| 摘要 |
Compounds are provided that act as potent antagonists of the CCR2 receptor. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR2- mediated diseases and as controls in assays for the identification of CCR2 antagonists. A compound of the formula (I) or a salt thereof: where: R1 and R2 are each independently hydrogen, halogen, C1-8alkyl, -CN. or C1-8 R3 is independently hydrogen; R4 is hydrogen; R5 is halogen or C1-8 alkyl; R6 is hydrogen; X1 is CR7, N or NO; X2 and X4 are N or NO; X3 is CR7; X6 and X7 are each independently selected from CR7, N, and NO; each R7 is independently haloalkyl, provided that at least one of R1 1 or R2 is other than hydrogen; each selected from the group consisting of hydrogen, halogen, substituted or unsubstituted C2-8 alkyl, substituted or unsubstitued C2-8 alke.pi.yl, substituted or -C(O)NR0R8, -OC(O)NR9R8 , -NR10C(O)R8, -NR10C(O)NR9R8, -NR9R8, -NR10CO2R8, -SR8, -S(O)R8, -S(O)2R8, -S(O)2NR9R8, -N10S(O)2R8, substituted or unsubstituted C6-10 aryl, substituted or unsubstituted 5- to 10-membered heteroaryl and substituted or unsubstituted 3- to 10-membered heterocyclyl; unsubstituted C2-8 alkynyl, -CN. =O, -NO2, -OR6, -OC(O)R8, -CO2R8, -C(O)R8, |
