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    • 13. 发明申请
    • NEW ARALKYL-1,4-DIHYDROPYRIDINES, A METHOD FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM
    • 新的ARALKYL-1,4-二氢吡啶类,其制备方法和含有它们的药物组合物
    • WO1988005043A1
    • 1988-07-14
    • PCT/EP1987000815
    • 1987-12-21
    • BOEHRINGER BIOCHEMIA ROBIN S.P.A.FRIGERIO, MarcoZALIANI, AndreaGANDOLFI, Carmelo, A.GERMINI, MauroTOFANETTI, OdoardoTOGNELLA, Sergio
    • BOEHRINGER BIOCHEMIA ROBIN S.P.A.
    • C07D211/90
    • C07D401/06C07D211/90C07D409/06
    • 1,4-Dihydropyridines of formula (I), wherein: X is a -CO2R1, cyano, nitro, -COCH3 group; R and R1, that can be the same or different, are a primary, secondary or tertiary, saturated or unsaturated, linear or branched C1-C6 alkyl group that can be substituted or not by one or more hydroxy, C1-C7-monoalkylamino, di-C1-C7-alkylamino, benzylamino, C1-C6-alkoxy, phenoxy groups optionally substituted by one or more C1-C6 alkyl, C1-C6 alkoxy, halo-C1-C6 alkyl, halo-C1-C6-alkoxy, halogen, nitro, cyano, C1-C6 alkoxycarbonyl, C1-C6 alkylthio, NHCOR5, SO2R6, C1-C4-alkylamino, di(C1-C4)alkylamino, hydroxy; R2 is hydrogen; R3 is hydrogen or a hydroxy, -OCOR5, OSO2R6, azide, amino, -NHPO(OR7)2, -NHCOR5 group, a C1-C4-alkoxy group or a fluorine, chlorine, bromine or iodine atom, a SH group, a SCOR6 or a C1-C6-alkylthio, phenylthio or benzylthio group; R4 is an optionally substituted aromatic or an optionally substituted 5- or 6-membered heteroaromatic group, containing one or more heteroatoms selected in the group of N,S,O, wherein the substituent is selected from one or more hydroxy, C1-C7-monoalkylamino, di-C1-C7-alkylamino, benzylamino, C1-C6-alkoxy, phenoxy groups optionally substituted by one or more C1-C6 alkyl, C1-C6 alkoxy, halo-C1-C6 alkyl, halo-C1-C6-alkoxy, halogen, nitro, cyano, C1-C6 alkoxycarbonyl, C1-C6 alkylthio, NHCOR5, SO2R6, C1-C4-alkylamino, di(C1-C4)alkylamino, hydroxy; Y is one or more substituents, that can be the same or different, selected in the group of C1-C4-alkoxy, halogen, nitro, cyano, C1-C6-alkoxycarbonyl, C1-C6-alkylthio, halo-C1-C6-alkyl, halo-C1-C6-alkoxy, NHCOR5 or NHSO2R6; R5 is hydrogen or a C1-C4-alkyl, thrihalomethyl, C1-C4-alkoxy or phenyl group, optionally substituted by one or more nitro, halogen, C1-C4-alkyl, C1-C4-alkoxy, amino groups; R6 is hydrogen or a C1-C4-alkyl, trihalomethyl, phenyl, or p-methylphenyl group; R7 is a C1-C4-alkyl group or a phenyl group, are useful as antihypertensive, cytoprotecting or anti-ulcer agents.