Patent ID: 7659246
Filing Date: 2010-02-09
Classification: A61K,A61P

Abstract:
1. A method of treatment of osteoarthritis, comprising the step of administering an effective amount of an inhibitor of a C5a G protein-coupled receptor to a subject in need of such treatment, in which the inhibitor is a compound which (a) is an antagonist of a C5a G protein-coupled receptor, (b) has substantially no agonist activity, and (c) is a cyclic peptide or peptidomimetic compound of formula I: where A is H, alkyl, aryl, NH 2 , NH-alkyl, N(alkyl) 2 , NH-aryl, NH-acyl, NH-benzoyl, NHSO 3 , NHSO 2 -alkyl, NHSO 2 -aryl, OH, O-alkyl, or O-aryl; B is an alkyl, aryl, phenyl, benzyl, naphthyl or indole group, or B is the side chain of L-phenylalanine or L-phenylglycine; C is the side chain of glycine, alanine, leucine, valine, proline, hydroxyproline, or thioproline; D is the side chain of D-leucine, D-homoleucine, D-cyclohexylalanine, D-homocyclohexylalanine, D-valine, D-norleucine, D-homo-norleucine, D-phenylalanine, D-tetrahydroisoquinoline, D-glutamine, D-glutamate, or D-tyrosine; E is the side chain of an amino acid selected from the group consisting of L-phenylalanine, L-tryptophan and L-homotryptophan, or is L-1-napthyl or L-3-benzothienyl alanine; F is the side chain of L-arginine, L-homoarginine, L-citrulline, or L-canavanine, or a bioisostere thereof; and X