4-OXOQUINOLINE COMPOUND AND ITS USING AS HIV INTEGRASE INHIBITOR Russian patent published in 2006 - IPC C07D215/56 C07D401/06 C07D409/06 C07D417/06 A61K31/47 A61P31/12 A61P31/18 

FIELD: organic chemistry, biochemistry, medicine.

SUBSTANCE: invention relates to a new biologically active compound of 4-oxoquinoline that is useful as an anti-HIV agent and to its pharmaceutically acceptable salt. Invention describes an anti-HIV agent comprising compound of 4-oxoquinoline represented by the following formula [I] or its pharmaceutically acceptable salt as an active component wherein ring Cy represents phenyl group, naphthyl group or pyridyl group and each this group is substituted optionally with 1-5 substituted chosen from the following group A wherein A represents the group consisting of cyano-group, phenyl group, nitro-group, halogen atom, (C₁-C₄)-alkyl group, halogen-(C₁-C₄)-alkyl group, halogen-(C₁-C₄)-alkoxy-group, -OR^a1, -SR^a1, -NR^a1R^a2, -CONR^a1R^a2, -SO₂NR^a1R^a2, -NR^a1COR^a3, -SO₂R^a3, -NR^a1SO₂R^a3 and -COOR^a1 wherein R^a1 and R^a2 are similar or different and each represents hydrogen atom, (C₁-C₄)-alkyl group or benzyl group, and R^a3 represents (C₁-C₄)-alkyl group; R¹ represent a substitute chosen from the following group B, or (C₁-C₁₀)-alkyl group optionally substituted with 1-3 substitutes chosen from halogen atom and the following group B wherein the group B represents the group consisting of phenyl group optionally substituted with phenyl group or 1-5 halogen atoms; (C₃-C₆)-cycloalkyl group, imidazolyl group, benzothiophenyl group, thiazolyl group optionally substituted with 1-3 (C₁-C₆)-alkyl groups, morpholinyl group, pyridyl group, -OR^a4, -SR^a4, -NR^a4R^a5, -CONR^a4R^a5, -SO₂NR^a4R^a5, -COR^a6, -NR^a4COR^a6, -SO₂R^a6, -NR^a4SO₂R^a6, -COOR^a4 and -NR^a5COOR^a6 wherein R^a4 and R^a5 are similar or different and each represents hydrogen atom, (C₁-C₄)-alkyl group or phenyl group; R^a6 represents (C₁-C₄)-alkyl group; R² represents hydrogen atom or (C₁-C₄)-alkyl group; R³¹ represents hydrogen atom, cyano-group, hydroxy-group, halogen atom or (C₁-C₄)-alkoxy-group; X represents -C-R^32, and Y represents -C-R³³ or nitrogen atom wherein R³² and R³³ are similar or different and each represents hydrogen atom, cyano-group, halogen atom, pyrrolidinyl group, (C₁-C₁₀)-alkyl group optionally substituted with 1-3 halogen atoms, -OR^a7, -SR^a7, -NR^a7R^a8, -NR^a7COR^a9, -COOR^a10 or -N=CH-NR^a10R^a11 wherein R^a7 and R^a8 are similar or different and each represents hydrogen atom, phenyl group or (C₁-C₁₀)-alkyl group optionally substituted with (C₃-C₆)-cycloalkyl group or hydroxy-group; R^a9 represents (C₁-C₄)-alkyl group and R^a10 and R^a11 are similar or different and each represents hydrogen atom or (C₁-C₄)-alkyl group. Also, invention describes compound of the formula (III) given in the invention description, integrase inhibitor, antiviral agent, ant-HIV composition, anti-HIV agent, using compound of 4-oxoqionoline, method for inhibition of integrase activity, method for prophylaxis or treatment of viral infectious disease, pharmaceutical composition used for inhibition of integrase activity, antiviral composition and commercial package (variants). Invention provides the development of a pharmaceutical agent possessing inhibitory effect on activity of integrase.

EFFECT: valuable medicinal properties of compound, agent and composition.

40 cl, 7 tbl, 250 ex