| abstract |
The present invention relates to a novel compound that exhibits antiviral activity, and more particularly inhibitory activity toward the integrase of the human immunodeficiency virus (HIV). The subject matter of the present invention is a novel annelated 9-hydroxy-1,8-dioxo-1,3,4,8-tetrahydro-2Н-pyrido[1,2-α]pyrazine-7-carboxamide having the general formula 1 and 2, and its stereoisomer, pharmaceutically acceptable salt, solvate and crystalline or polycrystalline form (I) and (II), where: ring А1 is an optionally methyl-substituted 5-7 membered saturated heterocycle or bicyclic heterocycle, ring А2 is a 5-6 membered optionally methyl-substituted saturated or partially saturated monocyclic heterocycle, ring А3 is a 5-6 membered monocyclic saturated cycloalkane and tetrahydro-2H-pyran, R is a 5-7 membered monocyclic or bicyclic heterocyclic radical, optionally substituted by one, two or three optionally identical substituents, which includes 1-4 heteroatoms selected from the group consisting of O, S and N, excluding (2S,5R,13aS)-8-hydroxy-7,9-dioxo-N-{[3-(trifluoromethyl)-pyridine-2-yl]methyl}-2,3,4,5,7,9,13,13а-octahydro-2,5-methanopyrido[1',2':4,5]pyrazino[2,1-b][1,3]oxazepino-10-carboxamide (formula А4) and (1R,4S,12aR)-N-[(3,5-difluoropyridine-2-yl)methyl]-7-hydroxy-6,8-dioxo-1,2,3,4,6,8,12,12а-octahydro-1,4-methanodipyrido[1,2-α:1',2'-d]pyrazine-9-carboxamide (formula А5). |