N-(1-ethyl-1H-pyrazol-4-yl)-2-[3-methoxy-5-(7-methoxyquinolin-4-yloxy)pyridin-2-yl]acetamide | 947763-01-1

• 分子结构分类: 有机化合物 - 有机氧化合物
• 英文名称: N-(1-ethyl-1H-pyrazol-4-yl)-2-[3-methoxy-5-(7-methoxyquinolin-4-yloxy)pyridin-2-yl]acetamide
• 英文别名: N-(1-ethylpyrazol-4-yl)-2-[3-methoxy-5-(7-methoxyquinolin-4-yl)oxypyridin-2-yl]acetamide
• CAS: 947763-01-1
• 化学式: C₂₃H₂₃N₅O₄
• 分子量: 433.467
• InChiKey: QZXMREJVHYOFOD-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2
• 重原子数：
  32
• 可旋转键数：
  8
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.22
• 拓扑面积：
  100
• 氢给体数：
  1
• 氢受体数：
  7

反应信息

• 作为产物：
  描述：

  4-氨基-1-乙基吡唑 、 在 N,N-二异丙基乙胺 、 Methanaminium,N-[(dimethylamino)(3H-1,2,3-triazolo[4,5-b]pyridin-3-yloxy)methylene]-N-methyl-, hexafluorophosphate(1-) 作用下， 以 N,N-二甲基甲酰胺 为溶剂， 反应 1.0h， 以62%的产率得到N-(1-ethyl-1H-pyrazol-4-yl)-2-[3-methoxy-5-(7-methoxyquinolin-4-yloxy)pyridin-2-yl]acetamide
  参考文献：
  名称：

  Discovery of new quinoline ether inhibitors with high affinity and selectivity for PDGFR tyrosine kinases

  摘要：

  A new series of quinoline ether inhibitors, which potently and selectively inhibit PDGFR tyrosine kinases, is described in this Letter. Compounds 23 and 33 are selective, low nanomolar inhibitors of PDGFR alpha and beta, display good pharmacokinetics in rat and dog and are active in vivo at low doses when given orally twice daily. Further evaluation of these compounds is warranted. (C) 2012 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2012.03.074

文献信息

• QUINOLINE DERIVATIVES
  申请人：Jung Frederic Henri

  公开号：US20090076075A1

  公开（公告）日：2009-03-19

  The invention concerns quinoline derivatives of Formula I or a pharmaceutically-acceptable salt thereof, wherein each of X 1 , p, R 1 , q, R 2 , R 3 , R 4 , R 5 Ring A, r and R 6 has any of the meanings defined hereinbefore in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use in the treatment of cell proliferative disorders.

  这项发明涉及公式I的喹啉衍生物或其药用盐，其中X 1 ，p，R 1 ，q，R 2 ，R 3 ，R 4 ，R 5 ，环A，r和R 6 中的每一个具有在描述中定义的任何含义；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于治疗细胞增殖紊乱的药物的药物中的使用。
• [EN] QUINOLINE DERIVATIVES<br/>[FR] DÉRIVÉS DE LA QUINOLINE
  申请人：ASTRAZENECA AB

  公开号：WO2007099323A2

  公开（公告）日：2007-09-07

  [EN] The invention concerns quinoline derivatives of Formula (I) or a pharmaceutically-acceptable salt thereof, wherein each of X¹, p, R¹, q, R², R³, R⁴, R⁵, Ring A, r and R⁶ has any of the meanings defined hereinbefore in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use in the treatment of cell proliferative disorders.
  [FR] L'invention concerne des dérivés de la quinoline de formule (I) ou un sel pharmaceutiquement acceptable de ceux-ci, X¹, p, R¹, q, R², R³, R⁴, R⁵, le cycle A, r et R⁶ ayant chacun l'une des significations définies dans la description ; des procédés pour leur préparation, des compositions pharmaceutiques qui les contiennent et leur utilisation dans la fabrication d'un médicament à utiliser dans le traitement de troubles prolifératifs cellulaires.
• Discovery of new quinoline ether inhibitors with high affinity and selectivity for PDGFR tyrosine kinases
  作者：Patrick A. Plé、Frédéric Jung、Sue Ashton、Laurent Hennequin、Romuald Laine、Christine Lambert-van der Brempt、Rémy Morgentin、Georges Pasquet、Sian Taylor

  DOI：10.1016/j.bmcl.2012.03.074

  日期：2012.5

  A new series of quinoline ether inhibitors, which potently and selectively inhibit PDGFR tyrosine kinases, is described in this Letter. Compounds 23 and 33 are selective, low nanomolar inhibitors of PDGFR alpha and beta, display good pharmacokinetics in rat and dog and are active in vivo at low doses when given orally twice daily. Further evaluation of these compounds is warranted. (C) 2012 Elsevier Ltd. All rights reserved.