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    Pyrazolone Compounds Useful for Treatment of Cerebrovascular Disorders Associated with Ischemic Stroke
    1.
    发明申请
    Pyrazolone Compounds Useful for Treatment of Cerebrovascular Disorders Associated with Ischemic Stroke 有权
    吡唑啉酮化合物可用于治疗与缺血性中风相关的脑血管疾病

    公开(公告)号：US20070249700A1

    公开(公告)日：2007-10-25

    申请号：US11659799

    申请日：2005-08-10

    申请人： Satoshi Yuki ,  Takuma Nakano ,  Hiroko Suzuki

    发明人： Satoshi Yuki ,  Takuma Nakano ,  Hiroko Suzuki

    IPC分类号： A61K31/415 ,  A61P9/10

    CPC分类号： A61K31/4152 ,  A61K2039/545

    摘要： A drug for the treatment of cerebrovascular disorders associated with insufficient cerebral circulation such as ischemic stroke, which comprises a pharmaceutically effective amount of a pyrazolone compound of structural or a pharmaceutically acceptable salt thereof, or a pseudo-polymorphic form thereof, administered at a controlled dose so that the plasma concentration of unchanged form is kept constant for a predetermined period of time and so that the compound may exhibit a higher effect.

    摘要翻译： 一种用于治疗与脑缺血性脑血管疾病相关的脑血管障碍的药物，例如缺血性卒中，其包含药物有效量的结构或其药学上可接受的盐或其假多晶型形式的吡唑啉酮化合物，其以受控剂量 使得不变形式的血浆浓度在预定时间段内保持恒定，使得化合物可以表现出更高的效果。

    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。

    Remedy and preventive for nervous system disorders
    3.
    发明授权
    Remedy and preventive for nervous system disorders 失效
    补救和预防神经系统疾病

    公开(公告)号：US5952337A

    公开(公告)日：1999-09-14

    申请号：US809544

    申请日：1997-05-07

    申请人： Ken-Ichi Saito ,  Tomoko Bessho ,  Satoshi Yuki ,  Haruyuki Chaki ,  Mitsuo Egawa

    发明人： Ken-Ichi Saito ,  Tomoko Bessho ,  Satoshi Yuki ,  Haruyuki Chaki ,  Mitsuo Egawa

    IPC分类号： A61K31/00 ,  A61K31/4741 ,  A61P9/10 ,  A61P25/28 ,  C07D491/04 ,  C07D491/048 ,  A61K31/44

    CPC分类号： C07D491/04 ,  A61K31/00 ,  A61K31/4741

    摘要： An agent comprising a 4-aminoacyltetrahydrofuro�2,3-b!quinoline derivative represented by formula (I): ##STR1## (wherein R.sup.1 represents an alkyl group having 2 to 6 carbon atoms, etc.) or an acid addition salt or a hydrate or a solvent of them as an active ingredient. The compound has a protecting action against neuronal cell death and is useful as a therapeutic or prophylactic agent for cerebrovascular diseases, traumatic head injuries or postencephalitis.

    摘要翻译： PCT No.PCT / JP95 / 01861 Sec。 371日期1997年5月7日 102（e）日期1997年5月7日PCT提交1995年9月19日PCT公布。 第WO96 / 09058号公报 日期：1996年3月28日包含由式（I）表示的4-氨基酰基四氢呋喃并[2,3-b]喹啉衍生物：其中R1表示碳原子数2〜6的烷基等）或酸加成盐 或它们的水合物或溶剂作为活性成分。 该化合物具有对神经元细胞死亡的保护作用，可用作脑血管疾病，创伤性头部损伤或脑后脑炎的治疗或预防剂。

    Prophylactic and therapeutic composition for circulatory disorders and method of treatment
    4.
    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。

    Pyrazolone compounds useful for treatment of cerebrovascular disorders associated with ischemic stroke
    10.
    发明授权
    Pyrazolone compounds useful for treatment of cerebrovascular disorders associated with ischemic stroke 有权
    吡唑啉酮化合物可用于治疗与缺血性卒中相关的脑血管疾病

    公开(公告)号：US09259416B2

    公开(公告)日：2016-02-16

    申请号：US11659799

    申请日：2005-08-10

    申请人： Satoshi Yuki ,  Takuma Nakano ,  Hiroko Suzuki

    发明人： Satoshi Yuki ,  Takuma Nakano ,  Hiroko Suzuki

    IPC分类号： A61K31/4152 ,  A61K39/00

    CPC分类号： A61K31/4152 ,  A61K2039/545

    摘要： A drug for the treatment of cerebrovascular disorders associated with insufficient cerebral circulation such as ischemic stroke, which comprises a pharmaceutically effective amount of a pyrazolone compound of structural Formula (I): or a pharmaceutically acceptable salt thereof, or a pseudo-polymorphic form thereof, administered at a controlled dose so that the plasma concentration of unchanged form is kept constant for a predetermined period of time and so that the compound may exhibit a higher effect.

    摘要翻译： 一种用于治疗与缺血性脑卒中相关的脑血管疾病不足的药物，其包含药学有效量的结构式（I）的吡唑啉酮化合物或其药学上可接受的盐或其假多晶型物， 以可控剂量施用，使得不变形式的血浆浓度在预定时间段内保持恒定，并且使得化合物可以表现出更高的效果。