[1,2,4]噻唑并[1,5-a]吡啶-6-甲胺 | 943894-99-3

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 三唑并吡啶类
• 中文名称: [1,2,4]噻唑并[1,5-a]吡啶-6-甲胺
• 中文别名: [1,2,4]三唑并[1,5-A]吡啶-6-基甲胺
• 英文名称: [1,2,4]triazolo[1,5-a]pyridin-6-ylmethanamine
• CAS: 943894-99-3
• 化学式: C₇H₈N₄
• 分子量: 148.167
• InChiKey: BWYNVMZVYPDEIC-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -0.4
• 重原子数：
  11
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.14
• 拓扑面积：
  56.2
• 氢给体数：
  1
• 氢受体数：
  3

安全信息

• 海关编码：
  2933990090

反应信息

• 作为反应物：
  描述：

  [1,2,4]噻唑并[1,5-a]吡啶-6-甲胺 在 溶剂黄146 、 N,N-二异丙基乙胺 、 sodium nitrite 作用下， 以 水 为溶剂， 反应 1.5h， 生成 5-Bromo-3-([1,2,4]triazolo[1,5-a]pyridin-6-ylmethyl)triazolo[4,5-b]pyrazine
  参考文献：
  名称：

  Discovery of (S)-1-(1-(Imidazo[1,2-a]pyridin-6-yl)ethyl)-6-(1-methyl-1H-pyrazol-4-yl)-1H-[1,2,3]triazolo[4,5-b]pyrazine (Volitinib) as a Highly Potent and Selective Mesenchymal–Epithelial Transition Factor (c-Met) Inhibitor in Clinical Development for Treatment of Cancer

  摘要：

  HGF/c-Met signaling has been implicated in human cancers. Herein we describe the invention of a series of novel triazolopyrazine c-Met inhibitors. The structure activity relationship of these compounds was investigated, leading to the identification of compound 28, which demonstrated favorable pharmacokinetic properties in mice and good antitumor activities in the human glioma xenograft model in athymic nude mice.

  DOI：

  10.1021/jm500510f
• 作为产物：
  描述：

  2-氨基-5-氰基吡啶 在 吡啶 、 氨 、 氢气 、 hydroxylamine-O-sulfonic acid 作用下， 以 甲醇 、 乙醇 、 N,N-二甲基甲酰胺 为溶剂， 反应 2.0h， 生成 [1,2,4]噻唑并[1,5-a]吡啶-6-甲胺
  参考文献：
  名称：

  Discovery of (S)-1-(1-(Imidazo[1,2-a]pyridin-6-yl)ethyl)-6-(1-methyl-1H-pyrazol-4-yl)-1H-[1,2,3]triazolo[4,5-b]pyrazine (Volitinib) as a Highly Potent and Selective Mesenchymal–Epithelial Transition Factor (c-Met) Inhibitor in Clinical Development for Treatment of Cancer

  摘要：

  HGF/c-Met signaling has been implicated in human cancers. Herein we describe the invention of a series of novel triazolopyrazine c-Met inhibitors. The structure activity relationship of these compounds was investigated, leading to the identification of compound 28, which demonstrated favorable pharmacokinetic properties in mice and good antitumor activities in the human glioma xenograft model in athymic nude mice.

  DOI：

  10.1021/jm500510f

文献信息

• [EN] CERTAIN TRIAZOLOPYRIDINES AND TRIAZOLOPYRAZINES, COMPOSITIONS THEREOF AND METHODS OF USE THEREFOR<br/>[FR] CERTAINES TRIAZOLOPYRIDINES ET TRIAZOLOPYRAZINES, LEURS COMPOSITIONS ET LEURS PROCEDES D'UTILISATION
  申请人：HUTCHISON MEDIPHARMA LTD

  公开号：WO2011079804A1

  公开（公告）日：2011-07-07

  Provided are certain triazolopyridines and triazolopyrazines, compositions thereof and methods of use therefor.

  提供了某些三唑吡啶和三唑吡嗪，以及它们的组成物和使用方法。
• CERTAIN TRIAZOLOPYRIDINES AND TRIAZOLOPYRAZINES, COMPOSITIONS THEREOF AND METHODS OF USE THEREFOR
  申请人：SU Wei-Guo

  公开号：US20120245178A1

  公开（公告）日：2012-09-27

  Provided are certain triazolopyridines and triazolopyrazines, compositions thereof and methods of use therefor.

  提供了某些三唑吡啶和三唑吡嗪，以及它们的组成物和使用方法。
• [EN] QUINAZOLINE AND QUINOLINE COMPOUNDS AND USES THEREOF<br/>[FR] COMPOSÉS QUINAZOLINE ET QUINOLÉINE, ET UTILISATIONS DE CEUX-CI
  申请人：MILLENNIUM PHARM INC

  公开号：WO2016118565A1

  公开（公告）日：2016-07-28

  This invention provides compounds of formula (I) or a pharmaceutically acceptable salt thereof, wherein T, J, R, R4, Rq, o, RA, W and RB and subsets thereof are as described in the specification. The compounds are inhibitors of NAMPT and are thus useful for treating cancer, inflammatory conditions, and/or T-cell mediated autoimmune disease.

  这项发明提供了式（I）的化合物或其药用盐，其中T、J、R、R4、Rq、o、RA、W和RB及其子集如规范中所述。这些化合物是NAMPT的抑制剂，因此可用于治疗癌症、炎症性疾病和/或T细胞介导的自身免疫疾病。
• CERTAIN TRIAZOLOPYRIDINES AND TRIAZOLOPYRAZINES, COMPOSITIONS THEREOF AND METHODS OF USE THEREFOR
  申请人：Su Wei-Guo

  公开号：US20120264739A1

  公开（公告）日：2012-10-18

  Provided are certain triazolopyridines and triazolopyrazines, compositions thereof and methods of use therefor.

  提供了某些三唑并吡啶和三唑并嘧啶，以及它们的组成物和使用方法。
• NAMPT INHIBITORS
  申请人：AbbVie Inc.

  公开号：US20130303508A1

  公开（公告）日：2013-11-14

  Disclosed are compounds which inhibit the activity of NAMPT, compositions containing the compounds and methods of treating diseases during which NAMPT is expressed.

  本发明涉及一种抑制NAMPT活性的化合物，包括含有该化合物的组合物以及治疗NAMPT表达疾病的方法。