(4-{2-[(4-bromophenyl)amino]benzoxazol-5-yloxy}-(2-pyridyl))-N-methylcarboxamide | 611217-04-0

• 分子结构分类: 有机化合物 - 有机氧化合物
• 英文名称: (4-{2-[(4-bromophenyl)amino]benzoxazol-5-yloxy}-(2-pyridyl))-N-methylcarboxamide
• 英文别名: 4-((2-((4-bromophenyl)amino)-1,3-benzoxazol-5-yl)oxy)-N-methyl-2-pyridinecarboxamide；4-(2-(4-bromophenylamino)benzo[d]oxazol-5-yloxy)-N-methylpicolinamide；4-[[2-(4-bromoanilino)-1,3-benzoxazol-5-yl]oxy]-N-methylpyridine-2-carboxamide
• CAS: 611217-04-0
• 化学式: C₂₀H₁₅BrN₄O₃
• 分子量: 439.268
• InChiKey: MZCRQBOVCGGSLE-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.4
• 重原子数：
  28
• 可旋转键数：
  5
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.05
• 拓扑面积：
  89.3
• 氢给体数：
  2
• 氢受体数：
  6

反应信息

• 作为产物：
  描述：

  N-甲基-4-氯-2-吡啶甲酰胺 在 双(三甲基硅烷基)氨基钾 、 potassium carbonate 作用下， 以 DMF (N,N-dimethyl-formamide) 为溶剂， 反应 0.6h， 生成 (4-{2-[(4-bromophenyl)amino]benzoxazol-5-yloxy}-(2-pyridyl))-N-methylcarboxamide
  参考文献：
  名称：

  Substituted benzazoles and methods of their use as inhibitors of Raf kinase

  摘要：

  提供了新的替代苯唑化合物、组合物和抑制人类或动物主体中Raf激酶活性的方法。这些新化合物组合物可以单独使用，也可以与至少一种额外药物结合，用于治疗由Raf激酶介导的疾病，如癌症。

  公开号：

  US20040122237A1

文献信息

• [EN] FUSED AZOLES SUCH AS 2,5-DISUBSTITUTED BENZIMIDAZOLES, BENZOXAZOLES AND BENZOTHIAZOLES AS KINASE INHIBITORS<br/>[FR] AZOLES FUSIONNES TELS QUE BENZIMIDAZOLES, BENZOXAZOLES ET BENZOTHIAZLES 2,5-DISUBSTITUES COMME INHIBITEURS DE KINASE
  申请人：AMGEN INC

  公开号：WO2004085425A1

  公开（公告）日：2004-10-07

  The invention relates to compounds of the formulae (I) to (III) wherein the substituents are as defined in the specification. These compounds have kinase inhibitory activity, such as VEGFR/KDR inhibitory activity. Accordingly, the compounds of the formulae (I) to (III) would be useful in the prevention and treatment of angiogenesis related disorders, ophthalmological conditions, proliferative diseases, inflammatory diseases, and other pathological conditions as described in the specification.

  这项发明涉及式(I)至(III)的化合物，其中取代基如规范中所定义。这些化合物具有激酶抑制活性，如VEGFR/KDR抑制活性。因此，式(I)至(III)的化合物在预防和治疗与血管生成相关的疾病、眼科疾病、增生性疾病、炎症性疾病以及规范中描述的其他病理状况中将会有用。
• Heterocyclic compounds and methods of use
  申请人：——

  公开号：US20040209892A1

  公开（公告）日：2004-10-21

  Selected compounds are effective for prophylaxis and treatment of diseases, such as angiogenesis mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.

  选定的化合物对于预防和治疗血管生成介导的疾病等疾病有效。本发明涵盖了新颖的化合物、类似物、前药和其药学上可接受的盐、药物组合物以及预防和治疗癌症等疾病和其他疾病或病况的方法。本发明还涉及制备这些化合物的过程以及在这些过程中有用的中间体。
• Substituted benz-azoles and methods of their use as inhibitors of Raf kinase
  申请人：——

  公开号：US20040087626A1

  公开（公告）日：2004-05-06

  New substituted benz-azole compounds, compositions and methods of inhibition of Raf kinase activity in a human or animal subject are provided. The new compounds compositions may be used either alone or in combination with at least one additional agent for the treatment of a Raf kinase mediated disorder, such as cancer.

  提供了新的取代苯并咪唑化合物、组合物和抑制人类或动物主体中Raf激酶活性的方法。这些新的化合物组合物可以单独使用或与至少一种其他药物联合使用，用于治疗Raf激酶介导的疾病，如癌症。
• SUBSTITUTED BENZ-AZOLES AND METHODS OF THEIR USE AS INHIBITORS OF RAF KINASE
  申请人：Amiri Payman

  公开号：US20100196368A1

  公开（公告）日：2010-08-05

  New substituted benz-azole compounds, compositions and methods of inhibition of Raf kinase activity in a human or animal subject are provided. The new compounds compositions may be used either alone or in combination with at least one additional agent for the treatment of a Raf kinase mediated disorder, such as cancer.

  本发明提供了新的取代苯并唑化合物、组合物和抑制人类或动物主体中Raf激酶活性的方法。新的化合物组成物可以单独使用或与至少一种其他药物联合使用，用于治疗Raf激酶介导的疾病，如癌症。
• Substituted benzazoles and methods of their use as inhibitors of raf kinase
  申请人：Novartis AG

  公开号：US08299108B2

  公开（公告）日：2012-10-30

  New substituted benz-azole compounds, compositions and methods of inhibition of Raf kinase activity in a human or animal subject are provided. The new compounds compositions may be used either alone or in combination with at least one additional agent for the treatment of a Raf kinase mediated disorder, such as cancer.

  提供了新的取代苯唑化合物、组成和抑制人或动物体内Raf激酶活性的方法。这些新化合物组成可以单独使用，也可以与至少一种额外的药物联合使用，用于治疗Raf激酶介导的疾病，如癌症。