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Indazolyl-triazole derivatives as IRAK inhibitors
专利权人:
Merck Serono S.A.
发明人:
JORAND-LEBRUN, Catherine,CROSIGNANI, Stefano,DORBAIS, Jerome,GRIPPI-VALLOTTON, Tania,PRETRE, Adeline
申请号:
ES11801711
公开号:
ES2592713T3
申请日:
2011.12.16
申请国别(地区):
ES
年份:
2016
代理人:
摘要:
Compound of formula (I) ** Formula ** in which Q indicates Ar or Het, E indicates - (CH2) mCO-, - (CH2) mSO2, - (CH2) q-, - (CH2) mNHCO-, or a single bond, R1 indicates H, OH, NH-C1-C6 alkyl, O-C1-C6 alkyl, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, Cyc, Hal, Het1, OHet 1, CO- Het1, NH-Het1, CO-Ar1, O-Ar1, Ar1, NH-Ar1, - (CH2) qHet1, -CONH- (CH2) qHet1, -CONHHet1, - (CH2) qO-Het1, - (CH2) qO -Ar1, - (CH2) qAr1, -CONH- (CH2) qAr1, -CONH-Ar1, -CONH-C3-C6 cycloalkyl, - (CH2) qHal, - (CH2) qCyc, CF3, - (CH2) sNH- (CH2) q-Het1, - (CH2) sNH- (CH2) q-Ar110, in which NH-C1-C6 alkyl, O-C1-C6 alkyl, C1-C6 alkyl, C2-C6 alkenyl, C2 alkynyl C6, C3-C6 cycloalkyl may be substituted with 1 to 3 groups independently selected from O-C1-C3 alkyl, OH, CONH2, NH2, R2 indicates H, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, Hal, CF3, preferably H, R3 indicates Het1, Ar1, NRaRb, COOH, - (CH2) qHet1, - (CH2) qAr1, - (CH2) qNRaRb, - (CH2) qCOOH, or C1-C6 alkyl wherein 1 to 3 hydrogen atoms can e star independently substituted by OH or CF3. R4 indicates H, C1-C6 alkyl, C2-C6 alkenyl, Hal; Ra indicates H, linear, branched or cyclic C1-C6 alkyl, Rb indicates H, Hetb, Arb, -CO-Hetb, -CO-Arb, a C3-C8 cycloalkyl or a linear or branched alkyl having 1 to 6 atoms carbon, in which 1 to 3 hydrogen atoms may be substituted by Hetb, Arb, NH2, N (C1-C6 alkyl) 2, NH (C1-C6 alkyl), N (C1-C6 alkyl) (C3 cycloalkyl) -C8), NH (C3-C8 cycloalkyl), O (C1-C6 alkyl), CN, OH, CF3, Hal, n is 0, 1, 2, 3 or 4, m is 0, 1, 2, 3 or 4, q is 1, 2 or 3, s is 0, 1, 2 or 3, Hal indicates Cl, Br, I, F, preferably Cl or F, Ar indicates a divalent condensed bicyclic or monocyclic arylene group having 6 to 14 carbon atoms, which may be further substituted with 1 to 4 substituents selected from Hal, C1-C6 alkyl, - (CH2) mC1-C6 alkyl, CN, OH, NO2, CF3, - (CH2) mCOOH, - ( CH2) mCOO-C1-C6 alkyl; Het indicates an unsaturated, saturated or aromatic, bicyclic condensed or monocyclic divalent heterocyclic group having 1 to 5 heteroatoms i
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