2-[4-(6,7-dimethoxyquinolin-4-yloxy)pyrazol-1-yl]acetic acid | 883977-06-8

• 分子结构分类: 有机化合物 - 有机氧化合物
• 英文名称: 2-[4-(6,7-dimethoxyquinolin-4-yloxy)pyrazol-1-yl]acetic acid
• 英文别名: 2-[4-(6,7-dimethoxyquinolin-4-yl)oxypyrazol-1-yl]acetic acid
• CAS: 883977-06-8
• 化学式: C₁₆H₁₅N₃O₅
• 分子量: 329.312
• InChiKey: MNBDEOWWSIYIOR-UHFFFAOYSA-N

物化性质

• 沸点：
  559.3±50.0 °C(Predicted)
• 密度：
  1.38±0.1 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  1.7
• 重原子数：
  24
• 可旋转键数：
  6
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.19
• 拓扑面积：
  95.7
• 氢给体数：
  1
• 氢受体数：
  7

反应信息

• 作为反应物：
  描述：

  2-[4-(6,7-dimethoxyquinolin-4-yloxy)pyrazol-1-yl]acetic acid 、 间氨基苯甲醚 在 N,N-二异丙基乙胺 作用下， 以 N,N-二甲基甲酰胺 为溶剂， 生成 2-[4-(6,7-dimethoxyquinolin-4-yl)oxypyrazol-1-yl]-N-(3-methoxyphenyl)acetamide
  参考文献：
  名称：

  Discovery of AZD2932, a new Quinazoline Ether Inhibitor with high affinity for VEGFR-2 and PDGFR tyrosine kinases

  摘要：

  A new series of Quinazoline Ether Inhibitor which potently inhibits VEGFR-2 and PDGFR tyrosine kinases is described here. In vitro, pharmacokinetics and in vivo evaluations led to the selection of AZD2932. (C) 2011 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2011.11.019
• 作为产物：
  描述：

  4-氯 -6,7-二甲氧基喹啉 在 potassium carbonate 、 三氟乙酸 作用下， 以 二氯甲烷 、 N,N-二甲基乙酰胺 、 水 为溶剂， 反应 19.0h， 生成 2-[4-(6,7-dimethoxyquinolin-4-yloxy)pyrazol-1-yl]acetic acid
  参考文献：
  名称：

  Discovery of AZD2932, a new Quinazoline Ether Inhibitor with high affinity for VEGFR-2 and PDGFR tyrosine kinases

  摘要：

  A new series of Quinazoline Ether Inhibitor which potently inhibits VEGFR-2 and PDGFR tyrosine kinases is described here. In vitro, pharmacokinetics and in vivo evaluations led to the selection of AZD2932. (C) 2011 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2011.11.019

文献信息

• [EN] QUINOLINE DERIVATIVES<br/>[FR] DERIVES DE LA QUINOLEINE
  申请人：ASTRAZENECA AB

  公开号：WO2006040522A1

  公开（公告）日：2006-04-20

  The invention concerns quinoline derivatives of Formula (I) or a pharmaceutically-acceptable salt, solvate or pro-drug thereof, wherein each of p, R1, q, R2, R3, R4, R5, Ring A, r and R6 has any of the meanings defined in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use in the treatment of cell proliferative disorders or in the treatment of disease states associated with angiogenesis and/or vascular permeability.

  该发明涉及公式（I）的喹啉衍生物或其药用可接受的盐、溶剂合物或前药，其中p、R1、q、R2、R3、R4、R5、环A、r和R6中的每一个具有描述中定义的任何含义；制备它们的方法，含有它们的药物组合物以及它们在制备用于治疗细胞增殖障碍或与血管生成和/或血管通透性相关的疾病状态的药物的用途。
• Quinoline derivatives
  申请人：Jung Frederic Henri

  公开号：US20090036485A1

  公开（公告）日：2009-02-05

  The invention concerns quinoline derivatives of Formula (I) or a pharmaceutically-acceptable salt, solvate or pro-drug thereof, wherein each of p, R 1 , q, R 2 , R 3 , R 4 , R 5 , Ring A, r and R 6 has any of the meanings defined in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use in the treatment of cell proliferative disorders or in the treatment of disease states associated with angiogenesis and/or vascular permeability.

  本发明涉及式(I)的喹啉衍生物或其药学上可接受的盐、溶剂或前药，其中p、R1、q、R2、R3、R4、R5、环A、r和R6中的每一个都具有在说明书中定义的任何含义；其制备方法，含有它们的制药组合物以及它们在制造用于治疗细胞增殖性疾病或与血管生成和/或血管通透性相关的疾病状态的药物中的使用。
• QUINOLINE DERIVATIVES
  申请人：AstraZeneca AB

  公开号：EP1802603A1

  公开（公告）日：2007-07-04