C-2' methylated derivatives of paclitaxel for use as...

C - Chemistry – Metallurgy – 07 – D

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C07D 493/04 (2006.01) A61K 31/337 (2006.01) A61K 31/36 (2006.01) A61P 35/00 (2006.01) C07D 305/14 (2006.01) C07D 407/02 (2006.01) C07D 407/12 (2006.01)

Patent

CA 2456523

Taxane derivatives of formula (I) in which: R is trifluoromethyl, phenyl, 2- furyl, 2-thienyl; R1 is t-butoxycarbonyl or benzoyl; R2 is hydroxy; R3 is hydrogen or, together with R2, it forms the residue of a cyclic carbonate of formula: I I with the proviso that when R3 is hydrogen, R is different from phenyl.Compounds of formula (I) have antitumor activity.

L'invention concerne des dérivés taxane correspondant à la formule (I), dans laquelle : R représente trifluorométhyle, phényle, 2-furyle, 2-thiényle; R?1¿ représente t-butoxycarbonyle ou benzoyle; R¿2? représente hydroxy; R¿3? représente hydrogène ou bien forme, avec R¿2?, le résidu d'un carbonate cyclique de formule (a), à condition que quand R¿3? représente hydrogène, R ne représente pas phényle. Lesdits composés correspondant à la formule (I) présentent une activité antitumorale.

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