Amino methyl imidazoles and related compounds as C5a receptor modulators

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:
• C3-C7cycloalkyl, or C3-C7cycloalkenyl, each of which is optionally substituted;
• R1 represents:
• (i) hydrogen, hydroxy, halogen, amino, cyano, nitro, C1-C2haloalkyl or C1-C2 haloalkoxy;
• (ii) C1-C4alkyl, C2-C4alkenyl, C1-C4alkoxy, C3-C7cycloalkyl, (C3-C7cycloalkyl)C1-C2alkyl, or mono- or di-C1-C6alkylamino, or
• (iii) phenylC0-C4carbhydryl or (5- or 6-membered heteroaryl)C0-C4carbhydryl, each of which is optionally substituted;
• R2 is optionally substituted C1-C7 alkyl or optionally substituted C2-C7 alkenyl;
• R3 is hydrogen or C1-C6alkyl;
• R4 represents:
• (i) C1-C6alkyl, C2-C6alkenyl or C2-C6alkynyl, each of which is optionally substituted;
• (ii) optionally substituted arylC0-C2alkyl having 1 ring or 2 fused rings;
• (iii) optionally substituted arylC1-C2alkyl, 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)C0-C4alkyl;
• R5 and R6 are independently chosen from hydrogen and C1-C6alkyl;
• 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.