[(2R,3S,4R,5R)-5-(6-aminopurin-9-yl)-3,4-dihydroxyoxolan-2-yl]methyl dihydrogen phosphate;[(2R,3S,4R,5R)-5-(2,4-dioxopyrimidin-1-yl)-3,4-dihydroxyoxolan-2-yl]methyl dihydrogen phosphate

• 分子结构分类: 有机化合物 - 核苷、核苷酸和类似物 - 嘧啶核苷酸
• 英文名称: [(2R,3S,4R,5R)-5-(6-aminopurin-9-yl)-3,4-dihydroxyoxolan-2-yl]methyl dihydrogen phosphate;[(2R,3S,4R,5R)-5-(2,4-dioxopyrimidin-1-yl)-3,4-dihydroxyoxolan-2-yl]methyl dihydrogen phosphate
• 化学式: C19H27N7O16P2
• 分子量: 671.4
• InChiKey: VGQHQOKIMNKUEF-ZLOOHWKQSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -4.6
• 重原子数：
  44
• 可旋转键数：
  8
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.53
• 拓扑面积：
  352
• 氢给体数：
  10
• 氢受体数：
  20

文献信息

• A DELIVERY SYSTEM FOR TARGETED DELIVERY OF A THERAPEUTICALLY ACTIVE PAYLOAD
  申请人：Technische Universität Dresden

  公开号：EP3315139A1

  公开（公告）日：2018-05-02

  The present invention provides the modular design and assembly of novel targeting bio-conjugates, exclusively assembled by means of biotin-biotin binding element conjugation, comprising mono-biotinylated cell binding component, a tetrameric biotin-binding element, and mono-biotinylated payload for therapeutic and diagnostic purposes. In addition, there is provided a method of delivering the payload, such as therapeutic oligonucleotides, via mono-biotinylated targeting devices, such as antibodies or ligands, into eukaryotic cells by means of receptor-mediated endocytosis. The targeting bio-conjugates are suitable for use in the areas of medicine, pharmacy and biomedical research.

  本发明提供了新型靶向生物轭合物的模块化设计和组装，这些轭合物专门通过生物素-生物素结合元件共轭的方式组装，包括单生物素化细胞结合元件、四聚体生物素结合元件和用于治疗和诊断目的的单生物素化有效载荷。此外，还提供了一种通过单生物素化的靶向装置（如抗体或配体），通过受体介导的内吞作用将有效载荷（如治疗性寡核苷酸）送入真核细胞的方法。这种靶向生物共轭物适用于医学、药学和生物医学研究领域。
• Eimeria vaccine with improved efficacy
  申请人：Intervet Inc.

  公开号：US10758601B2

  公开（公告）日：2020-09-01

  The present invention relates to the fields of veterinary parasitology and -vaccinology; more specifically the invention relates to a composition comprising live Eimeria oocysts and a pharmaceutically acceptable carrier. The composition is characterised in that it comprises a TLR3 agonist. The composition can be used to prepare a vaccine for poultry against Coccidiosis. The vaccine can be applied for example as a coarse spray on day-old chicks. The TLR3 agonist in the vaccine allows for a reduction of the dose of Eimeria oocysts up to 4 fold, while obtaining the same level of protection against challenge as from a vaccine without the TLR3 agonist. Alternatively, when employing a conventional dose of Eimeria oocysts in the vaccine, the TLR3 agonist causes an earlier onset of immunity, resulting in a significant reduction of the intestinal lesion score upon challenge, already at 2 instead of at 3 weeks after vaccination.

  本发明涉及兽医寄生虫学和疫苗学领域；更具体地说，本发明涉及一种由活艾美拉虫卵囊和药学上可接受的载体组成的组合物。该组合物的特征在于它包含一种 TLR3 激动剂。该组合物可用于制备家禽球虫病疫苗。例如，该疫苗可作为粗喷雾剂喷洒在雏鸡身上。疫苗中的 TLR3 激动剂可使卵囊艾美耳蚴的剂量减少 4 倍，同时获得与不含 TLR3 激动剂的疫苗相同的抗挑战保护水平。另外，如果在疫苗中使用常规剂量的艾美拉虫卵囊，TLR3 激动剂会使免疫开始得更早，从而使接种后 2 周而不是 3 周的肠道病变评分显著降低。
• Delivery system for targeted delivery of a therapeutically active payload
  申请人：TECHNISCHE UNIVERSITÄT DRESDEN

  公开号：US11504432B2

  公开（公告）日：2022-11-22

  The present invention provides the modular design and assembly of novel targeting bio-conjugates, exclusively assembled by means of biotin-biotin binding element conjugation, comprising mono-biotinylated cell binding component, a tetrameric biotin-binding element, and mono-biotinylated payload for therapeutic and diagnostic purposes. In addition, there is provided a method of delivering the payload, such as therapeutic oligonucleotides, via mono-biotinylated targeting devices, such as antibodies or ligands, into eukaryotic cells by means of receptor-mediated endocytosis. The targeting bio-conjugates are suitable for use in the areas of medicine, pharmacy and biomedical research.

  本发明提供了新型靶向生物轭合物的模块化设计和组装，这些轭合物专门通过生物素-生物素结合元件共轭的方式组装，包括单生物素化细胞结合元件、四聚体生物素结合元件和用于治疗和诊断目的的单生物素化有效载荷。此外，还提供了一种通过单生物素化的靶向装置（如抗体或配体），通过受体介导的内吞作用将有效载荷（如治疗性寡核苷酸）送入真核细胞的方法。这种靶向生物共轭物适用于医学、药学和生物医学研究领域。
• USE OF COMPOUNDS FOR THE TREATMENT OF PAIN
  申请人：Akron Molecules AG

  公开号：EP2846788A1

  公开（公告）日：2015-03-18
• EIMERIA VACCINE WITH IMPROVED EFFICACY
  申请人：Intervet International B.V.

  公开号：EP3558350A1

  公开（公告）日：2019-10-30