FLAVONE, XANTHONE AND COUMARONE DERIVATIVES AND PHARMACEUTICAL COMPOSITION BASED ON THE SAME Russian patent published in 2005 - IPC

FIELD: organic chemistry, pharmacology.

SUBSTANCE: invention relates to new flavone, xanthone and coumarone derivatives of formula I

[R and R¹ each are independently lower C₁-C₆-alkyl or together with nitrogen atom attached thereto form 4-8-membered heterocycle, optionally containing one or more heteroatoms, selected from group comprising N or O, wherein said heterocycle is optionally substituted with benzyl; Z has formula (A) , wherein R³ and R4 each are independently hydrogen, optionally substituted aromatic group containing in cyclic structure from 5 to 10 carbon atoms, wherein substituents are the same or different and represent lower C₁-C₄-alkyl, OR¹⁰ (OR¹⁰ is hydrogen, saturated or unsaturated lower C₁-C₆-alkyl or formula ) or linear or branched C₁-C₆-hydrocarbon; or R² and R³ together with carbon atom attached thereto form 5-6-membered carbocycle; and R⁴ represents hydrogen or attaching site of group –OCH₂-C≡CCH₂NRR¹; or formula (B) , wherein R⁵ is hydrogen, linear or branched lower C1-C6-hydrocarbon, with the proviso, that when Z represents R and R¹ both are not methyl or R and R¹ together with nitrogen atom attached thereto cannot form groups , or ]. Also disclosed are drug component with proliferative activity for prophylaxis or treatment of neoplasm and pharmaceutical composition with proliferative activity based on the same. Derivatives of present invention have antyproliferative properties and are useful as modulators of drug resistance in cancer chemotherapy; as well as in pharmaceuticals for prophylaxis or treatment of neoplasm, climacteric disorders or osteoporosis.

EFFECT: new compounds with value bioactive effect.

31 cl, 2 tbl, 32 ex