4-Isopropoxy-2-methyl-1,1-dioxo-1,2-dihydro-1λ⁶-benzo[e][1,2]thiazine-3-carboxylic acid pyridin-2-ylamide | 118854-49-2

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯并噻嗪类
• 英文名称: 4-Isopropoxy-2-methyl-1,1-dioxo-1,2-dihydro-1λ⁶-benzo[e][1,2]thiazine-3-carboxylic acid pyridin-2-ylamide
• 英文别名: 4-Isopropoxy-2-methyl-N-(2-pyridinyl)-2H-1,2-benzothiazine-3-carboxamide 1,1-Dioxide；2-methyl-1,1-dioxo-4-propan-2-yloxy-N-pyridin-2-yl-1λ6,2-benzothiazine-3-carboxamide
• CAS: 118854-49-2
• 化学式: C₁₈H₁₉N₃O₄S
• 分子量: 373.433
• InChiKey: QVXLLXYBMYQMMD-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.6
• 重原子数：
  26
• 可旋转键数：
  4
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.22
• 拓扑面积：
  97
• 氢给体数：
  1
• 氢受体数：
  6

反应信息

• 作为产物：
  描述：

  2-碘代丙烷 、 吡罗昔康 在 potassium carbonate 作用下， 以 丙酮 为溶剂， 反应 96.0h， 以63%的产率得到4-Isopropoxy-2-methyl-1,1-dioxo-1,2-dihydro-1λ⁶-benzo[e][1,2]thiazine-3-carboxylic acid pyridin-2-ylamide
  参考文献：
  名称：

  Hammen, Philip D.; Berke, Helen; Bordner, Jon, Journal of Heterocyclic Chemistry, 1989, vol. 26, p. 11 - 16

  摘要：

  DOI：

文献信息

• USE OF PRODRUGS TO AVOID GI MEDIATED ADVERSE EVENTS
  申请人：Franklin Richard

  公开号：US20120202756A1

  公开（公告）日：2012-08-09

  The present invention relates to prodrugs of a wide variety of drugs and pharmaceutical compositions containing such prodrugs. Methods for minimizing locally mediated (from within the gut lumen) adverse gastrointestinal events associated with the underivatised drug and increasing the sustainment of plasma drug levels with the aforementioned prodrugs are also provided. Thus, the present invention relates to the use of prodrugs of a wide diversity of drugs (other than opioids) to transiently inactivate them and so reduce directly, locally mediated adverse gastrointestinal (GI) side-effects normally evident after administration of the parent compound. Additionally, such prodrugs may confer improved pharmacokinetics.

  本发明涉及各种药物的前药和含有这些前药的制药组合物。还提供了一种方法，用于最小化与未衍生药物相关的局部介导（来自肠腔内）不良胃肠事件，并使用上述前药增加血浆药物水平的持续性。因此，本发明涉及使用各种药物（除阿片类药物外）的前药，以短暂地使它们失活，从而减少通常在给予原始化合物后出现的直接、局部介导的不良胃肠（GI）副作用。此外，这些前药可能提供改善的药代动力学。
• [EN] USE OF PRODRUGS TO AVOID GI MEDIATED ADVERSE EVENTS<br/>[FR] UTILISATION DE PROMÉDICAMENTS POUR ÉVITER LES ÉVÉNEMENTS INDÉSIRABLES À MÉDIATION GI
  申请人：SHIRE LLC

  公开号：WO2012046062A1

  公开（公告）日：2012-04-12

  The present invention relates to prodrugs of a wide variety of drugs and pharmaceutical compositions containing such prodrugs. Methods for minimizing locally mediated (from within the gut lumen) adverse gastrointestinal events associated with the underivatised drug and increasing the sustainment of plasma drug levels with the aforementioned prodrugs are also provided. Thus, the present invention relates to the use of prodrugs of a wide diversity of drugs (other than opioids) to transiently inactivate them and so reduce directly, locally mediated adverse gastrointestinal (GI) side–effects normally evident after administration of the parent compound. Additionally, such prodrugs may confer improved pharmacokinetics.
• Hammen, Philip D.; Berke, Helen; Bordner, Jon, Journal of Heterocyclic Chemistry, 1989, vol. 26, p. 11 - 16
  作者：Hammen, Philip D.、Berke, Helen、Bordner, Jon、Braisted, Andrew C.、Lombardino, Joseph G.、Whipple, Earl B.

  DOI：——

  日期：——

表征谱图