4-amino-1-[(2R,4S,5R)-4-hydroxy-5-(hydroxymethyl)-3-methylideneoxolan-2-yl]pyrimidin-2-one;dihydrate

• 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: 4-amino-1-[(2R,4S,5R)-4-hydroxy-5-(hydroxymethyl)-3-methylideneoxolan-2-yl]pyrimidin-2-one;dihydrate
• 化学式: C10H17N3O6
• 分子量: 275.26
• InChiKey: XTYUGPDATYNDMJ-YPMAUOMFSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -3.02
• 重原子数：
  19
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.4
• 拓扑面积：
  110
• 氢给体数：
  5
• 氢受体数：
  6

文献信息

• 2'-Deoxy-2'-methylidenecytidine dihydrate, methods for its production and compositions
  申请人：YOSHITOMI PHARMACEUTICAL INDUSTRIES, LTD.

  公开号：EP0443471A1

  公开（公告）日：1991-08-28

  Novel stable, non-hygroscopic 2'-deoxy-2'-methylidenecytidine (1) and its methods for production, and compositions with improved solubility containing same and saccharide(s).

  新型稳定、不吸湿的 2'-deoxy-2'-methylidenecytidine (1)及其生产方法，以及含有 2'-deoxy-2'-methylidenecytidine (1)和糖的溶解性更好的组合物。
• NOVEL 2'-METHYLIDENENUCLEOTIDE COMPOUND, PROCESS FOR PRODUCING THE SAME, AND PHARMACEUTICAL USE THEREOF
  申请人：Matsuda, Akira

  公开号：EP0690068A1

  公开（公告）日：1996-01-03

  A novel 2'-methylidenenucleotide compound represented by general formula (I) or a salt thereof, a process for producing the same, and a pharmaceutical use thereof. In said formula, R represents hydrogen or halogen; R¹ and R² represent each independently a fatty acid residue or a hydrocarbon residue; and R³ and R⁴ represent each independently hydrogen, halogen or alkyl. The compound and salts thereof have an excellent antitumor activity against mammals. More specifically, they have a remarkable activity of inhibiting growth of mouse tumors, cultured human tumor cells or human tumors transplanted to nude mice, and hence are efficacious in curing or inhibiting the recurrence of mammalian pulmonary cancer, digestive cancer, mamary cancer, head and neck cancers, gynecologic cancer, urologic cancer, leukemia, melanoma, lymphatic metastatic tumor, and so forth. Also they are useful as an antitumor drug because they have an increased bioavailability and are lowly toxic. Further they have the effects of persistent and increased activities.

  一种由通式(I)代表的新型 2'-亚甲基烯核苷酸化合物或其盐，一种生产该化合物的工艺及其药物用途。在所述式中，R 代表氢或卤素；R¹ 和 R² 各自独立地代表脂肪酸残基或烃残基；R³ 和 R⁴ 各自独立地代表氢、卤素或烷基。该化合物及其盐类对哺乳动物具有极佳的抗肿瘤活性。更具体地说，它们具有抑制小鼠肿瘤、培养的人类肿瘤细胞或移植到裸鼠身上的人类肿瘤生长的显著活性，因此在治疗或抑制哺乳动物肺癌、消化系统癌症、乳腺癌、头颈部癌症、妇科癌症、泌尿系统癌症、白血病、黑色素瘤、淋巴转移性肿瘤等方面具有疗效。此外，它们还可作为抗肿瘤药物，因为它们具有更高的生物利用度和低毒性。此外，它们还具有持续和增强活性的作用。
• LIPOSOME PREPARATION
  申请人：YOSHITOMI PHARMACEUTICAL INDUSTRIES, LTD.

  公开号：EP0750910A1

  公开（公告）日：1997-01-02

  A liposome preparation comprising a water-soluble 2'-deoxy-2'-methylidenecytidine compound encapsulated therein and a compound which positively charges the surface of lipid membrane. This liposome preparation is not only expected to decrease toxicity to myeloid tissue, which is caused by a water-soluble 2'-deoxycytidine compound having anti-malignant tumor activity, but also expected to accumulate the active ingredient in tumor tissues by virtue of an improved residence thereof in blood. Therefore, the preparation can maintain or enhance anti-tumor effects without causing side effects, and is useful for the treatment of malignant tumors.

  一种脂质体制剂，其中封装了一种水溶性 2'-脱氧-2'-亚甲基胞嘧啶化合物和一种能使脂膜表面带正电荷的化合物。这种脂质体制剂不仅可以降低具有抗恶性肿瘤活性的水溶性 2'- 脱氧胞嘧啶化合物对骨髓组织的毒性，还可以通过改善其在血液中的停留时间在肿瘤组织中积累活性成分。因此，该制剂可以保持或增强抗肿瘤效果，而不会产生副作用，可用于治疗恶性肿瘤。
• JPH06179693A
  申请人：——

  公开号：JPH06179693A

  公开（公告）日：1994-06-28
• JPH06128162A
  申请人：——

  公开号：JPH06128162A

  公开（公告）日：1994-05-10