4-{[7-(苄氧基)-6-甲氧基-4-喹啉基]氧基}-2-氟苯胺 | 479690-02-3

• 分子结构分类: 有机化合物 - 有机氧化合物
• 中文名称: 4-{[7-(苄氧基)-6-甲氧基-4-喹啉基]氧基}-2-氟苯胺
• 英文名称: 2-Fluoro-4-[(7-benzyloxy-6-methoxy-4-quinolyl)-oxy]aniline
• 英文别名: 4-[(7-Benzyloxy-6-methoxy-4-quinolyl)oxy]-2-fluoro-aniline；4-{[7-(Benzyloxy)-6-methoxy-4-quinolyl]oxy}-2-fluoroaniline；2-fluoro-4-(6-methoxy-7-phenylmethoxyquinolin-4-yl)oxyaniline
• CAS: 479690-02-3
• 化学式: C₂₃H₁₉FN₂O₃
• 分子量: 390.414
• InChiKey: HROUAIPPYJIEIU-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.6
• 重原子数：
  29
• 可旋转键数：
  6
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.09
• 拓扑面积：
  66.6
• 氢给体数：
  1
• 氢受体数：
  6

反应信息

• 作为反应物：
  描述：

  4-{[7-(苄氧基)-6-甲氧基-4-喹啉基]氧基}-2-氟苯胺 、 4-叔丁基苯硼酸 在 copper diacetate 、 三乙胺 作用下， 以 氯仿 为溶剂， 以82%的产率得到N-(4-{[7-(Benzyloxy)-6-methoxy-4-quinolyl]oxy}-2-fluorophenyl)-N-[4-(tert-butyl)phenyl]amine
  参考文献：
  名称：

  EP1447405

  摘要：

  公开号：
• 作为产物：
  描述：

  7-(benzyloxy)-4-(3-fluoro-4-nitrophenoxy)-6-methoxyquinoline 在 氯化铵 作用下， 以 乙醇 、 水 为溶剂， 反应 18.0h， 以94%的产率得到4-{[7-(苄氧基)-6-甲氧基-4-喹啉基]氧基}-2-氟苯胺
  参考文献：
  名称：

  QUINOLINE DERIVATIVE AND QUINAZOLINE DERIVATIVE INHIBITING SELF-PHOSPHORYLATION OF HEPATOCYTUS PROLIFERATOR RECEPTOR, AND MEDICINAL COMPOSITION CONTAINING THE SAME

  摘要：

  公开号：

  EP1411046B1

文献信息

• [EN] QUINOLINE DERIVATIVES AS AXL KINASE INHIBITORS<br/>[FR] DÉRIVÉS DE QUINOLINES UTILISÉS COMME INHIBITEURS DES KINASES AXL
  申请人：MAX PLANCK GESELLSCHAFT

  公开号：WO2009127417A1

  公开（公告）日：2009-10-22

  The present invention relates to novel compounds which are inhibitors of receptor tyrosine kinases of the AXL receptor family. These compounds are suitable for the treatment or prevention of disorders associated with, accompanied by or caused by hyperfunction of a receptor of the AXL family. The compounds are suitable for the treatment of hyperproliferative disorders, such as cancer, particularly cancer metastases.

  本发明涉及一种新型化合物，它们是AXL受体家族的受体酪氨酸激酶抑制剂。这些化合物适用于治疗或预防与AXL家族受体的受体功能亢进相关、伴随或引起的疾病。这些化合物适用于治疗增生性疾病，如癌症，特别是癌症转移。
• Quinoline derivative and quinazoline derivative inhibiting self-phosphorylation of hepatocytus proliferator receptor and medicinal composition containing the same
  申请人：——

  公开号：US20040242603A1

  公开（公告）日：2004-12-02

  An objective of the present invention is to provide compounds having potent antitumor activity. The compounds of the present invention are represented by formula (I) or a pharmaceutically acceptable salt or solvate thereof: 1 wherein X=CH or N; Z=O or S; L=O or S; M=CR 10 R 11 , wherein R 10 and R 11 =H, alkyl, or alkoxy, NR 12 wherein R 12 =H or alkyl; R 1 , R 2 , and R 3 =H or optionally substituted alkoxy; R 4 =H; R 5-8 =H, halogen, alkoxy or the like; and R 9 =alkyl optionally substituted by —R 14 , -T-R 15 , or —NR 16 R 17 wherein T=O, S, or NH; R 14 =an optionally substituted carbocyclic or heterocyclic ring; and R 15-17 =alkyl or an optionally substituted carbocyclic or heterocyclic ring, or —NR 18 R 19 wherein R 18 and R 19 =H, optionally substituted alkyl, or an optionally substituted carbocylic or heterocyclic ring, or optionally substituted carbocyclic or heterocyclic ring.

  本发明的目标是提供具有强效抗肿瘤活性的化合物。本发明的化合物由以下式子（I）或其药学上可接受的盐或溶剂表示：1其中X = CH或N；Z = O或S；L = O或S；M = CR10R11，其中R10和R11 = H，烷基或烷氧基，NR12，其中R12 = H或烷基；R1、R2和R3 = H或可选取代烷氧基；R4 = H；R5-8 = H、卤素、烷氧基或类似物；以及R9 = 烷基，可选取代-R14、-T-R15或-NR16R17，其中T = O、S或NH；R14 = 可选取代的碳环或杂环；R15-17 = 烷基或可选取代的碳环或杂环，或-NR18R19，其中R18和R19 = H、可选取代的烷基或可选取代的碳环或杂环，或可选取代的碳环或杂环。
• Quinoline or quinazoline derivatives inhibiting auto-phosphorylation of fibroblast growth factor receptors
  申请人：Miwa Atsushi

  公开号：US20050049264A1

  公开（公告）日：2005-03-03

  An objective of the present invention is to provide novel compounds which have inhibitory activity against autophosphorylation of an FGF receptor family and, when orally or intraveneously administered, can suppress the growth of cancer cells. The compounds of the present invention are represented by formula (I) or a pharmaceutically acceptable salt or solvate thereof: wherein X represents CH or N; Z represents O or S; Q represents NR 10 , CR 11 R 2 , carbonyl, O, S(═O)m, wherein m is 0 to 2, or urea; R 1 to R 3 each independently represent H, OH, halogen, nitro, amino, alkyl, alkoxy or the like in which the alkyl and alkoxy groups are optionally substituted; R 4 represents H; R 5 to R 8 each independently represent H, halogen, alkyl, or alkoxy; and R 9 represents an optionally substituted carbocyclic or heterocyclic group.

  本发明的目标是提供新型化合物，其具有对FGF受体家族自磷酸化的抑制活性，并在口服或静脉注射时能够抑制癌细胞的生长。本发明的化合物由公式（I）或其药学上可接受的盐或溶剂表示：其中X代表CH或N; Z代表O或S; Q代表NR10，CR11R2，羰基，O，S（═O）m，其中m为0到2，或脲基; R1至R3各自独立地表示H、OH、卤素、硝基、氨基、烷基、烷氧基或其类似物，其中烷基和烷氧基基团可选择性地被取代; R4表示H; R5至R8各自独立地表示H、卤素、烷基或烷氧基; R9表示一个可选择性取代的碳环或杂环基团。
• 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 DERIVATIVE AND QUINAZOLINE DERIVATIVE INHIBITING SELF&minus;PHOSPHORYLATION OF HEPATOCYTUS PROLIFERATOR RECEPTOR, AND MEDICINAL COMPOSITION CONTAINING THE SAME
  申请人：KIRIN BEER KABUSHIKI KAISHA

  公开号：EP1411046A1

  公开（公告）日：2004-04-21

  An objective of the present invention is to provide compounds having potent antitumor activity. The compounds of the present invention are represented by formula (I) or a pharmaceutically acceptable salt or solvate thereof: wherein X = CH or N; Z = O or S; L = O or S; M = CR10R11, wherein R10 and R11 = H, alkyl, or alkoxy, NR12 wherein R12 = H or alkyl; R1, R2, and R3 = H or optionally substituted alkoxy; R4 = H; R5-8 = H, halogen, alkoxy or the like; and R9 = alkyl optionally substituted by -R14, -T-R15, or -NR16R17 wherein T = O, S, or NH; R14 = an optionally substituted carbocyclic or heterocyclic ring; and R15-17 = alkyl or an optionally substituted carbocyclic or heterocyclic ring, or -NR18R19 wherein R18 and R19 = H, optionally substituted alkyl, or an optionally substituted carbocylic or heterocyclic ring, or optionally substituted carbocyclic or heterocyclic ring.

  本发明的目的是提供具有强效抗肿瘤活性的化合物。本发明的化合物由式（I）或其药学上可接受的盐或溶液表示： 其中 X = CH 或 N；Z = O 或 S；L = O 或 S；M = CR10R11，其中 R10 和 R11 = H、烷基或烷氧基，NR12，其中 R12 = H 或烷基；R1、R2 和 R3 = H 或任选取代的烷氧基；R4 = H；R5-8 = H、卤素、烷氧基或类似物；R9 = 任选被 -R14、-T-R15 或 -NR16R17 取代的烷基，其中 T = O、S 或 NH；R14 = 任选取代的碳环或杂环；以及 R15-17 = 烷基或任选取代的碳环或杂环，或 -NR18R19 其中 R18 和 R19 = H、任选取代的烷基或任选取代的碳环或杂环，或任选取代的碳环或杂环。