DEGRADATION DE LA KINASE 8 CYCLINE-DEPENDANTE (CDK8) PAR CONJUGAISON D'INHIBITEURS DE CDK8 AVEC UN LIGAND DE TYPE LIGASE E3 ET LEURS PROCEDES D'UTILISATION
GRAY, NATHANAEL,ZHANG, TINGHU,OLSON, CALLA M.,LIANG, YANKE,KWIATKOWSKI, NICHOLAS
申请号：
CA3020543
公开号：
CA3020543A1
申请日:
2017.04.21
申请国别(地区):
CA
年份:
2017
代理人:
摘要：
The present application provides bifunctional compounds of Formula (la) or (lb): or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof, which act as protein degradation inducing moieties for cyclin-dependent kinase 8 (CDK8). The present application also relates to methods for the targeted degradation of CDK8 through the use of the bifunctional compounds that link a ubiquitin ligase-bindmg moiety to a ligand that is capable of binding to CDK8 which can be utilized in the treatment of disorders modulated by CDK8.
