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    QUINAZOLINONE AND ISOQUINOLINONE ACETAMIDE DERIVATIVES
    96.
    发明公开
    QUINAZOLINONE AND ISOQUINOLINONE ACETAMIDE DERIVATIVES 有权
    CHINAZOLINON-和异喹啉酮的乙酰胺衍生物

    公开(公告)号：EP2069315A2

    公开(公告)日：2009-06-17

    申请号：EP07842157.5

    申请日：2007-09-10

    申请人： N.V. Organon

    发明人： LETOURNEAU, Jeffrey ,  JOKIEL, Patrick ,  NAPIER, Susan, Elizabeth ,  HO, Koc-Kan ,  OHLMEYER, Michael ,  MCARTHUR, Duncan Robert ,  FIONA, Jeremiah ,  RATCLIFFE, Paul David ,  JURGEN, Schulz

    IPC分类号： C07D239/70 ,  C07D243/08 ,  C07D217/24 ,  A61K31/519 ,  A61K31/5513 ,  A61K31/472 ,  A61K31/4725 ,  A61K31/496 ,  A61P25/24

    CPC分类号： C07D403/04 ,  C07D217/24 ,  C07D239/91 ,  C07D401/04 ,  C07D405/12 ,  C07D409/04 ,  C07D409/12 ,  C07D471/08 ,  C07D487/04

    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, C1-6alkyloxy, cyano and COOR11; or one of R7 and R8 is Y, CH2Y or CH2CH2Y, wherein Y is a 4-6 membered saturated heterocyclic ring comprising a heterocyclic moiety selected from O, SO2 and NR10, said ring being optionally substituted with 1 -2 substituents selected from methyl or halogen; or one of R7 or R8 together with R5 forms a 6-8 membered heterocyclic ring being optionally substituted with one or two substituents selected from methyl, halogen, hydroxy and oxo or one of R7 and R8 together with R12 forms a 4-8 membered saturated or unsaturated heterocyclic ring optionally comprising a further heteroato

    MALONAMIDE DERIVATIVES BLOCKING THE ACTIVTIY OF GAMMA-SECRETASE
    100.
    发明授权
    MALONAMIDE DERIVATIVES BLOCKING THE ACTIVTIY OF GAMMA-SECRETASE 有权
    γ-分泌BLOCKING MALONAMIDDERIVATE的活动

    公开(公告)号：EP1711470B1

    公开(公告)日：2009-04-15

    申请号：EP04764665.8

    申请日：2004-08-31

    申请人： F. Hoffmann-La Roche AG

    发明人： FLOHR, Alexander ,  GALLEY, Guido ,  JAKOB-ROETNE, Roland ,  KITAS, Eric, Argirios ,  PETERS, Jens-Uwe ,  WOSTL, Wolfgang

    IPC分类号： C07D223/18 ,  C07D223/16 ,  C07D243/14 ,  C07D313/14 ,  A61K31/5513 ,  A61K31/55

    CPC分类号： C07D223/16 ,  A61K31/335 ,  A61K31/55 ,  A61K31/5513 ,  C07D223/20 ,  C07D243/24 ,  C07D273/00 ,  C07D313/14

    摘要： The invention relates to malonamide derivatives of formula (I), wherein: R1 is one of the following groups (Formulae a), b), c), d)); R2 is lower alkyl, lower alkinyl, -(CH2)n-O-lower alkyl, -(CH2)n-S-lower alkyl, -(CH2)n-CN, -(CR'R')n-CF3, -(CR'R')n-CHF2, -(CR'R')n-CH2F, -(CH2)n-C(O)O-lower alkyl, -(CH2)n-halogen, or is -(CH2)n-cycloalkyl, optionally substituted by one or more substituents, selected from the group consisting of phenyl, halogen or CF3; R',R' are independently from n and from each other hydrogen, lower alkyl, lower alkoxy, halogen or hydroxy; R3, R4 are independently from each other hydrogen, lower alkyl, lower alkoxy, phenyl or halogen; R5 is hydrogen, lower alkyl, -(CH2)n-CF3 or -(CH2)n-cycloalkyl; R6 is hydrogen or halogen; R7 is hydrogen or lower alkyl; R8 is hydrogen, lower alkyl, lower alkinyl, -(CH2)n-CF3,-(CH2)n-cycloalkyl or -(CH2)n-phenyl, optionally substituted by halogen; R9 is hydrogen, lower alkyl, -C(O)H, -C(O)-lower alkyl, -C(O)-CF3,-C(O)-CH2F,-C(O)-CHF2,-C(O)-cycloalkyl,-C(O)-(CH2)n-O-lower alkyl,-C(O)O-(CH2)n-cycloalkyl, -C(O)-phenyl, optionally substituted by one or more substituents selected from the group consisting of halogen or -C(O)O-lower alkyl, or is -S(O)2-lower alkyl, -S(O)2-CF3,-(CH2)n-cycloalkyl or is -(CH2)n-phenyl, optionally substituted by halogen; n is 0, 1, 2, 3 or 4; and to pharmaceutically suitable acid addition salts, optically pure enantiomers, racemates or diastereomeric mixture thereof. These compounds may be used for the treatment of Alzheimer's disease.