4-(4-{5-amino-6-[(R)-1-(2,6-dichloro-3-fluorophenyl)ethoxy]pyrazin-2-yl}benzoyl)piperazine-1-carboxylic acid tert-butyl ester | 877399-80-9

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二嗪烷类
• 英文名称: 4-(4-{5-amino-6-[(R)-1-(2,6-dichloro-3-fluorophenyl)ethoxy]pyrazin-2-yl}benzoyl)piperazine-1-carboxylic acid tert-butyl ester
• 英文别名: tert-butyl 4-[4-[5-amino-6-[(1R)-1-(2,6-dichloro-3-fluorophenyl)ethoxy]pyrazin-2-yl]benzoyl]piperazine-1-carboxylate
• CAS: 877399-80-9
• 化学式: C₂₈H₃₀Cl₂FN₅O₄
• 分子量: 590.482
• InChiKey: XYXYREBTJQXBIZ-MRXNPFEDSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.8
• 重原子数：
  40
• 可旋转键数：
  7
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.36
• 拓扑面积：
  111
• 氢给体数：
  1
• 氢受体数：
  8

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。
• [EN] AMINOHETEROARYL COMPOUNDS AS PROTEIN TYROSINE KINASE INHIBITORS<br/>[FR] COMPOSES AMINOHETEROARYLES EN TANT QU'INHIBITEURS DES PROTEINES TYROSINE KINASES
  申请人：PFIZER

  公开号：WO2006021886A1

  公开（公告）日：2006-03-02

  Aminoheteroaryl compounds 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.

  提供了氨基杂环芳基化合物，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。
• Aminoheteroaryl compounds as protein kinase inhibitors
  申请人：Cui Jean Jingrong

  公开号：US20060178374A1

  公开（公告）日：2006-08-10

  Aminoheteroaryl compounds 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.

  提供了氨基杂环芳基化合物，以及它们的合成和使用方法。优选化合物是c-Met蛋白激酶的强力抑制剂，并且在治疗异常细胞生长障碍，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：PIERRE FABRE MEDICAMENT

  公开号：US20140186356A1

  公开（公告）日：2014-07-03

  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.

  本发明还涉及一种包括抗c-Met抗体拮抗剂和氨基杂环芳烃化合物的组合物，特别是作为药物。本发明还包括一种制药组合物，该组合物包括所述的抗c-Met抗体和所述的氨基杂环芳烃化合物，用于同时、分离或顺序使用。本发明涉及使用本发明的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。