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    Tricyclic aminoalkyl derivatives
    4.
    发明授权
    Tricyclic aminoalkyl derivatives 失效
    三环氨基烷基衍生物

    公开(公告)号：US4070373A

    公开(公告)日：1978-01-24

    申请号：US291426

    申请日：1972-09-22

    申请人： Werner Winter ,  Max Thiel ,  Kurt Stach, deceased ,  by Werner Plattner, administrator ,  Wolfgang Schaumann ,  Karl Dietmann

    发明人： Werner Winter ,  Max Thiel ,  Kurt Stach, deceased ,  by Werner Plattner, administrator ,  Wolfgang Schaumann ,  Karl Dietmann

    IPC分类号： C07D311/90 ,  C07D313/12 ,  C07D337/12 ,  C07D337/16

    CPC分类号： C07D337/16 ,  C07D311/90 ,  C07D313/12 ,  C07D337/12 ,  C07C2103/18

    摘要： Novel tricyclic aminoalkyl derivatives are disclosed which are characterized by valuable pharmacological activities and namely by cardiac and circulatory activities. The tricyclic aminoalkyl derivatives are compounds of the formula: ##STR1## wherein X is an oxygen or a sulfur atom, a saturated or unsaturated, straight chain or branched alkylene group containing up to 3 carbon atoms, an oxymethylene, thiamethylene or thiaethylene group or a valency bond, R.sub.1 is hydrogen, halogen, alkyl, alkoxy or trifluoromethyl, R.sub.2 is hydrogen or hydroxyl, R.sub.3 is hydrogen or together with R.sub.2 represents a further valency bond, R.sub.4 and R.sub.5 which may be the same or different are each hydrogen or lower alkyl, A is alkylene which is substituted by an optionally acylated hydroxyl group, Y is an oxygen or sulfur atom or an optionally alkylated imino group and Z is aryl, aralkyl, cycloalkyl or cycloalkyl-alkyl which may be substituted by halogen, hydroxyl, nitro, amino, alkoxy, aralkoxy, alkyl, trifluoromethyl, alkylamino or alkylsulfonyl group, and the acid addition salts thereof with pharmacologically acceptable acids.

    摘要翻译： 公开了新颖的三环氨基烷基衍生物，其特征在于有价值的药理活性，即通过心脏和循环活性。 三环氨基烷基衍生物是下式的化合物：其中X是氧或硫原子，含有至多3个碳原子的饱和或不饱和的直链或支链亚烷基，亚甲基，亚亚甲基或亚硫代亚乙基或 化合键，R 1是氢，卤素，烷基，烷氧基或三氟甲基，R 2是氢或羟基，R 3是氢或与R 2一起代表另外的价键，可以相同或不同的R 4和R 5各自是氢或低级烷基 A是被任意酰化的羟基取代的亚烷基，Y是氧或硫原子或任选烷基化的亚氨基，Z是可以被卤素，羟基，硝基取代的芳基，芳烷基，环烷基或环烷基 - 烷基， 氨基，烷氧基，芳烷氧基，烷基，三氟甲基，烷基氨基或烷基磺酰基，及其与药理学上可接受的酸的酸加成盐。

    Indolin-2-one derivatives preparation thereof and intermediates for the preparation thereof
    6.
    发明授权
    Indolin-2-one derivatives preparation thereof and intermediates for the preparation thereof 失效

    公开(公告)号：US4642309A

    公开(公告)日：1987-02-10

    申请号：US780704

    申请日：1985-09-26

    申请人： Helmut Michel ,  Klaus Marzenell ,  Wolfgang Kampe ,  Wolfgang Bartsch ,  Wolfgang Schaumann

    发明人： Helmut Michel ,  Klaus Marzenell ,  Wolfgang Kampe ,  Wolfgang Bartsch ,  Wolfgang Schaumann

    IPC分类号： A61K31/40 ,  A61K31/403 ,  A61K31/404 ,  A61P9/00 ,  A61P9/08 ,  A61P25/02 ,  C07D209/34 ,  C07D401/06 ,  C07D403/06 ,  C07D405/12 ,  C07D405/14 ,  C07D409/06

    CPC分类号： C07D401/06 ,  C07D209/34 ,  C07D403/06 ,  C07D405/12 ,  C07D405/14 ,  C07D409/06

    摘要： The present invention provides indolin-2-one derivatives of the general formula: ##STR1## wherein R.sub.1 is a C.sub.1 -C.sub.6 alkyl radical or a radical of the general formula: ##STR2## in which A is a straight-chained or branched C.sub.2 -C.sub.4 alkylene radical and Z is an oxygen or sulphur atom, R.sub.2 and R.sub.3, which can be the same or different, are hydrogen or halogen atoms, hydroxyl groups, C.sub.2 -C.sub.6 alkanoyl radicals, C.sub.2 -C.sub.4 alkenyl radicals, C.sub.2 -C.sub.4 alkynyl radicals, C.sub.1 -C.sub.6 alkyl radicals, C.sub.1 -C.sub.6 alkoxy radicals, C.sub.2 -C.sub.4 alkenyloxy radicals, C.sub.2 -C.sub.4 alkynyloxy radicals, C.sub.1 -C.sub.6 alkylthio radicals, C.sub.2 -C.sub.6 alkanoylamido radicals or radicals of the general formula: ##STR3## in which R.sub.4 and R.sub.5, which can be the same or different, are hydrogen atoms, C.sub.1 -C.sub.6 alkyl radicals or C.sub.3 -C.sub.10 cycloalkyl radicals or R.sub.4 and R.sub.5 together represent a C.sub.2 -C.sub.8 alkylene radical optionally interrupted by an oxygen or sulphur atom or by an >N-R.sub.6 group, in which R.sub.6 is a hydrogen atom or a C.sub.1 -C.sub.6 alkyl radical, X is a hydrogen atom, Y is a hydrogen atom or a group of the general formula ##STR4## in which Q is a hydrogen atom or, together with X, can also represent a bond and R.sub.7 is a heterocyclic radical which is optionally substituted one or more times by hydroxyl or C.sub.1 -C.sub.6 alkyl or is a phenyl radical which is optionally substituted one or more times by halogen, hydroxyl, mercapto, carboxyl, C.sub.1 -C.sub.6 alkoxycarbonyl, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, C.sub.1 -C.sub.6 alkylthio, C.sub.1 -C.sub.6 alkylsulphinyl, C.sub.1 14 C.sub.6 alkylsulphonyl, C.sub.2 -C.sub.6 alkanoylamido, C.sub.1 -C.sub.6 alkylsulphonylamido, methylenedioxy, nitro, cyano or amino, with the proviso that R.sub.1 cannot be a C.sub.1 -C.sub.6 alkyl radical when X and Y are both hydrogen atoms; as well as the pharmacologically acceptable salts thereof.The present invention also provides intermediates of the general formula: ##STR5## in which R.sub.7 is a heterocyclic radical which is optionally substituted one or more times by hydroxy or C.sub.1 -C.sub.6 alkyl or is a phenyl radical which is optionally substituted one or more times by hydroxyl, halogen, mercapto, carboxyl, C.sub.1 -C.sub.6 alkoxycarbonyl, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, C.sub.1 -C.sub.6 alkylthio, C.sub.1 14 C.sub.6 alkylsulphinyl, cyano C.sub.1 -C.sub.6 alkylsulphonyl, C.sub.2 -C.sub.6 alkanoylamido, C.sub.1 -C.sub.6 alkylsulphonylamido, nitro amino or methylenedioxy.Furthermore, the invention provides processes for the preparation of the above indolin-2-one derivatives and the above intermediates, as well as pharmaceutical compositions containing the above indolin-2-one derivatives.