SUBSTITUTED INDOLE-, INDENE-, PYRANOINDOLE AND TETRAHYDROCARBAZOLE- ALKANOIC ACID DERIVATIVES AS INHIBITORS OF PLA2 AND LIPOXYGENASE

摘要

2070422 9106537 PCTABS00005 There are disclosed compounds of the formula: A(CH2)nO-B, wherein A is C4-C8 alkyl, phenoxyethyl, phenoxyphenyl or a group having formula (a) or (b), wherein X is -N- or (c); Z is (d), (e), (f), (g), -S- or -O-; 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 benzen ring; R3 is hydrogen or lower alkyl; n is 1-2; B is (h), (i), (j) or (k); wherein R4 is -CO2R2, (l), (m), (n), (o) or (p); m is 0-3; R5 is (q); 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 (r); R7 is lower alkyl; Y is -CH2- or -O-; R8 is lower alkyl or -(CH2)mCO2R3; R9 is (s) 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; 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.