cabozantinib malate

• 分子结构分类: 有机化合物 - 有机氧化合物
• 英文名称: cabozantinib malate
• 英文别名: XL184 (S-malate);BMS-907351 (S-malate)；1-N-[4-(6,7-dimethoxyquinolin-4-yl)oxyphenyl]-1-N'-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide;2-hydroxybutanedioic acid
• 化学式: C₄H₆O₅*C₂₈H₂₄FN₃O₅
• 分子量: 635.603
• InChiKey: HFCFMRYTXDINDK-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.45
• 重原子数：
  46
• 可旋转键数：
  11
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.22
• 拓扑面积：
  194
• 氢给体数：
  5
• 氢受体数：
  12

反应信息

• 作为产物：
  描述：

  苹果酸 、 卡博替尼 以 四氢呋喃 、 水 、 4-甲基-2-戊酮 为溶剂， 反应 18.0h， 以86.68%的产率得到cabozantinib malate
  参考文献：
  名称：

  [EN] MALATE SALT OF N- (4- { [ 6, 7-BIS (METHYLOXY) QUIN0LIN-4-YL] OXY}PHENYL)-N' - (4 -FLUOROPHENYL) CYCLOPROPANE-1,1-DICARBOXAMIDE, AND CRYSTALLINE FORMS THEROF FOR THE TREATMENT OF CANCER
  [FR] SEL DE MALATE DE N-(4-{[6,7-BIS(MÉTHYLOXY)QUINOLIN-4-YL]OXY}PHÉNYL)-N'-(4-FLUOROPHÉNYL)CYCLOPROPANE-1,1-DICARBOXAMIDE ET FORMES CRISTALLINES DE CELUI-CI POUR LE TRAITEMENT DU CANCER

  摘要：

  公开号：

  WO2010083414A8

文献信息

• Method of Treating Cancer
  申请人：Exelixis, Inc.

  公开号：US20140057908A1

  公开（公告）日：2014-02-27

  This invention is directed to the treatment of cancer, particularly castration-resistant prostate cancer and osteoblastic bone metastases, with a dual inhibitor of MET and VEGF.

  本发明旨在使用MET和VEGF的双重抑制剂治疗癌症，特别是去势抵抗性前列腺癌和骨转移性骨转移癌。
• Method for Treating Osteoporosis
  申请人：Exelixis, Inc.

  公开号：US20140228401A1

  公开（公告）日：2014-08-14

  This invention is directed to the treatment of osteoporosis using N-(4-[6,7-bis(methyloxy)quinolin-4-yl]oxy}phenyl)-N′-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide.

  本发明涉及使用N-(4-[6,7-双甲氧基喹啉-4-基]氧基}苯基)-N'-(4-氟苯基)环丙烷-1,1-二羧酰胺治疗骨质疏松症。
• METHOD OF TREATING LUNG ADENOCARCINOMA
  申请人：EXELIXIS, INC.

  公开号：US20140121239A1

  公开（公告）日：2014-05-01

  This invention is directed to the treatment of cancer in a patient, particularly a patient with lung adenocarcinoma, and more particularly a patient with KIF5B-RET fusion-positive non-small cell lung cancer, with an inhibitor of MET, VEGF, and RET which is a compound of Formula I: or a pharmaceutically acceptable salt thereof.

  本发明针对治疗患有癌症的患者，特别是患有肺腺癌的患者，更具体地说是患有KIF5B-RET融合阳性非小细胞肺癌的患者，使用MET、VEGF和RET抑制剂进行治疗，该抑制剂是公式I的化合物或其药学上可接受的盐。
• Method of Treating Lung Adenocarcinoma
  申请人：EXELIXIS, INC.

  公开号：US20150238477A1

  公开（公告）日：2015-08-27

  This invention is directed to the treatment of cancer in a patient, particularly a patient with lung adenocarcinoma, and more particularly a patient with KIF5B-RET fusion-positive non-small cell lung cancer, with an inhibitor of MET, VEGF, and RET which is a compound of Formula I: or a pharmaceutically acceptable salt thereof.

  本发明旨在治疗患有癌症的患者，特别是患有肺腺癌的患者，更具体地说是患有KIF5B-RET融合阳性的非小细胞肺癌的患者，使用MET、VEGF和RET的抑制剂，该抑制剂是化合物I的一种，或其药学上可接受的盐。
• AN IMPROVED PROCESS FOR THE PREPARATION OF CABOZANTINIB AND ITS PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF
  申请人：NATCO PHARMA LIMITED

  公开号：US20210188776A1

  公开（公告）日：2021-06-24

  The present invention relates to an improved process for the preparation of N-(4-(6,7-dimethoxyquinolin-4-yloxy)phenyl)-N′-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide compound of formula-1 which is represented by the following structural formula: