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    • 75. 发明授权
    • Dihydropyridine compounds and their use in reducing blood sugar
    • 二氢吡啶化合物及其在降血糖中的应用
    • US4786641A
    • 1988-11-22
    • US87491
    • 1987-08-20
    • Siegfried GoldmannHans-Jurgen AhrWalter PulsHilmar BischoffDieter PetzinnaKlaus SchlossmannJoachim Bender
    • Siegfried GoldmannHans-Jurgen AhrWalter PulsHilmar BischoffDieter PetzinnaKlaus SchlossmannJoachim Bender
    • A61K31/465A61K31/445A61K31/451A61P3/08C07D211/90C07D491/04C07D491/044C07D491/048A61K31/44
    • C07D491/04C07D211/90
    • 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.
    • 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。