4-(7-bromo-1-ethylimidazo[4,5-c]pyridin-2-yl)-1,2,5-oxadiazol-3-amine | 607370-99-0

• 物质功能分类: 医药中间体 - 杂环化合物
• 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-(7-bromo-1-ethylimidazo[4,5-c]pyridin-2-yl)-1,2,5-oxadiazol-3-amine
• 英文别名: SB-738004；4-(7-bromo-1-ethyl-1H-imidazo[4,5-c]pyridin-2-yl)oxadiazolidin-3-ylamine；4-(7-bromo-1-ethyl-1H-imidazo[4,5-c]pyridin-2-yl)furazan-3-ylamine；4-(7-Bromo-1-ethyl-1H-imidazo[4,5-c]pyridin-2-yl)-1,2,5-oxadiazol-3-amine
• CAS: 607370-99-0
• 化学式: C₁₀H₉BrN₆O
• 分子量: 309.125
• InChiKey: FNMHGQSBPQSGMV-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.5
• 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：
  95.6
• 氢给体数：
  1
• 氢受体数：
  6

安全信息

• 海关编码：
  2934999090

反应信息

• 作为反应物：
  描述：

  4-(7-bromo-1-ethylimidazo[4,5-c]pyridin-2-yl)-1,2,5-oxadiazol-3-amine 在 正丁基锂 、 (polystyrylmethyl)trimethylammonium cyanoborohydride 、 溶剂黄146 作用下， 以 四氢呋喃 、 甲醇 为溶剂， 生成 4-(1-Ethyl-7-piperidin-1-ylmethyl-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：

  (3-溴-5-硝基-吡啶-4-基)-乙基-胺 在 盐酸 、 铁粉 、 溶剂黄146 、 sodium nitrite 作用下， 以 甲醇 为溶剂， 反应 8.0h， 生成 4-(7-bromo-1-ethylimidazo[4,5-c]pyridin-2-yl)-1,2,5-oxadiazol-3-amine
  参考文献：
  名称：

  KR20230120815A

  摘要：

  公开号：

文献信息

• [EN] INHIBITORS OF Akt ACTIVITY<br/>[FR] INHIBITEURS DE L'ACTIVITE DE AKT
  申请人：SMITHKLINE BEECHAM CORP

  公开号：WO2005011700A1

  公开（公告）日：2005-02-10

  Invented are novel 1 H-imidazo[4,5-c]pyridin-2-yI compounds, the use of such compounds as inhibitors of protein kinase B activity and in the treatment of cancer and arthritis.

  发明了新型的1H-咪唑[4,5-c]吡啶-2-基化合物，这些化合物用作蛋白激酶B活性的抑制剂，并用于治疗癌症和关节炎。
• [EN] CANCER TREATMENT METHOD<br/>[FR] METHODE DE TRAITEMENT DU CANCER
  申请人：SMITHKLINE BEECHAM CORP

  公开号：WO2005046678A1

  公开（公告）日：2005-05-26

  The present invention relates to a method of treating cancer in a mammal and to pharmaceutical combinations useful in such treatment. In particular, the method relates to a cancer treatment method that includes administering an erb family inhibitor and a PI3K and/or Akt inhibitor to a mammal suffering from a cancer.

  本发明涉及一种治疗哺乳动物癌症的方法以及在这种治疗中有用的药物组合。具体而言，该方法涉及一种癌症治疗方法，其中向患有癌症的哺乳动物施用一种erb家族抑制剂和一种PI3K和/或Akt抑制剂。
• [EN] MICROBIOCIDAL 4-(IMIDAZO[4,5-C]PYRIDIN-2-YL)-1,2,5-OXADIAZOL-3- AMINE COMPOUNDS HAVING AN OXIME GROUP IN POSITION 7<br/>[FR] COMPOSÉS 4-(IMIDAZO[4,5-C]PYRIDIN-2-YL)-1,2,5-OXADIAZOL-3-AMINE MICROBIOCIDES COMPRENANT UN GROUPE OXIME EN POSITION 7
  申请人：SYNGENTA PARTICIPATIONS AG

  公开号：WO2016038143A1

  公开（公告）日：2016-03-17

  The present invention provides compounds of formula (I) wherein Y1, Y2, Υ3, Υ4 and Υ5 are as defined in the claims. The invention further relates to compositions which comprise these compounds and to their use in agriculture or horticulture for controlling or preventing infestation of plants by phytopathogenic microorganisms, preferably fungi.

  本发明提供了式（I）的化合物，其中Y1、Y2、Υ3、Υ4和Υ5如权利要求所定义。本发明还涉及包含这些化合物的组合物，并且涉及它们在农业或园艺中的使用，用于控制或预防植物被植物病原微生物，特别是真菌的侵染。
• [EN] IMIDAZOPYRIDINE DERIVATIVES AS KINASE INHIBITORS<br/>[FR] DERIVES D'IMIDAZOPYRIDINE EN TANT QU'INHIBITEURS DE KINASE
  申请人：GLAXO GROUP LTD

  公开号：WO2003080610A1

  公开（公告）日：2003-10-02

  A compound of the formula: (I) and-physiologically acceptable salts and or N-oxides thereof wherein, X1 is N or CR.3; X2 is N or CR'4; X3 ,is..N or CR5; X4 is N or CR6 with the proviso that at least one but not more than two of X1, X 2, X,3. and X4 represents N. R1 is a 5-, or 6-membered heterocyclic group selected from group a, b, c or d formula: (II) wherein X5 is a group selected from N or CR7: and X6, is a group selected from O, S or NR8; X7 and X8; which maybe the same or, different is a group selected from N or CR9; ; X9, is a group selected from O, S or NR8 and X10 is N or CR10 ; X11 , X12 and X13 may be the same or different and selected from a group N or CR11 ; processes for their preparation, pharmaceutical compositions containing them and their use in medicine.

  化合物的式子为：（I），其生理上可接受的盐和/或N-氧化物，其中，X1为N或CR.3；X2为N或CR'4；X3为N或CR5；X4为N或CR6，但至少其中一个但不超过两个X1、X2、X3和X4代表N。R1是从a、b、c或d组中选择的5-或6-成员杂环基，式子为：（II），其中X5是从N或CR7选择的基团；X6是从O、S或NR8选择的基团；X7和X8可以相同或不同，是从N或CR9选择的基团；X9是从O、S或NR8选择的基团，X10是N或CR10；X11、X12和X13可以相同或不同，是从N或CR11的基团中选择的；制备它们的过程，包含它们的制药组合物以及它们在医学上的用途。
• 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。