THK5351 | 1707147-26-9

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡啶及其衍生物
• 英文名称: THK5351
• 英文别名: Thk-5351；(2S)-1-fluoro-3-[2-[6-(methylamino)pyridin-3-yl]quinolin-6-yl]oxypropan-2-ol
• CAS: 1707147-26-9
• 化学式: C₁₈H₁₈FN₃O₂
• 分子量: 327.358
• InChiKey: DLVXFZWSPCOWSN-CQSZACIVSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.8
• 重原子数：
  24
• 可旋转键数：
  6
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.22
• 拓扑面积：
  67.3
• 氢给体数：
  2
• 氢受体数：
  6

反应信息

• 作为产物：
  描述：

  Carbamic acid, N-[5-[6-[(2S)-2-[[(1,1-dimethylethyl)dimethylsilyl]oxy]-3-fluoropropoxy]-2-quinolinyl]-2-pyridinyl]-N-methyl-, 1,1-dimethylethyl ester 在 三氟乙酸 作用下， 以 氯仿 为溶剂， 反应 16.0h， 以632 mg的产率得到THK5351
  参考文献：
  名称：

  TAU IMAGING PROBE

  摘要：

  本发明的目的是提供一种由公式(I)表示的化合物，该化合物对tau具有高度特异性，可以以满意的灵敏度成像tau，并且具有高的脑内转移率，低或不识别的寻骨性能以及低或不可检测的毒性。

  公开号：

  US20160244411A1

文献信息

• [EN] QUINOLINE DERIVATES AS PRECURSORS OF 18F-LABELLED RADIOTRACERS AND RADIOLABELLING METHOD<br/>[FR] DÉRIVÉS DE QUINOLINE UTILISÉS EN TANT QUE PRÉCURSEURS DE RADIOTRACEURS MARQUÉS 18F ET PROCÉDÉ DE RADIOMARQUAGE
  申请人：GE HEALTHCARE LTD

  公开号：WO2015091558A1

  公开（公告）日：2015-06-25

  The present invention relates to the field of radiopharmaceuticals for in vivo imaging, in particular to precursors for the preparation of 18F-labelled tau imaging radiotracers. The invention provides alternative methods of preparation of such precursors, with fewer process steps. Also provided are protected quinoline intermediates useful in the synthesis, and methods of 18F-radiofluorination using precursors prepared via the method of the invention.

  本发明涉及体内成像放射性药物领域，特别是用于制备18F标记的tau成像放射性示踪剂的前体。本发明提供了制备这种前体的替代方法，步骤更少。还提供了在合成中有用的受保护的喹啉中间体，以及使用通过本发明方法制备的前体的18F-放射性氟化方法。
• [EN] RADIOLABELLING METHOD<br/>[FR] PROCÉDÉ DE RADIOMARQUAGE
  申请人：GE HEALTHCARE LTD

  公开号：WO2016000798A1

  公开（公告）日：2016-01-07

  The present invention relates to the field of radiopharmaceuticals for in vivo imaging, in particular to automated methods for the preparation and purification of 18F-labelled tau imaging radiotracers. Also provided are interchangeable cassettes useful in the methods, and the use of automated synthesizers and cassettes in the methods.

  本发明涉及体内成像的放射性药物领域，特别是涉及用于制备和纯化18F标记tau成像放射性示踪剂的自动化方法。本发明还提供了在该方法中有用的可互换的盒式结构以及自动化合成器和盒式结构在该方法中的使用。
• Radiolabelling method
  申请人：GE Healthcare Limited

  公开号：US10220105B2

  公开（公告）日：2019-03-05

  The present invention relates to the field of radiopharmaceuticals for in vivo imaging, in particular to automated methods for the preparation and purification of 18F-labelled tau imaging radiotracers. Also provided are interchangeable cassettes useful in the methods, and the use of automated synthesizers and cassettes in the methods.

  本发明涉及用于体内成像的放射性药物领域，特别是涉及制备和纯化 18F 标记的 tau 成像放射性核素的自动化方法。本发明还提供了在这些方法中有用的可互换盒，以及在这些方法中自动合成器和盒的使用。
• RADIOLABELLING METHOD
  申请人：GE Healthcare Limited

  公开号：US20170106104A1

  公开（公告）日：2017-04-20

  The present invention relates to the field of radiopharmaceuticals for in vivo imaging, in particular to automated methods for the preparation and purification of 18 F-labelled tau imaging radiotracers. Also provided are interchangeable cassettes useful in the methods, and the use of automated synthesizers and cassettes in the methods.
• COMPOUNDS FOR TAU PROTEIN DEGRADATION
  申请人：Dana-Farber Cancer Institute, Inc.

  公开号：US20210154184A1

  公开（公告）日：2021-05-27

  Provided herein are bifunctional compounds that bind tau protein and/or promote targeted ubiquitination for the degradation of tau protein. In particular, provided are compounds that can bind tau protein, a protein whose aggregation is implicated in a variety of neurodegenerative disease (e.g., tauopathies), and can promote its degradation by recruiting an E3 ubiquitin ligase (e.g., Cereblon), which can ubiquitinate tau protein, marking it for proteasomal degradation. Also provided are radiolabeled forms of the bifunctional compounds, pharmaceutical compositions comprising the bifunctional compounds, methods of detecting and/or diagnosing neurological disorders, methods of detecting and/or diagnosing pathological aggregation of tau protein (e.g., in the central nervous system), methods of treating and/or preventing neurological disorders, and methods of promoting the degradation of tau protein by E3 ubiquitin ligase activity in a subject by administering a compound or composition described herein.