- 专利标题: Tetrahydronaphthalene and tetrahydroisoquinoline derivatives as estrogen receptor degraders
-
申请号: US16744414申请日: 2020-01-16
-
公开(公告)号: US10899742B1公开(公告)日: 2021-01-26
- 发明人: Andrew P. Crew , Yimin Qian , Hanqing Dong , Jing Wang
- 申请人: Arvinas Operations, Inc.
- 申请人地址: US CT New Haven
- 专利权人: Arvinas Operations, Inc.
- 当前专利权人: Arvinas Operations, Inc.
- 当前专利权人地址: US CT New Haven
- 代理机构: Cooley LLP
- 代理商 Ivor R. Elrifi; Thomas J. Paxton
- 主分类号: A61K31/496
- IPC分类号: A61K31/496 ; C07D401/14 ; A61K47/54 ; A61P15/00 ; A61P35/00 ; A61K31/454 ; A61K31/4545 ; A61K31/4725 ; A61K31/497 ; A61K31/501 ; A61K31/519 ; A61K31/5386 ; A61K31/551 ; A61K38/05 ; A61K38/06 ; A61K45/06 ; C07D401/04 ; C07D471/04 ; C07D471/10 ; C07D487/04 ; C07D487/08 ; C07D487/10 ; C07D498/10 ; C07K5/078 ; C07K5/083 ; C07K5/062
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.
信息查询
IPC分类: