Hypoxanthine, 9-(2-deoxy-beta-D-erythro-pentofuranosyl)-

• 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: Hypoxanthine, 9-(2-deoxy-beta-D-erythro-pentofuranosyl)-
• 英文别名: 9-[4-hydroxy-5-(hydroxymethyl)oxolan-2-yl]-1H-purin-6-one
• 化学式: C₁₀H₁₂N₄O₄
• 分子量: 252.23
• InChiKey: VGONTNSXDCQUGY-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -1.7
• 重原子数：
  18
• 可旋转键数：
  2
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.5
• 拓扑面积：
  109
• 氢给体数：
  3
• 氢受体数：
  5

文献信息

• FUNCTIONALIZED 3-ALKYNYL PYRAZOLOPYRIMIDINE ANALOGUES AS UNIVERSAL BASES AND METHODS OF USE
  申请人：Vorobiev Alexei

  公开号：US20130261014A1

  公开（公告）日：2013-10-03

  3-alkynyl inosine analogs and their uses as universal bases are provided. The inosine analogues can be incorporated into nucleic acid primers and probes. They do not significantly destabilize nucleic acid duplexes. As a result, the novel nucleic acid primers and probes incorporating the inosine analogues can be used in a variety of methods. The analogs function unexpectedly well as universal bases. Not only do they stabilize duplexes substantially more than hypoxanthine opposite A, C, T, and G but they are also recognized in primers by polymerases, allowing efficient amplification.

  提供了3-炔基肌苷类似物及其作为通用碱基的用途。这些肌苷类似物可以被合并到核酸引物和探针中。它们不会显著破坏核酸双链。因此，包含这些肌苷类似物的新型核酸引物和探针可以用于各种方法。这些类似物意外地作为通用碱基发挥良好作用。它们不仅比嘌呤对A、C、T和G稳定双链更多，而且在引物中被聚合酶识别，从而实现高效扩增。
• Beta-L-2'-Deoxy-Nucleosides for the Treatment of Hepatitis B
  申请人：Gosselin Gilles

  公开号：US20080188440A1

  公开（公告）日：2008-08-07

  This invention is directed to a method for treating a host infected with hepatitis B comprising administering an effective amount of an anti-HBV biologically active 2′-deoxy-β-L-erythro-pentofuranonucleoside or a pharmaceutically acceptable salt or prodrug thereof, wherein the 2′-deoxy-β-L-erythro-pentofuranonucleoside has the formula: wherein R is selected from the group consisting of H, straight chained, branched or cyclic alkyl, CO-alkyl, CO-aryl, CO-alkoxyalkyl, CO-aryloxyalkyl, CO-substituted aryl, alkylsulfonyl, arylsulfonyl, aralkylsulfonyl, amino acid residue, mono, di, or triphosphate, or a phosphate derivative; and BASE is a purine or pyrimidine base which may be optionally substituted. The 2′-deoxy-β-L-erythro-pentofuranonucleoside or a pharmaceutically acceptable salt or prodrug thereof may be administered either alone or in combination with another 2′-deoxy-β-L-erythro-pentofuranonucleoside or in combination with another anti-hepatitis B agent.

  该发明涉及一种治疗乙型肝炎感染宿主的方法，包括给予有效量的抗HBV生物活性2'-去氧-β-L-核糖核苷或其药学上可接受的盐或前药，其中2'-去氧-β-L-核糖核苷的化学式为：其中R选自H、直链、支链或环烷基、CO-烷基、CO-芳基、CO-烷氧基烷基、CO-芳氧基烷基、CO-取代芳基、烷基磺酰基、芳基磺酰基、芳基烷基磺酰基、氨基酸残基、单、二或三磷酸盐或磷酸衍生物；BASE是一种可以选择性地取代的嘌呤或嘧啶碱基。2'-去氧-β-L-核糖核苷或其药学上可接受的盐或前药可以单独或与另一种2'-去氧-β-L-核糖核苷或与另一种抗乙型肝炎药物联合使用。
• beta-L-2'-Deoxy-Nucleosides for the Treatment of Hepatitis B
  申请人：Gosselin Gilles

  公开号：US20070087995A1

  公开（公告）日：2007-04-19

  This invention is directed to a method for treating a host infected with hepatitis B comprising administering an effective amount of an anti-HBV biologically active 2′-deoxy-β-L-erythro-pentofuranonucleoside or a pharmaceutically acceptable salt or prodrug thereof, wherein the 2′-deoxy-β-L-erythro-pentofuranonucleoside has the formula: wherein R is selected from the group consisting of H, straight chained, branched or cyclic alkyl, CO-alkyl, CO-aryl, CO-alkoxyalkyl, CO-aryloxyalkyl, CO-substituted aryl, alkylsulfonyl, arylsulfonyl, aralkylsulfonyl, amino acid residue, mono, di, or triphosphate, or a phosphate derivative; and BASE is a purine or pyrimidine base which may be optionally substituted. The 2′-deoxy-β-L-erythro-pentofuranonucleoside or a pharmaceutically acceptable salt or prodrug thereof may be administered either alone or in combination with another 2′-deoxy-β-L-erythro-pentofuranonucleoside or in combination with another anti-hepatitis B agent.

  本发明涉及一种治疗患有乙型肝炎的宿主的方法，包括给予有效量的抗HBV生物活性2'-脱氧-β-L-erythro-戊糖核苷或其药学上可接受的盐或前药，其中2'-脱氧-β-L-erythro-戊糖核苷的化学式为：其中R选自H，直链，支链或环烷基，CO-烷基，CO-芳基，CO-烷氧基烷基，CO-芳氧基烷基，CO-取代芳基，烷基磺酰基，芳基磺酰基，芳基烷基磺酰基，氨基酸残基，单磷酸、二磷酸或三磷酸，或磷酸衍生物；BASE是一种嘌呤或嘧啶碱基，可选择性地被取代。2'-脱氧-β-L-erythro-戊糖核苷或其药学上可接受的盐或前药可以单独或与另一种2'-脱氧-β-L-erythro-戊糖核苷或其他抗乙型肝炎药物联合使用。
• BETA-L-2'-DEOXY-NUCLEOSIDES FOR THE TREATMENT OF HEPATITIS B
  申请人：Gosselin Gilles

  公开号：US20120264707A1

  公开（公告）日：2012-10-18

  This invention is directed to a method for treating a host infected with hepatitis B comprising administering an effective amount of an anti-HBV biologically active 2′-deoxy-β-L-erythro-pentofuranonucleoside or a pharmaceutically acceptable salt or prodrug thereof, wherein the 2′-deoxy-β-L-erythro-pentofuranonucleoside has the formula: wherein R is selected from the group consisting of H, straight chained, branched or cyclic alkyl, CO-alkyl, CO-aryl, CO-alkoxyalkyl, CO-aryloxyalkyl, CO-substituted aryl, alkylsulfonyl, arylsulfonyl, aralkylsulfonyl, amino acid residue, mono, di, or triphosphate, or a phosphate derivative; and BASE is a purine or pyrimidine base which may be optionally substituted. The 2′-deoxy-β-L-erythro-pentofuranonucleoside or a pharmaceutically acceptable salt or prodrug thereof may be administered either alone or in combination with another 2′-deoxy-β-L-erythro-pentofuranonucleoside or in combination with another anti-hepatitis B agent.

  本发明涉及一种治疗乙型肝炎感染宿主的方法，包括给予有效量的抗乙肝病毒生物活性2'-脱氧-β-L-赤霉糖核苷或其药学上可接受的盐或前药，其中2'-脱氧-β-L-赤霉糖核苷的化学式为：其中R选自H，直链、支链或环烷基，CO-烷基，CO-芳基，CO-烷氧基烷基，CO-芳氧基烷基，CO-取代芳基，烷基磺酰基，芳基磺酰基，芳基烷基磺酰基，氨基酸残基，单、二或三磷酸盐或磷酸衍生物；BASE是一种嘌呤或嘧啶碱基，可以选择性地被取代。2'-脱氧-β-L-赤霉糖核苷或其药学上可接受的盐或前药可以单独或与另一种2'-脱氧-β-L-赤霉糖核苷或其他抗乙肝药物联合使用。
• Beta - L-2'-Deoxy-Nucleosides for the treatment of Hepatitis B
  申请人：Novartis AG

  公开号：EP1431304B1

  公开（公告）日：2014-12-03

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