4-[4-(4-Fluoro-phenyl)-5-pyridin-4-yl-oxazol-2-yl]-1-methyl-piperidin-4-ol

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 唑类
• 英文名称: 4-[4-(4-Fluoro-phenyl)-5-pyridin-4-yl-oxazol-2-yl]-1-methyl-piperidin-4-ol
• 英文别名: 4-[4-(4-fluorophenyl)-5-pyridin-4-yl-1,3-oxazol-2-yl]-1-methylpiperidin-4-ol
• 化学式: C₂₀H₂₀FN₃O₂
• 分子量: 353.396
• InChiKey: OLWWIAFRNOFHTL-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.2
• 重原子数：
  26
• 可旋转键数：
  3
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.3
• 拓扑面积：
  62.4
• 氢给体数：
  1
• 氢受体数：
  6

反应信息

• 作为产物：
  描述：

  1-(4-氟苯基)-2-(4-吡啶基)乙酮 在 正丁基锂 、 ammonium oxalate 、 溴 、 溶剂黄146 作用下， 以 四氢呋喃 为溶剂， 生成 4-[4-(4-Fluoro-phenyl)-5-pyridin-4-yl-oxazol-2-yl]-1-methyl-piperidin-4-ol
  参考文献：
  名称：

  SAR of 4-hydroxypiperidine and hydroxyalkyl substituted heterocycles as novel p38 map kinase inhibitors

  摘要：

  The 4-hydroxypiyeridine substituent was found to confer high p38 selectivity devoid of COX-1 affinity, when attached to a series of pyridinyl substituted heterocycles. Pyridinyloxazole 11 showed a promising in vivo profile with bioavailability of 64% and ED50 in rat collagen induced arthritis of 10 mg/kg po bid. In contrast to pyridinylimidazoles such as SE 203580, 11 did not inhibit human cytochrome P450 isoenzymes. (C) 2000 Elsevier Science Ltd. All rights reserved.

  DOI：

  10.1016/s0960-894x(00)00200-6

文献信息

• Treatment of pain by inhibition of p38 map kinase
  申请人：Protter A. Andrew

  公开号：US20080039461A1

  公开（公告）日：2008-02-14

  The present invention relates to methods for the prevention or treatment of pain by the inhibition of p38 MAP kinase.
• PHARMACEUTICAL COMPOSITIONS FOR TREATMENT OF RESPIRATORY AND GASTROINTESTINAL DISORDERS
  申请人：Jung Birgit

  公开号：US20100099651A1

  公开（公告）日：2010-04-22

  The present invention relates to novel pharmaceutical compositions comprising at least one EGFR kinase inhibitor and at least one additional active compound selected from beta-2 mimetics, steroids, PDE-IV inhibitors, p38 MAP kinase inhibitors, NK 1 antagonists, anticholinergics and endothelin antagonists, processes for preparing the compositions and the use thereof as medicament in the treatment of respiratory or gastrointestinal complaints, as well as inflammatory diseases of the joints, the skin or the eyes.
• US7244441B2
  申请人：——

  公开号：US7244441B2

  公开（公告）日：2007-07-17
• US7268139B2
  申请人：——

  公开号：US7268139B2

  公开（公告）日：2007-09-11