TRICYCLIC LIPOXYGENASE INHIBITING COMPOUNDS, COMPOSITIONS, METHODS OF USE

摘要

Compounds of formula (I), wherein R1 is hydrogen, C1 to C4 alkyl, C2 to C4 alkenyl, or NR2R3, wherein R2 and R3 are independently selected from hydrogen, C1 to C4 alkyl and hydroxyl, but R2 and R3 are not simultaneously hydroxyl; X is oxygen, sulfur, SO2, or NR4, wherein R4 is hydrogen, C1 to C6 alkyl, C1 to C6 alkoyl or aroyl; A is selected from C1 to C6 alkylene and C2 to C6 alkenylene; Y is selected independently at each occurrence from hydrogen, halogen, hydroxy, cyano, nitro, halosubstituted alkyl, C1 to C12 alkyl, C2 to C12 alkenyl, C1 to C12 alkoxy, C3 to C8 cycloalkyl, aryl, aryloxy, aroyl, C1 to C12 arylalkyl, C2 to C12 arylalkenyl, C1 to C12 arylalkoxy, C1 to C12 arylthioalkoxy, and substituted derivatives of aryl, aryloxy, aroyl, C1 to C12 arylalkyl, C2 to C12 arylalkenyl, C1 to C12 arylalkoxy, or C1 to C12 arylthioalkoxy, wherein substituents are independently selected from halo, nitro, cyano, C1 to C12 alkyl, alkoxy, and halosubstituted alkyl; n is a number having the values 0-4; when n = 0 then Y = hydrogen; and M is hydrogen, a pharmaceutically acceptable cation, aroyl, or C1 to C12 alkoyl. These compounds are potent inhibitors of 5- and/or 12-lipoxygenase enzymes. Also disclosed are lipoxygenase inhibiting compositions and a method of inhibiting lipoxygenase.