Diphenyl - indol-2-on compounds and their use in the...

A - Human Necessities – 61 – K

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Details

A61K 31/404 (2006.01) A61K 31/407 (2006.01) A61K 31/4188 (2006.01) A61K 31/429 (2006.01) A61K 31/437 (2006.01) A61K 31/4439 (2006.01) A61K 31/4745 (2006.01) A61K 31/496 (2006.01) A61K 31/5025 (2006.01) A61K 31/5377 (2006.01) A61K 45/06 (2006.01) A61P 35/00 (2006.01)

Patent

CA 2562399

The present invention relates to substituted 3,3-diphenyl-1,3-dihydro-indol-2- one compounds, and the use of such compounds for the preparation of a medicament for the treatment of cancer in a mammal. It is postulated that the compounds inhibit protein synthesis and/or inhibit activation of the mTOR pathway ehich is an effective method for reducing cell growth and the treatment of cancer. Examples of such cancers are breast cancer, renal cancer, multiple myeloma, leucemia, glia blastoma, rhabdomyosarcoma, prostate, soft tissue sarcoma, colorectal sarcoma, gastric carcinoma, head and neck squamous cell carcinoma, uterine, cervical, melanoma, lymphoma, and pancreatic cancer. A particular subclass of compounds are represented by the formula (II) wherein at least one of X1 and X2 is a heteroatom substituent, e.g. 6-chloro-3,3-bis- (4-hydroxy-phenyl)-7-methyl-1,3-dihydro-indol-2-one.

L'invention concerne des composés de 3,3-diphényl-1,3-dihydro-indol-2-one substitués ainsi que l'utilisation de ces composés dans la préparation d'un médicament permettant de traiter le cancer chez un mammifère. D'une manière plus spécifique, l'invention concerne le traitement des cancers dans lequel l'inhibition de la synthèse des protéines et/ou l'inhibition de l'activation de la voie de mTOR est une méthode efficace pour réduire la croissance cellulaire. Ces cancers sont, par exemple, le cancer du sein, le cancer du rein, le myélome multiple, la leucémie, le blastome de la glie, le rhabdomyosarcome, le cancer de la prostate, le sarcome des tissus mous, le sarcome colorectal, le carcinome gastrique, l'épithélioma spinocellulaire de la tête et du cou, le cancer de l'utérus, le cancer du col de l'utérus, le mélanome, le lymphome et le cancer du pancréas. Une sous-classe particulière de composés sont représentes par la formule (II) dans laquelle X1 et/ou X2 représentent un substituant d'hétéroatome, par exemple, le 6-chloro-3,3-bis-(4-hydroxy-phényl)-7-méthyl-1,3-dihydro-indol-2-one.

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