Patent ID: 8026218
Filing Date: 2011-09-27
Classification: A61K,A61P,C07K

Abstract:
1. A chimeric compound of formula (1) comprising an agonist opioid receptor binding moiety at its N-terminus and an antagonist neurokinin-1 (NK1) receptor binding moiety at its C-terminus, wherein: X1 is absent or is Tyr or substituted Tyr; X2 is absent or is Gly or D-amino acid; X3 is absent or is Gly; X4 is Phe or substituted Phe; X5 is Phe, Leu, Met, Gly, DPhe, Nle, Nle(R3), DCys, Cys, Ser(O—R4), substituted Cys, or substituted DCys; X6 is absent or is Pro, Ala, DLeu, DPro, Ser(O—R4) or Aib; X7 is absent or is Leu, Cys, DCys, Ser(O—R4), Pen, DPen, Ala, DAla, beta Ala, alpha Abu, gamma Abu, Ava, or Aib; X8 is absent or is Ser(O—R4); R1 is O, NH, or N—R5; R2 is benzyl (Bzl) or substituted benzyl; R3 is alkyl or a substituted alkyl; R4 is sugar; R5 is alkyl or substituted alkyl, or salts thereof, wherein the chimeric compound is optionally a cyclic compound, wherein the C-terminus moiety optionally comprises an antagonist of substance P, with the proviso that the chimeric compound is not Tyr-DAla-Gly-Phe-Gly-Trp-O-Bzl(CF wherein the compound induces analgesia.