2-aminopentanedioic acid bis-methylamide | 1417404-45-5

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 羧酸及其衍生物
• 英文名称: 2-aminopentanedioic acid bis-methylamide
• 英文别名: (2S)-2-amino-N,N'-dimethylpentanediamide
• CAS: 1417404-45-5
• 化学式: C₇H₁₅N₃O₂
• 分子量: 173.215
• InChiKey: TZSRAYKNIRAOHN-YFKPBYRVSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -1.7
• 重原子数：
  12
• 可旋转键数：
  4
• 环数：
  0.0
• sp3杂化的碳原子比例：
  0.71
• 拓扑面积：
  84.2
• 氢给体数：
  3
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  2-aminopentanedioic acid bis-methylamide 、 以 四氢呋喃 为溶剂， 生成 (2S)-2-[[13-(2,4-difluoroanilino)-2-oxotricyclo[9.4.0.03,8]pentadeca-1(11),3(8),4,6,12,14-hexaene-5-carbonyl]amino]-N,N'-dimethylpentanediamide
  参考文献：
  名称：

  Dibenzosuberones as p38 Mitogen-Activated Protein Kinase Inhibitors with Low ATP Competitiveness and Outstanding Whole Blood Activity

  摘要：

  p38 alpha mitogen-activated protein (MAP) kinase is a main target in drug research concerning inflammatory diseases. Nevertheless, no inhibitor of p38 alpha MAP kinase has been introduced to the market. This might be attributed to the fact that there is no inhibitor which combines outstanding activity in biological systems and selectivity. Herein an approach to the development of such inhibitors on the basis of the highly selective molecular probe Skepinone-L is described. Introduction of a "deep pocket" moiety addressing the DFG motif led to an increased activity of the compounds. Hydrophilic moieties, addressing the solvent-exposed area adjacent to hydrophilic region II, conserved a high activity of the compounds in a whole blood assay. Combined with their outstanding selectivity and low ATP competitiveness, these inhibitors are very interesting candidates for use in biological systems and in therapy.

  DOI：

  10.1021/jm301539x

文献信息

• [EN] POLYETHYLENE GLYCOL-CONJUGATED GLUCOCORTICOID PRODRUGS AND COMPOSITIONS AND METHODS THEREOF<br/>[FR] PROMÉDICAMENTS GLUCOCORTICOÏDES CONJUGUÉS À DU POLYÉTHYLÈNE GLYCOL ET COMPOSITIONS ET MÉTHODES ASSOCIÉES
  申请人：UNIV NEBRASKA

  公开号：WO2017083794A1

  公开（公告）日：2017-05-18

  Polyethylene glycol (PEG)-conjugated glucocorticoid prodrugs, methods of preparation, and use for the treatment of diseases and disorders are disclosed. In particular, PEG-conjugated dexamethasone compounds and methods of using them for treating inflammatory and autoimmune diseases, including but not limited to lupus, are disclosed.

  本文揭示了聚乙二醇（PEG）共轭的糖皮质激素前药、制备方法以及用于治疗疾病和障碍的用途。具体来说，揭示了PEG共轭的地塞米松化合物以及使用它们治疗炎症和自身免疫疾病的方法，包括但不限于狼疮。
• Polyethylene glycol-conjugated glucocorticoid prodrugs and compositions and methods thereof
  申请人：Board of Regents of the University of Nebraska

  公开号：US10485809B2

  公开（公告）日：2019-11-26

  Polyethylene glycol (PEG)-conjugated glucocorticoid prodrugs, methods of preparation, and use for the treatment of diseases and disorders are disclosed. In particular, PEG-conjugated dexamethasone compounds and methods of using them for treating inflammatory and autoimmune diseases, including but not limited to lupus, are disclosed.

  本发明公开了聚乙二醇（PEG）共轭糖皮质激素原药、制备方法以及治疗疾病和失调的用途。特别是公开了 PEG 结合的地塞米松化合物及其用于治疗炎症和自身免疫性疾病（包括但不限于狼疮）的方法。
• POLYETHYLENE GLYCOL-CONJUGATED GLUCOCORTICOID PRODRUGS AND COMPOSITIONS AND METHODS THEREOF
  申请人：Board of Regents of the University of Nebraska

  公开号：EP3374369B1

  公开（公告）日：2020-03-18
• US7205332B2
  申请人：——

  公开号：US7205332B2

  公开（公告）日：2007-04-17
• US8906844B2
  申请人：——

  公开号：US8906844B2

  公开（公告）日：2014-12-09