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NON-PEPTIDIC GAPDH AGGREGATION INHIBITOR

外国特許コード F170009135
整理番号 S2015-1593-C0
掲載日 2017年7月20日
出願国 世界知的所有権機関(WIPO)
国際出願番号 2016JP066999
国際公開番号 WO 2016199796
国際出願日 平成28年6月8日(2016.6.8)
国際公開日 平成28年12月15日(2016.12.15)
優先権データ
  • 特願2015-116140 (2015.6.8) JP
発明の名称 (英語) NON-PEPTIDIC GAPDH AGGREGATION INHIBITOR
発明の概要(英語) [Problem] To provide a novel non-peptidic compound that can be used as a GAPDH aggregation inhibitor.
[Solution] Provided is a GAPDH aggregation inhibitor which contains, as an active ingredient, a compound represented by chemical formula 1 (wherein R1, R2 and R3 independently represent a hydrogen atom, a halogen atom, or an aliphatic hydrocarbon group having 1 to 10 carbon atoms inclusive), or a polysulfurized derivative or a pharmacologically acceptable salt thereof. The compound has a GAPDH aggregation-inhibiting activity, and therefore can inhibit the aggregation of various proteins associated with cerebral neurodegenerative diseases in the brain to contribute to the amelioration of various cerebral nerve diseases associated with the aggregation of the proteins, such as Alzheimer's disease, Parkinson's disease and cerebral infarction, or to the prevention of these diseases from becoming severe.
従来技術、競合技術の概要(英語) BACKGROUND ART
Cognitive impairment and Alzheimer's disease is mainly characterized disease required provision can be made quickly. Such as Alzheimer's disease amyloidosis related to aggregation GAPDH is, if the aggregation of amyloid β GAPDH aggregation or deposition can be prevented from being pointed out. In such a situation, the inventors of the present invention, the specific amino acid sequence having 10-20 amino acid residues of a peptide consisting GAPDH found inhibiting aggregation, performing a patent application (patent document 1).
However, degradation of the peptide in the gastrointestinal tract as well as faster metabolism in the body, the transition into the brain by intravenous administration and is small. In addition, the synthesis of the peptide and the method of purification and it is difficult to appear the problem, peptide similar to the non-peptide compounds (mimic) is desired.
  • 出願人(英語)
  • ※2012年7月以前掲載分については米国以外のすべての指定国
  • OSAKA PREFECTURE UNIVERSITY PUBLIC CORPORATION
  • 発明者(英語)
  • NAKAJIMA Hidemitsu
国際特許分類(IPC)
指定国 National States: AE AG AL AM AO AT AU AZ BA BB BG BH BN BR BW BY BZ CA CH CL CN CO CR CU CZ DE DK DM DO DZ EC EE EG ES FI GB GD GE GH GM GT HN HR HU ID IL IN IR IS JP KE KG KN KP KR KZ LA LC LK LR LS LU LY MA MD ME MG MK MN MW MX MY MZ NA NG NI NO NZ OM PA PE PG PH PL PT QA RO RS RU RW SA SC SD SE SG SK SL SM ST SV SY TH TJ TM TN TR TT TZ UA UG US UZ VC VN ZA ZM ZW
ARIPO: BW GH GM KE LR LS MW MZ NA RW SD SL SZ TZ UG ZM ZW
EAPO: AM AZ BY KG KZ RU TJ TM
EPO: AL AT BE BG CH CY CZ DE DK EE ES FI FR GB GR HR HU IE IS IT LT LU LV MC MK MT NL NO PL PT RO RS SE SI SK SM TR
OAPI: BF BJ CF CG CI CM GA GN GQ GW KM ML MR NE SN ST TD TG

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