Synthesis of combretastatin a-4 prodrugs and trans-isomers...

C - Chemistry – Metallurgy – 07 – F

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C07F 9/12 (2006.01) C07F 9/09 (2006.01)

Patent

CA 2314238

Combretastatin A-4 has been previously selected for pre-clinical development as antineoplastic agents. However, it is essentially insoluble in water. New water soluble derivatives of combretastatin A-4 and its qualified analogs have been discovered and synthesized through a multistage process using other derivatives of combretastatin A-4 as intermediates. These water soluble derivatives are herein denominated as "Combretastatin A-4 Prodrugs".

Selon cette invention, on a déjà utilisé la Combrestatine A-4 pour le développement préclinique, en tant qu'agent antinéoplasique; cependant, elle est généralement insoluble dans l'eau. On a découvert et synthétisé de nouveaux dérivés hydrosolubles de la Combrestatine A-4, ainsi que leurs analogues agréés, en passant par un procédé à plusieurs étapes et en utilisant comme intermédiaires d'autres dérivés de la Combrestatine A-4. Ces dérivés hydrosolubles sont désignés dans l'invention comme des "promédicaments à base de Combrestatine A-4".

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