LONG-ACTING STABLE PEPTIDE GHRELIN ANALOGS FOR THE TREATMENT OF CACHEXIA

摘要

The present invention provides long-acting stable peptide ghrelin analogs of general formulae (Sar)S(Dpr-X1)mLSPEHQKAQQRKESKKPPA(K-Z)LQPR (I), and/or (Sar)S(Dpr-X2)FLSPEHQKAQQR(K-Z)ES (II), wherein Dpr is diaminopropionic acid, Sar is sarcosin, X1 represents a fatty acid residue selected from the group comprising octanoyl, decanoyl, myristoyl, 9-decenoyl and N-10-undecynoyl bound to Dpr through an amide bond, X2 represents decanoyl or myristoyl, m represents a non-coded amino acid selected from the group comprising phenylalanine, naphtylalanine, cyclohexylalanine, t-butylalanine and dichlorophenylalanine, Z is palmitoyl which can be optionally bound to the secondary aminogroup of lysine through an amide bond or Z is not present. The compounds of the invention are suitable for use in a method of treatment of cachexia and/or anorexia.