YALE UNIVERSITY;GLAXOSMITHKLINE INTELLECTUAL PROPERTY DEVELOPMENT LIMITED;CAMBRIDGE ENTERPRISE LIMITED UNIVERSITY OF CAMBRIDGE
发明人:
Craig M. Crews,Dennis Buckley,Alessio Ciulli,William Jorgensen,Peter C. Gareiss,Inge Van Molle,Jeffrey Gustafson,Hyun-Seop Tae,Julien Michel,Dentin Wade Hoyer,Anke G. Roth,John David Harling,Ian Edwar
申请号：
US14371956
公开号：
US20140356322A1
申请日:
2013.01.11
申请国别(地区):
US
年份:
2014
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 that are degraded and/or otherwise inhibited by bifunctional compounds of the present invention. In particular, the present invention is directed to compounds, which contain on one end a VHL ligand that binds to the ubiquitin ligase and on the other end a moiety that 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 of the present invention, consistent with the degradation/inhibition of targeted polypeptides.
