| abstract |
Abstract of the Disclosure This invention provides benzene derivatives, of Formula I I and pharmaceutically acceptable salts thereof, wherein R1 is hydrogen; Z is -(CH2)n2- or phenylene; n is 1-8; R2 is hydroxy, halo, or -O-(CH2)m-Y; R3 is C1-C6 alkyl, C1-C6 alkanoyl, C2-C4 alkenyl, C1-C4 alkoxy, hydroxy-substituted C1-C3 alkyl, or -CH2-D; A is a bond or straight or branched chain C1-C10 alkylidene; R4 is C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, 1,2,4-triazol-1-yl, hydroxy, -CN, halo, -N3, -NR5R6, -COR7, -S(O)p-(C1-C4 alkyl), 5-tetrazolyl optionally substituted with a C1-C4 alkyl group or -(CH2)q-COOR', or phenyl optionally substituted with one or two groups selected from halo, cyano, C1-C3 alkyl, trifluoromethyl, -CH2CN, -CH2Br, C1-C4 alkoxy, -S(O)p-(C1-C4 alkyl), acetenyl, -COOR', 5-tetrazolyl, or 5-tetrazolyl substituted with C1-C4 alkyl or -(CH2)q-COOR'; where each R' is independently hydrogen or C1-C4 alkyl; m is 1-4; q is 1-4; Y is hydrogen or -CN; D is halo, C1-C4 alkoxy, or -S-(C1-C4 alkyl); R5 and R6 are independently hydrogen, C1-C3 alkyl, or C2-C4 alkanoyl, or when taken together with the nitrogen atom to which they are attached form a morpholino ring; R7 is hydroxy, C1-C4 alkoxy, halo, -NR5R6, -NHOH, , or C1-C3 alkyl; and each p is 0, 1, or 2, provided that when A is a bond, R4 must be C1-C6 alkyl or an optionally substituted phenyl group, and further provided that when one of R5 and R6 is C2-C4 alkanoyl, the other of R5 and R6 is hydrogen. The compounds are leukotriene antagonists, and are useful for the treatment of inflammatory disorders. |