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    Rhodanine derivatives, process for their preparation, and aldose reductase inhibitor containing the rhodanine derivatives as active ingredient
    2.
    发明授权
    Rhodanine derivatives, process for their preparation, and aldose reductase inhibitor containing the rhodanine derivatives as active ingredient 失效
    罗丹宁衍生物，其制备方法和含有绕丹宁衍生物作为活性成分的醛糖还原酶抑制剂

    公开(公告)号：US4464382A

    公开(公告)日：1984-08-07

    申请号：US292076

    申请日：1981-08-12

    申请人： Tadao Tanouchi ,  Masanori Kawamura ,  Akio Ajima ,  Tetsuya Mohri ,  Masaki Hayashi ,  Hiroshi Terashima ,  Fumio Hirata ,  Takeshi Morimura

    发明人： Tadao Tanouchi ,  Masanori Kawamura ,  Akio Ajima ,  Tetsuya Mohri ,  Masaki Hayashi ,  Hiroshi Terashima ,  Fumio Hirata ,  Takeshi Morimura

    IPC分类号： C12N9/99 ,  A61K31/425 ,  A61K31/426 ,  A61K31/44 ,  A61P3/08 ,  A61P27/02 ,  A61P27/12 ,  A61P43/00 ,  C07D277/20 ,  C07D277/36 ,  C07D333/00 ,  C07D417/06 ,  C07D417/14

    CPC分类号： C07D277/20

    摘要： The rhodanine derivatives of the general formula: ##STR1## wherein (I) R.sup.1 and R.sup.2 are taken together to represent a tetramethylene or pentamethylene group; (II) R.sup.1 represents a hydrogen atom, and R.sup.2 represents (1) a cycloalkyl or cycloalkenyl group of 4-7 carbon atoms which is unsubstituted or substituted by at least one alkyl group of 1-4 carbon atoms, (2) an anthryl or naphthyl group, (3) a phenyl group which is unsubstituted or substituted, (4) a heterocyclic group containing at least one of nitrogen, oxygen and sulfur atoms which is unsubstituted or substituted (5) a ##STR2## group (wherein R.sup.4 represents a hydrogen atom, a halogen atom, phenyl group or an alkyl group of 1-5 carbon atoms; and R.sup.5 represents a hydrogen atom, a phenyl group or an alkyl group of 1-5 carbon atoms) or ##STR3## group; or (III) R.sup.1 and R.sup.2, which may be the same or different with each other, each represents a phenyl group which is unsubstituted or substituted; and R.sup.3 represents a hydrogen atom, an alkyl group of 1-12 carbon atoms, an aralkyl group of 7-13 carbon atoms, a cycloalkyl or cycloalkenyl group of 4-7 carbon atoms which is unsubstituted or substituted by at least one alkyl group of 1-4 carbon atoms, or a phenyl group which is unsubstituted or substituted, possess a strong inhibitory activity on aldose reductase.

    摘要翻译： 通式：（I）的绕丹宁衍生物其中（I）R 1和R 2一起表示四亚甲基或五亚甲基; （II）R1表示氢原子，R2表示（1）未被取代或被至少一个1-4个碳原子的烷基取代的4-7个碳原子的环烷基或环烯基，（2）蒽基或 萘基，（3）未取代或取代的苯基，（4）含有未取代或取代的氮，氧和硫原子中的至少一个的杂环基（5）基团（其中R 4表示 氢原子，卤素原子，苯基或1-5个碳原子的烷基; R5表示氢原子，苯基或1-5个碳原子的烷基）或基团; 或（III）可以相同或不同的R 1和R 2各自表示未取代或取代的苯基; 并且R 3表示氢原子，1-12个碳原子的烷基，7-13个碳原子的芳烷基，4-7个碳原子的环烷基或环烯基，其未被取代或被至少一个烷基 1-4个碳原子或未取代或取代的苯基对醛糖还原酶具有强烈的抑制活性。

    Rhodanine derivatives, process for their preparation, and aldose reductase inhibitor containing the rhodanine derivatives as active ingredient
    3.
    发明授权
    Rhodanine derivatives, process for their preparation, and aldose reductase inhibitor containing the rhodanine derivatives as active ingredient 失效
    罗丹宁衍生物，其制备方法和含有绕丹宁衍生物作为活性成分的醛糖还原酶抑制剂

    公开(公告)号：US4831045A

    公开(公告)日：1989-05-16

    申请号：US96091

    申请日：1987-09-10

    申请人： Tadao Tanouchi ,  Masanori Kawamura ,  Akio Ajima ,  Tetsuya Mohri ,  Masaki Hayashi ,  Hiroshi Terashima ,  Fumio Hirata ,  Takeshi Morimura

    发明人： Tadao Tanouchi ,  Masanori Kawamura ,  Akio Ajima ,  Tetsuya Mohri ,  Masaki Hayashi ,  Hiroshi Terashima ,  Fumio Hirata ,  Takeshi Morimura

    IPC分类号： C12N9/99 ,  A61K31/425 ,  A61K31/426 ,  A61K31/44 ,  A61P3/08 ,  A61P27/02 ,  A61P27/12 ,  A61P43/00 ,  C07D277/20 ,  C07D277/36 ,  C07D333/00 ,  C07D417/06 ,  C07D417/14

    CPC分类号： C07D277/20

    摘要： The rhodanine derivatives of the general formula: ##STR1## [wherein (I) R.sup.1 and R.sup.2 are taken together to represent a tetramethylene or pentamethylene group; (II) R.sup.1 represents a hydrogen atom, and R.sup.2 represents (1) a cycloalkyl or cycloalkenyl group of 4-7 carbon atoms which is unsubstituted or substituted by at least one alkyl group of 1-4 carbon atoms, (2) an anthryl or naphthyl group, (3) a phenyl group which is unsubstituted or substituted by at least one of (a) halogen atom, (b) trifluoromethyl group, (c) hydroxyl group, (d) nitro group, (e) carboxyl group, (f) amino group which may be substituted by alkyl group(s) of 1-4 carbon atoms, (g) alkyl, alkoxy or alkylthio group of 1-5 carbon atoms, (h) phenyl group, (i) heterocyclic group containing at least one of nitrogen, oxygen and sulfur atoms which is unsubstituted or substituted by at least one of the above-described substituents (a) to (h), and (j) alkyl group of 1-4 carbon atoms which is substituted by at least one of the above-described substituents (c), (h) and (i), (4) a heterocyclic group containing at least one of nitrogen, oxygen and sulfur atoms which is unsubstituted or substituted by at least one of oxo group and the above-described substituents (a) to (h) and (j), or (5) a ##STR2## (wherein R.sup.4 represents a hydrogen atom, a halogen atom, phenyl group or an alkyl group of 1-5 carbon atoms; and R.sup.5 represents a hydrogen atom, a phenyl group or an alkyl group of 1-5 carbon atoms) or ##STR3## or (III) R.sup.1 and R.sup.2, which may be the same or different with each other, each represents a phenyl group which is unsubstituted or substituted by at least one of the above-described substituents (a) to (j); and R.sup.3 represents a hydrogen atom, an alkyl group of 1-12 carbon atoms, an aralkyl group of 7-13 carbon atoms, a cycloalkyl or cycloalkenyl group of 4-7 carbon atoms which is unsubstituted or substituted by at least one alkyl group of 1-4 carbon atoms, or a phenyl group which is unsubstituted or substituted by at least one of the above-described substituents (a) to (j)] and, when R.sup.3 represents a hydrogen atom, non-toxic salts of the acids possess a strong inhibitory activity on aldose reductase, and are useful for the prevention and treatment of nerve disturbances such as neuralgia, retinopathy, diabetic cataract and renal disturbances such as tubular nephropathy.

    Rhodanine derivatives, process for their preparation, and aldose reductase inhibitor containing the rhodanine derivatives as active ingredients
    4.
    发明授权
    Rhodanine derivatives, process for their preparation, and aldose reductase inhibitor containing the rhodanine derivatives as active ingredients 失效

    公开(公告)号：US4791126A

    公开(公告)日：1988-12-13

    申请号：US96808

    申请日：1987-09-10

    申请人： Tadao Tanouchi ,  Masanori Kawamura ,  Akio Ajima ,  Tetsuya Mohri ,  Masaki Hayashi ,  Hiroshi Terashima ,  Fumio Hirata ,  Takeshi Morimura

    发明人： Tadao Tanouchi ,  Masanori Kawamura ,  Akio Ajima ,  Tetsuya Mohri ,  Masaki Hayashi ,  Hiroshi Terashima ,  Fumio Hirata ,  Takeshi Morimura

    IPC分类号： C07D277/20 ,  C07D277/36 ,  A61K31/425

    CPC分类号： C07D277/20

    摘要： The rhodanine derivatives of the general formula: ##STR1## [wherein (I) R.sup.1 and R.sup.2 are taken together to represent a tetramethylene or pentamethylene group; (II) R.sup.1 represents a hydrogen atom, and R.sup.2 represents (1) a cycloalkyl or cycloalkenyl group of 4-7 carbon atoms which is unsubstituted or substituted by at least one alkyl group of 1-4 carbon atoms, (2) an anthryl or naphthyl group, (3) a phenyl group which is unsubstituted or substituted by at least one of (a) halogen atom, (b) trifluoromethyl group, (c) hydroxyl group, (d) nitro group, (e) carboxyl group, (f) amino group which may be substituted by alkyl group(s) of 1-4 carbon atoms, (g) alkyl, alkoxy or alkylthio group of 1-5 carbon atoms, (h) phenyl group, (i) heterocyclic group containing at least one of nitrogen, oxygen and sulfur atoms which is unsubstituted or substituted by at least one of the above-described substituents (a) to (h), and (j) alkyl group of 1-4 carbon atoms which is substituted by at least one of the above-described substituents (c), (h) and (i), (4) a heterocyclic group containing at least one of nitrogen, oxygen and sulfur atoms which is unsubstituted or substituted by at least one of oxo group and the above-described substituents (a) to (h) and (j), or (5) a ##STR2## group (wherein R.sup.4 represents a hydrogen atom, a halogen atom, phenyl group or an alkyl group of 1-5 carbon atoms; and R.sup.5 represents a hydrogen atom, a phenyl group or an alkyl group of 1-5 carbon atoms) or ##STR3## group; or (III) R.sup.1 and R.sup.2, which may be the same or different with each other, each represents a phenyl group which is unsubstituted or substituted by at least one of the above-described substituents (a) to (j); and R.sup.3 represents a hydrogen atom, an alkyl group of 1-12 carbon atoms, an aralkyl group of 7-13 carbon atoms, a cycloalkyl or cycloalkenyl group of 4-7 carbon atoms which is unsubstituted or substituted by at least one alkyl group of 1-4 carbon atoms, or a phenyl group which is unsubstituted or substituted by at least one of the above-described substituents (a) to (j)] and, when R.sup.3 represents hydrogen atom, non-toxic salts of the acids possess a strong inhibitory activity on aldose reductase, and are useful for the prevention and treatment of nerve disturbances such as neuralgia, retinopathy, diabetic cataract and renal disturbances such as tubular nephropathy.

    Novel cinnamoylamide derivatives
    5.
    发明授权
    Novel cinnamoylamide derivatives 失效
    新型氰胺衍生物

    公开(公告)号：US5093366A

    公开(公告)日：1992-03-03

    申请号：US691509

    申请日：1991-04-25

    申请人： Hisao Nakai ,  Hiroshi Terashima ,  Yoshinobu Arai

    发明人： Hisao Nakai ,  Hiroshi Terashima ,  Yoshinobu Arai

    IPC分类号： A61K8/44 ,  A61Q7/00 ,  A61Q19/00

    CPC分类号： A61K8/44 ,  A61Q19/00 ,  A61Q7/00

    摘要： A cinnamoylamide derivative of general formula: ##STR1## [wherein, (i) in case that R.sup.2 represents a methyl group and R.sup.3 represents a hydrogen atom,(R.sup.1).sub.n represents a group selected out of3-pentyl group,4-pentyl group,4-neopentyl group,4-(2-ethylbutyl) group,4-(2-methylpentyl) group,2-fluoro-4-pentyloxy group,4-butylthio group,4-cyclobutylmethyl group,4-cyclohexylmethyl group,4-(4-phenylbutyl) group and4-phenoxy group, and(ii) in case that R.sup.2 represents a hydrogen atom and R.sup.3 represents a methyl group,(R.sup.1).sub.n represents a group selected out of3-pentyl group and4-penethyl group.]or non-toxic salts thereof possess an inhibitory activity on 5.alpha.-reductase, and therefore be useful for treating and/or preventing agent for alopecia, acnes or prostatic hyperfrophy.