SUBSTITUTED PYRIMIDINES AND USE THEREOF AS JNK MODULATORS Russian patent published in 2013 - IPC C07D403/04 C07D487/04 C07D471/04 A61K31/506 A61K31/416 A61K31/404 A61P29/00 A61P35/00 A61P25/00 

FIELD: chemistry.

SUBSTANCE: invention relates to novel pyrimidine derivatives of general formula (I), or pharmaceutically acceptable salts thereof, where X¹ denotes N, N-R³, C-R³ or O; X² denotes N, CH or C-CH₃; X³ denotes N or C, where X¹, X² and X³ all do not simultaneously denote N; X⁴, X⁵ each independently denotes C or N; X⁶ denotes N or C-R¹ ; where at least two and not more than four of X¹, X², X³, X⁴, X⁵ and X⁶ denotes N; and where the bonds between X¹ and X², X² and X³, X³ and X⁴, X⁴ and X⁵, X⁵ and X¹, as well as X⁵ and X⁶ can each independently be single or double, or , can form an aromatic ring, under the condition that a chemically stable structure is formed; R denotes -(cyclohexyl)R²; R¹ denotes a halide, nitro group, -CN, -CH₂CN, -OH, -NH₂, -COOH or -Y¹R⁴; Y¹ denotes -O-, -SO₂, -NHSO₂-, -C(O)O- or a bond; R⁴ denotes (C₁-C₆)alkyl, phenyl or benzyl, each of which is substituted with 0-3 times with a hydroxy group or a halogen; n equals 0, 1 or 2; R³ denotes H or (C₁-C₆)alkyl; R² denotes H, -OH, =O or -Y²-Y³-Y⁴-R⁵, where Y² denotes -C(O)-, -C(O)NR^a-, -NH- or a bond; Y³ denotes (C₁-C₆)alkylene or a bond; Y⁴ denotes -NR^a-, -S-, -SO₂-, -NR^aC(O)-, -NHSO₂- or a bond; R⁵ denotes (C₁-C₆)alkyl, (C₃-C₁₀)cycloalkyl, a 5-6-member heterocyclyl containing 1-2 heteroatoms selected from N and O, where R⁵ is optionally substituted with -OH or -NHR^a; where each R^a independently denotes hydrogen or (C₁-C₆)alkyl; Z denotes hydrogen. The invention also relates to a pharmaceutical composition based on a compound of formula (I).

EFFECT: obtaining novel pyrimidine derivatives which are useful for therapeutic or preventive treatment of a c-Jun N-terminal kinase-mediated disorder.

14 cl, 3 tbl, 26 ex