CREW, ANDREW P.,HORNBERGER, KEITH R.,SNYDER, LAWRENCE B.,ZIMMERMANN, KURT,WANG, JING,BERLIN, MICHAEL,CREWS, CRAIG M.,DONG, HANQING
申请号:
CA3038979
公开号:
CA3038979A1
申请日:
2017.10.11
申请国别(地区):
CA
年份:
2018
代理人:
摘要:
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.