Patent ID: 6211145
Filing Date: 2001-04-03
Classification: A61K,C07K

Abstract:
A bicyclic depsipeptide having the formula (1) ##STR28##wherein:R 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, D, E and J independently are a residue of an amino acid selected from the group of alanine, valine, leucine, isoleucine, serine, threonine, lysine, hydroxylysine, arginine, cysteine, methionine, phenylalamine, tyrosine, tryptophan, histidine, proline, 4-hydroxyproline, aspartic acid, glutamic acid, 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 or a (C.sub.1 -C.sub.4) alkyl substituted amino acid residue of said amino acid; B and F are the same or different and a residue of an amino acid selected from the group consisting of cysteine, aspartic acid, glutamic acid, lysine, hydroxylysine and serine; G is a disulfide bond, an amido bond or an ester bond; W is a residue of an amino acid selected from the group consisting of aspartic acid and glutamic acid; Z is a residue of an amino acid selected from the group consisting of aspartic acid, asparagine, glutamic acid and glutamine; l, m, n, p and q independently are 0 or 1; provided that G is formed by binding each other a thiol, carboxy, hydroxyl or amino group contained in the amino acid residues B and F, a free amino, carboxyl, hydroxyl, mercapto or .omega.-carbamido group which possibly exists in said amino acid residue may be protected by a group commonly used in peptide chemistry as a protective group and when A, B, D, E, F, J, 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 a peptide linkage with its adjacent amino acid, or a and an acceptable carrier thereof.