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15 条记录 (耗时 0.015 秒)

    1,4-Dihydropyridine derivatives substituted in the 2 position, and their use as medicaments
    4.
    发明授权
    1,4-Dihydropyridine derivatives substituted in the 2 position, and their use as medicaments 失效

    公开(公告)号：US4188395A

    公开(公告)日：1980-02-12

    申请号：US856559

    申请日：1977-12-01

    申请人： Friedrich Bossert ,  Egbert Wehinger ,  Horst Meyer ,  Arend Heise ,  Stanislav Kazda ,  Kurt Stoepel ,  Robertson Towart ,  Wulf Vater ,  Klaus Schlossmann

    发明人： Friedrich Bossert ,  Egbert Wehinger ,  Horst Meyer ,  Arend Heise ,  Stanislav Kazda ,  Kurt Stoepel ,  Robertson Towart ,  Wulf Vater ,  Klaus Schlossmann

    IPC分类号： A61K31/4427 ,  A61K31/455 ,  A61P3/06 ,  A61P9/00 ,  A61P9/06 ,  A61P9/08 ,  A61P9/10 ,  A61P9/12 ,  C07D211/90 ,  C07D401/04 ,  C07D401/06 ,  C07D401/14 ,  C07D213/55 ,  A61K31/44

    CPC分类号： C07D401/04 ,  C07D211/90 ,  C07D401/14

    摘要： The present invention provides 1,4-dihydropyridine derivatives of the formula in which ##STR1## R represents hydrogen, alkyl, alkenyl, alkoxyalkyl, aryl or aralkyl, the alkyl and aryl groups being optionally substituted,A represents a straight-chain or branched alkylene radical,R.sup.1 represents (a) an optionally substituted alkylthio group or (b) a group of the formula O--CO-alkyl, O--CO-aryl or O--CO-aralkyl, the alkyl and aryl groups being optionally substituted or (c) a phthalimido radical which is optionally substituted in the benzene ring, Y and Z are identical or different and each represents a group of the formula COOR.sup.2 or COR.sup.2,whereinR.sup.2 represents alkyl, alkenyl, alkinyl, alkoxyalkyl, hydroxyalkyl, aminoalkyl, alkylaminoalkyl or aralkyl, the alkyl and aryl radicals being optionally substituted, orY and Z are identical or different and each represents a cyano radical or a radical of the formula S(O).sub.n --R.sup.3,whereinR.sup.3 represents alkyl, alkenyl, alkoxyalkyl, aminoalkyl, alkylaminoalkyl, aryl or aralkyl, the alkyl and aryl radicals mentioned being optionally substituted, and n represents 0, 1 or 2,R.sup.4 represents hydrogen or alkyl, the alkyl radical being optionally substituted or interrupted by oxygen, or represents the radical A--R.sup.1,whereinA and R.sup.1 have the abovementioned meaning, and X represents an aryl radical, which optionally contains one to three identical or different substituents selected from phenyl, alkyl, alkenyl, alkinyl, alkoxy, alkinoxy, acyloxy, halogen, trifluoromethyl, trifluoromethoxy, hydroxyl, nitro, cyano, azido, amino, alkylamino, acylamino, carbalkoxy, carboxamido, sulphonamide and S(O).sub.n -alkyl (n=0 to 2), or represents a quinolyl, pyridyl, pyrimidyl, thienyl, furyl or pyrryl radical which is optionally substituted by alkyl, alkylamino, nitro or halogen, or represents an optionally substituted aralkyl, cycloalkyl, cycloalkenyl or styryl radical, and acid addition salts thereof.Also included in the invention are methods for the preparation of the 1,4-dihydropyridine derivatives of the invention, compositions containing said derivatives and methods for their use.

    Benzodiazepine-diones, a process for their production and their use as medicaments
    7.
    发明授权
    Benzodiazepine-diones, a process for their production and their use as medicaments 失效
    苯二氮卓类药物，其生产过程及其用作药物

    公开(公告)号：US4187306A

    公开(公告)日：1980-02-05

    申请号：US922419

    申请日：1978-07-06

    申请人： Karl H. Mayer ,  Helmut Heitzer ,  Friedrich Hoffmeister ,  Arend Heise ,  Stanislav Kazda

    发明人： Karl H. Mayer ,  Helmut Heitzer ,  Friedrich Hoffmeister ,  Arend Heise ,  Stanislav Kazda

    IPC分类号： A61K31/55 ,  A61P25/04 ,  A61P25/20 ,  A61P25/28 ,  A61P29/00 ,  C07D239/91 ,  C07D487/04 ,  C07D471/04

    CPC分类号： C07D487/04 ,  C07D239/91 ,  Y10S514/916

    摘要： The invention covers compounds of the formula ##STR1## in which R.sup.1 and R.sup.5 each represents 0, 1, 2, 3 or 4 of the following substituents: alkyl, hydroxyl, acyloxy, alkoxy, nitro, amino, alkylamino, dialkylamino, acylamino, acylalkylamino, alkoxycarbonylamino, halogen, trifluoromethyl, cyano, carboxyl, alkoxycarbonyl, aminocarbonyl, alkylaminocarbonyl, dialkylaminocarbonyl, aminosulphonyl, alkylaminosulphonyl, dialkylaminoamino, R.sup.2 is hydrogen, optionally substituted alkyl, aralkyl or aryl or heterocyclo-alkyl, acyl or alkoxycarbonyl, and R.sup.3 and R.sup.4 are each hydrogen, or optionally substituted alkyl, aralkyl, aryl or hetero-aryl, are useful as medicaments which have an action on the central nervous system, in particular as, for example, tranquilizers and/or antiamnesics. Also included in the invention are methods for preparing said compounds, compositions containing them and methods for the use of said compounds and compositions.

    摘要翻译： 本发明涵盖下式的化合物，其中R 1和R 5各自表示0,1,2,3或4个以下取代基：烷基，羟基，酰氧基，烷氧基，硝基，氨基，烷基氨基，二烷基氨基，酰氨基，酰基烷基氨基 烷氧基羰基，氨基羰基，氨基磺酰基，烷基氨基磺酰基，二烷基氨基氨基，R2是氢，任意取代的烷基，芳烷基或芳基或杂环烷基，酰基或烷氧基羰基，R3和R4是 每个氢或任选取代的烷基，芳烷基，芳基或杂芳基可用作对中枢神经系统具有作用的药物，特别是例如镇定剂和/或抗病毒药物。 本发明还包括制备所述化合物的方法，含有它们的组合物和使用所述化合物和组合物的方法。