Rotigotine-2-Azidoacetate | 1424879-51-5

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 羧酸及其衍生物
• 英文名称: Rotigotine-2-Azidoacetate
• 英文别名: [(6S)-6-[propyl(2-thiophen-2-ylethyl)amino]-5,6,7,8-tetrahydronaphthalen-1-yl] 2-azidoacetate
• CAS: 1424879-51-5
• 化学式: C₂₁H₂₆N₄O₂S
• 分子量: 398.529
• InChiKey: ITTNWDBBSDZWSC-KRWDZBQOSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  6.1
• 重原子数：
  28
• 可旋转键数：
  10
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.48
• 拓扑面积：
  72.1
• 氢给体数：
  0
• 氢受体数：
  6

反应信息

• 作为产物：
  描述：

  罗替戈汀 在 盐酸 、 4-二甲氨基吡啶 、 N,N'-二环己基碳二亚胺 作用下， 生成 Rotigotine-2-Azidoacetate
  参考文献：
  名称：

  Subcutaneous Delivery of Poly(oxazoline) Polymer Conjugates

  摘要：

  本公开提供了聚合物共轭物，包括聚合物和一个药物，该药物通过含有可水解基团的连接基团与聚合物相连。

  公开号：

  US20160303250A1

文献信息

• [EN] POLYOXAZOLINE ANTIBODY DRUG CONJUGATES<br/>[FR] CONJUGUÉS ANTICORPS-MÉDICAMENT DE POLYOXAZOLINE
  申请人：SERINA THERAPEUTICS INC

  公开号：WO2016019340A1

  公开（公告）日：2016-02-04

  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.

  本公开描述了聚合物偶联物，包括聚合物-抗体-药物偶联物（聚合物ADCs），以及使用这些偶联物治疗人类疾病。该聚合物偶联物可以含有大量的聚合物结合剂，从而有效提高抗体的药物抗体比率（DAR），显著超过目前现有技术。当使用针对低密度抗原的抗体作为靶点抗体时，这一点可能尤为重要。与传统的ADC相比，所述聚合物ADC具有改善的药代动力学和溶解性。毒素与聚合物之间的连接器可以根据需要在肿瘤内特定部位和特定条件下释放毒素进行定制。当前公开的聚合物ADC的另一个特点是，可以在聚合物主链上附着一个纯化部分，以提供聚合物ADC的纯化便利。
• Subcutaneous delivery of poly(oxazoline) conjugates
  申请人：Moreadith Randall

  公开号：US08383093B1

  公开（公告）日：2013-02-26

  The present disclosure provides polymer conjugates comprising a polymer and an agent, the agent linked to the polymer via a linking group containing a hydrolyzable moiety.

  本公开提供了聚合物共轭物，包括聚合物和一种药剂，该药剂通过含有可水解基团的连接基团与聚合物连接。
• Subcutaneous Delivery of Poly(oxazoline) Conjugates
  申请人：Serina Therapeutics, Inc.

  公开号：US20130177521A1

  公开（公告）日：2013-07-11

  The present disclosure provides polymer conjugates comprising a polymer and an agent, the agent linked to the polymer via a linking group containing a hydrolyzable moiety.

  本公开提供了聚合物共轭物，包括聚合物和代理物，代理物通过含有可水解基团的连接基团与聚合物连接。
• SUBCUTANEOUS DELIVERY OF POLY(OXAZOLINE) POLYMER CONJUGATES
  申请人：Serina Therapeutics, Inc.

  公开号：US20140112880A1

  公开（公告）日：2014-04-24

  The present disclosure provides polymer conjugates comprising a polymer and an agent, the agent linked to the polymer via a linking group containing a hydrolyzable moiety.

  本公开提供了聚合物共轭物，包括聚合物和一个代理，该代理通过含有可水解基团的连接基团与聚合物连接。
• Polyoxazoline Antibody Drug Conjugates
  申请人：Serina Therapeutics, Inc.

  公开号：US20160030592A1

  公开（公告）日：2016-02-04

  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.

  本公开说明书描述了高分子共轭物，包括高分子-抗体-药物共轭物（高分子ADC），以及使用这些共轭物治疗人类疾病。高分子共轭物可以包含大量高分子结合的药物，从而有效地将抗体的药物比例（DAR）显著提高到目前可用技术之外。当用于低密度抗原的抗体时，这可能特别重要。所述的高分子ADC相对于传统ADC具有改进的药代动力学和溶解度。代理和高分子之间的连接剂可以定制以在肿瘤内所需的位置和条件下释放毒素。本公开说明书的高分子ADC的另一个特点是可以将净化基团附加到高分子骨架上，以提供高分子ADC的易于纯化性。