4-((5-chloropyridin-3-yl)oxy)aniline

• 分子结构分类: 有机化合物 - 有机氧化合物
• 英文名称: 4-((5-chloropyridin-3-yl)oxy)aniline
• 英文别名: 5-(4-aminophenoxy)-3-chloropyridine；4-(5-chloropyridin-3-yl)oxyaniline
• 化学式: C₁₁H₉ClN₂O
• 分子量: 220.658
• InChiKey: CWQRKGHVWXNTGF-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.3
• 重原子数：
  15
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  48.1
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  4-((5-chloropyridin-3-yl)oxy)aniline 、 2,4-二氯苯磺酰氯 在 吡啶 作用下， 以 二氯甲烷 为溶剂， 生成 1-(3-chloro-5-pyridyloxy)-4-(2,4-dichlorobenzenesulfonamido)benzene
  参考文献：
  名称：

  Discovery of INT131: A selective PPARγ modulator that enhances insulin sensitivity

  摘要：

  PPAR gamma is a member of the nuclear hormone receptor family and plays a key role in the regulation of glucose homeostasis. This Letter describes the discovery of a novel chemical class of diarylsulfonamide partial agonists that act as selective PPAR gamma modulators (SPPAR gamma Ms) and display a unique pharmacological profile compared to the thiazolidinedione (TZD) class of PPAR gamma full agonists. Herein we report the initial discovery of partial agonist 4 and the structure-activity relationship studies that led to the selection of clinical compound INT131 (3), a potent PPAR gamma partial agonist that displays robust glucose-lowering activity in rodent models of diabetes while exhibiting a reduced side-effects profile compared to marketed TZDs. (C) 2012 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmc.2012.11.058
• 作为产物：
  描述：

  5-氯-3-羟基吡啶 在 tin(II) chloride dihdyrate 、 caesium carbonate 作用下， 以 乙酸乙酯 、 N,N-二甲基甲酰胺 为溶剂， 生成 4-((5-chloropyridin-3-yl)oxy)aniline
  参考文献：
  名称：

  Discovery of INT131: A selective PPARγ modulator that enhances insulin sensitivity

  摘要：

  PPAR gamma is a member of the nuclear hormone receptor family and plays a key role in the regulation of glucose homeostasis. This Letter describes the discovery of a novel chemical class of diarylsulfonamide partial agonists that act as selective PPAR gamma modulators (SPPAR gamma Ms) and display a unique pharmacological profile compared to the thiazolidinedione (TZD) class of PPAR gamma full agonists. Herein we report the initial discovery of partial agonist 4 and the structure-activity relationship studies that led to the selection of clinical compound INT131 (3), a potent PPAR gamma partial agonist that displays robust glucose-lowering activity in rodent models of diabetes while exhibiting a reduced side-effects profile compared to marketed TZDs. (C) 2012 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmc.2012.11.058

文献信息

• [EN] AGRICULTURAL CHEMICALS<br/>[FR] PRODUITS CHIMIQUES AGRICOLES
  申请人：GLOBACHEM NV

  公开号：WO2019141980A1

  公开（公告）日：2019-07-25

  The present invention relates to picolinic acid derivatives that are useful in treating fungal diseases ofplants.

  本发明涉及烟酸衍生物，用于治疗植物的真菌性病害。
• PPAR-&ggr; modulators
  申请人：Tularik Inc.

  公开号：US06200995B1

  公开（公告）日：2001-03-13

  Modulators of PPAR&ggr; activity are provided which are useful in pharmaceutical compositions and methods for the treatment of conditions such as type II diabetes and obesity.

  PPAR&ggr;活性调节剂提供了，这些调节剂在制药组合物和治疗类型II糖尿病和肥胖等疾病的方法中很有用。
• PPARgamma modulators
  申请人：Tularik Inc.

  公开号：US20010027200A1

  公开（公告）日：2001-10-04

  Modulators of PPAR&ggr; activity are provided which are useful in pharmaceutical compositions and methods for the treatment of conditions such as type II diabetes and obesity.

  提供了PPAR&ggr;活性的调节剂，这些调节剂在制药组合物和治疗2型糖尿病和肥胖等疾病的方法中非常有用。
• PPARγ modulators
  申请人：Amgen Inc.

  公开号：US07439242B2

  公开（公告）日：2008-10-21

  Modulators of PPARγ activity are provided which are useful in pharmaceutical compositions and methods for the treatment of conditions such as type II diabetes and obesity.

  提供了PPARγ活性的调节剂，这些调节剂在制药组合物和治疗II型糖尿病和肥胖症等疾病的方法中非常有用。
• PPAR-GAMMA MODULATORS
  申请人：TULARIK, INC.

  公开号：EP1053227A1

  公开（公告）日：2000-11-22