Use of low molecular weight compounds for preparing a...

A - Human Necessities – 61 – K

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A61K 31/52 (2006.01) A61K 31/4015 (2006.01) A61K 31/439 (2006.01) A61K 31/4745 (2006.01) A61K 31/519 (2006.01) A61P 35/00 (2006.01)

Patent

CA 2476825

The present invention provides novel compounds, corresponding to formulae I and II, respectively, which are able to reactivate the apoptosis-inducing function of mutant p53 proteins. This reactivation is provided by restoration of sequence-specific DNA-binding activity and transcriptional transactivation function to mutant p53 proteins, and modulation of the conformation-dependent epitopes of the p53 protein. Accordingly, the substances according to the invention will be used in pharmaceutical compositions and methods for treatment of patients suffering from various types of tumours.

L'invention concerne de nouveaux composés correspondant respectivement aux formules (I) et (II) et pouvant être capable de réactiver la fonction d'induction d'apoptose des protéines p53 mutantes. Ladite réactivation est effectuée par la restauration de l'activité de liaison d'ADN de séquence spécifique et d'une fonction de transactivation transcriptionnelle des protéines p53 mutantes, et de la modulation d'épitopes dépendant de la conformation-dépendants de la protéine p53. Selon l'invention, lesdites substances peuvent être utilisées dans des compositions pharmaceutiques et des méthodes de traitement pour des patients souffrant de tumeurs de types différents.

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