3-[5-(2-fluoro-3-methoxy-phenyl)-pyridin-2-yloxy]-azetidine-1-carboxylic acid pyridazin-3-ylamide | 1186234-40-1

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡啶及其衍生物
• 英文名称: 3-[5-(2-fluoro-3-methoxy-phenyl)-pyridin-2-yloxy]-azetidine-1-carboxylic acid pyridazin-3-ylamide
• 英文别名: 3-[5-(2-fluoro-3-methoxyphenyl)pyridin-2-yl]oxy-N-pyridazin-3-ylazetidine-1-carboxamide
• CAS: 1186234-40-1
• 化学式: C₂₀H₁₈FN₅O₃
• 分子量: 395.393
• InChiKey: GQVNLDQKGBHOIC-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.8
• 重原子数：
  29
• 可旋转键数：
  5
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.2
• 拓扑面积：
  89.5
• 氢给体数：
  1
• 氢受体数：
  7

反应信息

• 作为产物：
  描述：

  3-(5-bromo-pyridin-2-yloxy)-azetidine-1-carboxylic acid 4-nitro-phenyl ester 在 1,1'-双(二苯膦基)二茂铁二氯化钯(II)二氯甲烷复合物 sodium hydride 、 potassium carbonate 作用下， 以 四氢呋喃 、 水 、 N,N-二甲基甲酰胺 、 mineral oil 为溶剂， 反应 0.5h， 生成 3-[5-(2-fluoro-3-methoxy-phenyl)-pyridin-2-yloxy]-azetidine-1-carboxylic acid pyridazin-3-ylamide
  参考文献：
  名称：

  [EN] AZETIDINE DERIVATIVES
  [FR] DÉRIVÉS D'AZÉTIDINE

  摘要：

  式（I）的化合物是脂肪酸酰胺水解酶（FAAH）的抑制剂，对于需要抑制FAAH活性的疾病或医疗状况具有益处，如焦虑、抑郁、疼痛、炎症、进食、睡眠、神经退行性和运动障碍：式（I）其中Ar1是可选择取代的苯基或可选择取代的具有5或6个环原子的单环杂芳基；Ar2是可选择取代的苯基，可选择取代的具有5或6个环原子的单环杂芳基或在每个融合环中具有5或6个环原子的可选择取代的融合双环杂芳基；Ar3是从可选择取代的苯基和可选择取代的具有5或6个环原子的单环杂芳基基团组成的羰基基团。

  公开号：

  WO2009109743A1

文献信息

• Azetidine derivatives as FAAH inhibitors
  申请人：Roughley Stephen

  公开号：US08450346B2

  公开（公告）日：2013-05-28

  Compounds of formula (I) are inhibitors of fatty acid amide hydrolase, (FAAH), and which are useful in the treatment of diseases or medical conditions which benefit from inhibition of FAAH activity, such as anxiety, depression pain, inflammation, and eating, sleep, neurodegenerative and movement disorders: Formula (I) Wherein Ar1 is optionally substituted phenyl or optionally substituted monocyclic heteroaryl having 5 or 6 ring atoms; Ar2 is optionally substituted phenyl, optionally substituted monocyclic heteroaryl having 5 or 6 ring atoms or optionally substituted fused bicyclic heteroaryl having 5 or 6 ring atoms in each fused ring; and Ar3 is a divalent radical selected from the group consisting of optionally substituted phenylene and optionally substituted monocyclic heteroarylene radicals having 5 or 6 ring atoms.

  公式（I）的化合物是脂肪酸酰胺水解酶（FAAH）的抑制剂，对于需要抑制FAAH活性的疾病或医疗条件的治疗非常有用，如焦虑、抑郁、疼痛、炎症、进食、睡眠、神经退行性和运动障碍等： 公式（I）中，Ar1是可选择的取代苯基或可选择的取代的含有5或6个环原子的单环杂芳基；Ar2是可选择的取代苯基、可选择的取代含有5或6个环原子的单环杂芳基或可选择的取代融合的双环杂芳基，在每个融合环中有5或6个环原子；Ar3是从可选择的取代苯撑基和可选择的取代含有5或6个环原子的单环杂芳撑基的群中选择的二价基团。
• Azetidine Derivatives
  申请人：Roughley Stephen

  公开号：US20120028953A1

  公开（公告）日：2012-02-02

  Compounds of formula (I) are inhibitors of fatty acid amide hydrolase, (FAAH), and which are useful in the treatment of diseases or medical conditions which benefit from inhibition of FAAH activity, such as anxiety, depression pain, inflammation, and eating, sleep, neurodegenerative and movement disorders: Formula (I) Wherein Ar 1 is optionally substituted phenyl or optionally substituted monocyclic heteroaryl having 5 or 6 ring atoms; Ar 2 is optionally substituted phenyl, optionally substituted monocyclic heteroaryl having 5 or 6 ring atoms or optionally substituted fused bicyclic heteroaryl having 5 or 6 ring atoms in each fused ring; and Ar 3 is a divalent radical selected from the group consisting of optionally substituted phenylene and optionally substituted monocyclic heteroarylene radicals having 5 or 6 ring atoms.

  公式（I）的化合物是脂肪酸酰胺水解酶（FAAH）的抑制剂，对于需要抑制FAAH活性的疾病或医疗条件具有治疗作用，例如焦虑、抑郁、疼痛、炎症、饮食、睡眠、神经退行性和运动障碍：公式（I）中，Ar1是可选取取代苯基或可选取取代的5或6个环原子的单环杂芳基；Ar2是可选取取代苯基、可选取取代的5或6个环原子的单环杂芳基或在每个融合环中具有5或6个环原子的可选取取代的融合双环杂芳基；而Ar3是从可选取取代的苯基和可选取取代的5或6个环原子的单环杂芳基组成的二价基团中选择的。
• Azetidine derivatives
  申请人：Vernalis (R&D) Ltd.

  公开号：US09006269B2

  公开（公告）日：2015-04-14

  Compounds of formula (I) are inhibitors of fatty acid amide hydrolase, (FAAH), and which are useful in the treatment of diseases or medical conditions which benefit from inhibition of FAAH activity, such as anxiety, depression pain, inflammation, and eating, sleep, neurodegenerative and movement disorders: Wherein Ar1 is optionally substituted phenyl or optionally substituted monocyclic heteroaryl having 5 or 6 ring atoms; Ar2 is optionally substituted phenyl, optionally substituted monocyclic heteroaryl having 5 or 6 ring atoms or optionally substituted fused bicyclic heteroaryl having 5 or 6 ring atoms in each fused ring; and Ar3 is a divalent radical selected from the group consisting of optionally substituted phenylene and optionally substituted monocyclic heteroarylene radicals having 5 or 6 ring atoms.

  式（I）的化合物是脂肪酸酰胺水解酶（FAAH）的抑制剂，对于需要抑制FAAH活性的疾病或医疗状况具有治疗作用，例如焦虑、抑郁、疼痛、炎症、进食、睡眠、神经退行性和运动障碍： 其中Ar1是可以选择性取代的苯基或具有5或6个环原子的可以选择性取代的单环杂芳基；Ar2是可以选择性取代的苯基，具有5或6个环原子的可以选择性取代的单环杂芳基或在每个融合环中具有5或6个环原子的可以选择性取代的融合双环杂芳基；Ar3是从包括可以选择性取代的苯撑基和具有5或6个环原子的可以选择性取代的单环杂芳撑基的基团中选择的二价基团。
• AZETIDINE DERIVATIVES
  申请人：Vernalis (R&D) Ltd.

  公开号：EP2265578A1

  公开（公告）日：2010-12-29
• US8450346B2
  申请人：——

  公开号：US8450346B2

  公开（公告）日：2013-05-28