MX2017011919A - Compuestos y metodos para la degradacion mejorada de proteinas especificas. - Google Patents
Compuestos y metodos para la degradacion mejorada de proteinas especificas.Info
- 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
- targeted
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title abstract 5
- 102000004169 proteins and genes Human genes 0.000 title abstract 5
- 108090000623 proteins and genes Proteins 0.000 title abstract 5
- 230000015556 catabolic process Effects 0.000 title abstract 3
- 238000006731 degradation reaction Methods 0.000 title abstract 3
- 238000000034 method Methods 0.000 title 1
- 102000006275 Ubiquitin-Protein Ligases Human genes 0.000 abstract 2
- 108010083111 Ubiquitin-Protein Ligases Proteins 0.000 abstract 2
- 230000001588 bifunctional effect Effects 0.000 abstract 2
- 230000005764 inhibitory process Effects 0.000 abstract 2
- 229920001184 polypeptide Polymers 0.000 abstract 2
- 102000004196 processed proteins & peptides Human genes 0.000 abstract 2
- 108090000765 processed proteins & peptides Proteins 0.000 abstract 2
- 230000000694 effects Effects 0.000 abstract 1
- 239000003112 inhibitor Substances 0.000 abstract 1
- 239000003446 ligand Substances 0.000 abstract 1
- 230000000144 pharmacologic effect Effects 0.000 abstract 1
- 230000034512 ubiquitination Effects 0.000 abstract 1
- 238000010798 ubiquitination Methods 0.000 abstract 1
Classifications
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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
- C07D471/04—Ortho-condensed systems
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- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
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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.
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 |
Publications (1)
Publication Number | Publication Date |
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MX2017011919A true MX2017011919A (es) | 2018-05-22 |
Family
ID=56919612
Family Applications (2)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
MX2017011919A MX2017011919A (es) | 2015-03-18 | 2016-03-18 | Compuestos y metodos para la degradacion mejorada de proteinas especificas. |
MX2021010482A MX2021010482A (es) | 2015-03-18 | 2017-09-15 | Compuestos y metodos para la degradacion mejorada de proteinas especificas. |
Family Applications After (1)
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MX2021010482A MX2021010482A (es) | 2015-03-18 | 2017-09-15 | Compuestos y metodos para la degradacion mejorada de proteinas especificas. |
Country Status (11)
Country | Link |
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US (3) | US10730870B2 (es) |
EP (1) | EP3270917A4 (es) |
JP (3) | JP7269731B2 (es) |
KR (2) | KR20230175343A (es) |
CN (1) | CN108601764A (es) |
AU (3) | AU2016232705C1 (es) |
BR (1) | BR112017019751A2 (es) |
CA (1) | CA2979070A1 (es) |
HK (1) | HK1249058A1 (es) |
MX (2) | MX2017011919A (es) |
WO (1) | WO2016149668A1 (es) |
Cited By (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
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 |
Families Citing this family (168)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
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 |
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AU2020273338A1 (en) | 2020-12-17 |
JP2018512449A (ja) | 2018-05-17 |
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