PORT, MARC,ROUSSEAUX, OLIVIER,MULLER, ROBERT,BURTEA, CARMEN
申请号：
EP10195948.4
公开号：
EP2322538B9
申请日:
2008.03.28
申请国别(地区):
EP
年份:
2012
代理人:
摘要：
Peptide compounds (signal-bond-peptide) (I), where the signal is signal entity, bond (optionally present) is a chemical bond and the peptide is a peptide comprising a peptide targeting vascular cell adhesion molecule comprising peptides, and their salts, are new. Peptide compound of formula (signal-bond-peptide) (I), where the signal is signal entity, bond (optionally present) is a chemical bond and the peptide is a peptide comprising a peptide targeting vascular cell adhesion molecule comprising a peptide of formula X1-X2-X3-X4-X5-X6-X7-X8-X9 (SEQ ID NO: 1), preferably Cys-Asn-Asn-Ser-Lys-Ser-His-Thr-Cys (SEQ ID NO: 2) and peptide Asn-Asn-Ser-Lys-Ser-His-Thr (SEQ ID NO: 3), and a peptide of formula X10-X11-X12-X13-X14-X15-X16-X17-X18 (SEQ ID NO: 4), preferably Cys-Met-Lys-Thr-Asn-Thr-Arg-Leu-Cys (SEQ ID NO: 5), and their salts, are new. X1 : absent, cysteine or methionine； X2, X3 : asparagine or glutamine； X4 : serine or threonine； X5 : lysine, arginine, histidine or ornithine； X6 : serine or threonine； X7 : histidine, arginine or lysine； X8 : threonine or serine； X9 : absent, cysteine or methionine； X10 : cysteine or methionine； X11 : methionine or cysteine； X12 : lysine, arginine or alanine； X13 : threonine or serine； X14 : aspartic acid or glutamic acid； X15 : threonine or serine； X16 : arginine, alanine or lysine； X17 : leucine, isoleucine or valine； and X18 : cysteine or methionine. Independent claims are included for: (1) a composition for medical imaging comprising (I) and excipient, for parenteral administration； and (2) a preparation of the composition comprising adding (I) in an injectable medium comprising excipient. ACTIVITY : Cardiovascular-Gen； Cardiant； Vasotropic； Cerebroprotective； Nephrotropic. MECHANISM OF ACTION : Cellular adhesion inhibitor. The ability of (I) to inhibit cellular adhesion was tested using ELISA. The result showed that the Asn-Asn-Ser-Lys-Ser-His-Thr (SEQ ID NO: 3) exhibited IC 50 value of 6.3x 10 -5>； M.
