4-methoxy-3-({4-[(3-methyl-1H-indazol-6-yl)amino]-2-pyrimidinyl}amino)benzenesulfonamide | 444731-17-3

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: 4-methoxy-3-({4-[(3-methyl-1H-indazol-6-yl)amino]-2-pyrimidinyl}amino)benzenesulfonamide
• 英文别名: 4-methoxy-3-[[4-[(3-methyl-2H-indazol-6-yl)amino]pyrimidin-2-yl]amino]benzenesulfonamide
• CAS: 444731-17-3
• 化学式: C₁₉H₁₉N₇O₃S
• 分子量: 425.471
• InChiKey: YPFGLZQCUOYDCU-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.5
• 重原子数：
  30
• 可旋转键数：
  6
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.11
• 拓扑面积：
  156
• 氢给体数：
  4
• 氢受体数：
  9

反应信息

• 作为产物：
  描述：

  帕唑帕尼杂质57 、 3-氨基-4-甲氧基苯磺酰胺 以 乙醇 为溶剂， 以89%的产率得到4-methoxy-3-({4-[(3-methyl-1H-indazol-6-yl)amino]-2-pyrimidinyl}amino)benzenesulfonamide
  参考文献：
  名称：

  Discovery of 5-[[4-[(2,3-Dimethyl-2H-indazol-6-yl)methylamino]-2-pyrimidinyl]amino]-2-methyl-benzenesulfonamide (Pazopanib), a Novel and Potent Vascular Endothelial Growth Factor Receptor Inhibitor

  摘要：

  Inhibition of the vascular endothelial growth factor (VEGF) signaling pathway has emerged as one of the most promising new approaches for cancer therapy. We describe herein the key steps starting from an initial screening hit leading to the discovery of pazopanib, N(4)-(2,3-dimethyl-2H-indazol-6-yl)-N(4)-methyl-N(2)-(4-methyl-3-sulfonamidophenyl)-2,4-pyrimidinediamine, a potent pan-VEGF receptor (VEGFR) inhibitor under clinical development for renal-cell cancer and other solid tumors.

  DOI：

  10.1021/jm800566m

文献信息

• Chemical compounds
  申请人：Boloor Amogh

  公开号：US20070015756A1

  公开（公告）日：2007-01-18

  Pyrimidine derivatives, which are useful as VEGFR2 inhibitors are described herein. The described invention also includes methods of making such pyrimidine derivatives as well as methods of using the same in the treatment of hyperproliferative diseases.

  本文描述了一种有用于VEGFR2抑制剂的嘧啶衍生物。所述发明还包括制备此类嘧啶衍生物的方法，以及在治疗过度增殖性疾病中使用它们的方法。
• 2,4-Pyrimidinediamine compounds and their uses
  申请人：——

  公开号：US20040029902A1

  公开（公告）日：2004-02-12

  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受体信号级联引起化学介质释放的2,4-嘧啶二胺化合物，以及合成这些化合物的中间体和方法，以及在多种情境下使用这些化合物的方法，包括在治疗和预防由通过激活IgE和/或IgG受体信号级联引起的脱颗粒化和其他过程释放化学介质的疾病中。
• 2,4-PYRIMIDINEDIAMINE COMPOUNDS AND THEIR USES
  申请人：Singh Rajinder

  公开号：US20070225321A1

  公开（公告）日：2007-09-27

  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.

  本发明提供了能够抑制IgE和/或IgG受体信号级联反应从而导致化学介质释放的2,4-嘧啶二胺化合物，以及合成这些化合物的中间体和方法，以及在各种情况下使用这些化合物的方法，包括用于治疗和预防通过去颗粒化和其他通过激活IgE和/或IgG受体信号级联反应引起的化学介质释放所表征的，由化学介质引起或相关的疾病。
• CHEMICAL COMPOUNDS
  申请人：Boloor Amogh

  公开号：US20070270427A1

  公开（公告）日：2007-11-22

  Pyrimidine derivatives, which are useful as VEGFR2 inhibitors are described herein. The described invention also includes methods of making such pyrimidine derivatives as well as methods of using the same in the treatment of hyperproliferative diseases.

  本文描述了作为VEGFR2抑制剂有用的嘧啶衍生物。所述发明还包括制备此类嘧啶衍生物的方法，以及在治疗过度增殖性疾病中使用它们的方法。
• Chemical Compounds
  申请人：Boloor Amogh

  公开号：US20120277258A1

  公开（公告）日：2012-11-01

  Pyrimidine derivatives, which are useful as VEGFR2 inhibitors are described herein. The described invention also includes methods of making such pyrimidine derivatives as well as methods of using the same in the treatment of hyperproliferative diseases.

  本文描述了一种作为VEGFR2抑制剂有用的嘧啶衍生物。所述发明还包括制备此类嘧啶衍生物的方法，以及使用它们治疗增生性疾病的方法。