8-methoxy-5-methyl-2-[2-(2-phenyl-1H-imidazol-4-yl)-ethyl]-[1,2,4]triazolo[1,5-a]pyridine | 1312325-33-9

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 唑类
• 英文名称: 8-methoxy-5-methyl-2-[2-(2-phenyl-1H-imidazol-4-yl)-ethyl]-[1,2,4]triazolo[1,5-a]pyridine
• 英文别名: 8-methoxy-5-methyl-2-[2-(2-phenyl-1H-imidazol-5-yl)ethyl]-[1,2,4]triazolo[1,5-a]pyridine
• CAS: 1312325-33-9
• 化学式: C₁₉H₁₉N₅O
• 分子量: 333.393
• InChiKey: PZXRSPLRNPVZSM-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.2
• 重原子数：
  25
• 可旋转键数：
  5
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.21
• 拓扑面积：
  68.1
• 氢给体数：
  1
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  8-methoxy-5-methyl-2-[2-(2-phenyl-1H-imidazol-4-yl)-ethyl]-[1,2,4]triazolo[1,5-a]pyridine 、 碘甲烷 在 caesium carbonate 作用下， 以 丁酮 为溶剂， 反应 7.0h， 以20%的产率得到8-methoxy-5-methyl-2-[2-(1-methyl-2-phenyl-1H-imidazol-4-yl)-ethyl]-[1,2,4]triazolo[1,5-a]pyridine
  参考文献：
  名称：

  [EN] 2-ARYLIMIDAZOLE DERIVATIVES AS PDE10A ENZYME INHIBITORS
  [FR] DÉRIVÉS DE 2-ARYLIMIDAZOLE EN TANT QU'INHIBITEURS DE L'ENZYME PDE10A

  摘要：

  这项发明涉及一类PDE10A酶抑制剂化合物。该发明提供了一种包含本发明化合物的治疗有效量和药学可接受载体的药物组合物。本发明还提供了制备式(I)化合物的方法。本发明进一步提供了一种治疗神经退行性疾病的方法，包括向患有神经退行性疾病的对象施用式(I)化合物的治疗有效量。本发明还提供了一种治疗药物成瘾的方法，包括向患有药物成瘾的对象施用式(I)化合物的治疗有效量。本发明还提供了一种治疗精神障碍的方法，包括向患有精神障碍的对象施用式(I)化合物的治疗有效量。

  公开号：

  WO2011072696A1

文献信息

• 2-ARYLIMIDAZOLE DERIVATIVES AS PDE10A ENZYME INHIBITORS
  申请人：Püschl Ask

  公开号：US20120302548A1

  公开（公告）日：2012-11-29

  This invention is directed to compounds, which are PDE10A enzyme inhibitors. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. The present invention also provides processes for the preparation of the compounds of formula I. The present invention further provides a method of treating a subject suffering from a neurodegenerative disorder comprising administering to the subject a therapeutically effective amount of a compound of formula I. The present invention also provides a method of treating a subject suffering from a drug addiction comprising administering to the subject a therapeutically effective amount of a compound of formula I. The present invention further provides a method of treating a subject suffering from a psychiatric disorder comprising administering to the subject a therapeutically effective amount of a compound of formula I.

  本发明涉及一种PDE10A酶抑制剂化合物。本发明提供一种药物组合物，该药物组合物包括本发明的化合物的治疗有效量和药学上可接受的载体。本发明还提供了制备式I化合物的方法。本发明还提供了一种治疗神经退行性疾病的方法，包括向患者施用式I化合物的治疗有效量。本发明还提供了一种治疗药物成瘾的方法，包括向患者施用式I化合物的治疗有效量。本发明还提供了一种治疗精神障碍的方法，包括向患者施用式I化合物的治疗有效量。
• (2-aryl-1H-imidazol-4-yl)-linked heterocycle derivatives
  申请人：Püschl Ask

  公开号：US08501797B2

  公开（公告）日：2013-08-06

  This invention is directed to compounds of formula I having the structure which are PDE10A enzyme inhibitors. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. The present invention also provides processes for the preparation of the compounds of formula I. The present invention further provides a method of treating a subject suffering from a neurodegenerative disorder comprising administering to the subject a therapeutically effective amount of a compound of formula I The present invention also provides a method of treating a subject suffering from a drug addiction comprising administering to the subject a therapeutically effective amount of a compound of formula I. The present invention further provides a method of treating a subject suffering from a psychiatric disorder comprising administering to the subject a therapeutically effective amount of a compound of formula I.

  本发明涉及公式I的化合物，其结构为，这些化合物是PDE10A酶抑制剂。本发明提供了一种药物组合物，包括本发明化合物的治疗有效量和药学上可接受的载体。本发明还提供了制备公式I化合物的方法。本发明还提供了一种治疗神经退行性疾病的方法，包括向患者输注本发明化合物的治疗有效量。本发明还提供了一种治疗药物成瘾的方法，包括向患者输注本发明化合物的治疗有效量。本发明还提供了一种治疗精神障碍的方法，包括向患者输注本发明化合物的治疗有效量。
• 2-arylimidazole derivatives as PDE10A enzyme inhibitors
  申请人：H. Lundbeck A/S

  公开号：US08927738B2

  公开（公告）日：2015-01-06

  This invention is directed to compounds of formula I having the structure which are PDE10A enzyme inhibitors. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. The present invention also provides processes for the preparation of the compounds of formula I. The present invention further provides a method of treating a subject suffering from a neurodegenerative disorder comprising administering to the subject a therapeutically effective amount of a compound of formula I. The present invention also provides a method of treating a subject suffering from a drug addiction comprising administering to the subject a therapeutically effective amount of a compound of formula I. The present invention further provides a method of treating a subject suffering from a psychiatric disorder comprising administering to the subject a therapeutically effective amount of a compound of formula I.

  本发明涉及一种具有以下结构的公式I化合物，它们是PDE10A酶抑制剂。本发明提供了一种制药组合物，包括本发明化合物的治疗有效量和药学上可接受的载体。本发明还提供了制备公式I化合物的方法。本发明还提供了一种治疗神经退行性疾病的方法，包括向患者施用公式I化合物的治疗有效量。本发明还提供了一种治疗药物成瘾的方法，包括向患者施用公式I化合物的治疗有效量。本发明还提供了一种治疗精神障碍的方法，包括向患者施用公式I化合物的治疗有效量。
• US8501797B2
  申请人：——

  公开号：US8501797B2

  公开（公告）日：2013-08-06
• US8927738B2
  申请人：——

  公开号：US8927738B2

  公开（公告）日：2015-01-06