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    Prophylactic and therapeutic composition for circulatory disorders and method of treatment
    2.
    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
    3.
    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。

    4-phenylphthalazine derivatives which inhibit platelet aggregation
    7.
    发明授权
    4-phenylphthalazine derivatives which inhibit platelet aggregation 失效
    抑制板聚集的4-苯基苯胺衍生物

    公开(公告)号：US5089494A

    公开(公告)日：1992-02-18

    申请号：US675259

    申请日：1991-03-27

    申请人： Norimichi Iwase ,  Yasuhiro Morinaka ,  Yoshikuni Tamao ,  Toshiji Kanayama

    发明人： Norimichi Iwase ,  Yasuhiro Morinaka ,  Yoshikuni Tamao ,  Toshiji Kanayama

    IPC分类号： C07D237/34

    CPC分类号： C07D237/34

    摘要： 4-Phenylphthalazine derivatives having platelet aggregation inhibitory activity of the formula: ##STR1## wherein R.sup.1 is an alkyl or hydroxyalkyl group of 1-5 carbon atoms; R.sup.2 is a hydrogen atom or an alkyl group of 1-5 carbon atoms; or R.sup.1 and R.sup.2, when taken together, may represent an alkylene group of 2-6 carbon atoms, said group optionally containing one or more oxygen atoms; R.sup.3 and R.sup.4 are independently a hydrogen or halogen atom, an alkyl or alkoxy group of 1-4 carbon atoms, or when two of R.sup.3 are adjacently positioned, (R.sup.3)l may represent a --O--(CH.sub.2).sub.p --O-- group and/or when two of R.sup.4 are adjacently positioned, (R.sup.4).sub.m may represent a --O--(CH.sub.2).sub.p --O-- group; R.sup.5 is a hydrogen or halogen atom, an alkyl or alkoxy group of 1-4 carbon atoms, a trifluoromethyl group or a hydroxy group, or when two of R.sup.5 are adjacently positioned, (R.sup.5).sub.n may represent a --O--(CH.sub.2).sub.p --O-- group; p is an integer of 1-3; l and m are independently an integer of 1-2; and n is an integer of 1-3, and optical isomers and pharmaceutically acceptable acid addition salts thereof.

    3,6-disubstituted pyradazine derivatives
    8.
    发明授权
    3,6-disubstituted pyradazine derivatives 失效
    3,6-二取代的哒嗪衍生物

    公开(公告)号：US5462941A

    公开(公告)日：1995-10-31

    申请号：US215426

    申请日：1994-03-21

    申请人： Norimichi Iwase ,  Yasuhiro Morinaka ,  Yoshikuni Tamao ,  Toshiji Kanayama ,  Kumi Yamada

    发明人： Norimichi Iwase ,  Yasuhiro Morinaka ,  Yoshikuni Tamao ,  Toshiji Kanayama ,  Kumi Yamada

    IPC分类号： A61K31/50 ,  A61K31/502 ,  A61P7/02 ,  A61P9/00 ,  A61P9/10 ,  C07D237/34 ,  C07D241/44 ,  C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D405/04 ,  C07D405/14 ,  C07D409/04 ,  C07D409/12 ,  C07D409/14 ,  C07D417/04 ,  C07D417/14 ,  C07D491/04 ,  C07D491/048 ,  C07D495/04 ,  C07D521/00 ,  C07D247/02

    CPC分类号： C07D231/12 ,  C07D233/56 ,  C07D237/34 ,  C07D249/08 ,  C07D403/04 ,  C07D405/04 ,  C07D409/04 ,  C07D409/12 ,  C07D409/14 ,  C07D417/04 ,  C07D491/04 ,  C07D495/04

    摘要： A 3,6-disubstituted pyridazine derivative having excellent platelet agglutination inhibitory effects. It is useful for a preventive medicine or a therapeutic medicine for a cerebrovascular disorder such as cerebral thrombosis and cerebral embolism, an ischemic heart disease such as myocardial infarction, and a circulation disorder such as peripheral circulation disorder. A pharmaceutical composition containing a compound of the present invention as an effective ingredient and a process for preparing the same are also disclosed. The compound has the formula (I) ##STR1## wherein A represents an alkyl group having 3 to 6 carbon atoms; a cycloalkyl group having 5 to 7 carbon atoms; a phenyl group, a thienyl group, a furyl group, a thiazolyl group, a phenoxy group, a phenylalkyl group having 7 to 9 carbon atoms, a phenylthio group, a 5-6 membered saturated heterocyclic group containing one or more nitrogen atoms, a pyridyl group or an imidazolyl group each of which may have at least one substituent selected from the group consisting of an alkyl group having 1 to 4 carbon atoms, an alkoxy group having 1 to 4 carbon atoms and a halogen atom; B represents (a) --NH--D wherein D represents ##STR2## (4) --CH.sup.3 R.sup.4 ; or (5) an alkyl group having 3 to 8 carbon atoms; or ##STR3## and the ring C represents a benzene ring.

    摘要翻译： 具有优异的血小板凝集抑制作用的3,6-二取代哒嗪衍生物。 对脑血栓形成和脑栓塞，心肌梗死等缺血性心脏病，周围循环障碍等循环障碍的脑血管障碍的预防药或治疗药有用。 还公开了含有本发明化合物作为有效成分的药物组合物及其制备方法。 该化合物具有式（I）其中A表示具有3至6个碳原子的烷基; 具有5至7个碳原子的环烷基; 苯基，噻吩基，呋喃基，噻唑基，苯氧基，具有7〜9个碳原子的苯基烷基，苯硫基，含有一个或多个氮原子的5-6元饱和杂环基， 吡啶基或咪唑基，其各自可具有至少一个选自具有1至4个碳原子的烷基，具有1至4个碳原子的烷氧基和卤素原子的取代基; （A）-NH-D其中D表示（1）图像（2）图像（3）（4）-CH 3 R 4; 或（5）碳原子数为3〜8的烷基; 或（B），环C表示苯环。

    Sialic acid derivatives
    10.
    发明授权
    Sialic acid derivatives 失效
    唾液酸衍生物

    公开(公告)号：US5783564A

    公开(公告)日：1998-07-21

    申请号：US669219

    申请日：1996-06-24

    申请人： Haruyuki Chaki ,  Naoko Ando ,  Yasuhiro Morinaka ,  Ken-ichi Saito ,  Tomoko Yugami ,  Rie Yoshida

    发明人： Haruyuki Chaki ,  Naoko Ando ,  Yasuhiro Morinaka ,  Ken-ichi Saito ,  Tomoko Yugami ,  Rie Yoshida

    IPC分类号： C07J17/00 ,  C07J41/00 ,  A61K31/70 ,  A61K31/58

    CPC分类号： C07J41/0005 ,  C07J17/005

    摘要： Sialic acid derivatives represented by the general formula (I): wherein R.sup.1 is a steroidal compound residue; R.sup.2 is H or alkyl; R.sup.3 is alkyl; ##STR1## wherein each of R.sup.6 and R.sup.7 is H, alkyl or the like and I is an integer of 0 to 6; or the like; X is O or S; R.sup.4 is H or acyl; and R.sup.5 is R.sup.14 O--(R.sup.14 is H or acyl) or R.sup.15 NH--(R.sup.15 is acyl or the like); their salts, hydrates or solvates are provided. Sialic acid derivatives of the present invention are expected to be effective medicines for the prevention and therapy of senile dementia including Alzheimer's disease and the like, because they increase ChAT activity in cholinergic neurons.

    摘要翻译： 由通式（I）表示的唾液酸衍生物：其中R1是甾族化合物残基; R2是H或烷基; R3是烷基; 其中R6和R7各自为H，烷基等，I为0-6的整数; 或类似物; X是O或S; R4是H或酰基; R5为R14O-（R14为H或酰基）或R15NH-（R15为酰基等）; 提供它们的盐，水合物或溶剂合物。 预期本发明的唾液酸衍生物是预防和治疗老年性痴呆（包括阿尔茨海默氏病等）的有效药物，因为它们增加胆碱能神经元中的ChAT活性。