| 摘要 |
Peptides, peptidomimetics and derivatives thereof of the following general formula (I): H2N-GHRPX1X2X3-ß-X4X5X6X7X8X9X10-X11, in which X1 - X10 denote one of the 20 g genetically coded amino acids, wherein X8, X9 and X10 individually or jointly may also denote a single chemical bond; X11 denotes OR1 in which R1 equals hydrogen or (C1 C10 ) alkyl, NR2R3 with R2 and R3 are equal or different and denote hydrogen, (C1 C10) alkyl or a residue -W-PEG5-60K, in which the PEG residue is atteched via a suitable spacer W to the N-atom, or a residue NH-Y-Z-PEG5-60K, in which Y denotes a single chemical bond or a genetically coded amino acids from the group S, C, K or R and in which Z denotes a spacer, via which a polyethylene glycol (PEG)-residue can be attached, as well as their physiologically acceptable salts, and in which additionally ß denotes an amino acid, whether genetically coded or not, or a peptidomimetic element, which have the additional property of inducing a bend or turn in the peptide backbone. Such amino acids include without limitation L-proline, D-proline, L-hydroxyproline, D-hydroxyproline, L-(O-benzyl)-hydroxyproline, D-(O-benzyl)-hydroxyproline, L-(O-tert, butyl)-hydroxyproline, 4-(O-2-naphtyl)-hydroxyproline, 4-(O-2-naphtyl-methyl)-hydroxyproline, 4-(O-phenyl)-hydroxyproline, 4-(4-phenyl-benzyl)-proline, cis-3-phenyl-proline, cis-4-phenyl-proline, trans-4-phenyl-proline, cis-5-phenyl-proline, trans-5-phenyl-proline, 4-benzyl-proline, 4-bromobenzyl-proline, 4-cyclohexyl-proline, 4-fluor-proline, L-tetrahydroisoquinoline-2-carboxyric acid (L-Tic), all diastereomers of octahydro-indole-2-carboxylic acid (Oic), and all diastereomers of 1-aza-bicyclo[3,3,0]octane-2-carboxylic acid or a residue selected from a group of peptidomimetic residues.
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