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141 条记录 (耗时 0.039 秒)

    2-halogen-substituted N-indolylethyl-sulphonamides and inhibiting platelet aggregation and antagonizing thromboxane A.sub.2 therewith
    78.
    发明授权
    2-halogen-substituted N-indolylethyl-sulphonamides and inhibiting platelet aggregation and antagonizing thromboxane A.sub.2 therewith 失效
    2-卤素取代的N-吲哚基乙基磺酰胺，并且抑制血小板聚集并拮抗血栓素A2

    公开(公告)号：US5015657A

    公开(公告)日：1991-05-14

    申请号：US436858

    申请日：1989-11-15

    申请人： Horst Boshagen ,  Elisabeth Perzborn ,  Volker-Bernd Fiedler

    发明人： Horst Boshagen ,  Elisabeth Perzborn ,  Volker-Bernd Fiedler

    IPC分类号： A61K31/40 ,  A61K31/403 ,  A61K31/404 ,  A61P7/02 ,  C07D209/30

    CPC分类号： C07D209/30

    摘要： Inhibiting platelet aggregation and antagonizing thromboxane A.sub.2 with new 2-halogen-substituted N-indolyethyl-sulphonamides of the formula ##STR1## in which R.sup.1 represents hydrogen, halogen, trifluoromethyl, carboxyl or alkoxycarbonyl having up to 8 carbon atoms, orrepresents straight-chain or branched alkyl having up to 8 carbon atoms, or represents cycloalkyl having 3 to 8 carbon atoms, which is optionally substituted by carboxyl, halogen, alkoxy or alkoxycarbonyl having in each case up to 8 carbon atoms, cyano or hydroxyl, orrepresents a group of the formula --S(O).sub.n --R.sup.5,--NR.sup.6 R.sup.7 or --OR.sup.8represents straight-chain or branched alkyl having up to 10 carbon atoms, which is optionally substituted by halogen, phenyl, hydroxyl or cyano, orrepresents aryl having 6 to 10 carbon atoms, which is optionally substituted by up to 5 identical or different substituents from the group comprising halogen, cyano, trifluoromethyl, trifluoromethoxy, trifluoromethylthio, alkyl, alkoxy, alkoxycarbonyl or alkylthio having in each case up to 8 carbon atoms, hydroxyl, carboxyl, phenyl, phenoxy, benzyloxy and benzylthio, or by a group of the formula --NR.sup.6 R.sup.7,R.sup.3 represents halogen,R.sup.4 represents hydrogen or straight-chain or branched alkyl having up to 8 carbon atoms, or represents phenylandm represents one of the numbers 2, 3 or 4, and salts thereof.

    摘要翻译： 抑制血小板聚集和拮抗血栓素A2与新的2-卤素取代的N-取代的N-取代的N-取代的N-取代的N-取代的N-取代的N-取代的N-取代的N-取代的N-取代的N-取代的N-取代的N-取代的N-取代的N-取代的N-取代的N-取代的N-取代的N-取代的N-取代的N- 具有至多8个碳原子的直链或支链烷基，或代表具有3-8个碳原子的环烷基，其任选被羧基，卤素，烷氧基或烷氧基羰基所取代，每种情况下最多具有8个碳原子，氰基或羟基，或 表示式-S（O）n -R 5，-NR 6 R 7或-OR 8表示具有至多10个碳原子的直链或支链烷基，其任选被卤素，苯基，羟基或氰基取代，或表示芳基 具有6至10个碳原子，其任选被至多5个相同或不同的取代基取代，所述取代基包括卤素，氰基，三氟甲基，三氟甲氧基，三氟甲硫基，烷基，烷氧基，烷氧基羰基或 具有至多8个碳原子的烷硫基，羟基，羧基，苯基，苯氧基，苄氧基和苄硫基，或由-NR 6 R 7基团，R 3表示卤素，R 4表示氢或具有直链或支链烷基的直链或支链烷基 8个碳原子，或表示苯基，m表示数2，3或4中的一个，及其盐。

    Cycloalkano(1,2-B) indole-sulponamides
    79.
    发明授权
    Cycloalkano(1,2-B) indole-sulponamides 失效
    环咯烷（1,2-B）吲哚磺胺

    公开(公告)号：US4988820A

    公开(公告)日：1991-01-29

    申请号：US556592

    申请日：1990-07-20

    申请人： Horst Boshagen ,  Ulrich Rosentreter ,  Folker Lieb ,  Hermann Oediger ,  Friedel Seuter ,  Elisabeth Perzborn ,  Volker-Bernd Fiedler

    发明人： Horst Boshagen ,  Ulrich Rosentreter ,  Folker Lieb ,  Hermann Oediger ,  Friedel Seuter ,  Elisabeth Perzborn ,  Volker-Bernd Fiedler

    IPC分类号： C07D209/80 ,  C07D209/86 ,  C07D209/88 ,  C07D491/10

    CPC分类号： C07D209/80 ,  C07D209/86 ,  C07D209/88 ,  C07D491/10

    摘要： Cycloalkano[1,2-b]indole-sulphonamides of the formula ##STR1## in which R.sup.1 represents hydrogen, halogen, trifluoromethyl, carboxyl or alkoxycarbonyl, represents a group of the formula --S(O).sub.m R.sup.3, in which R.sup.3 denotes alkyl or aryl, and m denotes one of the numbers 0, 1 or 2, represents a group of the formula ##STR2## in which R.sup.4 and R.sup.5 are identical or different and represent hydrogen, alkyl, aryl, aralkyl or acetyl, represents a group of the formula --OR.sup.6, in which R.sup.6 denotes hydrogen, alkyl, aryl, aralkyl, alkyl-SO.sub.2 --, aryl--SO.sub.2 --, aralkyl--SO.sub.2 -- or trifluoromethyl, or represents alkyl, alkenyl or cycloalkyl, each of which is optionally substituted by carboxyl, alkoxycarbonyl, halogen, hydroxyl, alkoxy, alkylthio or cyano, R.sup.2 represents aryl which is optionally substituted up to 5 times by halogen, cyano, trifluoromethyl, trifluoromethoxy, trifluoromethylthio, alkyl, carboxyalkyl, alkoxycarbonylalkyl, alkoxy, alkylthio, hydroxyl, carboxyl, alkoxycarbonyl, phenyl, phenoxy, benzyloxy, benzylthio or a group of the formula ##STR3## in which R.sup.4 and R.sup.5 have the abovementioned meaning, x represents the number 1, 2 or 3, and y represents the number 0 or 1, where appropriate in an isomeric form, and their salts are disclosed. These compounds are useful to inhibit platelet aggregation and to antagonize thromboxane A.sub.2.

    摘要翻译： 其中R 1表示氢，卤素，三氟甲基，羧基或烷氧基羰基的式[IMAGE]的环烷基[1,2-b]吲哚磺酰胺代表式-S（O）m R 3的基团，其中R 3表示烷基或 芳基，m表示数字0,1或2中的一个，表示其中R 4和R 5相同或不同并且表示氢，烷基，芳基，芳烷基或乙酰基的式“IMAGE”的基团，表示 其中R 6表示氢，烷基，芳基，芳烷基，烷基-SO 2 - ，芳基-SO 2 - ，芳烷基-SO 2 - 或三氟甲基，或表示烷基，烯基或环烷基，其各自任选被羧基， 氰基，三氟甲基，三氟甲氧基，三氟甲硫基，烷基，羧基烷基，烷氧基羰基烷基，烷氧基，烷硫基，羟基，羧基，烷氧基羰基，烷氧基羰基，烷硫基， 苯基，苯氧基，苄氧基，苄硫基 或其中R 4和R 5具有上述含义的式“IMAGE”的基团，x表示数字1,2或3，并且y代表数字0或1，其中适当的是异构体形式，并且其公开的盐 。 这些化合物可用于抑制血小板聚集和拮抗血栓素A2。