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    Thiazole derivative and leukotriene antagonist containing the same as the effective ingredients
    1.
    发明授权
    Thiazole derivative and leukotriene antagonist containing the same as the effective ingredients 失效
    噻唑衍生物和含有与有效成分相同的白三烯拮抗剂

    公开(公告)号：US4902700A

    公开(公告)日：1990-02-20

    申请号：US279225

    申请日：1988-11-28

    申请人： Yosio Hayasi ,  Tomei Oguri ,  Masaki Shimoda ,  Mikio Tsutsui ,  Kazuo Takahashi ,  Hitoshi Miida

    发明人： Yosio Hayasi ,  Tomei Oguri ,  Masaki Shimoda ,  Mikio Tsutsui ,  Kazuo Takahashi ,  Hitoshi Miida

    IPC分类号： C07D417/12 ,  A61K31/425 ,  A61K31/426 ,  A61K31/428 ,  A61P37/08 ,  A61P43/00 ,  C07D277/20 ,  C07D277/22 ,  C07D277/24 ,  C07D277/28 ,  C07D277/30 ,  C07D277/56 ,  C07D277/64 ,  C07D277/82

    CPC分类号： C07D277/82 ,  C07D277/24 ,  C07D277/28 ,  C07D277/30 ,  C07D277/56 ,  C07D277/64

    摘要： Disclosed are a thiazole derivative represented by the following formula, a pharmaceutically acceptable salt thereof and leukotriene antagonist containing the same as the active ingredients: ##STR1## wherein R.sub.1 and R.sub.2 each independently represent a hydrogen atom, an alkyl group having 1 to 8 carbon atoms, a lower alkoxycarbonyl group or a substituted or unsubstituted phenyl group or cooperatively represent a tetramethylene group corresponding to a fused cyclohexane ring or a butadienylene group which is unsubstituted or substituted with a halogen atom, a lower alkoxy group, a lower alkoxycarbonyl group or an alkyl group having 1 to 3 carbon atoms corresponding to a fused benzene ring; R.sub.3, R.sub.4, R.sub.5 and R.sub.6 each independently represent a hydrogen atom, a hydroxyl group, a lower alkoxy group, an alkyl group having 1 to 3 carbon atoms or a halogen atom; A represents a linking group having 2 to 4 chain members; B represents a linking group having 2 to 5 chain members; and Q represents a carboxyl group, a lower alkoxy group, a hydroxyl group, an alkoxycarbonyl group having 2 to 6 carbon atoms or a 5-tetrazolyl group.

    摘要翻译： 公开了由下式表示的噻唑衍生物，其药学上可接受的盐和含有与活性成分相同的白三烯拮抗剂：其中R 1和R 2各自独立地表示氢原子，具有1至8个碳原子的烷基 低级烷氧基羰基或取代或未取代的苯基，或协同表示对应于未被取代或被卤素原子，低级烷氧基，低级烷氧基羰基或烷基取代的稠环己烷环或丁二烯基的四亚甲基 对应于稠合苯环的具有1至3个碳原子的基团; R 3，R 4，R 5和R 6各自独立地表示氢原子，羟基，低级烷氧基，碳原子数1〜3的烷基或卤素原子。 A表示具有2至4个链成员的连接基团; B表示具有2至5个链成员的连接基团; Q表示羧基，低级烷氧基，羟基，碳原子数2〜6的烷氧基羰基或5-四唑基。

    .gamma.-butyrolactone derivatives, process for preparing the same and immunomodulating compositions containing the same as active ingredients
    3.
    发明授权
    .gamma.-butyrolactone derivatives, process for preparing the same and immunomodulating compositions containing the same as active ingredients 失效
    γ-丁内酯衍生物，其制备方法和含有该活性成分的免疫调节组合物

    公开(公告)号：US4613613A

    公开(公告)日：1986-09-23

    申请号：US647979

    申请日：1984-09-06

    申请人： Tomei Oguri ,  Yasuhiro Morinaka ,  Shuichiro Kadowaki

    发明人： Tomei Oguri ,  Yasuhiro Morinaka ,  Shuichiro Kadowaki

    IPC分类号： A61K31/365 ,  A61P29/00 ,  C07D307/33 ,  C07D307/58 ,  C07D307/94 ,  A61K31/34 ,  C07D307/10 ,  C07D307/26

    CPC分类号： C07D307/33 ,  C07D307/58 ,  C07D307/94

    摘要： A .gamma.-butyrolactone derivative represented by the following formula: ##STR1## wherein R.sup.1 represents a hydrogen atom, a straight or branched alkyl group having 1-8 carbon atoms, a phenyl group; R.sup.2 and R.sup.3 may be the same or different and each represents a hydrogen atom, a straight or branched alkyl group having 1-8 carbon atoms, a cycloalkyl group having 3-10 carbon atoms, a benzyl group, a phenyl group, a phenyl group substituted with a substituent selected from the group consisting of a halogen atom, an alkoxy group, a nitro group, an amino group, an alkyl group having 1-4 carbon atoms, a nitrile group and an alkoxycarbonyl group; R.sup.2 and R.sup.3 may be linked to form an alkylene group having 4-6 carbon atoms; X represents a hydrogen atom, a straight or branched alkyl group having 1-8 carbon atoms, a cycloalkyl group having 3-10 carbon atoms, a benzyl group or a substituent represented by the formula ##STR2## (wherein R.sup.4 represents a straight or branched alkyl group having 1-8 carbon atoms, a cycloalkyl group having 3-10 carbon atoms, a benzyl group, a phenyl group or a phenyl group substituted with a substituent selected from the group consisting of a halogen atom, an alkoxy group, a nitro group, an alkylthio group, a nitrile group, an alkoxycarbonyl group and an alkyl group having 1-4 carbon atoms) or a salt thereof. The invention also provides an immunomodulating composition wherein the aforedescribed compound is the active component.

    摘要翻译： 由下式表示的γ-丁内酯衍生物：其中R1表示氢原子，具有1-8个碳原子的直链或支链烷基，苯基; R2和R3可以相同或不同，各自表示氢原子，具有1-8个碳原子的直链或支链烷基，具有3-10个碳原子的环烷基，苄基，苯基，苯基 被选自卤素原子，烷氧基，硝基，氨基，具有1-4个碳原子的烷基，腈基和烷氧羰基组成的组中的取代基取代; R2和R3可以连接形成具有4-6个碳原子的亚烷基; X表示氢原子，具有1-8个碳原子的直链或支链烷基，具有3-10个碳原子的环烷基，苄基或由式“IMAGE”表示的取代基（其中R4表示直链或支链 具有1-8个碳原子的烷基，具有3-10个碳原子的环烷基，苄基，苯基或被选自卤素原子，烷氧基，硝基的取代基取代的苯基 基团，烷硫基，腈基，烷氧基羰基和具有1-4个碳原子的烷基）或其盐。 本发明还提供一种免疫调节组合物，其中上述化合物是活性成分。