3-[(R)-1-(2,6-dichloro-3-fluorophenyl)ethoxy]-5-(1-piperidin-4-yl-1H-pyrazol-4-yl)pyridin-2-ylamine acetate | 877399-53-6

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡啶及其衍生物
• 英文名称: 3-[(R)-1-(2,6-dichloro-3-fluorophenyl)ethoxy]-5-(1-piperidin-4-yl-1H-pyrazol-4-yl)pyridin-2-ylamine acetate
• 英文别名: Crizotinib acetate；acetic acid;3-[(1R)-1-(2,6-dichloro-3-fluorophenyl)ethoxy]-5-(1-piperidin-4-ylpyrazol-4-yl)pyridin-2-amine
• CAS: 877399-53-6
• 化学式: C₂H₄O₂*C₂₁H₂₂Cl₂FN₅O
• 分子量: 510.396
• InChiKey: LFCVDLCLKZRGFW-UTONKHPSSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  5.13
• 重原子数：
  34
• 可旋转键数：
  5
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.35
• 拓扑面积：
  115
• 氢给体数：
  3
• 氢受体数：
  8

反应信息

• 作为产物：
  描述：

  (R)-N,N-bis(tert-butoxycarbonyl)-3-(1-(2,6-dichloro-3-fluorophenyl)ethoxy)-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)pyridin-2-amine 在 盐酸 、 bis-triphenylphosphine-palladium(II) chloride 、 sodium carbonate 作用下， 以 1,4-二氧六环 、 乙二醇二甲醚 、 水 为溶剂， 反应 29.0h， 生成 3-[(R)-1-(2,6-dichloro-3-fluorophenyl)ethoxy]-5-(1-piperidin-4-yl-1H-pyrazol-4-yl)pyridin-2-ylamine acetate
  参考文献：
  名称：

  Combination of a C-Met antagonist and an aminoheteroaryl compound for the treatment of cancer

  摘要：

  该发明还涉及一种包含抗c-Met抗体拮抗剂和氨基杂环芳烃化合物的组合物，特别用作药物。本发明还包括一种药物组合物，其中包括所述抗c-Met抗体和所述氨基杂环芳烃化合物作为联合产品，用于同时、分开或顺序使用。该发明涉及使用该发明的组合物治疗哺乳动物体内的癌症。

  公开号：

  US09375425B2

文献信息

• Enantiomerically pure aminoheteroaryl compounds as protein kinase inhibitors
  申请人：Cui Jean Jingrong

  公开号：US20060046991A1

  公开（公告）日：2006-03-02

  Enantiomerically pure compound of formula 1 are provided, as well as methods for their synthesis and use. Preferred compounds are potent inhibitors of the c-Met protein kinase, and are useful in the treatment of abnormal cell growth disorders, such as cancers.

  提供了式1的对映纯化合物，以及它们的合成和使用方法。优选化合物是c-Met蛋白激酶的强效抑制剂，并且在治疗异常细胞生长紊乱，如癌症方面具有用处。
• Pyrazole-substituted aminoheteroaryl compounds as protein kinase inhibitors
  申请人：Cui Jean Jingrong

  公开号：US20060128724A1

  公开（公告）日：2006-06-15

  Compounds of formula 1 are provided, as well as methods for their synthesis and use. Preferred compounds are potent inhibitors of the c-Met protein kinase, and are useful in the treatment of abnormal cell growth disorders, such as cancers.

  提供了化学式1的化合物，以及它们的合成和使用方法。首选的化合物是c-Met蛋白激酶的强效抑制剂，并且在治疗异常细胞生长障碍，例如癌症方面非常有用。
• COMBINATION OF A C-MET ANTAGONIST AND AN AMINOHETEROARYL COMPOUND FOR THE TREATMENT OF CANCER
  申请人：GOETSCH Liliane

  公开号：US20110117098A1

  公开（公告）日：2011-05-19

  The invention also relates to a composition comprising an antibody antagonist to c-Met and an aminoheteroaryl compound, particularly as a medicament. The present invention also comprises a pharmaceutical composition comprising said anti c-Met antibody and said aminoheteroaryl compound as combination products for simultaneous, separate or sequential use. The invention relates to the use of the composition of the invention for the treatment of cancer in a mammal.

  该发明还涉及一种包含抗c-Met抗体拮抗剂和氨基杂环芳烃化合物的组合物，特别作为药物。本发明还包括一种制药组合物，该制药组合物包括上述抗c-Met抗体和氨基杂环芳烃化合物，用于同时、分开或顺序使用。该发明涉及使用该组合物治疗哺乳动物的癌症。
• Combination of a c-Met antagonist and an aminoheteroaryl compound for the treatment of cancer
  申请人：Goetsch Liliane

  公开号：US08623359B2

  公开（公告）日：2014-01-07

  The invention also relates to a composition comprising an antibody antagonist to c-Met and an aminoheteroaryl compound, particularly as a medicament. The present invention also comprises a pharmaceutical composition comprising said anti c-Met antibody and said aminoheteroaryl compound as combination products for simultaneous, separate or sequential use. The invention relates to the use of the composition of the invention for the treatment of cancer in a mammal.

  该发明还涉及一种组合物，包括针对c-Met的抗体拮抗剂和氨基杂环芳烃化合物，特别是作为药物。本发明还包括一种制药组合物，该组合物包括所述抗c-Met抗体和所述氨基杂环芳烃化合物，作为同时、分离或顺序使用的组合产品。该发明涉及使用该组合物治疗哺乳动物的癌症。
• Combination of a c-Met antagonist and an aminoheteroaryl compound for the treatment of cancer
  申请人：Pierre Fabre Medicament

  公开号：EP2143441A1

  公开（公告）日：2010-01-13

  The invention also relates to a composition comprising an antibody antagonist to c-Met and an aminoheteroaryl compound, particularly as a medicament. The present invention also comprises a pharmaceutical composition comprising said anti c-Met antibody and said aminoheteroaryl compound as combination products for simultaneous, separate or sequential use. The invention relates to the use of the composition of the invention for the treatment of cancer in a mammal.

  本发明还涉及一种由 c-Met 抗体拮抗剂和氨基杂芳基化合物组成的组合物，特别是作为一种药物。本发明还包括一种药物组合物，该组合物包含所述抗 c-Met 抗体和所述氨基杂芳基化合物，作为同时、单独或连续使用的组合产品。本发明涉及本发明组合物用于治疗哺乳动物癌症的用途。