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29 条记录 (耗时 0.028 秒)

    New amidino and guanidino derivatives
    5.
    发明公开
    New amidino and guanidino derivatives 失效
    脒基和胍基衍生物。

    公开(公告)号：EP0351385A2

    公开(公告)日：1990-01-17

    申请号：EP89830325.0

    申请日：1989-07-12

    申请人： BOEHRINGER INGELHEIM ITALIA S.p.A.

    发明人： Donetti, Arturo ,  Turconi, Marco ,  Nicola, Massimo ,  Micheletti, Rosamaria

    IPC分类号： C07D211/46 ,  C07D451/06 ,  C07D451/04 ,  C07D401/12 ,  C07C281/16 ,  A61K31/16 ,  A61K31/325 ,  C07C261/04 ,  A61K31/275 ,  C07C257/12 ,  A61K31/46

    CPC分类号： C07D451/04 ,  C07C257/12 ,  C07C261/04 ,  C07C279/36 ,  C07D211/46 ,  C07D401/12 ,  C07D451/06 ,  C07D451/12 ,  C07D451/14

    摘要： New pharmacologically active amidino and guanidino derivatives which are 5-HT 3 receptor antagonists useful as antiemetic, gastric prokinetic and antimigrainic agents of the following general formula (I)
    wherein

    A is a group selected from substituted benzene
    wherein R 2 is H, C 1-6 alkyl, C 1-6 alkoxy optionally substituted by halogen, hydroxy, acetyl, or R 2 is C 1-6 alkeniloxy, C 1-6 alkyniloxy, halogen, amino, C 1-6 alkylamino, nitro, sulphonylamino
    n is 0-4 mono- or bicyclic heterocycle selected from


    wherein R 3 is H, halogen, C 1-6 alkoxy R 4 is H, C 1-6 alkyl
    X represents -O- or -NH-B is a group selected from


    wherein m is 1, 2
    p is 0, 1, 2
    q is 0,1,2, 3
    R 5 is H, C 1-6 alkyl
    R represents H, C 1-6 alkyl optionally substituted by halogen, NR 6 R 7 in which R 6 is H, C 1-6 alkyl, N0 2 , CN and R 7 is H, C 1-6 alkyl;
    R 1 represents H, C 1-6 alkyl optionally substituted by halogen, CN, tautomers thereof, optical isomers thereof and acid addition salts thereof.

    The processes for the preparation of the compounds of general formula (I) as well as pharmaceutical compositions containing them are also described.

    摘要翻译： 新的药理学活性的脒基和胍基衍生物，其是用作以下通式（I）的止吐，胃促动力和抗偏头痛剂的5-HT 3受体拮抗剂A-CO-X-B-1 = N-R1（I）其中A为 选自取代苯的基团，其中R2是H，C1-6烷基，任选被卤素取代的C1-6烷氧基，羟基，乙酰基或R2是C1-6链烯氧基，C1-6烷氧基，卤素，氨基，C1 -6-烷基氨基，硝基，磺酰基氨基n为0-4个选自的单环或双环杂环，其中R 3为H，卤素，C 1-6烷氧基R 4为H，C 1-6烷基X为-O-或-NH- 是选自的基团，其中m是1,2，p是0,1,2 q是0,1,2,3，R5是H，C1-6烷基，R表示H，任选被卤素取代的C1-6烷基 NR 6 R 7，其中R 6为H，C 1-6烷基，NO 2，CN和R 7为H，C 1-6烷基; R 1表示H，任选被卤素取代的C 1-6烷基，CN，其互变异构体，其旋光异构体及其酸加成盐。 还描述了制备通式（I）化合物的方法以及含有它们的药物组合物。

    Benzimidazolone derivatives as 5-HT1A and 5-HT2 antagonists
    9.
    发明公开
    Benzimidazolone derivatives as 5-HT1A and 5-HT2 antagonists 无效
    Benzimidazolonderivate als 5-HT1A和5-HT2拮抗剂。

    公开(公告)号：EP0526434A1

    公开(公告)日：1993-02-03

    申请号：EP92830427.8

    申请日：1992-07-30

    申请人： BOEHRINGER INGELHEIM ITALIA S.p.A.

    发明人： Turconi, Marco ,  Bietti, Giuseppe ,  Giraldo, Ettore ,  Borsini, Franco ,  Bignotti, Maura

    IPC分类号： C07D235/26 ,  A61K31/415 ,  C07D403/12 ,  C07D405/12 ,  A61K31/505

    CPC分类号： C07D403/06 ,  C07D235/26 ,  C07D403/12 ,  C07D405/12

    摘要： Pharmacologically active benzimidazolone derivatives as 5-HT 1A and 5-HT₂ receptors, useful in the treatment of CNS disorders of formula:

    wherein
    R₁ and R₂ may be at the same time or not a hydrogen atom, halogen, trifluoromethyl, C₁₋₆ alkyl, C₁₋₆ alkoxy, C₁₋₆ alkylthio, C₁₋₆ acyl, carboxyl, C₁₋₆ alkoxy- carbonyl, hydroxy, nitro, amino optionally C₁₋₄ alkyl N-mono or di-substituted, C₁₋₆ acylamino, C₁₋₆ alkoxycarbonylamino, carbamoyl optionally C₁₋₄ alkyl N-mono or di-substituted, cyano, C₁₋₆ alkylsulphinyl, C₁₋₆ alkylsulphonyl, amino sulphonyl optionally C₁₋₄ alkyl N-mono or di-substituted, C₁₋₄ alkyl N-mono or di-substituted aminosulphonylamino, aminosulphonylamino;
       R₃ is hydrogen, C₁₋₆ alkyl, C₂₋₆ alkenyl or C₂-C₆ alkynyl;
       A is -CO- or -CONH- or it is absent;
       B is a straight or branched, saturated or unsaturated C₂₋₆ alkyl;
       m and n are both independently an integer from 1 to 3;
       R₄ is an aryl, aralkyl, a heteroaryl or heteroaralkyl group, each group being optionally substituted by one or more substituents selected from halogen, trifluoromethyl, cyano, C₁₋₃ alkoxy, C₁₋₄ alkyland acid addition salts thereof.
       The process for the preparation of the compounds of formula I as well as pharmaceutical compositions containing them are also described.

    摘要翻译： 药理学活性的苯并咪唑酮衍生物作为5-HT1A和5-HT2受体，可用于治疗下式的CNS病症：其中R 1和R 2可以同时或不同时为氢原子，卤素，三氟甲基，C 1-6 烷基，C 1-6烷氧基，C 1-6烷硫基，C 1-6酰基，羧基，C 1-6烷氧羰基，羟基，硝基，氨基任选C 1-4烷基N-单或二取代，C 1-6酰氨基，C 1 -6烷氧基羰基氨基，氨基甲酰基任选C 1-4烷基N-单或二取代，氰基，C 1-6烷基亚磺酰基，C 1-6烷基磺酰基，氨基磺酰基任选C 1-4烷基N-单或二取代的C 1-4烷基N 单 - 或二 - 取代氨基磺酰基氨基，氨基磺酰基氨基; R3是氢，C1-6烷基，C2-6烯基或C2-C6炔基; A是-CO-或-CONH-或不存在; B是直链或支链，饱和或不饱和的C 2-6烷基; m和n分别为1〜3的整数; R4是芳基，芳烷基，杂芳基或杂芳烷基，每个基团任选地被一个或多个选自卤素，三氟甲基，氰基，C 1-3烷氧基，C 1-4烷基及其酸加成盐的取代基取代。 还描述了制备式I化合物的方法以及含有它们的药物组合物。