Canlitinib | 2222730-78-9

• 分子结构分类: 有机化合物 - 有机氧化合物
• 英文名称: Canlitinib
• 英文别名: 6-[4-[2-fluoro-4-[[1-[(4-fluorophenyl)carbamoyl]cyclopropanecarbonyl]amino]phenoxy]-6-methoxyquinolin-7-yl]oxyhexanoic acid
• CAS: 2222730-78-9
• 化学式: C₃₃H₃₁F₂N₃O₇
• 分子量: 619.6
• InChiKey: PCKYITPVOLEZKL-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  6.1
• 重原子数：
  45
• 可旋转键数：
  14
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.27
• 拓扑面积：
  136
• 氢给体数：
  3
• 氢受体数：
  10

文献信息

• QUINOLINYL-SUBSTITUTED CARBOXYLIC ACID COMPOUND OR PHARMACEUTICALLY ACCEPTABLE SALT THEREOF, PHARMACEUTICAL COMPOSITION THEREOF, AND USE THEREOF
  申请人：Beijing Konruns Pharmaceutical Co., Ltd.

  公开号：EP3530654A1

  公开（公告）日：2019-08-28

  The present application provides a quinolyl-substituted carboxylic acid compound as shown in formula (I) or a pharmaceutically acceptable salt thereof, as well as a method for preparing the compound, a use of the compound, and a formulation containing the quinolyl-substituted carboxylic acid compound or the pharmaceutically acceptable salt thereof. This type of compounds are inhibitors for AXL and/or VEGFR2 protein kinase, and can be used to treat diseases caused by abnormality of the two protein kinases, such as, tumor, etc.;

  本申请提供了一种如式（I）所示的喹啉基取代的羧酸化合物或其药学上可接受的盐，以及该化合物的制备方法、该化合物的用途和含有该喹啉基取代的羧酸化合物或其药学上可接受的盐的制剂。这类化合物是 AXL 和/或 VEGFR2 蛋白激酶的抑制剂，可用于治疗由这两种蛋白激酶异常引起的疾病，如肿瘤等；
• Quinolyl-substituted carboxylic acid compound or pharmaceutically acceptable salt thereof, pharmaceutical composition of the same, and use of the same
  申请人：BEIJING KONRUNS PHARMACEUTICAL CO., LTD.

  公开号：US10723701B2

  公开（公告）日：2020-07-28

  The present application provides a quinolyl-substituted carboxylic acid compound as shown in formula (I) or a pharmaceutically acceptable salt thereof, as well as a method for preparing the compound, a use of the compound, and a formulation containing the quinolyl-substituted carboxylic acid compound or the pharmaceutically acceptable salt thereof. This type of compounds are inhibitors for AXL and/or VEGFR2 protein kinase, and can be used to treat diseases caused by abnormality of the two protein kinases, such as, tumor, etc.

  本申请提供了一种如式（I）所示的喹啉基取代的羧酸化合物或其药学上可接受的盐，以及该化合物的制备方法、该化合物的用途和含有该喹啉基取代的羧酸化合物或其药学上可接受的盐的制剂。这类化合物是 AXL 和/或 VEGFR2 蛋白激酶的抑制剂，可用于治疗由这两种蛋白激酶异常引起的疾病，如肿瘤等。
• [EN] CRYSTAL FORMS OF COMPOUND, PREPARATION METHOD THEREFOR, PHARMACEUTICAL COMPOSITION AND APPLICATION THEREOF<br/>[FR] FORMES CRISTALLINES DE COMPOSÉ, PROCÉDÉ DE PRÉPARATION CORRESPONDANT, COMPOSITION PHARMACEUTIQUE ET UTILISATION ASSOCIÉES<br/>[ZH] 化合物晶型、其制备方法、药物组合物以及应用
  申请人：BEIJING KONRUNS PHARMACEUTICAL CO LTD

  公开号：WO2020216188A1

  公开（公告）日：2020-10-29

  本发明提供了用于治疗蛋白激酶AXL和/或VEGFR2相关疾病的化合物6-[[4-[2-氟-4-[[1-[(4-氟苯基)氨基甲酰基]环丙烷羰基]氨基]苯氧基]-6-甲氧基-7-喹啉基]氧基]己酸的三种晶型：晶型AB、晶型M和晶型F。本发明还提供了用于制备这三种晶型的方法及包含这三种晶型的药物组合物。本发明的晶型AB、晶型M和晶型F均具有良好的化学稳定性，并且本发明的三种晶型的制备方法简单易行，产物收率和纯度高，能够稳定且批量化生产，有利于推广和应用。本发明的晶型AB、晶型M、晶型F在高温、高湿、氧化条件下也较为稳定，有利于储存和运输，有利于工业化生产。此外，本发明的晶型AB、晶型M和晶型F具有较高的生物利用度，符合临床用药要求。
• QUINOLYL-SUBSTITUTED CARBOXYLIC ACID COMPOUND OR PHARMACEUTICALLY ACCEPTABLE SALT THEREOF, PHARMACEUTICAL COMPOSITION OF THE SAME, AND USE OF THE SAME
  申请人：BEIJING KONRUNS PHARMACEUTICAL CO., LTD.

  公开号：US20190256470A1

  公开（公告）日：2019-08-22

  The present application provides a quinolyl-substituted carboxylic acid compound as shown in formula (I) or a pharmaceutically acceptable salt thereof, as well as a method for preparing the compound, a use of the compound, and a formulation containing the quinolyl-substituted carboxylic acid compound or the pharmaceutically acceptable salt thereof. This type of compounds are inhibitors for AXL and/or VEGFR2 protein kinase, and can be used to treat diseases caused by abnormality of the two protein kinases, such as, tumor, etc.;
• Crystalline Form of Compound, Method for Preparing the Same, Pharmaceutical Composition and Use
  申请人：Beijing Konruns Pharmaceutical Co., Ltd.

  公开号：US20220259152A1

  公开（公告）日：2022-08-18

  The present disclosure relates to the field of pharmaceutical technology, providing three crystalline forms, i.e., a crystalline form AB, a crystalline form M and a crystalline form F, of the compound 6-[[4-[2-fluoro-4-[[1-[(4-fluorophenyl)aminoformyl]cyclopropanecarbonyl]-amino]phenoxy]-6-methoxy-7-quinolyl]oxy]hexanoic acid for treatment of diseases related to protein kinases AXL and/or VEGFR2. The present disclosure also provides methods for preparing these three crystalline forms and pharmaceutical compositions comprising these three crystalline forms. The crystalline form AB, the crystalline form M and the crystalline form F of the present disclosure all have good chemical stability, and the preparation processes of the three crystalline forms of the present disclosure are simple for implementation with high product yield and purity, allowing stable and mass production that facilitates promotion and application.