floxuridine | 688007-28-5

• 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: floxuridine
• 英文别名: 5-fluoro-1-[(4S,5R)-4-hydroxy-5-(hydroxymethyl)oxolan-2-yl]pyrimidine-2,4-dione
• CAS: 688007-28-5
• 化学式: C₉H₁₁FN₂O₅
• 分子量: 246.195
• InChiKey: ODKNJVUHOIMIIZ-GFCOJPQKSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -1.2
• 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] DRUGS CONJUGATED WITH HEXOSE PHOSPHATE AND METHODS OF MAKING AND USING SAME<br/>[FR] MÉDICAMENTS CONJUGUÉS À DU PHOSPHATE D'HEXOSE ET LEURS PROCÉDÉS DE FABRICATION ET D'UTILISATION
  申请人：PARK JOO YOUN

  公开号：WO2022072425A1

  公开（公告）日：2022-04-07

  A drug conjugate, composition, and method for delivering active antimicrobials based on existing antibiotics through a hexose phosphate transporter (UhpT) by conjugating the antimicrobials with non-metabolizable hexose phosphates. Methods of co-administering antibiotics with non-metabolizable hexose phosphates as antimicrobials are also disclosed. Non-metabolizable hexose phosphates can constitutively and strongly induce expression of UhpT which significantly improves the efficacy and/or antimicrobial spectrum of antibiotics. This drug conjugate, composition and method will permit reuse of many FDA approved antibiotics that have been abandoned or fallen into disuse due to their current low efficacy and/or resistance to these antibiotics by pathogens.

  一种药物结合物、组合物和方法，通过将抗微生物药物与非代谢六糖磷酸酯结合，通过六糖磷酸转运体（UhpT）传递活性抗微生物药物，基于现有抗生素。还公开了联合给予抗生素和非代谢六糖磷酸酯作为抗微生物药物的方法。非代谢六糖磷酸酯可以构成性地和强烈地诱导UhpT的表达，从而显著提高抗生素的功效和/或抗微生物谱。这种药物结合物、组合物和方法将允许重复使用许多已被FDA批准但由于当前低功效和/或病原体对这些抗生素的抗药性而被放弃或停用的抗生素。
• Compositions Containing Antiviral Compounds and Methods of Using the Same
  申请人：Cantrell Gary L.

  公开号：US20090258843A1

  公开（公告）日：2009-10-15

  The present invention is directed to compositions and methods for the treatment of various diseases, pathological disorders, and medical conditions such as viral infections and cancer. The compositions include (A) an antiviral compound or a pharmaceutically acceptable salt thereof; and (B) an agent selected from the group consisting of a substituted or unsubstituted imidazole or a pharmaceutically acceptable salt thereof; a non-steroidal anti-inflammatory agent or a pharmaceutically acceptable salt thereof; an amino acid or a pharmaceutically acceptable salt thereof; a carboxylic acid or a pharmaceutically acceptable salt thereof; a sulfonic acid or a pharmaceutically acceptable salt thereof; and a combination thereof.

  本发明涉及用于治疗各种疾病、病理障碍和医疗条件，如病毒感染和癌症的组合物和方法。所述组合物包括（A）抗病毒化合物或其药学上可接受的盐；和（B）从以下组中选择的药剂：取代或未取代的咪唑或其药学上可接受的盐；非甾体抗炎药或其药学上可接受的盐；氨基酸或其药学上可接受的盐；羧酸或其药学上可接受的盐；磺酸或其药学上可接受的盐；或其组合物。
• [EN] DINUCLEOSIDE-5',5'-PYROPHOSPHATES<br/>[FR] 5',5'-PYROPHOSPHATES DE DINUCLEOSIDES
  申请人：GRUPPO LEPETIT S.P.A.

  公开号：WO1996002554A1

  公开（公告）日：1996-02-01

  (EN) 5',5'-Pyrophosphates of non-naturally occurring nucleosides selected from thymine-3'-azido-2',3'-dideoxy-D-riboside, 5-fluorouracil-2'-deoxy-D-riboside, uracil-3'-azido-2',3'-dideoxy-D-riboside, guanine-2',3'-dideoxy-D-riboside, hypoxanthine-2',3'-dideoxy-D-riboside, cytosine-2',3'-dideoxy-D-riboside, and adenine-2',3'-dideoxy-D-riboside, are described as well as their manufacture and use as therapeutical agents against tumors and retroviral infections including HIV infections. The compounds may be administered as the active ingredients of pharmaceutical compositions or as pro-drugs encapsulated into biological carriers, e.g., transformed erythrocytes, for targeting to specific cell population responsible of the development of the pathological disorders.(FR) L'invention concerne des 5',5'-pyrophosphates de nucléosides d'origine non naturelle, sélectionnés parmi le thymine-3'-azido-2',3'-didésoxy-D-riboside, le 5-fluorouracil-2'-désoxy-D-riboside, l'uracil-3'-azido-2',3'-didésoxy-D-riboside, le guanine-2',3'-didésoxy-D-riboside, l'hypoxanthine-2',3'-didésoxy-D-riboside, le cytosine-2',3'-didésoxy-D-riboside et l'adénine-2',3'-didésoxy-D-riboside. L'invention concerne également leur procédé de production et leur utilisation en tant qu'agents thérapeutiques contre les tumeurs et les infections rétrovirales y compris les infections au VIH. Ces composés peuvent être administrés en tant que principe actif de compositions pharmaceutiques ou sous forme de promédicaments encapsulés dans des excipients biologiques, par ex. des érythrocytes transformés, afin de lutter contre des populations de cellules cibles responsables du développement de troubles pathologiques.

  由非天然来源的核苷酸制成，从以下核苷酸中选择：thaltsyzine-3'-azido-2'，3'-dideoxy-D-ribose（脱氧核糖核苷酸），5-氟尿嘧啶-2'-脱氧-D-ribose（脱氧核糖核苷酸），尿嘧啶-3'-azido-2'，3'-dideoxy-D-ribose（脱氧核糖核苷酸），鸟嘌呤-2'，3'-dideoxy-D-ribose（脱氧核糖核苷酸），嘌呤呤-2'，3'-dideoxy-D-ribose（脱氧核糖核苷酸），胞嘧啶-2'，3'-dideoxy-D-ribose（脱氧核糖核苷酸），以及腺嘌呤-2'，3'-dideoxy-D-ribose（脱氧核糖核苷酸），这些脱氧核糖核苷酸亚酯及其合成方法，用于治疗肿瘤和逆转RNA病毒感染，包括HIV感染。这些化合物可作为药物成分或作为前驱药包裹在生物载体中（如已转化的红细胞）进行特定细胞群的靶向。
• DINUCLEOSIDE-5',5'-PYROPHOSPHATES
  申请人：GRUPPO LEPETIT S.p.A.

  公开号：EP0773951A1

  公开（公告）日：1997-05-21
• Cell culture medium
  申请人：Genetix Limited

  公开号：EP1818392B1

  公开（公告）日：2010-08-25