5-(5-fluoro-1H-indol-2-yl)-N-methylpyridin-2-amine | 1053183-14-4

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吲哚及其衍生物
• 英文名称: 5-(5-fluoro-1H-indol-2-yl)-N-methylpyridin-2-amine
• 英文别名: 5-(5-fluoro-1H-indol-2-yl)-N-methylpyridine-2-amine
• CAS: 1053183-14-4
• 化学式: C₁₄H₁₂FN₃
• 分子量: 241.268
• InChiKey: VNLDZPGDHVKUHH-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.1
• 重原子数：
  18
• 可旋转键数：
  2
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.07
• 拓扑面积：
  40.7
• 氢给体数：
  2
• 氢受体数：
  3

反应信息

• 作为产物：
  描述：

  tert-butyl 5-fluoro-2-[6-(methylamino)pyridin-3-yl]-1H-indole-1-carboxylate 在 三氟乙酸 、 水 、 碳酸氢钠 作用下， 以 二氯甲烷 为溶剂， 反应 15.0h， 生成 5-(5-fluoro-1H-indol-2-yl)-N-methylpyridin-2-amine
  参考文献：
  名称：

  WO2008/108729

  摘要：

  公开号：

文献信息

• [EN] NOVEL SUBSTITUTED INDOLES<br/>[FR] NOUVEAUX INDOLES SUBSTITUÉS
  申请人：MERCK & CO INC

  公开号：WO2009155024A1

  公开（公告）日：2009-12-23

  The present invention relates to novel amyloid binding compounds and methods for measuring effects of the compounds, by measuring changes of amyloid plaque level in living patients. More specifically, the present invention relates to a method of using the compounds of this invention as tracers in positron emission tomography (PET) imaging to study amyloid deposits in brain in vivo to allow diagnosis of Alzheimer's disease. Thus, the present invention relates to use of the novel amyloid binding compounds as a diagnostic. The invention further relates to a method of measuring clinical efficacy of Alzheimer's disease therapeutic agents. Specifically, the present invention relates to novel aryl or heteroaryl substituted indole derivatives, compositions, and therapeutic uses and processes for making such compounds.

  本发明涉及新型淀粉样蛋白结合化合物和测量这些化合物效果的方法，通过测量活体患者中淀粉样斑块水平的变化。更具体地说，本发明涉及一种使用该发明化合物作为示踪剂的方法，用于正电子发射断层扫描（PET）成像研究大脑中的淀粉样沉积，以便诊断阿尔茨海默病。因此，本发明涉及将新型淀粉样蛋白结合化合物用作诊断的用途。该发明还涉及一种测量阿尔茨海默病治疗药物临床疗效的方法。具体而言，本发明涉及新型芳基或杂环芳基取代的吲哚衍生物、组合物和治疗用途，以及制备这类化合物的过程。
• Novel-2-Heteroaryl Substituted Indoles 695
  申请人：Arzel Erwan

  公开号：US20100098631A1

  公开（公告）日：2010-04-22

  The present invention relates to novel 2-heteroaryl substituted indole derivatives, precursors thereof, and therapeutic uses of such compounds, having the structural formula (Ia) below: and to their pharmaceutically acceptable salt, compositions and methods of use. Furthermore, the invention relates to novel 2-heteroaryl substituted indole derivatives that are suitable for imaging amyloid deposits in living patients, their compositions, methods of use and processes to make such compounds. More specifically, the present invention relates to a method of imaging amyloid deposits in brain in vivo to allow antemortem diagnosis of Alzheimer's disease as well as measuring clinical efficacy of Alzheimer?s disease therapeutic agents.

  本发明涉及新颖的2-杂环芳基取代吲哚衍生物、其前体物和这些化合物的治疗用途，具有下式（Ia）的结构式，以及它们的药学上可接受的盐、组合物和使用方法。此外，本发明还涉及适用于成像活体患者中淀粉样沉积物的新型2-杂环芳基取代吲哚衍生物、它们的组合物、使用方法和制备这些化合物的方法。更具体地说，本发明涉及一种在体内成像脑中的淀粉样沉积物，以允许抗死前诊断阿尔茨海默病，并测量阿尔茨海默病治疗剂的临床疗效的方法。
• Novel Substituted Indoles
  申请人：Barrow James C.

  公开号：US20110076230A1

  公开（公告）日：2011-03-31

  The present invention relates to novel amyloid binding compounds and methods for measuring effects of the compounds, by measuring changes of amyloid plaque level in living patients. More specifically, the present invention relates to a method of using the compounds of this invention as tracers in positron emission tomography (PET) imaging to study amyloid deposits in brain in vivo to allow diagnosis of Alzheimer's disease. Thus, the present invention relates to use of the novel amyloid binding compounds as a diagnostic. The invention further relates to a method of measuring clinical efficacy of Alzheimer's disease therapeutic agents. Specifically, the present invention relates to novel aryl or heteroaryl substituted indole derivatives, compositions, and therapeutic uses and processes for making such compounds.

  本发明涉及新型淀粉样蛋白结合化合物及测量这些化合物的效果的方法，通过测量活体患者淀粉样斑块水平的变化。更具体地，本发明涉及使用这些化合物作为追踪剂在正电子发射断层扫描（PET）成像中研究大脑内的淀粉样沉积物，以诊断阿尔茨海默病。因此，本发明涉及将新型淀粉样蛋白结合化合物用作诊断工具。本发明还涉及测量阿尔茨海默病治疗药物的临床疗效的方法。具体而言，本发明涉及新型芳基或杂环芳基取代的吲哚衍生物、组成物和治疗用途以及制备这些化合物的过程。
• NOVEL 2-HETEROARYL SUBSTITUTED INDOLES 695
  申请人：AstraZeneca AB

  公开号：EP2121655A1

  公开（公告）日：2009-11-25
• NOVEL SUBSTITUTED INDOLES
  申请人：Merck Sharp & Dohme Corp.

  公开号：EP2296474A1

  公开（公告）日：2011-03-23