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Cyclobutyl purine derivative, angiogenesis promoting agent, lumenization promoting agent, neurocyte growth promoting agent, and drug 実績あり

外国特許コード F120006247
整理番号 S2009-0108-N0
掲載日 2012年2月17日
出願国 欧州特許庁(EPO)
出願番号 09829176
公報番号 2377865
公報番号 2377865
出願日 平成21年11月27日(2009.11.27)
公報発行日 平成23年10月19日(2011.10.19)
公報発行日 平成26年12月17日(2014.12.17)
国際出願番号 JP2009070062
国際公開番号 WO2010061931
国際出願日 平成21年11月27日(2009.11.27)
国際公開日 平成22年6月3日(2010.6.3)
優先権データ
  • 2009JP070062 (2009.11.27) WO
  • 特願2008-303239 (2008.11.27) JP
発明の名称 (英語) Cyclobutyl purine derivative, angiogenesis promoting agent, lumenization promoting agent, neurocyte growth promoting agent, and drug 実績あり
発明の概要(英語) Provided is a compound having at least one selected from the group consisting of cell growth promoting activity, angiogenesis promoting activity, lumen formation promoting activity, cell migration promoting activity, and neurocyte growth promoting activity, which is a chemically stable low-molecular-weight substance that has high absorbability and can be supplied stably at a low cost because of its low molecular weight.
A cyclobutyl purine derivative, a tautomer or stereoisomer thereof, or a salt, solvate, or hydrate thereof according to the present invention is a cyclobutyl purine derivative represented by the following general formula (1), a tautomer or stereoisomer thereof, or a salt, solvate, or hydrate thereof. (see diagramm) (see diagramm)
特許請求の範囲(英語) [claim1]
1. A compound for use in a method of treatment which comprises promoting angiogenesis, promoting lumen formation, or promoting neurocyte growth: wherein the compound is a cyclobutyl purine derivative represented by the following general formula (1), a tautomer or stereoisomer thereof, or a salt, solvate, or hydrate thereof: (see diagramm) where: X 1' is a halogeno group, an alkyl group, an alkylthio group, a thio group (thiol group), an amino group, a hydroxy group, an alkoxy group, an alkynyl group, or a cyano group; X 2' is a halogeno group, an amino group, a hydroxy group, an alkoxy group, a thio group (thiol group), or an alkylthio group; X 3' is a hydrogen atom, a halogeno group, an alkyl group, an alkylthio group, an amino group, a hydroxy group, an alkoxy group, a hydroxyphenyl group, or a carbamoyl group; R 1' and R 2' are the same or different, and are each independently a hydrogen atom, a halogeno group, a carboxyl group, an alkyl group, an acyl group, a carbamoyl group, an acyloxy group, a hydroxyalkyl group, an acyloxyalkyl group, an alkoxyalkyl group, a haloalkyl group, or a phosphonooxyalkyl group; and when X 1' is an amino group and X 3' is a hydrogen atom, R 1' and R 2' are each independently an atom or substituent other than a hydroxyalkyl group.
[claim2]
2. The compound for use according to claim 1 wherein the compound is a cyclobutyl purine derivative, a tautomer or stereoisomer thereof, or a salt, solvate, or hydrate thereof wherein, in the general formula (1), X 1' is a chloro group or a methylthio group.
[claim3]
3. The compound for use according to claim 1 or 2 wherein the compound is a cyclobutyl purine derivative, a tautomer or stereoisomer thereof, or a salt, solvate, or hydrate thereof wherein, in the general formula (1), X 2' is an amino group.
[claim4]
4. The compound for use according to any one of claims 1 to 3 wherein the compound is a cyclobutyl purine derivative, a tautomer or stereoisomer thereof, or a salt, solvate, or hydrate thereof wherein, in the general formula (1), R 1' and R 2' are hydroxymethyl groups.
[claim5]
5. The compound for use according to any one of claims 1 to 4 wherein the compound is a cyclobutyl purine derivative, a tautomer or stereoisomer thereof, or a salt, solvate, or hydrate thereof wherein, in the general formula (1), X 1' is a chloro group or a thiomethoxy group, X 2' is an amino group, and R 1' and R 2' are hydroxymethyl groups.
[claim6]
6. The compound for use according to any one of claims 1 to 5 wherein the compound is a cyclobutyl purine derivative, a tautomer or stereoisomer thereof, or a salt, solvate, or hydrate thereof which is 6-amino-2-chloro-9-[trans-trans-2,3-bis(hydroxymethyl)cyclobutyl]purine or 6-amino-2-thiomethoxy-9-[trans-trans-2,3-bis(hydroxymethyl)cyclobutyl] purine, a tautomer or stereoisomer thereof, or a salt, solvate, or hydrate thereof.
[claim7]
7. The compound for use according to claim 1 wherein the compound is a cyclobutyl purine derivative, a tautomer or stereoisomer thereof, or a salt, solvate, or hydrate thereof which is
2-amino-6,8-dimethoxy-9-[trans-trans-2,3-bis(hydroxymethyl)cyclobutyl] purine, 8-bromo-9-[trans-trans-2,3-bis(acetyloxymethyl)cyclobutyl]guanine, or 2-amino-6,8-dichloro-9-[trans-trans-2,3-bis(acetyloxymethyl)cyclobutyl] purine, a tautomer or stereoisomer thereof, or a salt, solvate or hydrate thereof.
[claim8]
8. The compound for use according to any one of the preceding claims, which is for use as a wound healing agent, therapeutic agent for Alzheimer's disease, prophylactic agent for Alzheimer's disease, therapeutic agent for infarction diseases, prophylactic agent for infarction diseases, or a hair growth agent.
[claim9]
9. A composition suitable for oral or parenteral administration comprising a cyclobutyl purine derivative, a tautomer or stereoisomer thereof or a salt, solvate or hydrate thereof for use according to any one of the preceding claims.
[claim10]
10. Use of a cyclobutyl purine derivative in the manufacture of a medicament for use in promoting angiogenesis, promoting lumen formation or promoting neurocyte growth,
wherein the cyclobutyl purine derivative is represented by the following general formula (1), a tautomer or stereoisomer thereof or a salt, solvate or hydrate thereof: (see diagramm) where : X 1' is a halogeno group, an alkyl group, an alkylthio group, a thio group (thiol group), an amino group, a hydroxy group, an alkoxy group, an alkynyl group, or a cyano group; X 2' is a halogeno group, an amino group, a hydroxy group, an alkoxy group, a thio group (thiol group), or an alkylthio group; X 3' is a hydrogen atom, a halogeno group, an alkyl group, an alkylthio group, an amino group, a hydroxy group, an alkoxy group, a hydroxyphenyl group, or a carbamoyl group; R 1' and R 2' are the same or different, and are each independently a hydrogen atom, a halogeno group, a carboxyl group, an alkyl group, an acyl group, a carbamoyl group, an acyloxy group, a hydroxyalkyl group, an acyloxyalkyl group, an alkoxyalkyl group, a haloalkyl group, or a phosphonooxyalkyl group; and when X 1' is an amino group and X 3' is a hydrogen atom, R 1' and R 2' are each independently an atom or substituent other than a hydroxyalkyl group.
[claim11]
11. Use according to claim 10 wherein the cyclobutyl purine derivative is as further defined in any one of claims 2 to 7.
[claim12]
12. Use according to claim 10 or 11 wherein the medicament is for use as a wound healing agent, therapeutic agent for Alzheimer's disease, prophylactic agent for Alzheimer's disease, therapeutic agent for infarction diseases, prophylactic agent for infarction diseases, or a hair growth agent.
  • 出願人(英語)
  • KAGAWA UNIVERSITY
  • 発明者(英語)
  • TSUKAMOTO IKUKO
  • KONISHI RYOJI
  • TOKUDA MASAAKI
  • KUBOTA YASUO
  • MARUYAMA TOKUMI
  • KOSAKA HIROAKI
  • IGARASHI JUNSUKE
国際特許分類(IPC)
欧州特許分類/主・副
  • C07D473/18
  • C07D473/24
  • C07D473/34
  • C07D473/40
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 MK MT NL NO PL PT RO SE SI SK SM TR
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