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[1,2,4]-triazolo [1,5-a]-pyrimidinyl derivatives substituted with piperidine, morpholine or piperazine as oga inhibitors

A substituent, A-B technology, applied in the field of O-GlcNAc hydrolase inhibitors, can solve problems such as not easy to separate

Inactive Publication Date: 2019-10-11
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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  • [1,2,4]-triazolo [1,5-a]-pyrimidinyl derivatives substituted with piperidine, morpholine or piperazine as oga inhibitors
  • [1,2,4]-triazolo [1,5-a]-pyrimidinyl derivatives substituted with piperidine, morpholine or piperazine as oga inhibitors
  • [1,2,4]-triazolo [1,5-a]-pyrimidinyl derivatives substituted with piperidine, morpholine or piperazine as oga inhibitors

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Embodiment Construction

[0055] 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 Supranuclear palsy, Down syndrome, frontotemporal dementia, frontotemporal dementia with Parkinson's disease-17, Pick's disease, corticobasal degeneration, and argyrophilic granular dementia; or for the prophylaxis or treatment of associated tauopathies Physiological neurodegenerative disease, especially a neurodegenerative disease selected from amyotrophic lateral sclerosis or frontotemporal dementia caused by mutations in C9ORF72.

[0056] In one embodiment, the invention relates to compounds of formula (I) as mentioned herein, and tautomeric and stereoisomeric forms thereof, wherein

[0057] A-B ...

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Abstract

The present invention relates to O-GlcNAc hydrolase (OGA) inhibitors. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes for preparing such compoundsand 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.

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 conditions in which inhibition of OGA is beneficial (such as tauopathies, especially Alzheimer's disease) silent disease or progressive supranuclear palsy; and neurodegenerative diseases with tau pathology, particularly 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 p...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D487/04C07D519/00A61K31/519A61P25/28
CPCA61P25/28C07D487/04C07D519/00C07D471/04
Inventor J.M.巴托洛梅-内布瑞达A.A.特拉班科-苏阿瑞兹M.J.阿尔卡扎-瓦卡
Owner JANSSEN PHARMA NV
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