4-(6,7-dimethoxyquinolin-4-yloxy)-2,3-dimethylphenylamine | 286371-45-7

• 分子结构分类: 有机化合物 - 有机氧化合物
• 英文名称: 4-(6,7-dimethoxyquinolin-4-yloxy)-2,3-dimethylphenylamine
• 英文别名: 4-[(6,7-dimethoxy-4-quinolyl)oxy]-2,3-dimethylaniline；4-(6,7-dimethoxyquinolin-4-yl)oxy-2,3-dimethylaniline
• CAS: 286371-45-7
• 化学式: C₁₉H₂₀N₂O₃
• 分子量: 324.379
• InChiKey: ZKPSHRUKJGWIHO-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.7
• 重原子数：
  24
• 可旋转键数：
  4
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.21
• 拓扑面积：
  66.6
• 氢给体数：
  1
• 氢受体数：
  5

反应信息

• 作为反应物：
  描述：

  对甲氧基苯异氰酸酯 、 4-(6,7-dimethoxyquinolin-4-yloxy)-2,3-dimethylphenylamine 在 氯仿 、 乙醚 、 resultant precipitate 作用下， 以 氯仿 为溶剂， 反应 16.0h， 以to give 115 mg (yield 78%) of the title compound的产率得到N-{4-[(6,7-Dimethoxy-4-quinolyl)oxy]-2,3-dimethylphenyl}-N'-(4-methoxyphenyl)urea
  参考文献：
  名称：

  Quinoline derivatives and quinazoline derivatives

  摘要：

  本发明的目的是提供具有抗肿瘤活性且不改变细胞形态的化合物。本发明揭示了由式（I）表示的化合物及其药学上可接受的盐和溶剂和包含所述化合物的制药组合物：其中X和Z各自独立地表示CH或N；R1至R3表示H，取代烷氧基，未取代烷氧基或类似物；R4表示H；R5至R8表示H，卤素，烷基，烷氧基，烷硫基，硝基或氨基，前提是R5至R8不同时表示H；R9和R10表示H，烷基或烷基羰基；R11表示烷基，烯基，炔基或芳基烷基。

  公开号：

  US20070027318A1
• 作为产物：
  描述：

  4-氯 -6,7-二甲氧基喹啉 以 氯苯 为溶剂， 生成 4-(6,7-dimethoxyquinolin-4-yloxy)-2,3-dimethylphenylamine
  参考文献：
  名称：

  Orally active anti-proliferation agents: novel diphenylamine derivatives as FGF-R2 autophosphorylation inhibitors

  摘要：

  (6,7-二取代喹啉-4-基氧苯基)(4-取代苯基)胺衍生物通过在人瘢痕胃癌细胞系OCUM-2MD3中进行成纤维细胞生长因子受体2（FGF-R2）的细胞自体磷酸化试验而被合成和评估。我们还进行了代谢稳定性研究，结果显示喹啉环7位的取代基会影响其生物稳定性。在本研究中，我们显著改善了双苯胺衍生物的溶解性和代谢稳定性。最具潜力的化合物15e在口服给药时表现出肿瘤体积的显著减少。 ©2003 Elsevier Ltd. 保留所有权利。

  DOI：

  10.1016/j.bmcl.2003.12.019

文献信息

• [EN] URACIL DERIVATIVES AS AXL AND C-MET KINASE INHIBITORS<br/>[FR] DÉRIVÉS D'URACILE COMME INHIBITEURS D'AXL ET C-MET KINASES
  申请人：CEPHALON INC

  公开号：WO2013074633A1

  公开（公告）日：2013-05-23

  The present invention provides compounds of Formula I, or pharmaceutically acceptable salt forms thereof, wherein Ra, Rb, Rc, Rd, D, W, R1a, R1b, R1c,Y, R3, X, E and G are as defined herein, methods of treatment and uses thereof.

  本发明提供了式I的化合物，或其药用盐形式，其中Ra、Rb、Rc、Rd、D、W、R1a、R1b、R1c、Y、R3、X、E和G的定义如本文所述，以及其治疗方法和用途。
• Quinoline derivatives and quinazoline derivatives having azolyl group
  申请人：KIRIN BEER KABUSHIKI KAISHA

  公开号：US20030087907A1

  公开（公告）日：2003-05-08

  An object of the present invention is to provide compounds having potent antitumor activity. The compounds according to the present invention are compounds represented by formula (I) or pharmaceutically acceptable salts or solvates thereof: 1 wherein X and Z represent CH or N; Y represents O or S; R 1 , R 2 , and R 3 represent H, alkoxy or the like; R 4 represents H; R 5 , R 6 , R 7 , and R 8 represent H, halogen, alkoxy or the like; R 9 and R 10 represent H, alkyl or the like; and R 11 represents optionally substituted azolyl.

  本发明的一个目的是提供具有强效抗肿瘤活性的化合物。根据本发明的化合物是由式（I）表示的化合物或其药学上可接受的盐或溶剂：其中X和Z表示CH或N；Y表示O或S；R1、R2和R3表示H、烷氧基或类似物；R4表示H；R5、R6、R7和R8表示H、卤素、烷氧基或类似物；R9和R10表示H、烷基或类似物；R11表示选择性取代的唑基。
• Quinoline and quinazoline derivatives and drugs containing the same
  申请人：——

  公开号：US20040132727A1

  公开（公告）日：2004-07-08

  There are provided compounds which can be used in the treatment of diseases mediated by the autophosphorylation of a PDGF receptor, specifically, compounds which can inhibit neointima formation hypertrophy. The compounds are those represented by formula (I) or pharmacologically acceptable salts or solvates thereof: 1 wherein R 1 and R 2 represent hydrogen, alkyl or the like; R 3 , R 4 , R 5 and R 6 represent hydrogen, halogen, alkyl, alkoxy or the like; R 11 and R 12 represent hydrogen, alkyl, alkylcarbonyl or the like; and A represents any one of formulae (i) to (x), provided that compounds wherein R 3 , R 4 , R 5 and R 6 represent hydrogen and A represents group (v) wherein u is 0 (zero) and R 19 represents phenyl optionally substituted by halogen, alkyl, or alkoxy are excluded.

  提供了一些化合物，可用于治疗由PDGF受体自磷酸化介导的疾病，特别是可抑制新内膜形成肥大的化合物。这些化合物由式（I）或其药理学上可接受的盐或溶剂表示：1其中R1和R2表示氢，烷基或类似物；R3、R4、R5和R6表示氢，卤素，烷基，烷氧基或类似物；R11和R12表示氢，烷基，烷基羰基或类似物；而A表示公式（i）到（x）中的任意一个，但其中R3、R4、R5和R6表示氢，A表示组（v）其中u为0（零）且R19表示苯基，可选地被卤素，烷基或烷氧基取代的化合物被排除。
• Quinoline derivatives and quinazoline derivatives inhibiting autophosphorylation of macrophage colony stimulating factor receptor
  申请人：Kubo Kazuo

  公开号：US20060235033A1

  公开（公告）日：2006-10-19

  An objective of the present invention is to provide compounds which have inhibitory activity against autophosphorylation of macrophage colony-stimulating factor receptors. The compounds of the present invention are represented by formula (I) and salt and solvate thereof: wherein X represents CH or N; Z represents O or S; R 1 , R 2 , and R 3 represent H, optionally substituted alkoxy or the like; R 4 represents H; R 5 , R 6 , R 7 , and R 8 represent H, halogen, alkyl, alkoxy, trifluoromethyl or the like; R 9 and R 10 represent H, alkyl or the like; and any one of R 11 and R 12 represents H with the other representing alkyl and R 13 represents an optionally substituted carbocyclic or heterocyclic ring or the like, or R 11 represents H and R 12 and R 13 combine together to form a bicyclic carbocyclic ring.

  本发明的目标是提供具有抑制巨噬细胞集落刺激因子受体自磷酸化活性的化合物。本发明的化合物由式（I）及其盐和溶剂化物表示：其中X表示CH或N；Z表示O或S；R1、R2和R3表示H、可选地取代的烷氧基或类似物；R4表示H；R5、R6、R7和R8表示H、卤素、烷基、烷氧基、三氟甲基或类似物；R9和R10表示H、烷基或类似物；R11和R12中的任意一个表示H，另一个表示烷基，R13表示可选地取代的碳环或杂环环或类似物，或R11表示H，R12和R13结合形成双环碳环。
• 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。