PYRIMIDINE SUBSTITUTED MACROCYCLIC HCV INHIBITORS Russian patent published in 2013 - IPC C07D403/12 C07D487/04 A61K31/40 A61P31/12 

FIELD: medicine, pharmaceutics.

SUBSTANCE: there are described new pyrimidine substituted macrocyclic compounds of genral formula (I) , wherein A= -C(=O)OR¹ or -C(=O)-NH-SO₂-R²; R¹ = H or C_1-6alkyl; R² = phenyl, thienyl, C_3-7cycloalkyl optionally substituted by C_1-6alkyl; X = N or CH; E = NR⁵; R⁵ = H or C_1-6alkyl; n = 4 or 5; R⁷=H, C_1-6alkyl, C_1-6alkoxy, phenyl optionally substituted by C_1-6alkoxy; R⁸ =C_1-6alkoxy, phenyl optionally substituted by C_1-6alkoxy, morpholino or -NR^aR^b, wherein R^a and R^b independently mean H or C_1-6alkyl; R⁹ = R^q = H; or their pharmaceutically acceptable addition salts, or stereoisomers, and pharmaceutical compositions containing them.

EFFECT: compounds are inhibitors of HCV NS3 serine protease and can find application in treating chronic hepatic disorders, particularly chronic hepatitis.

10 cl, 1 tbl, 25 ex