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    3-oxo-2,1-benzisoxazol-1(3H)-carboxamides for treatment of CNS diseases
    8.
    发明授权
    3-oxo-2,1-benzisoxazol-1(3H)-carboxamides for treatment of CNS diseases 失效
    3-氧代-2,1-苯并异恶唑-1（3H） - 甲酰胺，用于治疗CNS疾病

    公开(公告)号：US06589949B1

    公开(公告)日：2003-07-08

    申请号：US10149658

    申请日：2002-10-22

    申请人： Toshiya Moriwaki ,  Chantal Fürstner ,  Bernd Riedl ,  Jens-Kerim Ergüden ,  Frank Böss ,  Bernard Schmidt ,  Franz-Josef van der Staay ,  Werner Schröder ,  Karl-Heinz Schlemmer ,  Nagahiro Yoshida

    发明人： Toshiya Moriwaki ,  Chantal Fürstner ,  Bernd Riedl ,  Jens-Kerim Ergüden ,  Frank Böss ,  Bernard Schmidt ,  Franz-Josef van der Staay ,  Werner Schröder ,  Karl-Heinz Schlemmer ,  Nagahiro Yoshida

    IPC分类号： A61K315377

    CPC分类号： C07D261/20

    摘要： The invention relates to novel 3-oxo-2,1-benzisomazol-1(3H)-carboxamides (I), where R1, R2 are the same or different and independently=H, halogen, C1 C6 alkyl C1 C6 alkoxy, C1 C3 perfluoroalkyl, or a group NR5R6; R3, R4 are the same or different and independently=C1 C8 alkyl, whose carbon chain is optionally interrupted by an O, S or NR7 and is optionally singly or severally substituted by C3 C6 cycloalkyl, C1 C4 alkoxy, OH, halogen or NR8R9; C3 C8 cycloalkyl whose carbon chain is optionally interrupted by an O, S or NR10 and is optionally singly or severally substituted by C1 C4 alkoxy, OH, halogen or NR11R12, or R3 and R4 together with a nitrogen atom form a saturated or partially unsaturated 3- to 10-membered mono- or bi-cyclic heteocycle, which, optionally, contains up to two further heteroatoms, from N, O or S and is, optionally, substituted by C1 C4 alkyl, C1 C4 alkoxy, OH, halogen, COOR13 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.

    摘要翻译： 本发明涉及新的3-氧代-2,1-苯并异恶唑-1（3H） - 甲酰胺（I），其中R 1，R 2相同或不同且独立地为H，卤素，C 1 -C 6烷基C 1 -C 6烷氧基，C 1 C 3 全氟烷基或NR5R6基团; R 3，R 4相同或不同且独立地为C 1 -C 8烷基，其碳链任选地被O，S或NR 7中断，并且任选地被C 3 -C 6环烷基，C 1 -C 4烷氧基，OH，卤素或NR 8 R 9单独或多个取代; C 8 -C 8环烷基，其碳链任选地被O，S或NR 10中断，并且任选地被C 1 -C 4烷氧基，OH，卤素或NR 11 R 12单独或多个取代，或者R 3和R 4与氮原子一起形成饱和或部分不饱和的3 至10元单环或双环杂环，其任选地含有至多两个另外的N，O或S的杂原子，并且任选地被C 1 -C 4烷基，C 1 -C 4烷氧基，OH，卤素，COOR 13 或NR14R15和X = O或S.本发明还涉及其生产方法及其在生产用于预防和/或治疗中枢神经系统疾病的药物中的用途，特别是认知障碍，例如阿尔茨海默病 疾病和其他形式的痴呆，脑梗塞，头骨和脑外伤和疼痛。