申请人:Elf Sanofi
公开号:US05268375A1
公开(公告)日:1993-12-07
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; or R.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.
本发明涉及公式##STR1##的化合物,其中:R.sub.1和R.sub.2相似或不同,且各自独立地为氢或从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或氮杂环中选择的基团;但须满足R.sub.1或R.sub.2中至少有一个基团不是氢;R.sub.3为氢、C.sub.1-C.sub.6烷基、C.sub.2-C.sub.6烯基、C.sub.3-C.sub.7环烷基、苯基、苯基烷基或苯基烯基;R.sub.4和R.sub.5各自独立地为C.sub.1-C.sub.6烷基、C.sub.3-C.sub.7环烷基、苯基或苯基烷基;或R.sub.4和R.sub.5结合在一起,形成公式(CH.sub.2).sub.n或公式(CH.sub.2).sub.p Y (CH.sub.2).sub.q的基团,其中Y为氧原子、硫原子、取代碳原子或基团N-R.sub.6,其中R.sub.6为氢、C.sub.1-C.sub.4烷基、苯基烷基、C.sub.1-C.sub.4烷基羰基、C.sub.1-C.sub.4卤代烷基羰基、C.sub.1-C.sub.4多卤代烷基羰基、苯并环、α-氨基酰基或N-保护基;或R.sub.4和R.sub.5与它们结合的碳原子一起形成茚环或金刚烷;p+q=m;n为2到11之间的整数;m为2到5之间的整数;X为氧原子或硫原子;z和t为零或z+t=1;以及其盐。