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    • 1. 发明公开
    • Aminoguanidine derivatives and inhibitory agents on maillard reaction containing them as active ingredients
    • 氨基胍衍生物以及含有它们作为活性成分的美拉德反应抑制物质。
    • EP0325936A2
    • 1989-08-02
    • EP89100345.1
    • 1989-01-10
    • ONO PHARMACEUTICAL CO., LTD.
    • Ohuchida, Shuichi Ono Pharmaceutical Co., Ltd.Toda, Masaaki Ono Pharmaceutical Co., Ltd.Miyamoto, Tsumoru Ono Pharmaceutical Co., Ltd.
    • C07C133/10C07D213/76A61K31/155A61K31/44
    • C07D213/77C07C281/16
    • An aminoguanidine derivative of the general formula:
      (wherein, R 1b represents carbocyclic or heterocyclic ring substituted or unsubstituted by from 1 to 3 group(s) selected from halogen atom, alkyl or alkoxy group of from 1 to 4 carbon atom(s), nitro group, phenoxy group, amino group, hydroxy group and acylamino group of from 2 to 4 carbon atom(s), X b represents single-bond, alkylene group of from 1 to 4 carbon atom(s) or alkenylene group of from 2 to 4 carbon atoms, or R 1b together with X b represents alkyl group of from 1 to 4 carbon atom(s), R 2b represents hydrogen atom, alkyl group of from 1 to 4 carbon atom(s) or phenyl group substituted or unsubstituted by from 1 to 3 group(s) selected from halogen atom, alkyl or alkoxy group of from 1 to 4 carbon atom(s), hydroxy and nitro group.), or an acid addition salt thereof possesses inhibitory activity on Maillard reaction, and these is useful for prevention and/or treatment of several diabetic complications and deseases induced by aging.
    • 通式的氨基胍衍生物:(worin,R <1B> darstellt碳环或由选自卤素原子,烷基或烷氧基中选择的1至4个碳1〜3组(多个)的杂环substituiertem奥德unsubstituiertem 原子(一个或多个),硝基,苯氧基,氨基,羟基和酰氨基的2至4个碳原子(一个或多个),XB darstellt单键,亚烷基,1〜4个碳原子的(S)或亚烯基的 从2至4个碳原子的基团,或R <1B>与XB darstellt烷基,1至4个碳原子(一个或多个)中,R <2B> darstellt氢原子,烷基,1至4个碳原子的(一起小号 ),或者被选自卤素原子,烷基或具有1至4个碳原子(一个或多个),羟基和硝基的烷氧基基团选自1至3个基团的苯基substituiertem奥德unsubstituiertem。),或酸加成盐具有 上的美拉德反应,和合成的抑制活性是用于预防和/或治疗糖尿病并发症和几个deseases的INDU有用 老化土木工程署。
    • 2. 发明公开
    • Carbazoyl derivatives
    • 卡博基衍生物
    • EP0323590A3
    • 1990-05-02
    • EP88120926.6
    • 1988-12-14
    • ONO PHARMACEUTICAL CO., LTD.
    • Ohuchida, Shuichi Ono Pharmaceutical Co., Ltd.Toda, Masaaki Ono Pharmaceutical Co., Ltd.Miyamoto, Tsumoru Ono Pharmaceutical Co., Ltd.
    • C07C109/06C07C133/02C07D213/79A61K31/175
    • C07D213/87C07C243/28C07C243/32C07C243/36C07C243/38C07C281/06C07C2601/08C07C2601/14
    • A carbazoyl derivative of the general formula:
      (wherein, R 1b represents a bond, alkylene group of from 1 to 6 carbon atom(s) or alkenylene group of from 2 to 6 carbon atoms,
      R 2b represents a carbocyclic or heterocyclic ring unsubstituted or substituted by from one to three halogen atom(s), hydroxy group, nitro group, amino group, alkyl or alkoxy group of from 1 to 4 carbon atom(s), 3-aminoureido group, phenoxy group or acylamino group of from 2 to 5 carbon atoms, or R 1b together with R 2b , represents an alkyl group of from 1 to 12 carbon atom(s) unsubstituted or substituted by 3-aminoureido group,
      R 3b represents (1) a hydrogen atom,
      (2) an alkyl group of from 1 to 6 carbon atom(s) or
      (3) a phenyl or benzyl group unsubstituted or substituted by from one to three halogen atom, alkyl or alkoxy group of from 1 to 4 carbon atom(s), hydroxy group or nitro group,
      X b represents a bond or imino gorup,
      with the proviso that the compounds wherein the groups shown by X b -R 1b -R 2b represent a phenyl group, 4-aminophenyl gorup, anilino group and 2-thienyl group and the groups shown by R 3b represent a hydrogen atom, are excluded.), or an acid addition salt thereof possesses inhibitory activity on Maillard reaction, and therfore is useful for treating and/or prevention of several diabetic complications and deseases induced by aging.
    • 咔唑基衍生物,其通式为:CHEM(其中R 1b表示键,1-6个碳原子的亚烷基或2至6个碳原子的亚烯基,R 2b表示 未取代或被一至三个卤素原子,羟基,硝基,氨基,1-4个碳原子的烷基或烷氧基取代或被取代的碳环或杂环,3-氨基脲基,苯氧基 或2至5个碳原子的酰基氨基或R 1b与R 2b一起代表未被取代或被3-氨基脲基取代的1至12个碳原子的烷基,R 3b, 代表(1)氢原子,(2)1至6个碳原子的烷基或(3)未被取代或被一至三个卤素原子取代的苯基或苄基,烷基或烷氧基 1至4个碳原子,羟基或硝基,Xb表示键或亚氨基,条件是其中由Xb-R 1b -R 2b表示的基团, 代表苯基,4-氨基苯基gorup,苯胺基和2-噻吩基,R 3b所示的基团代表氢原子),或其酸加成盐对美拉德反应具有抑制活性, 因此可用于治疗和/或预防由老化引起的若干糖尿病并发症和疾病。
    • 4. 发明公开
    • Aminoguanidine derivatives
    • 氨基嘌呤衍生物
    • EP0339496A3
    • 1991-05-08
    • EP89107168.0
    • 1989-04-20
    • ONO PHARMACEUTICAL CO., LTD.
    • Ohuchida, Shuichi Ono Pharmaceutical Co., Ltd.Toda, Masaaki Ono Pharmaceutical Co., Ltd.Miyamoto, Tsumoru Ono Pharmaceutical Co., Ltd.
    • C07C133/10C07D295/12C07D211/46C07D213/81C07D217/04A61K31/155A61K31/395A61K31/34
    • C07D213/75C07C281/16C07C2601/08C07C2601/14C07D211/46C07D217/06C07D295/215C07D307/52
    • A aminoguanidine derivatives of the general formula:
      (wherein, R 1b represents a hydrogen atom, alkyl group of from 1 to 6 carbon atom(s), cycloalkyl group of from 5 to 7 carbon atoms or carbocyclic or heterocyclic ring unsubstituted or substituted by from one to three halogen atom(s), alkyl group(s) of from 1 to 4 carbon atom(s), alkoxy group(s) of from 1 to 4 carbon atom(s) or nitro group, X b represents a bond, alkylene group of from 1 to 4 carbon atom(s) or alkenylene group of from 2 to 4 carbon atoms,
      R 2b represents a hydrogen atom, alkyl group of from 1 to 6 carbon atom(s) or phenyl group,
      R 3b represents a hydrogen atom, phenyl group, alkyl group of from 1 to 4 carbon atom(s), phenylalkyl group of from 7 to 10 carbon atoms or pyridyl group
      represents a heterocyclic ring, which contains nitrogen atom or one nitrogen and one oxygen atom, of from 3 to 10 carbon atoms unsubstituted or substituted by a hydroxy group. With the proviso that the compounds wherein R 2b represents a hydrogen atom, -X b -R 1b represents a hydrogen atom, methyl group, ethyl group or phenyl group and R 3b represents a hydrogen atom or methyl group, are excluded.) or acid addition salt thereof possess inhibitory activity on Maillard reaciton, and therefore is useful for treating and/or prevention of several diabetic complications and diseases induced by aging.
    • 具有以下通式的氨基胍衍生物:其中R 1b表示氢原子,1至6个碳原子的烷基,5至7个碳原子的环烷基或碳环或杂环 未取代或被1至3个卤素原子取代,1至4个碳原子的烷基,1至4个碳原子的烷氧基或硝基,Xb 表示1〜4个碳原子的亚烷基或2〜4个碳原子的亚链烯基,R 2b表示氢原子,1〜6个碳原子的烷基或苯基 基团,R 3b表示氢原子,苯基,1至4个碳原子的烷基,7至10个碳原子的苯基烷基或吡啶基表示含有氮的杂环 原子或一个氮原子和一个氧原子,未被取代或被羟基取代的3-10个碳原子,条件是其中R 2b, 表示氢原子,-Xb-R 1b表示氢原子,甲基,乙基或苯基,R 3b表示氢原子或甲基))或其酸加成盐具有抑制活性 在美拉德反应中,因此可用于治疗和/或预防几种糖尿病并发症和老化引起的疾病。
    • 5. 发明公开
    • Aminoguanidine derivatives
    • 氨基胍衍生物
    • EP0339496A2
    • 1989-11-02
    • EP89107168.0
    • 1989-04-20
    • ONO PHARMACEUTICAL CO., LTD.
    • Ohuchida, Shuichi Ono Pharmaceutical Co., Ltd.Toda, Masaaki Ono Pharmaceutical Co., Ltd.Miyamoto, Tsumoru Ono Pharmaceutical Co., Ltd.
    • C07C133/10C07D295/12C07D211/46C07D213/81C07D217/04A61K31/155A61K31/395A61K31/34
    • C07D213/75C07C281/16C07C2601/08C07C2601/14C07D211/46C07D217/06C07D295/215C07D307/52
    • A aminoguanidine derivatives of the general formula:
      (wherein, R 1b represents a hydrogen atom, alkyl group of from 1 to 6 carbon atom(s), cycloalkyl group of from 5 to 7 carbon atoms or carbocyclic or heterocyclic ring unsubstituted or substituted by from one to three halogen atom(s), alkyl group(s) of from 1 to 4 carbon atom(s), alkoxy group(s) of from 1 to 4 carbon atom(s) or nitro group, X b represents a bond, alkylene group of from 1 to 4 carbon atom(s) or alkenylene group of from 2 to 4 carbon atoms,
      R 2b represents a hydrogen atom, alkyl group of from 1 to 6 carbon atom(s) or phenyl group,
      R 3b represents a hydrogen atom, phenyl group, alkyl group of from 1 to 4 carbon atom(s), phenylalkyl group of from 7 to 10 carbon atoms or pyridyl group
      represents a heterocyclic ring, which contains nitrogen atom or one nitrogen and one oxygen atom, of from 3 to 10 carbon atoms unsubstituted or substituted by a hydroxy group.
      With the proviso that the compounds wherein R 2b represents a hydrogen atom, -X b -R 1b represents a hydrogen atom, methyl group, ethyl group or phenyl group and R 3b represents a hydrogen atom or methyl group, are excluded.) or acid addition salt thereof possess inhibitory activity on Maillard reaciton, and therefore is useful for treating and/or prevention of several diabetic complications and diseases induced by aging.
    • 具有以下通式的氨基胍衍生物:其中R 1b表示氢原子,1至6个碳原子的烷基,5至7个碳原子的环烷基或碳环或杂环 未取代或被1至3个卤素原子取代,1至4个碳原子的烷基,1至4个碳原子的烷氧基或硝基,Xb 表示1〜4个碳原子的亚烷基或2〜4个碳原子的亚链烯基,R 2b表示氢原子,1〜6个碳原子的烷基或苯基 基团,R 3b表示氢原子,苯基,1至4个碳原子的烷基,7至10个碳原子的苯基烷基或吡啶基表示含有氮的杂环 原子或一个氮原子和一个氧原子,未被取代或被羟基取代的3-10个碳原子,条件是其中R 2b, 表示氢原子,-Xb-R 1b表示氢原子,甲基,乙基或苯基,R 3b表示氢原子或甲基))或其酸加成盐具有抑制活性 在美拉德反应中,因此可用于治疗和/或预防几种糖尿病并发症和老化引起的疾病。
    • 6. 发明公开
    • Carbazoyl derivatives
    • 肼衍。
    • EP0323590A2
    • 1989-07-12
    • EP88120926.6
    • 1988-12-14
    • ONO PHARMACEUTICAL CO., LTD.
    • Ohuchida, Shuichi Ono Pharmaceutical Co., Ltd.Toda, Masaaki Ono Pharmaceutical Co., Ltd.Miyamoto, Tsumoru Ono Pharmaceutical Co., Ltd.
    • C07C109/06C07C133/02C07D213/79A61K31/175
    • C07D213/87C07C243/28C07C243/32C07C243/36C07C243/38C07C281/06C07C2601/08C07C2601/14
    • A carbazoyl derivative of the general formula:
      (wherein, R 1b represents a bond, alkylene group of from 1 to 6 carbon atom(s) or alkenylene group of from 2 to 6 carbon atoms,
      R 2b represents a carbocyclic or heterocyclic ring unsubstituted or substituted by from one to three halogen atom(s), hydroxy group, nitro group, amino group, alkyl or alkoxy group of from 1 to 4 carbon atom(s), 3-aminoureido group, phenoxy group or acylamino group of from 2 to 5 carbon atoms, or R 1b together with R 2b , represents an alkyl group of from 1 to 12 carbon atom(s) unsubstituted or substituted by 3-aminoureido group,
      R 3b represents (1) a hydrogen atom,
      (2) an alkyl group of from 1 to 6 carbon atom(s) or
      (3) a phenyl or benzyl group unsubstituted or substituted by from one to three halogen atom, alkyl or alkoxy group of from 1 to 4 carbon atom(s), hydroxy group or nitro group,
      X b represents a bond or imino gorup,
      with the proviso that the compounds wherein the groups shown by X b -R 1b -R 2b represent a phenyl group, 4-aminophenyl gorup, anilino group and 2-thienyl group and the groups shown by R 3b represent a hydrogen atom, are excluded.),
      or an acid addition salt thereof possesses inhibitory activity on Maillard reaction, and therfore is useful for treating and/or prevention of several diabetic complications and deseases induced by aging.
    • 咔唑基衍生物,其通式为:CHEM(其中R 1b表示键,1-6个碳原子的亚烷基或2至6个碳原子的亚烯基,R 2b表示 未取代或被一至三个卤素原子,羟基,硝基,氨基,1-4个碳原子的烷基或烷氧基取代或被取代的碳环或杂环,3-氨基脲基,苯氧基 或2至5个碳原子的酰基氨基或R 1b与R 2b一起代表未被取代或被3-氨基脲基取代的1至12个碳原子的烷基,R 3b, 代表(1)氢原子,(2)1至6个碳原子的烷基或(3)未被取代或被一至三个卤素原子取代的苯基或苄基,烷基或烷氧基 1至4个碳原子,羟基或硝基,Xb表示键或亚氨基,条件是其中由Xb-R 1b -R 2b表示的基团, 代表苯基,4-氨基苯基gorup,苯胺基和2-噻吩基,R 3b所示的基团代表氢原子),或其酸加成盐对美拉德反应具有抑制活性, 因此可用于治疗和/或预防由老化引起的若干糖尿病并发症和疾病。