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    Dihydropyridine compounds and their use in reducing blood sugar
    4.
    发明授权
    Dihydropyridine compounds and their use in reducing blood sugar 失效
    二氢吡啶化合物及其在降血糖中的应用

    公开(公告)号：US4786641A

    公开(公告)日：1988-11-22

    申请号：US87491

    申请日：1987-08-20

    申请人： Siegfried Goldmann ,  Hans-Jurgen Ahr ,  Walter Puls ,  Hilmar Bischoff ,  Dieter Petzinna ,  Klaus Schlossmann ,  Joachim Bender

    发明人： Siegfried Goldmann ,  Hans-Jurgen Ahr ,  Walter Puls ,  Hilmar Bischoff ,  Dieter Petzinna ,  Klaus Schlossmann ,  Joachim Bender

    IPC分类号： A61K31/465 ,  A61K31/445 ,  A61K31/451 ,  A61P3/08 ,  C07D211/90 ,  C07D491/04 ,  C07D491/044 ,  C07D491/048 ,  A61K31/44

    CPC分类号： C07D491/04 ,  C07D211/90

    摘要： Blood-sugar-lowering dihydropyridines of the formula ##STR1## in which R.sup.1 represents phenyl, naphthyl, thienyl, pyridyl, chromenyl or thiochromenyl, it being possible for the radicals mentioned each to carry up to 2 identical or different substituents from the series comprising halogen, alkyl, alkoxy and alkylthio with in each case up to 6 carbon atoms, fluoroalkyl and fluoroalkoxy with in each case up to 3 carbon atoms and 3 fluorine atoms, nitro and cyano,R.sup.2 represents straight-chain, branched or cyclic alkyl which has up to 8 carbon atoms, can be interrupted in the alkyl chain by an oxygen or a sulphur atom and can be substituted by halogen, phenyl, cyano, hydroxyl, amino, alkylamino or dialkylamino with in each case up to 3 carbon atoms per alkyl group or by N-benzylmethylamino,R.sup.3 represents straight-chain, branched or cyclic alkyl which has up to 6 carbon atoms, can be interrupted in the alkyl chain by an oxygen atom and can be substituted by halogen, hydroxyl, amino, phenyl, morpholino, carboxy or alkoxycarbonyl with up to 4 carbon atoms andR.sup.4 and R.sup.5 each represent hydroxyl, orR.sup.4 and R.sup.5 together represent --O--,or a physiologically acceptable salt thereof.

    摘要翻译： 其中R1代表苯基，萘基，噻吩基，吡啶基，色烯基或硫代色烯基的式“IMAGE”的降血糖二氢吡啶类，各自所提及的基团有可能从包含卤素的系列中携带多达2个相同或不同的取代基 ，烷基，烷氧基和烷硫基，在每种情况下最多6个碳原子，氟代烷基和氟代烷氧基，在每种情况下最多3个碳原子和3个氟原子，硝基和氰基，R2表示直链，支链或环状的烷基， 至8个碳原子，可以通过氧或硫原子在烷基链中被中断，并且可以被卤素，苯基，氰基，羟基，氨基，烷基氨基或二烷基氨基取代，在每种情况下，每个烷基最多为3个碳原子，或 通过N-苄基甲基氨基，R3表示具有多至6个碳原子的直链，支链或环状烷基，可以在烷基链中被氧原子中断，并可被卤素，羟基，氨基，苯基， 具有至多4个碳原子的直链，羧基或烷氧基羰基，且R 4和R 5各自表示羟基，或者R 4和R 5一起表示-O-或其生理上可接受的盐。

    Substituted 1,8-naphthyridines and their use in medicaments
    10.
    发明授权
    Substituted 1,8-naphthyridines and their use in medicaments 失效
    取代的1,8-萘啶并用于药物

    公开(公告)号：US5034399A

    公开(公告)日：1991-07-23

    申请号：US496757

    申请日：1990-03-21

    申请人： Walter Hubsch ,  Rolf Angerbauer ,  Peter Fey ,  Thomas Philipps ,  Hilmar Bischoff ,  Dieter Petzinna ,  Delf Schmidt

    发明人： Walter Hubsch ,  Rolf Angerbauer ,  Peter Fey ,  Thomas Philipps ,  Hilmar Bischoff ,  Dieter Petzinna ,  Delf Schmidt

    IPC分类号： A61K31/435 ,  A61P3/06 ,  A61P9/10 ,  C07D471/04

    CPC分类号： C07D471/04

    摘要： Inhibitors of 3-hydrooxy-3-methyl-glutarylcoenzyme A reductase which are 1,8-naphthyridines of the formula ##STR1## in which Arepresents a 3- to 7-membered heterocycle which is optionally substituted, or aryl which is optionally substituted,Brepresents cycloalkyl or alkyl which is optionally substituted, aryl which is optionally substituted,D and E are identical or different andrepresents hydrogen, halogen, mercapto, hydroxyl, alkoxy, alkyl which is optionally substituted, or a group of the formula --NR.sup.1 R.sup.2, aryl, aryloxy or arylthio having 6 to 10 carbon atoms, which is optionally substituted,Yrepresents a group of the formula ##STR2## in which Jdenotes hydrogen, hydroxyl, mercapto or halogen, or alkyl, alkoxy or alkylthio which are optionally substituted, aryloxy, benzyloxy or arylthio or a group of the formula --NR.sup.1 R.sup.2,Zdenotes oxygen or sulphur,Gdenotes hydrogen, alkyl or alkenyl which is optionally substituted,Xrepresents a group of the formula --CH.sub.2 --CH.sub.2 -- or --CH.dbd.CH--,andRrepresents a group of the formula ##STR3## in which R.sup.5denotes hydrogen or alkyl, andR.sup.6denotes hydrogen or alkyl, which may be substituted by phenyl, ordenotes aryl or a cation,and their salts.

    摘要翻译： 作为式“IMAGE”的1,8-萘啶的3-羟基-3-氧代-3-甲基 - 戊二酰辅酶A还原酶的抑制剂，其中A表示任选取代的3-至7-元杂环，或任选取代的芳基， B代表任选取代的环烷基或烷基，任选取代的芳基，D和E相同或不同，代表氢，卤素，巯基，羟基，烷氧基，任选被取代的烷基，或式-NR1R2的基团， 芳基，芳氧基或具有6至10个碳原子的芳硫基，其任选被取代，Y表示下式的基团，其中J表示氢，羟基，巯基或卤素，或任选被取代的烷基，烷氧基或烷硫基， 芳氧基，苄氧基或芳硫基或式-NR1R2的基团，Z表示氧或硫，G表示氢，任选被取代的烷基或烯基，X表示式-CH 2 -CH 2 - 或-CH = CH- ，和R 表示式为“IMAGE”的基团，其中R5表示氢或烷基，R6表示氢或可被苯基取代的烷基，或表示芳基或阳离子及其盐。