HETEROCYCLIC ANTIVIRAL COMPOUNDS Russian patent published in 2013 - IPC C07D471/04 C07D487/04 A61K31/5025 A61K31/437 A61P31/12 A61P31/18 

FIELD: medicine.

SUBSTANCE: present invention describes compounds of formula I: wherein: X¹ and X² independently represent CH or N; R¹ represents fluorine or hydrogen; R² represents hydrogen, halogen; Ar represents phenyl substituted by 1-3 groups optionally substituted in each specific case in a group consisting of hydrogen, halogen, cyano group; R³ is independently specified in each specific case in a group consisting of: (i) CH₂OH; (ii) CH₂O-C(=O)(CH₂)_nCO₂R⁴, wherein n has a value of 2 to 5; (iii) CH₂O-C(=O)CH₂OCH₂CO₂R⁴; (iv) CH₂OCOR⁵; (v) CH₂OC(=O)CHR⁶NH₂; (vi) C(=O)R⁵, and (vii) CH₂OP(=O)(OH)₂; R⁴ represents hydrogen or C_1-10 alkyl; R⁵ represents hydrogen or C_1-10 alkyl, C_1-3 dialkylamino-C_1-10 alkyl, C_1-6 alkoxy or pyridinyl, R⁶ represents C_1-6 alkyl or a side chain of a natural amino acid; or a pharmaceutically acceptable salt thereof. Besides, the invention describes a pharmaceutical composition having HTVRT inhibitory activity and containing a compound according to cl.1.

EFFECT: there are prepared and described new compounds inhibiting HIV-1 reverse transcriptase and effective for preventing and treating HIV-1 infections and treating AIDS or ARC.

13 ex, 3 dwg