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    • 10. 发明授权
    • Dinitrogen heterocyclic derivatives N-substituted by a biphenylmethyl
group, and the pharmaceutical compositions in which they are present
    • 通过联苯甲基N-取代的二氮杂环衍生物及其存在的药物组合物
    • US5268375A
    • 1993-12-07
    • US843239
    • 1992-02-28
    • Claude BernhartBernard FerrariPierre Perreaut
    • Claude BernhartBernard FerrariPierre Perreaut
    • A61K31/505A61P9/00A61P9/12A61P27/02A61P43/00C07D233/70C07D235/02C07D239/22C07D239/70C07D403/10C07D413/10C07D417/10C07D233/36A61K31/415C07D239/36
    • C07D235/02C07D239/22C07D239/70C07D403/10C07D413/10C07D417/10Y02P20/55
    • This invention relates to compounds of formula ##STR1## in which: R.sub.1 and R.sub.2 are similar or different and are each independently hydrogen or a group selected from CO.sub.2 N.dbd.C(NH.sub.2).sub.2, CONHNHCONH.sub.2, CONHNHCSNH.sub.2, C(OC.sub.2 H.sub.5).dbd.NCO.sub.2 CH.sub.3, COCH.sub.2 CO.sub.2 H.sub.5, N(OH)-CONHCOOC.sub.2 NCO.sub.2 CH.sub.3, COCH.sub.2 CO.sub.2 H.sub.5, N(OH)-CONHCOOC.sub.2 H.sub.5, C(OC.sub.2 H.sub.5).dbd.NH or a nitrogen heterocycle; with the proviso that at least one of the substituents R.sub.1 or R.sub.2 is other than hydrogen;R.sub.3 is a hydrogen, a C.sub.1 -C.sub.6 alkyl, a C.sub.2 -C.sub.6 alkenyl, a C.sub.3 -C.sub.7 cycloalkyl, a phenyl, a phenylalkyl, or a phenylalkenyl;R.sub.4 and R.sub.5 are each independently a C.sub.1 -C.sub.6 alkyl, a C.sub.3 -C.sub.7 cycloalkyl, a phenyl or a phenylalkyl; orR.sub.4 and R.sub.5, bonded together, are either a group of the formula (CH.sub.2).sub.n or a group of the formula (CH.sub.2).sub.p Y (CH.sub.2).sub.q, in which Y is either an oxygen atom, or a sulfur atom, or a substituted carbon atom, or a group N-R.sub.6, in which R.sub.6 is a hydrogen, a C.sub.1 -C.sub.4 alkyl, a phenylalkyl, a C.sub.1 -C.sub.4 alkylcarbonyl, a C.sub.1 -C.sub.4 halogenoalkylcarbonyl, a C.sub.1 -C.sub.4 polyhalogenoalkylcarbonyl, a benzolyl, an .alpha.-aminoacyl or a N-protecting group, or R.sub.4 and R.sub.5, together with the carbon atom to which they are bonded, form an indane or an adamantine; p+q=m; n is an integer between 2 and 11; m is an integer between 2 and 5; X is an oxygen or a sulfur atom; and z and t are zero or z+t=1; and its salts.
    • 本发明涉及式(I)的化合物,其中:R 1和R 2相同或不同,各自独立地为氢或选自CO 2 N = C(NH 2)2,CONHNHCONH 2,CONHNHCSNH 2,C(OC 2 H 5)= NCO2CH3,COCH2CO2H5,N(OH)-CONHCOOC2NCO2CH3,COCH2CO2H5,N(OH)-CONHCOOC2H5,C(OC2H5)= NH或氮杂环; 条件是至少一个取代基R 1或R 2不是氢; R 3是氢,C 1 -C 6烷基,C 2 -C 6烯基,C 3 -C 7环烷基,苯基,苯基烷基或苯基烯基; R 4和R 5各自独立地为C 1 -C 6烷基,C 3 -C 7环烷基,苯基或苯基烷基; 或者R 4和R 5键合在一起,是式(CH 2)n的基团或式(CH 2)p Y(CH 2)q的基团,其中Y是氧原子或硫原子,或 取代的碳原子或基团N-R6,其中R6是氢,C1-C4烷基,苯基烷基,C1-C4烷基羰基,C1-C4卤代烷基羰基,C1-C4多卤代烷基羰基,苯甲酰基, α-氨基酰基或N-保护基,或R 4和R 5与它们所键合的碳原子一起形成二氢化茚或金刚烷; p + q = m; n是2和11之间的整数; m是2和5之间的整数; X是氧或硫原子; z和t为零或z + t = 1; 及其盐。