topotecan

• 分子结构分类: 有机化合物 - 生物碱及其衍生物 - 喜树碱
• 英文名称: topotecan
• 英文别名: 10-[(Dimethylamino)methyl]-4-ethyl-4,9-dihydroxy-1H-pyrano[3',4':6,7]indolizino[1,2-b]quinoline-3,14(4H,12H)-dione；8-[(dimethylamino)methyl]-19-ethyl-7,19-dihydroxy-17-oxa-3,13-diazapentacyclo[11.8.0.02,11.04,9.015,20]henicosa-1(21),2,4(9),5,7,10,15(20)-heptaene-14,18-dione
• 化学式: C₂₃H₂₃N₃O₅
• 分子量: 421.453
• InChiKey: UCFGDBYHRUNTLO-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.5
• 重原子数：
  31
• 可旋转键数：
  3
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.35
• 拓扑面积：
  103
• 氢给体数：
  2
• 氢受体数：
  7

反应信息

• 作为反应物：
  描述：

  topotecan 在 盐酸 作用下， 以 甲醇 、 水 为溶剂， 反应 2.0h， 生成 盐酸拓扑替康
  参考文献：
  名称：

  NOVEL CRYSTALLINE POLYMORPHIC FORM OF A CAMPTOTHECIN ANALOGUE

  摘要：

  该发明涉及拓扑替康盐酸盐的新晶型，以及制备该晶型的方法。特征XRPD图谱和FT-IR图谱如图1和图2所示。

  公开号：

  US20070105885A1

文献信息

• Composition Containing Novel Glutamic Acid Derivative And Block Copolymer, And Use Thereof
  申请人：Nippon Kayaku Kabushiki Kaisha

  公开号：US20200190101A1

  公开（公告）日：2020-06-18

  Provided is a pharmaceutical preparation that is suitable for more effectively exhibiting the efficacy of a glutamic acid derivative, which is a GGT-recognizable prodrug, by producing a composition including a glutamic acid derivative capable of rapidly releasing a physiologically active substance by being recognized by GGT, or a pharmacologically acceptable salt thereof; and a block copolymer in which a polyethylene glycol segment is linked to a polyamino acid segment with a hydrophobic group. Particularly, the composition based on a glutamic acid derivative that uses an antitumor compound as a physiologically active substance is capable of effectively accumulating the glutamic acid derivative at a tumor affected area, exhibits a superior effect against tumors, and is capable of suppressing the release of a physiologically active substance in bone marrow tissue where the expression ratio of GGT is low. Therefore, side effects such as myelosuppression, which pose a problem in the use of antitumor drugs, may be avoided.

  提供的是一种药物制剂，适用于更有效地展现谷氨酸衍生物的功效，该衍生物是一种GGT可识别的前药，通过制备包括一种能够被GGT识别从而快速释放生理活性物质的谷氨酸衍生物或其药理学可接受的盐的组合物；以及一种嵌段共聚物，其中聚乙二醇段与一个疏水基团连接到一个聚氨基酸段。特别是，基于谷氨酸衍生物的组合物使用抗肿瘤化合物作为生理活性物质，能够有效地在受肿瘤影响的区域积累谷氨酸衍生物，对肿瘤具有优越效果，并能够抑制在GGT表达比例较低的骨髓组织中释放生理活性物质。因此，可以避免使用抗肿瘤药物时可能出现的骨髓抑制等副作用。
• Anti-cancer agents, compositions and methods of treating cancers
  申请人：Lam Marina K.

  公开号：US20080255175A1

  公开（公告）日：2008-10-16

  Compounds and compositions useful in methods for treating cancer in mammals. The compounds of the invention are of the formula: or a pharmaceutically acceptable salt, entantiomer or disastereomer thereof, wherein the “A” ring is a nitrogen-aryl group; each occurrence of Y is independently oxygen or H 2 ; Z is oxygen or —CH 2 —; X is nitrogen or —CH; R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , and R 7 are subsitutents; n is an integer from 1-7; m is an integer having a value of 1-5; and the dotted line represents an optional bond.

  在治疗哺乳动物癌症方法中有用的化合物和组合物。发明的化合物的公式为： 或其药学上可接受的盐、对映体或二对映体，其中“A”环是一个氮芳基团； 每个Y的出现独立地是氧或H2； Z是氧或—CH2—； X是氮或—CH； R1、R2、R3、R4、R5、R6和R7是取代基； n是1-7之间的整数； m是一个值为1-5的整数；以及 虚线代表一个可选键。
• Active agent delivery systems and methods for protecting and administering active agents
  申请人：Mickle Travis

  公开号：US20070232529A1

  公开（公告）日：2007-10-04

  The present invention relates to active agent delivery systems and more specifically to compositions that comprise amino acids, as single amino acids or peptides, covalently attached to active agents and methods for administering conjugated active agent compositions.

  本发明涉及活性物质输送系统，更具体地涉及包含氨基酸（作为单个氨基酸或肽）与活性物质共价连接的组合物以及用于给予共轭活性物质组合物的方法。
• ACTIVE AGENT DELIVERY SYSTEMS AND METHODS FOR PROTECTING AND ADMINISTERING ACTIVE AGENTS
  申请人：Mickle Travis

  公开号：US20090253792A1

  公开（公告）日：2009-10-08

  The present invention relates to active agent delivery systems and more specifically to compositions that comprise amino acids, as single amino acids or peptides, covalently attached to active agents and methods for administering conjugated active agent compositions.

  本发明涉及活性剂递送系统，更具体地涉及包含氨基酸（作为单个氨基酸或肽）与活性剂共价连接的组合物以及给予共轭活性剂组合物的方法。
• ACTIVE AGENT DELIVERY SYSTEMS AND METHODS FOR PROTECTING AND ADMINISTERING ACTIVE AGENTS
  申请人：Mickle Travis

  公开号：US20090306228A1

  公开（公告）日：2009-12-10

  The present invention relates to active agent delivery systems and more specifically to compositions that comprise amino acids, as single amino acids or peptides, covalently attached to active agents and methods for administering conjugated active agent compositions.

  本发明涉及活性剂递送系统，更具体地涉及包含氨基酸，作为单个氨基酸或肽，与活性剂共价结合的组合物以及用于给予共轭活性剂组合物的方法。