Patent ID: RE41287

Claim:
A compound, which has antagonist activity against a C5a receptor, has no agonist activity against a C5a receptor, and has the general formula II: where A is H, alkyl, aryl, NH 2 , NHalkyl, N(alkyl) 2 , NHaryl or NHacyl; B is an alkyl, aryl, phenyl, benzyl, naphthyl or indole group, or the side chain of a D- or L-amino acid selected from the group consisting of phenylalanine, homophenylalanine, tryptophan, homotryptophan, tyrosine, and homotyrosine; C is the side chain of D-, L- or homo-amino acid selected from the group consisting of proline, alanine, leucine valine, isoleucine, arginine, histidine, aspartate, glutamate, glutamine, asparagine, lysine, tyrosine, phenylalanine, cyclohexylalanine, norleucine, tryptophan, cysteine and methionine; D is the side chain of a D- or L-amino acid selected from the group consisting of cyclohexylalanine, homocyclohexylalanine, leucine, norleucine, homoleucine, homonorleucine and tryptophan; E is the side chain of a D- or L-amino acid selected from the group consisting of tryptophan and homotryptophan; F is the side chain of a D- or L-amino acid selected from the group consisting of arginine, homoarginine, lysine and homolysine or is one of the following side-chains or another mimetic of an arginine side chain, where X is NCN, NNO 2 , CHNO 2 or NSO 2 NH 2 ; n is an integer from 1 to 4, and R 1 is H or an alkyl, aryl, CN, NH 2 , OH, —CO—CH 2 CH 3 , —CO—CH 3 , —CO—CH 2 CH 2 CH 3 , —CO—CH 2 Ph, or —CO-Ph; and X 1 is —(CH 2 ) n NH— or (CH 2 ) n —S—, —(CH 2 ) 2 O—, —(CH 2 ) 3 O—, —(CH 2 ) 3 —, —(CH 2 ) 4 —, or —CH 2 COCHRNH—, where R is the side chain of any common or uncommon amino acid, and where n is an integer of from 1 to 4.