申请人:Korea Research Institute of Chemical Technology
公开号:US06011044A1
公开(公告)日:2000-01-04
The present invention relates to a novel pyrrolo[3,2-c]quinoline derivatives containing haloalkoxy group, represented by Formula I, their pharmaceutically acceptable salts; process for preparation thereof; and pharmaceutical composition thereof for treating gastric ulcer. ##STR1## in which R.sub.1 is haloalkoxy group of C.sub.1 -C.sub.6 including trifluoromethoxy, difluoromethoxy and trifluoroethoxy group. R.sub.2 and R.sub.3, which are the same or different, are each hydrogen, halogen, hydroxy, benzyloxy, alkyl group of C.sub.1 -C.sub.6, alkoxy group of C.sub.1 -C.sub.6. A is --CH.sub.2 --CH.sub.2 -- or --CH.dbd.CH--, and R.sub.4 is hydrogen, halogen, amino, alkylamino group of C.sub.1 -C.sub.6, and NH(CH.sub.2).sub.n OH in which n is 1-6. Pyrrolo[3,2-c]quinoline derivatives having haloalkoxy group, and their pharmaceutically acceptable salts, which reversibly inhibit gastric acid secretion of mammal, are usefully utilized for gastric ulcer therapeutics.
本发明涉及一种新的含有卤代烷氧基的吡咯并[3,2-c]喹啉衍生物,其化学式为I,其药学上可接受的盐;其制备方法;以及用于治疗胃溃疡的药物组成物。
在式中,R₁是C₁-C₆的卤代烷氧基,包括三氟甲氧基、二氟甲氧基和三氟乙氧基。R₂和R₃相同或不同,分别是氢、卤素、羟基、苄氧基、C₁-C₆的烷基、C₁-C₆的烷氧基。A是--CH₂--CH₂--或--CH=CH--,R₄是氢、卤素、氨基、C₁-C₆的烷基氨基,以及NH(CH₂)nOH,其中n为1-6。
具有卤代烷氧基的吡咯并[3,2-c]喹啉衍生物及其药学上可接受的盐,可逆地抑制哺乳动物的胃酸分泌,可用于治疗胃溃疡。