XANTHINE-PHOSPHODIESTERASE V INHIBITORS, METHOD OF PREPARATION THEREOF, PHARMACEUTICAL COMPOSITION, USE, AND TREATMENT METHOD Russian patent published in 2007 - IPC C07D473/04 A61K31/522 A61P15/00 A61P9/00 

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, -SO_0-2R⁵⁰, -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