N-desmethylfluperlapine | 67121-74-8

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯氮卓类
• 英文名称: N-desmethylfluperlapine
• 英文别名: N-Demethyl-Fluperlapine；3-fluoro-6-piperazin-1-yl-11H-dibenzo[b,e]azepine；3-fluoro-6-piperazin-1-yl-11H-benzo[c][1]benzazepine
• CAS: 67121-74-8
• 化学式: C₁₈H₁₈FN₃
• 分子量: 295.359
• InChiKey: ZIDVTHAJFUGQLK-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.5
• 重原子数：
  22
• 可旋转键数：
  1
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.28
• 拓扑面积：
  27.6
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为产物：
  描述：

  甲醇 在 1-氯乙基氯甲酸酯 作用下， 以 四氢呋喃 为溶剂， 反应 20.0h， 生成 N-desmethylfluperlapine
  参考文献：
  名称：

  [EN] AMINO SUBSTITUTED DIARYL[A,D]CYCLOHEPTENE ANALOGS AS MUSCARINIC AGONISTS AND METHODS OF TREATMENT OF NEUROPSYCHIATRIC DISORDERS
  [FR] ANALOGUES DE DIARYL[A,D]CYCLOHEPTENE AMINO SUBSTITUES UTILISES COMME AGONISTES MUSCARINIQUES, ET PROCEDES DE TRAITEMENT DE TROUBLES NEUROPSYCHIATRIQUES

  摘要：

  公开号：

  WO2005063254A3

文献信息

• Amino substituted diaryl[a,d]cycloheptene analogs as muscarinic agonists and methods of treatment of neuropsychiatric disorders
  申请人：Ek Fredrik

  公开号：US20050192268A1

  公开（公告）日：2005-09-01

  Disclosed herein are analogs of clozapine and pharmaceutically acceptable salts, esters, amides, or prodrugs thereof; methods of synthesizing the analogs; and methods of using the analogs for treating neuorpsychiatric disorders. In some embodiments, the analogs are amino substituted diaryl[a,d]cycloheptenes.

  本文披露了氯氮平的类似物及其药用可接受的盐，酯，酰胺或前药；合成类似物的方法；以及使用类似物治疗神经精神障碍的方法。在某些实施例中，类似物是氨基取代的二芳基[a，d]环庚烯。
• Amino bustituted diaryl[a,d]cycloheptene analogs as muscarinic agonists and methods of treatment of neuropsychiatric disorders
  申请人：Ek Fredrik

  公开号：US20060199798A1

  公开（公告）日：2006-09-07

  Disclosed herein are analogs of clozapine and pharmaceutically acceptable salts, esters, amides, or prodrugs thereof; methods of synthesizing the analogs; and methods of using the analogs for treating neuorpsychiatric disorders. In some embodiments, the analogs are amino substituted diaryl[a,d]cycloheptenes.

  本文公开了氯氮平的类似物及其药学上可接受的盐、酯、酰胺或前药；合成这些类似物的方法；以及使用这些类似物治疗神经精神障碍的方法。在某些实施例中，这些类似物是氨基取代的二芳基[a，d]环庚烯。
• AMINO SUBSTITUTED DIARYL[a,d]CYCLOHEPTENE ANALOGS AS MUSCARINIC AGONISTS AND METHODS OF TREATMENT OF NEUROPSYCHIATRIC DISORDERS
  申请人：Ek Fredrik

  公开号：US20090239840A1

  公开（公告）日：2009-09-24

  Disclosed herein are analogs of clozapine and pharmaceutically acceptable salts, esters, amides, or prodrugs thereof; methods of synthesizing the analogs; and methods of using the analogs for treating neuorpsychiatric disorders. In some embodiments, the analogs are amino substituted diaryl[a,d]cycloheptenes.

  本文披露了氯氮平的类似物及其药学上可接受的盐、酯、酰胺或前药；合成类似物的方法；以及使用类似物治疗神经精神障碍的方法。在某些实施例中，这些类似物是氨基取代的二芳基[a，d]环庚烯。
• Use of N-desmethylclozapine and related compounds as dopamine stabilizing agents
  申请人：Burstein S. Ethan

  公开号：US20060252744A1

  公开（公告）日：2006-11-09

  Disclosed herein is the use of N-desmethylclozapine (NDMC) and related compounds to treat a variety of neuropsychiatric diseases including psychosis. It is shown that NDMC and related compounds are agonists or partial agonists at D2 and D3 dopamine receptors and thus may be effective as a dopamine stabilizing agent, allowing it to be used to treat or provide reduced incidence of Extrapyramidal symptoms (EPS) and/or tardive dyskinesias (TD). Also disclosed is administering NDMC and related compounds in combination with other anti-psychotic agents.

  本文披露了使用N-去甲基氯氮平（NDMC）及相关化合物治疗多种神经精神疾病，包括精神病的方法。研究表明，NDMC及相关化合物是D2和D3多巴胺受体的激动剂或部分激动剂，因此可能作为多巴胺稳定剂起作用，从而可用于治疗或减少肌张力障碍症状（EPS）和/或迟发性运动障碍（TD）。本文还披露了将NDMC及相关化合物与其他抗精神病药物联合使用的方法。
• Dibenzo-condensed azepine, diazepine, oxazepine and thiazepine derivatives as muscarinic agonists and methods of treatment of neuropsychiatric disorders
  申请人：Acadia Pharmaceuticals Inc.

  公开号：EP2088147A1

  公开（公告）日：2009-08-12

  Disclosed herein are analogs of clozapine and pharmaceutically acceptable salts, esters, amides, or prodrugs thereof; methods of synthesizing the analogs; and methods of using the analogs for treating neuorpsychiatric disorders. In some embodiments, the analogs are amino substituted diaryl[a,d]cycloheptenes.

  本文公开了氯氮平的类似物及其药学上可接受的盐、酯、酰胺或原药；合成这些类似物的方法；以及使用这些类似物治疗神经精神疾病的方法。在某些实施方案中，类似物是氨基取代的二芳基[a,d]环庚烯。