Benzenesulfonamide derivatives and use thereof
    1.
    发明授权
    Benzenesulfonamide derivatives and use thereof 失效
    苯磺酰胺衍生物及其用途

    公开(公告)号:US5597848A

    公开(公告)日:1997-01-28

    申请号:US397068

    申请日:1995-03-16

    CPC分类号: C07C311/29 C07C311/19

    摘要: A benzenesulfonamide derivative represented by the following general formula: ##STR1## wherein R.sup.1 represents a hydrogen atom, a lower alkyl group, a lower alkoxy group or a halogen atom; R.sup.2 represents a C.sub.1 -C.sub.10 straight- or branched-chain alkyl group, a C.sub.3 -C.sub.8 cycloalkyl group which may be substituted with one or more C.sub.1 -C.sub.6 alkyl groups on its ring, a C.sub.1 -C.sub.6 alkyl group substituted with one or more C.sub.3 -C.sub.8 cycloalkyl groups, 1-adamantylmethyl group, 2-norbornylmethyl group, or a C.sub.1 -C.sub.6 alkyl group substituted with one or more phenyl groups whose benzene ring may have one or more substituents; R.sup.3 represents a hydrogen atom or a lower alkyl group; and n is an integer of from 2 to 4, and a pharmacologically acceptable salt thereof. The present compounds have thromboxane A.sub.2 antagonistic activity, leucotriene antagonistic activity and the like and useful as a platelet aggregation inhibitor, antithrombotic agent, antiasthmatic agent and antiallergic agent.

    摘要翻译: PCT No.PCT / JP93 / 01382 Sec。 371日期1995年3月16日 102(e)1995年3月16日PCT PCT 1993年9月29日PCT公布。 公开号WO94 / 07848 日本1994年4月14日由以下通式表示的苯磺酰胺衍生物:其中R 1表示氢原子,低级烷基,低级烷氧基或卤素原子; R2表示C1-C10直链或支链烷基,可以在其环上被一个或多个C 1 -C 6烷基取代的C 3 -C 8环烷基,被一个或多个C 3取代的C 1 -C 6烷基 -C8环烷基,1-金刚烷基甲基,2-降冰片基甲基或被苯环可以具有一个或多个取代基的一个或多个苯基取代的C 1 -C 6烷基; R3表示氢原子或低级烷基; n为2〜4的整数,及其药理学上可接受的盐。 本发明化合物具有血栓素A2拮抗活性,白三烯拮抗活性等,可用作血小板聚集抑制剂,抗血栓形成剂,止喘剂和抗过敏剂。

    Piperidine derivative, method for preparation thereof, and a
pharmaceutical composition comprising the same
    7.
    发明授权
    Piperidine derivative, method for preparation thereof, and a pharmaceutical composition comprising the same 失效
    哌啶衍生物,其制备方法和包含其的药物组合物

    公开(公告)号:US5153207A

    公开(公告)日:1992-10-06

    申请号:US520064

    申请日:1990-05-03

    IPC分类号: C07D211/46 C07D211/54

    CPC分类号: C07D211/54 C07D211/46

    摘要: A piperidine derivative represented by the following general formula (I): ##STR1## wherein R.sub.1 and R.sub.2 are the same or different and each independently represents a hydrogen atom, a halogen atom, a lower alkyl group, or a lower alkoxy group; R.sub.3 represents a hydrogen atom or a lower alkyl group; X represents an oxygen atom or a sulfur atom; Y represents an alkylene group having 1 to 7 carbon atoms which may be optionally substituted with a lower alkyl group, or Y represents an --A--O--B-- group wherein A and B are the same or different and each independently represents an alkylene group having 1 to 3 carbon atoms which may be optionally substituted with a lower alkyl group is disclosed. Also disclosed are a pharmacologically acceptable salt of a compound of formula (I), an antihistaminic and antiallergic agent comprising a compound of formula (I), a pharmaceutical composition comprising a compound of formula (I), and a method for the treatment of an allergic disease by administering a compound of formula (I).

    Piperidine derivatives and pharmaceutical compositions comprising the
same
    8.
    发明授权
    Piperidine derivatives and pharmaceutical compositions comprising the same 失效
    哌啶衍生物和包含其的药物组合物

    公开(公告)号:US5095022A

    公开(公告)日:1992-03-10

    申请号:US538085

    申请日:1990-06-13

    IPC分类号: C07D211/70 C07D405/04

    CPC分类号: C07D405/04 C07D211/70

    摘要: A piperidine derivative represented by the following general formula (I): ##STR1## wherein R represents a hydrogen atom or a lower alkyl group; X represents --CH.dbd.CH--, --CH.sub.2 CH.sub.2 --, or --CH.sub.2 O--; Y represents an alkylene group having 1 to 5 carbon atoms which may be optionally substituted with a lower alkyl group, or Y represents an --A--O--B-- group wherein A and B are the same or different and each independently represented an alkylene group having 1 to 3 carbon atoms which may be optionally substituted with a lower alkyl group is disclosed. Also disclosed are a pharmacologically acceptable salt of a compound of formula (I), a method for preparation of a compound of formula (I), an antihistaminic and antiallergic agent comprising a compound of formula (I), a pharmaceutical composition comprising a compound of formula (I), and a method for the treatment of an allergic disease by administering a compound of formula (I).

    Pyrazine-2-carboxamide derivatives useful in treating allergic disease
    9.
    发明授权
    Pyrazine-2-carboxamide derivatives useful in treating allergic disease 失效
    吡嗪-2-甲酰胺衍生物,用于治疗过敏性疾病

    公开(公告)号:US4792547A

    公开(公告)日:1988-12-20

    申请号:US941918

    申请日:1986-12-15

    摘要: Novel pyrazine derivatives useful for treatment of bronchial asthma, allergic gastorenteric trouble, hay fever urticaria, allertic rhinitis, and allergic conjunctivitis, and pharmaceutical compositions thereof, are disclosed. The compounds have the formula I as follows: ##STR1## wherein R represents hydrogen or ##STR2## wherein R.sub.1 and R.sub.2 may be the same or different and each independently represents hydrogen, straight or branched-chain lower-alkyl, or cycloalkyl having three to six carbon atoms inclusive, phenyl which may be substituted with halogen, lower-alkyl, or lower-alkoxy, or wherein R.sub.1 and R.sub.2 together represent alkylene of four to six carbon atoms, inclusive, optionally interrupted by one or two nitrogen atoms or one oxygen atom and said ring being optionally substituted by straight or branched-chain lower-alkyl having one to six carbon atoms inclusive, hydroxy, or phenyl,and pharmaceutically-acceptable salts thereof.

    摘要翻译: 用于治疗支气管哮喘,过敏性胃炎,花粉荨麻疹,过敏性鼻炎和过敏性结膜炎的新颖吡嗪衍生物及其药物组合物。 化合物具有如下式I:其中R表示氢或者其中R 1和R 2可以相同或不同,并且各自独立地表示氢,直链或支链低级烷基或具有三个至 6个碳原子,可被卤素,低级烷基或低级烷氧基取代的苯基,或其中R 1和R 2一起代表四至六个碳原子的亚烷基,包括任选地被一个或两个氮原子或一个氧 所述环任选被具有1-6个碳原子的直链或支链低级烷基,羟基或苯基取代,及其药学上可接受的盐。