帕唑帕尼杂质57 | 444731-66-2

• 物质功能分类: 分析化学 - 标准品 - 药典标准品和杂质标准品
• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯并吡唑类
• 中文名称: 帕唑帕尼杂质57
• 英文名称: N-(2-chloro-4-pyrimidinyl)-N-(3-methyl-1H-indazol-6-yl)amine
• 英文别名: N-(2-chloropyrimidin-4-yl)-3-methyl-2H-indazol-6-amine
• CAS: 444731-66-2
• 化学式: C₁₂H₁₀ClN₅
• 分子量: 259.698
• InChiKey: SVNKYHODKSWCIB-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.1
• 重原子数：
  18
• 可旋转键数：
  2
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.08
• 拓扑面积：
  66.5
• 氢给体数：
  2
• 氢受体数：
  4

反应信息

• 作为反应物：
  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
• 作为产物：
  描述：

  2,4-二氯嘧啶 、 3-甲基-6-氨基吲唑 在 碳酸氢钠 作用下， 以 四氢呋喃 、 乙醇 为溶剂， 反应 4.0h， 以89%的产率得到帕唑帕尼杂质57
  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

• [EN] COMPOSITIONS AND PROCESSES<br/>[FR] COMPOSITIONS ET PROCÉDÉS
  申请人：GLAXO WELLCOME MFG PTE LTD

  公开号：WO2011050159A1

  公开（公告）日：2011-04-28

  Methods of making intermediates useful in the synthesis of pazopanib and compositions of such intermediates are described.

  描述了制备帕唑帕尼布中间体并使其在合成过程中有用的方法和该中间体的组合物。
• 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。
• 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。
• Pyrimidineamines as angiogenesis modulators
  申请人：Novartis AG

  公开号：EP2311825B1

  公开（公告）日：2015-10-07