PYRIDINE, QUINOLINE, AND ISOQUINOLINE N-OXIDES AS KINASE INHIBITORS
    5.
    发明申请
    PYRIDINE, QUINOLINE, AND ISOQUINOLINE N-OXIDES AS KINASE INHIBITORS 有权
    吡啶,喹啉和异喹啉N-氧化物作为激酶抑制剂

    公开(公告)号:US20070265315A1

    公开(公告)日:2007-11-15

    申请号:US11775457

    申请日:2007-07-10

    摘要: This invention relates to urea compounds containing a pyridine, quinoline, or isoquinoline functionality which is oxidized at the nitrogen heteroatom and which are useful in the treatment of (i) raf mediated diseases, for example, cancer, (ii) p38 mediated diseases such as inflammation and osteoporosis, and (iii) VEGF mediated diseases such as angogenesis disorders.

    摘要翻译: 本发明涉及含有吡啶,喹啉或异喹啉官能团的脲化合物,其在氮杂原子处被氧化并且可用于治疗(i)raf介导的疾病,例如癌症,(ii)p38介导的疾病,例如 炎症和骨质疏松症,和(iii)VEGF介导的疾病,如血管发生障碍。

    3-oxo-2,1-benzisoxazol-1(3H)-carboxamides for treatment of CNS diseases
    6.
    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

    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。