6-trifluoromethyl-3-amino-1,2-benzisoxazole | 81465-91-0

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯并异恶唑
• 英文名称: 6-trifluoromethyl-3-amino-1,2-benzisoxazole
• 英文别名: 6-Trifluoromethyl-benzo[d]isoxazol-3-ylamine；6-(trifluoromethyl)-1,2-benzoxazol-3-amine
• CAS: 81465-91-0
• 化学式: C₈H₅F₃N₂O
• 分子量: 202.136
• InChiKey: YYCXXQOOYBPTDY-UHFFFAOYSA-N

物化性质

• 沸点：
  304.2±37.0 °C(Predicted)
• 密度：
  1.493±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  2.2
• 重原子数：
  14
• 可旋转键数：
  0
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.12
• 拓扑面积：
  52
• 氢给体数：
  1
• 氢受体数：
  6

反应信息

• 作为产物：
  描述：

  2-氟-4-三氟甲基苯腈 、 alkaline earth salt of/the/ methylsulfuric acid 在 盐酸 、 potassium tert-butylate 、 三氟乙酸 作用下， 生成 6-trifluoromethyl-3-amino-1,2-benzisoxazole
  参考文献：
  名称：

  Use of the Kaiser Oxime Resin in the Solid-Phase Synthesis of 3-Aminobenzisoxazoles

  摘要：

  DOI：

  10.1021/jo9901034

文献信息

• [EN] AMINOBENZISOXAZOLE COMPOUNDS AS AGONISTS OF A7-NICOTINIC ACETYLCHOLINE RECEPTORS<br/>[FR] COMPOSÉS D'AMINOBENZISOXAZOLE EN TANT QU'AGONISTES DES RÉCEPTEURS DE L'ACÉTYLCHOLINE Α7-NICOTINIQUE
  申请人：FORUM PHARMACEUTICALS INC

  公开号：WO2016201096A1

  公开（公告）日：2016-12-15

  The present invention relates to novel aminobenzisoxazole compounds, and pharmaceutical compositions of the same, that are suitable as agonists or partial agonists of ot7-nAChR, and methods of preparing these compounds and compositions, and the use of these compounds and compositions in methods of maintaining, treating and/or improving cognitive function. In particular, methods of administering the compound or composition to a patient in need thereof, for example a patient with a cognitive deficiency and/or a desire to enhance cognitive function, that may derive a benefit therefrom.

  本发明涉及新型氨基苯并异噁唑化合物及其药物组合物，适用作ot7-nAChR的激动剂或部分激动剂，以及制备这些化合物和组合物的方法，以及利用这些化合物和组合物在维持、治疗和/或改善认知功能的方法。具体而言，本发明涉及将该化合物或组合物用于需要的患者的给药方法，例如认知功能缺陷和/或希望增强认知功能的患者，可能从中获益。
• Aminobenzisoxazole compounds as agonists of α7-nicotinic acetylcholine receptors
  申请人：FORUM PHARMACEUTICALS, INC.

  公开号：US10370370B2

  公开（公告）日：2019-08-06

  The present invention relates to novel aminobenzisoxazole compounds, and pharmaceutical compositions of the same, that are suitable as agonists or partial agonists of Alpha7-nAChR, and methods of preparing these compounds and compositions, and the use of these compounds and compositions in methods of maintaining, treating and/or improving cognitive function. In particular, methods of administering the compound or composition to a patient in need thereof, for example a patient with a cognitive deficiency and/or a desire to enhance cognitive function, that may derive a benefit therefrom.

  本发明涉及适用于作为 Alpha7-nAChR 激动剂或部分激动剂的新型氨基苯并异噁唑化合物及其药物组合物、制备这些化合物和组合物的方法，以及将这些化合物和组合物用于维持、治疗和/或改善认知功能的方法。特别是，将化合物或组合物施用给有需要的患者的方法，例如，有认知缺陷和/或希望提高认知功能的患者，这些患者可从中获益。
• AMINOBENZISOXAZOLE COMPOUNDS AS AGONISTS OF A7-NICOTINIC ACETYLCHOLINE RECEPTORS
  申请人：Axovant Sciences GmbH

  公开号：EP3307269A1

  公开（公告）日：2018-04-18
• Aminobenzisoxazole Compounds as Agonists of Alpha7-Nicotinic Acetylcholine Receptors
  申请人：FORUM PHARMACEUTICALS, INC.

  公开号：US20180134696A1

  公开（公告）日：2018-05-17

  The present invention relates to novel aminobenzisoxazole compounds, and pharmaceutical compositions of the same, that are suitable as agonists or partial agonists of Alpha7-nAChR, and methods of preparing these compounds and compositions, and the use of these compounds and compositions in methods of maintaining, treating and/or improving cognitive function. In particular, methods of administering the compound or composition to a patient in need thereof, for example a patient with a cognitive deficiency and/or a desire to enhance cognitive function, that may derive a benefit therefrom.
• Use of the Kaiser Oxime Resin in the Solid-Phase Synthesis of 3-Aminobenzisoxazoles
  作者：Salvatore D. Lepore、Michael R. Wiley

  DOI：10.1021/jo9901034

  日期：1999.6.1