N-piperidin-4-yl-6-(trifluoromethyl)pyridazin-3-amine | 935981-71-8

• 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: N-piperidin-4-yl-6-(trifluoromethyl)pyridazin-3-amine
• 英文别名: n-Piperidin-4-yl-6-(trifluormethyl)pyridazin-3-amine
• CAS: 935981-71-8
• 化学式: C₁₀H₁₃F₃N₄
• mdl: MFCD25732854
• 分子量: 246.235
• InChiKey: CVOFGOFXRSCPTA-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.2
• 重原子数：
  17
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.6
• 拓扑面积：
  49.8
• 氢给体数：
  2
• 氢受体数：
  7

反应信息

• 作为反应物：
  描述：

  N-piperidin-4-yl-6-(trifluoromethyl)pyridazin-3-amine 、 3',4'-二氟苯乙酮 在 titanium(IV) isopropylate 、 sodium cyanoborohydride 作用下， 以 乙醇 为溶剂， 反应 2.0h， 以55%的产率得到N-[1-(3,4-difluoro-α-methylbenzyl)piperidin-4-yl]-6-(trifluoromethyl)pyridazin-3-amine
  参考文献：
  名称：

  WO2007/48779

  摘要：

  公开号：
• 作为产物：
  描述：

  tert-butyl 4-{[6-(trifluoromethyl)pyridazin-3-yl]amino}piperidine-1-carboxylate 以95的产率得到N-piperidin-4-yl-6-(trifluoromethyl)pyridazin-3-amine
  参考文献：
  名称：

  Crystal form of phenylamino pyrimidine derivatives

  摘要：

  本发明涉及(3,5-双三氟甲基)-N-[4-甲基-3-(4-吡啶-3-基-嘧啶-2-基氨基)-苯基]-苯甲酰胺（式I）的一种特定结晶形式，其制备方法，含有该结晶形式的制药组合物以及其作为人类抗肿瘤剂的用途。式I化合物，也称为AN-019。

  公开号：

  US08067422B2

文献信息

• Crystal form of phenylamino pyrimidine derivatives
  申请人：Natco Pharma Limited

  公开号：US08067422B2

  公开（公告）日：2011-11-29

  The present invention relates to a particular form of the (3,5-bis trifluoromethyl)-N-[4-methyl-3-(4-pyridin-3yl-pyrimidin-2ylamino)-phenyl]-benzamide (formula I), processes for the preparation thereof, pharmaceutical compositions containing this crystal form, and their use as anti tumor agent in humans. The compound of formula I, also known as AN-019, is:

  本发明涉及(3,5-双三氟甲基)-N-[4-甲基-3-(4-吡啶-3-基-嘧啶-2-基氨基)-苯基]-苯甲酰胺（式I）的一种特定结晶形式，其制备方法，含有该结晶形式的制药组合物以及其作为人类抗肿瘤剂的用途。式I化合物，也称为AN-019。
• Piperidin-4-Yl-Pyridazin-3-Ylamine Derivatives as Fast Dissociating Dopamine 2 Receptor Antagonists
  申请人：De Bruyn Marcel Frans Leopold

  公开号：US20080227791A1

  公开（公告）日：2008-09-18

  The present invention relates to compounds that are fast dissociating dopamine 2 receptor antagonists, processes for preparing these compounds, pharmaceutical compositions comprising these compounds as an active ingredient. The compounds find utility as medicines for treating or preventing central nervous system disorders, for example schizophrenia, by exerting an antipsychotic effect without motor side effects.

  本发明涉及快速解离的多巴胺2受体拮抗剂化合物，制备这些化合物的方法，以及包含这些化合物作为活性成分的制药组合物。这些化合物可用作治疗或预防中枢神经系统疾病的药物，例如精神分裂症，通过发挥抗精神病作用而不产生运动副作用。
• PIPERIDIN-4-YL-PYRIDAZIN-3-YLAMINE DERIVATIVES AS FAST DISSOCIATING DOPAMINE 2 RECEPTOR ANTAGONISTS
  申请人：Janssen Pharmaceutica N.V.

  公开号：US20150141432A1

  公开（公告）日：2015-05-21

  The present invention relates to compounds that are fast dissociating dopamine 2 receptor antagonists, processes for preparing these compounds, pharmaceutical compositions comprising these compounds as an active ingredient. The compounds find utility as medicines for treating or preventing central nervous system disorders, for example schizophrenia, by exerting an antipsychotic effect without motor side effects.

  本发明涉及快速解离的多巴胺2受体拮抗剂化合物，制备这些化合物的方法，以及包含这些化合物作为活性成分的制药组合物。这些化合物可用作治疗或预防中枢神经系统疾病的药物，例如精神分裂症，通过发挥抗精神病作用而不产生运动副作用。
• Piperidin-4-yl-pyridazin-3-ylamine derivatives as fast dissociating dopamine 2 receptor antagonists
  申请人：De Bruyn Marcel Frans Leopold

  公开号：US08940743B2

  公开（公告）日：2015-01-27

  The present invention relates to compounds that are fast dissociating dopamine 2 receptor antagonists, processes for preparing these compounds, pharmaceutical compositions comprising these compounds as an active ingredient. The compounds find utility as medicines for treating or preventing central nervous system disorders, for example schizophrenia, by exerting an antipsychotic effect without motor side effects.

  本发明涉及快速解离的多巴胺2受体拮抗剂化合物，制备这些化合物的过程，以及以这些化合物作为活性成分的制药组合物。这些化合物可用作治疗或预防中枢神经系统疾病的药物，例如精神分裂症，通过产生抗精神病作用而不产生运动副作用。
• FAST DISSOCIATING DOPAMINE 2 RECEPTOR ANTAGONISTS
  申请人：De Bruyn Marcel Frans Leopold

  公开号：US20170022181A1

  公开（公告）日：2017-01-26

  The present invention relates to compounds that are fast dissociating dopamine 2 receptor antagonists, processes for preparing these compounds, pharmaceutical compositions comprising these compounds as an active ingredient. The compounds find utility as medicines for treating or preventing central nervous system disorders, for example schizophrenia, by exerting an antipsychotic effect without motor side effects.