N-(1-(imidazol-2-ylmethyl)piperidin-4-yl)-N-((4-methylphenyl)methyl)-N'-phenylmethylcarbamide | 359877-58-0

• 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-(1-(imidazol-2-ylmethyl)piperidin-4-yl)-N-((4-methylphenyl)methyl)-N'-phenylmethylcarbamide
• 英文别名: 3-benzyl-1-[1-(1H-imidazol-2-ylmethyl)piperidin-4-yl]-1-[(4-methylphenyl)methyl]urea
• CAS: 359877-58-0
• 化学式: C₂₅H₃₁N₅O
• 分子量: 417.554
• InChiKey: WXKDDAORWSJMCM-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.2
• 重原子数：
  31
• 可旋转键数：
  7
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.36
• 拓扑面积：
  64.3
• 氢给体数：
  2
• 氢受体数：
  3

反应信息

• 作为产物：
  描述：

  tert-butyl 4-((4-methylphenyl)methyl)aminopiperidine carboxylate 在 盐酸 作用下， 以 1,4-二氧六环 、 甲醇 、 乙醚 、 乙醇 、 二氯甲烷 为溶剂， 反应 145.0h， 生成 N-(1-(imidazol-2-ylmethyl)piperidin-4-yl)-N-((4-methylphenyl)methyl)-N'-phenylmethylcarbamide
  参考文献：
  名称：

  AZACYCLIC COMPOUNDS

  摘要：

  提供用于治疗修改血清素能受体活性具有有益效果的疾病状态的化合物和方法。在方法中，将有效量的化合物施用于需要此类治疗的病人。

  公开号：

  US20150259291A1

文献信息

• Azacyclic compounds
  申请人：——

  公开号：US20020004513A1

  公开（公告）日：2002-01-10

  Compounds and methods are provided for the treatment of disease conditions in which modification of serotonergic receptor activity has a beneficial effect. In the method, an effective amount of a compound is adminstered to a patient in need of such treatment.

  提供了用于治疗疾病病况的化合物和方法，其中修改5-羟色胺受体活性具有益处。在该方法中，向需要这种治疗的患者施用化合物的有效量。
• [EN] AZACYCLIC COMPOUNDS FOR USE IN THE TREATMENT OF SEROTONIN RELATED DISEASES<br/>[FR] COMPOSES AZACYCLIQUES UTILISES DANS LE TRAITEMENT DE MALADIES LIEES A LA SEROTONINE
  申请人：ACADIA PHARM INC

  公开号：WO2001066521A1

  公开（公告）日：2001-09-13

  Compound and methods are provided for the treatment of disease conditions in which modification of serotonergic receptor activity has a beneficial effect. In the method, an effective amount of a compound of formula (II) is administered to a patient in need of such treatment.

  提供了一种化合物和方法，用于治疗疾病状态，其中修饰5-羟色胺受体活性具有益处。在该方法中，将II式化合物的有效量用于需要此类治疗的患者。
• USE OF 4-AMINO-PIPERIDINES FOR TREATING SLEEP DISORDERS
  申请人：van Kammen Daniel

  公开号：US20080051429A1

  公开（公告）日：2008-02-28

  Inverse agonists and antagonists of serotonin receptors are disclosed for use in treating sleep disorders such as insomnia, and specifically sleep maintenance insomnia. The compound increase slow wave sleep, decrease the number of awakenings after sleep onset, and decrease the time awake after sleep onset.

  揭示了逆向激动剂和拮抗剂的血清素受体，用于治疗睡眠障碍，如失眠，特别是睡眠维持失眠。该化合物增加慢波睡眠，减少入睡后醒来的次数，减少入睡后清醒的时间。
• METHODS OF TREATMENT USING SELECTIVE 5-HT2A INVERSE AGONISTS
  申请人：ANDERSSON Carl-Magnus A.

  公开号：US20110301191A1

  公开（公告）日：2011-12-08

  Compounds and methods are provided for the treatment of disease conditions in which modification of serotonergic receptor activity has a beneficial effect. In the method, an effective amount of a compound is administered to a patient in need of such treatment.

  本发明提供了用于治疗疾病状态的化合物和方法，其中修改5-羟色胺受体活性具有益处。在该方法中，向需要此类治疗的患者施用有效量的化合物。
• 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。