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4-Oxadiazol-2-yl-indazoles as inhibitors of PI3 kinases
专利权人:
GLAXO GROUP LIMITED
发明人:
HAMBLIN, JULIE,HARRISON, ZOE,JONES, PAUL,KEELING, SUZANNE,LE, JOELLE,LUNNISS, CHRISTOPHER,PARR, NIGEL
申请号:
ES10706663
公开号:
ES2542551T3
申请日:
2010.03.05
申请国别(地区):
ES
年份:
2015
代理人:
摘要:
A compound of formula (I): ** Formula ** in which R 1 is 9 or 10 membered bicyclic heteroaryl, wherein the 9 or 10 membered bicyclic heteroaryl contains one to three heteroatoms independently selected from oxygen and nitrogen, and is optionally substituted with C1-6 alkyl, C3-6 cycloalkyl, halo, -CN or -NHSO2R5, or pyridinyl optionally substituted with one or two substituents independently selected from C1-6 alkyl, -OR6, halo and -NHSO2R7; X is -CH2NR2R3, C1-6 alkyl, -CH2phenyl, - (CH2) nOR10, -CH2SO2R11 or - (CH2) C3-6 cycloalkyl; R2 and R3, together with the nitrogen atom to which they are attached, bind to form a 6 or 7 membered heterocyclyl or a 9 or 10 membered bicyclic heterocyclyl in which the 6 or 7 membered heterocyclyl or the bicyclic heterocyclyl of 9 or 10 members optionally contains an oxygen atom, a sulfur atom or an additional nitrogen atom and is optionally substituted with one to three substituents independently selected from oxo, C1-6 alkyl, - (CH2) mNR8R9, phenyl optionally substituted with halo, and 6-membered heteroaryl in which the 6-membered heteroaryl contains one or two nitrogen atoms, a 7-membered bridged heterocyclyl in which the 7-membered bridged heterocyclyl optionally contains an additional nitrogen atom and is optionally substituted with one to three substituents independently selected from C1-6 alkyl, or a 10-membered bicyclic spiro heterocyclyl in which the spiro heterocyclyl 10-membered bicyclic optionally contains an oxygen atom, or R2 is hydrogen and R3 is C1-6 alkyl optionally substituted with one or two substituents independently selected from -OR12 and -NR13R14; R4 is hydrogen or methyl; each of R6, R12 and R15 is independently hydrogen or C1-4 alkyl; each of R5 and R7 is independently C1-6 alkyl or phenyl in which the phenyl is optionally substituted with one or two substituents independently selected from halo and -OR15; R8 and R9, together with the nitrogen atom to which they are attached, bind to form a 5- or 6-membered he
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