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Non-competitive NMDA receptor antagonists

机译:非竞争性NMDA受体拮抗剂

摘要

Disclosed herein are non-competitive NMDA receptor antagonists having chemical structures similar to that of phencyclidine (PCP). These antagonists contain a polycyclic ring structure in place of the cycloalkyl ring of PCP. The antagonists also differ from PCP in that they include an electron withdrawing group, a hydroxyl group, or an amine group at the para position of the phenyl ring. The antagonists disclosed herein are useful for treating or ameliorating a symptom of ailments associated with over excitation of cells (e.g., neurons) that express NMDA receptors. Examples of ailments that can be treated and for which symptoms can be ameliorated include epilepsy, neurodegenerative disease (e.g., Alzheimer's and Parkinson's diseases), drug addiction, neuropathic pain, and neuronal and glutamate-dependent tumors.
机译:本文公开了具有与苯环利定(PCP)相似的化学结构的非竞争性NMDA受体拮抗剂。这些拮抗剂包含多环结构代替PCP的环烷基环。拮抗剂与PCP的不同之处还在于它们在苯环的对位包含吸电子基团,羟基或胺基。本文公开的拮抗剂可用于治疗或缓解与表达NMDA受体的细胞(例如神经元)过度兴奋有关的疾病症状。可以治疗并且可以减轻症状的疾病的例子包括癫痫,神经退行性疾病(例如阿尔茨海默氏病和帕金森氏病),成瘾,神经性疼痛以及神经元和谷氨酸依赖性肿瘤。

著录项

  • 公开/公告号US2012129889A1

    专利类型

  • 公开/公告日2012-05-24

    原文格式PDF

  • 申请/专利权人 ADEBOYE ADEJARE;

    申请/专利号US201213361974

  • 发明设计人 ADEBOYE ADEJARE;

    申请日2012-01-31

  • 分类号A61K31/445;A61P25;A61P35;A61P27/02;

  • 国家 US

  • 入库时间 2022-08-21 17:32:50

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