DERIVATIVES OF VARIOLIN B, METHOD FOR THEIR PREPARING, INTERMEDIATE COMPOUNDS AND PHARMACEUTICAL COMPOSITION Russian patent published in 2007 - IPC C07D471/14 A61K31/519 A61P35/00 

FIELD: organic chemistry, chemical technology, medicine, oncology, pharmacy.

SUBSTANCE: invention relates to novel derivative of variolin B of the general formula (I) or their pharmaceutically acceptable salts possessing antitumor activity. In the general formula (I) radical R¹ means aromatic group representing aromatic group representing phenyl optionally substituted with nitro-group, amino-group or alkyl-substituted amino-group, or aromatic group represents 5-6-membered heterocycle with two nitrogen atoms or sulfur atom as heteroatoms optionally substituted with (C₁-C₁₂)-alkyl, -OH, unsubstituted amino-group or amino-group substituted with (C₁-C₄)-acyl, phenyl-(C₁-C₄)-alkyl wherein phenyl group can be substituted with -OR¹, or (C₁-C₁₂)-alkylthio-group, (C₁-C₁₂)-alkyl- or phenylsulfonyl, (C₁-C₁₂)-alkyl- or phenylsulfinyl or -OR¹ wherein R¹ is chosen from (C₁-C₁₂)-alkyl or phenyl; R² represents hydrogen atom; R³ represents oxo-group when a dotted line is between nitrogen atom to which R² is bound and carbon atom to which R³ is absent, or R² is absent when R³ represents optionally protected amino-group wherein a substitute is chosen from (C₁-C₄)-acyl, phenylsulfonyl and (C₁-C₄)-alkylphenylsulfonyl when a dotted line forms a double bond between nitrogen atom to which R² is bound and carbon atom to which R² is bound; R⁴ represent hydrogen atom. Also, invention relates to a method for synthesis of compounds of the invention and to intermediate substances for their realization. Also, invention relates to a pharmaceutical composition based on variolin B derivatives.

EFFECT: improved method of synthesis, valuable medicinal property of compounds and pharmaceutical composition.

22 cl, 5 sch, 1 tbl, 50 ex