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FURO[3,2-B]- AND THIENO[3,2-B]PYRIDINE DERIVATIVES AS TBK1 AND IKKε INHIBITORS
专利权人:
Merck Patent GmbH
发明人:
EGGENVAJLER Khans-Mikhael (DE),ЭГГЕНВАЙЛЕР Ханс-Михаэль (DE),KHELTSEMANN Gyunter (DE),ХЁЛЬЦЕМАНН Гюнтер (DE),DORSH Diter (DE),ДОРШ Дитер (DE),EGGENVAJLER Khans-Mikhael,ЭГГЕНВАЙЛЕР Ханс-Михаэль,KHELTSEMANN Gyunter,ХЁЛЬЦЕМАНН Гюнтер,DORSH Diter,ДОРШ Дитер
申请号:
RU2014136366
公开号:
RU0002622034C2
申请日:
2013.01.03
申请国别(地区):
RU
年份:
2017
代理人:
摘要:
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 exИзобретение относится к новому соединению формулы I, в которой X означает О или S,R1 означает O(CYY)nHet1 или O(CYY)nCyc, R2 означает Ar или Het2, Het1 означает пирролидинил, тетрагидроимидазолил, дигидропиразолил, тетрагидропиразолил, тетрагидропиранил, дигидропиридил, тетрагидропиридил, пиперидинил, морфолинил, гексагидропиримидинил, азепанил, тетрагидрофуранил, фурил, тиенил, пиразолил, пиридил, хроманил или пиперазинил, к
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