2-[2-(5,8-dimethyl-[1,2,4]triazolo[1,5-a]pyrazin-2-yl)propyl]-5H-imidazo[2,1-a]isoindole | 1447715-71-0

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 三唑并吡嗪类
• 英文名称: 2-[2-(5,8-dimethyl-[1,2,4]triazolo[1,5-a]pyrazin-2-yl)propyl]-5H-imidazo[2,1-a]isoindole
• CAS: 1447715-71-0
• 化学式: C₂₀H₂₀N₆
• 分子量: 344.419
• InChiKey: AZLYDFXTIFIBDK-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.5
• 重原子数：
  26
• 可旋转键数：
  3
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.3
• 拓扑面积：
  60.9
• 氢给体数：
  0
• 氢受体数：
  4

反应信息

• 作为产物：
  描述：

  2-氨基-3,6-二甲基吡嗪 在 palladium 10% on activated carbon 、 氢气 、 2,4,6-三甲基苯磺酰羟胺 、 溶剂黄146 、 1,8-二氮杂双环[5.4.0]十一碳-7-烯 作用下， 以 甲醇 、 乙醇 、 二氯甲烷 、 乙腈 为溶剂， 20.0~200.0 ℃ 、300.01 kPa 条件下， 反应 100.33h， 生成 2-[2-(5,8-dimethyl-[1,2,4]triazolo[1,5-a]pyrazin-2-yl)propyl]-5H-imidazo[2,1-a]isoindole
  参考文献：
  名称：

  [EN] IMIDAZOLE DERIVATIVES AS PDE10A ENZYME INHIBITORS
  [FR] DÉRIVÉS D'IMIDAZOLE UTILISÉS COMME INHIBITEURS D'ENZYMES PDE10A

  摘要：

  这项发明涉及一种PDE10A酶抑制剂化合物。该发明提供了包括该发明化合物的治疗有效量和药用载体的药物组合物。本发明还提供了制备式I化合物的方法。本发明还提供了一种治疗患有神经退行性疾病的受试者的方法，包括向受试者投予式I化合物的治疗有效量。本发明还提供了一种治疗患有药物成瘾的受试者的方法，包括向受试者投予式I化合物的治疗有效量。本发明还提供了一种治疗患有精神障碍的受试者的方法，包括向受试者投予式I化合物的治疗有效量。

  公开号：

  WO2013107856A1

文献信息

• [EN] IMIDAZOLE DERIVATIVES AS PDE10A ENZYME INHIBITORS<br/>[FR] DÉRIVÉS D'IMIDAZOLE UTILISÉS COMME INHIBITEURS D'ENZYMES PDE10A
  申请人：LUNDBECK & CO AS H

  公开号：WO2013107856A1

  公开（公告）日：2013-07-25

  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. 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.

  这项发明涉及一种PDE10A酶抑制剂化合物。该发明提供了包括该发明化合物的治疗有效量和药用载体的药物组合物。本发明还提供了制备式I化合物的方法。本发明还提供了一种治疗患有神经退行性疾病的受试者的方法，包括向受试者投予式I化合物的治疗有效量。本发明还提供了一种治疗患有药物成瘾的受试者的方法，包括向受试者投予式I化合物的治疗有效量。本发明还提供了一种治疗患有精神障碍的受试者的方法，包括向受试者投予式I化合物的治疗有效量。