FURO[3,2-B]- AND THIENO[3,2-B]PYRIDINE DERIVATIVES AS TBK1 AND IKKε INHIBITORS Russian patent published in 2017 - IPC C07D491/04 C07D495/04 A61K31/4355 A61K31/4365 A61P35/00 A61P19/02 A61P17/06 A61P25/28 A61P27/00 

FIELD: pharmacology.

SUBSTANCE: invention relates to a novel compound of formula I , wherein X means O or S, R¹ means O(CYY)_nHet¹ or O(CYY)_nCyc, R² means Ar or Het², Het¹ means pyrrolidinyl, tetrahydro imidazolyl, dihydropyrazolyl, tetrahydropyrazolyl, tetrahydropyranyl, dihydropyridyl, tetrahydropyridyl, piperidinyl, morpholinyl, hexahydropyrimidinyl, azepanyl, tetrahydrofuranyl, furyl, thienyl, pyrazolyl, pyridyl, chromanyl or piperazinyl, each of which is unsubstituted or monosubstituted by A, COOA, OY and/or =O (carbonyl oxygen), Het² means mono- or bicyclic saturated, unsaturated or aromatic heterocycle which contains from 1 to 2 N, O and/or S atoms, which may be unsubstituted or monosubstituted by A, (CYY)_p-OY, (CYY)_p-Het¹, -CO-Het¹ and/or =O, Ar means phenyl, which is unsubstituted or monosubstituted by Hal, A, (CYY)_p-OY, (CYY)_p-Het¹, (CYY)_p-COOY, CO(CYY)_pNH₂, CO-NYA, CONY(CYY)_mNYCOOA, CO-Het¹, O(CYY)_p-NYY, CONY(CYY)_pHet¹ and/or CONH(CYY)_pNHCOA, Y means H or an alkyl, which contains 1, 2, 3 or 4 C-atom, A is an unbranched or branched alkyl that contains from 1 to 10 C-atoms, Cyc means a cycloalkyl, which contains from 3 to 7 C-atoms, which is unsubstituted or monosubstituted by A, Hal means F, Cl, Br or I, n means 0, 1 or 2, m means 1, 2 or 3, p means 0, 1, 2, 3, or 4 and pharmaceutically applicable salts and stereoisomers thereof, including mixtures thereof in all ratios.

EFFECT: compounds are inhibitors of TVK1 and ε IKK, and can be used in particular for the treatment of malignant neoplasms and inflammatory diseases.

6 cl, 3 tbl, 120 ex