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    1,4-Dihydropyridine derivatives substituted in the 2 position, and their use as medicaments
    6.
    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.

    1,4-Dihydropyridines
    8.
    发明授权
    1,4-Dihydropyridines 失效
    1,4-二氢吡啶类

    公开(公告)号：US4044141A

    公开(公告)日：1977-08-23

    申请号：US654278

    申请日：1976-02-02

    申请人： Friedrich Bossert ,  Egbert Wehinger ,  Kurt Stoepel ,  Wulf Vater ,  Stanislav Kazda

    发明人： Friedrich Bossert ,  Egbert Wehinger ,  Kurt Stoepel ,  Wulf Vater ,  Stanislav Kazda

    IPC分类号： C07D211/02 ,  A61K31/4427 ,  A61K31/455 ,  A61P9/08 ,  A61P9/12 ,  C07D211/90 ,  C07D401/04 ,  C07D213/55

    CPC分类号： C07D401/04 ,  C07D211/90 ,  Y10S514/929

    摘要： 1,4-Dihydropyridines characterized by a carbo(arylalkoxy) group in the 5-position, an aryl group in the 4-position and a alkanoyl or carbalkoxy group in the 3-position and further optionally substituted in the 1,2 and 6-positions are coronary dilating, spasmolytic and hypotensive agents. The compounds, of which 2,6-dimethyl-3-carbomethoxy-4-(2-nitrophenyl)-5-carbobenzoxy-1,4-dihydropyridine is a representative embodiment, are prepared through the reaction of an ylidene-.beta.-dicarbonyl compound, which may be generated in situ from the corresponding .beta.-dicarbonyl compound and an aldehyde, and an enaminocarboxylic acid ester, which may also be generated in situ from a .beta.-dicarbonyl compound and an amine.

    摘要翻译： 其特征在于5-位上的碳（芳基烷氧基）基团，4-位上的芳基和3-位的烷酰基或烷氧基，并且进一步任选被1,2和6-位取代的1,4-二氢吡啶， 位置是冠状动脉扩张，解痉和降血压药。 其中2,6-二甲基-3-甲酯基-4-（2-硝基苯基）-5-苄氧羰基-1,4-二氢吡啶的代表性实例是通过亚基-β-二羰基 化合物，其可以由相应的β-二羰基化合物和醛和烯氨基羧酸酯原位产生，其也可以由β-二羰基化合物和胺原位产生。