2'-O-methylcytidine-5'-[bis(isopropyloxycarbonyloxymethyl)]phosphate | 444019-29-8

• 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: 2'-O-methylcytidine-5'-[bis(isopropyloxycarbonyloxymethyl)]phosphate
• 英文别名: [[(2R,3R,4R,5R)-5-(4-amino-2-oxopyrimidin-1-yl)-3-hydroxy-4-methoxyoxolan-2-yl]methoxy-(propan-2-yloxycarbonyloxymethoxy)phosphoryl]oxymethyl propan-2-yl carbonate
• CAS: 444019-29-8
• 化学式: C₂₀H₃₂N₃O₁₄P
• 分子量: 569.46
• InChiKey: ZDLIHDRWVMLVGK-MWQQHZPXSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.6
• 重原子数：
  38
• 可旋转键数：
  17
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.7
• 拓扑面积：
  213
• 氢给体数：
  2
• 氢受体数：
  14

反应信息

• 作为产物：
  描述：

  氯甲基碳酸异丙酯 、 2′-O-methylcytidine-5′-phosphate 在 四磷十氧化物 、 N,N-二异丙基乙胺 作用下， 以 N,N-二甲基甲酰胺 为溶剂， 反应 49.0h， 以2.5 mg的产率得到2'-O-methylcytidine-5'-[bis(isopropyloxycarbonyloxymethyl)]phosphate
  参考文献：
  名称：

  NUCLEOSIDE DERIVATIVES AS INHIBITORS OF RNA-DEPENDENT RNA VIRAL POLYERMASE

  摘要：

  本发明提供了核苷类化合物及其某些衍生物，这些化合物是RNA依赖性RNA病毒聚合酶的抑制剂。这些化合物是RNA依赖性RNA病毒复制的抑制剂，对于治疗RNA依赖性RNA病毒感染非常有用。它们特别适用于作为乙型肝炎病毒（HCV）NS5B聚合酶的抑制剂，作为HCV复制的抑制剂，和/或用于治疗丙型肝炎感染。该发明还描述了含有这种核苷类化合物的药物组合物，单独使用或与其他针对RNA依赖性RNA病毒感染，特别是HCV感染的药物一起使用。还公开了使用本发明的核苷类化合物抑制RNA依赖性RNA聚合酶、抑制RNA依赖性RNA病毒复制和/或治疗RNA依赖性RNA病毒感染的方法。

  公开号：

  US20170183373A1

文献信息

• Nucleoside derivatives as inhibitors of RNA-dependent RNA viral polymerase
  申请人：——

  公开号：US20020147160A1

  公开（公告）日：2002-10-10

  The present invention provides nucleoside compounds and certain derivatives thereof which are inhibitors of RNA-dependent RNA viral polymerase. These compounds are inhibitors of RNA-dependent RNA viral replication and are useful for the treatment of RNA-dependent RNA viral infection. They are particularly useful as inhibitors of hepatitis C virus (HCV) NS5B polymerase, as inhibitors of HCV replication, and/or for the treatment of hepatitis C infection. The invention also describes pharmaceutical compositions containing such nucleoside compounds alone or in combination with other agents active against RNA-dependent RNA viral infection, in particular HCV infection. Also disclosed are methods of inhibiting RNA-dependent RNA polymerase, inhibiting RNA-dependent RNA viral replication, and/or treating RNA-dependent RNA viral infection with the nucleoside compounds of the present invention.

  本发明提供了核苷化合物及其某些衍生物，这些衍生物是RNA依赖性RNA病毒聚合酶的抑制剂。这些化合物是RNA依赖性RNA病毒复制的抑制剂，可用于治疗RNA依赖性RNA病毒感染。它们特别适用于作为丙型肝炎病毒（HCV）NS5B聚合酶的抑制剂，作为HCV复制的抑制剂，以及/或用于治疗丙型肝炎感染。本发明还描述了包含这种核苷化合物的药物组合物，单独使用或与其他对RNA依赖性RNA病毒感染，特别是HCV感染有效的制剂组合使用。还公开了使用本发明的核苷化合物抑制RNA依赖性RNA聚合酶、抑制RNA依赖性RNA病毒复制和/或治疗RNA依赖性RNA病毒感染的方法。
• Nucleoside derivatives as inhibitors of rna-dependent rna viral polymerase
  申请人：——

  公开号：US20040110717A1

  公开（公告）日：2004-06-10

  The present invention provides nucleoside derivatives which are inhibitors of RNA-dependent RNA viral polymerase. These compounds are inhibitors of RNA-dependent RNA viral replication and are useful for the treatment of RNA-dependent RNA viral infection. They are particularly useful as inhibitors of hepatitis C virus (HCV) NS5B polymerase, as inhibitors of HCV replication, and/or for the treatment of hepatitis C infection. The invention also describes pharmaceutical compositions containing such nucleoside derivatives alone or in combination with other agents active against RNA-dependent RNA viral infection, in particular HCV infection. Also disclosed are methods of inhibiting RNA-dependent RNA polymerase, inhibiting RNA-dependent RNA viral replication, and/or treating RNA-dependent RNA viral infection with the nucleoside derivatives of the present invention.

  本发明提供了一种核苷酸衍生物，其是RNA依赖性RNA病毒聚合酶的抑制剂。这些化合物是RNA依赖性RNA病毒复制的抑制剂，可用于治疗RNA依赖性RNA病毒感染。它们特别适用于作为丙型肝炎病毒（HCV）NS5B聚合酶的抑制剂，作为HCV复制的抑制剂，和/或用于治疗丙型肝炎感染。该发明还描述了含有这种核苷酸衍生物的制药组合物，单独或与其他对RNA依赖性RNA病毒感染活性的制剂结合使用，特别是HCV感染。还揭示了使用本发明的核苷酸衍生物抑制RNA依赖性RNA聚合酶、抑制RNA依赖性RNA病毒复制和/或治疗RNA依赖性RNA病毒感染的方法。
• Nucleoside derivatives as inhibitors of rna-dependent RNA viral polymerase
  申请人：Bhat Balkrishen

  公开号：US20070275912A1

  公开（公告）日：2007-11-29

  The present invention provides nucleoside compounds and certain derivatives thereof which are inhibitors of RNA-dependent RNA viral polymerase. These compounds are inhibitors of RNA-dependent RNA viral replication and are useful for the treatment of RNA-dependent RNA viral infection. They are particularly useful as inhibitors of hepatitis C virus (HCV) NS5B polymerase, as inhibitors of HCV replication, and/or for the treatment of hepatitis C infection. The invention also describes pharmaceutical compositions containing such nucleoside compounds alone or in combination with other agents active against RNA-dependent RNA viral infection, in particular HCV infection. Also disclosed are methods of inhibiting RNA-dependent RNA polymerase, inhibiting RNA-dependent RNA viral replication, and/or treating RNA-dependent RNA viral infection with the nucleoside compounds of the present invention.

  本发明提供了一种核苷类化合物及其某些衍生物，它们是RNA依赖性RNA病毒聚合酶的抑制剂。这些化合物是RNA依赖性RNA病毒复制的抑制剂，可用于治疗RNA依赖性RNA病毒感染。它们特别适用于作为丙型肝炎病毒（HCV）NS5B聚合酶的抑制剂，作为HCV复制的抑制剂，和/或用于治疗丙型肝炎感染。本发明还描述了单独或与其他对RNA依赖性RNA病毒感染活性的药物组合使用的核苷类化合物的制药组合物，特别是用于HCV感染。还公开了使用本发明的核苷类化合物抑制RNA依赖性RNA聚合酶，抑制RNA依赖性RNA病毒复制，和/或治疗RNA依赖性RNA病毒感染的方法。
• NUCLEOSIDE DERIVATIVES AS INHIBITORS OF RNA-DEPENDENT RNA VIRAL POLYMERASE
  申请人：Bhat Balkrishen

  公开号：US20140309412A1

  公开（公告）日：2014-10-16

  The present invention provides nucleoside compounds and certain derivatives thereof which are inhibitors of RNA-dependent RNA viral polymerase. These compounds are inhibitors of RNA-dependent RNA viral replication and are useful for the treatment of RNA-dependent RNA viral infection. They are particularly useful as inhibitors of hepatitis C virus (HCV) NS5B polymerase, as inhibitors of HCV replication, and/or for the treatment of hepatitis C infection. The invention also describes pharmaceutical compositions containing such nucleoside compounds alone or in combination with other agents active against RNA-dependent RNA viral infection, in particular HCV infection. Also disclosed are methods of inhibiting RNA-dependent RNA polymerase, inhibiting RNA-dependent RNA viral replication, and/or treating RNA-dependent RNA viral infection with the nucleoside compounds of the present invention.

  本发明提供了核苷酸化合物及其某些衍生物，它们是RNA依赖性RNA病毒聚合酶的抑制剂。这些化合物是RNA依赖性RNA病毒复制的抑制剂，并且对于RNA依赖性RNA病毒感染的治疗非常有用。它们特别适用于作为丙型肝炎病毒（HCV）NS5B聚合酶的抑制剂，作为HCV复制的抑制剂和/或用于丙型肝炎感染的治疗。本发明还描述了单独或与其他针对RNA依赖性RNA病毒感染，特别是HCV感染的药物组合中含有这种核苷酸化合物的制药组合物。还揭示了使用本发明的核苷酸化合物抑制RNA依赖性RNA聚合酶，抑制RNA依赖性RNA病毒复制和/或治疗RNA依赖性RNA病毒感染的方法。
• US6777395B2
  申请人：——

  公开号：US6777395B2

  公开（公告）日：2004-08-17