Invention Grant
- Patent Title: Estrogen-related receptor alpha based protac compounds and associated methods of use
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Application No.: US14822309Application Date: 2015-08-10
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Publication No.: US10071164B2Publication Date: 2018-09-11
- Inventor: Andrew Crew , Craig Crews , Hanqing Dong , Eunhwa Ko , Jing Wang
- Applicant: Yale University , Arvinas, Inc.
- Applicant Address: US CT New Haven US CT New Haven
- Assignee: Yale University,Arvinas, Inc.
- Current Assignee: Yale University,Arvinas, Inc.
- Current Assignee Address: US CT New Haven US CT New Haven
- Agency: Saul Ewing Arnstein & Lehr LLP
- Agent Kathryn Doyle; Domingos J. Silva
- Main IPC: C07K5/062
- IPC: C07K5/062 ; C07K5/097 ; A61K45/06 ; A61K31/427 ; A61K31/426 ; A61K38/00 ; A61K47/48

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
- US20160045607A1 ESTROGEN-RELATED RECEPTOR ALPHA BASED PROTAC COMPOUNDS AND ASSOCIATED METHODS OF USE Public/Granted day:2016-02-18
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