发明名称 QUINAZOLINONE AND ISOQUINOLINONE ACETAMIDE DERIVATIVES
摘要 The present invention relates to a quinazolinone or isoquinolinone derivative of formula I, wherein R1 is C1-6alkyl, C3-6cycloalkyl, C3-6cycloalkylC1-3alkyl, C2-6alkenyl, C2-6alkynyl, said C1-6alkyl, C3-6cycloalkyl and C3-6cycloalkylC1-3alkyl being optionally substituted with hydroxy, C1-6alkyloxy, cyano or one or more halogens; R2 is C6-10aryl optionally substituted with one to three substituents selected from halogen, hydroxy, cyano, C1-6alkyl, C3-6cycloalkyl, C1-6alkyloxy and C3-6cycloalkyloxy, said C1-6alkyl, C3-6 cycloalkyl, C1-6 alkyloxy and C3-6Cycloalkyloxy being optionally substituted with one or more halogens; or R2 is a 5-10 membered heteroaryl ring system comprising a heteroatom selected from N, O and S and optionally substituted with a substituent selected from methyl, C1-6alkyloxy and halogen; or R2 is C4-7cycloalkyl; R3 is an optional substituent selected from C1-6alkyl, C1-6alkyloxy and halogen, said C1-6alkyl and C1-6alkyloxy being optionally substituted with one or more halogens; R4 is a group located at the 6- or 7- position of the quinazolinone or isoquinolinone ring having the formula Il, wherein R5 together with one of R6 forms a 4-8 membered saturated or unsaturated heterocyclic ring optionally comprising a further heteroatomic moiety selected from O, S and NR9, said heterocyclic ring being optionally substituted with one or two substituents selected from methyl, halogen, hydroxy and oxo or R5 together with one of R7 and R8 forms a 6-8 membered heterocyclic ring optionally substituted with one or two substituents selected from methyl, halogen, hydroxy and oxo; Each R6 is independently H, halogen or C1-4alkyl optionally substituted with halogen or SO2CH3 or one of R6 together with R5 forms a 4-8 membered saturated or unsaturated heterocyclic ring optionally comprising a further heteroatomic moiety selected from O, S and NR9, said heterocyclic ring being optionally substituted with one or two substituents selected from methyl, halogen, hydroxy and oxo; R7 and R8 are independently H, C1-6alkyl, C3-6cycloalkyl, C3-6cycloalkylc1-3alkyl, cyanoC1-3alkyl, C6-10aryl, C6-10arylC1-3alkyl, C1-3alkyloxyC1-3alkyl or C1-6acyl said C1-6alkyl, C3-6cycloalkyl and C3-6cycloalkylC1-3alkyl being optionally substituted with hydroxy, 1 or more halogens or diC1-2alkylamino; or R7 and R8 together with the nitrogen to which they are bonded form a 4-8 membered saturated or unsaturated heterocyclic ring optionally comprising a further heteroatomic moiety selected from O, S and NR10, said heterocyclic ring being optionally substituted with one or two substituents selected from C1-6alkyl, halogen, hydroxy,
申请公布号 CA2663161(C) 申请公布日期 2014.10.28
申请号 CA20072663161 申请日期 2007.09.10
申请人 N.V. ORGANON;PHARMACOPEIA, L.L.C. 发明人 LETOURNEAU, JEFFREY;JOKIEL, PATRICK;NAPIER, SUSAN ELIZABETH;HO, KOC-KAN;OHLMEYER, MICHAEL;MCARTHUR, DUNCAN ROBERT;JEREMIAH, FIONA;RATCLIFFE, PAUL DAVID;SCHULZ, JURGEN
分类号 C07D403/04;A61K31/517;A61K31/551;A61P25/22;A61P25/24;C07D471/08 主分类号 C07D403/04
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