NITROGEN-CONTAINING TRICYCLIC DERIVATIVES HAVING HIV REPLICATION INHIBITION ACTIVITY Russian patent published in 2020 - IPC C07D487/06 C07D513/06 A61K31/4985 A61K31/554 A61P31/12 A61P31/18 

FIELD: pharmaceuticals.

SUBSTANCE: invention relates to a compound of formula (I-1-1B) having HIV replication inhibiting activity and a based pharmaceutical composition. In general formula I-1-1B, R¹ is C1-C6 alkyl or halogen; R² is C1-C6 alkyloxy; R³ is phenyl, optionally substituted with halogen, C1-C6 alkyl and/or C1-C6 alkyloxy, 6-member non-aromatic carbocyclyl, optionally substituted with C1-C6 alkyl, 9-member aromatic heterocyclyl containing one S atom, 6-member non-aromatic heterocyclyl optionally substituted with C1-C6 alkyl, or 10-member non-aromatic heterocyclyl, optionally substituted with halogen or C1-C6 alkyl; R⁴ denotes hydrogen; R^3A is hydrogen or halogen; R^4A is C1-C6 alkyl, optionally substituted with halogen, hydroxy or methoxy, halogen, C2-C4 alkynyl or 3-member non-aromatic carbocyclyl; R^a is hydrogen, C1-C6 alkyl, halogen C1-C6 alkyl, C1-C6alkylamino C1-C6alkyl, diCl-C6alkylamino C1-C6alkyl, C1-C6alkyloxyC1-C6alkyl or C1-C6alkylsulfonyl; or R represents 5–10 membered aromatic heterocyclyl containing from 1 to 3 heteroatoms selected from N, S or O, optionally substituted with one or more groups selected from Substituent Group E, or 5–9-member non-aromatic heterocyclyl containing 1 to 3 heteroatoms selected from N, S or O, optionally substituted with one or more groups selected from substituent group E; where group of substitutes E is C1-C6alkyl, halogen, C1-C6alkyloxy, diCl-C6alkylamino C1-C6alkyloxy, C1-C6alkylaminoC1-C6alkyloxy, aminoC1-C6alkyloxy, 4–6-member non-aromatic heterocyclyl C1-C6alkyloxy, where non-aromatic heterocyclyl contains 1 to 2 heteroatoms selected from N and O; 4–6-member non-aromatic heterocyclyloxy, where the non-aromatic heterocyclyl contains 1 to 2 heteroatoms selected from N and O, optionally substituted with C1-C6alkyl; 5–6-member non-aromatic heterocyclyl, where non-aromatic heterocyclyl contains from 1 to 2 heteroatoms, selected from N and O, optionally substituted with alkyl and/or oxo; diC1-C6alkylamino C1-C6alkyl; C1-C6alkylamino C1-C6alkyl; 4-6-member non-aromatic heterocyclyl C1-C6alkyl, where the non-aromatic heterocyclyl contains 1 to 2 heteroatoms selected from N and O; each R^b independently represents hydrogen, C1-C6alkyl, halogen C1-C6alkyl or C1-C6alkyloxyC1-C6alkyl; and each R^c independently represents hydrogen, C1-C6alkyl, galogenS1-C6 alkyl or C1-C6 alkyl S6alkiloksiS1.

EFFECT: disclosed are nitrogen-containing tricyclic derivatives having HIV replication inhibiting activity.

19 cl, 76 tbl, 72 ex