CREW, ANDREW P.,ZIMMERMANN, KURT,WANG, JING,BERLIN, MICHAEL,DONG, HANQING,ISHCHENKO, ALEXEY,QIAN, YIMIN,CREWS, CRAIG M.,JAIME-FIGUEROA, SAUL,BURSLEM, GEORGE
申请号：
CA3047586
公开号：
CA3047586A1
申请日:
2017.12.22
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 receptor tyrosine kinase (RTK) proteins. In particular, the present disclosure is directed to bifunctional compounds, which contain on one end a ligand which binds to an E3 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 effectuate ubiquitination, and therefore, degradation (and inhibition) of the target protein. The present disclosure exhibits a broad range of pharmacological activities associated with degradation/inhibition of target protein. Diseases or disorders that result from aggregation or accumulation of the target protein are treated or prevented with compounds and compositions of the present disclosure.
