Taxane derivatives

C - Chemistry – Metallurgy – 07 – D

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C07D 405/12 (2006.01) A61K 31/496 (2006.01) A61P 35/00 (2006.01)

Patent

CA 2314071

Taxane derivatives represented by general formula (1) or salts thereof and drugs containing the same as the active ingredient wherein A1 represents (a) (wherein R1 represents H or optionally substituted alkyl) or (b) (wherein R2 represents amino, mono- or dialkylamino, piperidino, pyrrolidino or morpholino); X represents H, alkoxycarbonyl or benzoyl; Y represents H or trialkylsilyl; A2 represents furyl, alkylfuryl, alkyl or fluorophenyl; Ac represents acetyl; and Bz represents benzoyl. These compounds are excellent in solubility in water and antitumor activity.

Dérivés de taxane représentés par la formule générale suivante (1) ou leurs sels et médicaments contenant ces dérivés et ces sels en tant qu'ingrédient actif dans laquelle A?1¿ représente (a) (dans laquelle R?1¿ représente H ou alkyle éventuellement substitué) ou (b) (dans laquelle R?2¿ représente amino, mono- ou dialkylamino, pipéridino, pyrrolidino ou morpholino); X représente H, alkoxycarbonyle ou benzoyle; Y représente H ou trialkylsilyle; A?2¿ représente furyle, alkylfuryle, alkyle ou fluorophényle; Ac représente acétyle; Bz représente benzoyle. Ces composés présentent une solubilité excellente dans l'eau et exercent une activé antitumorale.

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