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Novel heterocyclic derivatives as modulators of kinase activity
专利权人:
Merck Patent GmbH
发明人:
LAN, Ruoxi,HUCK, Bayard R.,CHEN, Xiaoling,XIAO, Yufang
申请号:
ES13802772
公开号:
ES2620119T3
申请日:
2013.11.15
申请国别(地区):
ES
年份:
2017
代理人:
摘要:
Compounds according to the following formula (I), ** Formula ** and pharmaceutically acceptable salts, solvates, solvates of salts, tautomers or stereoisomers, including mixtures thereof in all their proportions, wherein: X1 is N or CH, X2 is CH2 or NH, X3 is CH2 or CO, X4 is O, CH2 or NH, W is N or CH, R1 is Ar or Het, R2 is [C (R3) 2] pHet1 or [C (R3) 2] pN (R3) 2, R3 is H or alkyl with 1, 2, 3 or 4 carbon atoms, which is optionally substituted; Ar is phenyl that is unsubstituted or mono-, di- or trisubstituted by Hal, A, phenyl, CON (R3) 2, COOR3, NHCOA, NHSO2A, CHO, COA, SO2N (R3) 2, SO2A, [C (R3 ) 2] pOR3, [C (R3) 2] pN (R3) 2 and / or [C (R3) 2] pCN, Het is furyl, thienyl, pyrrolyl, imidazolyl, pyrazolyl, oxazolyl, isoxazolyl, oxadiazolyl, thiazolyl, triazolyl , tetrazolyl, pyridyl, pyrimidyl, pyridazinyl, pyrazinyl, indolyl, isoindolyl, benzimidazolyl, indazolyl or quinolyl, which is unsubstituted or mono-, di- or trisubstituted by Hal, A, [C (R3) 2] pOR3, [C ( R3) 2] pN (R3) 2, NO2, CN, [C (R3) 2] pCOOR3, CON (R3) 2, NR3COA, NR3SO2A, SO2NR3) 2, S (O) mA and / or O [C (R3 ) 2] qN (R3) 2, Het1 is dihydropyrrolyl, pyrrolidinyl, azetidinyl, oxetanyl, tetrahydroimidazolyl, dihydropyrazzolyl, tetrahydropyrazzolyl, tetrahydrofuranyl, dihydropyridyl, tetrahydropyridyl, piperidinyl, azepanyl, hepyrinyl, tetraphyrimyl, 1,3-dihydroxydiopyraxyl, thiopyrinoxyl, 1,3-dihydroxydiohylamino, thiopyrinoxyl, thiopyrinoxyl, thiopyrinoxyl, thiopyrinoxyl, thiopyrinoxyl, thiopyrinoxyl, thiopyrinoxyl, thiopyrinoxyl, thiopyrinoxyl, thiopyrinoxyl, [3] pyridyl or piperazinyl, which is unsubstituted or mono- or disusti A, A is unbranched or branched with 1-10 carbon atoms, where one or two non-adjacent CH- and / or CH2- groups can be replaced by N-, O- and / or S-atoms and in the that the atoms of H 1-7 can be replaced by F or Cl, Hal is F, Cl, Br or I, each m is independently 0, 1 or 2, each n is independently 0, 1 or 2, each p is independently 0, 1, 2, 3 or 4, each q is independently
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