MX2017011919A - Compuestos y metodos para la degradacion mejorada de proteinas especificas. - Google Patents

Compuestos y metodos para la degradacion mejorada de proteinas especificas.

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Publication number
MX2017011919A
MX2017011919A MX2017011919A MX2017011919A MX2017011919A MX 2017011919 A MX2017011919 A MX 2017011919A MX 2017011919 A MX2017011919 A MX 2017011919A MX 2017011919 A MX2017011919 A MX 2017011919A MX 2017011919 A MX2017011919 A MX 2017011919A
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Mexico
Prior art keywords
present
compounds
methods
degradation
targeted
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MX2017011919A
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English (en)
Inventor
Chen Xin
Qian Yimin
M Crews Craig
P Crew Andrew
Dong Hanqing
Wang Jing
Siu Kam
Jin Meizhong
Berlin Michael
Ferraro Caterina
Zimmerman Kurt
Snyder Lawrence
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Arvinas Inc
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Publication of MX2017011919A publication Critical patent/MX2017011919A/es

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Abstract

La presente invención se refiere a compuestos bifuncionales, que encuentran utilidad como moduladores de ubiquitinación específica, especialmente inhibidores de una variedad de polipéptidos y otras proteínas que son degradadas y/o de otra manera inhibidas por compuestos bifuncionales de acuerdo con la presente invención. En particular, la presente invención se dirige a los compuestos, que contienen en un extremo un ligando VHL que se une a la ubiquitina ligasa y en el otro extremo una porción que une una proteína objetivo de tal forma que la proteína objetivo está situada en proximidad a la ubiquitina ligasa para efectuar la degradación (e inhibición) de esa proteína. La presente invención exhibe una amplia gama de actividades farmacológicas asociadas con los compuestos de acuerdo con la presente invención, consistente con la degradación/inhibición de polipéptidos específicos.
MX2017011919A 2015-03-18 2016-03-18 Compuestos y metodos para la degradacion mejorada de proteinas especificas. MX2017011919A (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201562135125P 2015-03-18 2015-03-18
PCT/US2016/023258 WO2016149668A1 (en) 2015-03-18 2016-03-18 Compounds and methods for the enhanced degradation of targeted proteins

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MX2017011919A true MX2017011919A (es) 2018-05-22

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EP (1) EP3270917A4 (es)
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KR (2) KR20230175343A (es)
CN (1) CN108601764A (es)
AU (3) AU2016232705C1 (es)
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CA (1) CA2979070A1 (es)
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US11306105B2 (en) 2015-09-11 2022-04-19 Dana-Farber Cancer Institute, Inc. Cyano thienotriazolodiazepines and uses thereof
US11406645B2 (en) 2015-09-11 2022-08-09 Dana-Farber Cancer Institute, Inc. Acetamide thienotriazolodiazepines and uses thereof

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EP3608317A1 (en) 2012-01-12 2020-02-12 Yale University Compounds & methods for the enhanced degradation of targeted proteins & other polypeptides by an e3 ubiquitin ligase
WO2014097474A1 (ja) 2012-12-21 2014-06-26 独立行政法人放射線医学総合研究所 脳内に蓄積したタウタンパク質をイメージングするための新規化合物
GB201311888D0 (en) 2013-07-03 2013-08-14 Glaxosmithkline Ip Dev Ltd Novel compounds
GB201311891D0 (en) 2013-07-03 2013-08-14 Glaxosmithkline Ip Dev Ltd Novel compound
JP2017504651A (ja) 2014-01-31 2017-02-09 ダナ−ファーバー キャンサー インスティテュート, インコーポレイテッド ジアゼパン誘導体の使用
RU2016134947A (ru) 2014-01-31 2018-03-01 Дана-Фарбер Кансер Институт, Инк. Производные диаминопиримидин бензолсульфона и их применение
US10071164B2 (en) 2014-08-11 2018-09-11 Yale University Estrogen-related receptor alpha based protac compounds and associated methods of use
KR20200052995A (ko) 2015-01-20 2020-05-15 아비나스 오퍼레이션스, 인코포레이티드 안드로겐 수용체의 표적화된 분해를 위한 화합물 및 방법
US20170327469A1 (en) 2015-01-20 2017-11-16 Arvinas, Inc. Compounds and methods for the targeted degradation of androgen receptor
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