DIHYDROQUINONE AND DIHYDRONAPHTHYRIDINE INHIBITORS OF JNK KINASE Russian patent published in 2012 - IPC C07D215/48 C07D401/06 C07D401/12 C07D405/06 C07D405/12 C07D413/04 C07D471/04 A61K31/4375 A61K31/4709 A61P37/00 A61P29/00 A61P3/00 A61P25/00 

FIELD: chemistry.

SUBSTANCE: invention relates to novel derivatives of dihydroquinone and dihydronaphthyridinone of formula (I) or to its pharmaceutically acceptable salts, in which X represents group CR¹¹ or N; Y represents group -C(O)R³, oxazolyl or isoxazolyl; Z represents phenyl, pyrrolidinyl, piperidinyl, morpholinyl, tetrahydropyranyl, pyridinyl, pyrimidinyl or pyrazolyl, and is substituted with groups R¹ and R²; R¹ and R² each independently represents H, halogen, CN group, C_1-6alkyl or group -Y¹-Y²-Y³-R⁸, or R¹ and R² together form group -O(CH₂)_nO-, where n represents 1 or 2; Y¹ represents group -O-, -C(O)-, -C(O)O-, -C(O)NR⁹-, -NR⁹C(O), -S-, -SO₂- or bond; Y² represents heterocycloalkylene, C_1-6alkylene or bond, where heterocycloalkylene stands for cycloalkylene group, in which one, two carbon atoms are substituted with heteroatoms O or N, where heterocycloalkylene group also contains, at least, two carbon atoms and cycloalkylene represents ; Y³ represents group -O-, -C(O)-, -C(O)O-, -C(O)NR⁹-, -NR⁹C(O)-, -SO₂- or bond; R⁸ represents H, C_1-6alkyl, C_1-6alkoxy, cyclohexyl, pyrrolidinyl, piperidinyl, morpholinyl, piperazinyl, tetrahydropyranyl, or group -NR⁹R¹⁰, where R⁸, different from H, is optionally substituted with C_1-6alkyl, halogen, group -CF₃ or group -OH; R⁹ and R¹⁰ each independently represents H or C_1-6alkyl; R³ represents OH, C_1-6alkyl, C_1-6alkoxy, (C_1-6alkoxy)-C_1-6alkoxy; R⁴ represents C_1-6alkyl, phenyl, cyclopropyl, cyclobutyl, cyclobutyl, cyclohexyl, tetrahydropyranyl or tetrahydrothiophene 1,1 -dioxide, and is optionally substituted with C_1-6alkyl, hydroxyl group, C_1-6alkoxy, halogen, nitro group, amino group, cyano group or halo-lower alkyl; R⁵ and R⁶ each independently represents H, halogen, C_1-6alkyl, group -CF₃, C_1-6alkoxy; R⁷ represents H; R¹¹ represents H. Invention also re4lates to pharmaceutical composition based on formula (I) compound.

EFFECT: obtained are novel dihydroquinone and dihydronaphthyridinone derivatives, useful for treatment of disease mediated by JNK kinase.

9 cl, 4 tbl, 38 ex