MACROCYCLIC INTEGRASE INHIBITORS Russian patent published in 2015 - IPC C07D487/18 C07D498/18 C07D515/18 A61K31/529 A61P31/18 

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to a macrocyclic compound of general formula to its stereochemically isomer form, wherein R₁ represents F; R₂ represents H, F or Cl; R₃ represents C_1-4alkyl or cyclopropyl; R₄ represents methyl; J represents ---N(R₅)-SO₂-, ---C(=O)-N(R₅)-, ---N(R₅)-, or wherein a dashed line means an attachment point to a pyridazinone ring; K represents -(CHR₆)_P, or *-(CH₂)_q-CH=CH-CH₂-, wherein * means an attachment point to the group J; L represents -O-, -O-CH₂-* or -N(R₅)-C(=O)-*, wherein * means an attachment point to a phenyl ring; and R₅ represents hydrogen, C_1-4alkyl or C_3-5cycloalkyl; each R₆ independently represents hydrogen or C_1-3alkyl; p is equal to 3, 4, 5 or 6; q is equal to 2 or 3. The invention also refers to a pharmaceutical composition based on the compound of formula I and using the compound of formula I.

EFFECT: produced are the new macrocyclic compounds effective in treating or preventing HIV-infection.

13 cl, 6 tbl, 169 ex