SEMI-SYNTHETIC TAXANES AND PHARMACEUTICAL COMPOSITIONS BASED ON THEREOF Russian patent published in 2005 - IPC

FIELD: organic chemistry, medicine, pharmacy.

SUBSTANCE: invention relates to new semi-synthetic taxanes of the formula (1):

wherein R and R₁ can be similar or different and represent hydrogen atom (H), (C₁-C₁₈)-acyl group, benzoyl group; R₂ and R₃ represent hydrogen atom (H) or R₂ and R₃ in common form carbonate or thiocarbonate residue; R₄ represents benzoyl group optionally substituted at meta-position; R' represents hydrogen atom (H) or (C₁-C₄)-alkyl; R'' represents (C₁-C₄)-alkyl or phenyl; R''' represents tert.-butoxy-group under condition that R and R₁ both can't represent hydrogen atom (H). Also, invention relates to a pharmaceutical composition based on compounds of the formula (1) eliciting an anti-tumor, anti-angiogenic and anti-arthrosis effect. Invention provides preparing new compounds eliciting cytotoxicity comparable with cytotoxicity of other taxanes but showing reduced systemic toxicity that can be administrated by intravenous and oral routes.

EFFECT: valuable medicinal properties of compounds and pharmaceutical compositions.

6 cl, 1 tbl, 7 ex