N-(2-Chlorophenyl)imidazo[1,5-a]quinoxalin-4-amine

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二氮杂萘
• 英文名称: N-(2-Chlorophenyl)imidazo[1,5-a]quinoxalin-4-amine
• 化学式: C₁₆H₁₁ClN₄
• 分子量: 294.743
• InChiKey: AZAJFUFPLNAVHO-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.7
• 重原子数：
  21
• 可旋转键数：
  2
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  42.2
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为产物：
  描述：

  咪唑并[1,5-a]喹喔啉-4(5H)-酮 在 三氯氧磷 作用下， 生成 N-(2-Chlorophenyl)imidazo[1,5-a]quinoxalin-4-amine
  参考文献：
  名称：

  Discovery and initial SAR of imidazoquinoxalines as inhibitors of the Src-family kinase p56Lck

  摘要：

  We have identified a novel series of 1,5-imidizoquinoxalines as inhibitors of Lck with excellent potency (IC(50)s less than or equal to 5 nM) as well as good cellular activity against T-cell proliferation (IC(50)s < 1 muM). Structure-activity studies demonstrate the requirement for the core heterocycle in addition to an optimal 2.6-disubstituted aniline group. (C) 2002 Published by Elsevier Science Ltd.

  DOI：

  10.1016/s0960-894x(02)00191-9

文献信息

• US6235740B1
  申请人：——

  公开号：US6235740B1

  公开（公告）日：2001-05-22
• [EN] IMIDAZOQUINOXALINE PROTEIN TYROSINE KINASE INHIBITORS<br/>[FR] INHIBITEURS A BASE D'IMIDAZOQUINOXALINES DE LA PROTEINE TYROSINE KINASE
  申请人：BRISTOL-MYERS SQUIBB COMPANY

  公开号：WO1999009845A1

  公开（公告）日：1999-03-04

  (EN) Novel imidazoquinoxalines and salts thereof, pharmaceutical compositions containing such compounds, and methods of using such compounds in the treatment of protein tyrosine kinase-associated disorders such as immunologic disorders.(FR) La présente invention concerne de nouvelles imidazoquinoxalines et des sels de celles-ci, des compositions pharmaceutiques contenant ces composés et des procédés d'utilisation de ces composés dans le traitement de troubles associés à la protéine tyrosine kinase, tels que des troubles immunologiques.
• Discovery and initial SAR of imidazoquinoxalines as inhibitors of the Src-family kinase p56Lck
  作者：Ping Chen、Derek Norris、Edwin J. Iwanowicz、Steven H. Spergel、James Lin、Henry H. Gu、Zhongqi Shen、John Wityak、Tai-An Lin、Suhong Pang、Henry F. De Fex、Sidney Pitt、Ding Ren Shen、Arthur M. Doweyko、Donna A. Bassolino、Jacques Y. Roberge、Michael A. Poss、Bang-Chi Chen、Gary L. Schieven、Joel C. Barrish

  DOI：10.1016/s0960-894x(02)00191-9

  日期：2002.5

  We have identified a novel series of 1,5-imidizoquinoxalines as inhibitors of Lck with excellent potency (IC(50)s less than or equal to 5 nM) as well as good cellular activity against T-cell proliferation (IC(50)s < 1 muM). Structure-activity studies demonstrate the requirement for the core heterocycle in addition to an optimal 2.6-disubstituted aniline group. (C) 2002 Published by Elsevier Science Ltd.