E-[6-(3-amino-propenyl)-quinazolin-4-yl]-[3-chloro-4-(6-methyl-pyridin-3-yloxy)-phenyl]-amine | 383432-27-7

• 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: E-[6-(3-amino-propenyl)-quinazolin-4-yl]-[3-chloro-4-(6-methyl-pyridin-3-yloxy)-phenyl]-amine
• 英文别名: [6-((E)-3-amino-propenyl)-quinazolin-4-yl]-[3-chloro-4-(6-methyl-pyridin-3-yloxy)-phenyl]-amine；E-[6-(3-amino-propenyl)-quinazolin-4-yl]-[3-chloro-4-(6-methyl pyridin-3-yloxy)-phenyl]-amine；6-[(E)-3-aminoprop-1-enyl]-N-[3-chloro-4-(6-methylpyridin-3-yl)oxyphenyl]quinazolin-4-amine
• CAS: 383432-27-7
• 化学式: C₂₃H₂₀ClN₅O
• 分子量: 417.898
• InChiKey: VHSPZKNNNJSZSN-NSCUHMNNSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.4
• 重原子数：
  30
• 可旋转键数：
  6
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.09
• 拓扑面积：
  86
• 氢给体数：
  2
• 氢受体数：
  6

反应信息

• 作为反应物：
  描述：

  E-[6-(3-amino-propenyl)-quinazolin-4-yl]-[3-chloro-4-(6-methyl-pyridin-3-yloxy)-phenyl]-amine 、 溶剂黄146 在 N,N'-二环己基碳二亚胺 作用下， 以 二氯甲烷 为溶剂， 生成 E-N-(3-{4-[3-Chloro-4-(6-methyl-pyridin-3-yloxy)-phenylamino]-quinazolin-6-yl}-allyl)-acetamide
  参考文献：
  名称：

  Selective erbB2 inhibitor/anti-erbB antibody combinations in the treatment of cancer

  摘要：

  本发明涉及一种在哺乳动物中使用erbB2配体和抗体的组合治疗癌症的方法。更具体地，本发明涉及通过联合给予erbB2配体和erbB抗体来治疗癌症的方法。本发明还涉及一种在哺乳动物，特别是人类中治疗异常细胞生长的有用工具包。

  公开号：

  US20050101618A1
• 作为产物：
  描述：

  ((E)-3-{4-[3-chloro-4-(6-methyl-pyridin-3-yloxy)-phenylamino]-quinazolin-6-yl}-allyl)-carbamic acid tert-butyl ester 在 盐酸 、 水 作用下， 以 四氢呋喃 为溶剂， 反应 3.0h， 生成 E-[6-(3-amino-propenyl)-quinazolin-4-yl]-[3-chloro-4-(6-methyl-pyridin-3-yloxy)-phenyl]-amine
  参考文献：
  名称：

  Selective erbB2 inhibitor/anti-erbB antibody combinations in the treatment of cancer

  摘要：

  本发明涉及一种在哺乳动物中使用erbB2配体和抗体的组合治疗癌症的方法。更具体地，本发明涉及通过联合给予erbB2配体和erbB抗体来治疗癌症的方法。本发明还涉及一种在哺乳动物，特别是人类中治疗异常细胞生长的有用工具包。

  公开号：

  US20050101618A1

文献信息

• [EN] COMPLEXES OF E-2-METHOXY-N-(3-{4-[3-METHYL-4-(6-METHYL-PYRIDIN-3-YLOXY)-PHENYLAMINO]-QUINAZOLIN-6-YL}-ALLYL)-ACETAMIDE, THEIR METHOD OF PRODUCTION, AND USE<br/>[FR] COMPLEXES DE E-2-METHOXY-N-(3-{4-[3-METHYL-4-(6-METHYL-PYRIDIN-3-YLOXY)-PHENYLAMINO]-QUINAZOLIN-6-YL}-ALLYL)-ACETAMIDE ET PROCEDES DE FABRICATION ET D'UTILISATION CORRESPONDANTS
  申请人：PFIZER PROD INC

  公开号：WO2004056802A1

  公开（公告）日：2004-07-08

  The invention relates to complexes of E-2-Methoxy-N-(3-4-[3-methyl-4-(6-methyl­pyridin-3-yloxy)-phenylamino]-quinazolin-6-yl}-allyl)-acetamide having the following formula I: The invention also relates to pharmaceutical compositions containing the complexes of formula I. The invention further relates to methods of treating hyperproliferative diseases, such as cancers, in mammals, especially humans by administering the above complexes and to methods of preparing the above complexes.

  该发明涉及具有以下化学式I的E-2-甲氧基-N-(3-4-[3-甲基-4-(6-甲基吡啶-3-氧基)-苯胺基]-喹唑啉-6-基}-丙烯酰胺)的配合物。该发明还涉及含有化学式I的配合物的药物组合物。该发明还涉及通过给哺乳动物，特别是人类，投与上述配合物来治疗增生性疾病，如癌症的方法，以及制备上述配合物的方法。
• Selective erbB2 inhibitor/anti-erbB antibody combinations in the treatment of cancer
  申请人：Connell D. Richard

  公开号：US20050101618A1

  公开（公告）日：2005-05-12

  This invention relates to a method of treatment of cancer with a combination of an erbB2 ligand and an antibody, in mammals. More particularly, this invention relates to a method of treating cancer by administering an erbB2 ligand in combination with an erbB antibody. This invention also relates to a kit useful in the treatment of abnormal cell growth in mammals, especially humans.

  本发明涉及一种在哺乳动物中使用erbB2配体和抗体的组合治疗癌症的方法。更具体地，本发明涉及通过联合给予erbB2配体和erbB抗体来治疗癌症的方法。本发明还涉及一种在哺乳动物，特别是人类中治疗异常细胞生长的有用工具包。
• Substituted bicyclic derivatives for the treatment of abnormal cell growth
  申请人：——

  公开号：US20020169165A1

  公开（公告）日：2002-11-14

  The invention relates to compounds of the formula 1 1 and to pharmaceutically acceptable salts, prodrugs and solvates thereof, wherein R 1 , R 3 , R 4 , R 5 , R 11 , m and p are as defined herein. The invention also relates to methods of treating abnormal cell growth in mammals by administering the compounds of formula 1 and to pharmaceutical compositions for treating such disorders which contain the compounds of formula 1. The invention also relates to methods of preparing the compounds of formula 1.

  该发明涉及公式11的化合物，以及其药学上可接受的盐、前药和溶剂化物，其中R1、R3、R4、R5、R11、m和p如本文所定义。该发明还涉及通过给予公式1的化合物治疗哺乳动物的异常细胞增长的方法，并且涉及用含有公式1的化合物的制药组合物治疗这种疾病的方法。该发明还涉及制备公式1的化合物的方法。
• Salt forms of E-2-Methoxy-N-(3-{4-[3 methyl-4-(6-methyl-pyridin-3-yloxy)-phenylamino]-quinazolin-6-yl}-allyl)-acetamide and method of production
  申请人：Pfizer Inc.

  公开号：US20030158217A1

  公开（公告）日：2003-08-21

  The invention relates to succinate and malonate complexes of E-2-Methoxy-N-(3-{4-[3-methyl-4-(6-methyl-pyridin-3-yloxy)-phenylamino]-quinazolin-6-yl}-allyl)-acetamide having the following formula I: 1 More particular the present invention relates to monosuccinate, hemisuccinate, sesquisuccinate and di-malonate complexes of formula I. The invention also relates to pharmaceutical compositions containing the succinate and malonate complexes of formula I. The invention further relates to methods of treating hyperproliferative diseases, such as cancers, in mammals, especially humans by administering the above complexes and to methods of preparing the above complexes.

  本发明涉及E-2-甲氧基-N-(3-4-[3-甲基-4-(6-甲基吡啶-3-氧基)苯基]氨基喹唑啉-6-基)-丙烯酰胺的琥珀酸盐和丙二酸盐配合物，其具有以下化学式I：1。更具体地，本发明涉及式I的单琥珀酸盐、半琥珀酸盐、1.5倍琥珀酸盐和双丙二酸盐配合物。本发明还涉及含有式I的琥珀酸盐和丙二酸盐配合物的药物组合物。本发明还涉及通过给予上述配合物治疗哺乳动物，特别是人类的增殖异常性疾病，如癌症的方法以及制备上述配合物的方法。
• Small molecules for the treatment of abnormal cell growth
  申请人：Pfizer Inc.

  公开号：US20030171386A1

  公开（公告）日：2003-09-11

  This invention relates to small molecules that are useful in the treatment of abnormal cell growth, such as cancer, in mammals. This invention also relates to a method of using such small molecules in the treatment of abnormal cell growth in mammals, especially humans, and to pharmaceutical compositions containing such compounds. The invention further relates to small molecules that are selective for erbB2 receptor over the erbB1 receptor, wherein said erbB2 inhibitor has a range of selectivities for erbB2 over erbB1 between 50-1500.

  本发明涉及小分子化合物，可用于治疗哺乳动物中的异常细胞生长，如癌症。本发明还涉及使用这些小分子化合物治疗哺乳动物中的异常细胞生长的方法，特别是人类，并涉及含有这些化合物的制药组合物。本发明进一步涉及选择性针对erbB2受体而非erbB1受体的小分子化合物，其中所述erbB2抑制剂对erbB2与erbB1的选择性范围在50-1500之间。