ANELLATED 9-HYDROXY-1,8-DIOXO-1,3,4,8-TETRAHYDRO-2H-PYRIDO[1,2-A]PYRAZINE-7-CARBOXAMIDES - INTEGRASE INHIBITORS, METHODS FOR PREPARING AND USING THEREOF Russian patent published in 2020 - IPC C07D498/18 C07D498/14 C07D495/18 C07D495/14 A61K31/4985 A61K31/553 A61K31/537 A61K31/5365 A61K9/08 A61K9/19 A61P31/18 

FIELD: chemistry.

SUBSTANCE: present invention relates to novel anellated 9-hydroxy-1,8-dioxo-1,3,4,8-tetrahydro-2H-pyrido[1,2-a]pyrazine-7-carboxamide of general formula 1 or 2 and its stereoisomer, as well as to versions of its production method. In general formula 1 or 2

ring A¹ is optionally substituted with methyl 5–7-member saturated heterocycle or heterobicycle, ring A² is an optionally substituted with methyl saturated monocyclic heterocycle containing additionally an oxygen atom, ring A³ is 5–6 membered monocyclic saturated cycloalkane, R is optionally substituted with one, two or three substitutes 5–6-member monoheterocycle with 1–3 heteroatoms in ring or 8–10-member bicyclic heterocycle with 1–4 heteroatoms, where heteroatoms are selected from O, S, N and where substituents are selected from a halogen atom and C1-C3 alkyl. Preferably, the compound of general formula I, which is (3S,11aR)-6-hydroxy-N-[(2,6-difluoropyridin-3-yl)methyl]-3-methyl-5,7-dioxo-2,3,5,7,11,11a-hexahydro[1,3]oxazolo [3,2-a]pyrido[1,2-d]pyrazine-8-carboxamide (1.1.19), can be in form of a crystalline form having elementary cell parameters given in the claim.

EFFECT: compounds have antiviral activity on integrase of human immunodeficiency virus (HIV).

19 cl, 5 dwg, 4 tbl, 14 ex