Patent ID: 8007767

Claim:
A method for inhibiting signal-transducing activity of a cellular C5a receptor, comprising contacting a cell expressing C5a receptor with at least one compound of the formula: or a pharmaceutically acceptable form thereof, wherein: R represents: C 3 -C 7 cycloalkyl, or C 3 -C 7 cycloalkenyl, each of which is optionally substituted; R 1 represents: (i) hydrogen, hydroxy, halogen, amino, cyano, nitro, C 1 -C 2 haloalkyl or C 1 -C 2 haloalkoxy; (ii) C 1 -C 4 alkyl, C 2 -C 4 alkenyl, C 1 -C 4 alkoxy, C 3 -C 7 cycloalkyl, (C 3 -C 7 cycloalkyl)C 1 -C 2 alkyl, or mono- or di-C 1 -C 6 alkylamino, or (iii) phenylC 0 -C 4 carbhydryl or (5- or 6-membered heteroaryl)C 0 -C 4 carbhydryl, each of which is optionally substituted; R 2 is optionally substituted C 1 -C 7 alkyl or optionally substituted C 2 -C 7 alkenyl; R 3 is hydrogen or C 1 -C 6 alkyl; R 4 represents: (i) C 1 -C 6 alkyl, C 2 -C 6 alkenyl or C 2 -C 6 alkynyl, each of which is optionally substituted; (ii) optionally substituted arylC 0 -C 2 alkyl having 1 ring or 2 fused rings; (iii) optionally substituted arylC 1 -C 2 alkyl, wherein the aryl portion is fused to a 5- to 7-membered saturated or partially unsaturated ring having 0, 1 or 2 ring atoms independently chosen from N, O and S, with remaining ring atoms being carbon; or (iv) optionally substituted (4- to 12-membered heterocycle)C 0 -C 4 alkyl; R 5 and R6 are independently chosen from hydrogen and C 1 -C 6 alkyl; and Ar represents: (i) optionally substituted phenyl fused to a 5- to 7-membered saturated or partially unsaturated ring having 1 or 2 ring atoms independently chosen from N, O and S, with remaining ring atoms being carbon; or (ii) optionally substituted heteroaryl having 1 ring or 2 fused or pendant rings, from 5 to 7 members in each ring, and in at least one ring from 1 to 3 heteroatoms independently selected from N, O and S, and thereby reducing signal transduction by the C5a receptor.