Oga inhibitor compounds

A compound, free technology, applied in the direction of active ingredients of heterocyclic compounds, organic chemistry, drug combination, etc., can solve problems such as difficult separation

Inactive Publication Date: 2021-01-29
JANSSEN PHARMA NV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

This effectively makes tau less prone to dissociation from microtubules and reduces aggregation into neurotoxic tangles, which ultimately lead to neurotoxicity and neuronal cell death

Method used

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Embodiment Construction

[0068] The present invention relates to compounds of formula (I) as defined above and to pharmaceutically acceptable addition salts and solvates thereof. Compounds of formula (I) are inhibitors of O-GlcNAc hydrolase (OGA) and are useful for the prophylaxis or treatment of tauopathies, in particular tauopathies selected from the group consisting of: Alzheimer's disease, progressive nuclear Superior palsy, Down syndrome, frontotemporal dementia, frontotemporal dementia with Parkinson's disease-17, Pick's disease, corticobasal degeneration, and argyrophilic granular dementia; or may be used to prevent or treat neurological disorders associated with tauopathies Degenerative disease, especially a neurodegenerative disease selected from amyotrophic lateral sclerosis or frontotemporal dementia caused by mutations in C9ORF72.

[0069] In particular embodiments, the invention relates to compounds of formula (I) as mentioned herein, and tautomeric and stereoisomeric forms thereof, where...

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Abstract

The present invention relates to O-GIcNAc hydrolase (OGA) inhibitors having the structure shown in formula (I). The invention is also directed to pharmaceutical compositions comprising such compoundsto processes for preparing such compounds and compositions, and to the use of such compounds and compositions for the prevention and treatment of disorders in which inhibition of OGA is beneficial, such as tauopathies, in particular Alzheimer's disease or progressive supranuclear palsy; and neurodegenerative diseases accompanied by a tau pathology, in particular amyotrophic lateral sclerosis or frontotemporal lobe dementia caused by C90RF72 mutations. wherein RB is an aromatic heterobicyclic radical selected from the group consisting of (b-1) to (b-6).

Description

technical field [0001] The present invention relates to O-GlcNAc hydrolase (OGA) inhibitor having the structure shown in formula (I) [0002] [0003] wherein these groups are as defined in the specification. The invention also relates to pharmaceutical compositions comprising these compounds, processes for the preparation of these compounds and compositions, and the use of these compounds and compositions for the prevention and treatment of disorders in which inhibition of OGA is beneficial, such as tauopathies, Especially Alzheimer's disease or progressive supranuclear palsy; and neurodegenerative diseases with tau pathology, especially amyotrophic lateral sclerosis or frontotemporal dementia caused by C9ORF72 mutations. Background technique [0004] O-GlcN acylation is a reversible modification of proteins in which N-acetyl-D-glucosamine residues are transferred to the hydroxyl groups of serine and threonine residues, resulting in O-GlcN acylated proteins. More than ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D491/056C07D417/14C07D513/04A61P25/28A61K31/445
CPCC07D417/14C07D491/056C07D513/04C07D405/14C07D491/048C07D491/052C07D498/04
Inventor J·M·巴托洛梅-内布雷达A·A·特拉班科-苏亚雷斯A·I·德卢卡斯奥利瓦雷斯F·德尔加多-吉米涅兹S·康德-塞德J·A·维加拉米罗
Owner JANSSEN PHARMA NV
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