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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
Authority
MX
Mexico
Prior art keywords
present
compounds
methods
degradation
specific proteins
Prior art date
Application number
MX2017011919A
Other languages
English (en)
Other versions
MX385750B (es
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
Original Assignee
Arvinas Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Arvinas Inc filed Critical Arvinas Inc
Publication of MX2017011919A publication Critical patent/MX2017011919A/es
Publication of MX385750B publication Critical patent/MX385750B/es

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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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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 métodos para la degradación mejorada de proteinas específicas. MX385750B (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
MX385750B MX385750B (es) 2025-03-18

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EP (2) EP3270917A4 (es)
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KR (2) KR20230175343A (es)
CN (1) CN108601764A (es)
AU (4) AU2016232705C1 (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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CA2861066C (en) 2012-01-12 2024-01-02 Yale University Compounds and methods for the enhanced degradation of targeted proteins and other polypeptides by an e3 ubiquitin ligase
CA2894994C (en) 2012-12-21 2019-11-12 National Institute Of Radiological Sciences Compounds for imaging tau proteins that accumulate in brain
GB201311891D0 (en) 2013-07-03 2013-08-14 Glaxosmithkline Ip Dev Ltd Novel compound
GB201311888D0 (en) 2013-07-03 2013-08-14 Glaxosmithkline Ip Dev Ltd Novel compounds
EP3099677A4 (en) 2014-01-31 2017-07-26 Dana-Farber Cancer Institute, Inc. Diaminopyrimidine benzenesulfone derivatives and uses thereof
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
US20180228907A1 (en) 2014-04-14 2018-08-16 Arvinas, Inc. Cereblon ligands and bifunctional compounds comprising the same
US10071164B2 (en) 2014-08-11 2018-09-11 Yale University Estrogen-related receptor alpha based protac compounds and associated methods of use
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