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

外国特許コード F120006246
整理番号 S2009-0108-N0
掲載日 2012年2月17日
出願国 大韓民国
出願番号 20117012017
公報番号 20110075040
公報番号 101358626
出願日 平成21年11月27日(2009.11.27)
公報発行日 平成23年7月5日(2011.7.5)
公報発行日 平成26年2月4日(2014.2.4)
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
  • 特願2008-303239 (2008.11.27) JP
  • 2009JP70062 (2009.11.27) WO
発明の名称 (英語) Cyclobutyl purine derivative, angiogenesis promoting agent, lumenization promoting agent, neurocyte growth promoting agent, and drug UPDATE 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.
従来技術、競合技術の概要(英語) BACKGROUND ART
Conventionally, a nucleic acid bound to the 4-membered several derivatives, it is desirable to have antiviral action have been known. The derivatives include, for example a cyclobutyl purine derivative (see Patent document 1 ∼ 3), nucleic acids are bound to their oxetane rings (see Patent document No. 4) oxetanocin derivatives and the like can be mentioned.
On the other hand angiogenesis, such as nerve cell growth promoting agent, a growth factor derived from a living organism, (FGF) fibroblast growth factor, platelet derived growth factor (PD - ECGF), vascular endothelial growth factor (VEGF), such as nerve growth factor (NGF) are known. Thus, among these growth factors, about wound healing, hair growth tonic and the like which can be used as an active ingredient may also be used.
特許請求の範囲(英語) [claim1]
1. Represented by the following general formula (1) cyclobutyl purine derivative, a tautomer or stereoisomer thereof, or a salt thereof, a solvate or hydrate thereof: in the general formula (1), X1 is a halogeno group, linear or branched alkyl group having 1-8 carbon atoms, an alkylthio group having 1-8 carbon atoms in a straight chain or branched alkyl, thio group (thiol group), an amino group, a hydroxy group, an alkoxy group having 1-8 carbon atoms in a straight or branched, straight chain or branched alkynyl group having 1-8 carbon atoms or a cyano group, X2 is a halogeno group, amino group, a hydroxy group, an alkoxy group having 1-8 carbon atoms in a straight or branched, a thio group (thiol group) or thio group having 1-8 carbon atoms and is straight or branched alkyl, X3 represents a hydrogen atom, a halogeno group or an alkoxy group having 1-8 carbon atoms and is straight or branched, R1 and R2 is the same or different, each represents a hydrogen atom, a halogeno group, a carboxyl group, linear or branched alkyl group having 1-8 carbon atoms, and loosen 1-8 linear or branched carbon atoms, a carbamoyl group, an acyloxy group having 1-8 carbon atoms in a straight or branched, having 1-8 carbon atoms or a straight or branched hydroxyalkyl group, acyloxyalkyl group having a carbon number of 2-8 straight chain or branched, straight chain or branched alkoxy group having 2-8 carbon atoms, a haloalkyl group having 1-8 carbon atoms or a straight or branched 1-8 carbon atoms or an alkyl group having a straight or branched phosphonooxy, X1 X amino groups at the2 and X3 halogeno or both, X2 and X3 1-8 are all carbon atoms or an alkoxy group linear or branched, or X2 is a hydroxy group, X3 genoji and halo, R1 and R2 acyloxyalkyl group having 2-8 carbon atoms in a straight chain or branched all of the present invention.

[claim2]
2. Method according to claim 1, in the formula (1), the X1 cyclobutyl purine derivative is a chloro group, a tautomer or stereoisomer thereof, or a salt thereof, a solvate or hydrate thereof.

[claim3]
3. Method according to claim 1, in the formula (1), the X2 cyclobutyl purine derivative is an amino group, a tautomer or stereoisomer thereof, or a salt thereof, a solvate or hydrate thereof.

[claim4]
4. Method according to claim 1, in the formula (1), the R1 and R2 cyclobutyl purine derivative is a hydroxymethyl group, a tautomer or stereoisomer thereof, or a salt thereof, a solvate or hydrate thereof.

[claim5]
5. Method according to claim 1, in the formula (1), the X1 is a chloro group or a methoxy group, the X2 is amino group, the R1 and R2 cyclobutyl purine derivative is a hydroxymethyl group, a tautomer or stereoisomer thereof, or a salt thereof, a solvate or hydrate thereof.

[claim6]
6. Method according to claim 1, 6-- amino - -2- - chloro - -9- [trans-trans - -2,3- - bis (hydroxymethyl) cyclobutyl] purine or 6-- amino - -9- - methoxy - -2- - thio - [trans-trans - -2,3- - bis (hydroxymethyl) cyclobutyl] purine, a tautomer or stereoisomer thereof, or their salts, solvates or hydrates of the cyclobutyl purine derivative, a tautomer or stereoisomer thereof, or a salt thereof, solvate or hydrate thereof.

[claim7]
7. Represented by the following general formula (1') cyclobutyl purine derivative, a tautomer or stereoisomer thereof, or their salts, solvates or hydrates of about wound healing, alzheimer's therapeutic, prophylactic of Alzheimer's disease, ischemic disease treating agent, a hair growth agent for the prophylaxis and infarct disease selected from the group consisting of one or more medicines: in the general formula (1') in, X1 'is a halogeno group, an alkyl group having 1-8 carbon atoms or a straight or branched, having 1-8 carbon atoms in a straight chain or branched alkyl group, thio group (thiol group), an amino group, a hydroxy group, an alkoxy group having 1-8 carbon atoms in a straight or branched, having 1-8 carbon atoms in a straight chain or branched alkynyl group or a cyano group, X2 'is a halogeno group, amino group, a hydroxy group, an alkoxy group having 1-8 carbon atoms in a straight or branched, a thio group (thiol group) or thio group having 1-8 carbon atoms and is straight or branched alkyl, X3 'represents a hydrogen atom, a halogeno group, 1-8 linear or branched alkyl groups of carbon atoms, having 1-8 carbon atoms in a straight chain or branched alkylthio group, an amino group, a hydroxy group, an alkoxy group having 1-8 carbon atoms in a straight or branched, and hydroxyl group or a carbamoyl group, R1 ' and R2 'may be the same or different, each represents a hydrogen atom, a halogeno group, a carboxyl group, linear or branched alkyl group having 1-8 carbon atoms, linear or branched acyl group having a carbon number of 1-8, a carbamoyl group, an acyloxy group having 1-8 carbon atoms in a straight or branched, a carbon number of 1-8 linear or branched hydroxyalkyl group, acyloxyalkyl group having a carbon number of 2-8 straight chain or branched, having 2-8 carbon atoms in a straight chain or branched alkoxy group, a haloalkyl group having 1-8 carbon atoms or a straight or branched 1-8 carbon atoms or an alkyl group having a straight or branched phosphonooxy, X1 'X amino group and3 'which is a hydrogen atom, R1 ' and R2 'is a 1-8 linear or branched hydroxyalkyl group having carbon atoms other than carbon atoms or a substituent group.

[claim8]
8. Method according to claim 7, wherein in the general formula (1'), the X1 'medicament is chloro group.

[claim9]
9. Method according to claim 7, wherein in general formula (1'), the X2 'drug is an amino group.

[claim10]
10. Method according to claim 7, wherein in the general formula (1'), the R1 ' and R2 'medicament having a hydroxymethyl group.

[claim11]
11. Method according to claim 7, wherein in general formula (1'), the X1 'is a chloro group or a methoxy group, the X2 'is amino group, the X3 'is a hydrogen atom, the R1 ' and R2 'medicament is a hydroxymethyl group.

[claim12]
12. AMEND STATUS: Delete

[claim13]
13. AMEND STATUS: deletion

[claim14]
14. AMEND STATUS: deletion
  • 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
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