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    • 4. 发明授权
    • 3-oxo-2,1-benzisoxazol-1(3H)-carboxamides for treatment of CNS diseases
    • 3-氧代-2,1-苯并异恶唑-1(3H) - 甲酰胺,用于治疗CNS疾病
    • US06589949B1
    • 2003-07-08
    • US10149658
    • 2002-10-22
    • Toshiya MoriwakiChantal FürstnerBernd RiedlJens-Kerim ErgüdenFrank BössBernard SchmidtFranz-Josef van der StaayWerner SchröderKarl-Heinz SchlemmerNagahiro Yoshida
    • Toshiya MoriwakiChantal FürstnerBernd RiedlJens-Kerim ErgüdenFrank BössBernard SchmidtFranz-Josef van der StaayWerner SchröderKarl-Heinz SchlemmerNagahiro Yoshida
    • A61K315377
    • C07D261/20
    • 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.
    • 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。