E-N-(3-{4-[3-methyl-4-(6-methyl-pyridin-3-yloxy)-phenylamino]-quinazolin-6-yl}-allyl)-acetamide | 383432-36-8

• 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-N-(3-{4-[3-methyl-4-(6-methyl-pyridin-3-yloxy)-phenylamino]-quinazolin-6-yl}-allyl)-acetamide
• 英文别名: N-[(E)-3-[4-[3-methyl-4-(6-methylpyridin-3-yl)oxyanilino]quinazolin-6-yl]prop-2-enyl]acetamide
• CAS: 383432-36-8
• 化学式: C₂₆H₂₅N₅O₂
• 分子量: 439.517
• InChiKey: HRPLZSHMZXBHEQ-SNAWJCMRSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.4
• 重原子数：
  33
• 可旋转键数：
  7
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.15
• 拓扑面积：
  89
• 氢给体数：
  2
• 氢受体数：
  6

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。
• [EN] 4-ANILINO QUINAZOLINE DERIVATIVES FOR THE TREATMENT OF ABNORMAL CELL GROWTH<br/>[FR] DERIVES DE 4-ANILINO QUINAZOLINE PERMETTANT DE TRAITER UNE CROISSANCE CELLULAIRE ANORMALE
  申请人：PFIZER PROD INC

  公开号：WO2004054585A1

  公开（公告）日：2004-07-01

  The invention relates to compounds of the formula (1) and to pharmaceutically acceptable salts, prodrugs and solvates thereof, wherein R1, R2, R3 and R5 are as defined herein, and wherein the compound of formula (1) optionally further comprises a hydroxy substituent or an 0-glucuronic acid. 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).

  本发明涉及公式（1）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、R2、R3和R5如本文所定义，化合物公式（1）还可以进一步包含一个羟基取代基或0-葡萄糖醛酸。本发明还涉及通过给予公式（1）的化合物来治疗哺乳动物中的异常细胞生长的方法，以及包含公式（1）的化合物的用于治疗此类疾病的制药组合物。本发明还涉及制备公式（1）的化合物的方法。
• Dosing schedule for a novel anticancer agent
  申请人：Bhattacharya Kumar Samit

  公开号：US20050119288A1

  公开（公告）日：2005-06-02

  The invention is directed to methods for the a method for treating overexpression of the erbB2 in a mammal in need of treatment by administering to the mammal a therapeutically effective amount of a first inhibitor of an erbB2 receptor and then, after an interval of less than 24 hours, administering to the mammal from one to six therapeutically effective amounts of the same or different inhibitor of the erbB2 receptor. The invention is also directed to a slow daily infusion of the erbB2 inhibitor. The overexpression of the erbB2 receptor can result in abnormal cell growth and lead to cancer. By the methods of the invention, the efficacy and safety of the inhibitors is increased. The invention is also directed to kits for facilitating the dose administration method of the invention.

  本发明涉及一种治疗需要治疗的哺乳动物体内erbB2过度表达的方法，该方法是给哺乳动物注射治疗有效量的第一种erbB2受体抑制剂，然后在间隔少于24小时后，给哺乳动物注射一至六种治疗有效量的相同或不同的erbB2受体抑制剂。本发明还涉及每天缓慢输注 erbB2 抑制剂。erbB2受体的过度表达可导致细胞异常生长并引发癌症。通过本发明的方法，可以提高抑制剂的疗效和安全性。本发明还涉及用于促进本发明剂量给药方法的试剂盒。
• SUBSTITUTED BICYCLIC DERIVATIVES FOR THE TREATMENT OF ABNORMAL CELL GROWTH
  申请人：Pfizer Products Inc.

  公开号：EP1292591B1

  公开（公告）日：2005-02-02
• 4-ANILINO QUINAZOLINE DERIVATIVES FOR THE TREATMENT OF ABNORMAL CELL GROWTH
  申请人：Pfizer Products Inc.

  公开号：EP1575592A1

  公开（公告）日：2005-09-21