Withacnistin compounds for treatment of cancer

A - Human Necessities – 61 – K

Patent

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A61K 31/58 (2006.01)

Patent

CA 2641262

The subject invention pertains to the treatment of tumors and cancerous tissues and the prevention of tumorigenesis and malignant transformation through the modulation of STAT3 intracellular signaling. The subject invention concerns pharmaceutical compositions containing one or more withacnistin compounds, or a pharmaceutically acceptable salt or derivative thereof. In one embodiment, the subject invention concerns a composition comprising a mixture of withacnistin, 3-methoxy-2,3-dihydrowithacnistin, and 3-ethoxy-2,3- dihydrowithacnistin, or a salt or derivative of any of the foregoing.,Another aspect of the invention concerns methods of inhibiting the growth of a tumor by administering one or more withacnistin compounds, or a pharmaceutically acceptable salt or derivative thereof, to a patient, wherein the tumor is characterized by the constitutive activation of the STAT3 intracellular signaling pathway. The present invention further pertains to methods of moderating the STAT3 signaling pathway in vitro or in vivo using one or more withacnistin compounds, or a pharmaceutically acceptable salt or derivative thereof.

La présente invention concerne le traitement des tumeurs et des tissus cancéreux et la prévention de la tumorigenèse et de la transformation maligne par la modulation de la signalisation intracellulaire STAT3. L'invention concerne des compositions pharmaceutiques contenant un ou plusieurs composés de withacnistine ou un de leurs sels ou dérivés pharmaceutiquement acceptables. Dans un mode de réalisation, la présente invention concerne une composition comprenant un mélange de withacnistine, de 3-méthoxy-2,3-dihydrowithacnistine et de 3-ethoxy-2,3-dihydrowithacnistine, ou un sel ou dérivé de l'un quelconque des précédents. Un autre aspect de l'invention concerne des procédés permettant d'inhiber la croissance d'une tumeur en administrant à un patient un ou plusieurs composés de withacnistine, ou un de leurs sels ou dérivés pharmaceutiquement acceptables, ladite tumeur étant caractérisée par l'activation constitutive de la voie de signalisation intracellulaire STAT3. L'invention concerne en outre des procédés de modération de la voie de signalisation STAT3 in vitro ou in vivo en utilisant un ou plusieurs composés de withacnistine, ou un de leurs sels ou dérivés pharmaceutiquement acceptables.

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