NEUE 3-OXO-2,1-BENZISOXAZOL-1(3H)-CARBOXAMIDE ZUR BEHANDLUNG VON ZNS-ERKRANKUNGEN
    3.
    发明公开
    NEUE 3-OXO-2,1-BENZISOXAZOL-1(3H)-CARBOXAMIDE ZUR BEHANDLUNG VON ZNS-ERKRANKUNGEN 审中-公开
    NEW -3-氧代-2,1-苯并异恶唑-1(3H)羧酰胺FOR CNS障碍的治疗

    公开(公告)号:EP1242394A1

    公开(公告)日:2002-09-25

    申请号:EP00983231.2

    申请日:2000-12-06

    CPC分类号: C07D261/20

    摘要: The invention relates to novel 3-oxo-2,1-benzisoxazol-1(3H)-carboxamides (I), where R1, R2 are the same or different and independently = H, halogen, C¿1? C6 alkyl, C1 C6 alkoxy, C1 C3 perfluoroalkyl, or a group NR?5R6; R3, R4¿ are the same or different and independently = C¿1? C8 alkyl, whose carbon chain is optionally interrupted by an O, S or NR?7¿ and is optionally singly or severally substituted by C¿3? C6 cycloalkyl, C1 C4 alkoxy, OH, halogen or NR?8R9; C¿3 C8 cycloalkyl whose carbon chain is optionally interrupted by an O, S or NR10 and is optionally singly or severally substituted by C¿1? C4 alkoxy, OH, halogen or NR?11R12; or R3 and R4¿ together with a nitrogen atom form a saturated or partially unsaturated 3- to 10-membered mono- or bi-cyclic heterocycle, which, optionally, contains up to two further heteroatoms, from N, O or S and is, optionally, substituted by C¿1? C4 alkyl, C1 C4 alkoxy, OH, halogen, COOR?13 or NR14R15¿and X = O or S. The invention further relates to methods for production thereof and use thereof in the production of medicaments for the prophylaxis and/or treatment of diseases of the central nervous system, in particular, cognitive disorders, such as Alzheimer's disease and other forms of dementia, cerebral infarct, skull and brain trauma and pain.