TETRAHYDRO-4N-PYRIDO[1,2-a]PYRIMIDINE AND RELATED COMPOUNDS, USED AS INHIBITORS OF HIV-INTEGRASE Russian patent published in 2008 - IPC C07D471/04 A61K31/519 A61P31/18 

FIELD: chemistry.

SUBSTANCE: invention pertains to compounds with general formulae (I) and (II) and their pharmaceutical salts, their use as inhibitors of HIV-integrase and to pharmaceutical salts based on them. In formula (I) , R¹ represents H or NR²R⁵; R² represents CH₃; R⁵ represents 1) C(O)CH₂SO₂CH₃, 2) C(O)C(O)N(CH₃)₂, 3) SO₂N(CH₃)₂ or 4) SO₂R²⁰ where R²⁰ represents , , or ; or alternatively, R² and R⁵ together with a nitrogen atom, to which they are bonded, form or , R³ represents hydrogen; R⁴ represents 1) n-fluorobenzyl, 2) 4-fluro-3-methylbenzyl, 3) 3-chlorobenzyl or 4) 3-chloro-4-methylbenzyl; R¹² and R¹⁴ both represent H, except that, when R⁵ represents C(O)C(O)N(CH₃)₂ and R⁴ represents n-fluorobenzyl, and n equals 1, then R¹² and R¹⁴ both represent H, or both represent CH₃; and n is an integer, equal to 0, 1 or 2.

EFFECT: compounds can be used for treating HIV-infection.

12 cl, 5 dwg, 1 tbl, 8 ex