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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。
    • 7. 发明授权
    • Positive inotropic 3-nitro-5-substituted ester and
thioester-1,4-dihydropyridines
    • 正性收缩性3-硝基-5-取代酯和硫酯-1,4-二氢吡啶
    • US4645775A
    • 1987-02-24
    • US734502
    • 1985-05-15
    • Jurgen StoltefussFred R. HeikerGerhard FranckowiakMatthias SchrammGunter ThomasRainer Gross
    • Jurgen StoltefussFred R. HeikerGerhard FranckowiakMatthias SchrammGunter ThomasRainer Gross
    • A61K31/4427A61K31/455A61P9/04A61P9/12C07D211/90C07D401/12C07D413/04
    • C07D401/12C07D211/90C07D413/04
    • Novel 3-nitro-dihydropyridine derivatives of the formula ##STR1## in which R.sub.1 and R.sub.2 each independently is hydrogen, C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.12 -alkoxy, C.sub.1 -C.sub.4 -halogenoalkoxy, halogen, nitro, C.sub.1 -C.sub.4 -halogenoalkyl, C.sub.1 -C.sub.4 -halogenoalkylmercapto, ##STR2## Z 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, C.sub.1 -C.sub.4 -halogenoalkyl, C.sub.1 -C.sub.4 -halogenoalkoxy or nitro, orR.sub.1 and R.sub.2, together with 2 C atoms of the phenyl ring form the ring ##STR3## X is oxygen or sulphur, A is a hydrocarbon radical with up to 12 C atoms which optionally contains one or two identical or different chain members from the group comprising O, S and CO and/or which is optionally substituted by hydroxyl or aliphatic acyloxy with up to 4 C atoms,R.sub.3 is --O--COR.sub.6, --S--CO--R.sub.6, SH, OH , NH.sub.2, ##STR4## NH--COR.sub.6, COOR.sub.6, NR.sub.7 R.sub.8 or CONR.sub.7 R.sub.8, R.sub.6 is hydrogen or an aliphatic radical with up to 6 C atoms or a phenyl radical, andR.sub.7 and R.sub.8 each independently is hydrogen or an aliphatic radical with up to 6 C atoms or a phenyl radical,or a physiologically acceptable salts thereof, which are active in circulation and exhibit positive inotropic activity.
    • 其中R 1和R 2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,C 1 -C 4 - 卤代烷基的新颖的3-硝基 - 二氢吡啶衍生物 ,C 1 -C 4卤代烷基巯基,Z为氧或硫,R 4和R 5各自独立地为氢,C 1 -C 4 - 烷基,C 1 -C 6 - 烷氧基,卤素,C 1 -C 4 - 卤代烷基,C 1 -C 4卤代烷氧基或 硝基或R1和R2与苯环的2 C原子一起形成环,X是氧或硫,A是具有至多12个C原子的烃基,其任选地含有一个或两个相同或不同的链成员 由包含O,S和CO的基团和/或其任选被具有至多4个C原子的羟基或脂族酰氧基取代,R 3是-O-COR 6,-S-CO-R 6,SH,OH,NH 2, > NH-COR 6,COOR 6,NR 7 R 8或CONR 7 R 8,R 6是氢或具有至多6个C原子或苯基的脂族基团,并且R 7和R 8各自独立地为氢或至多6个碳原子的脂族基团 oms或苯基或其生理上可接受的盐,其在循环中具有活性并表现出正性肌力活性。