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New imidazol-piperidinyl 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:
ES13798851
公开号:
ES2656096T3
申请日:
2013.11.15
申请国别(地区):
ES
年份:
2018
代理人:
摘要:
Compound according to the following formula (I), ** Formula ** or a pharmaceutically acceptable salt, solvate, solvate salt, tautomer or stereoisomer thereof, where: X1 is N or CH, X2 is CH2 or NH, X3 is CH2, X4 is O, CH2 or NH, R1 is Ar, Het, or unbranched or branched alkyl with 1-10 C atoms, each of which is substituted with 1-6 of 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; R2 is [C (R3) 2] pHet1 or A, R3 is H or alkyl with 1, 2, 3 or 4 C atoms, 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, benzimdazolyl or inocyl ozolyl is not substituted or is 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, SO2N (R3) 2, S (O) mA and / or O [C (R3) 2] qN (R3) 2, Het1 is dihydropyrrolyl, pyrrolidinyl, azetidinyl, oxetanyl, tetrahydroimidazolyl, dihydropyrazzolyl, tetrahydropyrazolyl, tetrahydrofuranyl, dihydropyridyl, tetrahydropyridyl, piperidinyl, azepanyl, morpholinyl, hexahydro-pyridazinyl, hexahydropyrimidinyl, [1,3] dioxolanyl, tetrahydropyr anyl, pyridyl or piperazinyl, which is not substituted or mono or disubstituted by A, A is unbranched or branched alkyl with 1-10 C atoms, wherein one or two non-adjacent CH- and / or CH2 groups can be replaced by N-, O- and / or atoms of S and where 1-7 atoms of H- 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 2, 3 or 4.Compuesto de acuerdo con la siguiente fórmula (I),*
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