Novel inhibitors of ubiquitin isopeptidases

Details Novel inhibitors of ubiquitin isopeptidases Novel inhibitors of ubiquitin isopeptidases

A - Human Necessities

61

K

A61K 31/122 (2006.01) A61K 31/00 (2006.01) A61K 31/12 (2006.01) A61K 31/336 (2006.01) A61K 31/5575 (2006.01) A61K 45/06 (2006.01)

Patent

CA 2492523

A novel class of inhibitors of ubiquitin isopeptidases is disclosed that cause tumor cell death via molecular mechanisms independent of p53. Specifically, compounds containing an a,.szlig.-unsaturated ketone with a sterically accessible electrophilic .szlig.-carbon and related compounds are identified herein. Pharmaceutical compositions comprising the inhibitor compounds and methods of using the compounds for treating a variety of disease states are disclosed.

L'invention concerne une nouvelle classe d'inhibiteurs des ubiquitine isopeptidases, provoquant le mort des cellules tumorales par l'intermédiaire de mécanismes moléculaires indépendants de p53. L'invention concerne en particulier des composés contenant une cétone .alpha.,.szlig.-insaturée comprenant un carbone .szlig. électrophile stériquement accessible, ainsi que des composés analogues. L'invention concerne en outre des compositions pharmaceutiques comprenant ces composés inhibiteurs et des méthodes d'utilisation de ces composés pour le traitement de divers états pathologiques.

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