1-[(pyridin-3-yloxy)carbonyl]piperidine-4-carboxylic acid

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 哌啶类
• 英文名称: 1-[(pyridin-3-yloxy)carbonyl]piperidine-4-carboxylic acid
• 英文别名: 1-pyridin-3-yloxycarbonylpiperidine-4-carboxylic acid
• 化学式: C₁₂H₁₄N₂O₄
• 分子量: 250.254
• InChiKey: DRLUILPXAKTSBS-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.6
• 重原子数：
  18
• 可旋转键数：
  3
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.42
• 拓扑面积：
  79.7
• 氢给体数：
  1
• 氢受体数：
  5

反应信息

• 作为反应物：
  描述：

  1-[(pyridin-3-yloxy)carbonyl]piperidine-4-carboxylic acid 、 环己甲胺 在 1-羟基苯并三唑 、 盐酸-N-乙基-Nˊ-(3-二甲氨基丙基)碳二亚胺 作用下， 以 N,N-二甲基甲酰胺 为溶剂， 反应 15.0h， 生成 (pyridin-3-yl) 4-{[(cyclohexylmethyl)amino]carbonyl}piperidine-1-carboxylate
  参考文献：
  名称：

  Piperazine derivatives for the treatment of urinary incontinence and pain

  摘要：

  公开号：

  EP1849773B1
• 作为产物：
  描述：

  4-ethyl 1-pyridin-3-yl piperidine-1,4-dicarboxylate 生成 1-[(pyridin-3-yloxy)carbonyl]piperidine-4-carboxylic acid
  参考文献：
  名称：

  Pyridyl non-aromatic nitrogen-containing heterocyclic-1-carboxylate compound

  摘要：

  为了治疗与脂肪酸酰胺水解酶（FAAH）相关的疾病，特别是治疗尿频和尿失禁、过度活动的膀胱和/或疼痛，提供一种化合物。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-羧酸酯衍生物对增加有效膀胱容量、缓解尿频和具有出色的抗痛觉过敏效果，因此可用于治疗尿频和尿失禁、过度活动的膀胱和/或疼痛。

  公开号：

  US07919495B2

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。
• Azole compound
  申请人：Astellas Pharma Inc.

  公开号：US08207199B2

  公开（公告）日：2012-06-26

  A compound which is useful as an active ingredient of a pharmaceutical composition for treating neuropathic pain is provided. The present inventors have made extensive studies on compounds having an FAAH inhibitory activity, and as a result, have found that an azole compound substituted with an N-(pyridine-3-yl)oxycarbonyl-piperidin-4-yl group and a phenyl group or a pharmaceutically acceptable salt thereof has an excellent FAAH inhibitory activity, thereby completing the present invention. The compound of the present invention is confirmed to have an excellent FAAH inhibitory activity and an antiallodynic effect in rat models with neuropathic pain, and thus is useful as an agent for preventing and/or an agent for treating neuropathic pain.

  提供了一种化合物，该化合物可作为制备用于治疗神经病性疼痛的药物组合物的活性成分。本发明人对具有FAAH抑制活性的化合物进行了广泛的研究，并发现一种咪唑化合物，其取代有N-(吡啶-3-基)氧羰基哌啶-4-基团和苯基，或其药学上可接受的盐具有出色的FAAH抑制活性，从而完成了本发明。本发明的化合物已被证实在神经病性疼痛的大鼠模型中具有出色的FAAH抑制活性和抗痛觉过敏作用，因此可用作预防和/或治疗神经病性疼痛的药剂。
• 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。