Epothilone derivatives for the treatment of refractory tumors

A - Human Necessities – 61 – K

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A61K 31/425 (2006.01)

Patent

CA 2438598

A method of treating tumors in a mammal, especially a human that have demonstrated resistance to oncology with taxane oncology agents is disclosed. The method is effective where the tumor has initially been unresponsive to taxane therapy or has developed resistance during the course of treatment. The method comprising the administration of an epothilone derivative selected from those represented by formula I:[chemical drawing]The subject epothilone derivatives are advantageous in addition to their enhanced potency and effectiveness against tumors that have demonstrated resistance to therapy with taxane oncology agents in that both[chemical drawing]The subject epothilone derivatives are advantageous in addition to their enhanced potency and effectiveness against tumors that have demonstrated resistance to therapy with taxane oncology agents in that both are efficacious upon oral administration.

L'invention concerne un procédé de traitement des tumeurs chez un mammifère, notamment un être humain présentant une résistance à l'oncologie, à l'aide d'agents oncologiques à base de taxane. Ce procédé est efficace à l'endroit où la tumeur était initialement réfractaire au traitement à base de taxane ou à l'endroit où celle-ci a développé une résistance au cours du traitement. Le procédé consiste à administrer un dérivé d'épothilone choisi parmi ceux représentés par la formule I: [figure chimique]. Les dérivés d'épothilone de l'invention possèdent une capacité et une efficacité améliorées contre les tumeurs présentant une résistance au traitement à l'aide d'agents oncologiques à base de taxane, et possèdent tous deux une efficacité avantageuse lorsqu'ils sont administrés oralement.

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