1-(2-Deoxy-2-fluoro-beta-D-arabinofuranosyl)uracil

• 分子结构分类: 有机化合物 - 核苷、核苷酸和类似物 - 嘧啶核苷
• 英文名称: 1-(2-Deoxy-2-fluoro-beta-D-arabinofuranosyl)uracil
• 英文别名: 1-[3-fluoro-4-hydroxy-5-(hydroxymethyl)oxolan-2-yl]pyrimidine-2,4-dione
• 化学式: C₉H₁₁FN₂O₅
• 分子量: 246.19
• InChiKey: UIYWFOZZIZEEKJ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -1
• 重原子数：
  17
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.56
• 拓扑面积：
  99.1
• 氢给体数：
  3
• 氢受体数：
  6

文献信息

• [EN] POLYNUCLEOTIDE CONSTRUCTS HAVING DISULFIDE GROUPS<br/>[FR] CONSTRUCTIONS POLYNUCLÉOTIDIQUES CONTENANT DES GROUPES DISULFURE
  申请人：SOLSTICE BIOLOG LTD

  公开号：WO2015069932A1

  公开（公告）日：2015-05-14

  The invention features polynucleotide constructs containing one or more components (i) containing a disulfide linkage, where each of the one or more components is attached to an internudeotide bridging group or a terminal group of the polynucleotide construct, and each of the one or more components (i) contains one or more bulky groups proximal to the disulfide group. The invention also features polynucleotide constructs containing one or more components (i) containing a disulfide linkage, where each of the one or more components (i) is attached to an internudeotide bridging group or a terminal group of the polynucleotide construct, and each of the one or more components (i) contains at least 4 atoms in a chain between the disulfide linkage and the phosphorus atom of the internudeotide bridging group or the terminal group; and where the chain does not contain a phosphate, an amide, an ester, or an alkenylene. The invention also features methods of delivering a polynucleotide to a cell using the polynucleotide constructs of the invention.

  该发明涉及包含一个或多个组分（i）的聚核苷酸构造，其中每个一个或多个组分连接到聚核苷酸构造的一个核苷酸桥连基团或末端基团上，每个一个或多个组分（i）包含靠近二硫键的一个或多个臃肿基团。该发明还涉及包含一个或多个组分（i）的聚核苷酸构造，其中每个一个或多个组分（i）连接到聚核苷酸构造的一个核苷酸桥连基团或末端基团上，每个一个或多个组分（i）在二硫键和核苷酸桥连基团或末端基团的磷原子之间的链中至少包含4个原子；并且该链不包含磷酸酯、酰胺、酯或烯基烃。该发明还涉及使用该发明的聚核苷酸构造将聚核苷酸传递到细胞的方法。
• [EN] 4'-ALLENE-SUBSTITUTED NUCLEOSIDE DERIVATIVES<br/>[FR] DÉRIVÉS DE NUCLÉOSIDES 4'-ALLÈNE-SUBSTITUÉS
  申请人：ENANTA PHARM INC

  公开号：WO2010030858A1

  公开（公告）日：2010-03-18

  The present invention discloses compounds of formula (I), or its β-L enantiomer, or a pharmaceutically acceptable salt, ester, stereoisomer, tautomer, solvate, prodrug, or combination thereof: Formula (I) which inhibit, preventing or treating abnormal cellular proliferation and/or a viral infection, particularly by HIV, HCV or HBV. Consequently, the compounds of the present invention interfere with the replication cycle of a virus and are also useful as antiviral agents, or interfere with host cellular biochemical process and are also useful as antiproliferative agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from viral infection and/or cell proliferation. The invention also relates to methods of treating a viral infection and/or cell proliferation in a subject by administering a pharmaceutical composition comprising the compounds of the present invention. The present invention relates to novel antiviral/anti-proliferative compounds represented herein above, pharmaceutical compositions comprising such compounds, and methods for the treatment or prophylaxis of viral infection in a subject in need of such therapy with said compounds.

  本发明揭示了化合物的结构式（I），或其β-L对映体，或药学上可接受的盐、酯、立体异构体、互变异构体、溶剂合物、前药或其组合物：结构式（I），其能够抑制、预防或治疗异常细胞增殖和/或病毒感染，特别是HIV、HCV或HBV。因此，本发明的化合物干扰病毒的复制周期，并且也可作为抗病毒剂使用，或干扰宿主细胞的生化过程，也可作为抗增殖剂使用。本发明还涉及包含上述化合物的药物组合物，用于治疗患有病毒感染和/或细胞增殖的受试者。该发明还涉及通过给患有病毒感染和/或细胞增殖的受试者使用包含本发明化合物的药物组合物来治疗病毒感染和/或细胞增殖的方法。本发明涉及上述新型抗病毒/抗增殖化合物，包括这些化合物的药物组合物和治疗或预防需要此类化疗的受试者的病毒感染的方法。
• [EN] 2',4'-SUBSTITUTED NUCLEOSIDES AS ANTIVIRAL AGENTS<br/>[FR] NUCLÉOSIDES SUBSTITUÉS EN POSITION 2',4' EN TANT QU'AGENTS ANTIVIRAUX
  申请人：PHARMASSET INC

  公开号：WO2009067409A1

  公开（公告）日：2009-05-28

  Embodiments of the invention are to compounds of formulae (A), (A'), methods, and compositions for use in the treatment of viral infections. More specifically embodiments of the invention aur 2 ', 4 ' -substituted nucleoside compounds useful for the treatment of viral infections, such as HIV, HCV, and HBV infections.

  本发明的实施例涉及公式（A）、（A'）的化合物，方法和组合物，用于治疗病毒感染。更具体地，本发明的实施例为用于治疗病毒感染，如HIV、HCV和HBV感染的2'，4'-取代核苷化合物。
• OLIGONUCLEOTIDE WITH PROTECTED BASE
  申请人：Ajinomoto Co., Inc.

  公开号：US20150080565A1

  公开（公告）日：2015-03-19

  The present invention provides a protected nucleotide for elongation, which can be purified efficiently and in a high yield by a liquid-liquid extraction operation, and can achieve an oligonucleotide production method by a phosphoramidite method. It has been found that the above-mentioned problem can be solved by a particular oligonucleotide comprising a protected base and/or particular oligonucleotide protected by a branched chain-containing aromatic group at 3′-position.

  本发明提供了一种用于延伸的保护核苷酸，可以通过液液萃取操作高效率、高产量地纯化，并可通过磷酰胺酰胺法实现寡核苷酸的生产方法。发现通过在3'-位置含有支链含芳香基团的特定寡核苷酸和/或特定寡核苷酸保护基，可以解决上述问题。
• 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

表征谱图