6-溴-4-氯-7-甲氧基喹啉-3-羧酸乙酯 | 476194-45-3

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 喹啉及其衍生物
• 中文名称: 6-溴-4-氯-7-甲氧基喹啉-3-羧酸乙酯
• 英文名称: ethyl 6-bromo-4-chloro-7-methoxyquinoline-3-carboxylate
• CAS: 476194-45-3
• 化学式: C₁₃H₁₁BrClNO₃
• 分子量: 344.592
• InChiKey: VLEZWYGNJDQJMJ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.7
• 重原子数：
  19
• 可旋转键数：
  4
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.23
• 拓扑面积：
  48.4
• 氢给体数：
  0
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  6-溴-4-氯-7-甲氧基喹啉-3-羧酸乙酯 在 tris-(dibenzylideneacetone)dipalladium(0) 、 R-(+)-1,1'-联萘-2,2'-双二苯膦 caesium carbonate 、 溶剂黄146 作用下， 以 N,N-二甲基甲酰胺 、 甲苯 为溶剂， 反应 20.0h， 生成 ethyl 4-[(2,3-dichlorophenyl)amino]-7-methoxy-6-(4-methylpiperazin-1-yl)quinoline-3-carboxylate
  参考文献：
  名称：

  WO2007/119046

  摘要：

  公开号：
• 作为产物：
  描述：

  乙氧基甲叉丙二酸二乙酯 在 三氯氧磷 作用下， 以 二苯醚 为溶剂， 生成 6-溴-4-氯-7-甲氧基喹啉-3-羧酸乙酯
  参考文献：
  名称：

  [EN] COMPOUNDS FOR THE DEGRADATION OF BRD9 OR MTH1
  [FR] COMPOSÉS POUR LA DÉGRADATION DE BRD9 OU MTH1

  摘要：

  提供了通过泛素蛋白酶体途径降解BRD9或MTH1的化合物，用于治疗需要的受体。提供的化合物具有与BRD9或MTH1的靶向配体相连的E3泛素连接酶靶向基团（Degron）。

  公开号：

  WO2020051235A1

文献信息

• Novel 4-anilinoquinoline-3-carboxamides
  申请人：——

  公开号：US20040248923A1

  公开（公告）日：2004-12-09

  The present invention relates to novel compounds of formula (IA), which are JAK3 Kinase inhibitors, methods for their preparation and pharmaceutical compositions comprising them.

  本发明涉及公式（IA）的新型化合物，它们是JAK3激酶抑制剂，以及它们的制备方法和包含它们的药物组合物。
• 4-ANILINOQUINOLINE-3-CARBOXAMIDES AS CSF-1R KINASE INHIBITORS
  申请人：Cook Donald

  公开号：US20090054411A1

  公开（公告）日：2009-02-26

  The invention relates to chemical compounds of formula IA or IB: or pharmaceutically acceptable salts thereof which possess CSF-1R kinase inhibitory activity and are accordingly useful for their anti-cancer activity and thus in methods of treatment of the human or animal body. The invention also relates to processes for the manufacture of said chemical compounds, 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.

  该发明涉及化学式IA或IB的化合物：或其药学上可接受的盐，其具有CSF-1R激酶抑制活性，因此在抗癌活性和人或动物体的治疗方法中有用。该发明还涉及制造所述化学化合物的过程，包含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中的使用。
• CHEMICAL COMPOUNDS
  申请人：Dakin Leslie

  公开号：US20090270450A1

  公开（公告）日：2009-10-29

  The invention relates to chemical compounds of formula (I): or pharmaceutically acceptable salts thereof which possess CSF-1R kinase inhibitory activity and are accordingly useful for their anti-cancer activity and thus in methods of treatment of the human or animal body. The invention also relates to processes for the manufacture of said chemical compounds, 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.

  该发明涉及化学式（I）的化合物或其药学上可接受的盐，其具有CSF-1R激酶抑制活性，因此在抗癌活性方面有用，因此可以用于人或动物体的治疗方法。该发明还涉及制造所述化学化合物的过程，含有它们的制药组合物以及它们在制造用于在温血动物（例如人）中产生抗癌效果的药物中的使用。
• 3-Amido-4-anilinoquinolines as CSF-1R kinase inhibitors 2: Optimization of the PK profile
  作者：David A. Scott、Kirsten J. Bell、Cheryl T. Campbell、Donald J. Cook、Les A. Dakin、David J. Del Valle、Lisa Drew、Thomas W. Gero、Maureen M. Hattersley、Charles A. Omer、Boris Tyurin、Xiaolan Zheng

  DOI：10.1016/j.bmcl.2008.12.044

  日期：2009.2

  The optimization of compounds from the 3-amido-4-anilinoquinolines series of CSF-1R kinase inhibitors is described. The series has excellent activity and kinase selectivity. Excellent physical properties and rodent PK profiles were achieved through the introduction of cyclic amines at the quinoline 6-position. Compounds with good activity in a mouse PD model measuring inhibition of pCSF-1R were identified. (C) 2008 Elsevier Ltd. All rights reserved.
• Identification of 3-amido-4-anilinoquinolines as potent and selective inhibitors of CSF-1R kinase
  作者：David A. Scott、Carrie L. Balliet、Donald J. Cook、Audrey M. Davies、Thomas W. Gero、Charles A. Omer、Srinivasu Poondru、Maria-Elena Theoclitou、Boris Tyurin、Michael J. Zinda

  DOI：10.1016/j.bmcl.2008.12.046

  日期：2009.2

  3-Amido-4-anilinoquinolines are potent and highly selective inhibitors of CSF-1R. Their synthesis and SAR is reported, along with initial efforts to optimize the physical properties and PK through modi. cations at the quinoline 6- and 7-positions. (c) 2008 Elsevier Ltd. All rights reserved.