5-LIPOXYGENASE INHIBITORS

摘要

Novel compounds having the ability to inhibit 5-lipoxygenase enzyme and having formula (I) and the pharmaceutically acceptable salts thereof, wherein Ar<1> is a heterocyclic moiety which is selected from imidazolyl, pyrrolyl, pyrazolyl, 1,2,3-triazolyl, 1,2,4-triazolyl, indolyl, indazolyl and benzimidazolyl, which is bonded to X<1> through a ring nitrogen atom, and which may be optionally substituted with one or two substituents selected from halo, hydroxy, cyano, amino, C1-4 alkyl and the like; X<1> is a direct bond or C1-4 alkylene; Ar<2> is phenylene optionally substituted with halo, hydroxy, cyano, amino and the like; X<2> is -A-X- or -X-A- wherein A is a direct bond or C1-4 alkylene and X is oxy, thio, sulfinyl or sulfonyl; Ar<3> is phenylene, pyridylene, thienylene, furylene, oxazolylene or thiazolylene optionally substituted with one or two substituents selected from halo, hydroxy, cyano, amino, C1-4 alkyl and the like; R<1> and R<2> are each C1-4 alkyl, or together they form a group of formula -D<1>-Z-D<2>- which together with the carbon atom to which it is attached defines a ring having 3 to 8 atoms, wherein D<1> and D<2> are C1-4 alkylene and Z is a direct bond or oxy, thio, sulfinyl, sulfonyl, or vinylene, and D<1> and D<2> may be substituted by C1-3 alkyl; and Y is CONR<3>R<4>, CN, C(R<3>)=N-OR<4>, COOR<3>, COR<3> or CSNR<3>R<4>, wherein R<3> and R<4> are each H or C1-4 alkyl. These compounds are useful in the treatment or alleviation of inflammatory diseases, allergy and cardiovascular diseases in mammals and as the active ingredient in pharmaceutical compositions for treating such conditions.