2-[3-(4-methoxybenzyl)-4-oxo-3,4-dihydroquinazolin-6-yl]malonic acid diethyl ester | 943541-46-6

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二氮杂萘
• 英文名称: 2-[3-(4-methoxybenzyl)-4-oxo-3,4-dihydroquinazolin-6-yl]malonic acid diethyl ester
• 英文别名: 2-[3-(4-Methoxy-benzyl)-4-oxo-3,4-dihydro-quinazolin-6-yl]-malonic acid diethyl ester；diethyl 2-[3-[(4-methoxyphenyl)methyl]-4-oxoquinazolin-6-yl]propanedioate
• CAS: 943541-46-6
• 化学式: C₂₃H₂₄N₂O₆
• 分子量: 424.453
• InChiKey: GUQAPMDUCGIPMF-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3
• 重原子数：
  31
• 可旋转键数：
  10
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.3
• 拓扑面积：
  94.5
• 氢给体数：
  0
• 氢受体数：
  7

反应信息

• 作为反应物：
  描述：

  2-[3-(4-methoxybenzyl)-4-oxo-3,4-dihydroquinazolin-6-yl]malonic acid diethyl ester 在 甲醇 、 sodium hydroxide 、 水 、 盐酸 作用下， 以 水 为溶剂， 生成 2-[3-[(4-Methoxyphenyl)methyl]-4-oxoquinazolin-6-yl]acetic acid
  参考文献：
  名称：

  WO2007/75567

  摘要：

  公开号：
• 作为产物：
  描述：

  6-iodo-3-(4-methoxybenzyl)-3H-quinazolin-4-one 、 丙二酸二乙酯 在 copper(l) iodide 、 caesium carbonate 、 邻苯基苯酚 、 碳酸氢钠 作用下， 以 四氢呋喃 、 水 为溶剂， 反应 24.0h， 以69%的产率得到2-[3-(4-methoxybenzyl)-4-oxo-3,4-dihydroquinazolin-6-yl]malonic acid diethyl ester
  参考文献：
  名称：

  WO2007/75567

  摘要：

  公开号：

文献信息

• TRIAZOLOPYRIDAZINES AS KINASE MODULATORS
  申请人：Lu Tianbao

  公开号：US20090098181A1

  公开（公告）日：2009-04-16

  The invention is directed to triazolopyridazine compounds of Formula I: where R 1 , R 5 , R 6 , R 7 , R 8 , and A are as defined herein, the use of such compounds as protein tyrosine kinase modulators, particularly inhibitors of c-Met, and the use of such compounds to reduce or inhibit kinase activity of c-Met in a cell or a subject, and modulate c-Met expression in a cell or subject, and the use of such compounds for preventing or treating in a subject a cell proliferative disorder and/or disorders related to c-Met. The present invention is further directed to pharmaceutical compositions comprising the compounds of the present invention and to methods for treating conditions such as cancers and other cell proliferative disorders.

  本发明涉及式I的三唑并吡嗪化合物：其中R1、R5、R6、R7、R8和A如本文所定义，使用这种化合物作为蛋白酪氨酸激酶调节剂，特别是c-Met的抑制剂，并使用这种化合物来减少或抑制细胞或受体中c-Met的激酶活性，调节细胞或受体中c-Met的表达，并使用这种化合物预防或治疗细胞增殖性疾病和/或与c-Met相关的疾病。本发明还涉及包含本发明化合物的制药组合物以及治疗癌症和其他细胞增殖性疾病的方法。
• Triazolopyridazine compounds
  申请人：Janssen Pharmaceutica N.V.

  公开号：US08173654B2

  公开（公告）日：2012-05-08

  The invention is directed to triazolopyridazine compounds of Formula I: where R1, R5, R6, R7, R8, and A are as defined herein, the use of such compounds as protein tyrosine kinase modulators, particularly inhibitors of c-Met, and the use of such compounds to reduce or inhibit kinase activity of c-Met in a cell or a subject, and modulate c-Met expression in a cell or subject, and the use of such compounds for preventing or treating in a subject a cell proliferative disorder and/or disorders related to c-Met. The present invention is further directed to pharmaceutical compositions comprising the compounds of the present invention and to methods for treating conditions such as cancers and other cell proliferative disorders.

  本发明涉及式I的三唑并吡嗪化合物：其中R1、R5、R6、R7、R8和A如本文所定义，使用这些化合物作为蛋白酪氨酸激酶调节剂，特别是c-Met的抑制剂，使用这些化合物来减少或抑制细胞或主体中c-Met的激酶活性，并调节细胞或主体中c-Met的表达，以及使用这些化合物预防或治疗主体中的细胞增殖性疾病和/或与c-Met相关的疾病。本发明还涉及包含本发明化合物的制药组合物以及治疗癌症和其他细胞增殖性疾病的方法。
• Triazolopyridazines as kinase modulators
  申请人：Janssen Pharmaceutica N.V.

  公开号：US08030305B2

  公开（公告）日：2011-10-04

  The invention is directed to triazolopyridazine compounds of Formula I: where R1, R5, R6, R7, R8, and A are as defined herein, the use of such compounds as protein tyrosine kinase modulators, particularly inhibitors of c-Met, and the use of such compounds to reduce or inhibit kinase activity of c-Met in a cell or a subject, and modulate c-Met expression in a cell or subject, and the use of such compounds for preventing or treating in a subject a cell proliferative disorder and/or disorders related to c-Met. The present invention is further directed to pharmaceutical compositions comprising the compounds of the present invention and to methods for treating conditions such as cancers and other cell proliferative disorders.

  本发明涉及式I的三唑并吡嗪化合物：其中R1、R5、R6、R7、R8和A如本文所定义，以及使用这样的化合物作为蛋白酪氨酸激酶调节剂，特别是c-Met的抑制剂，并使用这样的化合物来减少或抑制细胞或主体中c-Met的激酶活性，并调节细胞或主体中c-Met的表达，以及使用这样的化合物预防或治疗主体中的细胞增殖性疾病和/或与c-Met相关的疾病。本发明还涉及包含本发明化合物的制药组合物以及治疗癌症和其他细胞增殖性疾病的方法。
• Substituted pyridinyl and pyrimidinyl derivatives as modulators of metabolism and the treatment of disorders related thereto
  申请人：Arena Pharmaceuticals, Inc.

  公开号：EP1911756A2

  公开（公告）日：2008-04-16

  The present invention relates to certain substituted pyridinyl and pyrimidinyl derivatives of Fomula (Ia) that are modulators of metabolism. Accordingly, compounds of the present invention are useful in the treatment of metabolic-related disorders and complications thereof, such as, diabetes and obesity.

  本发明涉及某些可调节新陈代谢的福莫拉（Ia）取代吡啶基和嘧啶基衍生物。 因此，本发明的化合物可用于治疗代谢相关疾病及其并发症，如糖尿病和肥胖症。
• TRIAZOLOPYRIDAZINES AS TYROSINE KINASE MODULATORS
  申请人：Janssen Pharmaceutica, N.V.

  公开号：EP1966214A1

  公开（公告）日：2008-09-10