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Oga inhibitor compounds

A compound and solvate technology, applied in the field of O-GlcNAc hydrolase inhibitors, can solve problems such as difficult separation

Active Publication Date: 2021-02-02
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

[0045] The present invention relates to compounds of formula (I) as defined above and 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 progressive supranuclear palsy, Down syndrome, frontotemporal dementia, frontotemporal dementia with parkinsonism-17, Pick's disease, corticobasal degeneration, and argyrophilic granular disease; or available For the prevention or treatment of neurodegenerative diseases associated with tau pathology, in particular neurodegenerative diseases selected from amyotrophic lateral sclerosis or frontotemporal dementia caused by C9ORF72 mutations.

[0046] In a particular embodiment, the invention relates to compounds of formula (I) as defined above, and tautomeric and stereoisomeric forms thereof, wherein R 1 selected from the grou...

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Abstract

The present invention relates to O-GIcNAc hydrolase (OGA) inhibitors of formula (I). The invention is also directed to pharmaceutical compositions comprising such compounds, to processes for preparingsuch 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 dementiacaused by C90RF72 mutations.

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 such compounds, processes for the preparation of such compounds and compositions, and the use of such compounds and compositions for the prevention and treatment of disorders in which inhibition of OGA is beneficial, such disorders are, for example, tauopathies, especially Alzheimer's disease or progressive supranuclear palsy; and neurodegenerative diseases with tauopathology, 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 acylat...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D401/04C07D519/00A61K31/44A61K31/437A61K31/5377A61K31/501A61P25/16A61P25/28
CPCC07D401/04C07D519/00A61P25/16A61P25/28C07D471/04
Inventor J·M·巴托洛梅-内布雷达A·A·特拉班科-苏亚雷斯G·J·特列萨登C·马丁尼兹拉门卡J·E·利纳茨D·欧赫里希P·J·J·A·伯恩斯特斯A·I·韦尔特Y·E·M·范罗斯布鲁克
Owner JANSSEN PHARMA NV
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