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Inhibitor of ischemic disorders

Foreign code F120006294
File No. FU-030P-EP
Posted date Mar 12, 2012
Country EPO
Application number 08828106
Gazette No. 2199275
Gazette No. 2199275
Date of filing Sep 1, 2008
Gazette Date Jun 23, 2010
Gazette Date Jan 13, 2016
International application number JP2008065680
International publication number WO2009028707
Date of international filing Sep 1, 2008
Date of international publication Mar 5, 2009
Priority data
  • 2008JP065680 (Sep 1, 2008) WO
  • P2007-225021 (Aug 31, 2007) JP
Title Inhibitor of ischemic disorders
Abstract 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.
Scope of claims [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.
  • Applicant
  • FUKUOKA UNIVERSITY
  • Inventor
  • TAKATA JIRO
  • MISHIMA KENICHI
  • NAKASHIMA MANABU
  • IWASAKI KATSUNORI
  • MATSUNAGA KAZUHISA
  • KARUBE YOSHIHARU
  • FUJIWARA MICHIHIRO
IPC(International Patent Classification)
Specified countries 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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