Imidazopyridine derivatives, their production, and pharmaceutical compositions containing them
申请人:YAMANOUCHI PHARMACEUTICAL CO. LTD.
公开号:EP0266890A1
公开(公告)日:1988-05-11
The present invention relates to imidazo-pyridine derivatives of formula (I) below(and pharmaceutically acceptable salts thereof) which possess H+, K+-adenosine triphosphatase inhibition activity and are useful as prophylactic and treating agents for gastric diseases; to pharmaceutical compositions containing them; and to processes for production thereof
wherein:
R' represents an alkenyl group having 4 to 6 carbon atoms,or an alkyl group having 1 to 10 carbon atoms which may have a cycloalkyl group substituent;
R2 represents a hydroxy group, a lower alkoxycarbonyl group, a lower alkyl group which may have a hydroxy, lower alkoxy, or lower alkoxycarbonyl group substituent, a phenyl group which may have a lower alkoxy group substituent or a lower acyloxyalkyl group which may have a lower acyloxy group substituent; and,
R3 represents a hydrogen atom, a lower alkyl group, a halogeno-Iower alkyl group, a lower alkoxyalkyl group, a hydroxy-lower alkyl group, a cyano-lower alkyl group, a mono-or di-lower alkylamino-lower alkyl group, an amino group, a mono-or di-lower alkylamino group, a nitroso group, a lower alkoxy-carbonyl group, a lower acylamino group, a lower alkylsulfonylamino group, a group of formula:
(wherein D is NH or S, E is N or CH,and R5 and R6 are the same or different and selected from a hydrogen atom and lower alkyl, lower alkoxycarbonyl and phenyl groups); a group of formula:
(wherein X is O, S or N-R7 wherein R7 is a sulfamoyl group, a lower acylamino group or a lower alkynyl group); or a group of formula:
(wherein Y is O or S and R8 is a cyano-lower alkyl group or a lower alkynyl group).
本发明涉及下式(I)所示的咪唑吡啶衍生物(及其药学上可接受的盐),其具有H+,K+-腺苷三磷酸酶抑制活性,并可用作胃病的预防和治疗剂;含有它们的药物组合物;以及生产它们的方法,其中:R'代表具有4至6个碳原子的烯基基团,或具有1至10个碳原子的烷基基团,可能具有环烷基基团取代基;R2代表羟基、较低的烷氧羰基基团、较低的烷基基团,可能具有羟基、较低的烷氧基或较低的烷氧羰基取代基,可能具有较低的烷氧基取代基或较低的酰氧基烷基基团的苯基,可能具有较低的酰氧基取代基;R3代表氢原子、较低的烷基基团、卤代较低的烷基基团、较低的烷氧基烷基基团、羟基较低的烷基基团、氰基较低的烷基基团、一或二较低的烷基氨基较低的烷基基团、氨基、一或二较低的烷基氨基基团、亚硝基基团、较低的烷氧基羰基基团、较低的酰氨基基团、较低的烷基磺酰氨基基团,下式的基团:(其中D为NH或S,E为N或CH,R5和R6相同或不同,选择自氢原子和较低的烷基、较低的烷氧羰基和苯基);下式的基团:(其中X为O、S或N-R7,其中R7为磺酰氨基基团、较低的酰氨基基团或较低的炔基基团);或下式的基团:(其中Y为O或S,R8为氰基较低的烷基基团或较低的炔基基团)。