Patent ID: 6821950
Filing Date: 2004-11-23
Classification: A61K,A61P,C07K

Abstract:
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, NH2, 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 a 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, NNO2, CHNO2 or NSO2NH2; n is an integer from 1 to 4, and R1 is H or an alkyl, aryl, CN, NH2, OH, â€”COâ€”CH2CH3, â€”COâ€”CH3, â€”COâ€”CH2CH2CH3, â€”COâ€”CH2Ph, or â€”CO-Ph; and X1 is â€”(CH2)nNHâ€” or (CH2)nâ€”Sâ€”, â€”(CH2)2Oâ€”, â€”(CH2)3Oâ€”, â€”(CH2)3â€”, â€”(CH2)4â€”, or â€”CH2COCHRNHâ€”, where R is the side chain of any common or uncommon amino acid, and where n is an integer of from 1 to 4.