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

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

    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

    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

    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

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

    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

    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。