申请人:Behringwerke Aktiengesellschaft
公开号:US05091521A1
公开(公告)日:1992-02-25
Compounds of the general formula I ##STR1## in which R.sup.1 represents a hydrogen atom or an alkyl group of the formula CH.sub.3 (CH.sub.2).sub.n --where n=0 to 5, R.sup.2 represents a hydrogen atom when X is a carbamoyl group, an alkyl group having 1 to 6 carbon atoms, a group, bonded in an ether-like fashion, of the formula R.sup.3 --O--CH.sub.2 --(CHR.sup.4).sub.m --CH.sub.2 -- in which R.sup.3 is a hydrogen atom or an alkyl group having 1 to 6 carbon atoms, R.sup.4 is a hydroxyl group or an alkyloxy group having 1 to 3 carbon atoms, and m is 0 to 2, represents a group, bonded in an ether-like fashion, of the formula H--(CH.sub.2).sub.a --(O--(CH.sub.2).sub.b).sub.c -- where a=0 to 4, b=1 to 4 and c=1 to 7, or R.sup.2 represents a radical, bonded in a O-glycoside fashion of the formula ##STR2## in which R.sup.5, R.sup.6 and R.sup.7, independently of one another, are a hydrogen atom or a hydroxyl group, and R.sup.8 is a hydrogen atom, a methyl group or a hydroxy methyl group, X represents a methylene group or a carbamoyl group or a covalent bond between R.sup.1 and the 2-carbon atom, A.sup.1 and A.sup.2 are indentical and represent the hydroxyl group, chloride, bromide, iodide, nitrate, acetate or trifluoroacetate, or A.sup.1 represents sulfate or carbonate and A.sup.2 represents H.sub.2 O or A.sup.1 and A.sup.2 together represent the dianion of an organic acid such as oxalic, malonic, hydroxymalonic, ethylmalonic, 1,1- or 1,2-cyclobutanedicarboxylic, phthalic, 3- or 4-carboxyphthalic, 3,4-dicarboxyphthalic or N-(carbamoylmethyl)-iminodiacetic acid, are described, and also a process for the preparation thereof, and a medicament containg these compounds.
通式I的化合物##STR1##中,其中R.sup.1代表氢原子或具有CH.sub.3(CH.sub.2).sub.n的烷基基团--其中n=0至5,R.sup.2代表氢原子当X为羰胺基团时,具有1至6个碳原子的烷基基团,以醚类似方式键合的基团,其化学式为R.sup.3--O--CH.sub.2--(CHR.sup.4).sub.m--CH.sub.2--其中R.sup.3是氢原子或具有1至6个碳原子的烷基基团,R.sup.4是羟基或具有1至3个碳原子的烷氧基团,m为0至2,代表以醚类似方式键合的基团,其化学式为H--(CH.sub.2).sub.a--(O--(CH.sub.2).sub.b).sub.c--其中a=0至4,b=1至4,c=1至7,或R.sup.2代表以O-糖苷方式键合的基团,其化学式为##STR2##其中R.sup.5、R.sup.6和R.sup.7,彼此独立地,是氢原子或羟基,R.sup.8是氢原子、甲基基团或羟甲基基团,X代表亚甲基基团或羰胺基团或R.sup.1和第2碳原子之间的共价键,A.sup.1和A.sup.2相同,代表羟基、氯化物、溴化物、碘化物、硝酸盐、乙酸盐或三氟乙酸盐,或A.sup.1代表硫酸盐或碳酸盐,A.sup.2代表H.sub.2O或A.sup.1和A.sup.2一起代表有机酸的二阴离子,例如草酸、丙二酸、羟基丙二酸、乙基丙二酸、1,1-或1,2-环丁二羧酸、邻苯二甲酸、3-或4-羧基邻苯二甲酸、3,4-二羧基邻苯二甲酸或N-(羰胺甲基)-亚胺二乙酸,以及其制备方法和含有这些化合物的药物也被描述。