申请人:G.D. Searle & Co.
公开号:EP0344414A1
公开(公告)日:1989-12-06
This invention relates to novel substituted imidazopyridine dervatives having the following formula
or a pharmaceuticaly acceptable acid addition salt: wherein
R₁ and R₂ are each independently selected from hydrogen; straight or branched chain alkyl of 1 to 15 carbon atoms; cycloalkyl having 3 to 8 carbon atoms; substituted cycloalkyl which can be substituted one or more by alkyl of 1 to 6 carbon atoms; bicycloalkyl having 3 to 8 carbon atoms in each ring; heterocyclicalkyl having 4 to 8 carbon atoms which can be optionally substituted by alkyl of 1 to 6 carbon atoms; heteroaromatic having 5 or 6 carbon atoms which can be optionally substituted by alkyl of 1 to 6 carbon atoms; phenyl; substituted phenyl which can be substituted one or more by a group independently selected from alkyl of 1 to 6 carbon atoms or halogen; straight or branched alkenyl having 3 to 15 carbon atoms with the proviso that the double bond of the alkenyl group cannot be adjacent to the nitrogen; cycloalkenyl having 5 to 8 carbon atoms with the proviso that the double bond cannot be adjacent to the nitrogen; R₁ and R₂ cannot both be hydrogen
Y is phenyl or phenyl substituted once or more than at one or more of the 2, 3, 5 or 6 position of the phenyl ring by substituents independently selected from the group consisting of alkoxy wherein the alkyl is 1 to 6 carbon atoms; halogen wherein the halogen is selected from bromo, fluoro, or chloro; straight or brnached chain alkyl having 1 to 6 carbon atoms; substituted straight or branched chain alkyl which can be substituted one or more by halogen; thioalkyl wherein the alkyl is 1 to 6 carbon atoms; alkoxyalkyl wherein the alkyl groups are each 1 to 6 carbon atoms; hydroxyalkyl wherein the alkyl is 1 to 6 carbon atoms; alkylthioalkyl wherein the alkyl group are each 1 to 6 carbon atoms; cyano; mercaptoalkyl wherein the alkyl is 1 to 6 carbon atoms; hydroxy; amino; alkylamino wherein the alkyl group are each 1 to 6 carbon atoms; and dialkylamino wherein the alkyl group are each 1 to 6 carbon atoms.
n is an integer of 1 to 5.
R₃ is a group substituted at one or more of the 4, 6, or 7 positions of the pyridine ring said group being independently selected from hydrogen; alkyl of 1 to 6 carbon atoms; halogen wherein the halogen is selected from bromo, fluoro or chloro; alkoxy wherein the alkyl is 1 to 6 carbon atoms.
R₄ is hydrogen or alkyl of 1 to 6 carbon atoms.
useful in the treatment of diseases or disorders mediated by platelet-activating factor. This invention relates to pharmaceutical compositions of such substituted imidazopyridines.
本发明涉及具有下式的新型取代咪唑吡啶防腐剂
或药物可接受的酸加成盐: 其中
R₁和 R₂各自独立地选自氢;1 至 15 个碳原子的直链或支链烷基;3 至 8 个碳原子的环烷基;可被 1 至 6 个碳原子的烷基取代一个或多个的取代环烷基;每个环中有 3 至 8 个碳原子的双环烷基;4 至 8 个碳原子的杂环烷基,可任选被 1 至 6 个碳原子的烷基取代;5 或 6 个碳原子的杂芳基,可任选被 1 至 6 个碳原子的烷基取代;苯基;可被一个或多个独立选自 1 至 6 个碳原子的烷基或卤素的基团取代的取代苯基;具有 3 至 15 个碳原子的直链或支链烯基,但烯基的双键不能与氮相邻;具有 5 至 8 个碳原子的环烯基,但双键不能与氮相邻;R₁ 和 R₂ 不能都是氢。
Y 是苯基或在苯基环的 2、3、5 或 6 位上被取代基取代一次或多次的苯基,取代基 独立选自由以下组成的基团:烷氧基(其中烷基为 1-6 个碳原子);卤素(其中卤素选 自溴、氟或氯);具有 1-6 个碳原子的直链或支链烷基;可被卤素取代一次或多次的取代 直链或支链烷基;硫代烷基,其中烷基为 1 至 6 个碳原子;烷氧基烷基,其中烷基各为 1 至 6 个碳原子;羟基烷基,其中烷基为 1 至 6 个碳原子;烷硫基烷基,其中烷基各为 1 至 6 个碳原子;氰基;巯基烷基,其中烷基为 1 至 6 个碳原子;羟基;氨基;烷基氨基,其中烷基各为 1 至 6 个碳原子;以及二烷基氨基,其中烷基各为 1 至 6 个碳原子。
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;烷氧基,其中烷基为 1 至 6 个碳原子。
R₄ 是氢或 1-6 个碳原子的烷基。
用于治疗由血小板活化因子介导的疾病或失调。本发明涉及此类取代咪唑吡啶的药物组合物。