(S)-4-Methyl-N-((S)-1-(((R)-4-Methyl-1-((R)-2-Methyloxiran-2-yl)-1-oxopentan-2-yl)aMino)-1-oxo-3-phenylpropan-2-yl)-2-((S)-2-(2-MorpholinoacetaMido)-4-phenylbutanaMido)pentanaMide

• 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: (S)-4-Methyl-N-((S)-1-(((R)-4-Methyl-1-((R)-2-Methyloxiran-2-yl)-1-oxopentan-2-yl)aMino)-1-oxo-3-phenylpropan-2-yl)-2-((S)-2-(2-MorpholinoacetaMido)-4-phenylbutanaMido)pentanaMide
• 英文别名: 4-methyl-N-[1-[[4-methyl-1-[(2R)-2-methyloxiran-2-yl]-1-oxopentan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]-2-[[2-[(2-morpholin-4-ylacetyl)amino]-4-phenylbutanoyl]amino]pentanamide
• 化学式: C₄₀H₅₇N₅O₇
• 分子量: 719.9
• InChiKey: BLMPQMFVWMYDKT-YPEOYEODSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.7
• 重原子数：
  52
• 可旋转键数：
  20
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.57
• 拓扑面积：
  159
• 氢给体数：
  4
• 氢受体数：
  8

文献信息

• STABLE COMPOSITIONS OF PEGYLATED CARFILZOMIB COMPOUNDS
  申请人：AMGEN INC.

  公开号：US20190142957A1

  公开（公告）日：2019-05-16

  The present invention provides stable pharmaceutical compositions of pegylated carfilzomib compounds, methods for preparing the compositions, and uses of the compositions for treating cancer, including hematologic malignancies such as multiple myeloma. The compositions can be stored in frozen form or lyophilized to dry solid form.

  本发明提供了聚乙二醇化卡非索米布化合物的稳定药物组合物，制备该组合物的方法，以及使用该组合物治疗癌症，包括血液恶性肿瘤如多发性骨髓瘤的用途。该组合物可以以冷冻形式或冻干成干固体形式储存。
• PROCESSES FOR THE PREPARATION OF CARFILZOMIB OR PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF
  申请人：LAURUS LABS LIMITED

  公开号：US20190284231A1

  公开（公告）日：2019-09-19

  The present invention relates to an improved process for the preparation of carfilzomib or a pharmaceutically acceptable salt thereof. The present invention also relates to a process for the preparation of amorphous form of carfilzomib.

  本发明涉及一种改进的制备卡非索米或其药学上可接受的盐的方法。本发明还涉及一种制备卡非索米非晶态的方法。
• Process for the Preparation of (S)-4-Methyl-N-((S)-1-(((S)-4-Methyl-1-((R)-2-Methyloxiran-2-YL)-1-OXO Pentan-2-YL) Amino)-1-OXO-3-Phenylpropan-2-YL)-2-((S)-2-(2-Morpholinoacetamido)-4-Phenylbutanamido) Pentanamide
  申请人：Biophore India Pharmaceuticals Pvt. Ltd

  公开号：US20170298093A1

  公开（公告）日：2017-10-19

  Novel methods for preparation of Carfilzomib and intermediates thereof with high stereo selection are reported. The synthetic procedures result in substantially pure Carfilzomib (I).

  报道了制备高立体选择性的卡菲索米布及其中间体的新方法。合成过程得到了几乎纯净的卡菲索米布(I)。
• STERILE INJECTABLE COMPOSITION COMPRISING CARFILZOMIB
  申请人：Cadila Healthcare Limited

  公开号：EP3536309A1

  公开（公告）日：2019-09-11

  The present invention relates to sterile injectable compositions comprising carfilzomib and one or more phospholipids. The present invention also relates to processes for preparing the sterile injectable compositions.

  本发明涉及包含卡非佐米和一种或多种磷脂的无菌注射剂组合物。本发明还涉及制备无菌注射用组合物的工艺。
• Process for the preparation of (S)-4-methyl-N-((S)-1-(((S)-4-methyl-1-((R)-2-methyloxiran-2-yl)-1-oxo-pentan-2-yl) amino)-1-oxo-3-phenylpropan-2-yl)-2-((S)-2-(2-morpholinoacetamido)-4-phenylbutanamido) pentanamide
  申请人：Biophore India Pharmaceuticals Pvt. Ltd

  公开号：US10329325B2

  公开（公告）日：2019-06-25

  Novel methods for preparation of Carfilzomib and intermediates thereof with high stereo selection are reported. The synthetic procedures result in substantially pure Carfilzomib (I).

  报告了制备卡非佐米及其具有高立体选择性的中间体的新方法。这些合成程序可得到纯度很高的 Carfilzomib (I)。