(7S,9aS)-7-(2,4-difluorophenoxy)methyl-2-(5-fluoro-pyrimidin-2-yl)-2,3,4,6,7,8,9,9a-octahydro-1H-pyrido[1,2-a]pyrazine

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二嗪烷类
• 英文名称: (7S,9aS)-7-(2,4-difluorophenoxy)methyl-2-(5-fluoro-pyrimidin-2-yl)-2,3,4,6,7,8,9,9a-octahydro-1H-pyrido[1,2-a]pyrazine
• 英文别名: (7S,9aS)-7-[(2,4-difluorophenoxy)methyl]-2-(5-fluoropyrimidin-2-yl)-1,3,4,6,7,8,9,9a-octahydropyrido[1,2-a]pyrazine
• 化学式: C₁₉H₂₁F₃N₄O
• 分子量: 378.397
• InChiKey: CKXICSUWGHINRM-BBRMVZONSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.2
• 重原子数：
  27
• 可旋转键数：
  4
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.47
• 拓扑面积：
  41.5
• 氢给体数：
  0
• 氢受体数：
  8

文献信息

• Dopamine D4 ligands for the treatment of novelty-seeking disorders
  申请人：——

  公开号：US20020049209A1

  公开（公告）日：2002-04-25

  The present invention provides a method of treating or preventing a novelty-seeking disorder such as pathological gambling, attention deficit disorder with hyperactivity disorder, substance addiction, drug addiction, alcohol addiction and sex addiction. using a compound which is a dopamine D4 receptor ligand, or a pharmaceutically acceptable salt thereof.

  本发明提供了一种治疗或预防新奇寻求障碍，如病理性赌博、注意力缺陷多动障碍、物质成瘾、药物成瘾、酒精成瘾和性成瘾的方法。所使用的化合物是多巴胺D4受体配体或其药学上可接受的盐。
• Dopamine D4 Ligands for the treatment of novelty-seeking disorders
  申请人：Pfizer Products Inc.

  公开号：EP1177792A2

  公开（公告）日：2002-02-06

  The use of a dopamine D4 receptor ligand in the manufacture of a medicament for the treatment or prevention of a novelty-seeking disorder, particularly pathological gambling, attention deficit disorder with hyperactivity disorder, substance addiction, drug addiction, alcohol addiction and sex addiction.

  使用多巴胺 D4 受体配体制造用于治疗或预防寻求新奇障碍的药物，特别是病态赌博、多动障碍性注意力缺陷症、药物成瘾、吸毒成瘾、酗酒成瘾和性成瘾。
• Combinations of D4 dopamine receptor antagonists with acetylcholine esterase inhibitors
  申请人：Pfizer Products Inc.

  公开号：EP1201268A2

  公开（公告）日：2002-05-02

  The present invention relates to a method of treating dementia or cognitive deficits associated with Alzheimer's Disease or Parkinson's Disease in a mammal, including a human, by administering to the mammal a D4 dopamine receptor antagonist in combination with an acetylcholine esterase inhibitor. It also relates to pharmaceutical compositions containing a pharmaceutically acceptable carrier, a D4 dopamine receptor antagonist and an acetylcholine esterase inhibitor.

  本发明涉及一种治疗与阿尔茨海默病或帕金森病相关的哺乳动物（包括人类）痴呆症或认知缺陷的方法，其方法是向哺乳动物施用 D4 多巴胺受体拮抗剂与乙酰胆碱酯酶抑制剂。它还涉及含有药学上可接受的载体、D4多巴胺受体拮抗剂和乙酰胆碱酯酶抑制剂的药物组合物。
• Combination treatment for depression, anxiety and psychosis comprising an antidepressant and/or anxiolytic and a D4 receptor antagonist
  申请人：Pfizer Products Inc.

  公开号：EP1213031A2

  公开（公告）日：2002-06-12

  The present invention relates to a method of treating depression, anxiety or psychosis in a mammal, including a human, by administering to the mammal a D4 receptor antagonist in combination with an antidepressant or an anxiolytic agent. It also relates to pharmaceutical compositions containing a pharmaceutically acceptable carrier, a D4 receptor antagonist and an antidepressant or an anxiolytic agent.

  本发明涉及一种治疗哺乳动物（包括人类）抑郁症、焦虑症或精神病的方法，其方法是向哺乳动物施用 D4 受体拮抗剂与抗抑郁剂或抗焦虑剂。它还涉及含有药学上可接受的载体、D4 受体拮抗剂和抗抑郁剂或抗焦虑剂的药物组合物。
• Combination treatment for dementia or cognitive deficits associated with alzheimer's disease and parkinson's disease
  申请人：——

  公开号：US20020052373A1

  公开（公告）日：2002-05-02

  The present invention relates to a method of treating dementia or cognitive deficits associated with Alzheimer's Disease or Parkinson's Disease in a mammal, including a human, by administering to the mammal a D4 dopamine receptor in combination with an acetylcholine esterase inhibitor. It also relates to pharmaceutical compositions containing a pharmaceutically acceptable carrier, a D4 dopamine receptor and an acetylcholine esterase inhibitor.

  本发明涉及一种治疗与阿尔茨海默病或帕金森病相关的哺乳动物（包括人类）痴呆症或认知缺陷的方法，其方法是向哺乳动物施用 D4 多巴胺受体与乙酰胆碱酯酶抑制剂。它还涉及含有药学上可接受的载体、D4 多巴胺受体和乙酰胆碱酯酶抑制剂的药物组合物。