bis(prop-2-enyl) (2S)-2-[[(2S)-6-amino-1-oxo-1-prop-2-enoxyhexan-2-yl]carbamoylamino]pentanedioate | 1069138-65-3

• 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: bis(prop-2-enyl) (2S)-2-[[(2S)-6-amino-1-oxo-1-prop-2-enoxyhexan-2-yl]carbamoylamino]pentanedioate
• CAS: 1069138-65-3
• 化学式: C₂₁H₃₃N₃O₇
• 分子量: 439.509
• InChiKey: XGOYBAWQPPCFJU-IRXDYDNUSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.5
• 重原子数：
  31
• 可旋转键数：
  20
• 环数：
  0.0
• sp3杂化的碳原子比例：
  0.52
• 拓扑面积：
  146
• 氢给体数：
  3
• 氢受体数：
  8

反应信息

• 作为反应物：
  描述：

  monosuccinate monohexanoate cisplatin(IV) 、 bis(prop-2-enyl) (2S)-2-[[(2S)-6-amino-1-oxo-1-prop-2-enoxyhexan-2-yl]carbamoylamino]pentanedioate 在 吗啉 、 四(三苯基膦)钯 作用下， 以 N,N-二甲基甲酰胺 为溶剂， 生成
  参考文献：
  名称：

  Targeted Conjugates Encapsulated in Particles and Formulations Thereof

  摘要：

  包括纳米颗粒和微粒在内的微粒子以及其药物配方，其中含有活性剂的共轭物，例如治疗、预防或诊断剂，通过连接体连接到靶向基团，已经设计出来，可以提供改善活性剂的时间空间传递和/或改善生物分布的效果。提供了制备共轭物、微粒子和其配方的方法。提供了将这些配方用于需要的受试者的方法，例如用于治疗或预防癌症或传染病。

  公开号：

  US20140187501A1

文献信息

• [EN] TARGETED CONJUGATES AND PARTICLES AND FORMULATIONS THEREOF<br/>[FR] CONJUGUÉS CIBLÉS, PARTICULES ET PRÉPARATIONS ASSOCIÉES
  申请人：BLEND THERAPEUTICS INC

  公开号：WO2016004043A1

  公开（公告）日：2016-01-07

  Particles, including nanoparticles and microparticles, and pharmaceutical formulations thereof, comprising conjugates of an active agent such as a therapeutic, prophylactic, or diagnostic agent attached to a targeting moiety via a linker have been designed which can provide improved temporospatial delivery of the active agent and/or improved biodistribution. Methods of making the conjugates, the particles, and the formulations thereof are provided. Methods of administering the formulations to a subject in need thereof are provided, for example, to treat or prevent cancer or infectious diseases.

  包括纳米颗粒和微粒子在内的粒子以及其制剂，包括将活性药剂（如治疗、预防或诊断药剂）与靶向基团通过连接剂结合的共轭物。这些设计可以提供改善活性药剂的时间空间传递和/或改善生物分布的效果。提供了制备共轭物、粒子和制剂的方法。提供了向需要的受试者（例如治疗或预防癌症或传染病）施用制剂的方法。
• METHODS FOR THE PREPARATION OF TARGETING AGENT FUNCTIONALIZED DIBLOCK COPOLYMERS FOR USE IN FABRICATION OF THERAPEUTIC NANOPARTICLES
  申请人：Pfizer Inc.

  公开号：EP2285350B1

  公开（公告）日：2017-11-15
• METHODS FOR THE PREPARATION OF TARGETING AGENT FUNCTIONALIZED DIBLOCK COPOLYMERS FOR USE IN FABRICATION OF THERAPEUTIC TARGETED NANOPARTICLES
  申请人：Ali Mir M.

  公开号：US20100104645A1

  公开（公告）日：2010-04-29

  This application provides methods of making nanoparticles using pre-functionalized poly(ethylene glycol) (also referred to as PEG) as a macroinitiator for the synthesis of diblock copolymers. These diblock copolymers comprise a poly(ethylene glycol) block bearing a targeting agent at its terminus and a second biocompatible and biodegradable hydrophobic polymer block (e.g. a poly(ester)). The poly(ethylene glycol) is hetero-bifunctional with a targeting moiety (agent) covalently bound to its α terminus and a polymerization initiating functional group (e.g., a hydroxyl group) present on its ω terminus. Ring opening polymerization yields the desired poly(ester)-poly(ethylene glycol)-targeting agent polymer that is used to impart targeting capability to therapeutic nanoparticles. This “polymerization from” approach typically employs precursors of the targeting agent wherein the reactivity of functional groups of the targeting agent is masked using protecting groups. Also described is a “coupling to” that utilized the poly(ethylene glycol)-targeting agent conjugate where the targeting agent remains in its native un-protected form. This method uses “orthogonal” chemistry that exhibit no cross reactivity towards functional groups typically found within targeting agents of interest. Nanoparticles produced according to the disclosed methods as well as their use in the treatment of various diseases are also provided.
• Methods for the Preparation of Targeting Agent Functionalized Diblock Copolymers for Use in Fabrication of Therapeutic Targeted Nanoparticles
  申请人：BIND BIOSCIENCES, INC

  公开号：US20130115192A1

  公开（公告）日：2013-05-09

  This application provides nanoparticles and methods of making nanoparticles using pre-functionalized poly(ethylene glycol)(also referred to as PEG) as a macroinitiator for the synthesis of diblock copolymers. Ring opening polymerization yields the desired poly(ester)-poly(ethylene glycol)-targeting agent polymer that is used to impart targeting capability to therapeutic nanoparticles. This “polymerization from” approach typically employs precursors of the targeting agent wherein the reactivity of functional groups of the targeting agent is masked using protecting groups. Also described is a “coupling to” that utilized the poly(ethylene glycol)-targeting agent conjugate where the targeting agent remains in its native un-protected form. This method uses “orthogonal” chemistry that exhibit no cross reactivity towards functional groups typically found within targeting agents of interest.
• SSTR-TARGETED CONJUGATES ENCAPSULATED IN PARTICLES AND FORMULATIONS THEREOF
  申请人：BLEND THERAPEUTICS, INC.

  公开号：US20160074526A1

  公开（公告）日：2016-03-17

  Particles, including nanoparticles and microparticles, and pharmaceutical formulations thereof, containing conjugates of an active agent such as a therapeutic, prophylactic, or diagnostic agent attached to a targeting moiety via a linker have been designed which can provide improved temporospatial delivery of the active agent and/or improved biodistribution. Methods of making the conjugates, the particles, and the formulations thereof are provided. Methods of administering the formulations to a subject in need thereof are provided, for example, to treat or prevent cancer or infectious diseases.