[2-(1H-Indol-3-yl)-ethyl]-(5-methyl-4-phenyl-thiazol-2-yl)-amine hydrobromide

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吲哚及其衍生物
• 英文名称: [2-(1H-Indol-3-yl)-ethyl]-(5-methyl-4-phenyl-thiazol-2-yl)-amine hydrobromide
• 英文别名: N-[2-(1H-indol-3-yl)ethyl]-5-methyl-4-phenyl-1,3-thiazol-2-amine;hydrobromide
• 化学式: BrH*C₂₀H₁₉N₃S
• 分子量: 414.369
• InChiKey: HXJUGRWDRUFJKQ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  5.83
• 重原子数：
  25
• 可旋转键数：
  5
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.15
• 拓扑面积：
  69
• 氢给体数：
  3
• 氢受体数：
  3

反应信息

• 作为产物：
  描述：

  2-溴苯丙酮 、 [2-(1H-吲哚-3-基)-乙基]-硫脲 以 甲醇 为溶剂， 反应 2.0h， 以94%的产率得到[2-(1H-Indol-3-yl)-ethyl]-(5-methyl-4-phenyl-thiazol-2-yl)-amine hydrobromide
  参考文献：
  名称：

  Five-membered heterocyclic compounds as inhibitors of SRC family protein kinase.

  摘要：

  本发明涉及公式（I）的新型取代芳香杂环衍生物，其中A、L1、L2、G、J、X和Y的定义如权利要求1所述。这些新型化合物对蛋白激酶的抑制具有用处，特别是对Src家族蛋白激酶的抑制。公开了通过将这些新型化合物与激酶接触来抑制激酶的方法。在另一实施方式中，本发明涉及含有这些新型化合物的药物组合物，以及它们用于制备用于治疗体内激酶非生理活性相关疾病或紊乱的药物，特别是用于癌症、免疫抑制和骨质疏松症的治疗。

  公开号：

  EP1555264A1

文献信息

• FIVE-MEMBERED HETEROCYCLIC COMPOUNDS AS INHIBITORS OF SRC FAMILY PROTEIN KINASE
  申请人：Sirenade Pharmaceuticals AG

  公开号：EP1709040A2

  公开（公告）日：2006-10-11
• [EN] KINASE INHIBITOR COMPOUNDS<br/>[FR] COMPOSES INHIBITEURS DE KINASES
  申请人：SIRENADE PHARMACEUTICALS AG

  公开号：WO2005068458A2

  公开（公告）日：2005-07-28

  The present invention refers to novel substituted aromatic heteroaryl derivatives of formula (I), with the definitions of a, L1, L2, G, J, X and Y according to claim 1. These novel compounds are useful for the inhibition of protein kinases, particularly of the inhibition of Src family protein kinases. Methods for inhibiting kinases by contacting kinases with these novel compounds are disclosed. In another embodiment the present invention refers to pharmaceutical compositions containing these novel compounds and their use of medicaments for treating diseases or disorders associated with unphysiological activity of kinases in the body, particularly for the treatment of cancer, immunosuppression, and osteoporosis.
• Five-membered heterocyclic compounds as inhibitors of SRC family protein kinase.
  申请人：Sireen AG

  公开号：EP1555264A1

  公开（公告）日：2005-07-20

  The present invention refers to novel substituted aromatic heteroaryl derivatives of formula (I). with the definitions of A, L1, L2, G, J, X and Y according to claim 1. These novel compounds are useful for the inhibition of protein kinases, particularly of the inhibition of Src family protein kinases. Methods for inhibiting kinases by contacting kinases with these novel compounds are disclosed. In another embodiment the present invention refers to pharmaceutical compositions containing these novel compounds and their use for the preparation of medicaments for treating diseases or disorders associated with unphysiological activity of kinases in the body, particularly for the treatment of cancer, immunosuppression, and osteoporosis.

  本发明涉及公式（I）的新型取代芳香杂环衍生物，其中A、L1、L2、G、J、X和Y的定义如权利要求1所述。这些新型化合物对蛋白激酶的抑制具有用处，特别是对Src家族蛋白激酶的抑制。公开了通过将这些新型化合物与激酶接触来抑制激酶的方法。在另一实施方式中，本发明涉及含有这些新型化合物的药物组合物，以及它们用于制备用于治疗体内激酶非生理活性相关疾病或紊乱的药物，特别是用于癌症、免疫抑制和骨质疏松症的治疗。