(2R,3R,4R,5R,6R)-5-Acetamido-2-(acetoxymethyl)-6-hydroxytetrahydro-2H-pyran-3,4-diyl Diacetate

• 分子结构分类: 有机化合物 - 有机氧化合物
• 英文名称: (2R,3R,4R,5R,6R)-5-Acetamido-2-(acetoxymethyl)-6-hydroxytetrahydro-2H-pyran-3,4-diyl Diacetate
• 英文别名: (5-acetamido-3,4-diacetyloxy-6-hydroxyoxan-2-yl)methyl acetate
• 化学式: C₁₄H₂₁NO₉
• 分子量: 347.32
• InChiKey: HUQNDNAQVPCTFV-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -0.5
• 重原子数：
  24
• 可旋转键数：
  8
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.71
• 拓扑面积：
  138
• 氢给体数：
  2
• 氢受体数：
  9

文献信息

• SOLID SUPPORTS AND PHOSPHORAMIDITE BUILDING BLOCKS FOR OLIGONUCLEOTIDE CONJUGATES
  申请人：AM Chemicals LLC

  公开号：US20180016232A1

  公开（公告）日：2018-01-18

  Novel non-nucleoside solid supports and phosphoramidite building blocks for preparation of synthetic oligonucleotides containing at least one non-nucleosidic moiety conjugated to a ligand of practical interest and synthetic processes for making the same are disclosed. Furthermore, oligomeric compounds are prepared using said solid supports and phosphoramidite building blocks, preferably followed by removal of protecting groups to provide oligonucleotides conjugated to ligands of interest.

  揭示了用于制备含有至少一个非核苷酸基团与实用兴趣配体共轭的合成寡核苷酸的新型非核苷酸固相支持体和磷酰胺酸酯构建块，以及制备这些固相支持体和磷酰胺酸酯构建块的合成过程。此外，使用所述固相支持体和磷酰胺酸酯构建块制备寡聚合物化合物，最好是在去除保护基的情况下，以提供与感兴趣的配体共轭的寡核苷酸。
• [EN] TARGETED NUCLEIC ACID CONJUGATE COMPOSITIONS<br/>[FR] COMPOSITIONS DE CONJUGUÉS D'ACIDES NUCLÉIQUES CIBLÉS
  申请人：PROTIVA BIOTHERAPEUTICS INC

  公开号：WO2017177326A1

  公开（公告）日：2017-10-19

  The invention provides conjugates that comprise a targeting moiety, a nucleic acid, and optional linking groups as well as synthetic intermediates and synthetic methods useful for preparing the conjugates. The conjugates are useful to target therapeutic nucleic acids to the liver and to treat liver diseases including hepatitis (e.g. hepatitis B and hepatitis D).

  这项发明提供了包括靶向基团、核酸和可选连接基团的共轭物，以及用于制备这些共轭物的合成中间体和合成方法。这些共轭物可用于将治疗性核酸靶向肝脏，并用于治疗包括肝炎（如乙型肝炎和丙型肝炎）在内的肝脏疾病。
• BIFUNCTIONAL COMPOUND WITH MONOSACCHARIDE AND N2S2 LIGAND, AND PREPARATION AND USE THEREOF
  申请人：LIU SHOW-WEN

  公开号：US20120009669A1

  公开（公告）日：2012-01-12

  A bifunctional compound with a monosaccharide and a N 2 S 2 ligand, and more particularly, a bifunctional compound with a N 2 S 2 ligand and aminohexylacetyl galactosamine (ah-GalNAc 4 ) is provided. A method for preparing the bifunctional compound with a monosaccharide and a N 2 S 2 ligand is also provided, including activating a carboxyl group in an organic ligand, reacting the activated carboxyl group with a galactopyranoside through amidation, and then hydrolyzing. The bifunctional compound of the present invention is widely useful in nuclear medicine for preparation of liver imaging agents for assisting in correct diagnosis of diseases.

  提供了一种具有单糖和N2S2配体的双功能化合物，更具体地说，提供了一种具有N2S2配体和氨基己酰半乳糖胺（ah-GalNAc4）的双功能化合物。还提供了一种制备具有单糖和N2S2配体的双功能化合物的方法，包括激活有机配体中的羧基，通过酰胺化将激活的羧基与半乳糖苷反应，然后水解。本发明的双功能化合物在核医学中广泛用于制备肝脏成像剂，以帮助正确诊断疾病。
• PRECURSOR USED FOR LABELING HEPATORCYTE RECEPTOR AND CONTAINING TRISACCHARIDE AND DIAMIDE DEMERCAPTIDE LIGAND, METHOD FOR PREPARING THE SAME, RADIOTRACER AND PHARMACEUTICAL COMPOSITION OF THE SAME
  申请人：LIU SHOW-WEN

  公开号：US20140031533A1

  公开（公告）日：2014-01-30

  A precursor used for labeling hepatocyte receptors and applied to radiotracers for imaging or pharmaceutical compositions for liver cancers is revealed. The precursor is a bifunctional compound. The bifunctional group includes a trisaccharide structure and a diamide dimercaptide (N 2 S 2 ) ligand. The trisaccharide has high affinity to asialoglycoprotein receptors (ASGPR) on surfaces of hepatocytes while N 2 S 2 ligand reacts with radioisotopes to form neutral complexes. Thus the precursor stays on surfaces of hepatocytes to provide radioisotope labeling or treatment effect of liver cancers.

  一种用于标记肝细胞受体并应用于用于肝癌成像或药物组合物的放射示踪剂的前体被揭示。该前体是一种双功能化合物。双功能基团包括三糖结构和二酰胺二巯基（N2S2）配体。三糖具有高亲和力，能与肝细胞表面的非糖蛋白受体（ASGPR）结合，而N2S2配体与放射性同位素反应形成中性络合物。因此，前体停留在肝细胞表面，提供放射同位素标记或治疗肝癌的效果。
• COMPOSITIONS AND METHODS FOR MODULATING COMPLEMENT FACTOR B EXPRESSION
  申请人：Ionis Pharmaceuticals, Inc.

  公开号：EP3608406A1

  公开（公告）日：2020-02-12

  The present embodiments provide methods, compounds, and compositions for treating, preventing, or ameliorating a disease associated with dysregulation of the complement alternative pathway by administering a Complement Factor B (CFB) specific inhibitor to a subject.

  本发明的实施方案提供了通过向受试者施用补体因子B（CFB）特异性抑制剂来治疗、预防或改善与补体替代途径失调相关的疾病的方法、化合物和组合物。