Invention Grant
- Patent Title: Modulators of estrogen receptor proteolysis and associated methods of use
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Application No.: US16810764Application Date: 2020-03-05
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Publication No.: US11384063B2Publication Date: 2022-07-12
- Inventor: Andrew P. Crew , Hanqing Dong , Jing Wang , Yimin Qian
- Applicant: Arvinas Operations, Inc.
- Applicant Address: US CT New Haven
- Assignee: Arvinas Operations, Inc.
- Current Assignee: Arvinas Operations, Inc.
- Current Assignee Address: US CT New Haven
- Agency: Cantor Colburn LLP
- Agent Bryan D. Zerhusen, Esq.; Nicholas R. Herrel, Esq.
- Main IPC: C07D401/14
- IPC: C07D401/14 ; C07D471/04 ; C07D409/12 ; C07D403/06 ; A61P35/00 ; C07D405/14 ; C07D413/14 ; C07D417/12 ; C07D417/14 ; C07D403/14

Abstract:
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 a cereblon, Von Hippel-Lindau ligase-binding moiety, Inhibitors of Apotosis Proteins, or mouse double-minute homolog 2 ligand, 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.
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