Global Patent Index - EP 1042509 A1

EP 1042509 A1 2000-10-11 - METHODS OF USING OLIGONUCLEOTIDE ARRAYS TO SEARCH FOR NEW KINASE INHIBITORS

Title (en)

METHODS OF USING OLIGONUCLEOTIDE ARRAYS TO SEARCH FOR NEW KINASE INHIBITORS

Title (de)

VERFAHREN DURCH GEBRAUCH AN OLIGONUKLEOTIDARRAYS ZUM SUCHEN VON NEUEN KINASE-INHIBITOREN

Title (fr)

TECHNIQUES PERMETTANT D'UTILISER DES BANQUES CHIMIQUES POUR RECHERCHER DE NOUVEAUX INHIBITEURS DES KINASES

Publication

EP 1042509 A1 (EN)

Application

EP 98964881 A

Priority

  • US 9827405 W
  • US 6879897 P

Abstract (en)

[origin: WO9934018A1] The generation of selective inhibitors for specific protein kinases would provide new tools for analyzing signal transduction pathways and possibly new therapeutic agents. We have invented an approach to the development of selective protein kinase inhibitors based on the unexpected binding mode of 2,6,9-trisubstituted purines to the ATP binding site of human CDK2. The most potent inhibitor, purvalanol B (IC50 = 6 nM), binds with a 30-fold greater affinity than the known CDK2 inhibitor, flavopiridol. The cellular effects of this class of compounds were examined and compared to those of flavopiridol by monitoring changes in mRNA expression levels for all genes in treated cells of Saccharomyces cerevisiae using high-density oligonucleotide probe arrays.

IPC 1-7 (main, further and additional classification)

C12Q 1/68; A61K 31/52; C12Q 1/48

IPC 8 full level (invention and additional information)

A61K 31/52 (2006.01); C07D 473/16 (2006.01); C12Q 1/68 (2006.01)

CPC (invention and additional information)

C12Q 1/6809 (2013.01); A61K 31/52 (2013.01); C07D 473/16 (2013.01); C12Q 1/6837 (2013.01); C12Q 1/6886 (2013.01); C12Q 2600/136 (2013.01); C12Q 2600/158 (2013.01)

Citation (search report)

See references of WO 9934018A1

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 9934018 A1 19990708; AU 2010399 A 19990719; EP 1042509 A1 20001011

INPADOC legal status


2003-01-02 [18D] DEEMED TO BE WITHDRAWN

- Effective date: 20020702

2000-10-11 [17P] REQUEST FOR EXAMINATION FILED

- Effective date: 20000719

2000-10-11 [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