6-(2,4-difluorophenoxy)-2-(trans-4-hydroxy-cyclohexylamino)-8-methyl-8H-pyrido[2,3-d]pyrimidin-7-one | 791580-19-3

• 分子结构分类: 有机化合物 - 有机氧化合物
• 英文名称: 6-(2,4-difluorophenoxy)-2-(trans-4-hydroxy-cyclohexylamino)-8-methyl-8H-pyrido[2,3-d]pyrimidin-7-one
• CAS: 791580-19-3
• 化学式: C₂₀H₂₀F₂N₄O₃
• 分子量: 402.401
• InChiKey: QXBFECQVSFWIBC-HDJSIYSDSA-N

反应信息

• 作为反应物：
  描述：

  6-(2,4-difluorophenoxy)-2-(trans-4-hydroxy-cyclohexylamino)-8-methyl-8H-pyrido[2,3-d]pyrimidin-7-one 在 盐酸 作用下， 以 甲醇 、 乙醚 为溶剂， 以1.6 g的产率得到6-(2,4-difluorophenoxy)-2-(trans-4-hydroxy-cyclohexylamino)-8-methyl-8H-pyrido[2,3-d]pyrimidin-7-one hydrochloride
  参考文献：
  名称：

  Discovery of 6-(2,4-Difluorophenoxy)-2-[3-hydroxy-1-(2-hydroxyethyl)propylamino]-8-methyl-8H-pyrido[2,3-d]pyrimidin-7-one (Pamapimod) and 6-(2,4-Difluorophenoxy)-8-methyl-2-(tetrahydro-2H-pyran-4-ylamino)pyrido[2,3-d]pyrimidin-7(8H)-one (R1487) as Orally Bioavailable and Highly Selective Inhibitors of p38α Mitogen-Activated Protein Kinase

  摘要：

  The development of a new series of p38 alpha inhibitors resulted in the identification of two clinical candidates, one of which was advanced into a phase 2 clinical study for rheumatoid arthritis. The original lead, an lck inhibitor that also potently inhibited p38a, was a screening hit from our kinase inhibitor library. This manuscript describes the optimization of the lead to p38-selective examples with good pharmacokinetic properties.

  DOI：

  10.1021/jm101423y

文献信息

• 6-Substituted pyrido-pyrimidines
  申请人：Chen Jeffrey Jian

  公开号：US20070135458A1

  公开（公告）日：2007-06-14

  The present invention provides compounds of the Formula I and II: wherein R 1 , R 3 , W, Z, X 1 , X 2 , Ar 1 , R 8 and R 9 are as defined herein, and methods and intermediates for their preparation and uses thereof.

  本发明提供了公式I和II的化合物：其中R1、R3、W、Z、X1、X2、Ar1、R8和R9如本文所定义，以及它们的制备方法和中间体以及它们的用途。
• US7169794B2
  申请人：——

  公开号：US7169794B2

  公开（公告）日：2007-01-30
• US7449581B2
  申请人：——

  公开号：US7449581B2

  公开（公告）日：2008-11-11