MX2021011827A - Moduladores del receptor de andrógenos y métodos para su uso como ligandos quiméricos que se dirigen a la proteólisis. - Google Patents

Moduladores del receptor de andrógenos y métodos para su uso como ligandos quiméricos que se dirigen a la proteólisis.

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Publication number
MX2021011827A
MX2021011827A MX2021011827A MX2021011827A MX2021011827A MX 2021011827 A MX2021011827 A MX 2021011827A MX 2021011827 A MX2021011827 A MX 2021011827A MX 2021011827 A MX2021011827 A MX 2021011827A MX 2021011827 A MX2021011827 A MX 2021011827A
Authority
MX
Mexico
Prior art keywords
methods
ligands
androgen receptor
receptor modulators
proteolysis targeting
Prior art date
Application number
MX2021011827A
Other languages
English (en)
Inventor
Raymond John Andersen
Han- Jie ZHOU
Original Assignee
Essa Pharma Inc
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Publication date
Application filed by Essa Pharma Inc filed Critical Essa Pharma Inc
Publication of MX2021011827A publication Critical patent/MX2021011827A/es

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    • C07D403/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
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    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
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    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
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    • C07D471/12—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains three hetero rings
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    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04—Ortho-condensed systems
    • C07D491/044—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
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Abstract

La presente invención se refiere a ligandos quiméricos bifuncionales que se dirigen a la proteólisis (compuestos Protac) que comprenden un aglutinante/modulador de ligasa y una molécula que se une a una proteína objetivo de interés y métodos para tratar varias enfermedades y afecciones con los compuestos Protac, inclusive enfermedades asociadas con receptores de andrógenos.
MX2021011827A 2019-03-28 2020-03-27 Moduladores del receptor de andrógenos y métodos para su uso como ligandos quiméricos que se dirigen a la proteólisis. MX2021011827A (es)

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US10471023B2 (en) 2015-03-12 2019-11-12 British Columbia Cancer Agency Branch Bisphenol ether derivatives and methods for using the same
US20170298033A1 (en) 2016-04-15 2017-10-19 The University Of British Columbia Bisphenol derivatives and their use as androgen receptor activity modulators
US11485713B2 (en) 2018-05-25 2022-11-01 Essa Pharma, Inc. Androgen receptor modulators and methods for their use
TW202136240A (zh) 2019-12-19 2021-10-01 美商亞文納營運公司 用於靶向降解雄激素受體之化合物及方法
JP2023522040A (ja) 2020-04-17 2023-05-26 エッサ ファーマ，インコーポレイテッド Ｎ末端ドメインアンドロゲン受容体阻害剤の固体形態およびその使用
CA3181782A1 (en) 2020-05-09 2021-11-18 Arvinas Operations, Inc. Methods of manufacturing a bifunctional compound, ultrapure forms of the bifunctional compound, and dosage forms comprising the same
KR20240053589A (ko) * 2021-07-30 2024-04-24 하이노바 파마슈티컬스 인코포레이티드 이중 기능성 키메라 헤테로 고리 화합물 및 이의 안드로겐 수용체 분해제로서의 용도
WO2023046283A1 (en) * 2021-09-22 2023-03-30 Fundació Institut De Recerca Biomèdica (Irb Barcelona) Compounds and their use in a method for modulating ar (androgen receptor) transcriptional activity
TW202329950A (zh) 2021-11-25 2023-08-01 大陸商江蘇恆瑞醫藥股份有限公司 一種用於雄激素受體蛋白靶向降解的嵌合體化合物、其製備方法及其在醫藥上的應用
WO2023180388A1 (en) 2022-03-24 2023-09-28 Glaxosmithkline Intellectual Property Development Limited 2,4-dioxotetrahydropyrimidinyl derivatives as degrons in protacs
WO2024006207A1 (en) * 2022-06-26 2024-01-04 Essa Pharma Inc. An n-terminal domain androgen receptor inhibitor and uses thereof

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US20180228907A1 (en) * 2014-04-14 2018-08-16 Arvinas, Inc. Cereblon ligands and bifunctional compounds comprising the same
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