N-[3-(hydroxymethyl)-5,7-dimethyladamantan-1-yl]acetamide | 356572-01-5

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 羧酸及其衍生物
• 英文名称: N-[3-(hydroxymethyl)-5,7-dimethyladamantan-1-yl]acetamide
• 英文别名: 1-acetamido-3,5-dimethyl-7-hydroxymethyladamantane；N-[3-(hydroxymethyl)-5,7-dimethyl-1-adamantyl]acetamide
• CAS: 356572-01-5
• 化学式: C₁₅H₂₅NO₂
• 分子量: 251.369
• InChiKey: JLHZGSKNUONKCB-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.8
• 重原子数：
  18
• 可旋转键数：
  2
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.93
• 拓扑面积：
  49.3
• 氢给体数：
  2
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  N-[3-(hydroxymethyl)-5,7-dimethyladamantan-1-yl]acetamide 在 盐酸 、 sodium hydroxide 、 sodium sulfate 作用下， 以 乙酸乙酯 、 二乙二醇 为溶剂， 生成 1-amino-3,5-dimethyl-7-hydroxymethyladamantane hydrochloride
  参考文献：
  名称：

  Methods for treating neuropsychiatric disorders with nmda receptor antagonists

  摘要：

  本发明涉及用于治疗患有神经精神障碍的人类患者的组合物和方法。具体而言，本发明提供了用于调节或拮抗神经元NMDA受体活性的组合物和方法，其中这种拮抗活性能够调节神经元的谷氨酸诱导的兴奋反应，从而抑制兴奋毒性效应，促进神经营养效应，并提供治疗效果以治疗神经精神障碍。

  公开号：

  US20040122090A1
• 作为产物：
  描述：

  5,7-dimethyl-3-(nitroxymethyl)adamantan-1-yl nitrate 、 乙腈 在 硫酸 作用下， 反应 4.0h， 以54%的产率得到N-[3-(hydroxymethyl)-5,7-dimethyladamantan-1-yl]acetamide
  参考文献：
  名称：

  1-Nitroxy-3-(nitrooxymethyl) 金刚烷的亲核取代反应

  摘要：

  摘要 1-nitro-3-(nitrooxymethyl)金刚烷与亲核试剂在100%硫酸中反应合成了一系列新型多官能笼化合物。桥头位置的硝氧基基团的取代伴随着硝氧基甲基片段的水解。

  DOI：

  10.1134/s1070428022070065

文献信息

• Aminoadamantane derivatives as therapeutic agents
  申请人：NeuroMolecular, Inc.

  公开号：US06444702B1

  公开（公告）日：2002-09-03

  The present invention provides novel aminoadamantane derivatives, methods of making the derivatives, compositions including the novel aminoadamantane derivatives, and methods for the treatment and prevention of neurological diseases using the derivatives and compositions. There are a variety of neurological disorders that can be treated using the present invention, including, for example, the following: neurological disorders arising from trauma, ischemic or hypoxic conditions that can be treated include stroke, hypoglycemia, cerebral ischemia, cardiac arrest, spinal cord trauma, head trauma, perinatal hypoxia, cardiac arrest and hypoglycemic neuronal damage; neurodegenerative disorders such as epilepsy, Alzheimer's disease, Huntington's disease Parkinsonism, and amyotrophic lateral sclerosis; other diseases or disorders such as convulsion, pain, depression, anxiety, schizophrenia, muscle spasms, migraine headaches, urinary incontinence, nicotine withdrawal, opiate tolerance and withdrawal, emesis, brain edema, tardive dyskinesia, AIDS-induced dementia, ocular damage, retinopathy, cognitive disorders, and neuronal injury associated with HIV-infection such as dysfunction in cognition, movement and sensation.

  本发明提供了新颖的氨基金刚烷衍生物，制备这些衍生物的方法，包括这些新型氨基金刚烷衍生物的组合物，以及使用这些衍生物和组合物进行神经系统疾病的治疗和预防的方法。本发明可以用来治疗多种神经系统疾病，包括但不限于以下疾病：由创伤、缺血或缺氧引起的神经系统疾病，如中风、低血糖、脑缺血、心脏骤停、脊髓损伤、头部创伤、围产期缺氧、心脏骤停和低血糖引起的神经元损伤；神经退行性疾病，如癫痫、阿尔茨海默病、亨廷顿病、帕金森症和肌萎缩性侧索硬化症；其他疾病或疾病，如抽搐、疼痛、抑郁症、焦虑症、精神分裂症、肌肉痉挛、偏头痛、尿失禁、尼古丁戒断反应、阿片类药物耐受性和戒断反应、呕吐、脑水肿、迟发性运动障碍、艾滋病相关痴呆、眼部损伤、视网膜病变、认知障碍，以及与HIV感染相关的神经元损伤，如认知、运动和感觉功能障碍。
• AMINOADAMANTANE DERIVATIVES AS THERAPEUTIC AGENTS
  申请人：Wang Yuqiang

  公开号：US20080183003A1

  公开（公告）日：2008-07-31

  The present invention provides novel aminoadamantane derivatives, methods of making the derivatives, compositions including the novel aminoadamantane derivatives, and methods for the treatment and prevention of neurological diseases using the derivatives and compositions. There are a variety of neurological disorders that can be treated using the present invention, including, for example, the following: neurological disorders arising from trauma, ischemic or hypoxic conditions that can be treated include stroke, hypoglycemia, cerebral ischemia, cardiac arrest, spinal cord trauma, head trauma, perinatal hypoxia, cardiac arrest and hypoglycemic neuronal damage; neurodegenerative disorders such as epilepsy, Alzheimer's disease, Huntington's disease Parkinsonism, and amyotrophic lateral sclerosis; other diseases or disorders such as convulsion, pain, depression, anxiety, schizophrenia, muscle spasms, migraine headaches, urinary incontinence, nicotine withdrawal, opiate tolerance and withdrawal, emesis, brain edema, tardive dyskinesia, AIDS-induced dementia, ocular damage, retinopathy, cognitive disorders, and neuronal injury associated with HIV-infection such as dysfunction in cognition, movement and sensation.

  本发明提供了新型氨基金刚烷衍生物，制备这些衍生物的方法，包括这些新型氨基金刚烷衍生物的组合物，以及使用这些衍生物和组合物治疗和预防神经系统疾病的方法。可以使用本发明治疗各种神经系统疾病，包括以下疾病：因创伤、缺血或缺氧引起的神经系统疾病，包括中风、低血糖、脑缺血、心脏骤停、脊髓损伤、头部损伤、围产期缺氧、心脏骤停和低血糖神经元损伤；神经退行性疾病，如癫痫、阿尔茨海默病、亨廷顿病帕金森综合症和肌萎缩性侧索硬化；其他疾病或疾病，如惊厥、疼痛、抑郁、焦虑、精神分裂症、肌肉痉挛、偏头痛、尿失禁、尼古丁戒断、阿片类药物耐受性和戒断、呕吐、脑水肿、迟发性运动障碍、艾滋病相关痴呆、眼损伤、视网膜病变、认知障碍以及与HIV感染相关的神经元损伤，如认知、运动和感觉功能障碍。
• Methods for Treating Neuropsychiatric Disorders with NMDA Receptor Antagonists
  申请人：Lipton Stuart A.

  公开号：US20100137448A1

  公开（公告）日：2010-06-03

  The present invention relates to compositions and methods for treating a human patient afflicted with a neuropsychiatric disorder. Specifically, the invention provides for compositions and methods of modulating or antagonizing the activity of neuronal NMDA receptors, wherein such antagonistic activity is capable of modulating the glutamate induced excitatory response of the neurons, thereby inhibiting an excitotoxic effect, promoting a neurotrophic effect, and thereby providing a therapeutic effect that treats the neuropsychiatric disorder.

  本发明涉及用于治疗患有神经精神障碍的人类患者的组合物和方法。具体而言，本发明提供了调节或拮抗神经元NMDA受体活性的组合物和方法，其中这种拮抗活性能够调节神经元的谷氨酸诱导的兴奋反应，从而抑制兴奋毒性效应，促进神经营养效应，从而提供治疗神经精神障碍的治疗效果。
• Methods for treating neuropsychiatric disorders with NMDA receptors antagonists
  申请人：Neuromolecular Inc.

  公开号：EP1852113A2

  公开（公告）日：2007-11-07

  The Present invention relates to compositions and methods for treating a human patient afflicted with a neuropsychiatric disorder. Specifically, the invention provides for compositions and methods of modulating or antagonizing the activity of neuronal NMDA receptors, wherein such antagonistic activity is capable of modulating the glutamate induced excitatory response of the neurons, thereby inhibiting an excitotoxic effect, promoting a neurotrophic effect, and thereby providing a therapeutic effect that treats the neuropsychiatric disorder.

  本发明涉及治疗患有神经精神疾病的人类患者的组合物和方法。具体而言，本发明提供了调节或拮抗神经元 NMDA 受体活性的组合物和方法，其中这种拮抗活性能够调节谷氨酸诱导的神经元兴奋反应，从而抑制兴奋毒性效应，促进神经营养效应，进而提供治疗神经精神障碍的疗效。
• EP1351670A4
  申请人：——

  公开号：EP1351670A4

  公开（公告）日：2004-07-07