苯达莫司汀 | 1219709-86-0

• 物质功能分类: 分析化学 - 标准品 - 药典标准品和杂质标准品
• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯并咪唑类
• 中文名称: 苯达莫司汀
• 英文名称: Deschloroethyl bendamustine
• 英文别名: 4-[5-(2-chloroethylamino)-1-methylbenzimidazol-2-yl]butanoic acid
• CAS: 1219709-86-0
• 化学式: C₁₄H₁₈ClN₃O₂
• 分子量: 295.76
• InChiKey: UMRNCYQXTUODGC-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.2
• 重原子数：
  20
• 可旋转键数：
  7
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.43
• 拓扑面积：
  67.2
• 氢给体数：
  2
• 氢受体数：
  4

文献信息

• PROCESS FOR THE PREPARATION OF BENDAMUSTINE HYDROCHLORIDE
  申请人：FRESENIUS KABI ONCOLOGY LIMITED

  公开号：US20140121383A1

  公开（公告）日：2014-05-01

  The present invention relates to an improved process for the synthesis of bendamustine, in particular, bendamustine hydrochloride of the formula (VI) and its intermediate 1-Methyl-5-[bis(2-chloroethyl)amino]-1H-benzimidazol-2-yl]lithium butanoate of formula (V), both having a purity of ≧99%, which is simple, convenient, economical, does not use hazardous chemicals and industrially viable.

  本发明涉及一种改进的苯达莫司汀合成工艺，特别是苯达莫司汀盐酸盐（化学式（VI））及其中间体1-甲基-5-[双(2-氯乙基)氨基]-1H-苯并咪唑-2-基]锂丁酸酯（化学式（V）），两者纯度≧99%，该工艺简单、方便、经济，不使用危险化学品且具有工业可行性。
• Bendamustine Solid Dispersions And Continuous Infusion
  申请人：Voudouris Vasilios

  公开号：US20150258069A1

  公开（公告）日：2015-09-17

  Provided herein are pharmaceutical compositions comprising nitrogen mustard, for example bendamustine hydrochloride, solid dispersions substantially free of degradants. Also provided are methods of producing and administering nitrogen mustards and in particular bendamustine hydrochloride solid dispersions substantially free of degradants. The pharmaceutical compositions can be used for any disease that is sensitive to treatment with bendamustine hydrochloride, such as neoplastic diseases.

  本文提供了含有氮芥的制药组合物，例如盐酸苯达莫司汀，这些组合物是基本无降解物的固体分散体。同时提供了生产和给药氮芥（特别是基本无降解物的盐酸苯达莫司汀固体分散体）的方法。这些制药组合物可用于对盐酸苯达莫司汀敏感的任何疾病，例如肿瘤性疾病。
• Bendamustine pharmaceutical compositions for lyophilisation
  申请人：CEPHALON, INC.

  公开号：EP2574334A1

  公开（公告）日：2013-04-03

  The present invention provides pharmaceutical formulations of lyophilized bendamustine suitable for pharmaceutical use. The present invention further provides methods of producing lyophilized bendamustine. The pharmaceutical formulations can be used for any disease that is sensitive to treatment with bendamustine, such as neoplastic diseases.

  本发明提供了适用于制药用途的冻干苯达莫司汀的药物制剂。本发明进一步提供了生产冻干苯达莫司汀的方法。这些药物制剂可用于任何对苯达莫司汀治疗敏感的疾病，如肿瘤性疾病。
• Liquid formulations of bendamustine
  申请人：CEPHALON, INC.

  公开号：EP2889029A1

  公开（公告）日：2015-07-01

  Stable liquid formulations ofbendamustine, and pharmaceutically acceptable salts thereof, and polar aprotic solvents, are described.

  描述了苯达莫司汀及其药学上可接受的盐类和极性烷基溶剂的稳定液体制剂。
• Bendamustine pharmaceutical compositions
  申请人：Voudouris Vasilios

  公开号：US10786486B2

  公开（公告）日：2020-09-29

  Provided herein are pharmaceutical formulations of dry-powder bendamustine suitable for pharmaceutical use. Also provided are methods of producing dry-powder bendamustine. The pharmaceutical formulations can be used for any disease that is sensitive to treatment with bendamustine, such as neoplastic diseases.

  本文提供了适用于制药的干粉苯达莫司汀药物制剂。还提供了生产干粉苯达莫司汀的方法。这些药物制剂可用于任何对苯达莫司汀治疗敏感的疾病，如肿瘤性疾病。