4-chloro-7-methoxy-5-((tetrahydro-2H-pyran-4-yl)oxy)quinazoline | 643086-67-3

• 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: 4-chloro-7-methoxy-5-((tetrahydro-2H-pyran-4-yl)oxy)quinazoline
• 英文别名: 4-chloro-7-(methyloxy)-5-(tetrahydro-2H-pyran-4-yloxy)quinazoline；4-chloro-7-methoxy-5-(oxan-4-yloxy)quinazoline
• CAS: 643086-67-3
• 化学式: C₁₄H₁₅ClN₂O₃
• 分子量: 294.738
• InChiKey: MSTUTJZYMNCUSX-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.9
• 重原子数：
  20
• 可旋转键数：
  3
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.43
• 拓扑面积：
  53.5
• 氢给体数：
  0
• 氢受体数：
  5

反应信息

• 作为反应物：
  描述：

  4-chloro-7-methoxy-5-((tetrahydro-2H-pyran-4-yl)oxy)quinazoline 、 3-氯-4-氟苯胺 在 N,N-二异丙基乙胺 、 异丙醇 作用下， 生成 (3-Chloro-4-fluoro-phenyl)-[7-methoxy-5-(tetrahydro-pyran-4-yloxy)-quinazolin-4-yl]-amine
  参考文献：
  名称：

  Inhibitors of epidermal growth factor receptor tyrosine kinase: Novel C-5 substituted anilinoquinazolines designed to target the ribose pocket

  摘要：

  A series of novel C-5 substituted anilinoquinazolines, selected on the basis of docking experiments and overlays with ATP in the active site of EGFR tyrosine kinase, have been prepared and found to be potent inhibitors. In vivo pharmacokinetics and disease model activity are discussed. (C) 2005 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2005.12.028
• 作为产物：
  描述：

  2,2-Dimethyl-propionic acid 7-methoxy-4-oxo-5-(tetrahydro-pyran-4-yloxy)-4H-quinazolin-3-ylmethyl ester 在 氨 、 N,N-二异丙基乙胺 、 三氯氧磷 作用下， 以 甲醇 、 1,2-二氯乙烷 为溶剂， 生成 4-chloro-7-methoxy-5-((tetrahydro-2H-pyran-4-yl)oxy)quinazoline
  参考文献：
  名称：

  Inhibitors of epidermal growth factor receptor tyrosine kinase: Novel C-5 substituted anilinoquinazolines designed to target the ribose pocket

  摘要：

  A series of novel C-5 substituted anilinoquinazolines, selected on the basis of docking experiments and overlays with ATP in the active site of EGFR tyrosine kinase, have been prepared and found to be potent inhibitors. In vivo pharmacokinetics and disease model activity are discussed. (C) 2005 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2005.12.028

文献信息

• [EN] QUINAZOLINE DERIVATIVES AS TAM FAMILY KINASE INHIBITORS<br/>[FR] DÉRIVÉS DE QUINAZOLINE SERVANT D'INHIBITEURS DES KINASES DE LA FAMILLE TAM
  申请人：SIGNALCHEM LIFESCIENCES CORP

  公开号：WO2015077375A1

  公开（公告）日：2015-05-28

  Disclosed are compounds, compositions and methods for treating diseases, syndromes, conditions and disorders that are affected by the modulation of the activity of, e.g., the inhibition of, one or more members of the TAM family kinases.

  揭示了一种用于治疗受到TAM家族激酶的活性调节（例如抑制）影响的疾病、综合症、状况和障碍的化合物、组合物和方法。
• [EN] QUINAZOLINE DERIVATIVES FOR USE IN THE TREATMENT OF CANCER<br/>[FR] DERIVES DE QUINAZOLINE UTILISES DANS LE TRAITEMENT DU CANCER
  申请人：ASTRAZENECA AB

  公开号：WO2004004732A1

  公开（公告）日：2004-01-15

  The invention concerns quinazoline derivatives of Formula (I) wherein each of Z, m, R1, n, R3,Z2 and R14 have any of the meanings defined hereinbefore in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use as an anti-invasive or anti-proliferative agent in the containment and/or treatment of solid tumour disease.

  这项发明涉及式（I）的喹唑啉衍生物，其中Z、m、R1、n、R3、Z2和R14中的每一个具有在描述中先前定义的任何含义；它们的制备方法，含有它们的药物组合物以及它们在制造用作抗侵袭或抗增殖剂的药物时在固体肿瘤疾病的控制和/或治疗中的用途。
• Quinzoline derivatives for use in the treatment of cancer
  申请人：Hennequin Francois Andre Laurent

  公开号：US20050250797A1

  公开（公告）日：2005-11-10

  The invention concerns quinazoline derivatives of Formula (I) wherein each of Z, m, R 1 , n, R 3 ,Z 2 and R 14 have any of the meanings defined hereinbefore in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use as an anti-invasive or anti-proliferative agent in the containment and/or treatment of solid tumour disease.

  本发明涉及公式（I）的喹唑啉衍生物，其中Z，m，R1，n，R3，Z2和R14中的每一个都具有本说明书中定义的任何含义；它们的制备过程，含有它们的制药组合物以及它们在制造用于抗侵袭或抗增殖剂的药物时，在包含和/或治疗实体肿瘤疾病方面的用途。
• RAF KINASE MODULATOR COMPOUNDS AND METHODS OF USE THEREOF
  申请人：Abraham Sunny

  公开号：US20110118245A1

  公开（公告）日：2011-05-19

  Compounds according to formula (I), compositions and methods are provided for modulating the activity of RAF kinases, including BRAF kinase and for the treatment, prevention, or amelioration of one or more symptoms of disease or disorder mediated by RAF kinases. Formula (I): or a pharmaceutically acceptable salt, solvate, clathrate of hydrate thereof, wherein X is O or S(O) t ; R a is O or S.

  提供了按照公式(I)的化合物、组合物和方法，用于调节RAF激酶的活性，包括BRAF激酶，并用于治疗、预防或缓解由RAF激酶介导的一种或多种疾病或障碍的症状。公式(I)：或其药学上可接受的盐、溶剂化合物、包合物或水合物，其中X为O或S(O)t；R为O或S。
• QUINAZOLINE COMPOUNDS
  申请人：Kallander Lara S.

  公开号：US20120220588A1

  公开（公告）日：2012-08-30

  Disclosed are compounds having the formula: wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 and R 7 are as defined herein, and methods of making and using the same.

  揭示了具有以下公式的化合物：其中R1、R2、R3、R4、R5、R6和R7如本文所定义，并且揭示了制备和使用它们的方法。