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MODULATORS OF BTK PROTEOLYSIS AND METHODS OF USE
专利权人:
Yale University
发明人:
Craig M. Crews,Saul Jaime-Figueroa,Momar Toure
申请号:
US16297282
公开号:
US20190276459A1
申请日:
2019.03.08
申请国别(地区):
US
年份:
2019
代理人:
摘要:
The present disclosure relates to bifunctional compounds, which find utility as modulators of Burton's Tyrosine Kinase (BTK). In particular, the present disclosure is directed to bifunctional compounds. One end of a bifunctional compound includes a Von Hippel-Lindau, Cereblon, Inhibitors of Apotosis Proteins, or Mouse Double-Minute Homolog 2 ligand that binds to the respective E3 ubiquitin ligase. The other end of a bifunctional compound includes a moiety that binds a target protein, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of target protein. Diseases or disorders that result from aggregation, accumulation, and/or overactivation of the target protein can be treated or prevented with compounds and compositions of the present disclosure.
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