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1. 发明申请

US20110098360A1 ADAMANTANE DERIVATIVE FOR INHIBITING TOXICITY OF AMYLOID OLIGOMER 审中-公开
标题翻译：用于抑制AMYLOID低聚物毒性的ADAMANTANE衍生物
公开(公告)号：US20110098360A1
公开(公告)日：2011-04-28
申请号：US12935244
申请日：2009-03-09
申请人： Min Yung Lee , So-Yeop Han , Jun Mo Chung , Pyung Lim Han , Jung Min Koh , Ha Yan Oak , Eun Kyung Hwang , In Sun Baek
发明人： Min Yung Lee , So-Yeop Han , Jun Mo Chung , Pyung Lim Han , Jung Min Koh , Ha Yan Oak , Eun Kyung Hwang , In Sun Baek
IPC分类号： A61K31/132 , C07C211/19 , A61P25/28 , A61P25/16 , A61P25/00 , A61P27/02
CPC分类号： A61K31/132
摘要： Disclosed is a pharmaceutical composition containing a compound useful for inhibiting neurotoxicity caused by beta amyloid. The pharmaceutical composition of the present disclosure contains 1,3,5,7-tetrakis(aminomethyl)adamantane, an analogous compound thereof or a salt thereof as an active ingredient. The inventors have studied methods for reducing the toxicity of beta amyloid oligomers based on the formation mechanism of dodecamers in consideration of the fact that especially the dodecamers from among the beta amyloid oligomers exhibit a significant activity as a toxin for synapses and neurons in cranial nerve diseases. The inventors have confirmed that the disclosed compound can induce structural epitope deformation of the dodecamer and thereby reduce toxicity of the beta amyloid oligomers. The pharmaceutical composition containing the compound is useful for preventing and treating cranial nerve diseases developed by the toxicity of beta amyloid oligomers, for example, Alzheimer's disease, Parkinson's disease, Huntington's disease, macular degeneration, prion disease, and the like (see FIG. 1).
摘要翻译：公开了含有可用于抑制由β淀粉样蛋白引起的神经毒性的化合物的药物组合物。本公开的药物组合物含有1,3,5,7-四（氨基甲基）金刚烷，其类似的化合物或其盐作为活性成分。本发明人研究了基于十二烷基化物形成机制降低β淀粉样蛋白低聚物的毒性的方法，考虑到特别是β淀粉样低聚物中的十二烷基化剂作为颅神经疾病中突触和神经元的毒素显示出显着的活性。发明人已经确认所公开的化合物可以诱导十二聚体的结构表位变形，从而降低β淀粉样寡聚物的毒性。含有该化合物的药物组合物可用于预防和治疗由β-淀粉样蛋白寡聚物（例如阿尔茨海默氏病，帕金森病，亨廷顿舞蹈病，黄斑变性，朊病毒病等）的毒性引起的颅神经疾病（见图1 ）。

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