3',5'-O-di-n-butanoyl-3-n-heptanoyloxymethyl-2'-deoxy-5-fluorouridine | 158720-28-6

• 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: 3',5'-O-di-n-butanoyl-3-n-heptanoyloxymethyl-2'-deoxy-5-fluorouridine
• 英文别名: 3',5'-O-dibutyryl-3-n-heptanoyloxymethyl-2'-deoxy-5-fluorouridine；[3-[(2R,4S,5R)-4-butanoyloxy-5-(butanoyloxymethyl)oxolan-2-yl]-5-fluoro-2,6-dioxopyrimidin-1-yl]methyl heptanoate
• CAS: 158720-28-6
• 化学式: C₂₅H₃₇FN₂O₉
• 分子量: 528.575
• InChiKey: ATQBHTLKQKEUPQ-XUVXKRRUSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.9
• 重原子数：
  37
• 可旋转键数：
  18
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.72
• 拓扑面积：
  129
• 氢给体数：
  0
• 氢受体数：
  10

文献信息

• Uridine derivative and process for preparing the same
  申请人：TANABE SEIYAKU CO., LTD.

  公开号：EP0588317A1

  公开（公告）日：1994-03-23

  A novel uridine derivative of the formula (I): wherein R¹ is acyloxy, R² is hydrogen, acyloxy, etc., R³ is aralkyloxy, acyloxy, etc., R⁴ is hydrogen, acyloxy, etc., R is hydrogen or a lower alkyl, and Y is fluorine or trifluoromethyl, and a process for preparing the same are provided. The uridine derivative (I) of the present invention exhibits an excellent anti-tumor activity in vivo.

  本发明提供了一种具有以下结构的新型尿苷衍生物（I）：其中R¹为酰氧基，R²为氢、酰氧基等，R³为芳基氧基、酰氧基等，R⁴为氢、酰氧基等，R为氢或较低的烷基，Y为氟或三氟甲基，以及制备该化合物的方法。本发明的尿苷衍生物（I）在体内展现出优异的抗肿瘤活性。
• Pharmaceutical preparation comprising fat emulsion of fat microparticles
  申请人：TANABE SEIYAKU CO., LTD.

  公开号：EP0599543A1

  公开（公告）日：1994-06-01

  A preparation comprising a fat emulsion of fat microparticles wherein said emulsion contains a stabilizer consisting essentially of a fatty acid, a basic amino acid and a saccharide is provided. In the preparation comprising a fat emulsion of fat microparticles of the present invention, said microparticles having a mean particle diameter of at most 100 nm are stable, and so the microparticles remain in blood without being uptaken by liver. Therefore in case of administering a pharmaceutical preparation prepared by using the above-mentioned preparation of the present invention, the pharmacological activity may be expressed at a desired site. Thus the preparation is extremely useful as a drug carrier for drug delivery system. Furthermore, the pharmaceutical preparation of the present invention which is lyophilized can be easily and rapidly reconstituted into the pharmaceutical preparation comprising a fat emulsion of stable fat microparticles having a mean particle diameter of about at most 100 nm by adding distilled water, even after a long-term storage.

  本发明提供了一种由脂肪微粒的脂肪乳液组成的制剂，其中所述乳液含有主要由脂肪酸、碱性氨基酸和糖组成的稳定剂。在本发明的包含脂肪微粒的脂肪乳液的制剂中，所述平均粒径不超过 100 nm 的微粒是稳定的，因此微粒在血液中不会被肝脏吸收。因此，在使用本发明的上述制剂制备的药物制剂时，可在所需部位发挥药理活性。因此，本发明制剂可作为药物载体用于给药系统。此外，本发明的冻干药物制剂即使经过长期储存，也可以通过添加蒸馏水，轻松快速地重组为由平均粒径最多约 100 nm 的稳定脂肪微粒组成的脂肪乳液药物制剂。
• US5650172A
  申请人：——

  公开号：US5650172A

  公开（公告）日：1997-07-22