Abstract: The present disclosure relates to bifunctional compounds, which find utility to degrade and (inhibit) Androgen Receptor. In particular, the present disclosure is directed to compounds, which contain on one end a cereblon ligand which binds to the E3 ubiquitin ligase and on the other end a moiety which binds Androgen Receptor, such that Androgen Receptor is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of Androgen Receptor. The present disclosure exhibits a broad range of pharmacological activities associated with compounds according to the present disclosure, consistent with the degradation/inhibition of Androgen Receptor.
Type:
Grant
Filed:
October 11, 2017
Date of Patent:
March 10, 2020
Assignee:
Arvinas, Inc.
Inventors:
Andrew P. Crew, Lawrence B. Snyder, Jing Wang
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.
Type:
Grant
Filed:
August 10, 2015
Date of Patent:
September 11, 2018
Assignees:
Yale University, Arvinas, Inc.
Inventors:
Andrew Crew, Craig Crews, Hanqing Dong, Eunhwa Ko, Jing Wang
Abstract: The present invention relates to bifunctional compounds, which find utility to degrade and (inhibit) TBK 1. In particular, the present invention is directed to compounds, which contain on one end an E3 ubiquitin ligase binding moiety which binds to an E3 ubiquitin ligase and on the other end a moiety which binds TBK1 such that TBK1 is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of TBK1. The present invention exhibits a broad range of pharmacological activities associated with compounds according to the present invention, consistent with the degradation/inhibition of TBK1.
Type:
Application
Filed:
June 6, 2016
Publication date:
May 31, 2018
Applicant:
Arvinas, Inc.
Inventors:
Andrew P. Crew, Jing Wang, Hanqing Dong, Yimin Qian, Craig M Crews