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    • 26. 发明授权
    • Benzylaminoaryl-dihydropyridinelactones and their use in medicaments
    • 苄基氨基芳基 - 二氢吡啶内酯及其在药物中的用途
    • US4904665A
    • 1990-02-27
    • US158184
    • 1988-02-18
    • Siegfried GoldmannRainer GrossMartin BechemMichael KayserMatthias SchrammSiegbert Hebisch
    • Siegfried GoldmannRainer GrossMartin BechemMichael KayserMatthias SchrammSiegbert Hebisch
    • A61K31/44A61P3/08A61P9/00A61P9/06A61P9/08A61P9/10C07D211/90C07D491/04C07D491/048
    • C07D491/04C07D211/90
    • A benzylaminoaryl-dihydropyridinelactone compound of the formula (I) ##STR1## in which R.sup.1 represents hydrogen, halogen, cyano, nitro, C.sub.6 -C.sub.12 -aryl, C.sub.1 -C.sub.8 -alkyl, C.sub.1 -C.sub.8 -alkoxy, C.sub.1 -C.sub.6 -alkylthio, trifluoromethyl, trifluoromethoxy, trifluoromethylthio, difluoromethoxy, di-C.sub.1 -C.sub.5 -alkylamino, C.sub.1 -C.sub.6 -alkoxycarboxyl or C.sub.1 -C.sub.6 -alkylsulphonyl,R.sup.2 represents hydrogen, or represents a straight-chain, branched or cyclic, saturated or unsaturated hydrocarbon radical having up to 10 carbon atoms which is optionally substituted by C.sub.1 -C.sub.6 -alkoxy, C.sub.1 -C.sub.6 -alkylthio, C.sub.1 -C.sub.6 -alkylsulphonyl, halogen, cyano, hydroxyl, pyridyl, thienyl, pyrimidyl, piperidinyl, phenyl or an amino group, where the amino group carries two identical or different substituents from the series comprising C.sub.1 -C.sub.5 -alkyl, phenyl or benzyl,R.sup.3 represents C.sub.1 -C.sub.5 -alkyl, or represents cyano, hydroxymethyl or formyl, andR.sup.4 represents hydrogen, halogen, C.sub.1 -C.sub.5 -alkyl or trifluoromethyl,and its isomers, isomeric mixtures, racemates or optical antipodes, and physiologically acceptable salts thereof. The compound being useful to improve the contractility of the heart and the tonus of the smooth muscles.
    • 式(I)的苄基氨基芳基 - 二氢吡啶内酯化合物其中R 1表示氢,卤素,氰基,硝基,C 6 -C 12 - 芳基,C 1 -C 8 - 烷基,C 1 -C 8 - 烷氧基,C 1 -C 6 - 烷硫基,三氟甲基,三氟甲氧基,三氟甲硫基,二氟甲氧基,二-C 1 -C 5烷基氨基,C 1 -C 6 - 烷氧基羧基或C 1 -C 6烷基磺酰基,R 2表示氢,或表示直链,支链或环状饱和或不饱和烃 具有至多10个碳原子的基团,其任选被C 1 -C 6 - 烷氧基,C 1 -C 6 - 烷硫基,C 1 -C 6 - 烷基磺酰基,卤素,氰基,羟基,吡啶基,噻吩基,嘧啶基,哌啶基,苯基或氨基取代, 其中氨基从包含C 1 -C 5 - 烷基,苯基或苄基的系列中携带两个相同或不同的取代基,R 3表示C 1 -C 5 - 烷基,或表示氰基,羟甲基或甲酰基,R 4表示氢,卤素,C 1 -C 5 - 烷基或三氟甲基,及其异构体,异构体混合物,外消旋体或光学抗体 es及其生理上可接受的盐。 该化合物可用于改善心脏和平滑肌紧张的收缩性。