Invention Grant
- Patent Title: Compounds and methods for the enhanced degradation of targeted proteins
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Application No.: US15074820Application Date: 2016-03-18
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Publication No.: US10730870B2Publication Date: 2020-08-04
- Inventor: Andrew P. Crew , Craig M. Crews , Xin Chen , Hanqing Dong , Caterina Ferraro , Yimin Qian , Kam Siu , Jing Wang , Meizhong Jin , Michael Berlin , Kurt Zimmermann , Lawrence Snyder
- Applicant: Arvinas, 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: Cantor Colburn LLP
- Agent Bryan D. Zerhusen, Esq.; Nicholas R. Herrel, Esq.
- Main IPC: C07D521/00
- IPC: C07D521/00 ; C07D471/04 ; C07D417/14 ; A61K45/06 ; C07D417/12 ; C07D403/06 ; C07D403/14 ; C07D401/14 ; C07D413/14 ; C07D405/14 ; C07D495/04

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
- US20160272639A1 COMPOUNDS AND METHODS FOR THE ENHANCED DEGRADATION OF TARGETED PROTEINS Public/Granted day:2016-09-22
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