(3E,10R,13S)-3-(2-aminoethoxyimino)-10,13-dimethyl-1,2,4,5,7,8,9,11,12,14,15,16-dodecahydrocyclopenta[a]phenanthrene-6,17-dione

• 分子结构分类: 有机化合物 - 脂质和类脂质分子 - 类固醇和类固醇衍生物
• 英文名称: (3E,10R,13S)-3-(2-aminoethoxyimino)-10,13-dimethyl-1,2,4,5,7,8,9,11,12,14,15,16-dodecahydrocyclopenta[a]phenanthrene-6,17-dione
• 化学式: C₂₁H₃₂N₂O₃
• 分子量: 360.5
• InChiKey: MPYLDWFDPHRTEG-ALZRTVPMSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.5
• 重原子数：
  26
• 可旋转键数：
  3
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.86
• 拓扑面积：
  81.8
• 氢给体数：
  1
• 氢受体数：
  5

文献信息

• Istaroxime-containing intravenous formulation for the treatment of acute heart failure (AHF)
  申请人：Windtree Therapeutics, Inc.

  公开号：US11197869B2

  公开（公告）日：2021-12-14

  Compositions for intravenous infusion of istaroxime, or a metabolite of istaroxime, in human patients suffering from heart failure are disclosed. Likewise, methods for extended infusion of istaroxime or its metabolites in individuals with heart failure are disclosed. In particular, some methods disclosed herein include the infusion of istaroxime, or a metabolite thereof, for a period of time that is greater than six hours in order to improve cardiac relaxation without triggering arrhythmogenic events in an individual suffering from heart failure. Other methods include administration of istaroxime until certain plasma concentration thresholds of istaroxime metabolites are achieved. Also disclosed are istaroxime metabolites with selective SERCA2a activation.

  本研究公开了用于心力衰竭患者静脉注射伊斯塔肟或伊斯塔肟代谢物的组合物。同样，还公开了对心力衰竭患者延长输注伊斯塔肟或其代谢物的方法。特别是，本文公开的一些方法包括输注伊沙洛肟或其代谢物超过6小时，以改善心衰患者的心脏松弛而不引发心律失常事件。其他方法包括服用伊斯塔肟，直到达到伊斯塔肟代谢物的特定血浆浓度阈值。还公开了具有选择性 SERCA2a 激活作用的异他肟代谢物。
• ISTAROXIME-CONTAINING INTRAVENOUS FORMULATION FOR THE TREATMENT OF ACUTE HEART FAILURE (AHF)
  申请人：Windtree Therapeutics, Inc.

  公开号：US20210252017A1

  公开（公告）日：2021-08-19

  Compositions for intravenous infusion of istaroxime, or a metabolite of istaroxime, in human patients suffering from heart failure are disclosed. Likewise, methods for extended infusion of istaroxime or its metabolites in individuals with heart failure are disclosed. In particular, some methods disclosed herein include the infusion of istaroxime, or a metabolite thereof, for a period of time that is greater than six hours in order to improve cardiac relaxation without triggering arrhythmogenic events in an individual suffering from heart failure. Other methods include administration of istaroxime until certain plasma concentration thresholds of istaroxime metabolites are achieved. Also disclosed are istaroxime metabolites with selective SERCA2a activation.