申请人:American Home Products Corporation
公开号:US05218124A1
公开(公告)日:1993-06-08
There are disclosed compounds of the formula A(CH.sub.2).sub.n O--B wherein A is a group having the formula ##STR1## wherein X is --N-- or ##STR2## Z is ##STR3## R.sup.1 is hydrogen, lower alkyl or phenyl; R.sup.2 is hydrogen or lower alkyl; or R.sup.1 and R.sup.2 taken together form a benzene ring, with the proviso that when X is --N--, Z is other than ##STR4## R.sup.3 is hydrogen or lower alkyl; n is 1-2; B is ##STR5## wherein Y is OR.sup.5 or N(OH)R.sup.8 ; R.sup.4 and R.sup.5 are each, independently, hydrogen or lower alkyl; R.sup.6 is hydrogen, halo or nitro; R.sup.7 is ##STR6## R.sup.8 is lower alkyl; m is 0-3; and the pharmacologically acceptable salts thereof, and their use in the treatment of inflammatory conditions, such as rheumatoid arthritis, ulcerative colitis, psoriasis and other immediate hypersensitivity reactions; in the treatment of leukotriene-mediated naso-bronchial obstructive air-passageway conditions, such as allergic rhinitis, allergic bronchial asthma and the like; and as gastric cytoprotective agents.
已披露的化合物的化学式为A(CH.sub.2).sub.n O--B,其中A是具有以下化学式的基团
##STR1##
其中X为--N--或##STR2##
Z为##STR3##
R.sup.1为氢、低碳烷基或苯基;R.sup.2为氢或低碳烷基;或R.sup.1和R.sup.2一起形成苯环,条件是当X为--N--时,Z不是##STR4##
R.sup.3为氢或低碳烷基;n为1-2;B为##STR5##
其中Y为OR.sup.5或N(OH)R.sup.8;R.sup.4和R.sup.5分别独立地为氢或低碳烷基;R.sup.6为氢、卤素或硝基;R.sup.7为##STR6##
R.sup.8为低碳烷基;m为0-3;以及其药理学上可接受的盐,以及它们在治疗炎症性疾病,如类风湿关节炎、溃疡性结肠炎、银屑病和其他即时过敏反应;在治疗白三烯介导的鼻支气管阻塞性通气道疾病,如过敏性鼻炎、过敏性支气管哮喘等;以及作为胃黏膜保护剂的用途。