申请人:BEECHAM GROUP PLC
公开号:EP0178438A1
公开(公告)日:1986-04-23
Compounds of the formula 1, a salt, quaternized derivate or a solvate thereof:
wherein:
n represents 0 or 1;
X and Y are both C- or one of X and Y is N and the other is CH;
R1 either represents NR2R3, in which R2 and R3 independently represent a hydrogen atom or an alkyl, aryl, aralkyl, or acyl group, or N, R2 and R3 together form a saturated or unsaturated, substituted or unsubstituted ring, optionally containing one or more further hetero atoms; and
R', R5, (and R5 present when X and Y are both C-) each represent hydrogen or a substituent, or
R1 represents NR7R7 in which R2 represents a hydrogen atom or an alkyl, aryl, aralkyl, or acyl group, and R7 and one of R4, R5, (and R6 when present) on a carbon atom of the pyridine ring adjacent to that carrying R1 are linked to complete a saturated or unsaturated, substituted or unsubstituted ring optionally containing one or more further hetero atoms. and the others of R4, R5 (and R6 when present) each represent hydrogen or a substituent;
R8 represents a hydrogen atom, an alkyl group, or, when X is C and one of R4, R5 or R6 is a substituent, R8 completes a ring therewith;
R9 represents a hydrogen atom, or an alkanoyl, alkoxycarbonyl, aryloxycarbonyl, aralkyloxycarbonyl, aralkanoyl, aroyl, alkylsulphonyl, arylsulphonyl, aralkylsulphonyl, or aralkyl group; and
R10, R", R12 and R13 each independently represents hydrogen or a substituent having gastric secretion inhibition activity, a process for their preparation and their use as pharmaceuticals.
式 1 的化合物、其盐、季铵化衍生物或溶液:
其中
n 代表 0 或 1;
X和Y均为C-,或X和Y中的一个为N,另一个为CH;
R1 代表 NR2R3,其中 R2 和 R3 独立地代表氢原子或烷基、芳基、芳烷基或酰基,或 N、R2 和 R3 共同形成饱和或不饱和、取代或未取代的环,可选择含有一个或多个杂原子;以及
R'、R5(以及当 X 和 Y 均为 C- 时出现的 R5)各自代表氢或取代基,或
R1 代表 NR7R7,其中 R2 代表氢原子或烷基、芳基、芳烷基或酰基,R7 与吡啶环上与携带 R1 的碳原子相邻的一个碳原子上的 R4、R5 和 R6 中的一个相连,以完成一个饱和或不饱和、取代或未取代的环,该环可选择含有一个或多个杂原子。 而 R4、R5 和 R6 中的其它各代表氢或取代基;
R8 代表氢原子、烷基,或者当 X 为 C 且 R4、R5 或 R6 之一为取代基时,R8 与之组成一个环;
R9 代表氢原子,或烷酰基、烷氧羰基、芳氧羰基、烷氧羰基、芳烷酰基、芳基磺酰基、烷基磺酰基或芳烷基;以及
R10、R"、R12 和 R13 各自独立地代表氢或具有胃分泌抑制活性的取代基、其制备方法和作为药物的用途。