DERIVATIVES OF BORRELIDIN AND PHARMACEUTICAL COMPOSITION BASED ON THEREOF Russian patent published in 2005 - IPC

FIELD: organic chemistry, medicine, pharmacy.

SUBSTANCE: invention relates to new derivatives of borrelidin of the general formula (I)

wherein R represents the group of the general formulae -COOR¹, -CONR²R³, -CONR⁴CONR²R⁵ or -CH₂OR⁶ wherein R¹ represents (C₂-C₆)-alkyl group, (C₁-C₆)-alkyl group substituted with hydroxyl group or 5-8-membered saturated nitrogen-containing heterocyclic group (it can comprise oxygen atom in addition to nitrogen atom) or 5-6-membered nitrogen-containing aromatic heterocyclic group or (C₃-C₆)-cycloalkyl group; R² and R³ are similar or different and represent independently hydrogen atom or (C₁-C₆)-alkyl group that can be substituted optionally with hydroxyl, (C₂-C₅)-alkoxycarbonyl or 5-8-membered saturated nitrogen-containing heterocyclic group (it can comprises oxygen atom in addition to nitrogen atom) or 5-6-membered aromatic homocyclic group or aromatic heterocyclic group comprising oxygen and/or nitrogen atom, 5-6-membered cycloalkyl or heteroaryl group; R⁴ and R⁵ are similar or different and represent independently hydrogen atom or (C₃-C₆)-cycloalkyl group; R⁶ represents hydrogen atom; also, invention relates to tautomers, solvates of these compounds, their mixtures and acid-additive salts. Also, invention relates to pharmaceutical compositions comprising compounds of the general formula (I) as an active component. Angiogenesis inhibitors of the present invention inhibit formation of new vessels in tissues of live organisms and can be used for prophylaxis and inhibition of the angiogenesis process arising in the tumor proliferation, and for prophylaxis of formation of tumor metastasis. Invention provides preparing new derivatives of borrelidin eliciting the value physiological effect.

EFFECT: valuable medicinal properties of compounds.

8 cl, 15 ex