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    • 9. 发明授权
    • Substituted indole-, indene-, pyranoindole- and
tetrahydrocarbazole-alkanoic acid derivatives as inhibitors of PLA2 and
lipoxygenase
    • 取代的吲哚,茚,吡喃吲哚和四氢咔唑 - 链烷酸衍生物作为PLA2和脂氧合酶的抑制剂
    • US5229516A
    • 1993-07-20
    • US911434
    • 1992-07-10
    • John H. MusserAnthony F. Kreft, IIIAmedeo A. FailliChristopher A. DemersonUresh S. ShahJames A. Nelson
    • John H. MusserAnthony F. Kreft, IIIAmedeo A. FailliChristopher A. DemersonUresh S. ShahJames A. Nelson
    • C07C323/62C07D209/22C07D215/14C07D401/12C07D401/14C07D417/12C07D491/04
    • C07D401/12C07C323/62C07D209/22C07D215/14C07D401/14C07D417/12C07D491/04
    • There are disclosed compounds of the formulaA(CH.sub.2).sub.n O-BwhereinA is C.sub.4 -C.sub.8 alkyl, phenoxyethyl, phenoxyphenyl or a group having the formula ##STR1## wherein ##STR2## R.sup.1 is hydrogen, lower alkyl, phenyl or phenyl substituted with trifluoromethyl;R.sup.2 is hydrogen or lower alkyl; orR.sup.1 and R.sup.2 taken together form a benzene ring;R.sup.3 is hydrogen or lower alkyl;n is 1-2;B is ##STR3## wherein ##STR4## m is 0-3; R.sup.5 is ##STR5## or phenyl or phenyl substituted by halo, lower alkylthio, lower alkylsulfinyl or lower alkylsulfonyl;R.sup.6 is A(CH.sub.2).sub.n O-- or halo; with the proviso that when R.sup.6 is halo, R.sup.5 is ##STR6## R.sup.7 is lower alkyl; Y is --CH.sub.2 -- or --O--;R.sup.8 is lower alkyl or --(CH.sub.2).sub.m CO.sub.2 R.sup.3 ;R.sup.9 is ##STR7## or --CH.sub.2 R.sup.10 ; R.sup.10 is lower alkyl, phenyl, phenyl substituted with carboxy, halo, loweralkylthio or loweralkylsulfinyl, pyridyl, furanyl or quinolinyl;R.sup.11 is lower alkyl or phenyl;Z is hydrogen, lower alkyl or --N(CH.sub.3)OH;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.
    • 公开了式A(CH 2)n O-B的化合物,其中A是C 4 -C 8烷基,苯氧基乙基,苯氧基苯基或具有下式的基团:其中R 1是氢,低级烷基 ,苯基或被三氟甲基取代的苯基; R2是氢或低级烷基; 或R 1和R 2一起形成苯环; R3是氢或低级烷基; n为1-2; B是 其中 m是0-3; R 5为苯基或被卤素,低级烷硫基,低级烷基亚磺酰基或低级烷基磺酰基取代的苯基; R6是A(CH2)nO-或卤素; 条件是当R 6为卤素时,R 5为低级烷基; Y是-CH 2 - 或-O-; R8是低级烷基或 - (CH2)mCO2R3; R9是或-CH2R10; R 10为低级烷基,苯基,被羧基,卤素,低级烷硫基或低级烷基亚磺酰基取代的苯基,吡啶基,呋喃基或喹啉基; R11为低级烷基或苯基; Z是氢,低级烷基或-N(CH 3)OH; 及其药理学上可接受的盐及其在治疗炎性病症如类风湿性关节炎,溃疡性结肠炎,牛皮癣和其他立即超敏反应中的用途; 治疗白三烯介导的鼻支气管阻塞性通气条件,如过敏性鼻炎,过敏性支气管哮喘等; 和作为胃细胞保护剂。