N-Methyl-citalopram

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: N-Methyl-citalopram
• 英文别名: [3H]-N-Methyl-citalopram；3-[5-cyano-1-(4-fluorophenyl)-3H-2-benzofuran-1-yl]propyl-trimethylazanium
• 化学式: C₂₁H₂₄FN₂O
• 分子量: 339.433
• InChiKey: SMMPNIKRSMVRKY-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.3
• 重原子数：
  25
• 可旋转键数：
  5
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.38
• 拓扑面积：
  33
• 氢给体数：
  0
• 氢受体数：
  3

反应信息

• 作为产物：
  描述：

  西酞普兰 、 碘甲烷 以 丙酮 为溶剂， 以0.5 g的产率得到N-Methyl-citalopram
  参考文献：
  名称：

  Serotonin reuptake inhibitors as drugs having peripheral-system-restricted activity

  摘要：

  揭示了一种新型的选择性血清素再摄取抑制剂化合物，这些化合物旨在在外周系统中发挥血清素再摄取抑制活性，同时不具有中枢神经系统活性，并公开了制备这些化合物的方法。进一步公开了含有这些化合物的药物组合物以及在治疗与外周血清素水平和/或活性以及/或血小板聚集有关的医疗状况中的用途。

  公开号：

  US09221779B2

文献信息

• NOVEL SEROTONIN REUPTAKE INHIBITORS AS DRUGS HAVING PERIPHERAL-SYSTEM-RESTRICTED ACTIVITY
  申请人：Ramot at Tel-Aviv University Ltd.

  公开号：US20130143960A1

  公开（公告）日：2013-06-06

  Serotonin reuptake inhibitor compounds which are designed to exert serotonin uptake inhibitory activity in the peripheral system while being devoid of CNS activity, and a process of preparing same are disclosed. Further disclosed are pharmaceutical compositions containing same and uses thereof in the treatment of medical conditions associated with peripheral serotonin levels and/or activity, and/or platelet aggregation.
• Multi-API Loading Prodrugs
  申请人：Alkermes Pharma Ireland Limited

  公开号：US20160024011A1

  公开（公告）日：2016-01-28

  The present invention accomplishes this by having multiple molecules of parent drugs attached to carrier moieties and by extending the period during which the parent drug is released and absorbed after administration to the patient and providing a longer duration of action per dose than the parent drug itself. Prodrug conjugates are suitable for sustained delivery of heteroaryl, lactam-amide-, imide-, sulfonamide-, carbamate-, urea-, benzamide-, acylaniline-, cyclic amide- and tertiary amine-containing parent drugs that are substituted at the amide nitrogen or oxygen atom with labile aldehyde-linked prodrug moieties. The carrier groups of the prodrugs can be hydrophobic to reduce the polarity and solubility of the parent drug under physiological conditions.
• US9278947B2
  申请人：——

  公开号：US9278947B2

  公开（公告）日：2016-03-08
• Serotonin reuptake inhibitors as drugs having peripheral-system-restricted activity
  申请人：Rehavi Moshe

  公开号：US09221779B2

  公开（公告）日：2015-12-29

  Novel serotonin reuptake inhibitor compounds which are designed to exert serotonin uptake inhibitory activity in the peripheral system while being devoid of CNS activity, and a process of preparing same are disclosed. Further disclosed are pharmaceutical compositions containing same and uses thereof in the treatment of medical conditions associated with peripheral serotonin levels and/or activity, and/or platelet aggregation.

  揭示了一种新型的选择性血清素再摄取抑制剂化合物，这些化合物旨在在外周系统中发挥血清素再摄取抑制活性，同时不具有中枢神经系统活性，并公开了制备这些化合物的方法。进一步公开了含有这些化合物的药物组合物以及在治疗与外周血清素水平和/或活性以及/或血小板聚集有关的医疗状况中的用途。