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Inhibitor of ischemic disorders

外国特許コード F120006293
整理番号 FU-030P-US
掲載日 2012年3月12日
出願国 アメリカ合衆国
出願番号 67512908
公報番号 20100217006
公報番号 8242302
出願日 平成20年9月1日(2008.9.1)
公報発行日 平成22年8月26日(2010.8.26)
公報発行日 平成24年8月14日(2012.8.14)
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
  • 特願2007-225021 (2007.8.31) JP
  • 2008WO-JP65680 (2008.9.1) WO
発明の名称 (英語) Inhibitor of ischemic disorders
発明の概要(英語) (US8242302)
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):
wherein R1 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, 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.
[claim2]
2. An inhibitor of ischemia-reperfusion disorder or a therapeutic agent of cerebral infarction, cerebral edema, or myocardial infarction, comprising, as an active ingredient, at least one substance selected from the group consisting of a farnesol carboxylic acid ester derivative, a pharmacologically acceptable salt thereof, a solvate thereof and a hydrate thereof, wherein said farnesol carboxylic acid ester derivative is represented by formula (2):
wherein R2 represents 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. The farnesol carboxylic acid ester derivative according to claim 1, wherein R1 is a residue selected from the group consisting of 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, said alkyl being methyl.
[claim4]
4. The inhibitor of ischemia-reperfusion disorder or the therapeutic agent of cerebral infarction, cerebral edema, or myocardial infarction according to claim 2, wherein R2 is a residue selected from the group consisting of 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, said alkyl being methyl.
[claim5]
5. A farnesol carboxylic acid ester derivative selected from the group consisting of farnesol sarcosinate, farnesol N-tert-butoxycarbonylglycinate, farnesol N,N-dimethylglycinate, farnesol N,N-dimethyl-beta -alaninate, farnesol N,N-diethyl-beta -alaninate, farnesol N-tert-butoxycarbonylsarcosinate, and hydrochloric acid salts thereof.
[claim6]
6. The inhibitor of ischemia-reperfusion disorder or the therapeutic agent of cerebral infarction, cerebral edema, or myocardial infarction according to claim 2, wherein said farnesol carboxylic acid ester derivative is farnesol N,N-dimethylglycinate or its hydrochloric acid salt.
  • 発明者/出願人(英語)
  • TAKATA JIRO
  • MISHIMA KENICHI
  • NAKASHIMA MANABU
  • IWASAKI KATSUNORI
  • MATSUNAGA KAZUHISA
  • KARUBE YOSHIHARU
  • FUJIWARA MICHIHIRO
  • FUKUOKA UNIVERSITY
国際特許分類(IPC)

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