HIV-INHIBITING 5-CARBO- OR HETEROCYCLIC SUBSTITUTED PYRIMIDINES Russian patent published in 2010 - IPC C07D239/48 C07D401/12 C07D405/12 C07D409/12 C07D417/12 C07D239/50 A61K31/506 A61P31/18 

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to novel compounds, which possess properties inhibiting HIV replication, of general formula (I) , in form of E-isomer, in which -a¹=a²-a³=a⁴- represents bivalent radical of formula -CH=CH-CH=CH- (a-1); -b¹=b²-b³=b⁴. Represents bivalent radical of formula -CH=CH-CH=CH- (b-1); n equals 0; m equals 2; each of R¹ radicals independently on each other stands for hydrogen atom; C_1-6alkyl; R^2a stands for cyanogroup; X₁ stands for -NR¹-; R³ represents C_2-6alkenyl, substituted with cyanogroup; R⁴ stands for C_1-6alkyl; R⁵ represents radical of formula -Y-Alk-L, -Alk'-Y-L or -Alk'-Y-Alk-L; each of radicals Alk or Alk' independently represents bivalent C_1-6alkyl or C_2-6 alkenyl group; L stands for aryl or Het; Y stands for NR¹; -CH=N-O-; Het stands for 5- or 6-member fully saturated ring system, in which one, two or three ring elements represent heteroatoms, each of which is independently selected from group, including nitrogen, oxygen and sulphur, and in which other ring elements represent carbon atoms; and, if possible, any nitrogen ring element can be optionally substituted with C_1-6alkyl; and ring system can be optionally bound with benzene ring; and in which any carbon atom of ring, including any carbon atom of optionally bound benzene ring, each independently can be substituted with substituent selected from such groups as halogen atom, C_1-6alkyl, hydroxyC_1-4alkyl, carboxyC_1-4alkyl, C_1-4 alkylcarbonyloxyC_1-4alkyl, di(C_1-4alkyl)aminoC_1-4alkyl, aryloxy, morpholinyl, aryl, Het¹; Het¹ stands for thienyl, isoxazolyl, thiadiazolyl, each of which can be optionally substituted with one or two C_1-4alkyl radicals; Q stands for hydrogen atom; each aryl represents phenyl or phenyl, substituted with one, two substituents, each of which is independently selected from such groups as halogen atom, C_1-6alkyl, C_2-6alkinyl, cyano, polyhalogen C_1-6alkyl or Het¹, as well as to its pharmaceutically acceptable additive salts Invention also relates to pharmaceutical composition.

EFFECT: creation of novel compounds, which possess properties inhibiting HIV replication

5 cl, 7 tbl, 14 ex