HIV-INHIBITING 5-(HYDROXYMETHYLENE- AND AMINOMETHYLENE)SUBSTITUTED PYRIMIDINES Russian patent published in 2012 - IPC C07D417/06 C07D401/06 C07D239/48 C07D403/06 C07D513/04 C07D417/14 A61K31/506 A61P31/18 

FIELD: chemistry.

SUBSTANCE: invention relates to novel substituted pyrimidine derivatives, having HIV replication inhibiting properties, or pharmaceutically acceptable salts thereof. In formula (1): R¹ denotes hydrogen; R² and R³ independently denote hydrogen; R⁷ and R⁸ denote C_1-6alkyl; R⁴ denotes cyano; R⁹ denotes C_1-6alkyl optionally substituted with cyano, C_2-6alkenyl substituted with cyano, C_2-6alkynyl optionally substituted with cyano; R⁵ denotes C_1-6alkyl optionally substituted with Ar or Het; C_2-6alkenyl optionally substituted with Ar or Het; C_2-6alkynyl optionally substituted with Ar or Het; C_3-7cycloalkyl; Ar; Het; R⁶ denotes H, Het; Y denotes -OR¹¹, -NR¹²R¹³; R¹¹ denotes hydrogen or C_1-6alkyl optionally substituted with hydroxy, C_1-6alkoxy or pyridyl; R¹² denotes hydrogen or C_1-6alkyl; R¹³ denotes hydrogen or C_1-6alkyl; or R¹² and R¹³ together with a nitrogen atom, which is substituted by said two substitutes, form a morpholinyl; imidazolyl; X denotes -NR¹-; Het denotes 5- or 6-member completely saturated ring, where one or two ring members are heteroatoms, each independently selected from nitrogen and sulphur, and where the rest of the ring members are carbon atoms; and where any member of the heterocycle with a nitrogen heteroatom can optionally be substituted with C_1-6alkyl; where the 5- or 6-member ring can optionally be annelated with a benzene or thiophene ring; each aryl independently denotes phenyl or phenyl substituted with one substitute selected from C_1-6alkoxy.

EFFECT: high efficiency of using said compounds.

7 cl, 4 ex, 1 tbl