1-[4-(6,7-dimethoxy-quinolin-4-yloxy)-phenyl]-3-(3-methoxy-propyl)-urea

• 分子结构分类: 有机化合物 - 有机氧化合物
• 英文名称: 1-[4-(6,7-dimethoxy-quinolin-4-yloxy)-phenyl]-3-(3-methoxy-propyl)-urea
• 英文别名: N-(3-Methoxypropyl)-N'-{4-[(6,7-dimethoxy-4-quinolyl)oxy]phenyl}urea；1-[4-(6,7-dimethoxyquinolin-4-yl)oxyphenyl]-3-(3-methoxypropyl)urea
• 化学式: C₂₂H₂₅N₃O₅
• 分子量: 411.458
• InChiKey: HPGMOIROOYBRQX-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.9
• 重原子数：
  30
• 可旋转键数：
  9
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.27
• 拓扑面积：
  90.9
• 氢给体数：
  2
• 氢受体数：
  6

反应信息

• 作为产物：
  描述：

  6,7-二甲氧基-4-(4-氨基苯氧基)喹啉 、 三光气 、 碳酸氢钠 、 3-甲氧基丙胺 在 乙酸乙酯 、 Brine 、 Sodium sulfate-III 、 silica gel 、 chloroform ethyl acetate 作用下， 以 甲苯 、 三乙胺 为溶剂， 反应 0.23h， 以to obtain 51 mg of the title compound (yield: 72%)的产率得到1-[4-(6,7-dimethoxy-quinolin-4-yloxy)-phenyl]-3-(3-methoxy-propyl)-urea
  参考文献：
  名称：

  Quinoline and quinazoline derivatives inhibiting platelet-derived growth

  摘要：

  本发明涉及一种新型喹啉衍生物和喹嗪衍生物，其由以下式子（I）所表示：##STR1## [其中R.sub.1和R.sub.2各自独立地为H或C.sub.1-C.sub.4-烷基，或者R.sub.1和R.sub.2共同形成C.sub.1-C.sub.3-亚烷基，X为O、S或CH.sub.2，W为CH或N，Q为取代芳基或取代杂环芳基]及其药学上可接受的盐，具有血小板源性生长因子受体自磷酸化抑制活性，以及含有这些化合物的制药组合物，以及用于治疗与异常细胞生长相关的疾病，如肿瘤的方法。

  公开号：

  US06143764A1

文献信息

• Quinoline Derivatives and Quinazoline Derivatives Inhibiting Autophosphrylation of Flt3 and Medicinal Compositions Containing the Same
  申请人：Miwa Atsushi

  公开号：US20080207617A1

  公开（公告）日：2008-08-28

  An objective of the present invention is to provide compounds and pharmaceuticals useful for the treatment of disease where the inhibition of autophosphorylation of FMS-like tyrosine kinase 3(Flt3) is therapeutically effective. The present invention relates to a pharmaceutical composition for use in the treatment or prevention of diseases where the inhibition of autophosphorylation of Flt3 therapeutically or prophylactically effective, which comprises a compound represented by formula (I) or a pharmaceutically acceptable salt or solvate thereof: wherein X represents CH or N; Z represents O or S; R 1 , R 2 , and R 3 represent H, OH, or optionally substituted alkoxy; R 4 represents H; R 5 , R 6 , R 7 , and R 8 represent H, Hal, alkyl or the like; and R 9 represents, e.g., alkyl substituted by t-butyl or the like.

  本发明的目标是提供化合物和药物，用于治疗抑制FMS样酪氨酸激酶3（Flt3）自磷酸化在治疗上具有疗效的疾病。本发明涉及一种药物组合物，用于治疗或预防抑制Flt3自磷酸化在治疗或预防上具有疗效的疾病，所述药物组合物包括以下公式（I）所表示的化合物或其药学上可接受的盐或溶剂：其中X代表CH或N；Z代表O或S；R1、R2和R3代表H、OH或可选取代的烷氧基；R4代表H；R5、R6、R7和R8代表H、卤素、烷基或类似物；R9代表例如被t-丁基或类似物取代的烷基。
• QUINOLINE DERIVATIVES AND QUINAZOLINE DERIVATIVES INHIBITING AUTOPHOSPHORYLATION OF Flt3 AND MEDICINAL COMPOSITIONS CONTAINING THE SAME
  申请人：KIRIN BEER KABUSHIKI KAISHA

  公开号：EP1566379A1

  公开（公告）日：2005-08-24

  An objective of the present invention is to provide compounds and pharmaceticals useful for the treatment of disease where the inhibition of autophosphorylation of FMS-like tyrosine kinase 3(Flt3) is therapeutically effective. The present invention relates to a pharmaceutical composition for use in the treatment or prevention of diseases where the inhibition of autophosphorylation of Flt3 therapeutically or prophylactically effective, which comprises a compound represented by formula (I) or a pharmaceutically acceptable salt or solvate thereof: wherein X represents CH or N; Z represents O or S; R1, R2, and R3 represent H, OH, or optionally substituted alkoxy; R4 represents H; R5, R6, R7, and R8 represent H, Hal, alkyl or the like; and R9 represents, e.g., alkyl substituted by t-butyl or the like.

  本发明的目的是提供用于治疗抑制FMS样酪氨酸激酶3(Flt3)的自身磷酸化具有治疗效果的疾病的化合物和药剂。本发明涉及一种用于治疗或预防抑制 Flt3 自身磷酸化具有治疗或预防效果的疾病的药物组合物，该药物组合物包含由式（I）代表的化合物或其药学上可接受的盐或溶液： 其中 X 代表 CH 或 N；Z 代表 O 或 S；R1、R2 和 R3 代表 H、OH 或任选取代的烷氧基；R4 代表 H；R5、R6、R7 和 R8 代表 H、Hal、烷基或类似物；以及 R9 代表例如被叔丁基或类似物取代的烷基。
• QUINOLINE DERIVATIVES AND QUINAZOLINE DERIVATIVES INHIBITING AUTOPHOSPHORYLATION OF GROWTH FACTOR RECEPTOR ORIGINATING IN PLATELET AND PHARMACEUTICAL COMPOSITIONS CONTAINING THE SAME
  申请人：KIRIN BEER KABUSHIKI KAISHA

  公开号：EP0860433B1

  公开（公告）日：2002-07-03
• US6143764A
  申请人：——

  公开号：US6143764A

  公开（公告）日：2000-11-07
• Quinoline and quinazoline derivatives inhibiting platelet-derived growth
  申请人：Kirin Beer Kabushiki Kaisha

  公开号：US06143764A1

  公开（公告）日：2000-11-07

  The present invention relates to novel quinoline derivatives and quinazoline derivatives represented by the following formula (I): ##STR1## [wherein R.sub.1 and R.sub.2 are each independently H or C.sub.1 -C.sub.4 -alkyl, or R.sub.1 and R.sub.2 together form C.sub.1 -C.sub.3 -alkylene, X is O, S or CH.sub.2, W is CH or N, and Q is a substituted aryl group or substituted heteroaryl group] and their pharmaceutically acceptable salts, having platelet-derived growth factor receptor autophosphorylation inhibitory activity, to pharmaceutical compositions containing these compounds, and to methods for the treatment of diseases associated with abnormal cell growth such as tumors.

  本发明涉及由以下式（I）表示的新型喹啉衍生物和喹唑啉衍生物：[其中R.sub.1和R.sub.2分别独立地为H或C.sub.1 -C.sub.4 -烷基，或R.sub.1和R.sub.2一起形成C.sub.1 -C.sub.3 -烷基，X为O、S或CH.sub.2，W为CH或N，Q为取代芳基或取代杂芳基]及其在药学上可接受的盐，具有血小板源性生长因子受体自磷酸化抑制活性，用于含有这些化合物的药物组合物，以及用于治疗与异常细胞生长（如肿瘤）相关的疾病的方法。