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    DÉRIVÉS DE 1-0X0-1,2-DIHYDROISOQUINOLEINE-5-CARBOXAMIDES ET DE 4-OXO-3,4-DIHYDROQUINAZOLINE-8-CARBOXAMIDES, LEUR PRÉPARATION ET LEUR APPLICATION EN THÉRAPEUTIQUE
    2.
    发明公开
    DÉRIVÉS DE 1-0X0-1,2-DIHYDROISOQUINOLEINE-5-CARBOXAMIDES ET DE 4-OXO-3,4-DIHYDROQUINAZOLINE-8-CARBOXAMIDES, LEUR PRÉPARATION ET LEUR APPLICATION EN THÉRAPEUTIQUE 审中-公开
    1-氧代-1,2-二氢异喹啉-5-羧酰胺和4-氧代-3,4-二氢喹唑啉-8-甲酰胺，其制备方法及其在治疗中的应用衍生物

    公开(公告)号：EP2185523A2

    公开(公告)日：2010-05-19

    申请号：EP08835688.6

    申请日：2008-07-25

    申请人： Sanofi-Aventis

    发明人： EVERS, Michel ,  GENEVOIS-BORELLA, Arielle ,  KARLSSON, Andreas ,  MALLERON, Jean-Luc

    IPC分类号： C07D217/24 ,  C07D239/88 ,  A61K31/472 ,  A61K31/498 ,  A61P25/00 ,  A61K31/517 ,  A61P35/00 ,  A61P9/00

    CPC分类号： C07D217/24 ,  C07D239/88

    摘要： The invention relates to the derivatives of 1-oxo-1,2-dihydro­isoquinoline-5-carboxamides and of 4-oxo-3,4-dihydroquinazoline-8-carboxamides, of general formula (I) in which: R1 represents a hydrogen atom, a (C
    1 -C
    10 )alkyl, (C
    3 -C
    7 )cycloalkyl, (CH
    2 )
    n -(C
    1 -C
    6 )alkenyl, (CH
    2 )
    n -(C
    1 -C
    6 )alkynyl or (C
    1 -C
    6 )alkyl-Z-(C
    1 -C
    6 )alkyl group in which Z represents a heteroatom chosen from O, N and S(O)
    m , or else R1 represents a COOR or S(O)
    m R group, an aryl or an aralkyl, the (C
    1 -C
    10 )alkyl, (C
    3 -C
    7 )cycloalkyl, (CH
    2 )
    n -(C
    1 -C
    6 )alkenyl, (CH
    2 )
    n -(C
    1 -C
    6 )alkynyl, (C
    1 -C
    6 )alkyl-Z-(C
    1 -C
    6 )alkyl, aryl or aralkyl groups; R2 represents one or more groups chosen from a hydrogen atom, a halogen atom, a (C
    1 -C
    6 )alkyl, (C
    3 -C
    7 )cycloalkyl, (C
    1 -C
    6 )alkenyl, (C
    1 -C
    6 )alkynyl or (C
    1 -C
    6 )alkyl-Z-(C
    1 -C
    6 )alkyl group, in which Z represents a heteroatom chosen from O, N and S(O)
    m , or else R2 represents a halo(C
    1 -C
    6 )alkyl, halo(C
    1 -C
    6 )alkoxy, hydroxy, (C
    1 -C
    6 )alkoxy, nitro, cyano or amino group, an NR7R8, COOR, CONR7R8, OCO(C
    1 -C
    6 )alkyl or S(O)
    m -NR7R8 group, or an aryl group; R4 and R5 represent, independently of one another, a hydrogen atom, or else R4 and R5 form, with the carbon atom which bears them, a saturated ring containing from 3 to 6 carbon atoms and optionally containing from 0 to 1 heteroatoms chosen from O, N or S; R6 represents a group chosen from a hydrogen atom, a halogen atom, a (C
    1 -C
    6 )alkyl, (C
    3 -C
    7 )cycloalkyl or (C
    3 -C
    7 )cycloalkyl(C
    1 -C
    6 )alkyl group, a halo(C
    1 -C
    6 )alkyl, nitro or amino group, an NR7R8 or COOR group, an NR7(SO
    2 )R8 or CONR7R8 group, or an aryl group; X represents a carbon atom or a nitrogen atom; m represents an integer between 0 and 2 and n represents an integer between 1 and 6. The invention also relates to the method of producing said derivatives and the application thereof in therapeutics as β-secretase for treating neurodegenerative disorders such as Alzheimer's disease.

    DÉRIVÉS DE 1-OXO-ISOINDOLINE-4-CARBOXAMIDES ET DE 1-OXO-1,2,3,4-TETRAHYDROISOQUINOLEINE-5-CARBOXAMIDES, LEUR PRÉPARATION ET LEUR APPLICATION EN THÉRAPEUTIQUE
    4.
    发明公开
    DÉRIVÉS DE 1-OXO-ISOINDOLINE-4-CARBOXAMIDES ET DE 1-OXO-1,2,3,4-TETRAHYDROISOQUINOLEINE-5-CARBOXAMIDES, LEUR PRÉPARATION ET LEUR APPLICATION EN THÉRAPEUTIQUE 审中-公开
    1-氧代异二氢吲哚-4-甲酰胺和1-氧代-1,2,3,4-四氢异喹啉-5-甲酰胺衍生物及其制备和治疗用途

    公开(公告)号：EP2185511A2

    公开(公告)日：2010-05-19

    申请号：EP08835551.6

    申请日：2008-07-25

    申请人： Sanofi-Aventis

    发明人： BAUDOIN, Bernard ,  EVERS, Michel ,  GENEVOIS-BORELLA, Arielle ,  KARLSSON, Andreas ,  MALLERON, Jean-Luc ,  MATHIEU, Magali

    IPC分类号： C07D209/46 ,  C07D217/24 ,  C07D413/12 ,  A61K31/4035 ,  A61K31/472 ,  A61P25/00 ,  A61P9/00 ,  A61P35/00

    CPC分类号： C07D209/46 ,  C07D217/24 ,  C07D413/12

    摘要： The invention relates to 1-oxo-isoindoline-4-carboxamide and 1-oxo-1,2,3,4-tetrahydroisoquinoline-5-carboxamide derivatives of general formula (I) where: R1 = H, C
    1 -C
    10 alkyl, C
    3 -C
    7 cycloalkyl, (CH
    2 )
    n -(C
    1 -C
    6 )alkenyl, (CH
    2 )n-(C
    1 -C
    6 )alkynyl, (C
    1 -C
    6 )alkyl-Z-(C
    1 -C
    6 )alkyl, where Z = a heteroatom chosen from O, N and S(O)
    m , or R1 = COOR, S(O)
    m R, aryl or aralkyl, R2 = one or more of H, halogen, C
    1 -C
    6 alkyl, C
    3 -C
    7 cycloalkyl, C
    1 -C
    6 alkenyl, C
    1 -C
    6 alkynyl, C
    1 -C
    6 alkyl-Z-(C
    1 -C
    6 )alkyl, where Z = a heteroatom chosen from O, N and S(O)
    m , or R2 = halo(C
    1 -C
    6 )alkyl, C
    1 -C
    6 alkoxy, halo(C
    1 -C
    6 )alkoxy, hydroxy, nitro, cyano, amino, NR7R8, COOR, CONR7R8, O- CO(C
    1 -C
    6 )alkyl, S(O)
    m -NR7R8, aryl; R3 = trifluoromethyl;R4 and R5 independently = H, or R4 and R5 together with the carbon to which they are attached form a saturated ring with 3 to 6 C and optionally containing O to 1 heteroatoms chosen from O, N or S; R6 = H,halogen, C
    1 - C
    6 alkyl, C
    3 -C
    7 cycloalkyl, C
    3 -C
    7 cycloalkyl-(C
    1 -C
    6 )alkyl, halo(C
    1 -C
    6 )alkyl, nitro, amino, NR7R8, COOR, NR7(SO2)R8, CONR7R8, aryl or heterocycle; X = C
    1 -C
    2 alkylene; m = a whole number from O to 2 and n = a whole number from1 to 6. The invention further relates to a method for preparation and therapeutic application thereof as ß-secretase inhibitors for the treatment of neurodegenerative disorders such as Alzheimers.