Oga inhibitor compounds

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

Inactive Publication Date: 2021-02-02
JANSSEN PHARMA NV
View PDF7 Cites 0 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

[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

[0047] R B is (b-1), (b...

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-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 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

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): C07D401/14C07D471/04A61P25/28A61K31/4375A61K31/4709
CPCC07D401/14C07D471/04A61P25/28
Inventor J·M·巴托洛梅-内布雷达A·A·特拉班科-苏亚雷斯C·M·马蒂尼兹-比图罗
Owner JANSSEN PHARMA NV
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Try Eureka
PatSnap group products