N1-[2-(4-methoxyphenyl)ethyl]-1-(4-methoxyphenyl)-1,2-ethanediamine | 1000307-33-4

• 分子结构分类: 有机化合物 - 生物碱及其衍生物 - 石蒜科生物碱
• 英文名称: N1-[2-(4-methoxyphenyl)ethyl]-1-(4-methoxyphenyl)-1,2-ethanediamine
• 英文别名: 1-(4-methoxyphenyl)-N-[2-(4-methoxyphenyl)ethyl]ethane-1,2-diamine
• CAS: 1000307-33-4
• 化学式: C₁₈H₂₄N₂O₂
• 分子量: 300.401
• InChiKey: MJTYGVIYMOYTLB-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.3
• 重原子数：
  22
• 可旋转键数：
  8
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.33
• 拓扑面积：
  56.5
• 氢给体数：
  2
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  N1-[2-(4-methoxyphenyl)ethyl]-1-(4-methoxyphenyl)-1,2-ethanediamine 、 N,N'-羰基二咪唑 以 N,N-二甲基甲酰胺 为溶剂， 反应 0.5h， 生成 5-(4-Methoxyphenyl)-1-[2-(4-methoxyphenyl)ethyl]imidazolidin-2-one
  参考文献：
  名称：

  Selective Kv1.5 Blockers: Development of (R)-1-(Methylsulfonylamino)-3-[2-(4-methoxyphenyl)ethyl]-4-(4-methoxyphenyl)-2-imidazolidinone (KVI-020/WYE-160020) as a Potential Treatment for Atrial Arrhythmia

  摘要：

  Atrial fibrillation is the most prevalent form of cardiac arrhythmia. Current treatments extend the atrial effective refractory period by nonselective blockade of cardiac ion channels. An alternative approach selectively targeting the Kv1.5 ion channel offers the opportunity for therapeutic benefit with decreased risk of adverse cardiovascular events. KVI-020 (4g) successfully demonstrated antiarrhythmic efficacy in a canine arrhythmia model, and these findings support its utility as an antiarrhythmic agent.

  DOI：

  10.1021/jm901042m
• 作为产物：
  描述：

  (4-methoxyphenyl)-[2-(4-methoxyphenyl)ethylamino]acetonitrile 在 lithium aluminium tetrahydride 、 sodium hydroxide 、 水 作用下， 以 乙醚 为溶剂， 反应 1.0h， 以100%的产率得到N1-[2-(4-methoxyphenyl)ethyl]-1-(4-methoxyphenyl)-1,2-ethanediamine
  参考文献：
  名称：

  KV1.5 POTASSIUM CHANNEL INHIBITORS

  摘要：

  本发明涉及1-N-氨基-2-咪唑啉酮及其衍生物，其作为Kv1.5钾通道抑制剂，提供房颤选择性抗心律失常药物。本发明还涉及含有上述Kv1.5钾通道抑制剂的组合物，以及治疗心律失常的方法。

  公开号：

  US20070299120A1

文献信息

• Kv1.5 potassium channel inhibitors
  申请人：Wyeth

  公开号：US07504517B2

  公开（公告）日：2009-03-17

  The present invention relates to 1-N-amino-2-imidazolidinones and derivatives thereof which are effective as Kv1.5 potassium channel inhibitors providing atrial-selective antiarrhythmic agents. The present invention further relates to compositions comprising said Kv1.5 potassium channel inhibitors, and to methods for treating cardiac arrhythmia.

  本发明涉及1-N-氨基-2-咪唑烷酮及其衍生物，其作为Kv1.5钾通道抑制剂，提供心房选择性抗心律失常剂。本发明还涉及包含上述Kv1.5钾通道抑制剂的组合物，以及治疗心律失常的方法。
• US7504517B2
  申请人：——

  公开号：US7504517B2

  公开（公告）日：2009-03-17
• US7803827B2
  申请人：——

  公开号：US7803827B2

  公开（公告）日：2010-09-28
• Selective Kv1.5 Blockers: Development of (<i>R</i>)-1-(Methylsulfonylamino)-3-[2-(4-methoxyphenyl)ethyl]-4-(4-methoxyphenyl)-2-imidazolidinone (KVI-020/WYE-160020) as a Potential Treatment for Atrial Arrhythmia
  作者：Benjamin E. Blass、Andrew Fensome、Eugene Trybulski、Ronald Magolda、Stephen J. Gardell、Kun Liu、Manoj Samuel、Irene Feingold、Christine Huselton、Chris M. Jackson、Laurent Djandjighian、Douglas Ho、James Hennan、John M. Janusz

  DOI：10.1021/jm901042m

  日期：2009.11.12

  Atrial fibrillation is the most prevalent form of cardiac arrhythmia. Current treatments extend the atrial effective refractory period by nonselective blockade of cardiac ion channels. An alternative approach selectively targeting the Kv1.5 ion channel offers the opportunity for therapeutic benefit with decreased risk of adverse cardiovascular events. KVI-020 (4g) successfully demonstrated antiarrhythmic efficacy in a canine arrhythmia model, and these findings support its utility as an antiarrhythmic agent.
• KV1.5 POTASSIUM CHANNEL INHIBITORS
  申请人：Janusz Michael John

  公开号：US20070299120A1

  公开（公告）日：2007-12-27

  The present invention relates to 1-N-amino-2-imidazolidinones and derivatives thereof which are effective as Kv1.5 potassium channel inhibitors providing atrial-selective antiarrhythmic agents. The present invention further relates to compositions comprising said Kv1.5 potassium channel inhibitors, and to methods for treating cardiac arrhythmia.

  本发明涉及1-N-氨基-2-咪唑啉酮及其衍生物，其作为Kv1.5钾通道抑制剂，提供房颤选择性抗心律失常药物。本发明还涉及含有上述Kv1.5钾通道抑制剂的组合物，以及治疗心律失常的方法。