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US Patent 11597720 Tetrahydronaphthalene and tetrahydroisoquinoline derivatives as estrogen receptor degraders

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Patent
Patent

Patent attributes

Patent Applicant
Arvinas
Arvinas
Current Assignee
Arvinas
Arvinas
Patent Jurisdiction
United States Patent and Trademark Office
United States Patent and Trademark Office
Patent Number
11597720
Date of Patent
March 7, 2023
Patent Application Number
16932072
Date Filed
July 17, 2020
Patent Citations
‌
US Patent 11104666 Tetrahydronaphthalene and tetrahydroisoquinoline derivatives as estrogen receptor degraders
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US Patent 10647698 Tetrahydronaphthalene and tetrahydroisoquinoline derivatives as estrogen receptor degraders
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US Patent 10899742 Tetrahydronaphthalene and tetrahydroisoquinoline derivatives as estrogen receptor degraders
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US Patent 11261178 Chroman derivatives having estrogen receptor degradation activity and uses thereof
Patent Primary Examiner
‌
Matthew P Coughlin
CPC Code
‌
C07D 401/14

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.

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