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NON-PEPTIDIC GAPDH AGGREGATION INHIBITOR

Foreign code F170009135
File No. S2015-1593-C0
Posted date Jul 20, 2017
Country WIPO
International application number 2016JP066999
International publication number WO 2016199796
Date of international filing Jun 8, 2016
Date of international publication Dec 15, 2016
Priority data
  • P2015-116140 (Jun 8, 2015) JP
Title NON-PEPTIDIC GAPDH AGGREGATION INHIBITOR
Abstract [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.
Outline of related art and contending technology 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.
Scope of claims (In Japanese)[請求項1]
化学式1(但し、式中のR1,R2,R3はそれぞれ独立に水素原子、ハロゲン原子、又は炭素原子数が1以上10以下の脂肪族炭化水素基である。)で示される化合物、又は化学式1で示される化合物のポリサルファー化誘導体、並びにそれらの薬理学的に許容される塩。
[化1]
[請求項2]
化学式1(但し、式中のR1,R2,R3はそれぞれ独立に水素原子、ハロゲン原子、又は炭素原子数が1以上10以下の脂肪族炭化水素基である。)で示される化合物、化学式1で示される化合物のポリサルファー化誘導体、それらの薬理学的に許容される塩からなる群から選ばれる1以上の化合物を有効成分とするGAPDH凝集阻害剤。
[化1]
[請求項3]
請求項1に記載の化合物を含有する医薬組成物。
[請求項4]
脳神経変性疾患又はその症状を予防、治療又は改善するための請求項3に記載の医薬組成物。
[請求項5]
前記脳神経変性疾患は、アルツハイマー病、パーキンソン病、ハンチントン病、脳梗塞の何れかである請求項4に記載の医薬組成物。
  • Applicant
  • ※All designated countries except for US in the data before July 2012
  • OSAKA PREFECTURE UNIVERSITY PUBLIC CORPORATION
  • Inventor
  • NAKAJIMA Hidemitsu
IPC(International Patent Classification)
Specified countries 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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