6-(((1S,2S)-2-(5-(difluoromethoxy)pyridin-2-yl)cyclopropyl)methoxy)-2-methyl-4-((5-methyl-1,3,4-thiadiazol-2-yl)methylamino)pyridazin-3(2H)-one

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二嗪类
• 英文名称: 6-(((1S,2S)-2-(5-(difluoromethoxy)pyridin-2-yl)cyclopropyl)methoxy)-2-methyl-4-((5-methyl-1,3,4-thiadiazol-2-yl)methylamino)pyridazin-3(2H)-one
• 英文别名: 6-[[(1S,2S)-2-[5-(difluoromethoxy)pyridin-2-yl]cyclopropyl]methoxy]-2-methyl-4-[(5-methyl-1,3,4-thiadiazol-2-yl)methylamino]pyridazin-3-one
• 化学式: C₁₉H₂₀F₂N₆O₃S
• 分子量: 450.469
• InChiKey: GEUKVFCTVXQZGN-YPMHNXCESA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.5
• 重原子数：
  31
• 可旋转键数：
  9
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.42
• 拓扑面积：
  130
• 氢给体数：
  1
• 氢受体数：
  11

文献信息

• [EN] SUBSTITUTED PYRIDIZINONE DERIVATIVES AS PDE10 INHIBITORS<br/>[FR] DÉRIVÉS DE PYRIDIZINONE SUBSTITUÉS UTILISÉS EN TANT QU'INHIBITEURS DE LA PDE10
  申请人：MERCK SHARP & DOHME

  公开号：WO2014139150A1

  公开（公告）日：2014-09-18

  The present invention is directed to substituted pyridizinone compounds of formula (I) 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.

  本发明涉及一种具有式（I）的取代吡啶酮化合物，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种化合物治疗神经学和精神疾病，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节功能障碍相关的疾病。
• SUBSTITUTED PYRIDIZINONE DERIVATIVES AS PDE10 INHIBITORS
  申请人：KUDUK Scott D.

  公开号：US20160016947A1

  公开（公告）日：2016-01-21

  The present invention is directed to substituted pyridizinone compounds of formula I 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.

  本发明涉及公式I的取代吡啶嗪酮化合物，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是有用的。本发明还涉及使用这些化合物治疗神经和精神障碍，例如精神分裂症、精神病或亨廷顿病，以及与纹状体低功能或基底节功能障碍相关的疾病。
• SUBSTITUTED PYRIDAZINONE DERIVATIVES AS PDE10 INHIBITORS
  申请人：Merck Sharp & Dohme Corp.

  公开号：EP2968324B1

  公开（公告）日：2018-04-18
• US9353104B2
  申请人：——

  公开号：US9353104B2

  公开（公告）日：2016-05-31
• [EN] SUBSTITUTED PYRIDIZINONE DERIVATIVES AS PDE10 INHIBITORS<br/>[FR] DÉRIVÉS DE PYRIDIZINONE SUBSTITUÉS EN TANT QU'INHIBITEURS DE PDE10
  申请人：MERCK SHARP & DOHME

  公开号：WO2014150114A1

  公开（公告）日：2014-09-25

  The present invention is directed to substituted pyridizinone compounds of formula I 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.