N-(4-fluorobenzyl)-N'-(4-isopropoxybenzyl)-N-piperidin-4-yl-carbamide oxalate | 639862-26-3

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯酚醚
• 英文名称: N-(4-fluorobenzyl)-N'-(4-isopropoxybenzyl)-N-piperidin-4-yl-carbamide oxalate
• 英文别名: 1-[(4-Fluorophenyl)methyl]-1-piperidin-4-yl-3-[(4-propan-2-yloxyphenyl)methyl]urea;oxalic acid
• CAS: 639862-26-3
• 化学式: C₂H₂O₄*C₂₃H₃₀FN₃O₂
• 分子量: 489.544
• InChiKey: SGRRDKYVRJXTCG-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.23
• 重原子数：
  35
• 可旋转键数：
  8
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.4
• 拓扑面积：
  128
• 氢给体数：
  4
• 氢受体数：
  8

反应信息

• 作为反应物：
  描述：

  N-(3-氯丙基)吗啉 、 N-(4-fluorobenzyl)-N'-(4-isopropoxybenzyl)-N-piperidin-4-yl-carbamide oxalate 在 caesium carbonate 、 sodium iodide 作用下， 以 N,N-二甲基甲酰胺 、 乙腈 为溶剂， 以32%的产率得到N-(4-fluorobenzyl)-N'-(4-isopropoxybenzyl)-N-[1-(3-morpholin-4-yl-propyl)piperidin-4-yl]carbamide oxalate
  参考文献：
  名称：

  WO2007/124136

  摘要：

  公开号：

文献信息

• Combination of a sedative and a neurotransmitter modulator, and methods for improving sleep quality and treating depression
  申请人：Sepracor Inc.

  公开号：EP2343073A2

  公开（公告）日：2011-07-13

  One aspect of the present invention relates to pharmaceutical compositions containing two or more active agents that when taken together can be used to treat, e.g., insomnia and/or depression. The first component of the pharmaceutical composition is a GABA receptor modulating compound. The second component of the pharmaceutical composition is a serotonin reuptake inhibitor, a norepinephrine reuptake inhibitor, a 5-HT2A modulator, or dopamine reuptake inhibitor. In certain embodiments, the pharmaceutical composition comprises eszopiclone. In a preferred embodiment, the pharmaceutical composition comprises eszopiclone and fluoxetine. The present invention also relates to a method of treating a sleep abnormality, treating insomnia, treating depression, augmenting antidepressant therapy, eliciting a dose-sparing effect, reducing depression relapse, improving the efficacy of antidepressant therapy or improving the tolerability of antidepressant therapy, comprising co-administering to a patient in need thereof a GABA-receptor-modulating compound; and a SRI, NRI, 5-HT2A modulator or DRI.

  本发明的一个方面涉及含有两种或两种以上活性剂的药物组合物，这些活性剂一起服用时可用于治疗失眠和/或抑郁症等。药物组合物的第一种成分是 GABA 受体调节化合物。药物组合物的第二种成分是血清素再摄取抑制剂、去甲肾上腺素再摄取抑制剂、5-HT2A调节剂或多巴胺再摄取抑制剂。在某些实施方案中，药物组合物包含艾佐匹克隆。在一个优选的实施方案中，药物组合物包括艾司佐匹克隆和氟西汀。本发明还涉及一种治疗睡眠异常、治疗失眠、治疗抑郁症、增强抗抑郁治疗、引起剂量节省效应、减少抑郁症复发、改善抗抑郁治疗的疗效或改善抗抑郁治疗的耐受性的方法，包括向有需要的患者联合施用GABA受体调节化合物；和SRI、NRI、5-HT2A调节剂或DRI。
• [EN] N-SUBSTITUTED PIPERIDINE DERIVATIVES AS SEROTONIN RECEPTOR AGENTS<br/>[FR] DERIVES DE PIPERIDINE SUBSTITUES EN N EN TANT QU'AGENTS RECEPTEURS DE LA SEROTONINE
  申请人：ACADIA PHARM INC

  公开号：WO2004000808A3

  公开（公告）日：2004-03-25
• COMBINATION OF A SEDATIVE AND A NEUROTRANSMITTER MODULATOR, AND METHODS FOR IMPROVING SLEEP QUALITY AND TREATING DEPRESSION
  申请人：SEPRACOR, INC.

  公开号：EP1691811A1

  公开（公告）日：2006-08-23
• PHARMACEUTICAL COMPOSITION COMPRISING AN AMPK ACTIVATOR AND A SEROTONERGIC AGENT AND METHODS OF USE THEREOF
  申请人：ALS Mountain Llc

  公开号：EP2983473A2

  公开（公告）日：2016-02-17
• Combination of sedative and a neurotransmitter modulator, and methods for improving sleep quality and treating depression
  申请人：Lalji Karim

  公开号：US20050176680A1

  公开（公告）日：2005-08-11

  One aspect of the present invention relates to pharmaceutical compositions containing two or more active agents that when taken together can be used to treat, e.g., insomnia and/or depression. The first component of the pharmaceutical composition is a GABA receptor modulating compound. The second component of the pharmaceutical composition is a serotonin reuptake inhibitor, a norepinephrine reuptake inhibitor, a 5-HT 2A modulator, or dopamine reuptake inhibitor. In certain embodiments, the pharmaceutical composition comprises eszopiclone. In a preferred embodiment, the pharmaceutical composition comprises eszopiclone and fluoxetine. The present invention also relates to a method of treating a sleep abnormality, treating insomnia, treating depression, augmenting antidepressant therapy, eliciting a dose-sparing effect, reducing depression relapse, improving the efficacy of antidepressant therapy or improving the tolerability of antidepressant therapy, comprising co-administering to a patient in need thereof a GABA-receptor-modulating compound; and a SRI, NRI, 5-HT 2A modulator or DRI.