INDOLE AND INDENE DERIVATIVES AS PLA2 AND LIPOXYGENASE INHIBITORS

摘要

There are disclosed compounds of the formula A(CH2)nO-B wherein A is C4-C8 alkyl, phenoxyethyl, phenoxyphenyl or a group having the formula wherein R1 is hydrogen, lower alkyl, phenyl or phenyl substituted with trifluoromethyl; R2 is hydrogen or lower alkyl; or R1 and R2 taken together form a benzene ring; R3 is hydrogen or lower alkyl; n is 1-2; B is wherein m is 0-3; R5 is or phenyl or phenyl substituted by halo, lower alkylthio, lower alkylsulfinyl or lower alkylsulfonyl; R6 is A(CH2)nO- or halo; with the proviso that when R6 is halo, R5 is R7 is lower alkyl; Y is -CH2- or -O-; R8 is lower alkyl or -(CH2)mCO2R3; R9 is or -CH2R10; R10 is lower alkyl, phenyl, phenyl substituted with carboxy, halo, loweralkylthio or loweralkylsulfinyl, pyridyl, furanyl or quinolinyl; R11 is lower alkyl or phenyl; Z is hydrogen, lower alkyl or -N(CH3)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.