Global Patent Index - EP 1095057 A1

EP 1095057 A1 2001-05-02 - 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

EP 1095057 A1 (EN)

Application

EP 99934642 A

Priority

  • EP 99934642 A
  • EP 9904826 W
  • EP 98112652 A

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 (main, further and additional classification)

C07K 5/117; A61K 38/04; C07K 5/062; C07K 5/072; C07K 5/083; C07K 5/097; C07K 5/113; C07K 7/06

IPC 8 full level (invention and additional information)

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 (invention and additional information)

C07K 7/06 (2013.01); 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); 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

EPO simple patent family

WO 0002904 A1 20000120; AU 5034699 A 20000201; EP 1095057 A1 20010502; JP 2002520333 A 20020709

INPADOC legal status


2003-09-17 [18W] APPLICATION WITHDRAWN

- Effective date: 20030724

2003-02-12 [17Q] FIRST EXAMINATION REPORT

- Effective date: 20021230

2001-05-02 [17P] REQUEST FOR EXAMINATION FILED

- Effective date: 20010108

2001-05-02 [AK] DESIGNATED CONTRACTING STATES:

- Kind Code of Ref Document: A1

- Designated State(s): AT BE CH CY DE DK ES FI FR GB GR IE IT LI LU MC NL PT SE

2001-05-02 [AX] REQUEST FOR EXTENSION OF THE EUROPEAN PATENT TO:

- Free text: AL PAYMENT 20010108;LT PAYMENT 20010108;LV PAYMENT 20010108;MK PAYMENT 20010108;RO PAYMENT 20010108;SI PAYMENT 20010108