2-(6-anilino-8-chloro-7-fluoro-5-methoxy-2-piperidin-1-yloxyquinazolin-4-yl)-N-methylacetamide

• 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-(6-anilino-8-chloro-7-fluoro-5-methoxy-2-piperidin-1-yloxyquinazolin-4-yl)-N-methylacetamide
• 化学式: C₂₃H₂₅ClFN₅O₃
• 分子量: 473.9
• InChiKey: NQEQBXZVUMJWGL-UHFFFAOYSA-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：
  0.35
• 拓扑面积：
  88.6
• 氢给体数：
  2
• 氢受体数：
  8

文献信息

• [EN] QUINAZOLINE INHIBITORS OF ACTIVATING MUTANT FORMS OF EPIDERMAL GROWTH FACTOR RECEPTOR<br/>[FR] INHIBITEURS QUINAZOLINE DE L'ACTIVATION DES FORMES MUTANTES DU RÉCEPTEUR DE CROISSANCE ÉPIDERMIQUE (EGFR)
  申请人：ASTRAZENECA AB

  公开号：WO2014135876A1

  公开（公告）日：2014-09-12

  The invention relates to compounds of formula(I), or a pharmaceutically acceptable salt thereof: Formula (I) which possess inhibitory activity against activating mutant forms of EGFR,and are accordingly useful for their anti-cancer activity and in methods of treatment of the human or animal body. The invention also relates pharmaceutical compositions containing them and to their use in the manufacture of medicaments of use in the production of an anti- cancer effect in a warm-blooded animal such as man.

  该发明涉及公式(I)的化合物，或其药用可接受的盐：公式(I)具有对EGFR激活突变形式的抑制活性，因此对其抗癌活性以及对人体或动物身体的治疗方法具有用处。该发明还涉及含有这些化合物的药物组合物，以及它们在制造用于在温血动物（如人类）中产生抗癌效果的药物中的用途。
• Quinazoline Inhibitors of activating mutant forms of Epidermal Growth Factor Receptor
  申请人：AstraZeneca AB

  公开号：US20150320751A1

  公开（公告）日：2015-11-12

  The invention relates to compounds of formula (I), or a pharmaceutically acceptable salt thereof: which possess inhibitory activity against activating mutant forms of EGFR, and are accordingly useful for their anti-cancer activity and in methods of treatment of the human or animal body. The invention also relates to processes for the manufacture of the compounds, or a pharmaceutically acceptable salt thereof, to pharmaceutical compositions containing them and to their use in the manufacture of medicaments of use in the production of an anti-cancer effect in a warm-blooded animal such as man.

  该发明涉及公式（I）的化合物或其药学上可接受的盐：该化合物具有抑制EGFR活化突变形式的活性，因此在抗癌活性及人体或动物体的治疗方法中有用。该发明还涉及制造该化合物或其药学上可接受的盐的过程，包含它们的制药组成物以及它们在制造用于在温血动物（如人）中产生抗癌效果的药物中的应用。
• QUINAZOLINE INHIBITORS OF ACTIVATING MUTANT FORMS OF EPIDERMAL GROWTH FACTOR RECEPTOR
  申请人：AstraZeneca AB

  公开号：US20160340342A1

  公开（公告）日：2016-11-24

  The invention relates to compounds of formula (I), or a pharmaceutically acceptable salt thereof: which possess inhibitory activity against activating mutant forms of EGFR, and are accordingly useful for their anti-cancer activity and in methods of treatment of the human or animal body. The invention also relates to processes for the manufacture of the compounds, or a pharmaceutically acceptable salt thereof, to pharmaceutical compositions containing them and to their use in the manufacture of medicaments of use in the production of an anti-cancer effect in a warm-blooded animal such as man.

  本发明涉及化合物I的公式，或其药学上可接受的盐：其具有抑制EGFR激活突变形式的活性，因此对于其抗癌活性以及在治疗人类或动物体的方法中是有用的。本发明还涉及制造该化合物或其药学上可接受的盐的过程，含有它们的制药组合物以及它们在制造用于在温血动物（如人类）中产生抗癌效果的药物的制剂中的使用。
• EP2964638B1
  申请人：——

  公开号：EP2964638B1

  公开（公告）日：2017-08-09
• US20140255428A1
  申请人：——

  公开号：US20140255428A1

  公开（公告）日：2014-09-11