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    Tricyclic aminoalkyl derivatives
    2.
    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。

    Carbazolyl-(4)-oxypropanolamine compounds and therapeutic compositions
    5.
    发明授权
    Carbazolyl-(4)-oxypropanolamine compounds and therapeutic compositions 失效
    （4） - 氧丙醇胺化合物和治疗组合物

    公开(公告)号：US4503067A

    公开(公告)日：1985-03-05

    申请号：US479921

    申请日：1983-04-04

    申请人： Fritz Wiedemann ,  Wolfgang Kampe ,  Max Thiel ,  Gisbert Sponer ,  Egon Roesch ,  Karl Dietmann

    发明人： Fritz Wiedemann ,  Wolfgang Kampe ,  Max Thiel ,  Gisbert Sponer ,  Egon Roesch ,  Karl Dietmann

    IPC分类号： A61K31/40 ,  A61K31/403 ,  A61P9/08 ,  A61P25/02 ,  C07D209/88 ,  C07D317/64 ,  C07D401/12 ,  C07D405/12 ,  C07D209/82

    CPC分类号： C07D209/88 ,  C07D317/64

    摘要： Carbazolyl-(4)-oxypropanolamine compounds of the formula ##STR1## wherein R.sub.1 is hydrogen, lower alkanoyl or aroyl;R.sub.2 is hydrogen, lower alkyl or arylalkyl;R.sub.3 is hydrogen or lower alkyl;R.sub.4 is hydrogen or lower alkyl, or when X is oxygen, R.sub.4 together with R.sub.5 can represent --CH.sub.2 --O--;X is a valency bond, --CH.sub.2 --, oxygen or sulfur;Ar is mono- or bicyclic aryl or pyridyl;R.sub.5 and R.sub.6 are individually selected from hydrogen, halogen, hydroxyl, lower alkyl, aminocarbonyl, lower alkoxy, aralkyloxy, lower alkylthio, lower alkylsulphinyl or lower alkylsulphonyl;R.sub.5 and R.sub.6 together can represent methylenedioxy;and the salts thereof with physiologically acceptable acids are outstandingly effective in the treatment and prophylaxis of circulatory and cardiac diseases, e.g., hypertension and angina pectoris.

    摘要翻译： 式（I）的羧基 - （4） - 氧丙醇胺化合物，其中R 1是氢，低级烷酰基或芳酰基; R2是氢，低级烷基或芳基烷基; R3是氢或低级烷基; R4是氢或低级烷基，或者当X是氧时，R4与R5一起可以代表-CH2-O-; X是价键，-CH 2 - ，氧或硫; Ar是单环或双环芳基或吡啶基; R5和R6分别选自氢，卤素，羟基，低级烷基，氨基羰基，低级烷氧基，芳烷氧基，低级烷硫基，低级烷基亚磺酰基或低级烷基磺酰基; R5和R6一起可以代表亚甲二氧基; 并且其与生理上可接受的酸的盐在治疗和预防循环和心脏疾病例如高血压和心绞痛方面是显着的。