7-{4-[4-(2,3-dichlorophenyl)-1-piperazinyl]butoxy}-3,4-dihydro-2(1H)-quinolinone hexanoate | 1258382-01-2

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二嗪烷类
• 英文名称: 7-{4-[4-(2,3-dichlorophenyl)-1-piperazinyl]butoxy}-3,4-dihydro-2(1H)-quinolinone hexanoate
• 英文别名: 7-[4-[4-(2,3-dichlorophenyl)piperazin-1-yl]butoxy]-3,4-dihydro-1H-quinolin-2-one;hexanoic acid
• CAS: 1258382-01-2
• 化学式: C₆H₁₂O₂*C₂₃H₂₇Cl₂N₃O₂
• 分子量: 564.552
• InChiKey: MUYITTPPBNOVJS-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  6.51
• 重原子数：
  38
• 可旋转键数：
  11
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.52
• 拓扑面积：
  82.1
• 氢给体数：
  2
• 氢受体数：
  6

文献信息

• Aripiprazole prodrug compositions
  申请人：ALKERMES PHARMA IRELAND LIMITED

  公开号：US10016415B2

  公开（公告）日：2018-07-10

  Described is a composition comprising (a) a population of particles of an aripiprazole prodrug having a volume based particle size (Dv50) of less than 1000 nm and (b) at least one surface stabilizer comprising an adsorbed component which is adsorbed on the surface of the aripiprazole prodrug particles and a free component available for solubilization of the aripiprazole prodrug. The surface stabilizer to prodrug ratio provides the optimal quantity of free surface stabilizer for the purposes of producing a lead-in formulation. Also described are methods of treatment using the aforementioned composition.

  所述组合物包括：(a)体积粒度（Dv50）小于 1000 纳米的阿立哌唑原药颗粒群；(b)至少一种表面稳定剂，包括吸附在阿立哌唑原药颗粒表面的吸附组分和可用于溶解阿立哌唑原药的游离组分。表面稳定剂与原药的比例为生产前导制剂提供了最佳的游离表面稳定剂数量。此外，还介绍了使用上述组合物进行治疗的方法。
• Compositions of multiple aripiprazole prodrugs
  申请人：ALKERMES PHARMA IRELAND LIMITED

  公开号：US10159671B2

  公开（公告）日：2018-12-25

  Described herein is a composition comprising: (a) a first population of particles of a first aripiprazole prodrug; and (b) a second population of particles of a second aripiprazole prodrug, different to the first aripiprazole prodrug. At least one of the first and second prodrug populations has a volume based particle size (Dv50) of less than about 1000 nm. Also described herein are methods of treatment using the aforementioned composition, and methods of making the aforementioned composition.

  本文描述了一种组合物，该组合物包含：(a) 第一种阿立哌唑原药的颗粒群；(b) 第二种阿立哌唑原药的颗粒群，与第一种阿立哌唑原药不同。第一种和第二种原药中至少有一种原药的体积粒度（Dv50）小于约1000纳米。本文还描述了使用上述组合物进行治疗的方法，以及制造上述组合物的方法。
• Aripiprazole prodrug composition
  申请人：ALKERMES PHARMA IRELAND LIMITED

  公开号：US10688091B2

  公开（公告）日：2020-06-23

  Described is a composition comprising (a) a population of particles of an aripiprazole prodrug having a volume based particle size (Dv50) of less than 1000 nm and (b) at least one surface stabilizer comprising an adsorbed component which is adsorbed on the surface of the aripiprazole prodrug particles and a free component available for solubilisation of the aripiprazole prodrug. The surface stabilizer to prodrug ratio provides the optimal quantity of free surface stabilizer for the purposes of producing a lead-in formulation. Also described are methods of treatment using the aforementioned composition.

  所述组合物包括：(a)体积粒度（Dv50）小于 1000 纳米的阿立哌唑原药颗粒群；(b)至少一种表面稳定剂，包括吸附在阿立哌唑原药颗粒表面的吸附组分和可用于阿立哌唑原药溶解的游离组分。表面稳定剂与原药的比例为生产前导制剂提供了最佳的游离表面稳定剂数量。此外，还介绍了使用上述组合物进行治疗的方法。
• ARIPIPRAZOLE PRODRUG COMPOSITIONS
  申请人：Alkermes Pharma Ireland Limited

  公开号：EP3182958A1

  公开（公告）日：2017-06-28
• COMPOSITIONS OF MULTIPLE ARIPIPRAZOLE PRODRUGS
  申请人：Alkermes Pharma Ireland Limited

  公开号：EP3416616A1

  公开（公告）日：2018-12-26