Invention Grant
- Patent Title: Compounds and methods for the targeted degradation of bromodomain- containing proteins
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Application No.: US18052096Application Date: 2022-11-02
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Publication No.: US12171831B2Publication Date: 2024-12-24
- Inventor: Yimin Qian , Hanqing Dong , Jing Wang , Michael Berlin , Andrew P. Crew , Craig M. Crews
- Applicant: Arvinas Operations, Inc. , YALE UNIVERSITY
- Applicant Address: US CT New Haven; US CT New Haven
- Assignee: Arvinas Operations, Inc.,YALE UNIVERSITY
- Current Assignee: Arvinas Operations, Inc.,YALE UNIVERSITY
- Current Assignee Address: US CT New Haven; US CT New Haven
- Agency: Lathrop GPM LLP
- Agent Brian C. Trinque
- Main IPC: C07D417/14
- IPC: C07D417/14 ; A61K45/06 ; A61K47/55 ; A61P35/00 ; C07D495/14 ; C07D519/00

Abstract:
The present invention relates to bifunctional compounds, which find utility as modulators of targeted ubiquitination, especially inhibitors of a variety of polypeptides and other proteins which are degraded and/or otherwise inhibited by bifunctional compounds according to the present invention. In particular, the present invention is directed to compounds, which contain on one end a VHL ligand which binds to the ubiquitin ligase and on the other end a moiety which binds a target protein such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of that protein. The present invention exhibits a broad range of pharmacological activities associated with compounds according to the present invention, consistent with the degradation/inhibition of targeted polypeptides.
Public/Granted literature
- US20230263893A1 COMPOUNDS AND METHODS FOR THE TARGETED DEGRADATION OF BROMODOMAIN-CONTAINING PROTEINS Public/Granted day:2023-08-24
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