Meizhong Jin,Andrew P. Crew,Hanqing Dong,Jing Wang,Kam Siu,Caterina Ferraro,Xin Chen,Yimin Qian
申请号:
US15002303
公开号:
US20160214972A1
申请日:
2016.01.20
申请国别(地区):
US
年份:
2016
代理人:
摘要:
The present invention relates to bifunctional compounds, which find utility to degrade and (inhibit) Androgen Receptor. 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 Androgen Receptor such that Androgen Receptor is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of Androgen Receptor. The present invention exhibits a broad range of pharmacological activities associated with compounds according to the present invention, consistent with the degradation/inhibition of Androgen Receptor.