2-((2R,3R,4R,5S)-3,4,5-trihydroxy-2-(hydroxymethyl)piperidin-1-yl)ethyl (5Z,8Z,11Z,14Z,17Z)-icosa-5,8,11,14,17-pentaenoate

• 分子结构分类: 有机化合物 - 脂质和类脂质分子 - 脂肪酰基
• 英文名称: 2-((2R,3R,4R,5S)-3,4,5-trihydroxy-2-(hydroxymethyl)piperidin-1-yl)ethyl (5Z,8Z,11Z,14Z,17Z)-icosa-5,8,11,14,17-pentaenoate
• 英文别名: 3-[(2R,3R,4R,5S)-3,4,5-trihydroxy-2-(hydroxymethyl)piperidin-1-yl]propyl (5Z,8Z,11Z,14Z,17Z)-icosa-5,8,11,14,17-pentaenoate
• 化学式: C₂₉H₄₇NO₆
• 分子量: 505.695
• InChiKey: LRFXUAUZQGGNLH-HKPLTUPWSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.2
• 重原子数：
  36
• 可旋转键数：
  19
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.62
• 拓扑面积：
  111
• 氢给体数：
  4
• 氢受体数：
  7

反应信息

• 作为产物：
  描述：

  1-脱氧野尻霉素 在 potassium carbonate 作用下， 以 N,N-二甲基甲酰胺 为溶剂， 反应 17.5h， 生成 2-((2R,3R,4R,5S)-3,4,5-trihydroxy-2-(hydroxymethyl)piperidin-1-yl)ethyl (5Z,8Z,11Z,14Z,17Z)-icosa-5,8,11,14,17-pentaenoate
  参考文献：
  名称：

  高血糖の治療のための組成物及び方法

  摘要：

  This invention relates to compounds of formula I or their pharmaceutically acceptable salts, as well as polymorphs, solvates, enantiomers, diastereoisomers, stereoisomers, and hydrates thereof. Compounds of formula 1 and pharmaceutical compositions comprising an effective amount for the treatment of hyperglycemia can be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, intravenous, non-oral administration, syrup form, or for injection. Such compositions can be used for the treatment of insulin resistance, diabetes, diabetes insipidus, type 1 diabetes, microvascular complications of type 2 diabetes, macrovascular complications, lipid disorders, prediabetes, obesity, arrhythmias, myocardial infarction, stroke, neuropathy, kidney complications, high triglyceride levels, cardiovascular complications, and postprandial hyperglycemia.【Selected drawing】None

  公开号：

  JP2016510306A

文献信息

• Compositions and methods for the treatment of hyperglycemia
  申请人：Kandula Mahesh

  公开号：US09150557B1

  公开（公告）日：2015-10-06

  The invention relates to the compounds of formula I or its pharmaceutical acceptable salts, as well as polymorphs, solvates, enantiomers, stereoisomers and hydrates thereof. The pharmaceutical compositions comprising an effective amount of compounds of formula I, and methods for the treatment of hyperglycemia may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, intravenous, parenteral administration, syrup, or injection. Such compositions may be used to treatment of insulin resistance, diabetes mellitus, diabetes insipidus, type 1 diabetes, type 2 diabetes, microvascular complications, macrovascular complications, lipid disorders, prediabetes, obesity, arrhythmia, myocardial infarction, stroke, neuropathy, renal complications, hypertriglyceridemia, cardiovascular complications, and post prandial hyperglycemia.

  该发明涉及公式I的化合物或其药用可接受的盐，以及其多晶型、溶剂合物、对映体、立体异构体和水合物。包括有效量的公式I化合物的药物组合物，以及治疗高血糖的方法可以制成口服、颊内、直肠、局部、经皮、经粘膜、静脉、肠道、糖浆或注射剂。这些组合物可以用于治疗胰岛素抵抗、糖尿病、尿崩症、1型糖尿病、2型糖尿病、微血管并发症、大血管并发症、脂质紊乱、糖尿病前期、肥胖、心律失常、心肌梗死、中风、神经病变、肾脏并发症、高三酰甘油血症、心血管并发症和餐后高血糖。
• US9150557B1
  申请人：——

  公开号：US9150557B1

  公开（公告）日：2015-10-06