Patent ID: 7517854
Filing Date: 2009-04-14
Classification: A61K,A61P,C07K

Abstract:
1. A peptide according to formula I: wherein, X1 represents Nle or X-Nle, wherein X represents an amino acid or a di-, tri-, tetra- or penta-peptide consisting of polar or hydrophilic amino acid residues selected from the D and L forms of Asp, Glu, His, Arg, homoArg, Tyr, Asn, Ser, Thr, Lys, Orn, Dap, Dab and Gln and wherein X may furthermore contain one or two amino acid residues selected from Gly, β-Ala or the D and L forms of Pro, Hyp, and Ala; and wherein the N-terminal amino group of X1 may optionally be acylated with an acyl moiety, R—C(O)—, wherein R presents an alkyl or alkenyl with up to 6 carbon atoms, wherein said alkyl may optionally be substituted with one or more substituents selected from hydroxyl and amino; X2 represents Glu or Asp; X3 represents Cit, Dab, Dap, cyclohexylglycine, cyclohexylalanine, Val, Ile, tert-butylglycine, Leu, Tyr, Glu, Ala, Nle, Met, Met(O), Met(O X4 represents D-Phe, wherein the phenyl moiety in D-Phe may optionally be substituted with one or more substituents selected from halogen, hydroxy, alkoxy, nitro, methyl, trifluoromethyl and cyano; X5 represents Arg; X6 represents Trp; X7 represents Lys or Orn, wherein to make the peptide of formula I cyclic an amide bond is formed between the side chain carboxyl of X2 and the side chain amine group of X7; R1 represents —N(R″) provided that if X3 represents Hyp, Ala, Pro, Glu, Lys or Gln, and X1 represents Ac-Nle, then X2 does not represent Asp; or a pharmaceutically acceptable salt thereof.