公开(公告)号：US4526784A

公开(公告)日：1985-07-02

申请号：US369761

申请日：1982-04-19

申请人： Fred R. Heiker ,  Lutz Muller ,  Walter Puls ,  Hilmar Bischoff

发明人： Fred R. Heiker ,  Lutz Muller ,  Walter Puls ,  Hilmar Bischoff

IPC分类号： C07H15/20 ,  C07H15/22 ,  A61K31/73 ,  C07H5/06

CPC分类号： C07H15/22 ,  Y10S514/866

摘要： The invention relates to animo-cyclitol derivatives of Formula (I) and their individual anomers. Also included in the invention are processes for the manufacture of said amino-cyclitol derivatives and their individual anomers, compositions containing said amino-cyclitol derivatives or anomers; and methods for the use of said derivatives and anomers for the treatment of diabetes, adiposity or hyperlipaemia.

摘要翻译： 本发明涉及式（I）的异环 - 旋环衍生物及其各自的末端异构体。 本发明还包括制备所述氨基 - 环醇衍生物及其各自的端基异构体的方法，含有所述氨基 - 环醇衍生物或前体的组合物; 以及用于所述衍生物和异头物用于治疗糖尿病，肥胖症或高脂血症的方法。

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。

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。

公开(公告)号：US4772611A

公开(公告)日：1988-09-20

申请号：US43656

申请日：1987-04-28

申请人： Jurgen Stoltefuss ,  Fred R. Heiker ,  Martin Bechem ,  Rainer Gross ,  Michael Kayser ,  Matthias Schramm ,  Gunter Thomas

发明人： Jurgen Stoltefuss ,  Fred R. Heiker ,  Martin Bechem ,  Rainer Gross ,  Michael Kayser ,  Matthias Schramm ,  Gunter Thomas

IPC分类号： A61K31/44 ,  A61K31/4427 ,  A61K31/4433 ,  A61K31/505 ,  A61P9/00 ,  C07D211/84 ,  C07D211/90 ,  C07D401/04 ,  C07D409/04 ,  C07D413/04 ,  C07D491/04 ,  C07D491/048 ,  A61K31/455

CPC分类号： C07D491/04 ,  C07D211/84 ,  C07D211/90

摘要： Novel cardioactive compounds of the formula ##STR1## in which R.sup.1 is alkyl, aryl or heterocyclic, preferably substituted phenyl,R.sup.2 is alkyl, preferably methyl,R.sup.3 is hydrogen, halogen, acyloxy or alkyl, preferably hydrogen, andR.sup.4 is phenyl, carbalkoxy or together with R.sup.3 forms a ring, preferably carbalkoxy,are produced by reducing the corresponding nitro compounds.

摘要翻译： 式（IMAGE）的新型心脏活性化合物，其中R 1是烷基，芳基或杂环，优选取代的苯基，R 2是烷基，优选甲基，R 3是氢，卤素，酰氧基或烷基，优选氢，R 4是苯基， 通过还原相应的硝基化合物与R3一起形成环，优选为烷氧基。

公开(公告)号：US4590179A

公开(公告)日：1986-05-20

申请号：US692100

申请日：1985-01-16

申请人： Fred R. Heiker ,  Lutz Muller ,  Walter Puls ,  Hilmar Bischoff

发明人： Fred R. Heiker ,  Lutz Muller ,  Walter Puls ,  Hilmar Bischoff

IPC分类号： C07H15/20 ,  C07H15/22 ,  A61K31/73

CPC分类号： C07H15/22 ,  Y10S514/866

摘要： The invention relates to amino-cyclitol derivatives of Formula (I) and their individual anomers. Also included in the invention are processes for the manufacture of said amino-cyclitol derivatives and their individual anomers, compositions containing said amino-cyclitol derivatives or anomers; and methods for the use of said derivatives and anomers for the treatment of diabetes, adiposity or hyperlipaemia.

摘要翻译： 本发明涉及式（I）的氨基 - 环醇衍生物及其各自的端基异构体。 本发明还包括制备所述氨基 - 环醇衍生物及其各自的端基异构体的方法，含有所述氨基 - 环醇衍生物或前体的组合物; 以及用于所述衍生物和异头物用于治疗糖尿病，肥胖症或高脂血症的方法。

公开(公告)号：US4588710A

公开(公告)日：1986-05-13

申请号：US692083

申请日：1985-01-16

申请人： Fred R. Heiker ,  Lutz Muller ,  Walter Puls ,  Hilmar Bischoff

发明人： Fred R. Heiker ,  Lutz Muller ,  Walter Puls ,  Hilmar Bischoff

IPC分类号： C07H15/20 ,  C07H15/22 ,  A61K31/73

CPC分类号： C07H15/22 ,  Y10S514/866

摘要： The invention relates to animo-cyclitol derivatives of Formula (I) and their individual anomers. Also included in the invention are processes for the manufacture of said amino-cyclitol derivatives and their individual anomers, compositions containing said amino-cyclitol derivatives or anomers; and methods for the use of said derivatives and anomers for the treatment of diabetes, adiposity or hyperlipaemia.

摘要翻译： 本发明涉及式（I）的异环 - 旋环衍生物及其各自的末端异构体。 本发明还包括制备所述氨基 - 环醇衍生物及其各自的端基异构体的方法，含有所述氨基 - 环醇衍生物或前体的组合物; 以及用于所述衍生物和异头物用于治疗糖尿病，肥胖症或高脂血症的方法。