Patent ID: 6489298
Filing Date: 2002-12-03
Classification: A61K,A61P,C07K

Abstract:
A method for treating pain in an individual which comprises administering a therapeutically effective amount of an active agent to a individual in need of pain treatment, said active agent selected from the group consisting of:(a) contulakin-G comprising the amino acid sequence Xaa1-Ser-Glu-Glu-Gly-Gly-Ser-Asn-Ala-Thr-Lys-Xaa2-Tyr-Ile-Leu (SEQ ID NO:1), where Xaa1 is pyro-Glu, Xaa2 is proline or hydroxyproline and Thr10 is modified to contain O-glycan; b) a generic contulakin-G having the following general formula Xaa1-Xaa2-Xaa3-Xaa3-Gly-Gly-Xaa2-Xaa4-Xaa5-Xaa6-Xaa7-Xaa8-Xaa7-Xaa9-Xaa10-lle-Leu (SEQ ID NO:2), where Xaa1 is pyro-Glu, Glu, Gln or &ggr;-carboxy-Glu; Xaa2 is Ser, Thr or S-glycan modified Cys; Xaa3 is Glu or &ggr;-carboxy-Glu; Xaa4 is Asn, N-glycan modified Asn or S-glycan modified Cys; Xaa5 is Ala or Gly; Xaa6 is Thr, Ser, S-glycan modified Cys, Tyr or any hydroxy containing unnatural amino acid; Xaa7 is Lys, N-methyl-Lys, N,N-dimethyl-Lys, N,N,N-trimethyl-Lys, Arg, ornithine, homoarginine or any unnatural basic amino acid; Xaa8 is Ala, Gly, Lys, N-methyl-Lys, N,N-dimethyl-Lys, N,N,N-trimethyl-Lys, Arg, ornithine, homoarginine, any unnatural basic amino acid or X-Lys where X is (CH2)n, phenyl, â€”(CH2)mâ€”(CH&boxH;CH)â€”(CH2)mH or â€”(CH2)mâ€”(Câ‰¡C)â€”(CH2)mH in which n is 1-4 and m is 0-2; Xaa9 is Pro or hydroxy-Pro; and Xaa10 is Tyr, mono-iodo-Tyr, di-iodo-Tyr, O-sulpho-Tyr, O-phospho-Tyr, nitro-Tyr, Trp, D-Trp, bromo-Trp, bromo-D-Trp, chloro-Trp, chloro-D-Trp, Phe, L-neo-Trp, or any unnatural aromatic amino acid, with the proviso that the generic contulakin-G is not desglycosylated contulakin-G; (c) a generic contulakin-G of (b) which is modified to contain an O-glycan, an S-glycan or an N-glycan; (d) a contulakin-G analog which comprises an N-terminal truncation of from 1 to 9 amino acids of the generic contulakin-G of (b); (e) a contulakin-G analog of (c), wherein an Ser-O-glycan, Thr-O-glycan or Cys-S-glycan is substituted for the amino acid residue at the truncated N-terminus; (f) a contulakin-G analog of (c), wherein an Ser-O-glycan, Thr-O-glycan or Cys-S-glycan is substituted for a residue at positions 2-9 of the generic contulakin-G; and (g) a contulakin-G analog which comprises an N-terminal truncation of 10 amino acids of the generic contulakin-G of (b) which is further modified to contain a Lys-N-glycan at residue 11 of the generic contulakin-G.