申请人:Bristol-Myers Company
公开号:US04200760A1
公开(公告)日:1980-04-29
Compounds of the formula ##STR1## wherein R.sup.1 is a straight or branched chain alkynyl group containing from 3 to 9 carbon atoms, inclusive; R.sup.2 is hydrogen, (lower)alkyl, halogen or hydroxymethyl; m is 1 or 2, and n is 2 or 3, provided that the sum of m and n is 3 or 4; X and Y each are independently hydrogen, nitro, cyano, --SO.sub.2 Ar or --COR.sup.3, provided that X and Y are not both hydrogen; R.sup.3 is (lower)alkyl, Ar, (lower)alkoxy, amino or (lower)-alkylamino; and Ar is an optionally substituted phenyl group; and nontoxic pharmaceutically acceptable acid addition salts thereof, are potent anti-ulcer agents. Processes for their preparation and novel intermediates are also disclosed.
该公式化合物为 ##STR1## 其中 R.sup.1 是含有3到9个碳原子的直链或支链炔基团;R.sup.2 是氢、(较低)烷基、卤素或羟甲基;m 为1或2,n 为2或3,但要求m和n的总和为3或4;X和Y各自独立地是氢、硝基、氰基、--SO.sub.2 Ar或--COR.sup.3,但要求X和Y不能都是氢;R.sup.3 是(较低)烷基、Ar、(较低)烷氧基、氨基或(较低)烷基氨基;Ar 是可选择取代的苯基团;以及其对应的无毒药用可接受酸盐是有效的抗溃疡剂。还公开了它们的制备方法和新颖中间体。