6-[difluoro(6-pyridin-4-yl[1,2,4]triazolo[4,3-b]pyridazin-3-yl)methyl]quinoline | 943540-74-7

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 喹啉及其衍生物
• 英文名称: 6-[difluoro(6-pyridin-4-yl[1,2,4]triazolo[4,3-b]pyridazin-3-yl)methyl]quinoline
• 英文别名: 6-[Difluoro-(6-pyridin-4-yl-[1,2,4]triazolo[4,3-b]pyridazin-3-yl)methyl]quinoline
• CAS: 943540-74-7
• 化学式: C₂₀H₁₂F₂N₆
• 分子量: 374.352
• InChiKey: KOAWAWHSMVKCON-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.7
• 重原子数：
  28
• 可旋转键数：
  3
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.05
• 拓扑面积：
  68.9
• 氢给体数：
  0
• 氢受体数：
  7

文献信息

• [EN] NEW COMPOUNDS<br/>[FR] NOUVEAUX COMPOSÉS
  申请人：JANSSEN PHARMACEUTICA NV

  公开号：WO2017050864A1

  公开（公告）日：2017-03-30

  The invention relates to new quinoxaline, quinoline and quinazolinone derivative compounds, to pharmaceutical compositions comprising said compounds, to processes for the preparation of said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.

  该发明涉及新的喹喔啉、喹啉和喹唑啉衍生物化合物，包括含有这些化合物的药物组合物，制备这些化合物的方法以及利用这些化合物治疗疾病，例如癌症。
• [EN] QUINOXALINE DERIVATIVES USEFUL AS FGFR KINASE MODULATORS<br/>[FR] DÉRIVÉS DE QUINOXALINE UTILES EN TANT QUE MODULATEURS DE LA KINASE FGFR
  申请人：ASTEX THERAPEUTICS LTD

  公开号：WO2015144803A1

  公开（公告）日：2015-10-01

  The invention relates to new quinoxaline derivative compounds of formula (I), to pharmaceutical compositions comprising said compounds, to processes for the preparation of said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.

  本发明涉及公式（I）的新喹喔啉衍生物化合物、包含该化合物的制药组合物、制备该化合物的工艺以及使用该化合物治疗疾病（例如癌症）的方法。
• TRIAZOLOPYRIDAZINES AS KINASE MODULATORS
  申请人：Lu Tianbao

  公开号：US20090098181A1

  公开（公告）日：2009-04-16

  The invention is directed to triazolopyridazine compounds of Formula I: where R 1 , R 5 , R 6 , R 7 , R 8 , and A are as defined herein, the use of such compounds as protein tyrosine kinase modulators, particularly inhibitors of c-Met, and the use of such compounds to reduce or inhibit kinase activity of c-Met in a cell or a subject, and modulate c-Met expression in a cell or subject, and the use of such compounds for preventing or treating in a subject a cell proliferative disorder and/or disorders related to c-Met. The present invention is further directed to pharmaceutical compositions comprising the compounds of the present invention and to methods for treating conditions such as cancers and other cell proliferative disorders.

  本发明涉及式I的三唑并吡嗪化合物：其中R1、R5、R6、R7、R8和A如本文所定义，使用这种化合物作为蛋白酪氨酸激酶调节剂，特别是c-Met的抑制剂，并使用这种化合物来减少或抑制细胞或受体中c-Met的激酶活性，调节细胞或受体中c-Met的表达，并使用这种化合物预防或治疗细胞增殖性疾病和/或与c-Met相关的疾病。本发明还涉及包含本发明化合物的制药组合物以及治疗癌症和其他细胞增殖性疾病的方法。
• CMET-INHIBITORS FOR USE IN DELAYING THE EMERGENCE IN RESISTANCE TO FGFR INHIBITORS
  申请人：Astex Therapeutics Limited

  公开号：EP3848034A1

  公开（公告）日：2021-07-14

  The invention relates to a combination of a first compound selected from N-(3,5-dimethoxyphenyl)-N'-(1-methylethyl)-N-[3-(1-methyl-1H-pyrazol-4-yl)quinoxalin-6-yl]ethane-1,2-diamine or a pharmaceutically acceptable salt thereof or a solvate thereof, and N-(2-fluoro-3,5-dimethoxyphenyl)-N-(1H-imidazol-2-ylmethyl)-3-(1-methyl-1H-pyrazol-4-yl)pyrido[2,3-b]pyrazin-6-amine or a pharmaceutically acceptable salt thereof or a solvate thereof; and a second compound which is a cMet inhibitor. The combination is for use in the treatment of a proliferative disorder, in particular for use in the treatment of cancer. The FGFR inhibitor (N-(3,5-dimethoxyphenyl)-N'-(1-methylethyl)-N-[3-(1-methyl-1H-pyrazol-4-yl)quinoxalin-6-yl]ethane-1,2-diamine or a pharmaceutically acceptable salt thereof or a solvate thereof, and N-(2-fluoro-3,5-dimethoxyphenyl)-N-(1H-imidazol-2-ylmethyl)-3-(1-methyl-1H-pyrazol-4-yl)pyrido[2,3-b]pyrazin-6-amine or a pharmaceutically acceptable salt thereof or a solvate thereof) and the cMet inhibitor can be administered simultaneously, separately or sequentially. The invention further relates to a pharmaceutical composition comprising a pharmaceutically acceptable carrier and a combination according to the invention.

  本发明涉及选自 N-(3,5-二甲氧基苯基)-N'-(1-甲基乙基)-N-[3-(1-甲基-1H-吡唑-4-基)喹喔啉-6-基]乙烷-1,2-二胺或其药学上可接受的盐或其溶液的第一种化合物的组合、和 N-(2-氟-3,5-二甲氧基苯基)-N-(1H-咪唑-2-基甲基)-3-(1-甲基-1H-吡唑-4-基)吡啶并[2,3-b]吡嗪-6-胺或其药学上可接受的盐或其溶液；第二种化合物是一种 cMet 抑制剂。 该组合物用于治疗增殖性疾病，特别是用于治疗癌症。 FGFR抑制剂（N-(3,5-二甲氧基苯基)-N'-(1-甲基乙基)-N-[3-(1-甲基-1H-吡唑-4-基)喹喔啉-6-基]乙烷-1,2-二胺或其药学上可接受的盐或其溶液，以及N-(2-氟-3、5-二甲氧基苯基)-N-(1H-咪唑-2-基甲基)-3-(1-甲基-1H-吡唑-4-基)吡啶并[2,3-b]吡嗪-6-胺或其药学上可接受的盐或其溶液)和 cMet 抑制剂可同时、分别或依次给药。 本发明还涉及一种药物组合物，该组合物包含药学上可接受的载体和根据本发明的组合物。
• Combinations
  申请人：ASTEX THERAPEUTICS LTD

  公开号：US10085982B2

  公开（公告）日：2018-10-02

  The invention relates to a combination of a first compound selected from N-(3,5-dimethoxyphenyl)-N′-(1-methylethyl)-N-[3-(1-methyl-1H-pyrazol-4-yl)quinoxalin-6-yl]ethane-1,2-diamine or a pharmaceutically acceptable salt thereof or a solvate thereof, and N-(2-fluoro-3,5-dimethoxyphenyl)-N-(1H-imidazol-2-ylmethyl)-3-(1-methyl-1H-pyrazol-4-yl)pyrido[2,3-b]pyrazin-6-amine or a pharmaceutically acceptable salt thereof or a solvate thereof; and a second compound which is a cMet inhibitor. The combination is for use in the treatment of a proliferative disorder, in particular for use in the treatment of cancer. The FGFR inhibitor (N-(3,5-dimethoxyphenyl)-N′-(1-methylethyl)-N-[3-(1-methyl-1H-pyrazol-4-yl)quinoxalin-6-yl]ethane-1,2-diamine or a pharmaceutically acceptable salt thereof or a solvate thereof, and N-(2-fluoro-3,5-dimethoxyphenyl)-N-(1H-imidazol-2-ylmethyl)-3-(1-methyl-1H-pyrazol-4-yl)pyrido[2,3-b]pyrazin-6-amine or a pharmaceutically acceptable salt thereof or a solvate thereof) and the cMet inhibitor can be administered simultaneously, separately or sequentially. The invention further relates to a pharmaceutical composition comprising a pharmaceutically acceptable carrier and a combination according to the invention.

  本发明涉及选自 N-(3,5-二甲氧基苯基)-N′-(1-甲基乙基)-N-[3-(1-甲基-1H-吡唑-4-基)喹喔啉-6-基]乙烷-1,2-二胺或其药学上可接受的盐或其溶液的第一种化合物的组合、和 N-(2-氟-3,5-二甲氧基苯基)-N-(1H-咪唑-2-基甲基)-3-(1-甲基-1H-吡唑-4-基)吡啶并[2,3-b]吡嗪-6-胺或其药学上可接受的盐或其溶液；第二种化合物是一种 cMet 抑制剂。该组合物用于治疗增殖性疾病，特别是用于治疗癌症。FGFR抑制剂（N-(3,5-二甲氧基苯基)-N′-(1-甲基乙基)-N-[3-(1-甲基-1H-吡唑-4-基)喹喔啉-6-基]乙烷-1,2-二胺或其药学上可接受的盐或其溶液，以及N-(2-氟-3、5-二甲氧基苯基)-N-(1H-咪唑-2-基甲基)-3-(1-甲基-1H-吡唑-4-基)吡啶并[2,3-b]吡嗪-6-胺或其药学上可接受的盐或其溶液)和 cMet 抑制剂可同时、分别或依次给药。本发明还涉及一种药物组合物，该组合物包含药学上可接受的载体和根据本发明的组合物。