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    5-Substituted amino-4-hydroxy-pentenoic acid derivatives and their use
    1.
    发明公开
    5-Substituted amino-4-hydroxy-pentenoic acid derivatives and their use 失效
    5-取代的氨基-4-羟基 - 苯甲酸衍生物及其用途

    公开(公告)号：EP0272583A3

    公开(公告)日：1990-01-10

    申请号：EP87118570.8

    申请日：1987-12-15

    申请人： Banyu Pharmaceutical Co., Ltd.

    发明人： Tanaka, Seiichi ,  Koike, Yutaka ,  Nakano, Masato ,  Atsuumi, Shugo ,  Morishima, Hajime ,  Matsuyama, Kenji

    IPC分类号： C07K5/02 ,  C07K5/06 ,  A61K37/64

    CPC分类号： C07K5/0207 ,  A61K38/00 ,  Y02P20/55

    摘要： A 5-substituted amino-4-hydroxy-pentenoic acid or its salt represented by the formula:
    wherein each of R¹ and R² which may be the same or different is a hydrogen atom, a lower alkyl group, an aralkyl group, a lower alkoxycarbonyl group, an aryloxycarbonyl group, an aralkyloxycarbonyl group or a lower alkanoyl group which may be substituted by from one to three substituents selected from the group consisting of an amino group, a hydroxyl group, a carboxyl group, an aryloxy group, an aralkyloxycarbonylamino group, a lower alkoxycarbonylamino group and a
    group (wherein each of X¹ and X² which may be the same or different is a hydrogen atom, a lower alkyl group, an aryl group or an aralkyl group, or X¹ and X² form together with the adjacent nitrogen atom a 5- or 6-membered heterocyclic group which may further contain a hetero atom selected from the group consisting of a nitrogen atom, an oxygen atom and a sulfur atom) and which may further contain a double bond in its carbon chain, each of R³, R⁴ and R⁶ which may be the same or different is a hydrogen atom, a lower alkyl group, a cycloalkyl group, a cycloalkylalkyl group, an aryl group, an aralkyl group or a residue of an acidic, neutral or basic amino acid, R⁵ is a hydrogen atom or a lower alkyl group, R⁷ is a hydrogen atom, a lower alkyl, cycloalkyl, cycloalkylalkyl or aralkyl group which may be substituted by one or two hydroxyl groups or a residue of an acidic, neutral or basic amino acid, R⁸ is a hydroxyl group, a -OY group (wherein Y is a lower alkyl group, an aryl group, an aralkyl group, a lower alkoxyalkyl group, a lower alkanoyloxyalkyl group, a lower alkoxycarbonyloxyalkyl group, or a 1-phthalidyl group) or a
    group (wherein each of Y¹ and Y² which may be the same or different is a hydrogen atom, a lower alkyl group, an aryl group, an aralkyl group or a cycloalkyl group, or Y¹ and Y² form together with the adjacent nitrogen atom a 5- or 6-membered heterocyclic group which may further contain a hetero atom selected from the group consisting of a nitrogen atom, an oxygen atom and a sulfur atom), and each of n and m which may be the same or different is 0 or 1.

    N-acylamino acid derivatives and their use
    3.
    发明公开
    N-acylamino acid derivatives and their use 失效
    N-乙酰氨基酸衍生物及其用途

    公开(公告)号：EP0309766A3

    公开(公告)日：1990-06-13

    申请号：EP88114374.7

    申请日：1988-09-02

    申请人： BANYU PHARMACEUTICAL CO., LTD.

    发明人： Morishima, Hajime ,  Koike, Yutaka ,  Nakano, Masato ,  Atsuumi, Shugo ,  Tanaka, Seiichi ,  Matsuyama, Kenji

    IPC分类号： C07C317/00 ,  C07D295/088 ,  C07C323/60 ,  C07D295/24 ,  C07C239/08 ,  A61K31/33 ,  A61K31/195

    CPC分类号： C07D207/08 ,  C07C59/66 ,  C07C323/00 ,  C07C323/43 ,  C07D211/14 ,  C07D215/12 ,  C07D233/64 ,  C07D239/38 ,  C07D257/04 ,  C07D285/125 ,  C07D295/084 ,  C07D295/125 ,  C07D295/13 ,  C07D295/24 ,  C07D307/38 ,  C07D319/18 ,  C07D401/12 ,  C07F7/1856

    摘要： An N-acylamino acid derivative of the formula:
    wherein each of R¹, R², R⁴ and R⁶ is hydrogen, lower alkyl, cycloalkyl, cycloalkylalkyl, aryl, aralkyl or a monocyclic or bicyclic heterocyclic group containing from 1 to 4 hetero atoms; each of R³ and R⁵ is hydrogen or lower alkyl; A is -CH(OH)-(CH₂) q R⁷ wherein R⁷ is hydrogen, lower alkyl, cycloalkyl, cyloalkylalkyl, aryl, aralkyl, a monocyclic or bicyclic heterocyclic group containing from 1 to 4 hetero atoms or -E-R¹⁰ wherein E is -S(O) i - wherein i is 0, 1 or 2, oxygen, -NR¹¹- wherein R¹¹ is hydrogen, lower alkyl, cycloalkyl, cycloalkylalkyl, aryl or aralkyl, or
    wherein each of R¹² and R¹³ is hydrogen, lower alkyl, cycloalkyl, cycloalkylalkyl, aryl or aralkyl, and R¹⁰ is hydrogen, lower alkyl, cycloalkyl, cycloalkylalkyl, aryl, aralkyl or a monocyclic or bicyclic heterocyclic group containing from 1 to 4 hetero atoms provided that when R¹⁰ is hydrogen, i is 0, and q is an integer of from 0 to 5; or -CH₂-CHR⁸-CO-R⁹ wherein R⁸ is hydrogen, lower alkyl, cycloalkyl, cycloalkylalkyl, aryl, aralkyl or a monocyclic or bicyclic heterocyclic group containig from 1 to 4 hetero atoms, and R⁹ is hydroxyl, -OX wherein X is alkyl, aryl, lower alkoxycarbonyloxyalkyl or 1-phthalidyl, or -N(Y¹)(Y²) wherein each of Y¹ and Y² is hydrogen, lower alkyl, aryl, aralkyl or cycloalkyl, or Y¹ and Y² form together with the adjacent nitrogen atom a 5- or 6-membered heterocyclic group which may contain a further hetero atom; m is 0, 1 or 2; and n is an integer of from 1 to 5, provided that when R¹ is hydrogen, m is 0; or a salt thereof, which is useful as hypotensive drugs.

    5-Substituted amino-4-hydroxy-pentanoic acid derivatives and their use
    4.
    发明公开
    5-Substituted amino-4-hydroxy-pentanoic acid derivatives and their use 失效
    5-取代的氨基-4-羟基 - 戊酸衍生物及其用途

    公开(公告)号：EP0264106A3

    公开(公告)日：1990-02-07

    申请号：EP87114954.8

    申请日：1987-10-13

    申请人： Banyu Pharmaceutical Co., Ltd.

    发明人： Koike, Yutaka ,  Nakano, Masato ,  Atsuumi, Shugo ,  Tanaka, Seiichi ,  Morishima, Hajime ,  Matsuyama, Kenji

    IPC分类号： C07K5/02 ,  C07D263/04 ,  A61K37/02 ,  A61K31/13

    CPC分类号： C07D263/04 ,  A61K38/00 ,  C07D263/06 ,  C07D413/14 ,  C07K5/0207 ,  C07K5/0227 ,  Y02P20/55 ,  Y10S530/86

    摘要： A 5-substituted amino-4-hydroxy-pentanoic acid derivative having the formula:
    wherein R¹ is a hydrogen atom, a lower alkoxycarbonyl group, an aryloxycarbonyl group, an aralkyloxycarbonyl group or a lower alkanoyl group which may be substituted by from one to three substituents selected from the group consisting of an amino group, a hydroxyl group, a carboxyl group, an aryloxy group, an aralkyloxycarbonylamino group, a lower alkoxycarbonylamino group
    wherein each of X¹ and X² which may be the same or different is a hydrogen atom, a lower alkyl group, an aryl group or an aralkyl group, or X¹ and X² form together with the adjacent nitrogen atom a 5- or 6-membered heterocyclic group which may further contain a hereto atom selected from the group consisting of a nitrogen atom, an oxygen atom and a sulfur atom which may further contain a double bond in its carbon chain, each of R², R³ and R⁵ which may be the same or different is a hydrogen atom, a lower alkyl group or a residue of an acidic, neutral or basic amino acid, R⁴ is a hydrogen atom or a lower alkyl group, R⁶ is a lower alkyl, cycloalkyl, cycloalkylalkyl or aralkyl group which is substituted by one or two hydroxyl groups, R⁷ is a hydroxyl group, a -OY group wherein Y is a lower alkyl group, an aryl group, an aralkyl group, a lower alkoxyalkyl group, a lower alkanoyloxyalkyl group, a lower alkoxycarbonyloxyalkyl group or a 1-phthalidyl group,
    wherein each of Y¹ and Y² which may be the same or different is a hydrogen atom, a lower alkyl group, an aryl group, an aralkyl group or a cycloalkyl group, or Y¹ and Y² form together with the adjacent nitrogen atom 5- or 5-membered heterocyclic group which may further contain a hereto atom selected from the group consisting of a nitrogen atom, an oxygen atom and a sulfur atom, and each of n and m which may be the same or different is 0 or 1.

    5-Substituted amino-4-hydroxy-pentenoic acid derivatives and their use
    5.
    发明公开
    5-Substituted amino-4-hydroxy-pentenoic acid derivatives and their use 失效
    N-取代基衍生物5-Amino-4-羟基 - 戊酸酯和Anwendung。

    公开(公告)号：EP0272583A2

    公开(公告)日：1988-06-29

    申请号：EP87118570.8

    申请日：1987-12-15

    申请人： Banyu Pharmaceutical Co., Ltd.

    发明人： Tanaka, Seiichi ,  Koike, Yutaka ,  Nakano, Masato ,  Atsuumi, Shugo ,  Morishima, Hajime ,  Matsuyama, Kenji

    IPC分类号： C07K5/02 ,  C07K5/06 ,  A61K37/64

    CPC分类号： C07K5/0207 ,  A61K38/00 ,  Y02P20/55

    摘要： A 5-substituted amino-4-hydroxy-pentenoic acid or its salt represented by the formula:
    wherein each of R¹ and R² which may be the same or different is a hydrogen atom, a lower alkyl group, an aralkyl group, a lower alkoxycarbonyl group, an aryloxycarbonyl group, an aralkyloxycarbonyl group or a lower alkanoyl group which may be substituted by from one to three substituents selected from the group consisting of an amino group, a hydroxyl group, a carboxyl group, an aryloxy group, an aralkyloxycarbonylamino group, a lower alkoxycarbonylamino group and a
    group (wherein each of X¹ and X² which may be the same or different is a hydrogen atom, a lower alkyl group, an aryl group or an aralkyl group, or X¹ and X² form together with the adjacent nitrogen atom a 5- or 6-membered heterocyclic group which may further contain a hetero atom selected from the group consisting of a nitrogen atom, an oxygen atom and a sulfur atom) and which may further contain a double bond in its carbon chain, each of R³, R⁴ and R⁶ which may be the same or different is a hydrogen atom, a lower alkyl group, a cycloalkyl group, a cycloalkylalkyl group, an aryl group, an aralkyl group or a residue of an acidic, neutral or basic amino acid, R⁵ is a hydrogen atom or a lower alkyl group, R⁷ is a hydrogen atom, a lower alkyl, cycloalkyl, cycloalkylalkyl or aralkyl group which may be substituted by one or two hydroxyl groups or a residue of an acidic, neutral or basic amino acid, R⁸ is a hydroxyl group, a -OY group (wherein Y is a lower alkyl group, an aryl group, an aralkyl group, a lower alkoxyalkyl group, a lower alkanoyloxyalkyl group, a lower alkoxycarbonyloxyalkyl group, or a 1-phthalidyl group) or a
    group (wherein each of Y¹ and Y² which may be the same or different is a hydrogen atom, a lower alkyl group, an aryl group, an aralkyl group or a cycloalkyl group, or Y¹ and Y² form together with the adjacent nitrogen atom a 5- or 6-membered heterocyclic group which may further contain a hetero atom selected from the group consisting of a nitrogen atom, an oxygen atom and a sulfur atom), and each of n and m which may be the same or different is 0 or 1.

    摘要翻译： 5-取代的氨基-4-羟基戊烯酸或其由下式表示的盐：其中R 1和R 2各自可以相同或不同，是氢原子，低级烷基 可以被1〜3个选自氨基，羟基，羧基的取代基取代的芳烷基，芳烷基，低级烷氧基羰基，芳氧基羰基，芳烷氧基羰基或低级烷酰基 ，芳氧基，芳烷氧基羰基氨基，低级烷氧基羰基氨基和基（其中X 1和X 2各自可以相同或不同，为氢原子，低级烷基， 芳基或芳烷基，或X 1和X 2与相邻的氮原子一起形成5-或6-元杂环基，其可进一步含有选自氮原子， 氧原子和硫原子），并且其还可以含有双键 其碳链，R 3，R 4和R 6各自可以相同或不同，是氢原子，低级烷基，环烷基，环烷基烷基，芳基， 芳烷基或酸性，中性或碱性氨基酸的残基，R 5是氢原子或低级烷基，R 7是氢原子，低级烷基，环烷基，环烷基烷基或芳烷基，其可以 被一个或两个羟基或酸性，中性或碱性氨基酸的残基取代，R 8是羟基，-OY基（其中Y是低级烷基，芳基，芳烷基 ，低级烷氧基烷基，低级烷酰氧基烷基，低级烷氧基羰氧基烷基或1-对苯二酰基）或基（其中Y 1和Y 2各自可以相同或不同， 氢原子，低级烷基，芳基，芳烷基或环烷基，或Y 1和Y 2与相邻的氮原子一起形成5-或6-元杂环 可以进一步含有选自氮原子，氧原子和硫原子的杂原子的基团），n和m可以相同或不同，为0或1。

    N-acylamino acid derivatives and their use
    10.
    发明公开
    N-acylamino acid derivatives and their use 失效
    N-Acylaminosäurederivateund deren Verwendung。

    公开(公告)号：EP0309766A2

    公开(公告)日：1989-04-05

    申请号：EP88114374.7

    申请日：1988-09-02

    申请人： BANYU PHARMACEUTICAL CO., LTD.

    发明人： Morishima, Hajime ,  Koike, Yutaka ,  Nakano, Masato ,  Atsuumi, Shugo ,  Tanaka, Seiichi ,  Matsuyama, Kenji

    IPC分类号： C07C317/00 ,  C07D295/088 ,  C07C323/60 ,  C07D295/24 ,  C07C239/08 ,  A61K31/33 ,  A61K31/195

    CPC分类号： C07D207/08 ,  C07C59/66 ,  C07C323/00 ,  C07C323/43 ,  C07D211/14 ,  C07D215/12 ,  C07D233/64 ,  C07D239/38 ,  C07D257/04 ,  C07D285/125 ,  C07D295/084 ,  C07D295/125 ,  C07D295/13 ,  C07D295/24 ,  C07D307/38 ,  C07D319/18 ,  C07D401/12 ,  C07F7/1856

    摘要： An N-acylamino acid derivative of the formula:
    wherein each of R¹, R², R⁴ and R⁶ is hydrogen, lower alkyl, cycloalkyl, cycloalkylalkyl, aryl, aralkyl or a monocyclic or bicyclic heterocyclic group containing from 1 to 4 hetero atoms; each of R³ and R⁵ is hydrogen or lower alkyl; A is -CH(OH)-(CH₂) q R⁷ wherein R⁷ is hydrogen, lower alkyl, cycloalkyl, cyloalkylalkyl, aryl, aralkyl, a monocyclic or bicyclic heterocyclic group containing from 1 to 4 hetero atoms or -E-R¹⁰ wherein E is -S(O) i - wherein i is 0, 1 or 2, oxygen, -NR¹¹- wherein R¹¹ is hydrogen, lower alkyl, cycloalkyl, cycloalkylalkyl, aryl or aralkyl, or
    wherein each of R¹² and R¹³ is hydrogen, lower alkyl, cycloalkyl, cycloalkylalkyl, aryl or aralkyl, and R¹⁰ is hydrogen, lower alkyl, cycloalkyl, cycloalkylalkyl, aryl, aralkyl or a monocyclic or bicyclic heterocyclic group containing from 1 to 4 hetero atoms provided that when R¹⁰ is hydrogen, i is 0, and q is an integer of from 0 to 5; or -CH₂-CHR⁸-CO-R⁹ wherein R⁸ is hydrogen, lower alkyl, cycloalkyl, cycloalkylalkyl, aryl, aralkyl or a monocyclic or bicyclic heterocyclic group containig from 1 to 4 hetero atoms, and R⁹ is hydroxyl, -OX wherein X is alkyl, aryl, lower alkoxycarbonyloxyalkyl or 1-phthalidyl, or -N(Y¹)(Y²) wherein each of Y¹ and Y² is hydrogen, lower alkyl, aryl, aralkyl or cycloalkyl, or Y¹ and Y² form together with the adjacent nitrogen atom a 5- or 6-membered heterocyclic group which may contain a further hetero atom; m is 0, 1 or 2; and n is an integer of from 1 to 5, provided that when R¹ is hydrogen, m is 0; or a salt thereof, which is useful as hypotensive drugs.

    摘要翻译： 下式的N-酰基氨基酸衍生物：其中R 1，R 2，R 4和R 6各自为氢，低级烷基，环烷基，环烷基烷基，芳基，芳烷基或 含有1至4个杂原子的单环或双环杂环基; R 3和R 5各自为氢或低级烷基; A是-CH（OH） - （CH 2）q R 7，其中R 7是氢，低级烷基，环烷基，环烷基烷基，芳基，芳烷基，含有1至4个杂原子或-ER的单环或双环杂环基 其中E是-S（O）i-，其中i是0,1或2，氧，-NR 1 - ，其中R 1是氢，低级烷基， 环烷基，环烷基烷基，芳基或芳烷基或CHEM，其中R 1和R 3各自为氢，低级烷基，环烷基，环烷基烷基，芳基或芳烷基，R 1， 0是氢，低级烷基，环烷基，环烷基烷基，芳基，芳烷基或含有1至4个杂原子的单环或双环杂环基，条件是当R 1为氢时，i为0，q为 0到5的整数; 或-CH 2 -CHR 8 -CO-R 9其中R 8是氢，低级烷基，环烷基，环烷基烷基，芳基，芳烷基或含1-4个杂原子的单环或双环杂环基，R 其中X是烷基，芳基，低级烷氧基羰基氧基烷基或1-苯酞基，或-N（Y 1）（Y 2），其中Y 1和Y 2各自为 氢，低级烷基，芳基，芳烷基或环烷基，或Y 1和Y 2与相邻的氮原子一起形成可含有另外的杂原子的5-或6-元杂环基; m为0,1或2; 且n为1至5的整数，条件是当R 1为氢时，m为0; 或其盐，其可用作降压药物。