Heteroaryl 4-amino-3-acylquinoline derivatives and their use as inhibitors of gastric secretion
申请人:SMITHKLINE BEECHAM INTERCREDIT B.V.
公开号:EP0336544A1
公开(公告)日:1989-10-11
Compounds of structure (I)
in which R¹ is hydrogen, C₁₋₆alkyl, C₁₋₆alkoxy, C₁₋₆alkoxylC₁₋₆alkyl, C₃₋₆cycloalkyl, C₃₋₆cycloalkylC₁₋₆alkyl, phenyl or phenylC₁₋₆alkyl, the phenyl groups being optionally substituted; R² is hydrogen, C₁₋₆alkyl, C₁₋₆alkoxy, CO₂H or CO₂C₁₋₆alkyl; m is 1, 2 or 3; p is 0 to 4; R³ is hydrogen, C₁₋₆alkyl, phenyl, C₁₋₆alkoxy, C₁₋₆alkylthio, C₁₋₆alkanoyl, amino, C₁₋₆alkylamino, di-C₁₋₆alkylamino, halogen, trifluoromethyl or cyano; n is 1 or 2; and X is S, O, NH or NC₁₋₄alkyl; processes for their preparation, intermediates used in their preparation, pharmaceutical compositions containing them and their use in therapy as anti-ulcer agents.
结构(I)的化合物
其中 R¹ 是氢、C₁₋₆烷基、C₁₋₆烷氧基、C₁₋₆烷基、C₃₋₆环烷基、C₃₋₆环烷基、C₁₋₆烷基、苯基或苯基,苯基基团任选被取代;R² 是氢、C₁₋₆烷基、C₁₋₆烷氧基、CO₂H 或 CO₂C₁₋₆烷基;m 是 1、2 或 3;p 是 0 至 4;R³ 是氢、C₁₋₆烷基、苯基、C₁₋₆烷氧基、C₁₋₆烷硫基、C₁₋₆烷酰基、氨基、C₁₋₆烷氨基、二₁₋₆烷氨基、卤素、三氟甲基或氰基;n 是 1 或 2;X为S、O、NH或NC₁₋₄烷基;其制备方法、制备过程中使用的中间体、含有它们的药物组合物以及它们在治疗中作为抗溃疡剂的用途。