N-[2-[2-[(2S,3S,4S,5S,6S)-3-acetamido-4,5-dihydroxy-6-(hydroxymethyl)oxan-2-yl]oxyethoxy]ethyl]-3-(4-methyl-2,5-dioxofuran-3-yl)propanamide

• 分子结构分类: 有机化合物 - 有机氧化合物
• 英文名称: N-[2-[2-[(2S,3S,4S,5S,6S)-3-acetamido-4,5-dihydroxy-6-(hydroxymethyl)oxan-2-yl]oxyethoxy]ethyl]-3-(4-methyl-2,5-dioxofuran-3-yl)propanamide
• 化学式: C₂₀H₃₀N₂O₁₁
• 分子量: 474.465
• InChiKey: RSILPKJOINTLOK-SVKXURNBSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -2.7
• 重原子数：
  33
• 可旋转键数：
  12
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.7
• 拓扑面积：
  190
• 氢给体数：
  5
• 氢受体数：
  11

反应信息

• 作为产物：
  描述：

  (aminoethoxy)ethoxy-2-(acetylamino)-2-deoxy-β-D-galactopyranoside 、 2,5-dihydro-4-methyl-2,5-dioxo-3-furanpropionyl chloride 在 吡啶 作用下， 以 二氯甲烷 为溶剂， 反应 1.5h， 生成 N-[2-[2-[(2S,3S,4S,5S,6S)-3-acetamido-4,5-dihydroxy-6-(hydroxymethyl)oxan-2-yl]oxyethoxy]ethyl]-3-(4-methyl-2,5-dioxofuran-3-yl)propanamide
  参考文献：
  名称：

  Peptide-based in vivo siRNA delivery system

  摘要：

  本发明涉及一种用于体内靶向RNA干扰（RNAi）多核苷酸递送到肝细胞的组合物。靶向RNAi多核苷酸与共靶向的蜜蜂毒素递送肽一起给予。递送肽提供膜穿透功能，以便将RNAi多核苷酸从细胞外移动到细胞内。可逆修饰提供递送肽的生理响应性。

  公开号：

  US09107957B2

文献信息

• Poly(vinyl ester) Polymers for In Vivo Nucleic Acid Delivery
  申请人：Wakefield Darren H.

  公开号：US20130121954A1

  公开（公告）日：2013-05-16

  The present invention is directed membrane active poly(vinyl ester) polymers and compositions for targeted delivery of RNA interference (RNAi) polynucleotides to cells in vivo. RNAi polynucleotides are conjugated to the poly(vinyl ester) polymers and the polymers are reversibly modified to enable in vivo targeted delivery. Membrane activity of the poly(vinyl ester) provides for movement of the RNAi polynucleotides from outside the cell to inside the cell. Reversible modification provides physiological responsiveness.

  本发明涉及膜活性聚乙烯酯聚合物和用于靶向递送RNA干扰（RNAi）多核苷酸至体内细胞的组合物。RNAi多核苷酸与聚乙烯酯聚合物结合，而聚合物可可逆地修饰以实现体内靶向递送。聚乙烯酯的膜活性可使RNAi多核苷酸从细胞外运动到细胞内。可逆修饰提供生理响应性。
• Peptide-Based In Vivo siRNA Delivery System
  申请人：Rozema David B.

  公开号：US20120165393A1

  公开（公告）日：2012-06-28

  The present invention is directed compositions for targeted delivery of RNA interference (RNAi) polynucleotides to hepatocytes in vivo. Targeted RNAi polynucleotides are administered together with co-targeted melittin delivery peptides. Delivery peptides provide membrane penetration function for movement of the RNAi polynucleotides from outside the cell to inside the cell. Reversible modification provides physiological responsiveness to the delivery peptides.

  本发明涉及用于体内靶向递送RNA干扰（RNAi）多核苷酸至肝细胞的组合物。靶向RNAi多核苷酸与共靶向的蜜蜂毒素递送肽一起给予。递送肽提供膜穿透功能，将RNAi多核苷酸从细胞外运动到细胞内。可逆修饰为递送肽提供生理响应性。
• Polyconjugates for In Vivo Delivery of Polynucleotides
  申请人：ROZEMA David B.

  公开号：US20120230938A1

  公开（公告）日：2012-09-13

  The present invention is directed to compounds, compositions, and methods useful for delivering polynucleotides or other cell-impermeable molecules to mammalian cells. Described are polyconjugates systems that incorporate targeting, anti-opsonization, anti-aggregation, and transfection activities into small biocompatible in vivo delivery vehicles. The use of multiple reversible or labile linkages connecting component parts provides for physiologically responsive activity modulation.

  本发明涉及化合物、组合物和方法，用于将多聚核苷酸或其他细胞不透过分子传递到哺乳动物细胞中。所述的聚合物共轭系统将定位、抗蛋白质吸附、抗聚集和转染活性结合到小型生物相容性体内递送载体中。使用多个可逆或不稳定的连接组件部分的连接提供了生理响应活性调节。
• Poly(acrylate) Polymers for In Vivo Nucleic Acid Delivery
  申请人：Arrowhead Madison Inc.

  公开号：US20150104408A1

  公开（公告）日：2015-04-16

  The present invention is directed membrane active poly(acrylate) polymers and compositions for targeted delivery of RNA interference (RNAi) polynucleotides cells in vivo. RNAi polynucleotides are conjugated to the poly(acrylate) polymers and the polymers are reversibly modified to enable in vivo targeted delivery. Membrane activity of the poly(acrylate) provides for movement of the RNAi polynucleotides from outside the cell to inside the cell. Reversible modification provides physiological responsiveness.
• RNAi Therapy for Hepatitis B Virus Infection
  申请人：Arrowhead Pharmaceuticals, Inc.

  公开号：US20170035796A1

  公开（公告）日：2017-02-09

  Described are compositions and methods for inhibition of Hepatitis B virus gene expression. RNA interference (RNAi) triggers and RNAi trigger conjugates for inhibiting the expression of Hepatitis B virus gene are described. Pharmaceutical compositions comprising one or more HBV RNAi triggers optionally with one or more additional therapeutics are also described. Delivery of the described HBV RNAi triggers to infected liver in vivo provides for inhibition of HBV gene expression and treatment.