[5-(6-amino-2-fluoropurin-9-yl)-3,4-dihydroxyoxolan-2-yl]methoxy-oxoniophosphinate

• 分子结构分类: 有机化合物 - 核苷、核苷酸和类似物 - 嘌呤核苷酸
• 英文名称: [5-(6-amino-2-fluoropurin-9-yl)-3,4-dihydroxyoxolan-2-yl]methoxy-oxoniophosphinate
• 化学式: C10H13FN5O7P
• 分子量: 365.21
• InChiKey: GIUYCYHIANZCFB-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -3.1
• 重原子数：
  24
• 可旋转键数：
  4
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.5
• 拓扑面积：
  186
• 氢给体数：
  5
• 氢受体数：
  12

文献信息

• Multi-arm polymer prodrugs
  申请人：Zhao Xuan

  公开号：US20080194612A1

  公开（公告）日：2008-08-14

  Provided herein are water-soluble prodrugs. The prodrugs of the invention comprise a water-soluble polymer having three or more arms, at least three of which are covalently attached to an active agent, e.g., a small molecule. The conjugates of the invention provide an optimal balance of polymer size and structure for achieving improved drug loading, since the conjugates of the invention possess three or more active agents releasably attached to a multi-armed water soluble polymer. The prodrugs of the invention are therapeutically effective, and exhibit improved properties in-vivo when compared to unmodified parent drug.

  本文提供了一种水溶性的前药。该发明的前药包括一个水溶性聚合物，具有三个或更多的臂，其中至少三个臂与活性剂（例如小分子）共价连接。本发明的结合物提供了聚合物大小和结构的最佳平衡，以实现改善药物负载，因为本发明的结合物具有三个或更多的活性剂可释放地连接到多臂水溶性聚合物上。本发明的前药具有治疗效果，并在体内表现出比未修改的母体药物更好的性能。
• Multi-Arm Polymer Prodrugs
  申请人：Zhao Xuan

  公开号：US20090074704A1

  公开（公告）日：2009-03-19

  Provided herein are water-soluble prodrugs, compositions comprising such prodrugs, and related methods of making and administering the same. The prodrugs of the invention comprise a water-soluble polymer having three or more arms, at least three of which are typically covalently attached to an active agent, e.g., a small molecule. The conjugates of the invention provide an optimal balance of polymer size and structure for achieving improved drug loading, since the conjugates of the invention possess three or more active agents releasably attached to a multi-armed water-soluble polymer. The prodrugs of the invention are therapeutically effective, and exhibit improved properties in-vivo when compared to unmodified parent drug.

  本文提供了水溶性前药、包含这种前药的组合物以及相关的制备和使用方法。本发明的前药包括具有三个或更多臂的水溶性聚合物，其中至少三个臂通常共价地连接到一个活性剂，例如小分子。本发明的共轭物提供了聚合物尺寸和结构的最佳平衡，以实现改进的药物装载，因为本发明的共轭物具有三个或更多的活性剂可释放地连接到多臂水溶性聚合物上。本发明的前药具有治疗效果，并且与未经修改的母药相比，在体内表现出改进的性质。
• MULTI-ARM POLYMER PRODRUGS
  申请人：Zhao Xuan

  公开号：US20100190933A1

  公开（公告）日：2010-07-29

  Provided herein are water-soluble prodrugs. The prodrugs of the invention comprise a water-soluble polymer having three or more arms, at least three of which are covalently attached to an active agent, e.g., a small molecule. The conjugates of the invention provide an optimal balance of polymer size and structure for achieving improved drug loading, since the conjugates of the invention possess three or more active agents releasably attached to a multi-armed water soluble polymer. The prodrugs of the invention are therapeutically effective, and exhibit improved properties in-vivo when compared to unmodified parent drug.

  本文提供的是水溶性前药。该发明的前药包括具有三个或更多臂的水溶性聚合物，其中至少三个臂与活性剂（例如小分子）共价连接。本发明的结合物提供了最佳的聚合物大小和结构平衡，以达到改进药物负载的目的，因为本发明的结合物具有三个或更多活性剂可释放地附着于多臂水溶性聚合物上。本发明的前药在治疗上是有效的，并且与未经修改的原始药物相比，在体内表现出改进的性质。
• COMBINATION THERAPY FOR TREATING CANCER
  申请人：Leukos Biotech, S.L.

  公开号：EP3348266A1

  公开（公告）日：2018-07-18

  The invention relates to a combination comprising an antineoplastic agent, e.g. an antimetabolite antineoplastic agent and a serotonin receptor (HTR) modulator, e.g. a HTR antagonist. In addition the invention relates to a pharmaceutical composition comprising a combination of the invention and a pharmaceutically acceptable excipient. The invention also relates to the combination and pharmaceutical composition according to the invention for use in medicine, particularly for use in the prevention and/or treatment of a hematological malignancy.

  本发明涉及一种组合物，包括一种抗肿瘤剂，如抗代谢抗肿瘤剂和一种5-羟色胺受体（HTR）调节剂，如HTR拮抗剂。此外，本发明还涉及一种药物组合物，其中包含本发明的组合物和一种药学上可接受的赋形剂。本发明还涉及根据本发明的组合物和药物组合物在医学中的应用，特别是在预防和/或治疗血液恶性肿瘤中的应用。
• Crystal form of fludarabine phosphate, preparation method therefor, and application thereof
  申请人：Zhejiang Hisun Pharmaceutical Co., Ltd.

  公开号：US10669302B2

  公开（公告）日：2020-06-02

  Provided are a new crystal form of fludarabine phosphate, a preparation method therefor, a pharmaceutical composition containing same, and an application thereof in preparing medicine. Crystal forms I and II of the fludarabine phosphate have excellent properties in terms of solubleness, dissolution rate, chemical stability, and processing adaptability.

  本发明提供了一种新的磷酸氟达拉宾晶体形式、其制备方法、含有该晶体形式的药物组合物及其在制备药物中的应用。磷酸氟达拉滨晶体 I 和 II 在溶解度、溶解速率、化学稳定性和加工适应性方面具有优异的性能。