CREW, ANDREW P.,BERLIN, MICHAEL,FLANAGAN, JOHN J.,DONG, HANQING,ISHCHENKO, ALEXEY
申请号:
CA3042260
公开号:
CA3042260A1
申请日:
2017.11.01
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 as modulators of tau protein. In particular, the present disclosure is directed to bifunctional compounds, which contain on one end a VHL or cereblon ligand which binds to the E3 ubiquitin ligase and on the other end a moiety which binds tau protein, such that tau protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of tau. The present disclosure exhibits a broad range of pharmacological activities associated with degradation/inhibition of tau protein. Diseases or disorders that result from aggregation or accumulation of tau protein are treated or prevented with compounds and compositions of the present disclosure.