申请人:ICI Americas Inc.
公开号:US04165377A1
公开(公告)日:1979-08-21
The invention relates to guanidine derivatives of imidazoles and thiazoles which are histamine H-2 antagonists and which inhibit the secretion of gastric acid, to methods for their manufacture, to pharmaceutical compositions containing them and to methods of using such guanidine derivatives and compositions. The guanidine derivatives are of the general formula I: ##STR1## in which X is S or NH, Y is CH.sub.2, a direct bond or a vinylene radical, m is 0 to 4 and n is 1 to 4, R.sup.1 is hydrogen, halogen or alkyl, R.sup.2 is hydrogen, alkyl, alkanoyl or aroyl, A is a 3,4-dioxocyclobuten-1,2-diyl radical or C.dbd.Z in which Z is O, S, NCN, NNO.sub.2, CHNO.sub.2, NCONH.sub.2, C(CN).sub.2, NCOR.sup.3, NCO.sub.2 R.sup.3, NSO.sub.2 R.sup.3 or NR.sup.4 in which R.sup.3 is alkyl or aryl and R.sup.4 is hydrogen or alkyl, B is alkoxy or alkylthio or NR.sup.5 R.sup.6 in which R.sup.5 and R.sup.6 are independently hydrogen, alkyl, alkenyl, cycloalkyl, hydroxyalkyl, alkoxyalkyl, alkylaminoalkyl or dialkylaminoalkyl; and the salts thereof.
该发明涉及嘌呤和噻唑的胍衍生物,它们是组织胺H-2拮抗剂,可以抑制胃酸分泌,涉及它们的制备方法,含有它们的药物组合物,以及使用这种胍衍生物和组合物的方法。这些胍衍生物的一般化学式为I:在该式中,X为S或NH,Y为CH.sub.2,直接键或乙烯基基团,m为0至4,n为1至4,R.sup.1为氢、卤素或烷基,R.sup.2为氢、烷基、烷酰基或芳酰基,A为3,4-二氧代环丁-1,2-二基基团或C.dbd.Z,其中Z为O、S、NCN、NNO.sub.2、CHNO.sub.2、NCONH.sub.2、C(CN).sub.2、NCOR.sup.3、NCO.sub.2 R.sup.3、NSO.sub.2 R.sup.3或NR.sup.4,其中R.sup.3为烷基或芳基,R.sup.4为氢或烷基,B为烷氧基、烷硫基或NR.sup.5 R.sup.6,其中R.sup.5和R.sup.6独立地为氢、烷基、烯基、环烷基、羟基烷基、烷氧基烷基、烷基氨基烷基或二烷基氨基烷基;以及它们的盐。