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Inhibitor of ischemic disorders

外国特許コード F120006294
整理番号 FU-030P-EP
掲載日 2012年3月12日
出願国 欧州特許庁(EPO)
出願番号 08828106
公報番号 2199275
公報番号 2199275
出願日 平成20年9月1日(2008.9.1)
公報発行日 平成22年6月23日(2010.6.23)
公報発行日 平成28年1月13日(2016.1.13)
国際出願番号 JP2008065680
国際公開番号 WO2009028707
国際出願日 平成20年9月1日(2008.9.1)
国際公開日 平成21年3月5日(2009.3.5)
優先権データ
  • 2008JP065680 (2008.9.1) WO
  • 特願2007-225021 (2007.8.31) JP
発明の名称 (英語) Inhibitor of ischemic disorders
発明の概要(英語) It is intended to provide a drug which is efficacious in treating and preventing diseases wherein ischemia or an inflammatory substance associated with ischemia participates in the onset or worsening thereof.
Because of containing as the active ingredient a substance selected from among farnesol, a farnesol derivative, a tocopherol derivative, a tocotrienol derivative, pharmacologically acceptable salts thereof and solvates thereof, the above-described inhibitor of ischemic disorders can exert therapeutic and preventive effects on diseases wherein ischemia or an inflammatory substance associated with ischemia participates in the onset or worsening thereof (for example, brain infarction, brain edema, cardiac infarction, etc.) not only by the administration in the acute ischemic stage but also by the therapeutic administration in subacute and/or chronic stages after ischemia-reperfusion.
It is also intended to provide a farnesol carboxylic acid ester derivative and a method of producing the same.
特許請求の範囲(英語) [claim1]
1. A farnesol carboxylic acid ester derivative represented by formula (1): (see diagramm) wherein R **1 represents a carboxylic acid residue having a nitrogen substituent selected from the group consisting of an N-acyl amino acid residue, an N-alkyl amino acid residue, an N,N-dialkyl amino acid residue, and a physiologically acceptable salt thereof, and the physiologically acceptable salt is selected from the group consisting of a hydrohalic acid salt, an alkylsulfonic acid salt, and an acidic sugar salt, and the amino group and the carbonyl group in the carboxylic acid residue having a nitrogen substituent are connected by a linear, branched or cyclic alkylene group having 1 to 6 carbon atoms.
[claim2]
2. A compound selected from the group consisting of farnesol, a farnesol derivative, a pharmacologically acceptable salt thereof, a solvate thereof and a hydrate thereof, for use in a method for the inhibition of ischemia-reperfusion disorder or for the therapeutic or preventive treatment of cerebral infarction, cerebral edema, or myocardial infarction, wherein said farnesol and farnesol derivative are represented by formula (2): (see diagramm) wherein R **2 represents a hydrogen atom or a carboxylic acid residue having a nitrogen substituent selected from the group consisting of an amino acid residue, an N-acyl amino acid residue, an N-alkyl amino acid residue, an N,N-dialkyl amino acid residue, a pyridinecarboxylic acid residue, and a physiologically acceptable salt thereof, and the physiologically acceptable salt is selected from the group consisting of a hydrohalic acid salt, an alkylsulfonic acid salt, and an acidic sugar salt.
[claim3]
3. A farnesol carboxylic acid ester derivative selected from the group consisting of
(2E, 6E) farnesol N,N-dimethylglycinate,
(2Z/E, 6Z/E) farnesol N,N-dimethylglycinate,
(2E, 6E) farnesol N,N-dimethylglycinate hydrochloride,
(2Z/E, 6Z/E) farnesol N,N-dimethylglycinate hydrochloride,
(2E, 6E) farnesol N,N-dimethyl-beta -alaninate,
(2E, 6E) farnesol N,N-dimethyl-beta -alaninate hydrochloride,
(2E, 6E) farnesol N,N-diethyl-beta -alaninate,
(2E, 6E) farnesol N,N-diethyl-beta -alaninate hydrochloride,
(2E, 6E) farnesol N-tert.-butoxycarbonylsarcosinate, or
(2E, 6E) farnesol N-tert.-butoxycarbonylglycinate.
[claim4]
4. A compound for use in a method for the inhibition of ischemia-reperfusion disorder or for the therapeutic or preventive treatment of cerebral infarction, cerebral edema, or myocardial infarction selected from the group consisting of
(2E, 6E) farnesol N,N-dimethylglycinate,
(2Z/E, 6Z/E) farnesol N,N-dimethylglycinate,
(2E, 6E) farnesol N,N-dimethylglycinate hydrochloride,
(2Z/E, 6Z/E) farnesol N,N-dimethylglycinate hydrochloride,
(2E, 6E) farnesol sarcosinate,
(2E, 6E) farnesol sarcosinate hydrochloride,
(2E, 6E) farnesol glycinate,
(2E, 6E) farnesol glycinate hydrochloride,
(2E, 6E) farnesol N,N-dimethyl-beta -alaninate,
(2E, 6E) farnesol N,N-dimethyl-beta -alaninate hydrochloride,
(2E, 6E) farnesol N,N-diethyl-beta -alaninate,
(2E, 6E) farnesol N,N-diethyl-beta -alaninate hydrochloride,
(2E, 6E) farnesol N-tert.-butoxycarbonylsarcosinate, or
(2E, 6E) farnesol N-tert.-butoxycarbonylglycinate.
  • 出願人(英語)
  • FUKUOKA UNIVERSITY
  • 発明者(英語)
  • TAKATA JIRO
  • MISHIMA KENICHI
  • NAKASHIMA MANABU
  • IWASAKI KATSUNORI
  • MATSUNAGA KAZUHISA
  • KARUBE YOSHIHARU
  • FUJIWARA MICHIHIRO
国際特許分類(IPC)
指定国 Contracting States: AT BE BG CH CY CZ DE DK EE ES FI FR GB GR HR HU IE IS IT LI LT LU LV MC MT NL NO PL PT RO SE SI SK TR

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