申请人:Merck & Co., Inc.
公开号:EP0020173A1
公开(公告)日:1980-12-10
Imidazole cyanoguanidines of formula
where
R1 is hydrogen or methyl;
R2 is lower alkyl; each of m and n independently of the other, is 0, 1, 2 or 3;
A is a phenylene, cyclohexylene, thienylene, tetrahydro- thienylene, or 1,3-dithianylene radical and is optionally substituted with a halogen;
Y is oxygen, sulfur, =NR3 or = CHR4 where R3 is hydrogen, cyano, lower alkyl, phenyl, lower alkylsulfonyl, or phenylsulfonyl; and
R4 is nitro, phenylsulfonyl, or lower alkylsulfonyl, and their pharmaceutically acceptable salts, are novel and are useful for the suppression of gastric acid secretion in mammals. Compositions for such uses containing the compounds are also disclosed. The compounds are made by introducing the of formula
group into an amine
式中的咪唑氰基胍
式中
R1 是氢或甲基
R2为低级烷基;m和n各自独立地为0、1、2或3;
A 是苯基、环己烯基、噻吩基、四氢噻吩基或 1,3-二噻吩基,可任选被卤素取代;
Y 是氧、硫、=NR3 或=CHR4,其中 R3 是氢、氰基、低级烷基、苯基、低级烷基磺酰基或苯基磺酰基;以及
R4 是硝基、苯磺酰基或低级烷基磺酰基,以及它们的药学上可接受的盐,都是新型的,可用于抑制哺乳动物的胃酸分泌。此外,还公开了含有这些化合物的此类用途的组合物。这些化合物是通过将式
基团引入胺