6-fluoro-1,4-imino-1,4,6-trideoxy-D-mannitol

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡咯烷类
• 英文名称: 6-fluoro-1,4-imino-1,4,6-trideoxy-D-mannitol
• 英文别名: (2S,3S,4R)-2-((S)-2-Fluoro-1-hydroxyethyl)pyrrolidine-3,4-diol；(2S,3S,4R)-2-[(1S)-2-fluoro-1-hydroxyethyl]pyrrolidine-3,4-diol
• 化学式: C₆H₁₂FNO₃
• 分子量: 165.165
• InChiKey: VOSUCXBUAJAOTO-KVTDHHQDSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -1.3
• 重原子数：
  11
• 可旋转键数：
  2
• 环数：
  1.0
• sp3杂化的碳原子比例：
  1.0
• 拓扑面积：
  72.7
• 氢给体数：
  4
• 氢受体数：
  5

反应信息

• 作为产物：
  描述：

  6-fluoro-1,4-imino-2,3-O-isopropylidene-1,4,6-trideoxy-D-mannitol 以 水 、 三氟乙酸 为溶剂， 生成 6-fluoro-1,4-imino-1,4,6-trideoxy-D-mannitol
  参考文献：
  名称：

  Derivatives of 1,4-dideoxy-1,4-imino-D-mannitol and a process for their

  摘要：

  本发明揭示了从4,5-脱水-1-偶氮-1-脱氧-2,3-O-异丙基亚甲基-D-他利醇或其三氟甲磺酸盐衍生物合成的1,4-脱氧-1,4-亚胺-D-甘露醇的新衍生物及其合成方法。这些新的衍生物包括6-氟-1,4-亚胺-1,4,6-脱氧-D-甘露醇以及N-正丁基和N-苄基衍生物的1,4-脱氧-1,4-氨基-D-甘露醇，具有有用的甘露糖苷酶抑制活性。

  公开号：

  US04996329A1

文献信息

• Derivatives of 1,4-dideoxy-1,4-imino-d-mannitol
  申请人：MONSANTO COMPANY

  公开号：EP0424350A1

  公开（公告）日：1991-04-24

  Novel derivatives of 1,4-dideoxy-1,4-­imino-D-mannitol and method for their synthesis from 4,5-anhydro-1-azido-1-deoxy-2,3-O-isopropylidene-­D-talitol or its triflate derivative are disclosed. The novel derivatives, 6-fluoro-1,3-imino-1,4,6-­trideoxy-D-mannitol and the N-butyl and N-benzyl derivatives of 1,4-dideoxy-1,4-imino-D-mannitol, have useful mannosidase inhibitory activity.

  本发明公开了 1,4-二脱氧-1,4-亚氨基-D-甘露糖醇的新型衍生物，以及从 4,5-脱水-1-叠氮-1-脱氧-2,3-O-异亚丙基-D-甘露糖醇或其三酯衍生物合成它们的方法。新型衍生物 6-氟-1,3-亚氨基-1,4,6-三脱氧-D-甘露醇和 1,4-二脱氧-1,4-亚氨基-D-甘露醇的 N-丁基和 N-苄基衍生物具有有效的甘露糖苷酶抑制活性。
• Dose escalation enzyme replacement therapy for treating acid sphingomyelinase deficiency
  申请人：Icahn School of Medicine at Mount Sinai

  公开号：US10188705B2

  公开（公告）日：2019-01-29

  The invention relates to dose escalation enzyme replacement therapy using acid sphingomyelinase (ASM) for the treatment of human subjects having acid sphingomyelinase deficiency (ASMD), and, in particular, patients with non-neurological manifestations of Niemann-Pick Disease (NPD), and in certain embodiments, NPD type B.

  本发明涉及使用酸性鞘磷脂酶（ASM）的剂量递增酶替代疗法，用于治疗患有酸性鞘磷脂酶缺乏症（ASMD）的人类受试者，特别是患有非神经系统表现的尼曼-皮克病（NPD）患者，在某些实施例中，还包括NPD B型患者。
• High mannose proteins and methods of making high mannose proteins
  申请人：Shire Human Genetic Therapies, Inc.

  公开号：EP2292256B1

  公开（公告）日：2018-08-01
• DOSE ESCALATION ENZYME REPLACEMENT THERAPY FOR TREATING ACID SPHINGOMYELINASE DEFICIENCY
  申请人：Icahn School of Medicine at Mount Sinai

  公开号：EP2470199B1

  公开（公告）日：2019-05-22
• DOSE ESCALATION ENZYME REPLACEMENT THERAPY FOR TREATING ACID SPHINOGMYELINASE DEFICIENCY
  申请人：Mount Sinai School of Medicine of New York Unive

  公开号：US20130078230A1

  公开（公告）日：2013-03-28

  The invention relates to dose escalation enzyme replacement therapy using acid sphingomyelinase (ASM) for the treatment of human subjects having acid sphingomyelinase deficiency (ASMD), and, in particular, patients with non-neurological manifestations of Niemann-Pick Disease (NPD), and in certain embodiments, NPD type B.