DERIVATIVES OF EPOTILONE AND METHODS FOR THEIR PREPARING, PHARMACEUTICAL COMPOSITION AND METHOD OF TREATMENT BASED ON THEREOF Russian patent published in 2004 - IPC

FIELD: organic chemistry, chemical technology, medicine, pharmacy. SUBSTANCE: invention relates to novel derivatives of epotilone of the formula (I) wherein a bond designated by wavy line means that the bond "a" is in cis- or in trans-form; (A) R₂ is absent or means oxygen atom; "a" means a simple or double bond; "b" is absent or means a simple bond; "c" is absent or means a simple bond under condition that if R₂ means oxygen atom then "b' and "c" both mean a simple bond and "a" means a simple bond; if R₂ is absent then "b" and "c" both are absent and "a" means a double bond; if "a" means a double bond then R₂,, "b" and "c" are absent; R₃ means radical taken among the group comprising hydrogen atom, (lower)alkyl being first of all methyl, ethyl, n-propyl, isopropyl, n-butyl, isobutyl, tert.-butyl, n-pentyl, n- hexyl; -OH; R₄ and R₅ mean independently of one another hydrogen atom; R₁ means radical of formulas: (a) , (b) , (c) , (d) ; (B) if R₃ means (lower)alkyl being first of all methyl, ethyl, n-propyl, isopropyl, n-butyl, isobutyl, tert.-butyl, n-pentyl, n-hexyl, , -OH and other symbols with exception of R₁ have values indicated above in (A) then R_1/ can mean radical of formulas: (e) , (f) , (g) , (h) , (i) also; (C) if R₃ means -OH and other symbols with exception of R₁ have above indicated values then R₁ can mean fragment of the formula (j) also; or salt of compound of the formula (I) if salt-forming group presents. Invention relates to pharmaceutical composition eliciting proliferative effect and containing compound of the formula (I) and pharmaceutically acceptable carrier. Invention relates to method for preparing compound of the formula (I) involving interaction of iodide of the formula (II) , a, b and c and a bond designated by wavy line have values indicated above with tin- -containing compound of the formula R₂, R₃, R₄, R₅, wherein has values indicated above and R means (lower)alkyl, methyl or n-butyl. Invention relates to method for preparing compound of the formula (I) involving interaction of tin-containing compound of the formula (IV) R_1/ with iodide of the formula -I and if necessary the conversion of formed compound of the formula (I) to another compound of the formula (I), the conversion of formed free compound of the formula (I) to salt of compound of the formula (I) and/or the conversion of formed salt of compound of the formula (I) to free compound of the formula (I) to other salt of compound of the formula (I), and/or separation of mixture of stereoisomers of compound of the formula (I) for corresponding isomers. Invention provides preparing new compounds eliciting proliferative effect. EFFECT: improved preparing methods, valuable medicinal properties of compounds, improved treatment method. 18 cl, 3 tbl