| 摘要 |
Compounds of formula (I), wherein X is O or C=O; Y is CN, S(O)uR8, NR5SO2R8, OR9, R10 or -C6H4R10; Z is -(O)y-(CR5R6)s-R10, -(O)y-(CR5R6)v-OR9 or R10; R1, R3 are, independently, aryl, substituted aryl, heteroaryl, lower alkyl or aralkyl; R2 is hydrogen, lower alkyl, halogen or lower alkoxy; R4 is hydrogen or lower alkyl; R5, R6 are, independently, each occurrence, hydrogen or lower alkyl; R7 is hydroxy, lower alkoxy or NR5R6; R8 is lower alkyl, aryl, substituted aryl or aralkyl; R9 is hydrogen, lower alkyl, aryl, substituted aryl, aralkyl, lower alkanoyl or aroyl; R10 is COR7, CONHSO2R8 or 1H-tetrazol-5-yl; m is an integer from 3 to 8; n and s are, independently, an integer from 1 to 12; t is an integer from 0 to 1; u is an integer from 0 to 2; v is an integer from 2 to 12; y is an integer from 0 to 1; and z is an integer from 0 to 1; with the proviso that either Y is R10 or -C6H4R10 or Z is -(O)y-(CR5R6)s-R10 or R10 and the further proviso that when n=1, Y is R10 or -C6H4R10, an optical isomer when R5 and R6 are not both hydrogen or the same lower alkyl and, when R7 is hydroxy, a pharmaceutically acceptable salt thereof with a base. The compounds of formula (I) are potent leukotriene B4 antagonists and are therefore useful in the treatment of inflammatory diseases such as psoriasis, rhinitis, chronic obstructive pulmonary disease, inflammatory bowel disease, asthma, acute respiratory distress syndrome, cystic fibrosis, allergy, arthritis such as rheumatoid arthritis, dermatitis such as contact dermatitis, NSAID-induced gastropathy, gout, ischemia/reperfusion injury, and trauma-induced inflammation such as spinal cord injury.
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