Patent ID: 6458764
Filing Date: 2002-10-01
Classification: A61K,A61P,C07K,Y10S

Abstract:
An hydrophobic GRF analog of formula A:Xâ€”GRF-peptideâ€ƒâ€ƒ(A) wherein;the GRP peptide is a peptide of formula B; A1-A2-Asp-Ala-Ile-Phe-Thr-A8-Ser-Tyr-Arg-Lys-A13-Leu-A15-Gln-Leu-A18-Ala-Arg-Lys-Leu-Leu-A24-A25-Ile-A27-A28-Arg-A30-R0â€ƒâ€ƒ(B) wherein,A1 is Tyr or His; A2 is Val or Ala; A8 is Asn or Ser; A13 is Val or Ile; A15 is Ala or Gly; A18 is Ser or Tyr; A24 is Gln or His; A25 is Asp or Glu; A27 is Met, Ile or Nle; A28 is Ser or Asn; A30 is a bond or any amino acid sequence of 1 up to 15 residues; R0 is NH2 or NH-(CH2)n-CONH2, with n=1 to 12 and; X is a hydrophobic tail anchored via an amide bond to the N-terminus of the peptide and said hydrophobic tail defining a backbone of 5 to 7 atoms;wherein said backbone can be substituted by C1-6 alkyl, C3-6 cycloalkyl, or C6-12 aryl; and comprises at least one rigidifying moiety connected to at least two atoms of the backbone; said moiety selected from the group consisting of double bond, triple bond, saturated or unsaturated C3-9 cycloalkyl, and C6-12 aryl and wherein X is selected from the group consisting of: