Water-soluble derivatives of paclitaxel, method for...

C - Chemistry – Metallurgy – 07 – D

Patent

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C07D 305/14 (2006.01) A61K 31/335 (2006.01) C07D 407/12 (2006.01) C07F 5/02 (2006.01) C07H 15/26 (2006.01)

Patent

CA 2336204

The invention relates to new paclitaxel derivatives showing an increased solubility in water. More particularly, the invention relates to glutarylpaclitaxel, glutarylpaclitaxel 6-aminohexanol glucuronide and to different amino acid derivatives of the glutarylpaclitaxel, all of which possess the cytotoxicity activity of the parent compound, paclitaxel. The present invention also relates to the use of such derivative for treating cancer. Also disclosed are fluorescent derivatives of paclitaxel for determining a concentration of paclitaxel in a medium or for detecting apoptotic cancer cells.

L'invention concerne de nouveaux dérivés de placlitaxel présentant une solubilité améliorée dans l'eau. L'invention concerne plus particulièrement le glutarylpaclitaxel, le glutarylpaclitaxel 6-aminohexanol glucuronide et différents dérivés acides aminés de glutarylpaclitaxel possédant tous l'activité cytotoxique du précurseur paclitaxel. L'invention concerne également l'utilisation de ces dérivés pour le traitement du cancer. L'invention concerne en outre des dérivés de paclitaxel fluorescents permettant de déterminer la concentration de paclitaxel dans un milieu ou de détecter les cellules cancéreuses apoptotiques.

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