2'-Deoxy-2'-Fluoro-2'-Methyluridine 5'-(Trihydrogen Diphosphate) | 1015073-44-5

• 分子结构分类: 有机化合物 - 有机氧化合物 - 有机含氧阴离子化合物
• 英文名称: 2'-Deoxy-2'-Fluoro-2'-Methyluridine 5'-(Trihydrogen Diphosphate)
• 英文别名: [(2R,3R,4R,5R)-5-(2,4-dioxopyrimidin-1-yl)-4-fluoro-3-hydroxy-4-methyloxolan-2-yl]methyl phosphono hydrogen phosphate
• CAS: 1015073-44-5
• 化学式: C₁₀H₁₅FN₂O₁₁P₂
• 分子量: 420.182
• InChiKey: VPPLCOBQDZAMRD-VPCXQMTMSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -3.8
• 重原子数：
  26
• 可旋转键数：
  6
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.6
• 拓扑面积：
  192
• 氢给体数：
  5
• 氢受体数：
  12

文献信息

• METHODS FOR TREATING HEPATITIS C VIRUS INFECTION
  申请人：Gilead Pharmasset LLC

  公开号：US20140249101A1

  公开（公告）日：2014-09-04

  Disclosed herein is a method of treating a subject infected with hepatitis C virus, said method comprising administering to the subject for a time period an effective amount of sofosbuvir, an effective amount of ribavirin and an effective amount of ledipasvir. In one aspect, the method comprises administering to the subject an interferon-free treatment regimen comprising an effective amount of sofosbuvir, an effective amount of ribavirin and an effective amount of ledipasvir. In a particular aspect, the method is sufficient to produce an undetectable amount of HCV RNA in the subject for at least 12 weeks after the end of the time period.
• METHODS OF PREVENTING AND TREATING RECURRENCE OF A HEPATITIS C VIRUS INFECTION IN A SUBJECT AFTER THE SUBJECT HAS RECEIVED A LIVER TRANSPLANT
  申请人：Gilead Pharmasset LLC

  公开号：US20140357595A1

  公开（公告）日：2014-12-04

  This application describes methods of preventing, treating or reducing the risk of recurrence of a hepatitis C virus infection in a subject after the subject has received a liver transplant. Disclosed herein are methods of preventing or reducing the risk of recurrence of a hepatitis C virus infection in a subject after the subject has received a liver transplant, the methods comprising administering to the subject an effective amount of Compound 1. Also disclosed are methods of reducing HCV RNA levels to about 25 IU/mL or lower in a subject having received a liver transplant comprising administering to the subject an effective amount of Compound 1.
• METHODS OF TREATING HEPATITIS C VIRUS INFECTION IN SUBJECTS WITH CIRRHOSIS
  申请人：Gilead Pharmasset LLC

  公开号：US20150150897A1

  公开（公告）日：2015-06-04

  Methods of treating hepatitis C virus infection in a subject with cirrhosis comprising administering to the subject an effective amount of Compound 1.
• Phosphoramidate nucleoside prodrug for treating viral diseases and cancer, processes for their preparation and their use
  申请人：Ivachtchenko Alexandre Vasilievich

  公开号：US20180030080A1

  公开（公告）日：2018-02-01

  The present invention pertains to chemotherapeutic agents and their use for treating viral and cancerous diseases. These compounds are inhibitors of HCV NS5B polymerase, HBV DNA polymerase and, HIV-1 reverse transcriptase (RT) inhibitor, and for treatment of hepatitis B and C infection in mammals. These compounds are also of interest for the treatment of cancer. The phosphoramidate nucleoside prodrug of the general formula 1, a stereoisomer, isotope-enriched analogue, pharmaceutically acceptable salt, hydrate, solvate, or crystalline or polymorphic form thereof, wherein: Ar is aryl or hetaryl; R 1 is H or CH 3 ; R 2 is the substituent selected from OCH 2 CH═CH 2 , OCH 2 CH≡CH, OCH 2 CH 2 CH 2 OCH 3 , R 3 is H or CH 3 ; R 4 is OH, OR 5 , NR 6 R 7 ; R 5 is C 1 -C 4 -alkyl; R 6 and R 7 are not necessarily the same substituents selected from H or CH 3 ; Z═O, or NH; an arrow (→) indicates the place of substituent connection; Nuc is R 8 and R 9 are not necessarily the same substituents selected from H, F, Cl, CH 3 or OH provided when continuous line and its accompanying dotted line ( ) together are the single carbon-carbon (C—C) bond or R 8 and R 9 are hydrogen provided when continuous line and its accompanying dotted line ( ) together are the double carbon-carbon bond (C═C); R 10 is the substituent selected from R 10.1 -R 10.5 ; R 11 is the substituent selected from H, F, Cl, CH 3 , or CF 3 ; R 12 is hydrogen, C 1 -C 4 -alkyl or C 3 -C 6 -cycloalkyl; X is oxygen or ethanediyl-1,1 (C═CH 2 ); Y is O, S, CH 2 , or HO—CH group provided when continuous line and its accompanying dotted line ( ) together are the single carbon-carbon (C—C) bond or Y is CH group provided when continuous line and its accompanying dotted line ( ) together are the double carbon-carbon bond (C═C), and compound of the general formula 1, stereoisomers, isotope-enriched analogues, pharmaceutically acceptable salts, hydrates, solvates, or crystalline or polymorphic forms thereof, wherein: Ar is aryl or hetaryl; R 1 is H or CH 3 ; R is isopropyl; Nuc is
• [EN] METHODS FOR TREATING HEPATITIS C VIRUS<br/>[FR] MÉTHODES DE TRAITEMENT DU VIRUS DE L'HÉPATITE C
  申请人：GILEAD PHARMASSET LLC

  公开号：WO2014137929A1

  公开（公告）日：2014-09-12

  Disclosed herein is a method of treating a subject infected with hepatitis C virus, said method comprising administering to the subject for a time period an effective amount of sofosbuvir, an effective amount of ribavirin and an effective amount of ledipasvir. In one aspect, the method comprises administering to the subject an interferon-free treatment regimen comprising an effective amount of sofosbuvir, an effective amount of ribavirin and an effective amount of ledipasvir. In a particular aspect, the method is sufficient to produce an undetectable amount of HCV RNA in the subject for at least 12 weeks after the end of the time period.