申请人:G.D. Searle & Co.
公开号:EP0417760A2
公开(公告)日:1991-03-20
This invention relates to substituted imidazopyridine dervatives having the following formula
and isomers thereof;
or a pharmaceutically acceptable acid addition salt thereof: wherein
R₁ and R₂ are each independently selected from hydrogen; straight or branched chain alkyl of 1 to 15 carbon atoms; cycloalkyl of 3 to 8 carbon atoms; substituted cycloalkyl which can be substituted one or more by alkyl of 1 to 6 carbon atoms; phenyl;
substituted phenyl which can be substituted one or more by alkyl of 1 to 6 carbon atoms or halogen; straight or branched alkenyl having 3 to 15 carbon atoms.
y is phenyl or phenyl substituted once or more than by alkyl of 1 to 6 carbon atoms; alkoxy wherein the alkyl is 1 to 6 carbon atoms; and halogen selected from the group consisting of bromo, fiuoro or chloro.
m is an integer from 0 to 5.
n is an integer from 1 to 5.
R₃ is a group substituted at one or more of the 4, 6 or 7 positions of the pyridine ring said groups being independently selected from hydrogen, alkyl of 1 to 6 carbon atoms; halogen wherein the halogen is selected from bromo, fluoro, or chloro;
or alkoxy wherein the alkyl is 1 to 6 carbon atoms;
R₄ is hydrogen or alkyl of 1 to 4 carbon atoms.
useful in the treatment of diseases or disorders mediated by platelet-activating factor. This invention also relates to pharmaceutical compositions of such substituted imidazopyridines.
本发明涉及具有下式的取代咪唑吡啶防腐剂及其异构体
及其异构体;
或其药学上可接受的酸加成盐: 其中
R₁和R₂各自独立地选自氢;1-15 个碳原子的直链或支链烷基;3-8 个碳原子的环烷基;可被 1-6 个碳原子的烷基取代一个或多个的取代环烷基;苯基;
可被 1 至 6 个碳原子的烷基或卤素取代一个或多个的取代苯基; 具有 3 至 15 个碳原子的直链或支链烯基。
y 是苯基或被 1 至 6 个碳原子的烷基取代一次或多次的苯基;烷氧基,其中烷基为 1 至 6 个碳原子;以及选自溴、氟或氯组成的组的卤素。
m 是 0 至 5 的整数。
n 是 1 至 5 的整数。
R₃ 是在吡啶环的一个或多个 4、6 或 7 位上被取代的基团,所述基团独立选自氢、1 至 6 个碳原子的烷基、卤素(其中卤素选自溴、氟或氯)或烷氧基(其中烷基选自烷氧基);
或烷氧基,其中烷基为 1 至 6 个碳原子;
R₄ 是氢或 1 至 4 个碳原子的烷基。
血小板活化因子是治疗由血小板活化因子介导的疾病或紊乱的有效药物。本发明还涉及此类取代咪唑吡啶的药物组合物。