1-[5-Azido-4-hydroxy-5-(hydroxymethyl)-3-methyloxolan-2-yl]pyrimidine-2,4-dione

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二嗪类
• 英文名称: 1-[5-Azido-4-hydroxy-5-(hydroxymethyl)-3-methyloxolan-2-yl]pyrimidine-2,4-dione
• 英文别名: 1-[5-azido-4-hydroxy-5-(hydroxymethyl)-3-methyloxolan-2-yl]pyrimidine-2,4-dione
• 化学式: C10H13N5O5
• 分子量: 283.24
• InChiKey: QFYAWFKDVAAWTO-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -0.1
• 重原子数：
  20
• 可旋转键数：
  3
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.6
• 拓扑面积：
  114
• 氢给体数：
  3
• 氢受体数：
  7

文献信息

• Phosphoramidate Derivatives of Nucleosides
  申请人：Jonckers Tim Hugo Maria

  公开号：US20120225839A1

  公开（公告）日：2012-09-06

  Compounds of formula I: including any possible stereoisomers thereof, wherein: R 1 is hydrogen, —C(═O)R 6 or —C(═O)CHR 7 —NH 2 ; R 2 is hydrogen; or C 1 -C 6 alkyl or phenyl, either of which is optionally substituted with 1, 2 or 3 substituents each independently selected from halo, C 1 -C 6 alkyl, C 2 -C 6 -alkenyl and C 1 -C 6 alkoxy, hydroxy or amino, or R 2 is naphtyl; or R 2 is indolyl, R 3 is hydrogen, C 1 -C 6 alkyl, benzyl; R 4 is hydrogen, C 1 -C 6 alkyl, benzyl; or R 3 and R 4 together with the carbon atom to which they are attached form C 3 -C 7 cycloalkyl; R 5 is C 1 -C 10 alkyl, C 3 -C 7 -cycloalkyl, benzyl, or phenyl, any of which being optionally substituted with 1, 2 or 3 substituents each independently selected from hydroxy, C 1 -C 6 alkoxy, amino, mono- and diC 1 -C 6 alkylamino; R 6 is C 1 -C 6 alkyl; R 7 is C 1 -C 6 alkyl; R 8 is hydrogen or halogen; or a pharmaceutically acceptable salt or solvate thereof are useful in the prophylaxis or treatment of HCV infections.

  化学式为I的化合物：包括其所有可能的立体异构体，其中：R1是氢，-C（═O）R6或-C（═O）CHR7-NH2; R2是氢；或C1-C6烷基或苯基，其中任意一个可以选择地被1、2或3个取代基取代，每个取代基独立地选择自卤素、C1-C6烷基、C2-C6烯基和C1-C6烷氧基、羟基或氨基，或R2是萘基；或R2是吲哚基，R3是氢、C1-C6烷基、苄基；R4是氢、C1-C6烷基、苄基；或R3和R4与它们所连接的碳原子共同形成C3-C7环烷基；R5是C1-C10烷基、C3-C7环烷基、苄基或苯基，其中任意一个都可以选择地被1、2或3个取代基取代，每个取代基独立地选择自羟基、C1-C6烷氧基、氨基、单和双C1-C6烷基氨基；R6是C1-C6烷基；R7是C1-C6烷基；R8是氢或卤素；或其药学上可接受的盐或溶剂，可用于预防或治疗HCV感染。
• PHOSPHORAMIDATE DERIVATIVES OF NUCLEOSIDES
  申请人：Janssen Products, L.P.

  公开号：EP2483288A2

  公开（公告）日：2012-08-08
• 2',4'-substituted nucleosides as antiviral agents
  申请人：Gilead Pharmasset LLC

  公开号：EP2631239B1

  公开（公告）日：2015-01-07
• 2',4'-SUBSTITUTED NUCLEOSIDES AS ANTIVIRAL AGENTS
  申请人：SOFIA MICHAEL JOSEPH

  公开号：US20120232029A1

  公开（公告）日：2012-09-13

  Embodiments of the invention are to compounds, methods, and compositions for use in the treatment of viral infections. More specifically embodiments of the invention are 2′,4′-substituted nucleoside compounds useful for the treatment of viral infections, such as HIV, HCV, and HBV infections.
• US8552021B2
  申请人：——

  公开号：US8552021B2

  公开（公告）日：2013-10-08