申请人:Allen & Hanburys Limited
公开号:US04128658A1
公开(公告)日:1978-12-05
Compounds of the general formula I: ##STR1## and physiologically acceptable salts thereof and N-oxides and hydrates, in which R.sub.1 and R.sub.2 which may be the same or different represent hydrogen, lower alkyl, cycloalkyl, lower alkenyl, aralkyl or lower alkyl interrupted by an oxygen atom or a group ##STR2## in which R.sub.4 represents hydrogen or lower alkyl or R.sub.1 and R.sub.2 may, together with the nitrogen atom to which they are attached, form a heterocyclic ring which may contain other heteroatoms selected from O and ##STR3## R.sub.3 is hydrogen, lower alkyl, lower alkenyl or alkoxyalkyl; X is --CH.sub.2 --, O or S; Y represents .dbd. S, .dbd. O, .dbd. NR.sub.5 or .dbd. CHR.sub.6 ; Alk denotes a straight or branched alkylene chain of 1 to 6 carbon atoms; R.sub.5 is H, nitro, cyano, lower alkyl, aryl, alkylsulphonyl, or arylsulphonyl; R.sub.6 represents nitro, arylsulphonyl or alkylsulphonyl; M is an integer from 2 to 4; and N is 1 or 2; or when X .dbd. S, or --CH.sub.2 --, n is zero, 1 or 2. These compounds have H.sub.2 -antagonist activity. Intermediates in the production thereof are also provided.
通式I的化合物:##STR1##及其生理上可接受的盐和N-氧化物和水合物,其中R.sub.1和R.sub.2可以相同也可以不同,代表氢、较低的烷基、环烷基、较低的烯基、芳基烷基或被氧原子或基团##STR2##中断的较低烷基,其中R.sub.4代表氢或较低烷基或R.sub.1和R.sub.2可以与它们连接的氮原子一起形成可能包含其他杂原子O和##STR3##的杂环环,R.sub.3是氢、较低烷基、较低烯基或烷氧基烷基;X是--CH.sub.2--、O或S;Y代表.dbd. S、.dbd. O、.dbd. NR.sub.5或.dbd. CHR.sub.6;Alk表示由1到6个碳原子的直链或支链烷基链;R.sub.5是H、硝基、氰基、较低烷基、芳基、烷基磺酰基或芳基磺酰基;R.sub.6代表硝基、芳基磺酰基或烷基磺酰基;M是从2到4的整数;N是1或2;或当X.dbd.S或--CH.sub.2--时,n为零、1或2。这些化合物具有H.sub.2-拮抗活性。还提供了其生产中间体。