(5-ethyl-2,5-diaza-bicyclo[2.2.1]hept-2-yl)-[6-(4-hydroxy-phenyl)-1H-pyrazolo[3,4-b]pyridin-4-yl]-methanone | 1431977-84-2

• 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: (5-ethyl-2,5-diaza-bicyclo[2.2.1]hept-2-yl)-[6-(4-hydroxy-phenyl)-1H-pyrazolo[3,4-b]pyridin-4-yl]-methanone
• 英文别名: (5-ethyl-2,5-diazabicyclo[2.2.1]heptan-2-yl)-[6-(4-hydroxyphenyl)-1H-pyrazolo[3,4-b]pyridin-4-yl]methanone
• CAS: 1431977-84-2
• 化学式: C₂₀H₂₁N₅O₂
• 分子量: 363.419
• InChiKey: KQRIRXJKDJIUIJ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2
• 重原子数：
  27
• 可旋转键数：
  3
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.35
• 拓扑面积：
  85.4
• 氢给体数：
  2
• 氢受体数：
  5

文献信息

• 6-(4-Hydroxy-phenyl)-1H-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors
  申请人：SANOFI

  公开号：US20130150340A1

  公开（公告）日：2013-06-13

  The present invention relates to 1H-pyrazolo[3,4-b]pyridine compounds of the formula I, in which R 1 , R 2 , R 3 and R 4 are defined as indicated below. The compounds of the formula I are kinase inhibitors, and are useful for the treatment of diseases associated with diabetes and diabetic complications, such as, diabetic nephropathy, diabetic neuropathy and diabetic retinopathy, for example. The invention furthermore relates to the use of compounds of the formula I, in particular as active ingredients in pharmaceuticals, and pharmaceutical compositions comprising them.

  本发明涉及式I的1H-吡唑并[3,4-b]吡啶化合物，其中R1、R2、R3和R4如下所示。式I的化合物是激酶抑制剂，对于治疗与糖尿病及糖尿病并发症相关的疾病，如糖尿病肾病、糖尿病神经病变和糖尿病视网膜病变等，具有用处。此外，本发明还涉及将式I的化合物用作药物中的活性成分，以及包含它们的药物组合物。
• 2,4-PYRIMIDINEDIAMINE COMPOUNDS AND THEIR USES
  申请人：Rigel Pharmaceuticals, Inc.

  公开号：US20130150349A1

  公开（公告）日：2013-06-13

  The present invention provides 2,4-pyrimidinediamine compounds that inhibit the IgE and/or IgG receptor signaling cascades that lead to the release of chemical mediators, intermediates and methods of synthesizing the compounds and methods of using the compounds in a variety of contexts, including in the treatment and prevention of diseases characterized by, caused by or associated with the release of chemical mediators via degranulation and other processes effected by activation of the IgE and/or IgG receptor signaling cascades.

  本发明提供了抑制IgE和/或IgG受体信号级联反应的2,4-嘧啶二胺化合物，这些反应导致化学介质释放，中间体和合成该化合物的方法以及在各种情况下使用该化合物的方法，包括在通过去颗粒化和其他由IgE和/或IgG受体信号级联激活引起的化学介质释放特征化，引起或与之相关的疾病的治疗和预防中。
• 2,4-Pyrimidinediamine Compounds and Their Uses
  申请人：Rigel Pharmaceuticals, Inc.

  公开号：US20140031350A1

  公开（公告）日：2014-01-30

  The present invention provides 2,4-pyrimidinediamine compounds that inhibit the IgE and/or IgG receptor signaling cascades that lead to the release of chemical mediators, intermediates and methods of synthesizing the compounds and methods of using the compounds in a variety of contexts, including in the treatment and prevention of diseases characterized by, caused by or associated with the release of chemical mediators via degranulation and other processes effected by activation of the IgE and/or IgG receptor signaling cascades.

  本发明提供了抑制IgE和/或IgG受体信号级联，导致化学介质释放的2,4-嘧啶二胺化合物，以及合成该化合物的中间体和方法，以及在各种情况下使用该化合物的方法，包括在通过去颗粒化和其他由IgE和/或IgG受体信号级联激活引起的化学介质释放所表征，引起或与之相关的疾病的治疗和预防中使用。
• 2,4-PYRIDINEDIAMINE COMPOUNDS AND THEIR USES
  申请人：RIGEL PHARMACEUTICALS, INC.

  公开号：US20140303154A1

  公开（公告）日：2014-10-09

  The present invention provides 2,4-pyrimidinediamine compounds that inhibit the IgE and/or IgG receptor signaling cascades that lead to the release of chemical mediators, intermediates and methods of synthesizing the compounds and methods of using the compounds in a variety of contexts, including in the treatment and prevention of diseases characterized by, caused by or associated with the release of chemical mediators via degranulation and other processes effected by activation of the IgE and/or IgG receptor signaling cascades.

  本发明提供了2,4-嘧啶二胺化合物，可抑制导致释放化学介质的IgE和/或IgG受体信号级联反应，提供了合成该化合物的中间体和方法，以及在各种情况下使用该化合物的方法，包括在通过去颗粒化和其他由激活IgE和/或IgG受体信号级联反应引起的释放化学介质的疾病的治疗和预防中使用。
• 6-(4-HYDROXY-PHENYL)-1H-PYRAZOLO[3,4-B]PYRIDINE-4-CARBOXYLIC ACID AMIDE DERIVATIVES AS KINASE INHIBITORS
  申请人：SANOFI

  公开号：EP2771340B1

  公开（公告）日：2016-04-13