4-(1-Ethyl-5-oxy-1H-imidazo[4,5-c]pyridin-2-yl)-furazan-3-ylamine | 607373-72-8

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 咪唑并吡啶类
• 英文名称: 4-(1-Ethyl-5-oxy-1H-imidazo[4,5-c]pyridin-2-yl)-furazan-3-ylamine
• 英文别名: 4-(1-Ethyl-5-oxidoimidazo[4,5-c]pyridin-5-ium-2-yl)-1,2,5-oxadiazol-3-amine
• CAS: 607373-72-8
• 化学式: C₁₀H₁₀N₆O₂
• 分子量: 246.228
• InChiKey: GBJXABCUMBEUMD-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -1.1
• 重原子数：
  18
• 可旋转键数：
  2
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.2
• 拓扑面积：
  108
• 氢给体数：
  1
• 氢受体数：
  6

反应信息

• 作为反应物：
  描述：

  4-(1-Ethyl-5-oxy-1H-imidazo[4,5-c]pyridin-2-yl)-furazan-3-ylamine 在 三氯氧磷 作用下， 以100%的产率得到4-(4-Chloro-1-ethyl-1H-imidazo[4,5-c]pyridin-2-yl)-furazan-3-ylamine
  参考文献：
  名称：

  (1H-Imidazo[4,5-c]pyridin-2-yl)-1,2,5-oxadiazol-3-ylamine derivatives: Further optimisation as highly potent and selective MSK-1-inhibitors

  摘要：

  The novel imidazo[4,5-c]pyridine 1,2,5-oxadiazol-3-yl template affords an excellent start point for identification of inhibitors of a number of protein kinases. Here we report on its optimisation for mitogen and stress-activated protein kinase-1 (MSK-1) inhibitory activity, and selectivity over other kinases. (c) 2005 Published by Elsevier Ltd.

  DOI：

  10.1016/j.bmcl.2005.05.020
• 作为产物：
  描述：

  4-(1-乙基-1H-咪唑并[4,5-c]吡啶-2-基)-1,2,5-噁二唑-3-胺 在 双氧水 作用下， 以 溶剂黄146 为溶剂， 反应 5.0h， 以53%的产率得到4-(1-Ethyl-5-oxy-1H-imidazo[4,5-c]pyridin-2-yl)-furazan-3-ylamine
  参考文献：
  名称：

  (1H-Imidazo[4,5-c]pyridin-2-yl)-1,2,5-oxadiazol-3-ylamine derivatives: Further optimisation as highly potent and selective MSK-1-inhibitors

  摘要：

  The novel imidazo[4,5-c]pyridine 1,2,5-oxadiazol-3-yl template affords an excellent start point for identification of inhibitors of a number of protein kinases. Here we report on its optimisation for mitogen and stress-activated protein kinase-1 (MSK-1) inhibitory activity, and selectivity over other kinases. (c) 2005 Published by Elsevier Ltd.

  DOI：

  10.1016/j.bmcl.2005.05.020

文献信息

• Imidazopyridine derivatives as kinase inhibitors
  申请人：Bailey Nicholas

  公开号：US20050197328A1

  公开（公告）日：2005-09-08

  A compound of the formula and physiologically acceptable salts and or N-oxides thereof wherein, X 1 is N or CR 3 ; X 2 is N or CR 4 ; X 3 is N or CR 5 ; X 4 is N or CR 6 . with the proviso that at least one but not more than two of X 1 , X 2 , X 3 and X 4 represents N. R 1 is a 5-, or 6-membered heterocyclic group selected from group a, b, c or d wherein X 5 is a group selected from N or CR 7 and X 6 is a group selected from O, S or NR 8; X 7 and X 8 which may be the same or different is a group selected from N or CR 9; X 9 is a group selected from O, S or NR 8 and X 10 is N or CR 10; X 11 , X 12 and X 13 may be the same or different and selected from a group N or CR 11 ; processes for their preparation, pharmaceutical compositions containing them and their use in medicine.

  式中化合物及其生理上可接受的盐和/或N-氧化物，其中： X1为N或CR3； X2为N或CR4； X3为N或CR5； X4为N或CR6； 但须满足X1、X2、X3和X4中至少一个但不超过两个为N； R1为从a、b、c或d组中选择的5-或6-成员杂环基，其中X5为N或CR7组，X6为O、S或NR8组； X7和X8可以相同或不同，为N或CR9组； X9为O、S或NR8组，X10为N或CR10组； X11、X12和X13可以相同或不同，为N或CR11组； 本发明还涉及其制备方法、包含它们的制药组合物以及它们在医学上的应用。
• IMIDAZOPYRIDINE DERIVATIVES AS KINASE INHIBITORS
  申请人：GLAXO GROUP LIMITED

  公开号：EP1490367B1

  公开（公告）日：2008-07-23
• US7348339B2
  申请人：——

  公开号：US7348339B2

  公开（公告）日：2008-03-25