(2S,3R,4R,5R,6R)-4-azido-2-[(2S,3R,4R,5R,6R)-4-azido-3,5-dihydroxy-6-(hydroxymethyl)oxan-2-yl]sulfanyl-6-(hydroxymethyl)oxane-3,5-diol

• 分子结构分类: 有机化合物 - 有机氧化合物
• 英文名称: (2S,3R,4R,5R,6R)-4-azido-2-[(2S,3R,4R,5R,6R)-4-azido-3,5-dihydroxy-6-(hydroxymethyl)oxan-2-yl]sulfanyl-6-(hydroxymethyl)oxane-3,5-diol
• 化学式: C12H20N6O8S
• 分子量: 408.39
• InChiKey: AZZIBGKZSLGNAF-NCFXGAEVSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -0.3
• 重原子数：
  27
• 可旋转键数：
  6
• 环数：
  2.0
• sp3杂化的碳原子比例：
  1.0
• 拓扑面积：
  194
• 氢给体数：
  6
• 氢受体数：
  13

文献信息

• Novel Galactoside Inhibitor of Galectins
  申请人：Galecto Biotech AB

  公开号：US20140121179A1

  公开（公告）日：2014-05-01

  The present invention relates to a compound of the general formula (I): The compound of formula (I) is suitable for treating pulmonary fibrosis, such as Idiopathic pulmonary fibrosis in a mammal. Furthermore the present invention concerns a method of monitoring development or progression of pulmonary fibrosis in a human subject, a method of monitoring or predicting exacerbation of symptoms in a human subject with pulmonary fibrosis as well as a method for treatment of pulmonary fibrosis, such as Idiopathic pulmonary fibrosis in a human subject having a galectin-3 level indicative of pulmonary fibrosis or exacerbation of symptoms.

  本发明涉及一种通式（I）的化合物：化合物（I）适用于治疗哺乳动物的肺纤维化，例如特发性肺纤维化。此外，本发明涉及一种监测人体主体肺纤维化发展或进展的方法，一种监测或预测肺纤维化患者症状恶化的方法，以及一种治疗肺纤维化的方法，例如对于具有提示肺纤维化或症状恶化的galectin-3水平的人类主体的特发性肺纤维化。
• Novel galactoside inhibitor of galectins
  申请人：GALECTO BIOTECH AB

  公开号：US20160096861A1

  公开（公告）日：2016-04-07

  Provided is a compound of the general formula (I): The compound of formula (I) is suitable for treating pulmonary fibrosis, such as Idiopathic pulmonary fibrosis in a mammal. Also provided is a method for treatment of pulmonary fibrosis, such as Idiopathic pulmonary fibrosis in a human subject having a galectin-3 level indicative of pulmonary fibrosis or exacerbation of symptoms as well as a method for making said compound.

  提供的是通式（I）的化合物：公式（I）的化合物适用于治疗哺乳动物的肺纤维化，如特发性肺纤维化。还提供了一种治疗肺纤维化的方法，例如对于人类患有表明肺纤维化或症状加剧的半乳糖凝集素-3水平的特发性肺纤维化患者，以及制备该化合物的方法。
• NOVEL SYNTHESIS OF GALACTOSIDE INHIBITORS
  申请人：Nilsson Ulf

  公开号：US20110130553A1

  公开（公告）日：2011-06-02

  Novel synthesis routes for preparation of thiodigalactosides and intermediates are presented. The method includes the use of a 3-azido-galactosyl thiouronium salt derivative, which is activated to the corresponding thiol in situ, which in turn is directly reacted with a 3-azido-galactosyl bromide resulting in the 3,3′-di-azido-thio-di-galactoside before the thiol has a chance to reduce the azido 10 group. Hence, in situ formation of the 3-azido-galactosyl thiol from the thiouronium salt is essential in the synthesis procedure, because any other method that generate the thiol separately results in extensive unwanted azide reduction.

  提出了用于制备硫代半乳糖苷和中间体的新型合成路线。该方法包括使用3-偶氮基-半乳糖基硫脲盐衍生物，该衍生物在原位激活为相应的巯基，然后直接与3-偶氮基-半乳糖基溴反应，形成3,3'-二偶氮基硫代二半乳糖苷，此时巯基还没有机会还原偶氮基。因此，在合成过程中原位形成3-偶氮基-半乳糖基巯基是必要的，因为任何其他单独生成巯基的方法都会导致大量不需要的偶氮基还原。
• Galactoside Inhibitor of Galectin-3 and its use for Treating Pulmonary Fibrosis
  申请人：GALECTO BIOTECH AB

  公开号：US20150274764A1

  公开（公告）日：2015-10-01

  The present invention relates to a compound of the general formula (I) for pulmonary administration. The compound of formula (I) is suitable for treating pulmonary fibrosis, such as Idiopathic pulmonary fibrosis in a mammal. Furthermore the present invention concerns a method for treatment of pulmonary fibrosis, such as Idiopathic pulmonary fibrosis in a human subject.

  本发明涉及一种适用于肺部给药的通式(I)化合物。通式(I)的化合物适用于治疗哺乳动物的肺纤维化，例如特发性肺纤维化。此外，本发明还涉及一种用于治疗肺纤维化的方法，例如用于治疗人体主体的特发性肺纤维化。
• DIAGNOSING PULMONARY FIBROSIS
  申请人：Galecto Biotech AB

  公开号：EP3278805A1

  公开（公告）日：2018-02-07

  The present invention relates to a method of diagnosing pulmonary fibrosis in a human subject comprising a) measuring a galectin-3 level in a body sample from the human subject using a suitable test method, b) comparing the galectin-3 level to a predetermined reference level, and c) determining whether the galectin-3 level is indicative of diagnosing the subject with pulmonary fibrosis.

  本发明涉及一种诊断人体肺纤维化的方法，包括 a) 使用合适的测试方法测量人体样本中的 galectin-3 水平；b) 将 galectin-3 水平与预定参考水平进行比较；以及 c) 确定 galectin-3 水平是否表明诊断对象患有肺纤维化。