发明名称 DERIVATIVES OF TAXANE, METHOD OF THEIR SYNTHESIS AND PHARMACEUTICAL COMPOSITION
摘要 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
申请公布号 RU2168513(C2) 申请公布日期 2001.06.10
申请号 RU19980122311 申请日期 1997.04.29
申请人 INDENA S.P.A. 发明人 BOMBARDELLI EHTSIO
分类号 C07D491/06;A61K31/337;A61K31/415;A61K31/4162;A61P35/00;C07D491/08;C07D491/16;C07D491/18;(IPC1-7):C07D491/08 主分类号 C07D491/06
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