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    New benzimidazoline-2-oxo-1-carboxylic acid derivatives useful as 5-ht receptor antagonists
    3.
    发明公开
    New benzimidazoline-2-oxo-1-carboxylic acid derivatives useful as 5-ht receptor antagonists 失效
    作为5-HT受体拮抗剂有用的新的苯并咪唑-2-氧代-1-羧酸衍生物

    公开(公告)号：EP0309423A3

    公开(公告)日：1989-11-29

    申请号：EP88830375.7

    申请日：1988-09-19

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

    发明人： Turconi, Marco ,  Donetti, Arturo ,  Micheletti, Rosamaria ,  Uberti, Annamaria ,  Nicola, Massimo ,  Giachetti, Antonio ,  Montagna, Ernesto

    IPC分类号： C07D451/12 ,  C07D453/02 ,  C07D401/12 ,  C07D451/14 ,  C07D403/12 ,  C07D453/06 ,  C07D451/04 ,  A61K31/46 ,  A61K31/445 ,  A61K31/435

    CPC分类号： C07D401/12 ,  C07D451/12 ,  C07D451/14 ,  C07D453/02 ,  C07D453/06 ,  C07D487/08

    摘要： New pharmacologically active benzimidazoline-2-oxo-1-carboxylic acid derivatives which are 5-HT receptor antagonists useful as antiemetic agents and as gastric prokinetic agents of the following formula:
    wherein R represents a hydrogen atom, C₁₋₆ alkyl, C₁₋₆ alkenyl or C₁₋₆ alkynil; 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 alkoxycarbonyl, 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, C₁₋₆alkylsulphinyl, C₁₋₆ alkylsulphonyl, amino sulphonyl optionally C₁₋₄ alkyl N-mono or di-substituted, C₁₋₄ alkyl N-mono or di-substituted aminosulphonylamino, aminosulphonylamino; Y is oxygen or is N - R₃ in which R₃ is a hydrogen, a C₁₋₆ alkyl or optionally substituted by one or more C₁₋₆ alkoxy benzyl; A is a group selected from: wherein p is 0, 1; r is 0, 1, 2, 3; R₄ is hydrogen atom or a C₁₋₄ alkyl; R₅ is a hydrogen atom, C₁₋₆ alkyl, C₃₋₈ cycloalkyl, C₃₋₈ cycloalkyl C₁₋₄ alkyl,substituted phenyl C₁₋₄ alkyl or R₅ is a group of formula
    wherein R₆ is hydrogen atom, C₁₋₄ alkyl or an amino group and R₇ is hydrogen atom or C₁₋₆ alkyl, tautomers thereof and acid addition salts of the aforesaid compounds. The processes for the preparation of the compounds of formula (I) as well as pharmaceutical compositions containing them are also described.

    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。

    Benzofused-N-containing heterocycle derivatives
    8.
    发明公开
    Benzofused-N-containing heterocycle derivatives 失效
    Benzo-annellierte-N-enthaltende杂环衍生物。

    公开(公告)号：EP0382687A2

    公开(公告)日：1990-08-16

    申请号：EP90830040.3

    申请日：1990-02-05

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

    发明人： Micheletti, Rosamaria ,  Doods, Henri Nico ,  Turconi, Marco ,  Sagrada, Angelo ,  Donetti, Arturo ,  Schiavi, Battista Giovanni

    IPC分类号： C07D215/54 ,  A61K31/47 ,  C07D451/12 ,  C07D401/12 ,  C07D453/06 ,  C07D487/04 ,  C07D453/02 ,  C07D403/12 ,  C07D401/06 ,  A61K31/435 ,  A61K31/46 ,  A61K31/40

    CPC分类号： C07D451/04 ,  C07D215/54 ,  C07D401/06 ,  C07D401/12 ,  C07D403/12 ,  C07D451/12 ,  C07D451/14 ,  C07D453/02 ,  C07D471/08 ,  C07D487/08

    摘要： Pharmacologically active benzofused-N-containing heterocycle derivatives are described as muscarinic receptor blocking agents useful for the treatment of gastrointestinal and respiratory tract disorders of the following formula:
    wherein
    R represents H or C₁₋₆ alkyl;
    R₁ and R₂ represent H, halogen, C₁₋₆ alkyl, C₁₋₆ alkoxy, C₁₋₆ alkylthio, C₁₋₆ alkoxycarbonyl, carboxyl, hydroxy, nitro, cyano, optionally C₁₋₄ alkyl mono- or disubstituted carbamoyl, optionally C₁₋₄ alkyl mono- or disubstituted amino, C₁₋₆ acylamino, C₁₋₄ alkoxy carbonylamino, C₁₋₆ alkylsulphynyl, C₁₋₆ alkylsulphonyl, C₁₋₆ acyl;
    R₃ represents H, C₁₋₆ alkyl, aryl, aralkyl or it may be absent;
    A represents CO, C = S, S -> O or
    B represents nitrogen when R₃ is absent and the B-D bond is single, or it is carbon;
    D represents CO, CH₂-CH₂,
    when the B-D bond is single, or D is C-R when the D-B bond is double, in which R₄ represents H, C₁₋₆ alkyl, aryl, aralkyl, hydroxy, C₁₋₄ alkoxy and R₅ represents H;
    X represents oxygen, N-R or it is absent;
    Y represents a basic group selected from:
    in which n is 2 or 3; p is 0 or 1 at the same time or not; q is 0, 2 or 3; R₆ and R₇ may be at the same time or not H, C₁₋₄ alkyl, aralkyl or, when R₇ is H or C₁₋₄ alkyl, R₆ may be
    in which R₈ represents H, C₁₋₄ alkyl or amino.
    The processes for the preparation of the compounds of formula (I) as well as pharmaceutical compositions containing them are also described.

    摘要翻译： 描述了药理学活性苯并稠合的含N的杂环衍生物作为可用于治疗胃肠道和呼吸道疾病的毒蕈碱受体阻断剂，其结构如下：其中R代表H或C 1-6烷基; R 1和R 2表示H，卤素，C 1-6烷基，C 1-6烷氧基，C 1-6烷硫基，C 1-6烷氧基羰基，羧基，羟基，硝基，氰基，任选C 1-4烷基单或二取代的氨基甲酰基， 4个烷基单取代或二取代的氨基，C 1-6酰氨基，C 1-4烷氧羰基氨基，C 1-6烷基亚磺酰基，C 1-6烷基磺酰基，C 1-6酰基; R 3表示H，C 1-6烷基，芳基，芳烷基或可不存在; A表示CO，C = S，S - > O或 B表示当R3不存在且B-D键单独或氮时的氮; 当BD键为单时，D表示CO，CH2-CH2，，当DB键为双键时，D表示CR，其中R4表示H，C1-6烷基，芳基，芳烷基，羟基，C1-4烷氧基 R5表示H; X表示氧，N-R或不存在; Y表示选自以下的基团：，其中n为2或3; p同时为0或1; q为0,2或3; R 6和R 7可以同时是H，C 1-4烷基，芳烷基，或者当R 7是H或C 1-4烷基时，R 6可以是其中R 8表示H，C 1-4烷基或氨基的CHEM。 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。