Looking for breakthrough ideas for innovation challenges? Try Patsnap Eureka!

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
View PDF14 Cites 1 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

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

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Oga inhibitor compounds
  • Oga inhibitor compounds
  • Oga inhibitor compounds

Examples

Experimental program
Comparison scheme
Effect test

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...

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

No PUM Login to View More

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

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
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
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Patsnap Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Patsnap Eureka Blog
Learn More
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic, Popular Technical Reports.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com