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    Prophylactic and therapeutic composition for circulatory disorders and method of treatment
    1.
    再颁专利
    Prophylactic and therapeutic composition for circulatory disorders and method of treatment 失效
    循环障碍的预防和治疗组合物及治疗方法

    公开(公告)号：USRE35801E

    公开(公告)日：1998-05-19

    申请号：US309558

    申请日：1994-09-20

    申请人： Hiroyoshi Nishi ,  Toshiaki Watanabe ,  Satoshi Yuki ,  Yasuhiro Morinaka ,  Katsuhiko Iseki ,  Hiroko Nakajima (nee Sakurai)

    发明人： Hiroyoshi Nishi ,  Toshiaki Watanabe ,  Satoshi Yuki ,  Yasuhiro Morinaka ,  Katsuhiko Iseki ,  Hiroko Nakajima (nee Sakurai)

    IPC分类号： C07D231/20 ,  C07D231/22 ,  C07D231/26 ,  C07D231/28 ,  C07D231/56 ,  A61K31/415

    CPC分类号： C07D231/56 ,  C07D231/20 ,  C07D231/22 ,  C07D231/26 ,  C07D231/28

    摘要： A prophylactic and therapeutic agent for circulatory disorders, comprising a pyrazolone derivative of the formula: ##STR1## wherein R.sub.1 represents a hydrogen atom, an aryl group, an alkyl group having 1 to 5 carbon atoms or an alkoxycarbonylalkyl group having a total carbon number of 3 to 6; R.sub.2 represents a hydrogen atom, an aryloxy group, an arylmercapto group, an alkyl group having 1 to 5 carbon atoms or hydroxyalkyl group having 1 to 3 carbon atoms or R.sub.1 and R.sub.2 taken together represent an alkylene group having 3 to 5 carbon atoms; R.sub.3 represents a hydrogen atom, an alkyl group having 1 to 5 carbon atoms, a cycloalkyl group having 5 to 7 carbon atoms, a hydroxyalkyl group having 1 to 3 carbon atoms, a benzyl group, a naphthyl group, or a phenyl group which is unsubstituted or substituted with 1 to 3 substituents which are the same or different selected from the group consisting of alkyl groups having 1 to 5 carbon atoms, alkoxy groups having 1 to 5 carbon atoms, hydroxyalkyl groups having 1 to 3 carbon atoms, alkoxycarbonyl groups having total carbon number of 2 to 5, alkylmercapto groups having 1 to 3 carbon atoms, alkylamino groups having 1 to 4 carbon atoms, dialkylamino groups having total carbon number of 2 to 8, halogen atoms, trifluoromethyl group, carboxyl group, cyano group, hydroxyl group, nitro group, amino group and acetamide group, or a pharmaceutically acceptable salt thereof as an active ingredient. The agent of the present invention is useful as a prophylactic and therapeutic agent for circulatory disorders, particularly as an inhibitor against lipid peroxidation and/or an agent for normalizing cerebral dysfunctions.

    摘要翻译： 一种循环系统疾病的预防和治疗剂，其包含下式的吡唑啉酮衍生物：其中R 1表示氢原子，芳基，具有1至5个碳原子的烷基或具有总碳数的烷氧基羰基烷基 3至6; R 2表示氢原子，芳氧基，芳基巯基，碳原子数1〜5的烷基或碳原子数1〜3的羟烷基，或者R 1和R 2一起表示碳原子数3〜5的亚烷基。 R3表示氢原子，碳原子数1〜5的烷基，碳原子数5〜7的环烷基，碳原子数1〜3的羟烷基，苄基，萘基或苯基， 未取代或被1〜3个选自碳原子数1〜5的烷基，碳原子数为1〜5的烷氧基，碳原子数1〜3的烷氧基，碳原子数1〜3的烷氧基，烷氧基羰基， 总碳数为2至5，具有1至3个碳原子的烷基巯基，具有1至4个碳原子的烷基氨基，总碳数为2至8的二烷基氨基，卤素原子，三氟甲基，羧基，氰基，羟基 基团，硝基，氨基和乙酰胺基，或其药学上可接受的盐作为活性成分。 本发明的药剂可用作循环障碍的预防和治疗剂，特别是作为抗脂质过氧化作用的抑制剂和/或用于使脑功能障碍正常化的药剂。

    Prophylactic and therapeutic composition for circulatory disorders and method of treatment
    2.
    发明授权
    Prophylactic and therapeutic composition for circulatory disorders and method of treatment 失效
    循环障碍的预防和治疗组合物及治疗方法

    公开(公告)号：US4857542A

    公开(公告)日：1989-08-15

    申请号：US122516

    申请日：1987-11-19

    申请人： Hiroyoshi Nishi ,  Toshiaki Watanabe ,  Satoshi Yuki ,  Yasuhiro Morinaka ,  Katsuhiko Iseki ,  Hiroko Sakurai

    发明人： Hiroyoshi Nishi ,  Toshiaki Watanabe ,  Satoshi Yuki ,  Yasuhiro Morinaka ,  Katsuhiko Iseki ,  Hiroko Sakurai

    IPC分类号： C07D231/20 ,  C07D231/22 ,  C07D231/26 ,  C07D231/28 ,  C07D231/56

    CPC分类号： C07D231/56 ,  C07D231/20 ,  C07D231/22 ,  C07D231/26 ,  C07D231/28

    摘要： A prophylactic and therapeutic agent for circulatory disorders, comprising a pyrazolone derivative of the formula: ##STR1## wherein R.sub.1 represents a hydrogen atom, an aryl group, an alkyl group having 1 to 5 carbon atoms or an alkoxycarbonylalkyl group having a total carbon number of 3 to 6; R.sub.2 represents a hydrogen atom, an aryloxy group, an arylmercapto group, an alkyl group having 1 to 5 carbon atoms or hydroxyalkyl group having 1 to 3 carbon atoms; or R.sub.1 and R.sub.2 taken together represent an alkylene group having 3 to 5 carbon atoms; R.sub.3 represents a hydrogen atom, an alkyl group having 1 to 5 carbon atoms, a cycloalkyl group having 5 to 7 carbon atoms, a hydroxyalkyl group having 1 to 3 carbon atoms, a benzyl group, a naphthyl group, or a phenyl group which is unsubstituted or substituted with 1 to 3 substituents which are the same or different selected from the group consisting of alkyl groups having 1 to 5 carbon atoms, alkoxy groups having 1 to 5 carbon atoms, hydroxyalkyl groups having 1 to 3 carbon atoms, alkoxycarbonyl groups having total carbon number of 2 to 5, alkylmercapto groups having 1 to 3 carbon atoms, alkylamino groups having 1 to 4 carbon atoms, dialkylamino groups having total carbon number of 2 to 8, halogen atoms, trifluoromethyl group, carboxyl group, cyano group, hydroxyl group, nitro group, amino group and acetamide group,or a pharmaceutically acceptable salt thereof as an acitve ingredient.The agent of the present invention is useful as a prophylactic and therapeutic agent for circulatory disorders, particularly as an inhibitor agaisnt lipid peroxidation and/or an agent for normalizing cerebral dysfunctions.

    摘要翻译： 一种循环系统疾病的预防和治疗剂，其包含下式的吡唑啉酮衍生物：其中R 1表示氢原子，芳基，具有1至5个碳原子的烷基或具有总碳数的烷氧基羰基烷基 3至6; R2表示氢原子，芳氧基，芳基巯基，碳原子数1〜5的烷基或碳原子数1〜3的羟烷基。 或R 1和R 2一起表示具有3至5个碳原子的亚烷基; R3表示氢原子，碳原子数1〜5的烷基，碳原子数5〜7的环烷基，碳原子数1〜3的羟烷基，苄基，萘基或苯基， 未取代或被1〜3个选自碳原子数1〜5的烷基，碳原子数为1〜5的烷氧基，碳原子数1〜3的烷氧基，碳原子数1〜3的烷氧基，烷氧基羰基， 总碳数为2至5，具有1至3个碳原子的烷基巯基，具有1至4个碳原子的烷基氨基，总碳数为2至8的二烷基氨基，卤素原子，三氟甲基，羧基，氰基，羟基 基团，硝基，氨基和乙酰胺基，或其药学上可接受的盐作为acitve成分。 本发明的药剂可用作循环障碍的预防和治疗剂，特别是作为抑制剂脂质过氧化作用的抑制剂和/或用于使脑功能障碍正常化的药剂。