1-(2-Aminoethyl)-3-pyrrolin-2-one

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡咯啉
• 英文名称: 1-(2-Aminoethyl)-3-pyrrolin-2-one
• 英文别名: 1-(2-aminoethyl)-2H-pyrrol-5-one
• 化学式: C₆H₁₀N₂O
• 分子量: 126.16
• InChiKey: LEHVKYAFISJAJX-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -1.1
• 重原子数：
  9
• 可旋转键数：
  2
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.5
• 拓扑面积：
  46.3
• 氢给体数：
  1
• 氢受体数：
  2

文献信息

• [EN] TERMINALLY MODIFIED POLYMERS AND CONJUGATES THEREOF<br/>[FR] POLYMÈRES MODIFIÉS EN EXTRÉMITÉ ET LEURS CONJUGUÉS
  申请人：MERSANA THERAPEUTICS INC

  公开号：WO2014008375A1

  公开（公告）日：2014-01-09

  A terminally modified polymer is provided herein. At least one terminus of the polymer is -O-(CH2)2-LM or -O-CH2-CH(OH)-CH2-CR1=CR2R3. LM, R1, R2, and R3 are defined herein Also disclosed are terminal conjugates comprising the polymer and a pharmaceutically useful modifier, as well as compositions comprising the conjugates, methods of their preparation, and methods of treating various disorders with the conjugates or their compositions.

  本文提供了一种终端修饰的聚合物。聚合物的至少一个末端是-O-(CH2)2-LM或-O- -CH(OH)- -CR1=CR2R3。LM、R1、R2和R3在此处有定义。还披露了包括聚合物和药用修饰剂的终端共轭物，以及包括这些共轭物的组合物、它们的制备方法以及使用这些共轭物或它们的组合物治疗各种疾病的方法。
• Polyoxazoline antibody drug conjugates
  申请人：Serina Therapeutics, Inc.

  公开号：US11065340B2

  公开（公告）日：2021-07-20

  In the present disclosure, polymer conjugates, including polymer-antibody-drug conjugates (polymer ADCs) are described, as well as the use of such conjugates to treat human disease. The polymer conjugates can contain a large number of polymer-bound agents, thus effectively increasing the drug antibody ration (DAR) of the antibody significantly beyond the currently available technology. This may be of particular importance when antibodies to low density antigens are used as target antibodies. The described polymer-ADCs have improved pharmacokinetics and solubility relative to traditional ADCs. The linker between agent and the polymer can be tailored to provide release of toxin at the desired site and under the desired conditions within the tumor. An additional feature of the polymer-ADCs of the current disclosure is that a purification moiety can be attached to the polymer backbone to provide ease of purification of the polymer-ADCs.

  本公开介绍了聚合物共轭物，包括聚合物-抗体-药物共轭物（聚合物 ADC），以及使用这种共轭物治疗人类疾病的方法。聚合物共轭物可包含大量与聚合物结合的药剂，从而有效提高抗体的药物抗体比（DAR），大大超过现有技术。当低密度抗原抗体被用作靶向抗体时，这一点可能尤为重要。与传统 ADC 相比，所述聚合物 ADC 改善了药代动力学和溶解性。药剂与聚合物之间的连接剂可进行定制，以便在肿瘤内的理想部位和理想条件下释放毒素。本公开的聚合物-ADC 的另一个特点是，可在聚合物骨架上连接纯化分子，使聚合物-ADC 易于纯化。
• Polyoxazoline Anitbody Drug Conjugates
  申请人：Serina Therapeutics, Inc.

  公开号：US20190000985A1

  公开（公告）日：2019-01-03

  In the present disclosure, polymer conjugates, including polymer-antibody-drug conjugates (polymer ADCs) are described, as well as the use of such conjugates to treat human disease. The polymer conjugates can contain a large number of polymer-bound agents, thus effectively increasing the drug antibody ration (DAR) of the antibody significantly beyond the currently available technology. This may be of particular importance when antibodies to low density antigens are used as target antibodies. The described polymer-ADCs have improved pharmacokinetics and solubility relative to traditional ADCs. The linker between agent and the polymer can be tailored to provide release of toxin at the desired site and under the desired conditions within the tumor. An additional feature of the polymer-ADCs of the current disclosure is that a purification moiety can be attached to the polymer backbone to provide ease of purification of the polymer-ADCs.