(E)-3-(2,5-difluorophenyl)-N-[(1S)-1-[3-(4-pyridin-2-ylpiperazin-1-yl)phenyl]ethyl]prop-2-enamide

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二嗪烷类
• 英文名称: (E)-3-(2,5-difluorophenyl)-N-[(1S)-1-[3-(4-pyridin-2-ylpiperazin-1-yl)phenyl]ethyl]prop-2-enamide
• 化学式: C₂₆H₂₆F₂N₄O
• 分子量: 448.5
• InChiKey: SMJMHUIFKXGSNJ-BLRBJFNZSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.7
• 重原子数：
  33
• 可旋转键数：
  6
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.23
• 拓扑面积：
  48.5
• 氢给体数：
  1
• 氢受体数：
  6

文献信息

• 3-(Pyridinyl-piperazin-1-yl)-phenylethyl amides as potassium channel openers
  申请人：——

  公开号：US20040110765A1

  公开（公告）日：2004-06-10

  The present invention provides piperazinyl phenylethyl amides and related derivatives having the general Formula I 1 wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , A and B are as defined in the specification, or a nontoxic pharmaceutically acceptable salt, solvate or hydrate thereof which are openers or activators of KCNQ potassium channels. The present invention also provides pharmaceutical compositions comprising said piperazinyl phenylethyl amides and to the method of treatment of disorders sensitive to KCNQ potassium channel opening activity such as migraine or a migraine attack, bipolar disorders, epilepsy, acute and chronic pain, and anxiety.

  本发明提供了具有一般式I1的哌嗪基苯乙基酰胺及相关衍生物，其中R1、R2、R3、R4、R5、R6、A和B如规范中定义，或其非毒性药学上可接受的盐、溶剂或水合物，这些化合物是KCNQ钾通道的开放剂或激活剂。本发明还提供了包含上述哌嗪基苯乙基酰胺的药物组合物，以及用于治疗对KCNQ钾通道开放活性敏感的疾病的方法，如偏头痛或偏头痛发作、双相情感障碍、癫痫、急性和慢性疼痛以及焦虑症。
• 3-(PYRIDINYL-PIPERAZIN-1-YL)-PHENYLETHYL AMIDES AS POTASSIUM CHANNEL OPENERS
  申请人：Bristol-Myers Squibb Company

  公开号：EP1572112A2

  公开（公告）日：2005-09-14
• EP1572112A4
  申请人：——

  公开号：EP1572112A4

  公开（公告）日：2006-12-06
• US7087609B2
  申请人：——

  公开号：US7087609B2

  公开（公告）日：2006-08-08
• [EN] 3-(PYRIDINYL-PIPERAZIN-1-YL)-PHENYLETHYL AMIDES AS POTASSIUM CHANNEL OPENERS<br/>[FR] 3-(PYRIDINYL-PIPERAZINE-1-YL)-PHENYLETHYL AMIDES UTILISES EN TANT QU'AGENTS D'OUVERTURE DE CANAL POTASSIQUE
  申请人：BRISTOL MYERS SQUIBB CO

  公开号：WO2004047745A2

  公开（公告）日：2004-06-10

  The present invention provides piperazinyl phenylethyl amides and related derivatives having the general Formula I [INSERT CHEMICAL STRUCTURE] wherein R1, R2, R3, R4, R5, R6, A and B are as defined in the specification, or a nontoxic pharmaceutically acceptable salt, solvate or hydrate thereof which are openers or activators of KCNQ potassium channels. The present invention also provides pharmaceutical compositions comprising said piperazinyl phenylethyl amides and to the method of treatment of disorders sensitive to KCNQ potassium channel opening activity such as migraine or a migraine attack, bipolar disorders, epilepsy, acute and chronic pain, and anxiety.