4-chloro-6-(2-chloroethoxy)-7-methoxyquinazoline | 692059-26-0

• 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-6-(2-chloroethoxy)-7-methoxyquinazoline
• CAS: 692059-26-0
• 化学式: C₁₁H₁₀Cl₂N₂O₂
• 分子量: 273.119
• InChiKey: RWNKOYZBHLRFEM-UHFFFAOYSA-N

物化性质

• 沸点：
  403.1±40.0 °C(Predicted)
• 密度：
  1.380±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  3
• 重原子数：
  17
• 可旋转键数：
  4
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.27
• 拓扑面积：
  44.2
• 氢给体数：
  0
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  4-chloro-6-(2-chloroethoxy)-7-methoxyquinazoline 在 四丁基碘化铵 、 N,N-二异丙基乙胺 作用下， 以 N,N-二甲基甲酰胺 为溶剂， 生成 1-(5-tert-butylisoxazol-3-yl)-3-(3-(7-methoxy-6-(2-morpholinoethoxy)quinazolin-4-yloxy)phenyl)urea
  参考文献：
  名称：

  4-Quinazolinyloxy-diaryl ureas as novel BRAFV600E inhibitors

  摘要：

  Aryl phenyl ureas with a 4-quinazolinoxy substituent at the meta-position of the phenyl ring are potent inhibitors of mutant and wild type BRAF kinase. Compound 7 (1-(5-tert-butylisoxazol-3-yl)-3-(3-(6,7-dimethoxyquinazolin-4-yloxy) phenyl) urea hydrochloride) exhibits good pharmacokinetic properties in rat and mouse and is efficacious in a mouse tumor xenograft model following oral dosing. (C) 2011 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2011.07.019
• 作为产物：
  描述：

  6-(2-chloroethoxy)-4-hydroxy-7-methoxyquinazoline 在 三乙胺 、 三氯氧磷 作用下， 生成 4-chloro-6-(2-chloroethoxy)-7-methoxyquinazoline
  参考文献：
  名称：

  4-Quinazolinyloxy-diaryl ureas as novel BRAFV600E inhibitors

  摘要：

  Aryl phenyl ureas with a 4-quinazolinoxy substituent at the meta-position of the phenyl ring are potent inhibitors of mutant and wild type BRAF kinase. Compound 7 (1-(5-tert-butylisoxazol-3-yl)-3-(3-(6,7-dimethoxyquinazolin-4-yloxy) phenyl) urea hydrochloride) exhibits good pharmacokinetic properties in rat and mouse and is efficacious in a mouse tumor xenograft model following oral dosing. (C) 2011 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2011.07.019

文献信息

• [EN] QUINAZOLINE DERIVATIVES FOR USE AGAINST CANCER<br/>[FR] DERIVES DE QUINAZOLINE A UTILISER CONTRE LE CANCER
  申请人：ASTRAZENECA AB

  公开号：WO2006040526A1

  公开（公告）日：2006-04-20

  The invention concerns quinazoline derivatives of Formula (I) or a pharmaceutically-acceptable salt, solvate or pro-drug thereof, wherein each of p, R1, q, R2, R3, R4, R5, Ring A, X1, R6, r and R7 has any of the meanings defined in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use in the treatment of cell proliferative disorders or in the treatment of disease states associated with angiogenesis and/or vascular permeability.

  本发明涉及式(I)喹唑啉衍生物或其药物可接受的盐、溶剂化物或前药，其中p、R1、q、R2、R3、R4、R5、环A、X1、R6、r和R7各自具有说明书中定义的任何含义；其制备方法、含有它们的药物组合物以及它们在制造用于治疗细胞增殖障碍或治疗与血管生成和/或血管通透性相关的疾病状态的药物中的应用。
• [EN] QUINAZOLINE DERIVATIVES AS SRC TYROSINE KINASE INHIBITORS<br/>[FR] DERIVES DE QUINAZOLINE UTILISES COMME INHIBITEURS DE SRC TYROSINE KINASE
  申请人：ASTRAZENECA AB

  公开号：WO2004041829A1

  公开（公告）日：2004-05-21

  The invention concerns quinazoline derivatives of Formula (I): (A chemical formula should be inserted here - please see paper copy enclosed herewith) wherein Z is an O, S, SO, SO2, N(R2) or C(R2)2 group wherein each R2 group is hydrogen or (1-8C) alkyl, m is 0, 1, 2 or 3, each R1 group is selected from halogeno, (1-8C) alkyl, (1-6C) alkoxy and any of the other meanings defined in the description, n is 0, 1, 2 or 3, and each R3 group is selected from halogeno, (1-8C) alkyl, (1-6C) alkoxy and any of the other meanings defined in the description, or pharmaceutically-acceptable salts thereof, processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use as an anti-invasive agent in the containment and/or treatment of solid tumour disease.

  该发明涉及式（I）的喹唑啉衍生物：其中Z是O、S、SO、SO2、N（R2）或C（R2）2基团，其中每个R2基团是氢或（1-8C）烷基，m为0、1、2或3，每个R1基团选自卤代烷基、（1-8C）烷基、（1-6C）烷氧基和描述中定义的其他含义，n为0、1、2或3，每个R3基团选自卤代烷基、（1-8C）烷基、（1-6C）烷氧基和描述中定义的其他含义，或其药用盐，其制备方法，含有它们的药物组合物以及它们在制备用作抗侵袭剂的药物中的使用，用于抑制和/或治疗实体肿瘤疾病。
• Combination product of inhibitor of the src family of non-recetpor tyrosine kinases and gemcitabine
  申请人：Barge Alan

  公开号：US20060142297A1

  公开（公告）日：2006-06-29

  The invention concerns a combination comprising an inhibitor of Src kinase and the cytotoxic agent gemcitabine, a pharmaceutical composition comprising such a combination and its use in the treatment or prophylaxis of cancer, particularly of pancreatic cancer.

  本发明涉及一种组合物，包括Src激酶抑制剂和细胞毒素吉西他滨，一种含有该组合物的药物组合物以及其在治疗或预防癌症，特别是胰腺癌方面的用途。
• Quinazoline derivatives as src tyrosine kinase inhibitors
  申请人：Ple Patrick

  公开号：US20060122199A1

  公开（公告）日：2006-06-08

  The invention concerns quinazoline derivatives of Formula (I): (A chemical formula should be inserted here—please see paper copy enclosed herewith) wherein Z is an O, S, SO, SO 2 , N(R 2 ) or C(R 2 ) 2 group wherein each R 2 group is hydrogen or (1-8C) alkyl, m is 0, 1, 2 or 3, each R 1 group is selected from halogeno, (1-8C) alkyl, (1-6C) alkoxy and any of the other meanings defined in the description, n is 0, 1, 2 or 3, and each R 3 group is selected from halogeno, (1-8C) alkyl, (1-6C) alkoxy and any of the other meanings defined in the description, or pharmaceutically-acceptable salts thereof, processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use as an anti-invasive agent in the containment and/or treatment of solid tumour disease.

  本发明涉及化合物的喹嗪啉衍生物，其化学式为（I）：（此处应插入化学式，请参阅随附的纸质副本），其中Z为O、S、SO、SO2、N（R2）或C（R2）2基团，其中每个R2基团为氢或（1-8C）烷基，m为0、1、2或3，每个R1基团选自卤代基、（1-8C）烷基、（1-6C）烷氧基和描述中定义的其他含义，n为0、1、2或3，每个R3基团选自卤代基、（1-8C）烷基、（1-6C）烷氧基和描述中定义的其他含义，或其药学上可接受的盐，以及制备它们的方法、含有它们的制药组合物和它们在制造用于抗侵袭剂在包含和/或治疗实体肿瘤疾病的药物的用途。
• Therapeutic agents comprising an anti-angiogenic agent in combination with an src-inhibitor and their therapeutic use
  申请人：Curwen Owen Jon

  公开号：US20060223815A1

  公开（公告）日：2006-10-05

  The invention relates to the use of an anti-angiogenic agent in combination with an inhibitor of the Src family of non-receptor tyrosine kinases in the manufacture of a medicament for use in the substantially normotensive treatment in a warm-blooded mammal such as a human being of a disease state associated with angiogenesis, the Src kinase inhibitor being administered in an amount effective to counteract substantially the hypertension induced by the anti-angiogenic agent.

  本发明涉及在制造一种药物时使用抗血管生成剂与Src家族非受体酪氨酸激酶抑制剂相结合，用于治疗与血管生成有关的疾病状态，如在温血哺乳动物（如人类）中进行实质性正常血压治疗。 Src激酶抑制剂的用量有效地对抗抗血管生成剂引起的高血压。