Non-peptidic GAPDH aggregation inhibitor

Patent metadata

Field	Value
Publication number	US-10137097-B2
Application number	US-201615574651-A
Country	US
Kind code	B2
Filing date	Jun 8, 2016
Priority date	Jun 8, 2015
Publication date	Nov 27, 2018
Grant date	Nov 27, 2018

Abstract

[Problem] Provided is a non-peptide compound which can be used as a GAPDH aggregation inhibitor. [Solution] Provided is a GAPDH aggregation inhibitor including as an active ingredient a compound represented by the chemical formula 1 wherein R 1 , R 2 , and R 3 are each independently a hydrogen atom, a halogen atom, or an aliphatic hydrocarbon group having a carbon number of from 1 to 10, a polysulfurized derivative thereof, or a pharmaceutically acceptable salt thereof. The present compound has a GAPDH aggregation inhibitory activity to suppress intracerebral aggregation of various proteins involved in cerebral neurodegenerative diseases, thereby contributing to improvement in various brain neurological diseases associated with aggregation of these proteins such as Alzheimer's disease, Parkinson's disease, and cerebral infarction, and prevention of advanced seriousness of these diseases.

First claim

The invention claimed is:

1. A compound represented by any of the chemical formula 1 wherein R 1 , R 2 , and R 3 are each independently a hydrogen atom, a halogen atom, or an aliphatic hydrocarbon group having a carbon number of from 1 to 10, the chemical formula 2 wherein R 1 , R 2 , and R 3 are each independently a hydrogen atom, a halogen atom, or an aliphatic hydrocarbon group having a carbon number of from 1 to 10, and n is an integer of 1 or more, or the chemical formula 3 wherein R 1 , R 2 , and R 3 are each independently a hydrogen atom, a halogen atom, or an aliphatic hydrocarbon group having a carbon number of from 1 to 10, and n is an integer of 1 or more, and a pharmaceutically acceptable salt thereof

2. A GAPDH aggregation inhibitor including as an active ingredient one or more compounds selected from the group consisting of a compound represented by any of the chemical formula 1 wherein R 1 , R 2 , and R 3 are each independently a hydrogen atom, a halogen atom, an aliphatic hydrocarbon group having a carbon number of from 1 to 10, the chemical formula 2 wherein R 1 , R 2 , and R 3 are each independently a hydrogen atom, a halogen atom, or an aliphatic hydrocarbon group having a carbon number of from 1 to 10, and n is an integer of 1 or more, or the chemical formula 3 wherein R 1 , R 2 , and R 3 are each independently a hydrogen atom, a halogen atom, or an aliphatic hydrocarbon group having a carbon number of from 1 to 10, and n is an integer of 1 or more, and a pharmaceutically acceptable salt thereof

3. A pharmaceutical composition comprising the compound according to claim 1 .

Assignees

• Univ Osaka Prefect Public Corp

Inventors

• Nakajima Hidemitsu

Classifications

• A61P25/16

  Anti-Parkinson drugs · CPC title

• C07C323/57

  the carbon skeleton being further substituted by nitrogen atoms, not being part of nitro or nitroso groups · CPC title

• A61K31/10

  Sulfides; Sulfoxides; Sulfones · CPC title

• A61K31/164

  of a carboxylic acid with an aminoalcohol, e.g. ceramides · CPC title

• A61P25/28

  for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia · CPC title