申请人:Pfizer Inc.
公开号:US04075343A1
公开(公告)日:1978-02-21
A novel series of 5-alkoxyimidazo[1,2-a]quinoline-2-carboxylic acids and esters thereof of the formula (I) ##STR1## wherein R is hydrogen or alkyl having from one to five carbon atoms; each of R.sup.1 and R.sup.2 is hydrogen, alkyl having from one to five carbon atoms, alkoxy having from one to five carbon atoms, fluoro, chloro, bromo, methylthio or methylsulfinyl, with the proviso that when R.sup.1 and R.sup.2 are both bulky groups, i.e. branched chain alkyl or branched chain alkoxy, they are located on non-adjacent positions; and when R.sup.1 and R.sup.2 are taken together they form tetramethylene, 1,3-butadienyl, methylenedioxy or ethylenedioxy, each said group being attached to adjacent carbon atoms of the benzenoid ring; R.sup.3 is alkyl having from one to five carbon atoms; and the pharmaceutically acceptable cationic salts of those compounds wherein R is hydrogen; compositions thereof; their use as antiallergy agents and certain intermediates for the preparation of said compounds of formula (I).
一系列的5-烷氧基咪唑并[1,2-a]喹啉-2-羧酸及其酯类,其化学式为(I) ##STR1## 其中,R为氢或具有1-5个碳原子的烷基;R.sup.1和R.sup.2中的每个都是氢、具有1-5个碳原子的烷基、具有1-5个碳原子的烷氧基、氟、氯、溴、甲硫基或甲基磺酰基,但是当R.sup.1和R.sup.2均为臃肿基,即支链烷基或支链烷氧基时,它们位于非相邻的位置;当R.sup.1和R.sup.2结合在一起时,它们形成四亚甲基、1,3-丁二烯基、亚甲基二氧基或乙基二氧基,每个所述基固定于苯环上相邻的碳原子上;R.sup.3为具有1-5个碳原子的烷基;以及其中R为氢的药学上可接受的阳离子盐;它们的组成物;它们作为抗过敏剂的用途以及制备上述化合物(I)的某些中间体。