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    • 1. 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。
    • 3. 发明授权
    • Certain 4-thienyl-dihydropyridines
    • 某些4-噻吩基 - 二氢吡啶类
    • US4801715A
    • 1989-01-31
    • US937870
    • 1986-12-04
    • Siegfried GoldmannHilmar BischoffWalter PulsJoachim BenderDieter PetzinnaKlaus Schlossmann
    • Siegfried GoldmannHilmar BischoffWalter PulsJoachim BenderDieter PetzinnaKlaus Schlossmann
    • A61K31/435A61P3/08A61P3/10C07D491/04C07D491/048
    • C07D491/04
    • Blood sugar levels are reduced by administration of novel 4-thienyl-dihydropyridines of the formula ##STR1## in which R.sup.1 represents 1 or 2 halogen atoms, or represents straight-chain, branched or cyclic alkyl with up to 8 carbon atoms,R.sup.2 represents a straight-chain, branched or cyclic, saturated or unsaturated hydrocarbon radical which has up to 15 carbon atoms, is optionally interrupted by one or two oxygen atoms, -N-phenyl or --SO.sub.n --(n=0, 1 or 2) and is optionally substituted by halogen, phenyl, hydroxyl, cyano, amino, C.sub.1 -C.sub.6 -alkylamino, di-C.sub.1 -C.sub.6 -alkylamino, pyridyl, piperidino, N-phenylpiperazino, N-methylpiperazino, morpholino or N-benzyl-N-benzyl-N-methyl-amino,R.sup.3 represents hydrogen, or represents straight-chain, branched or cyclic alkyl which has up to 6 carbon atoms and is optionally substituted by halogen, hydroxyl, amino or amino-C.sub.1 -C.sub.6 -alkoxy, or represents cyano or formyl andR.sup.4 represents hydrogen or a straight-chain, branched or cyclic alkyl radical which has up to 10 carbon atoms, is optionally interrupted by one or two oxygen atoms in the chain and is optionally substituted by halogen, cyano, hydroxyl, phenyl, carboxyl, C.sub.1 -C.sub.6 -alkoxycarbonyl, amino, C.sub.1 -C.sub.6 -alkylamino, di-C.sub.1 -C.sub.6 -alkylamino, formyl, piperidino, morpholino or thiomorpholino,or physiologically acceptable salts thereof.
    • 通过给予式“IMAGE”的新型4-噻吩基 - 二氢吡啶,其中R1代表1或2个卤素原子,或代表具有至多8个碳原子的直链,支链或环状烷基,降低血糖水平,R2代表 具有多至15个碳原子的直链,支链或环状饱和或不饱和烃基任选地被一个或两个氧原子间隔,-N-苯基或-SOn-(n = 0,1或2),并且是 任选被卤素,苯基,羟基,氰基,氨基,C 1 -C 6 - 烷基氨基,二-C 1 -C 6 - 烷基氨基,吡啶基,哌啶子基,N-苯基哌嗪子基,N-甲基哌嗪基,吗啉代或N-苄基-N-苄基-N 甲基 - 氨基,R 3表示氢,或表示具有多至6个碳原子并且任选被卤素,羟基,氨基或氨基-C 1 -C 6 - 烷氧基取代的直链,支链或环状烷基,或表示氰基或甲酰基 并且R 4表示氢或具有至多10个碳的直链,支链或环状烷基 氰基,羟基,苯基,羧基,C 1 -C 6 - 烷氧基羰基,氨基,C 1 -C 6 - 烷基氨基,二-C 1 -C 6烷基氨基,C 1 -C 6 - 烷基氨基, ,甲酰基,哌啶子基,吗啉代或硫代吗啉代,或其生理上可接受的盐。
    • 4. 发明授权
    • Dihydropyridinelactols and their use as medicaments which influence
blood sugar
    • 二氢嘧啶醇和它们作为影响血糖的药物的用途
    • US4721719A
    • 1988-01-26
    • US900866
    • 1986-08-27
    • Siegfried GoldmannFriedrich BossertHans J. AhrHilmar BischoffWalter PulsDieter PetzinnaKlaus SchlossmannJoachim Bender
    • Siegfried GoldmannFriedrich BossertHans J. AhrHilmar BischoffWalter PulsDieter PetzinnaKlaus SchlossmannJoachim Bender
    • C07D307/33A61K31/435A61K31/4355A61K31/44A61P3/08A61P3/10C07D491/04C07D491/048C07D495/04
    • C07D491/04
    • Reducing blood sugar with the novel dihydropyridinelactols, or salts thereof, of the formula ##STR1## in which R.sup.1 represents a phenyl, naphthyl, thienyl, pyridyl, chromonyl, thiochromonyl or thiochromenyl radical, the stated radicals optionally containing 1 or 2 identical or different substituents from the group consisting of fluorine, chlorine and bromine, alkyl, alkoxy and alkylthio, each having 1 to 6 carbon atoms, and fluoroalkyl or fluoroalkoxy, each having up to 3 carbon atoms and 3 fluorine atoms, and nitro and cyano,R.sup.2 represents a straight-chain, branched or cyclic alkyl having up to 12 carbon atoms which is optionally interrupted by 1 or 2 oxygen or sulphur atoms and which is optionally substituted by fluorine, chlorine, phenyl, cyano, hydroxyl, amino, C.sub.1 -C.sub.3 -alkylamino, di-C.sub.1 -C.sub.3 -alkylamino or N-benzylmethylamino,R.sup.3 represents cyano or straight-chain or branched alkyl which has up to 4 carbon atoms and is optionally interrupted in the chain by N-C.sub.1 -C.sub.3 -alkyl and/or oxygen, andR.sup.4 represents straight-chain, branched or cyclic alkyl which has up to 6 carbon atoms and is optionally interrupted by 1 or 2 oxygen atoms and is substituted by one or more radicals from amongst fluorine, chlorine, hydroxyl, phenyl, amino, carboxyl and C.sub.1 -C.sub.4 -alkoxycarbonyl.
    • 其中R 1表示苯基,萘基,噻吩基,吡啶基,苯并二氢吡喃基或硫代色烯基的新颖的二氢吡啶类醇或其盐,降低血糖,所述基团任选地含有1或2个相同或不同的取代基 由氟,氯和溴组成的组,每个具有1至6个碳原子的烷基,烷氧基和烷硫基,以及氟烷基或氟烷氧基,各自具有至多3个碳原子和3个氟原子,以及硝基和氰基,R2表示 任选被1或2个氧原子或硫原子间隔的碳原子数为12的直链,支链或环状烷基,任选被氟,氯,苯基,氰基,羟基,氨基,C 1 -C 3 - 烷基氨基, 二-C 1 -C 3 - 烷基氨基或N-苄基甲基氨基,R 3表示氰基或直链或支链烷基,其具有至多4个碳原子并且可选地被N-C 1 -C 3 - 烷基和/或氧中断, R4表示直链,支链或环状烷基,其具有多达6个碳原子,并且任选地被1或2个氧原子中断,并被氟,氯,羟基,苯基,氨基,羧基和C1中的一个或多个基团取代 -C 1-4 - 烷氧基羰基。