Substituted 4-oxo-quinoline-3-carboxamides
    1.
    发明授权
    Substituted 4-oxo-quinoline-3-carboxamides 失效
    取代的4-氧代 - 喹啉-3-甲酰胺

    公开(公告)号:US06413956B1

    公开(公告)日:2002-07-02

    申请号:US09565529

    申请日:2000-05-05

    IPC分类号: C07D40112

    摘要: Disclosed are compounds of Formula I: or the pharmaceutically acceptable salts thereof where, R1, R2, and W are defined herein. These compounds are highly selective agonists, antagonists or inverse agonists for GABAa brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABAa brain receptors and are therefore useful in the diagnosis and treatment of anxiety, depression, Down Syndrome, sleep and seizure disorders, overdose with benzodiazepine drugs and for enhancement of memory. Pharmaceutical compositions, including packaged pharmaceutical compositions, are further provided. Compounds of the invention are also useful as probes for the localization of GABAA receptors in tissue samples.

    摘要翻译: 公开了式I的化合物或其药学上可接受的盐,其中R1,R2和W如本文所定义。 这些化合物是GABAa脑受体的高度选择性激动剂,拮抗剂或反向激动剂或GABAa脑受体的激动剂,拮抗剂或反向激动剂的前药,因此可用于诊断和治疗焦虑症,抑郁症,唐氏综合征,睡眠和发作障碍, 过量与苯二氮卓类药物和增强记忆。 还提供药物组合物,包括包装的药物组合物。 本发明的化合物也可用作组织样品中GABA A受体定位的探针。

    6-(1H-indazol-6-yl)-N-[4-(morpholin-4-yl)phenyl]imidazo-[1,2-A]pyrazin-8-amine, or a pharmaceutically acceptable salt thereof, as a SYK inhibitor
    10.
    发明授权
    6-(1H-indazol-6-yl)-N-[4-(morpholin-4-yl)phenyl]imidazo-[1,2-A]pyrazin-8-amine, or a pharmaceutically acceptable salt thereof, as a SYK inhibitor 有权
    6-(1H-吲唑-6-基)-N- [4-(吗啉-4-基)苯基]咪唑并[1,2-A]吡嗪-8-胺或其药学上可接受的盐,为 SYK抑制剂

    公开(公告)号:US08450321B2

    公开(公告)日:2013-05-28

    申请号:US13441441

    申请日:2012-04-06

    IPC分类号: A61K31/495

    摘要: An imidazopyrazine having the structure or a pharmaceutically acceptable salt thereof, and pharmaceutical compositions thereof are provided herein. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of Syk activity, which comprises administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are provided. Also provided are methods for determining the presence or absence of Syk kinase in a sample.

    摘要翻译: 本文提供具有结构或其药学上可接受的盐的咪唑并嗪及其药物组合物。 治疗患有某些对抑制Syk活性有作用的疾病和病症的患者的方法,其包括给予这些患者一定量的至少一种有效减少疾病或病症体征或症状的化学实​​体。 还提供了用于确定样品中Syk激酶的存在或不存在的方法。