5-fluoro-N-4-[(5-methyl-1,3,4-thiadiazol-2-yl)methyl]-6-{[(1S,2S)-2-(1,5-naphthyridin-2-yl)cyclopropyl]methoxy}pyrimidine-2,4-diamine | 1424374-01-5

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡啶并嘧啶类
• 英文名称: 5-fluoro-N-4-[(5-methyl-1,3,4-thiadiazol-2-yl)methyl]-6-{[(1S,2S)-2-(1,5-naphthyridin-2-yl)cyclopropyl]methoxy}pyrimidine-2,4-diamine
• 英文别名: 5-Fluoro-N-4-[(5-methyl-1,3,4-thiadiazol-2-yl)methyl]-6-{[(1S,2S)-2-(1,5-naphthyridin-2-yl)cyclopropyl]methoxy}pyrimidin-2,4-diamin；5-fluoro-4-N-[(5-methyl-1,3,4-thiadiazol-2-yl)methyl]-6-[[(1S,2S)-2-(1,5-naphthyridin-2-yl)cyclopropyl]methoxy]pyrimidine-2,4-diamine
• CAS: 1424374-01-5
• 化学式: C₂₀H₁₉FN₈OS
• 分子量: 438.488
• InChiKey: RJGPJDKFDMFUNY-NEPJUHHUSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.4
• 重原子数：
  31
• 可旋转键数：
  7
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.3
• 拓扑面积：
  153
• 氢给体数：
  2
• 氢受体数：
  11

文献信息

• [EN] PYRIMIDINE PDE10 INHIBITORS<br/>[FR] INHIBITEURS PYRIMIDINES DE PDE10
  申请人：MERCK SHARP & DOHME

  公开号：WO2013028590A1

  公开（公告）日：2013-02-28

  The present invention is directed to pyrimidine compounds which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 10 (PDE10). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.

  本发明涉及嘧啶化合物，其可用作治疗与磷酸二酯酶10（PDE10）相关的中枢神经系统疾病的治疗剂。本发明还涉及利用这些化合物治疗神经系统和精神疾病，如精神分裂症、精神病或亨廷顿病，以及与纹状体功能不足或基底神经节功能障碍相关的疾病。
• PYRIMIDINE PDE10 INHIBITORS
  申请人：Cox Christopher D.

  公开号：US20140228368A1

  公开（公告）日：2014-08-14

  The present invention is directed to pyrimidine compounds which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 10 (PDE10). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.

  本发明涉及嘧啶化合物，其作为治疗与磷酸二酯酶10（PDE10）相关的中枢神经系统疾病的治疗剂。本发明还涉及使用这些化合物治疗神经系统和精神疾病，例如精神分裂症、精神病或亨廷顿病以及与纹状体功能减退或基底节功能障碍相关的疾病。
• EP2748151B1
  申请人：——

  公开号：EP2748151B1

  公开（公告）日：2016-03-16
• US9062059B2
  申请人：——

  公开号：US9062059B2

  公开（公告）日：2015-06-23