entered country: 2020-07-22
- Main IPC: A61K38/05
- IPC: A61K38/05 ; A61K47/62 ; A61K47/54

Abstract:
The present application provides bifunctional compounds of Formula X or an enantiomer, diastereomer, or stereoisomer thereof, or pharmaceutically acceptable salt, hydrate, solvate, or prodrug thereof, which act as protein degradation inducing moieties for Bruton's tyrosine kinase (BTK). The present application also relates to methods for the targeted degradation of BTK through the use of bifunctional compounds that link a ubiquitin ligase-binding moiety to a ligand that is capable of binding to BTK which can be utilized in the treatment of disorders modulated by BTK.
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