申请人:Yamanouchi Pharmaceutical Co., Ltd.
公开号:US04163844A1
公开(公告)日:1979-08-07
Novel nitrogen-containing heterocyclic compounds shown by the formula ##STR1## wherein Y represents an oxygen atom, a sulfur atom, or a group shown by ##STR2## (wherein m is 1 or 2); n represents 0 or 1; R.sub.1 and R.sub.4, which may be the same or different, each represents a hydrogen atom, a lower alkyl group, or a lower alkenyl group; R.sub.2 and R.sub.3, which may be the same or different, each represents a hydrogen atom, a hydroxyl group, a lower alkanoyloxy group, a lower alkyl group or a lower alkenyl group; said R.sub.2 and R.sub.3 may further form together a double bond; R.sub.5 and R.sub.6, which may be the same or different, each represents a hydrogen atom, a halogen atom, a hydroxyl group, a nitro group, an amino group, a lower alkoxy group, a mono or di lower alkylamino group, or a lower alkyl group; said R.sub.5 and R.sub.6 may further form together a lower alkylenedioxy group; and R.sub.7 represents a hydrogen atom, a halogen atom, a lower alkanoyl group, a phenyl group, a phenyl lower alkyl group, a lower alkyl group, a hydroxy lower alkyl group, a di lower alkylamino lower alkyl group, a pyrrolidino lower alkyl group, a piperidino lower alkyl group, a morpholino lower alkyl group, or a 4-lower alkylpiperazino lower alkyl group; (1) when said R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6 and R.sub.7 are hydrogen atom and n is 0, said Y is a group shown by ##STR3## and (2) when said R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.7 are hydrogen atom, at least one of said R.sub.5 and R.sub.6 is the aforesaid group other than hydrogen atom, and n is 0, said Y is oxygen atom or a group shown by ##STR4## and the pharmacologically acceptable non-toxic salts thereof. The compounds are strong analgesic anti-inflammatory agents.
根据以下公式显示的新型含氮杂环化合物:其中Y代表氧原子、硫原子或由##STR2##所示的基团(其中m为1或2);n代表0或1;R.sub.1和R.sub.4,可以相同也可以不同,分别代表氢原子、低烷基基团或低烯基基团;R.sub.2和R.sub.3,可以相同也可以不同,分别代表氢原子、羟基基团、低烷酰氧基团、低烷基基团或低烯基基团;所述的R.sub.2和R.sub.3还可以一起形成双键;R.sub.5和R.sub.6,可以相同也可以不同,分别代表氢原子、卤素原子、羟基基团、硝基基团、氨基基团、低烷氧基团、单或双低烷基氨基基团或低烷基基团;所述的R.sub.5和R.sub.6还可以一起形成低烷基二氧基基团;R.sub.7代表氢原子、卤素原子、低烷酰基团、苯基团、苯基低烷基基团、低烷基基团、羟基低烷基基团、双低烷基氨基低烷基基团、吡咯啉基低烷基基团、哌啶基低烷基基团、吗啉基低烷基基团或4-低烷基哌嗪基低烷基基团;(1)当所述的R.sub.1、R.sub.2、R.sub.3、R.sub.4、R.sub.5、R.sub.6和R.sub.7为氢原子且n为0时,所述的Y是由##STR3##所示的基团;(2)当所述的R.sub.1、R.sub.2、R.sub.3、R.sub.4和R.sub.7为氢原子,至少其中一个所述的R.sub.5和R.sub.6是上述的非氢原子基团,且n为0时,所述的Y是氧原子或由##STR4##所示的基团,以及其药理学上可接受的无毒盐。这些化合物是强效止痛抗炎剂。