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    2-amino-9-alkylpurines: GABA brain receptor ligands
    1.
    发明授权
    2-amino-9-alkylpurines: GABA brain receptor ligands 失效
    2-氨基-9-烷基嘌呤：GABA脑受体配体

    公开(公告)号：US06414147B1

    公开(公告)日：2002-07-02

    申请号：US09470940

    申请日：1999-12-22

    申请人： Kevin S. Currie ,  Pamela Albaugh ,  Paul Chen

    发明人： Kevin S. Currie ,  Pamela Albaugh ,  Paul Chen

    IPC分类号： C07D47318

    CPC分类号： C07D473/00 ,  C07D473/18 ,  C07D473/24

    摘要： Disclosed are compounds of the formula: or the pharmaceutically acceptable non-toxic salts thereof wherein: W is oxygen or sulfur; X is (un)substituted lower alkyl; or X is (un)substituted aryl or heteroaryl; Y is hydrogen or lower alkyl; Z is lower alkenyl, lower alkynyl, or (un)substituted lower alkyl; T is (un)substituted aryl or heteroaryl. The 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. Thus these compounds are useful in the diagnosis and treatment of anxiety, sleep and seizure disorders, Down's Syndrome, overdose with benzodiazepine drugs, and for the enhancement of memory.

    摘要翻译： 公开了下式的化合物或其药学上可接受的无毒盐，其中：W是氧或硫; X是（un）取代的低级烷基; 或者X是（未）取代的芳基或杂芳基; Y是氢或低级烷基; Z是低级烯基，低级炔基或（未）取代的低级烷基; T是（未）取代的芳基或杂芳基。该化合物是高度选择性的激动剂， 拮抗剂或GA​​BAa脑受体的反向激动剂，或GABAa脑受体的激动剂，拮抗剂或反向激动剂的前药。 因此，这些化合物可用于诊断和治疗焦虑症，睡眠和癫痫发作障碍，唐氏综合症，苯并二氮卓类药物过量以及增强记忆功能。

    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

    申请人： Scott A. Mitchell ,  Kevin S. Currie

    发明人： Scott A. Mitchell ,  Kevin S. Currie

    IPC分类号： A61K31/495

    CPC分类号： C07D471/04 ,  C07D487/04 ,  C07D491/107 ,  C07D498/04 ,  C07D498/08 ,  C07D519/00

    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。