1-methyl-2-(3-piperidin-4-ylpropyl)-1H-benzimidazole

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯并咪唑类
• 英文名称: 1-methyl-2-(3-piperidin-4-ylpropyl)-1H-benzimidazole
• 英文别名: 1-methyl-2-(3-piperidin-4-ylpropyl)benzimidazole
• 化学式: C₁₆H₂₃N₃
• 分子量: 257.379
• InChiKey: ZGHMWYDJZSIUJS-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.9
• 重原子数：
  19
• 可旋转键数：
  4
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.56
• 拓扑面积：
  29.8
• 氢给体数：
  1
• 氢受体数：
  2

反应信息

• 作为产物：
  描述：

  4-哌啶丁酸盐酸盐 、 N-甲基-1,2-苯二胺 在 磷酸 、 phosphorus pentoxide 、 sodium hydroxide 作用下， 以 水 为溶剂， 反应 3.5h， 生成 1-methyl-2-(3-piperidin-4-ylpropyl)-1H-benzimidazole
  参考文献：
  名称：

  Piperazine derivatives for the treatment of urinary incontinence and pain

  摘要：

  公开号：

  EP1849773B1

文献信息

• Pyridyl Non-Aromatic Nitrogen-Containing Heterocyclic-1-Carboxylate Compound
  申请人：Ishii Takahiro

  公开号：US20100009971A1

  公开（公告）日：2010-01-14

  A novel pyridyl non-aromatic nitrogen-containing heterocyclic-1-carboxylate compound or its pharmaceutically acceptable salt has a potent FAAH-inhibitory activity. Further, the pyridyl non-aromatic nitrogen-containing heterocyclic-1-carboxylate compound of the present disclosure is also useful in the treatment of urinary frequency and urinary incontinence, overactive bladder and/or pain.

  一种新型的吡啶基非芳香性含氮杂环-1-羧酸酯化合物或其药学上可接受的盐具有强效的FAAH抑制活性。此外，本公开的吡啶基非芳香性含氮杂环-1-羧酸酯化合物也可用于治疗尿频、尿失禁、过度活跃的膀胱和/或疼痛。
• Pyridyl Non-Aromatic Nitrogen-Containing Heterocyclic-1-Carboxylate Derivative
  申请人：Ishii Takahiro

  公开号：US20080306046A1

  公开（公告）日：2008-12-11

  [Problem] To provide a compound usable for treatment of diseases associated with fatty acid amide hydrolase (FAAH), especially for treatment of urinary frequency and urinary incontinence, overactive bladder and/or pain. [Means for Solution] We have found that a novel pyridyl non-aromatic nitrogen-containing heterocyclic-1-carboxylate derivative and its pharmaceutically acceptable salt has a potent FAAH-inhibitory activity. Further, the pyridyl non-aromatic nitrogen-containing heterocyclic-1-carboxylate derivative of the present invention has an excellent effect for increasing an effective bladder capacity, an excellent effect for relieving urinary frequency and an excellent anti-allodynia effect, and is therefore usable for treatment of urinary frequency and urinary incontinence, overactive bladder and/or pain.

  [问题] 提供一种可用于治疗与脂肪酸酰胺水解酶（FAAH）相关的疾病的化合物，特别是用于治疗尿频和尿失禁、过度活跃的膀胱和/或疼痛。 [解决方法] 我们发现一种新型的吡啶基非芳香性含氮杂环-1-羧酸酯衍生物及其药学上可接受的盐具有强效的FAAH抑制活性。此外，本发明的吡啶基非芳香性含氮杂环-1-羧酸酯衍生物具有优异的增加有效膀胱容量的效果，优异的缓解尿频的效果和优异的抗痛觉过敏效果，因此可用于治疗尿频和尿失禁、过度活跃的膀胱和/或疼痛。
• Pyridyl non-aromatic nitrogen-containing heterocyclic-1-carboxylate compound
  申请人：Astellas Pharma, Inc.

  公开号：US07919494B2

  公开（公告）日：2011-04-05

  A novel pyridyl non-aromatic nitrogen-containing heterocyclic-1-carboxylate compound and its pharmaceutically acceptable salt has a potent FAAH-inhibitory activity. Further, the pyridyl non-aromatic nitrogen-containing heterocyclic-1-carboxylate compound of the present disclosure is also useful in the treatment of urinary frequency and urinary incontinence, overactive bladder and/or pain.

  一种新型的含吡啶的非芳香族含氮杂环-1-羧酸酯化合物及其药学上可接受的盐具有强效的FAAH抑制活性。此外，本公开的吡啶基非芳香族含氮杂环-1-羧酸酯化合物在治疗尿频、尿失禁、过度活动的膀胱和/或疼痛方面也具有用途。
• PYRIDYL NON-AROMATIC NITROGENATED HETEROCYCLIC-1-CARBOXYLATE ESTER DERIVATIVE
  申请人：Astellas Pharma Inc.

  公开号：EP1849773A1

  公开（公告）日：2007-10-31

  [Problem] To provide a compound usable for treatment of diseases associated with fatty acid amide hydrolase (FAAH), especially for treatment of urinary frequency and urinary incontinence, overactive bladder and/or pain. [Means for Solution] We have found that a novel pyridyl non-aromatic nitrogen-containing heterocyclic-1-carboxylate derivative and its pharmaceutically acceptable salt has a potent FAAH-inhibitory activity. Further, the pyridyl non-aromatic nitrogen-containing heterocyclic-1-carboxylate derivative of the present invention has an excellent effect for increasing an effective bladder capacity, an excellent effect for relieving urinary frequency and an excellent anti-allodynia effect, and is therefore usable for treatment of urinary frequency and urinary incontinence, overactive bladder and/or pain.

  [问题]提供一种可用于治疗与脂肪酸酰胺水解酶（FAAH）相关疾病的化合物，特别是用于治疗尿频和尿失禁、膀胱过度活动症和/或疼痛。 [解决方法]我们发现，一种新型吡啶基非芳香族含氮杂环-1-羧酸酯衍生物及其药学上可接受的盐具有强效的 FAAH 抑制活性。此外，本发明的吡啶基非芳香族含氮杂环-1-羧酸酯衍生物在增加有效膀胱容量方面效果显著，在缓解尿频方面效果显著，在抗排尿障碍方面效果显著，因此可用于治疗尿频和尿失禁、膀胱过度活动症和/或疼痛。
• Piperidine and piperazine carboxylates as FAAH inhibitors
  申请人：Astellas Pharma Inc.

  公开号：EP2607362A1

  公开（公告）日：2013-06-26

  [Problem] To provide a compound usable for treatment of diseases associated with fatty acid amide hydrolase (FAAH), especially for treatment of urinary frequency and urinary incontinence, overactive bladder and/or pain. [Means for Solution] We have found that a novel pyridyl non-aromatic nitrogen-containing heterocyclic-1-carboxylate derivative and its pharmaceutically acceptable salt has a potent FAAH-inhibitory activity. Further, the pyridyl non-aromatic nitrogen-containing heterocyclic-1-carboxylate derivative of the present invention has an excellent effect for increasing an effective bladder capacity, an excellent effect for relieving urinary frequency and an excellent anti-allodynia effect, and is therefore usable for treatment of urinary frequency and urinary incontinence, overactive bladder and/or pain.

  [问题]提供一种可用于治疗与脂肪酸酰胺水解酶（FAAH）相关疾病的化合物，特别是用于治疗尿频和尿失禁、膀胱过度活动症和/或疼痛。 [解决方法]我们发现，一种新型吡啶基非芳香族含氮杂环-1-羧酸酯衍生物及其药学上可接受的盐具有强效的 FAAH 抑制活性。此外，本发明的吡啶基非芳香族含氮杂环-1-羧酸酯衍生物在增加有效膀胱容量方面效果显著，在缓解尿频方面效果显著，在抗排尿障碍方面效果显著，因此可用于治疗尿频和尿失禁、膀胱过度活动症和/或疼痛。