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Compounds and methods for the enhanced degradation of targeted proteins
专利权人:
Inc.;Yale University;Michael Berlin;Arvinas, Inc.;Lawrence Snyder;Arvinas;Kurt Zimmerman
发明人:
Berlin, Michael,Zimmerman, Kurt,Snyder, Lawrence,Crew, Andrew P.,Crews, Craig M.,Chen, Xin,Dong, Hanqing,Ferraro, Caterina,Jin, Meizhong,Qian, Yimin,Siu, Kam,Wang, Jing
申请号:
AU2016232705
公开号:
AU2016232705A1
申请日:
2016.03.18
申请国别(地区):
AU
年份:
2017
代理人:
摘要:
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.
来源网站:
中国工程科技知识中心
来源网址:
http://www.ckcest.cn/home/

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