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DEGRADATION OF PROTEIN KINASES BY CONJUGATION OF PROTEIN KINASE INHIBITORS WITH E3 LIGASE LIGAND AND METHODS OF USE
专利权人:
Dana-Farber Cancer Institute; Inc.
发明人:
Nathanael S. GRAY,James BRADNER,Li TAN,Hai-Tsang HUANG,Dennis BUCKLEY,Georg WINTER,Mette Ishoey ROSENBAUM
申请号:
US16343973
公开号:
US20190374528A1
申请日:
2017.11.10
申请国别(地区):
US
年份:
2019
代理人:
摘要:
The present application provides bifunctional compounds of Formula (I):or an enantiomer, diastereomer, or stereoisomer thereof, or pharmaceutically acceptable salt, hydrate, solvate, or prodrug thereof, which act as protein degradation inducing moieties for protein kinases (e.g., Bcr-Abl). The present application also relates to methods for the targeted degradation of one or more protein kinases through the use of the bifunctional compounds that link a ubiquitin ligase-binding moiety to a ligand that is capable of binding to one or more protein kinases which can be utilized in the treatment of disorders modulated by protein kinases.
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