ARYLALKOXYPHENYL-ALLYLIC ALCOHOLS AS AGENTS FOR THE TREATMENT OF HYPERSENSITIVE AILMENTS

摘要

The present invention is concerned with the therapeutic composition comprising as an active ingredient a compound of the formula: and salts thereof, wherein a = 1, 2 or 3; each b = 1 or 2 and is the same value as the other; Ar is phenyl or naphthyl containing one or two substituents selected from the group consisting of hydrogen, alkoxy, aryloxy, hydroxy, hydroxyalkyl, alkyl, aryl, halo, CF3, carboxy, carbalkoxy, carboxyalkoxy, carbalkoxyalkoxy, lower acyl, nitrilo, amino, nitro, mercapto or alkylthio; Ar1 is phenyl, naphthyl, or a nitrogen, oxygen or sulfur heterocyclic ring; each R1 is independently hydrogen, alkyl, carboxy, carbalkoxy, alkylenecarboxy, arylenecarboxy, alkylenecarbalkoxy, alkanoyl, formyl, nitrilo, amino, aminoalkylene, alkylamino, carboxamide, halo, trihalomethyl, hydroxy, alkoxy, aralkyloxy, aryloxy, nitro, sulfamyl, mercapto or alkylthio; each R is H or alkyl; Z is an alkylene chain containing up to 10 carbon atoms in the principal chain and up to a total of 12 carbon atoms and from 0 to 2 double bonds and Z when taken together with the carbon atom of (CR=CR) to which it is attached forms a cycloalkylidene ring; each R2 is a substituent attached to one of the carbon atoms of Z selected from the group consisting of OR4, SR4, N(R4)2, CHO and COR5; each R3 is H, cycloalkyl, aralkyl, aryl, lower dialkylamino, morpholino, piperazino, piperidino or CF3; each R4 is H, alkyl, benzoyl, lower alkanoyl, aryl or aralkyl; R5 is OR6 or N(R4)2; R6 is H, alkyl, aryl, or aralkyl; n = 1 or 2; n min = 1 or 2; n sec = 1 or 2; n''' = 1 or 2; X = -O(CHR7)m-, -NR4 (CHR7)m-, alkylene of up to 2 carbon atoms in the principal chain and up to a total of 4 carbon atoms, -C(R7) = C(R7)-, -C IDENTICAL C-, m = 0 or 1; m min = 0, 1, or 2; and R7 is H, CH3 or phenyl; wherein the group(s) designated [(R1)n@-Ar1-(X)b]a is (are) attached directly to Ar. In addition, the present invention relates to the method of using these compounds as lipoxygenase inhibitors possessing anti-inflammatory and anti-allergic responses.