Tricyclic aminoalkyl derivatives
    11.
    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

    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。

    Hypoglycaemically and hypolipidaemically active derivatives of
phenyl-alkane-carboxylic acids
    12.
    发明授权
    Hypoglycaemically and hypolipidaemically active derivatives of phenyl-alkane-carboxylic acids 失效
    苯基 - 烷烃 - 羧酸的低血糖和降血糖活性衍生物

    公开(公告)号:US4238506A

    公开(公告)日:1980-12-09

    申请号:US920508

    申请日:1978-06-29

    摘要: Phenyl-alkane-carboxylic acids of the formula ##STR1## wherein A is an aryl, aralkyl or arylvinyl radical optionally substituted by hydroxy, halogen, trifluoromethyl, alkyl, alkylthio, alkoxy, alkenyloxy, alkoxyalkoxy, alkyl-substituted amino, aryloxy or alkoxy-substituted aryloxy, or is an aryloxyalkyl or arylthioalkyl radical, or a heterocyclic ring system optionally substituted by halogen, alkyl or alkoxy,Y is a valency bond or an unbranched or branched lower alkylene radical containing up to 3 carbon atoms,X is a straight or branched, saturated or unsaturated divalent aliphatic hydrocarbon radical containing 2 to 8 carbon atoms, there being at least 2 carbon atoms between the benzene ring and the carboxyl group, andR is a hydrogen atom or a lower alkyl radical, as well as physiologically compatible salts, esters and amides thereof, exhibit hypoglycaemic and hypolipidaemic activity.

    摘要翻译: 式(I)的苯基 - 烷烃 - 羧酸其中A是任选被羟基,卤素,三氟甲基,烷基,烷硫基,烷氧基,烯氧基,烷氧基烷氧基,烷基取代的氨基,芳氧基 或烷氧基取代的芳氧基,或是芳氧基烷基或芳硫基烷基,或任选被卤素,烷基或烷氧基取代的杂环体系,Y是价态键或含有至多3个碳原子的无支链或支链低级亚烷基,X是 含有2至8个碳原子的直链或支链,饱和或不饱和的二价脂族烃基,苯环和羧基之间至少有2个碳原子,R是氢原子或低级烷基,以及 其生理上相容的盐,酯和酰胺显示出低血糖和降血脂活性。