Patent ID: 6316406
Filing Date: 2001-11-13
Classification: A61K,C07K

Abstract:
A depsipeptide having the formula (2): ##STR29##whereinR.sub.1 is a straight or branched alkyl group of 5-20 carbon atoms or a straight or branched alkoxymethyl group of 5-15 carbon atoms;A, B, D, E and F independently are a N-substituted glycine residue having the formula (3) ##STR30##in which R.sub.4 is an alkylene group of 1-4 carbon atoms and R.sub.5 is a hydrogen atom, a hydroxy group, a carboxy group or a carbamido group; or A, B, D, E and F independently are a residue of an amino acid selected from the group consisting of alanine, valine, leucine, isoleucine, serine, threonine, lysine, hydroxylysine, arginine, cysteine, methionine, phenylalanine, tyrosine, tryptophan, histidine, proline, 4-hydroxyproline, piperidine-4-carboxylic acid, homoproline, octahydroindole-2-carboxylic acid, norvaline, norleucine, .alpha.-t-butylglycine, cyclohexylglycine, azetidine-2-carboxylic acid, 3-(3-pyridyl)alanine, (3-N-methyl)piperidylalanine, 3-(2-naphthyl)alanine, .beta.-cyclohexylalanine, .beta.-t-butylalanine, 9-anthracenylalanine, .alpha.-methylalanine, 2-aminobutanoic acid, aspartic acid, asparagine, glutamic acid and glutamine; wherein said residue of an amino acid is optionally substituted at the .alpha.-nitrogen atom with a (C.sub.1 -C.sub.4) alkyl group;W is a residue of an amino acid selected from the group consisting of aspartic acid, glutamic acid and an amino acid of the formula (4) ##STR31##wherein p is an integer of 1-4;Z is a residue of an amino acid selected from the group consisting of aspartic acid, asparagine, glutamic acid, glutamine, alanine, serine and lysine or the N-substituted glycine residue of the formula (3);m and n are independently 0 or 1;provided that a free amino group, a free carboxy group, a free hydroxy group, a free mercapto group or a free .omega.-carbamido group possibly existing in said amino acid residues for the above A, B, D, E, F, W and Z may be protected by a group used as a protecting group in peptide chemistry; and further provided that when A, B, D, E, F, W and Z are a residue of lysine, hydroxylysine, glutamic acid or aspartic acid, either .alpha.- or .omega.-amino or carboxyl group existing in said residue may form the peptide linkage with its adjacent amino acid; and further provided that at least one of A, B, D, E, F, W and Z is the N-substituted glycine residue of the formula (3);or a pharmacologically acceptable salt thereof.