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    • 1. 发明授权
    • Tricyclic aminoalkyl derivatives
    • 三环氨基烷基衍生物
    • US4070373A
    • 1978-01-24
    • US291426
    • 1972-09-22
    • Werner WinterMax ThielKurt Stach, deceasedby Werner Plattner, administratorWolfgang SchaumannKarl Dietmann
    • Werner WinterMax ThielKurt Stach, deceasedby Werner Plattner, administratorWolfgang SchaumannKarl Dietmann
    • C07D311/90C07D313/12C07D337/12C07D337/16
    • C07D337/16C07D311/90C07D313/12C07D337/12C07C2103/18
    • 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.
    • 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。
    • 7. 发明授权
    • Adenosine-5'-carboxylic acid amides
    • 腺苷-5'-羧酸酰胺
    • US4224438A
    • 1980-09-23
    • US161338
    • 1971-07-09
    • Erich FaulandWolfgang KampeMax ThielKarl DietmannWolfgang Juhran
    • Erich FaulandWolfgang KampeMax ThielKarl DietmannWolfgang Juhran
    • C07H19/16A61K31/70C07H19/18
    • C07H19/16
    • Adenosine-5'-carboxylic acid derivatives of the general formula: ##STR1## wherein Z is two hydrogen atoms or a divalent lower alkylidene radical, ##STR2## R is an aliphatic or arylaliphatic radical, and R.sub.1 and R.sub.2 are independently a hydrogen, hydroxyl, amino, lower alkyl, lower alkenyl, optionally N-alkylated lower aminoalkyl, cycloalkyl, hydroxyalkyl or piperidinyl radical, orR.sub.1 and R.sub.2 taken together are a divalent ethylene radical containing 4-7 carbon atoms optionally interrupted by an oxygen or sulfur atom or by an imino, alkylimino or arylimino radical or a pharmacologically compatible salt thereof.The esters surprisingly can be prepared by esterifying the acid in the presence of sulfuric acid without hydrolyzing the sugar group. While the esters have some activity, they can be used to make the amides which are characterized by marked coronary activity.
    • 具有以下通式的腺苷-5'-羧酸衍生物:其中Z为两个氢原子或二价低级亚烷基,其中R 1和R 2独立为 氢,羟基,氨基,低级烷基,低级烯基,任选N-烷基化的低级氨基烷基,环烷基,羟基烷基或哌啶基,或者R 1和R 2一起是含有4-7个碳原子的任选被氧或硫中断的二价亚乙基 或亚氨基,亚氨基亚氨基或芳基亚氨基或其药理学上相容的盐。 这些酯令人惊奇地可以通过在硫酸存在下酯化酸而不水解糖基来制备。 虽然酯具有一些活性,但它们可用于制备以标记的冠状动脉为特征的酰胺。