4-(6-chloro-2,3-methylenedioxyanilino)-7-[3(4-cyanomethylpiperazin-1-yl)propoxy]-6-methoxyquinazoline | 401811-30-1

• 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-(6-chloro-2,3-methylenedioxyanilino)-7-[3(4-cyanomethylpiperazin-1-yl)propoxy]-6-methoxyquinazoline
• 英文别名: 4-(6-Chloro-2,3-methylenedioxyanilino)-7-[3-(4-cyanomethylpiperazin-1-yl)propoxy]-6-methoxyquinazoline；2-[4-[3-[4-[(5-chloro-1,3-benzodioxol-4-yl)amino]-6-methoxyquinazolin-7-yl]oxypropyl]piperazin-1-yl]acetonitrile
• CAS: 401811-30-1
• 化学式: C₂₅H₂₇ClN₆O₄
• 分子量: 510.98
• InChiKey: QTDVHHYSYHHNBA-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.8
• 重原子数：
  36
• 可旋转键数：
  9
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.4
• 拓扑面积：
  105
• 氢给体数：
  1
• 氢受体数：
  10

反应信息

• 作为产物：
  描述：

  4-(6-Chloro-2,3-methylenedioxyanilino)-6-methoxy-7-(3-piperazin-1-ylpropoxy)quinazoline 、 氯乙腈 、 碘化钾 、 potassium carbonate 在 乙酸乙酯 、 水 、 Brine 、 magnesium sulfate 、 crude product 、 silica 、 二氯甲烷 、 甲醇 作用下， 以 N,N-二甲基甲酰胺 为溶剂， 反应 16.0h， 以There was thus obtained the title compound (0.13 g) as a solid的产率得到4-(6-chloro-2,3-methylenedioxyanilino)-7-[3(4-cyanomethylpiperazin-1-yl)propoxy]-6-methoxyquinazoline
  参考文献：
  名称：

  Therapeutic use

  摘要：

  本发明涉及在温血动物中预防或治疗T细胞介导的疾病或医疗情况，如自身免疫疾病（如移植排斥或类风湿性关节炎）的药物制剂中使用式（I）的喹唑啉衍生物，其中m，R1，n，R2和R3中的每一个具有在说明书中定义的任何含义。

  公开号：

  US07157467B2

文献信息

• Quinazoline derivatives
  申请人：——

  公开号：US20040034046A1

  公开（公告）日：2004-02-19

  The invention concerns quinazoline derivatives of Formula (I) wherein each of m, R 1 , n, R 2 and R 3 have 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 as an anti-invasive 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m、R1、n、R2和R3中的每一个具有描述中定义的任意含义；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剂的药物中用于抑制和/或治疗实体肿瘤疾病的用途。
• [EN] QUINAZOLINE DERIVATIVES<br/>[FR] DERIVES DE QUINAZOLINE
  申请人：ASTRAZENECA AB

  公开号：WO2002016352A1

  公开（公告）日：2002-02-28

  The invention concerns quinazoline derivatives of Formula (I) wherein each of m, R?1, n, R2 and R3¿ have 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 as an anti-invasive agent in the containment and/or treatment of solid tumour disease.

  本发明涉及式（I）的喹唑啉衍生物，其中m、R1、n、R2和R3中的每一个具有在说明书中定义的任何含义；它们的制备过程，包含它们的制药组合物以及它们在制造用于抗侵袭剂治疗和/或治疗实体瘤疾病的药物中的使用。
• 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。
• 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。
• THERAPEUTIC AGENTS COMPRISING AN ANTI-ANGIOGENIC AGENT IN COMBINATION WITH AN SRC-INHIBITOR AND THEIR THERAPEUTIC USE
  申请人：CURWEN Jon Owen

  公开号：US20100029673A1

  公开（公告）日：2010-02-04

  The invention relates to a method for the production of an anti-cancer effect or a method for the treatment of a sold tumour disease by administration of an anti-angiogenic agent selected from 4-(4-fluoro-2-methylindol-5-yloxy)-6-methoxy-7-(3-(pyrrolidin-1-yl)propoxy)quinazoline and 4-(4-bromo-2-fluoroanilino)-6-methoxy-7-(1-methylpiperidin-4-ylmethoxy)quinazoline and pharmaceutically-acceptable acid-addition salts thereof, in combination with a Src kinase inhibitor selected from 4-(6-chloro-2,3-methylenedioxyanilino)-7-[2-(4-methylpiperazin-1-yl)ethoxy]-5-tetrahydropyran-4-yloxyquinazoline and pharmaceutically-acceptable acid-addition salts thereof.

  本发明涉及一种通过给予选择自4-(4-氟-2-甲基吲哚-5-氧基)-6-甲氧基-7-(3-(吡咯烷-1-基)丙氧基)喹唑啉和4-(4-溴-2-氟苯胺基)-6-甲氧基-7-(1-甲基哌啶-4-基甲氧基)喹唑啉及其药学上可接受的酸盐，结合选择自4-(6-氯-2,3-亚甲二氧基苯胺基)-7-[2-(4-甲基哌嗪-1-基)乙氧基]-5-四氢吡喃-4-氧基喹唑啉及其药学上可接受的酸盐的Src激酶抑制剂，以产生抗癌效应或治疗固体肿瘤疾病的方法。