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    Intermediate 8-carboxaldehyde-(-chromone and -thiochromone) derivatives
    6.
    发明授权
    Intermediate 8-carboxaldehyde-(-chromone and -thiochromone) derivatives 失效
    中间体8-甲醛 - （ - 色酮和硫代色酮）衍生物

    公开(公告)号：US4628107A

    公开(公告)日：1986-12-09

    申请号：US750571

    申请日：1985-06-28

    申请人： Siegfried Goldmann ,  Gerhard Franckowiak ,  Matthias Schramm ,  Gunter Thomas ,  Rainer Gross

    发明人： Siegfried Goldmann ,  Gerhard Franckowiak ,  Matthias Schramm ,  Gunter Thomas ,  Rainer Gross

    IPC分类号： C07D211/90 ,  C07D311/22 ,  C07D311/24 ,  C07D311/30 ,  C07D335/06 ,  C07D405/04 ,  C07D409/04 ,  C07D409/14 ,  C07D405/06 ,  C07D405/12 ,  C07D409/06 ,  C07D409/12

    CPC分类号： C07D335/06 ,  C07D211/90 ,  C07D311/22 ,  C07D311/24 ,  C07D311/30 ,  C07D405/04 ,  C07D409/04 ,  C07D409/14

    摘要： Novel chromone-8-aldehydes and thiochromone-8-aldehydes, useful in making pharmaceutically active dihydropyridines, of the formula ##STR1## in which R.sub.1 represents hydrogen, a C.sub.1 -C.sub.10 aliphatic hydrocarbon radical, a C.sub.1 -C.sub.10 alkyl carboxylate, or an aromatic or heteroaromatic ring which optionally has 1-5 identical or different halogen, C.sub.1 -C.sub.10 -alkyl, C.sub.1 -C.sub.10 -alkoxy, C.sub.1 -C.sub.10 -alkylthio, C.sub.1 -C.sub.10 -alkylsulphinyl, cyano, hydroxyl, nitro, C.sub.1 -C.sub.5 -monofluoroalkyl or polyfluoroalkyl, C.sub.1 -C.sub.5 monofluoroalkoxy or polyfluoroalkoxy, C.sub.1 -C.sub.6 monofluoroalkylthio or polyfluoroalkylthio, amino, C.sub.1 -C.sub.5 -monoalkylamino or C.sub.1 -C.sub.5 dialkylamino substituents,R.sub.2 represents hydrogen or 1 to 3 halogen atoms, A represents a single bond, a C.sub.1 -C.sub.20 alkylene chain or a C.sub.2 -C.sub.20 alkylene chain which can optionally be interrupted by oxygen or sulphur, andX represents oxygen or sulphur,are made from corresponding compounds which in 8-position carry an ester or olefinic radical.

    摘要翻译： 可用于制备药物活性二氢吡啶的新颖的色酮-8-醛和硫色酮-8-醛，其具有式“IMAGE”，其中R 1表示氢，C 1 -C 10脂族烃基，C 1 -C 10烷基羧酸酯或芳族 或任选具有1-5个相同或不同的卤素，C 1 -C 10 - 烷基，C 1 -C 10 - 烷氧基，C 1 -C 10 - 烷硫基，C 1 -C 10 - 烷基亚磺酰基，氰基，羟基，硝基，C 1 -C 5 - 单氟烷基或 多氟烷基，C 1 -C 5单氟烷氧基或多氟烷氧基，C 1 -C 6单氟烷硫基或多氟烷硫基，氨基，C 1 -C 5单烷基氨基或C 1 -C 5二烷基氨基取代基，R 2表示氢或1至3个卤素原子，A表示单键， 亚烷基链或可任选被氧或硫中断的C 2 -C 20亚烷基链，X表示氧或硫，由相应的8-位带有酯或烯基的化合物制成。

    Positive inotropic 3-nitro-5-substituted ester and thioester-1,4-dihydropyridines
    7.
    发明授权
    Positive inotropic 3-nitro-5-substituted ester and thioester-1,4-dihydropyridines 失效
    正性收缩性3-硝基-5-取代酯和硫酯-1,4-二氢吡啶

    公开(公告)号：US4645775A

    公开(公告)日：1987-02-24

    申请号：US734502

    申请日：1985-05-15

    申请人： Jurgen Stoltefuss ,  Fred R. Heiker ,  Gerhard Franckowiak ,  Matthias Schramm ,  Gunter Thomas ,  Rainer Gross

    发明人： Jurgen Stoltefuss ,  Fred R. Heiker ,  Gerhard Franckowiak ,  Matthias Schramm ,  Gunter Thomas ,  Rainer Gross

    IPC分类号： A61K31/4427 ,  A61K31/455 ,  A61P9/04 ,  A61P9/12 ,  C07D211/90 ,  C07D401/12 ,  C07D413/04

    CPC分类号： C07D401/12 ,  C07D211/90 ,  C07D413/04

    摘要： 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.

    摘要翻译： 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。

    3-Nitro-5-amide-1,4-dihydropyridines with positive inotropic activity
    8.
    发明授权
    3-Nitro-5-amide-1,4-dihydropyridines with positive inotropic activity 失效
    具有正性肌力活性的3-硝基-5-酰胺-1,4-二氢吡啶

    公开(公告)号：US4540684A

    公开(公告)日：1985-09-10

    申请号：US612093

    申请日：1984-05-18

    申请人： Jurgen Stoltefuss ,  Gerhard Franckowiak ,  Horst Boshagen ,  Siegfried Goldmann ,  Matthias Schramm ,  Gunter Thomas ,  Rainer Gross

    发明人： Jurgen Stoltefuss ,  Gerhard Franckowiak ,  Horst Boshagen ,  Siegfried Goldmann ,  Matthias Schramm ,  Gunter Thomas ,  Rainer Gross

    IPC分类号： A61K31/455 ,  A61P3/08 ,  A61P9/02 ,  A61P9/04 ,  C07D211/90 ,  C07D211/98 ,  A61K31/70 ,  C07D405/12

    CPC分类号： C07D211/90

    摘要： 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.

    摘要翻译： 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。

    5-Nitro 1,4-dihydropyridines having a positive inotropic effect
    9.
    发明授权
    5-Nitro 1,4-dihydropyridines having a positive inotropic effect 失效
    具有正性肌力作用的5-硝基1,4-二氢吡啶类

    公开(公告)号：US4537881A

    公开(公告)日：1985-08-27

    申请号：US627596

    申请日：1984-07-03

    申请人： Fred R. Heiker ,  Jurgen Stoltefuss ,  Gerhard Franckowiak ,  Matthias Schramm ,  Gunter Thomas ,  Rainer Gross

    发明人： Fred R. Heiker ,  Jurgen Stoltefuss ,  Gerhard Franckowiak ,  Matthias Schramm ,  Gunter Thomas ,  Rainer Gross

    IPC分类号： A61K31/70 ,  A61K31/7028 ,  A61P3/08 ,  A61P9/04 ,  A61P9/12 ,  C07H15/04 ,  C07H15/06 ,  C07H15/12 ,  C07H15/14 ,  C07H15/26 ,  A61K31/41 ,  A61K31/395 ,  C07D405/12

    CPC分类号： C07H15/06 ,  C07H15/04 ,  C07H15/14 ,  C07H15/26

    摘要： Novel 1,4-dihydropyridines of the fomula ##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## in which Z is oxygen or sulphur, andR.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, sulphur or the radical NR.sub.6, R.sub.6 is a C.sub.1 -C.sub.6 -alkyl group,A is a C.sub.2 -C.sub.10 -alkylene group, it being necessary that at least two C atoms are located in the alkylene chain which connects the carbonyloxy group to X, andR.sub.3 is a monosaccharide or disaccharide moiety or a protected monosaccharide or disaccharide moiety,or pharmaceutically acceptable addition salts thereof, which exhibit positive inotropic activity and are useful in treating circulatory disorders.

    摘要翻译： R1和R2各自独立地为氢，C1-C4-烷基，C1-C12-烷氧基，C1-C4-卤代烷氧基，卤素，硝基，C1-C4-卤代烷基， C1-C4卤代烷基巯基，其中Z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，C1-C4-卤代烷基，C1-C4-卤代烷基， 卤代烷氧基或硝基，或R 1和R 2与苯环的2 C原子一起形成环，X为氧，硫或基团NR 6，R 6为C 1 -C 6 - 烷基，A为C 2 - C10亚烷基，必须至少两个C原子位于将羰氧基连接到X的亚烷基链中，R3是单糖或二糖部分或受保护的单糖或二糖部分，或其药学上可接受的加成盐 ，其表现出正性肌力活性并且可用于治疗循环障碍。