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DÉRIVÉS DE TÉTRAHYDRONAPHTALÈNE ET DE TÉTRAHYDROISOQUINOLÉINE EN TANT QU'AGENTS DE DÉGRADATION DES RÉCEPTEURS DES STROGÈNES
专利权人:
Inc.;Arvinas Operations
发明人:
申请号:
EP20150584.9
公开号:
EP3689868A1
申请日:
2017.12.01
申请国别(地区):
EP
年份:
2020
代理人:
摘要:
The present disclosure relates to bifunctional compounds, which find utility as modulators of estrogen receptor (target protein). In particular, the present disclosure is directed to bifunctional compounds, which contain on one end at least one of a Von Hippel-Lindau ligand, a cereblon ligand, Inhibitors of Apoptosis Proteins ligand, mouse double-minute homolog 2 ligand, or a combination thereof, which binds to the respective E3 ubiquitin ligase, and on the other end a moiety which binds the target protein, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of 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.
来源网站:
中国工程科技知识中心
来源网址:
http://www.ckcest.cn/home/
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