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    • 6. 发明授权
    • Circulation-active fluoromethoxyphenyl dihydropyridine compounds
    • 循环活性氟甲氧基苯基二氢吡啶化合物
    • US5008279A
    • 1991-04-16
    • US263671
    • 1988-10-27
    • Gerhard FranckowiakJurgen StoltefussMartin BechemRainer GrossMichael KayserSiegbert HebischMatthias Schramm
    • Gerhard FranckowiakJurgen StoltefussMartin BechemRainer GrossMichael KayserSiegbert HebischMatthias Schramm
    • A61K31/445A61K31/451A61P9/08C07D211/90C07D401/12
    • C07D401/12C07D211/90
    • Circulation-active fluoromethoxyphenyldihydropyridines of the formula ##STR1## in which X stands for hydrogen or fluorine andR stands for straight-chain, branched or cyclic alkyl or alkenyl having 2 to 12 carbon atoms which can be interrupted by 1 to 2 oxygen and/or sulphur atoms in the chain, and which can be monosubstituted or polysubstituted(a) by hydroxyl, aryl having 6 to 12 carbon atoms, aryloxy having 6 to 12 carbon atoms, where the aryl radical is again substituted by alkyl having up to 4 carbon atoms, alkoxy having up to 4 carbon atoms or halogen, the substituents being identical or different, or(b) by carboxyl, alkoxycarbonyl having up to 6 carbon atoms, pyridyl, piperidyl, pyrimidyl, acyloxy having up to 7 carbon atoms, sulphamoyl, carbamoyl, halogen or cyano, the substituents being identical or different, or(c) by an amino group, where the amino group can carry one or two identical or different substituents from the group consisting of alkyl having up to 6 carbon atoms, benzyl, phenyl or acyl having up to 7 carbon atoms,and salts thereof.
    • 式(I)的循环活性氟甲氧基苯基二氢吡啶,其中X代表氢或氟,R代表可被1至2个氧中断的具有2至12个碳原子的直链,支链或环状烷基或链烯基 和/或链中的硫原子,并且其可以被羟基,具有6至12个碳原子的芳基,具有6至12个碳原子的芳氧基单取代或多取代(a),其中芳基再次被具有至多 4个碳原子,具有至多4个碳原子的烷氧基或卤素,取代基相同或不同,或(b)由羧基,具有至多6个碳原子的烷氧基羰基,吡啶基,哌啶基,嘧啶基,具有至多7个碳原子的酰氧基, 氨基甲酰基,氨基甲酰基,卤素或氰基,取代基相同或不同,或(c)氨基,其中氨基可以带有一个或两个相同或不同的取代基,由至多6个碳原子的烷基 ms,苄基,苯基或具有至多7个碳原子的酰基及其盐。
    • 7. 发明授权
    • Benzylaminoaryl-dihydropyridinelactones and their use in medicaments
    • 苄基氨基芳基 - 二氢吡啶内酯及其在药物中的用途
    • US4904665A
    • 1990-02-27
    • US158184
    • 1988-02-18
    • Siegfried GoldmannRainer GrossMartin BechemMichael KayserMatthias SchrammSiegbert Hebisch
    • Siegfried GoldmannRainer GrossMartin BechemMichael KayserMatthias SchrammSiegbert Hebisch
    • A61K31/44A61P3/08A61P9/00A61P9/06A61P9/08A61P9/10C07D211/90C07D491/04C07D491/048
    • C07D491/04C07D211/90
    • A benzylaminoaryl-dihydropyridinelactone compound of the formula (I) ##STR1## in which R.sup.1 represents hydrogen, halogen, cyano, nitro, C.sub.6 -C.sub.12 -aryl, C.sub.1 -C.sub.8 -alkyl, C.sub.1 -C.sub.8 -alkoxy, C.sub.1 -C.sub.6 -alkylthio, trifluoromethyl, trifluoromethoxy, trifluoromethylthio, difluoromethoxy, di-C.sub.1 -C.sub.5 -alkylamino, C.sub.1 -C.sub.6 -alkoxycarboxyl or C.sub.1 -C.sub.6 -alkylsulphonyl,R.sup.2 represents hydrogen, or represents a straight-chain, branched or cyclic, saturated or unsaturated hydrocarbon radical having up to 10 carbon atoms which is optionally substituted by C.sub.1 -C.sub.6 -alkoxy, C.sub.1 -C.sub.6 -alkylthio, C.sub.1 -C.sub.6 -alkylsulphonyl, halogen, cyano, hydroxyl, pyridyl, thienyl, pyrimidyl, piperidinyl, phenyl or an amino group, where the amino group carries two identical or different substituents from the series comprising C.sub.1 -C.sub.5 -alkyl, phenyl or benzyl,R.sup.3 represents C.sub.1 -C.sub.5 -alkyl, or represents cyano, hydroxymethyl or formyl, andR.sup.4 represents hydrogen, halogen, C.sub.1 -C.sub.5 -alkyl or trifluoromethyl,and its isomers, isomeric mixtures, racemates or optical antipodes, and physiologically acceptable salts thereof. The compound being useful to improve the contractility of the heart and the tonus of the smooth muscles.
    • 式(I)的苄基氨基芳基 - 二氢吡啶内酯化合物其中R 1表示氢,卤素,氰基,硝基,C 6 -C 12 - 芳基,C 1 -C 8 - 烷基,C 1 -C 8 - 烷氧基,C 1 -C 6 - 烷硫基,三氟甲基,三氟甲氧基,三氟甲硫基,二氟甲氧基,二-C 1 -C 5烷基氨基,C 1 -C 6 - 烷氧基羧基或C 1 -C 6烷基磺酰基,R 2表示氢,或表示直链,支链或环状饱和或不饱和烃 具有至多10个碳原子的基团,其任选被C 1 -C 6 - 烷氧基,C 1 -C 6 - 烷硫基,C 1 -C 6 - 烷基磺酰基,卤素,氰基,羟基,吡啶基,噻吩基,嘧啶基,哌啶基,苯基或氨基取代, 其中氨基从包含C 1 -C 5 - 烷基,苯基或苄基的系列中携带两个相同或不同的取代基,R 3表示C 1 -C 5 - 烷基,或表示氰基,羟甲基或甲酰基,R 4表示氢,卤素,C 1 -C 5 - 烷基或三氟甲基,及其异构体,异构体混合物,外消旋体或光学抗体 es及其生理上可接受的盐。 该化合物可用于改善心脏和平滑肌紧张的收缩性。