(2R,3S,4S,5R)-2-(6-amino-2-fluoropurin-9-yl)-5-(hydroxymethyl)oxolane-3,4-diol;pentyl N-[1-[(2R,3R,4S,5R)-3,4-dihydroxy-5-methyloxolan-2-yl]-5-fluoro-2-oxopyrimidin-4-yl]carbamate

• 分子结构分类: 有机化合物 - 核苷、核苷酸和类似物 - 嘌呤核苷
• 英文名称: (2R,3S,4S,5R)-2-(6-amino-2-fluoropurin-9-yl)-5-(hydroxymethyl)oxolane-3,4-diol;pentyl N-[1-[(2R,3R,4S,5R)-3,4-dihydroxy-5-methyloxolan-2-yl]-5-fluoro-2-oxopyrimidin-4-yl]carbamate
• 化学式: C25H34F2N8O10
• 分子量: 644.6
• InChiKey: NQAUPTOLEDVCQA-JGSHWEPZSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -1.08
• 重原子数：
  45
• 可旋转键数：
  9
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.6
• 拓扑面积：
  260
• 氢给体数：
  7
• 氢受体数：
  16

文献信息

• [EN] PROCESS<br/>[FR] PROCÉDÉ
  申请人：PHOSPHAGENICS LTD

  公开号：WO2018112512A1

  公开（公告）日：2018-06-28

  An efficient and commercial phosphorylation process of a complex alcohol, such as secondary and tertiary alcohols, with P4O10 at high temperatures, and a product obtained by the process.

  一种高效商业化的磷酸酯化过程，用于复杂醇类（如二级和三级醇），在高温下使用P4O10，以及该过程得到的产品。
• Macromolecules
  申请人：STARPHARMA PTY LTD

  公开号：US10265409B2

  公开（公告）日：2019-04-23

  A macromolecule includes i) a dendrimer with a core and at least one generation of lysine residue building units, the outermost generation of building units having surface amino groups, ii) a first terminal group covalently attached to a first surface amino group of a building unit, which includes a residue of docetaxel (DTX), and iii) a second terminal group covalently attached to a second surface amino group of a building unit, which includes a pharmacokinetic modifying agent. The pharmacokinetic modifying agent can be a polyethylene glycol (PEG). The first terminal group can be covalently attached to the surface amino group of the dendrimer through a diacid linker. The diacid linker can include a 2,2′-thiodiacetic acid residue. The diacid linker can form an ester bond with a hydroxyl group of the DTX and an amide bond with the surface amino group. A pharmaceutically acceptable salt of the macromolecule can be prepared.

  一种大分子包括 i) 树枝状聚合物，具有核心和至少一代赖氨酸残基构建单元，最外层的构建单元具有表面氨基；ii) 与构建单元的第一表面氨基共价连接的第一末端基团，其中包括多西他赛（DTX）残基；iii) 与构建单元的第二表面氨基共价连接的第二末端基团，其中包括药代动力学修饰剂。药代动力学修饰剂可以是聚乙二醇（PEG）。第一末端基团可通过二酸连接剂共价连接到树枝状聚合物的表面氨基上。二酸连接体可包括 2,2′-硫代乙酸残基。二酸连接体可与 DTX 的羟基形成酯键，与表面氨基形成酰胺键。可以制备大分子的药学上可接受的盐。
• PROCESS
  申请人：Avecho Biotechnology Limited

  公开号：EP3558903A1

  公开（公告）日：2019-10-30
• MACROMOLECULES
  申请人：Owen David

  公开号：US20140171375A1

  公开（公告）日：2014-06-19

  The present invention relates to a macromolecule comprising a dendrimer having surface amino groups to which at least two different terminal groups are attached including a pharmaceutically active agent and a pharmacokinetic modifying agent, the pharmaceutically active agent comprising a hydroxyl group and being attached to the surface amino group of the dendrimer through a diacid linker. Pharmaceutical compositions comprising the macromolecules and methods of treatment using the macromolecules are also described.
• US9744246B2
  申请人：——

  公开号：US9744246B2

  公开（公告）日：2017-08-29