DERIVATIVES OF TAXANE, METHOD OF THEIR SYNTHESIS AND PHARMACEUTICAL COMPOSITION Russian patent published in 2001 - IPC

FIELD: organic chemistry, pharmacy. SUBSTANCE: invention describes novel derivatives of taxane of the general formula (I) where R₁ and R₂ mean hydrogen atoms or R₁ and R₂ in common form cyclic carbonate or cyclic thiocarbonate group of the formula (a) or (b) ; R₃ means hydrogen atom ; R₄ means hydrogen atom or isoserine residue of the formula (2) where R₅ means C₁-C₅-alkyl group or phenyl residue; R₆ has the same values as R₅ or means tert.-butoxy-group. New derivatives of taxane show antitumor activity by inhibition of cell proliferation of normal and resistant tumor cell lines and by induction of apoptosis. These molecules have basic properties and therefore they can be administrated after salt formation in an aqueous medium without necessary use of toxicsurface-active substances. Invention describes method of their synthesis and pharmaceutical composition. EFFECT: new compounds indicated above, improved method of synthesis, valuable anti- -tumor properties. 10 cl, 1 tbl, 6 ex