| abstract |
The invention provides compounds and compositions of the formula:whereinthe subscript n is an integer of from 0 to 4;Ar is a member selected from the group consisting of substituted or unsubstituted aryl and substituted or unsubstituted heteroaryl;R1 is a member selected from the group consisting of substituted or unsubstituted (C5-C15)alkyl;R2 is a member selected from the group consisting of substituted or unsubstituted (C1-C8)alkyl;each R3 is independently a substituent selected from -halogen, -OR', -OC(O)R', -NR'R'', -SR', -R', -CN, -NO2, -CO2R', -CONR'R'', -C(O)R', -OC(O)NR'R'', -NR''C(O)R', -NR''C(O)2R', , -NR'-C(O)NR''R''', -NH-C(NH2)=NH, -NR'C(NH2)=NH, -NH-C(NH2)=NR-, -S(O)R', -S(O)2R', -S(O)2NR'R'', -N3, -CH(Ph)2, perfluoro(C1-C4)alkoxy, and perfluoro(C1-C4)alkyl, and where R', R'' and R''' are independently selected from hydrogen, (C1-C8)alkyl and heteroalkyl, unsubstituted aryl and heteroaryl, (unsubstituted aryl)-(C1-C4)alkyl, and (unsubstituted aryl)oxy-(C1-C4)alkyl;Y is a member selected from the group consisting of substituted or unsubstituted (C2-C8)alkylene and substituted or unsubstituted (C2-C8)heteroalkylene;and Z is -NR4R5, wherein R4 and R5 are independently selected from the group consisting of hydrogen and (C1-C8)alkyl.These compounds and compositions bind to the CXCR3 chemokine receptor and are useful for treating diseases and conditions responsive to the modulation of CXCR3 activity, such as multiple sclerosis, rheumatoid arthritis, psoriasis, cancer, infectious disease, angiogenesis, and graft rejection. |