Neptinib | 2085843-51-0

• 物质功能分类: 医药中间体 - 原料药中间体
• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二氮杂萘
• 英文名称: Neptinib
• 英文别名: (E)-N-[4-(3-chloro-4-fluoroanilino)-7-ethoxyquinazolin-6-yl]-4-(dimethylamino)but-2-enamide
• CAS: 2085843-51-0
• 化学式: C₂₂H₂₃ClFN₅O₂
• 分子量: 443.9
• InChiKey: RTAAZCCTCLCXHX-AATRIKPKSA-N

物化性质

• 沸点：
  623.6±55.0 °C(Predicted)
• 密度：
  1.334±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  4
• 重原子数：
  31
• 可旋转键数：
  8
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.23
• 拓扑面积：
  79.4
• 氢给体数：
  2
• 氢受体数：
  7

文献信息

• Pharmaceutical composition comprising neptinib or salt thereof and method for controlling impurity thereof
  申请人：SHENZHEN NEPTUNUS PHARMACEUTICAL RESEARCH INSTITUTE CO., LTD.

  公开号：US10668069B2

  公开（公告）日：2020-06-02

  A pharmaceutical composition including neptinib is provided. The composition includes neptinib or a pharmaceutically acceptable salt thereof, and an excipient at a low risk of compatibleness. Furthermore, the pharmaceutical composition of the present invention may also include pharmaceutically acceptable organic acid or inorganic acid as a stabilizer. The content of impurity A maintains a non-significant increase in the long-term and accelerated stability investigation for the pharmaceutical composition.

  提供了一种包括奈普替尼的药物组合物。该组合物包括奈普替尼或其药学上可接受的盐，以及相容性风险较低的赋形剂。此外，本发明的药物组合物还可以包括药学上可接受的有机酸或无机酸作为稳定剂。在药物组合物的长期稳定性和加速稳定性调查中，杂质 A 的含量保持无显著增加。
• A CRYSTAL FORM OF NEPTINIB di-P-METHYLBENZENESULFONATE, PREPARATION METHOD THEREOF, AND PHARMACEUTICAL COMPOSITION CONTAINING SAME
  申请人：SHENZHEN NEPTUNUS PHARMACEUTICAL RESEARCH INSTITUTE CO., LTD.

  公开号：US20170342037A1

  公开（公告）日：2017-11-30

  Provided is a composition of N-[4-[(3-chloro-4-fluorophenyl)amino]-7-[3-(ethoxy)-6-quinazolinyl]-4-(dimethylamino)-2-butenamide p-toluene sulfonate 1.5 hydrate α-polymorph. The α-polymorph has a stable form, a defined melting point, a good chemical stability, and a good endurance to high temperature and light irradiation, and is suitable for pharmaceutical use.
• PHARMACEUTICAL COMPOSITION COMPRISING NEPTINIB OR SALT THEREOF AND METHOD FOR CONTROLLING IMPURITY THEREOF
  申请人：SHENZHEN NEPTUNUS PHARMACEUTICAL RESEARCH INSTITUTE CO., LTD.

  公开号：US20190224201A1

  公开（公告）日：2019-07-25

  A pharmaceutical composition including neptinib is provided. The composition includes neptinib or a pharmaceutically acceptable salt thereof, and an excipient at a low risk of compatibleness. Furthermore, the pharmaceutical composition of the present invention may also include pharmaceutically acceptable organic acid or inorganic acid as a stabilizer. The content of impurity A maintains a non-significant increase in the long-term and accelerated stability investigation for the pharmaceutical composition.
• US9957237B2
  申请人：——

  公开号：US9957237B2

  公开（公告）日：2018-05-01