1-azabicyclo[2.2.2]octan-3-one derivatives and maleimide...

Details 1-azabicyclo[2.2.2]octan-3-one derivatives and maleimide... 1-azabicyclo[2.2.2]octan-3-one derivatives and maleimide...

A - Human Necessities

61

K

A61K 31/4015 (2006.01) A61K 31/439 (2006.01) A61K 31/52 (2006.01) A61P 35/00 (2006.01) C07D 207/452 (2006.01) C07D 453/02 (2006.01)

Patent

CA 2423192

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 tumors.

La présente invention concerne de nouveaux composés correspondant respectivement à la formule I et à la formule II et capables de réactiver la fonction d'induction d'apoptose de protéines p53 mutantes. Cette réactivation est obtenue par la restauration d'une activité de liaison à l''ADN séquence-spécifique et de la fonction de transactivation transcriptionnelle aux protéines p53 mutantes, et par modulation des épitopes conformation-dépendants de la protéine p53. En conséquence, les substances selon l'invention seront utilisées dans des compositions pharmaceutiques et des procédés de traitement de patients souffrant de différents types de tumeurs.

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