苯达莫司汀杂质A | 191939-34-1

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯并噻嗪类
• 中文名称: 苯达莫司汀杂质A
• 英文名称: Bendamustine Impurity D
• 英文别名: 4-[6-(2-chloroethyl)-3-methyl-7,8-dihydroimidazo[4,5-h][1,4]benzothiazin-2-yl]butanoic acid
• CAS: 191939-34-1
• 化学式: C₁₆H₂₀ClN₃O₂S
• 分子量: 353.9
• InChiKey: JOUZJTKKJDXTBE-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.6
• 重原子数：
  23
• 可旋转键数：
  6
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.5
• 拓扑面积：
  83.7
• 氢给体数：
  1
• 氢受体数：
  5

文献信息

• METHODS FOR THE PREPARATION OF BENDAMUSTINE
  申请人：Gayring Anton H.

  公开号：US20130310571A1

  公开（公告）日：2013-11-21

  Improved methods for the preparation and purification of bendamustine hydrochloride are described; such as method of preparing bendamustine hydrochloride comprising contacting a compound of formula HBI: with thionyl chloride

  本文描述了制备和纯化氯化苯达莫司汀的改进方法，例如通过将化合物HBI的配方与氯化硫酰接触来制备氯化苯达莫司汀的方法。
• Oral dosage forms of bendamustine and therapeutic use thereof
  申请人：ASTELLAS DEUTSCHLAND GMBH

  公开号：US10485787B2

  公开（公告）日：2019-11-26

  In the present invention there is provided a pharmaceutical composition for oral administration which comprises bendamustine or a pharmaceutically acceptable, ester, salt or solvate thereof as an active ingredient, and a pharmaceutically acceptable excipient and which shows a dissolution of the bendamustine of at least 60% in 20 minutes, 70% in 40 minutes and 80% in 60 minutes, as measured with a paddle apparatus at 50 rpm according to the European Pharmacopoeia in 500 ml of a dissolution medium at a pH of 1.5. The invention further relates to the above pharmaceutical composition for use for the oral treatment of a medical condition which is selected from chronic lymphocytic leukemia, acute lymphocytic leukaemia, chronic myelocytic leukaemia, acute myelocytic leukaemia, Hodgkin's disease, non-Hodgkin's lymphoma, multiple myeloma, breast cancer, ovarian cancer, small cell lung cancer and non-small cell lung cancer.

  本发明提供了一种用于口服给药的药物组合物，它包括作为活性成分的苯达莫司汀或其药学上可接受的酯类、盐类或溶解物，以及药学上可接受的赋形剂，并且根据《欧洲药典》，在500毫升pH值为1.5的溶解介质中，用桨叶仪器以50转/分的速度测量，苯达莫司汀在20分钟内的溶解度至少为60%，在40分钟内溶解度至少为70%，在60分钟内溶解度至少为80%。本发明进一步涉及上述药物组合物，用于口服治疗选自慢性淋巴细胞白血病、急性淋巴细胞白血病、慢性粒细胞白血病、急性粒细胞白血病、霍奇金病、非霍奇金淋巴瘤、多发性骨髓瘤、乳腺癌、卵巢癌、小细胞肺癌和非小细胞肺癌的病症。
• Solid dosage forms of bendamustine
  申请人：Astellas Deutschland GmbH

  公开号：US11160793B2

  公开（公告）日：2021-11-02

  In the present invention there is provided a pharmaceutical composition in a solid dosage form suitable or oral administration, the composition comprising bendamustine or a pharmaceutically acceptable ester, salt or solvate thereof as an active ingredient, and at least one pharmaceutically acceptable excipient, which is a pharmaceutically acceptable saccharide selected from the group consisting of one or more of a monosaccharide, a disaccharide, an oligosaccharide, a cyclic oligosaccharide, a polysaccharide and a saccharide alcohol, wherein the ratio by weight of the active ingredient to the saccharide excipient(s) is in the range of 1:1-5.

  本发明提供了一种适合口服的固体剂型药物组合物，该组合物包含作为活性成分的苯达莫司汀或其药学上可接受的酯、盐或溶液，以及至少一种药学上可接受的赋形剂、其中药学上可接受的糖类选自单糖、二糖、寡糖、环状寡糖、多糖和糖醇中的一种或多种，其中活性成分与糖类赋形剂的重量比在 1：1-5.
• SOLID DOSAGE FORMS OF BENDAMUSTINE
  申请人：Astellas Deutschland GmbH

  公开号：EP2367538B1

  公开（公告）日：2017-08-02
• ORAL DOSAGE FORMS OF BENDAMUSTINE
  申请人：Astellas Deutschland GmbH

  公开号：EP2367542A1

  公开（公告）日：2011-09-28

表征谱图