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21 条记录 (耗时 0.026 秒)

    Cyclic amine derivatives of substituted quinoxaline 2,3-diones as glutamate receptor antagonists
    2.
    发明授权
    Cyclic amine derivatives of substituted quinoxaline 2,3-diones as glutamate receptor antagonists 失效
    取代喹喔啉2,3-二酮的环胺衍生物作为谷氨酸受体拮抗剂

    公开(公告)号：US6110911A

    公开(公告)日：2000-08-29

    申请号：US272482

    申请日：1999-03-19

    申请人： Brian Edward Kornberg ,  Sham Shridhar Nikam ,  Michael Francis Rafferty ,  Po-Wai Yuen

    发明人： Brian Edward Kornberg ,  Sham Shridhar Nikam ,  Michael Francis Rafferty ,  Po-Wai Yuen

    IPC分类号： C07D241/44 ,  A61K31/4985 ,  A61K31/55

    CPC分类号： C07D241/44

    摘要： A novel series of substituted quinoxaline 2,3-diones useful as neuroprotective agents are taught. Novel intermediates, processes of preparation, and pharmaceutical compositions containing the compounds are also taught. The compounds are glutamate antagonists and are useful in the treatment of stroke, cerebral ischemia, or cerebral infarction resulting from thromboembolic or hemorrhagic stroke, cerebral vasospasms, hypoglycemia, cardiac arrest, status epilepticus, perinatal asphyxia, anoxia, seizure disorders, pain, Alzheimer's, Parkinson's, and Huntington's Diseases.

    摘要翻译： 教导了一系列用作神经保护剂的取代喹喔啉2,3-二酮。 还教导了新的中间体，制备方法和含有这些化合物的药物组合物。 这些化合物是谷氨酸拮抗剂，可用于治疗由血栓栓塞或出血性脑卒中，脑血管痉挛，低血糖症，心脏骤停，癫痫持续状态，围产期窒息，缺氧，癫痫发作，疼痛，阿尔茨海默病， 帕金森病和亨廷顿疾病。

    Tyrosine-derived compounds as calcium channel antagonists
    9.
    发明授权
    Tyrosine-derived compounds as calcium channel antagonists 失效
    酪氨酸衍生化合物作为钙通道拮抗剂

    公开(公告)号：US06180677B2

    公开(公告)日：2001-01-30

    申请号：US09381938

    申请日：1999-09-27

    申请人： Michael Francis Rafferty ,  Yuntao Song

    发明人： Michael Francis Rafferty ,  Yuntao Song

    IPC分类号： A61K3803

    CPC分类号： A61K31/4453 ,  A61K31/137 ,  A61K31/165 ,  A61K31/195

    摘要： The present invention provides compounds that block calcium channels and have the Formula I: and pharmaceutically acceptable salts, esters, and pro-drugs thereof, wherein R1 and R2 are independently H, phenylcyclopentylcarbonyl, C1-C7 alkyl, cyclohexylmethyl, benzyl, C1-C5 alkylbenzyl, or C1-C5 alkoxybenzyl, A is —C(O)— or —CH2—; R3 is H or —CH3; R4 is C1-C4 alkyl or piperidin-1-ylethyl; R5 is phenyl-(CH2)n—, C1-C4 alkylphenyl-(CH2)n—, or halophenyl-(CH2)n—; and n is 1 or 2. The present invention also provides pharmaceutical compositions containing the compounds of Formula I and methods of using them to treat stroke, cerebral ischemia, head trauma, and epilepsy.

    摘要翻译： 本发明提供了阻断钙通道并具有式I的化合物及其药学上可接受的盐，酯和前药，其中R 1和R 2独立地为H，苯基环戊基羰基，C 1 -C 7烷基，环己基甲基，苄基，C 1 -C 5烷基苄基 或C 1 -C 5烷氧基苄基，A是-C（O） - 或-CH 2 - ; R 3是H或-CH 3; R 4是C 1 -C 4烷基或哌啶-1-基乙基; R 5是苯基 - （CH 2） C 1 -C 4烷基苯基 - （CH 2）n - 或卤代苯基 - （CH 2）n - 并且n为1或2.本发明还提供了含有式I化合物的药物组合物及其用于治疗中风，脑缺血，头部创伤和癫痫的方法。