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

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 gr...

Full description

Saved in:
Bibliographic Details
Main Authors HOLUBOVA, Martina, MALETINSKA, Lenka, ZELEZNA, Blanka, KUNES, Jaroslav, ZEMENOVA, Jana
Format Patent
LanguageEnglish
French
German
Published 26.04.2017
Subjects
CHEMISTRY
METALLURGY
ORGANIC CHEMISTRY
PEPTIDES
Online AccessGet full text

Cover

More Information
Summary: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.
Bibliography:Application Number: EP20150739501