MR 121

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯并恶嗪类
• 英文名称: MR 121
• 英文别名: 1-(3-carboxypropyl)-11-ethyl-1,2,3,4,8,9,10,11-octahydrodipyrido[3,2-b:2',3'-i]phenoxazin-13-ium；4-(20-ethyl-2-oxa-20-aza-6,13-diazoniapentacyclo[12.8.0.03,12.05,10.016,21]docosa-1(14),3,5,10,12,15,21-heptaen-6-yl)butanoate
• 化学式: C₂₄H₂₈N₃O₃
• 分子量: 406.505
• InChiKey: PPHZUAWXHMGPCR-UHFFFAOYSA-O

计算性质

• 辛醇/水分配系数(LogP)：
  2.4
• 重原子数：
  30
• 可旋转键数：
  5
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.46
• 拓扑面积：
  65.1
• 氢给体数：
  1
• 氢受体数：
  5

反应信息

• 作为反应物：
  描述：

  L-赖氨酸 、 MR 121 在 N-羟基丁二酰亚胺 、 盐酸-N-乙基-Nˊ-(3-二甲氨基丙基)碳二亚胺 、 Carbonate buffer 作用下， 以 乙腈 为溶剂， 反应 12.0h， 生成
  参考文献：
  名称：

  Aggregation behavior of the red-absorbing oxazine derivative MR 121: A new method for determination of pure dimer spectra

  摘要：

  In this Letter, we investigated the dimerization behavior of the red-absorbing oxazine derivative MR 121. Thereby a new method to determine absorption spectra of pure non-fluorescent H-type dye dimers is presented. Therefore, the amino acid lysine is doubly labeled with the fluorescent dye in order to obtain an absorption spectrum mainly caused by dimers. By subtracting the fraction arising from monomeric dye, the dimer spectrum is generated. The extinction coefficient at absorption maximum (608 nm) was estimated to be 86000 +/- 2000 M-1 cm(-1) per dye. Furthermore, the equilibrium constant K-D for the dimerization reaction is determined to be 3300 +/- 300 M-1. (c) 2005 Elseiver B.V. All rights reserved.

  DOI：

  10.1016/j.cplett.2005.04.008

文献信息

• THIENOPYRIMIDINES HAVING MNK1/MNK2 INHIBITING ACTIVITY FOR PHARMACEUTICAL COMPOSITIONS
  申请人：Aicher Babette

  公开号：US20100056548A1

  公开（公告）日：2010-03-04

  The present invention relates to novel pharmaceutical compositions comprising thienopyrimidine compounds. Moreover, the present invention relates to the use of the thienopyrimidine compounds of the invention for the production of pharmaceutical compositions for the prophylaxis and/or treatment of diseases which can be influenced by the inhibition of the kinase activity of Mnk1 and/or Mnk2 (Mnk2a or Mnk2b) and/or variants thereof.

  本发明涉及包含噻唑嘧啶化合物的新型药物组合物。此外，本发明涉及使用本发明的噻唑嘧啶化合物制备预防和/或治疗可以受到Mnk1和/或Mnk2（Mnk2a或Mnk2b）及/或其变体的激酶活性抑制影响的疾病的药物组合物。
• THIENOPYRIMIDINES FOR PHARMACEUTICAL COMPOSITIONS
  申请人：Taylor Steven

  公开号：US20100143341A1

  公开（公告）日：2010-06-10

  The present invention relates to novel pharmaceutical compositions of general formula (I) comprising thienopyrimidine compounds. Moreover, the present invention relates to the use of the thienopyrimidine compounds of the invention for the production of pharmaceutical compositions for the prophylaxis and/or treatment of diseases which can be influenced by the inhibition of the kinase activity of Mnk1 and/or Mnk2 (Mnk2a or Mnk2b) and/or variants thereof.

  本发明涉及通式（I）的新型药物组合物，其包括噻唑嘧啶化合物。此外，本发明涉及使用本发明的噻唑嘧啶化合物生产药物组合物，用于预防和/或治疗可以通过抑制Mnk1和/或Mnk2（Mnk2a或Mnk2b）及/或其变体的激酶活性而受到影响的疾病。
• MNK1 or MNK2 Inhibitors
  申请人：Coulter Thomas Stephen

  公开号：US20090163520A1

  公开（公告）日：2009-06-25

  The present invention relates to the use of pyrazolopyrimidine compounds for the production of pharmaceutical compositions for the prophylaxis and/or treatment of diseases which can be influenced by the inhibition of the kinase activity of Mnk1 and/or Mnk2 (Mnk2a or Mnk2b) and/or variants thereof.

  本发明涉及使用吡唑并嘧啶化合物制备药物组合物，用于预防和/或治疗可以通过抑制Mnk1和/或Mnk2（Mnk2a或Mnk2b）激酶活性及/或其变体影响的疾病。
• PYRROLOPYRIMIDINES FOR PHARMACEUTICAL COMPOSITIONS
  申请人：Jäkel Stefan

  公开号：US20100105708A1

  公开（公告）日：2010-04-29

  The present invention relates to novel pyrrolopyrimidine compounds of the general formula (1) and pharmaceutical compositions comprising said pyrrolopyrimidine compounds. Moreover, the present invention relates to the use of the pyrrolopyrimidine compounds of the invention for the production of pharmaceutical compositions for the prophylaxis and/or treatment of diseases which can be influenced by the inhibition of the kinase activity of Mnk1 and/or Mnk2 (Mnk2a or Mnk2b) and/or variants thereof.
• US8633201B2
  申请人：——

  公开号：US8633201B2

  公开（公告）日：2014-01-21