5,8-Dihydroxy-1,4-bis[2-(2-hydroxyethylamino)ethylamino]-4a,9a-dihydroanthracene-9,10-dione

• 分子结构分类: 有机化合物 - 苯类化合物 - 蒽
• 英文名称: 5,8-Dihydroxy-1,4-bis[2-(2-hydroxyethylamino)ethylamino]-4a,9a-dihydroanthracene-9,10-dione
• 化学式: C₂₂H₃₀N₄O₆
• 分子量: 446.5
• InChiKey: BIVQCGYKQAFKHN-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.1
• 重原子数：
  32
• 可旋转键数：
  12
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.45
• 拓扑面积：
  163
• 氢给体数：
  8
• 氢受体数：
  10

文献信息

• PARTICULATE DRUG DELIVERY
  申请人：Cheng Jianjun

  公开号：US20080248126A1

  公开（公告）日：2008-10-09

  Methods for efficient preparation of drug-polymer (or oligomer) conjugates which are useful in the preparation of particles, including microparticles and nanoparticles, for delivery of the drug in vivo for therapeutic applications. The invention additionally provides certain drug-polymer and drug-oligomer conjugates which are useful in the preparation of particles for delivery of the drug in vivo. The invention also provides nanoparticles of this invention prepared by nanoprecipitation using drug-polymer/oligomer conjugates of the invention. The drug conjugates are formed during polymerization of the polymer or oligomer in which the drug is employed as an initiator of the polymerization of the monomers which form the polymer and/or oligomer. More specifically, the drug conjugates are formed by ring-opening polymerization of cyclic monomers in the presence of an appropriate ring-opening polymerization catalyst and the initiator (the drug). The method is particularly useful for formation of polymer/oligomer conjugates with drugs and other chemical species containing one or more hydroxyl groups or thiol groups.

  本发明提供了一种有效制备药物-聚合物（或寡聚物）共轭物的方法，该方法可用于制备微粒和纳米粒子，以在体内传递药物进行治疗应用。本发明还提供了某些药物-聚合物和药物-寡聚物共轭物，该共轭物可用于制备体内药物传递的微粒。本发明还提供了通过使用本发明的药物-聚合物/寡聚物共轭物制备的纳米粒子。药物共轭物是在聚合物或寡聚物的聚合过程中形成的，其中药物被用作引发单体聚合形成聚合物和/或寡聚物的引发剂。更具体地说，药物共轭物是通过在适当的开环聚合催化剂和引发剂（药物）的存在下开环聚合环状单体形成的。该方法特别适用于与含有一个或多个羟基或硫醇基团的药物和其他化学物质形成聚合物/寡聚物共轭物。
• CONJUGATES COMPRISING HYDROXYALKYL STARCH AND A CYTOTOXIC AGENT AND PROCESS FOR THEIR PREPARATION
  申请人：Knoller Helmut

  公开号：US20130217871A1

  公开（公告）日：2013-08-22

  The present invention relates to hydroxyalkyl starch conjugates and a method for preparing the same, the hydroxyalkyl starch conjugate comprising a hydroxyalkyl starch derivative and a cytotoxic agent, the cytotoxic agent comprising at least one primary hydroxyl group, wherein the hydroxyalkyl starch is linked via said primary hydroxyl group to the cytotoxic agent. The conjugates according to the present invention have a structure according to the following formula HAS′(-L-M) n wherein M is a residue of the cytotoxic agent, L is a linking moiety, HAS′ is the residue of the hydroxyalkyl starch derivative, and n is greater than or equal to 1, and wherein the hydroxyalkyl starch derivative has a mean molecular weight (MW) above the renal threshold and a molar substitution (MS) in the range of from 0.6 to 1.5.

  本发明涉及羟基烷基淀粉共轭物及其制备方法，所述羟基烷基淀粉共轭物包括羟基烷基淀粉衍生物和细胞毒素药物，所述细胞毒素药物包括至少一个主要羟基基团，其中羟基烷基淀粉通过所述主要羟基基团与细胞毒素药物连接。本发明的共轭物具有以下式子的结构：HAS'(-L-M)n，其中M是细胞毒素药物的残基，L是连接基团，HAS'是羟基烷基淀粉衍生物的残基，n大于等于1，且羟基烷基淀粉衍生物具有平均分子量(MW)高于肾小球阈值且摩尔取代(MS)在0.6至1.5范围内。
• PARTICULATE DRUG DELIVERY METHODS
  申请人：The Board of Trustees of the University of Illinois

  公开号：US20150314006A1

  公开（公告）日：2015-11-05

  Methods for efficient preparation of drug-polymer (or oligomer) conjugates useful in the preparation of particles, including microparticles and nanoparticles, for delivery of the drug in vivo for therapeutic applications are provided. The invention also provides nanoparticles prepared by nanoprecipitation using drug-polymer/oligomer conjugates of the invention. The drug conjugates are formed during polymerization of the polymer or oligomer in which the drug is employed as an initiator of the polymerization of the monomers which form the polymer and/or oligomer. More specifically, the drug conjugates are formed by ring-opening polymerization of cyclic monomers in the presence of an appropriate ring-opening polymerization catalyst and the initiator (the drug). The method is particularly useful for formation of polymer/oligomer conjugates with drugs and other chemical species containing one or more hydroxyl groups or thiol groups.

  提供了用于高效制备药物-聚合物（或低聚物）共轭物的方法，该方法可用于制备微粒和纳米粒子，以便在体内传递药物进行治疗应用。本发明还提供了使用本发明的药物-聚合物/低聚物共轭物制备的纳米粒子。药物共轭物是在聚合物或低聚物的聚合过程中形成的，其中药物被用作引发单体聚合的引发剂，这些单体形成聚合物和/或低聚物。更具体地说，药物共轭物是通过在适当的开环聚合催化剂和引发剂（药物）存在下的环开口聚合反应中形成的。该方法特别适用于形成聚合物/低聚物共轭物与含有一个或多个羟基或硫醇基团的药物和其他化学物质。
• US9789195B2
  申请人：——

  公开号：US9789195B2

  公开（公告）日：2017-10-17