FIELD: synthesis of biologically active compounds.
SUBSTANCE: invention relates to novel compounds of general formula I possessing polycyclic xanthine-phosphodiesterase inhibitor properties, to a method of preparation thereof, and also to pharmaceutical composition based on these novel compounds and use of compounds for treatment of various disorders, symptoms, and maladies caused by xanthine-phosphodiesterase V, in particular erectile dysfunction. In compounds of general formula I: 
, R1 and R2, independently from each other, each represents branched or linear C1-C15-alkyl optionally substituted by one or several substituents selected from hydroxy, amino, alkylamino, di-C1-C4-alkylamino, and tri-C1-C4-alkylsilyloxy; benzyl optionally substituted by one or several substituents in benzene ring selected from C1-C4-alkoxy groups; R3 represents phenyl optionally substituted by one or several substituents, 6-membered nitrogen-containing heteroaryl group optionally substituted by one or several substituents, or 5-membered heterocyclic group with 1 or 2 oxygen heteroatoms, condensed with phenyl ring and optionally substituted by one or several substituents; R4 represents С3-С15-cycloalkyl group optionally substituted by one or several substituents; С3-С15-cycoalkenyl group optionally substituted by one or several substituents; 3-8-membered heterocyclylalkyl group or S-oxides thereof optionally substituted by one or several substituents; or indanyl group; wherein one or several substituents for all R3 and R4 groups represent, independently from each other, C1-C4-alkyl, phenyl, 6-membered nitrogen-containing heterocycle, hydroxy-C1-C4-alkyl, С1-С4-alkylthio-C1-C4-alkyl, carboxy-C1-C4-alkyl, mono-, di-, and trihalo-C1-C4-alkyl, mono-, di-, and trihalo-C1-C4-alkoxy, C1-C4-alkoxy, hydroxy, halogen, nitro, -COOR50, -SO0-2R50, -SO2NR50R51, and -OCOR50, where R50 and R51 independently represent hydrogen atom or branched or linear optionally substituted C1-C6-alkyl.
EFFECT: expanded synthetic possibilities in heterocyclic compounds area and increased choice of erectile dysfunction treating drugs.
35 cl, 2 tbl
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