EP 1095057 A1 20010502 - MATRIX METALLOPROTEINASE INHIBITORS CONTAINING AMINOMALONIC ACID DERIVATIVES AND PEPTIDE BACKBONE MODIFIED DERIVATIVES THEREOF
Title (en)
MATRIX METALLOPROTEINASE INHIBITORS CONTAINING AMINOMALONIC ACID DERIVATIVES AND PEPTIDE BACKBONE MODIFIED DERIVATIVES THEREOF
Title (de)
MATRIX METALLOPROTEINASE INHIBITORE ENTHALTEND AMINOMALONSAÜREDERIVATE UND DEREN DERIVATE MIT EINER MODIFIZIERTEN PEPTIDHAUPTKETTE
Title (fr)
INHIBITEURS DE METALLOPROTEASES MATRICIELLES CONTENANT DES DERIVES D'ACIDE AMINOMALONIQUE ET LEURS DERIVES A SQUELETTE PEPTIDIQUE MODIFIE
Publication
Application
Priority
- EP 99934642 A 19990708
- EP 9904826 W 19990708
- EP 98112652 A 19980708
Abstract (en)
[origin: WO0002904A1] Novel peptides containing the sequence -Pro-Leu-Ama(NHOH)- were synthesized and characterized by spectroscopic techniques. Their inhibitory properties towards the activated form of native human gelatinase B (MMP-9) and the catalytic domain of neutrophil colagenase (cdMMP-8) were determined. The most effective inhibitor synthesized exhibits Ki values of 2x10<-6> M (cdMMP-8) and 5x10<-9> M(MMP-9) thus attaining interesting discrimination between the tested metalloproteinases. A most important feature of this type of inhibitor is its peptide nature making the compounds similar to natural substrates. In spite of the peptide character of the inhibitors synthesized, the P1-P1'-peptide bond shows a high resistance to cleavage by the proteinases.
IPC 1-7
C07K 5/117; C07K 5/113; C07K 7/06; C07K 5/083; C07K 5/097; C07K 5/062; C07K 5/072; A61K 38/04
IPC 8 full level
A61K 38/00 (2006.01); A61K 38/04 (2006.01); A61P 1/00 (2006.01); A61P 1/02 (2006.01); A61P 9/00 (2006.01); A61P 11/00 (2006.01); A61P 17/02 (2006.01); A61P 19/02 (2006.01); A61P 25/00 (2006.01); A61P 25/28 (2006.01); A61P 27/02 (2006.01); A61P 29/00 (2006.01); A61P 35/00 (2006.01); A61P 35/04 (2006.01); A61P 43/00 (2006.01); C07K 5/06 (2006.01); C07K 5/062 (2006.01); C07K 5/072 (2006.01); C07K 5/083 (2006.01); C07K 5/097 (2006.01); C07K 5/113 (2006.01); C07K 5/117 (2006.01); C07K 7/06 (2006.01)
CPC (source: EP)
A61P 1/00 (2017.12); A61P 1/02 (2017.12); A61P 9/00 (2017.12); A61P 11/00 (2017.12); A61P 17/02 (2017.12); A61P 19/02 (2017.12); A61P 25/00 (2017.12); A61P 25/28 (2017.12); A61P 27/02 (2017.12); A61P 29/00 (2017.12); A61P 35/00 (2017.12); A61P 35/04 (2017.12); A61P 43/00 (2017.12); C07K 5/06026 (2013.01); C07K 5/06104 (2013.01); C07K 5/0806 (2013.01); C07K 5/0808 (2013.01); C07K 5/0823 (2013.01); C07K 5/1021 (2013.01); C07K 5/1024 (2013.01); C07K 7/06 (2013.01); A61K 38/00 (2013.01)
Citation (search report)
See references of WO 0002904A1
Designated contracting state (EPC)
AT BE CH CY DE DK ES FI FR GB GR IE IT LI LU MC NL PT SE
DOCDB simple family (publication)
WO 0002904 A1 20000120; AU 5034699 A 20000201; EP 1095057 A1 20010502; JP 2002520333 A 20020709
DOCDB simple family (application)
EP 9904826 W 19990708; AU 5034699 A 19990708; EP 99934642 A 19990708; JP 2000559133 A 19990708