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    • 4. 发明授权
    • 3-Nitro-5-amide-1,4-dihydropyridines with positive inotropic activity
    • 具有正性肌力活性的3-硝基-5-酰胺-1,4-二氢吡啶
    • US4540684A
    • 1985-09-10
    • US612093
    • 1984-05-18
    • Jurgen StoltefussGerhard FranckowiakHorst BoshagenSiegfried GoldmannMatthias SchrammGunter ThomasRainer Gross
    • Jurgen StoltefussGerhard FranckowiakHorst BoshagenSiegfried GoldmannMatthias SchrammGunter ThomasRainer Gross
    • A61K31/455A61P3/08A61P9/02A61P9/04C07D211/90C07D211/98A61K31/70C07D405/12
    • C07D211/90
    • A 1,4-dihydropyridine derivative of the formula ##STR1## in which R and R.sub.1 each independently is hydrogen, C.sub.1 -C.sub.4 -alkyl, C.sub.1 to C.sub.12 -alkoxy, C.sub.1 -C.sub.4 -halogenoalkoxy, halogen, nitro, trifluoromethyl, ##STR2## X is oxygen or sulphur, R.sub.4 and R.sub.5 each independently is hydrogen, C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.6 -alkoxy, halogen, trifluoromethyl, amino or nitro, andR.sub.2 and R.sub.3 each independently is hydrogen, a C.sub.1 -C.sub.10 -alkyl, C.sub.2 -C.sub.10 -alkenyl or C.sub.3 -C.sub.10 -alkinyl radical which is optionally substituted by halogen, hydroxyl, C.sub.1 -C.sub.4 -alkoxy, amino, mono- and di-C.sub.1 -C.sub.4 -alkylamino, carbo-C.sub.1 -C.sub.6 -alkoxy and/or nitro, a C.sub.3 to C.sub.6 -membered cycloalkyl radical, a phenyl radical which is optionally substituted by C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.6 -alkoxy, halogen, amino and/or nitro, or a phenyl-C.sub.1 -C.sub.3 -alkyl radical, or a carbohydrate radical which is optionally bonded via a C.sub.1 -C.sub.8 -alkyl chain to the amide nitrogen atomor a pharmaceutically acceptable acid addition salt thereof, which improves the contractility of the heart, raises the blood pressure, lowers the blood sugar, reduces the swelling of mucous membranes and affects the salt and fluid balances of a patient.
    • 其中R和R 1各自独立地为氢,C 1 -C 4 - 烷基,C 1 -C 12 - 烷氧基,C 1 -C 4卤代烷氧基,卤素,硝基,三氟甲基, X是氧或硫,R4和R5各自独立地是氢,C1-C4-烷基,C1-C6-烷氧基,卤素,三氟甲基,氨基或硝基,R2和R3各自独立地是氢,C1-C10 - 烷基,C 2 -C 10 - 烯基或C 3 -C 10 - 炔基,其任选被卤素,羟基,C 1 -C 4 - 烷氧基,氨基,单 - 和二-C 1 -C 4 - 烷基氨基,C 1 -C 6 - 和/或硝基,C3至C6元环烷基,任选被C 1 -C 4 - 烷基,C 1 -C 6 - 烷氧基,卤素,氨基和/或硝基取代的苯基,或苯基-C 1 -C 3 - 烷基或通过C1-C8烷基链任选与酰胺氮原子键合的碳水化合物基团或其药学上可接受的酸加成盐,其改善心脏的收缩力,使血压升高 ure,降低血糖,减少粘膜肿胀,影响患者的盐和液体平衡。