MX2016013563A - Moduladores de la proteolisis basados en imida y metodos de uso asociados. - Google Patents
Moduladores de la proteolisis basados en imida y metodos de uso asociados.Info
- Publication number
- MX2016013563A MX2016013563A MX2016013563A MX2016013563A MX2016013563A MX 2016013563 A MX2016013563 A MX 2016013563A MX 2016013563 A MX2016013563 A MX 2016013563A MX 2016013563 A MX2016013563 A MX 2016013563A MX 2016013563 A MX2016013563 A MX 2016013563A
- Authority
- MX
- Mexico
- Prior art keywords
- compounds
- imide
- binds
- inhibition
- proteolysis
- Prior art date
Links
- 150000003949 imides Chemical class 0.000 title abstract 2
- 230000017854 proteolysis Effects 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 5
- 102000004169 proteins and genes Human genes 0.000 abstract 4
- 108090000623 proteins and genes Proteins 0.000 abstract 4
- 230000001588 bifunctional effect Effects 0.000 abstract 2
- 230000015556 catabolic process Effects 0.000 abstract 2
- 238000006731 degradation reaction Methods 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
- 102100032783 Protein cereblon Human genes 0.000 abstract 1
- 102000006275 Ubiquitin-Protein Ligases Human genes 0.000 abstract 1
- 108010083111 Ubiquitin-Protein Ligases Proteins 0.000 abstract 1
- 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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- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
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- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
- A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
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- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
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Abstract
La descripción se refiere a compuestos basados en imida, incluyendo compuestos bifuncionales que los comprenden, los cuales encuentran utilidad como moduladores de la ubiquitinación dirigida, en especial como inhibidores de una variedad de polipéptidos y otras proteínas que son degradadas y/o de otra manera inhibidas por los compuestos bifuncionales de acuerdo con la presente invención. En particular, la descripción proporciona compuestos que contienen, en un extremo, un ligando que se enlaza a la ligasa de ubiquitina E3 de cereblon, y en el otro extremo, una fracción que se enlaza a una proteína objetivo, de tal manera que la proteína objetivo se coloca en proximidad a la ligasa de ubiquitina para efectuar la degradación (y la inhibición) de esa proteína. Se pueden sintetizar compuestos que exhiben una amplia gama de actividades farmacológicas consistentes con la degradación/inhibición de polipéptidos objetivo de casi cualquier tipo.
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US201461979351P | 2014-04-14 | 2014-04-14 | |
PCT/US2015/025813 WO2015160845A2 (en) | 2014-04-14 | 2015-04-14 | Imide-based modulators of proteolysis and associated methods of use |
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KR (5) | KR20170002446A (es) |
CN (1) | CN106458993A (es) |
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MX (2) | MX2016013563A (es) |
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