4,5,6,7-tetrabromo-2-(4-methylpiperazin-1-yl)-1H-benzimidazole | 1292820-03-1

• 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: 4,5,6,7-tetrabromo-2-(4-methylpiperazin-1-yl)-1H-benzimidazole
• 英文别名: TBIPIP；4,5,6,7-tetrabromo-2-(4-methylpiperazin-1-yl)-1H-benzo[d] imidazole
• CAS: 1292820-03-1
• 化学式: C₁₂H₁₂Br₄N₄
• 分子量: 531.87
• InChiKey: LETIRTMCWFAJRS-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.5
• 重原子数：
  20
• 可旋转键数：
  1
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.42
• 拓扑面积：
  35.2
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为产物：
  描述：

  N-甲基哌嗪 、 2,4,5,6,7-五溴-1H-苯并咪唑 以 乙醇 为溶剂， 反应 16.0h， 生成 4,5,6,7-tetrabromo-2-(4-methylpiperazin-1-yl)-1H-benzimidazole
  参考文献：
  名称：

  A compound, a process for its preparation, a pharmaceutical composition, use of a compound, a method for modulating or regulating serine/threonine kinases and a serine/threonine kinases modulating agent

  摘要：

  这些发明的主题是一种化合物，其制备方法，一种药物组合物，一种化合物的用途，一种调节丝氨酸/苏氨酸激酶的方法和丝氨酸/苏氨酸激酶调节剂。本发明涉及具有激酶抑制活性的新型小分子化合物，具有作为药物剂的优越性能，其生产方法及用途。具体而言，本发明涉及新型四溴苯并咪唑衍生物，具有丝氨酸/苏氨酸激酶抑制性质，优选来自Pim、HIPK、DYRK和CLK激酶组的，表现出优越的药理作用，并可用于治疗疾病状况，尤其是依赖于丝氨酸/苏氨酸激酶的癌症，如白血病和前列腺癌。

  公开号：

  EP2366695A1

文献信息

• A compound, a process for its preparation, a pharmaceutical composition, use of a compound, a method for modulating or regulating serine/threonine kinases and a serine/threonine kinases modulating agent
  申请人：SELVITA S.A.

  公开号：EP2366695A1

  公开（公告）日：2011-09-21

  The subject of the inventions are a compound, a process for its preparation, a pharmaceutical composition, use of a compound, a method for modulating or regulating serine/threonine kinases and a serine/threonine kinases modulating agent. The present invention relates to novel small-molecule compounds with kinase inhibitory activity, having superior properties as pharmaceutical agents, production method thereof and uses thereof. In particular, this invention relates to new derivatives of tetrabromobenzimidazole with serine/threonine kinases inhibitory properties, preferably selected from the group of Pim, HIPK, DYRK and CLK kinases, which exhibits superior pharmacological actions, and can be useful for the treatment of disease conditions, especially cancers depending on serine/threonine kinases, such as leukemias and prostate cancer.

  这些发明的主题是一种化合物，其制备方法，一种药物组合物，一种化合物的用途，一种调节丝氨酸/苏氨酸激酶的方法和丝氨酸/苏氨酸激酶调节剂。本发明涉及具有激酶抑制活性的新型小分子化合物，具有作为药物剂的优越性能，其生产方法及用途。具体而言，本发明涉及新型四溴苯并咪唑衍生物，具有丝氨酸/苏氨酸激酶抑制性质，优选来自Pim、HIPK、DYRK和CLK激酶组的，表现出优越的药理作用，并可用于治疗疾病状况，尤其是依赖于丝氨酸/苏氨酸激酶的癌症，如白血病和前列腺癌。
• DERIVATIVES OF TETRABROMOBENZIMIDAZOLE, A PROCESS FOR THE PREPARATION THEREOF, A PHARMACEUTICAL COMPOSITION COMPRISING THE SAME, A METHOF OF USING THE SAME, A METHOD FOR MODULATING OR REGULATING SERINE/THREONINE KINASES, AND SERINE/THREONINE KINASES MODULATING AGENT
  申请人：Brzozka Krzysztof

  公开号：US20110112091A1

  公开（公告）日：2011-05-12

  A derivative of tetrabromobenzimidazole, a process for the preparation thereof, a pharmaceutical composition, a method for using the same, a method for modulating or regulating serine/threonine kinases, and a serine/threonine kinases modulating agent. The invention relates to novel small-molecule compounds with kinase inhibitory activity, having superior properties as pharmaceutical agents, production method thereof and uses thereof. In particular, this invention relates to new derivatives of tetrabromobenzimidazole with Pim kinases inhibitory properties, which exhibits superior pharmacological actions, and can be useful for the treatment of disease conditions, especially cancers depending on Pim kinases, such as leukemias and prostate cancer.

  一种四溴苯并咪唑的衍生物，其制备方法，一种药物组合物，一种使用该衍生物的方法，一种调节丝氨酸/苏氨酸激酶的方法，以及一种丝氨酸/苏氨酸激酶调节剂。该发明涉及具有激酶抑制活性的新型小分子化合物，具有作为药物剂的优越性能，其生产方法和用途。具体而言，本发明涉及具有Pim激酶抑制性能的四溴苯并咪唑的新衍生物，表现出卓越的药理作用，并可用于治疗疾病，特别是依赖于Pim激酶的白血病和前列腺癌等癌症。
• DERIVATIVES OF TETRABROMOBENZIMIDAZOLE, A PROCESS FOR THE PREPARATION THEREOF, A PHARMACEUTICAL COMPOSITION COMPRISING THE SAME, A METHOD OF USING THE SAME, A METHOD FOR MODULATING OR REGULATING SERINE/THREONINE KINASES, AND SERINE/THREONINE KINASES MODULATING AGENT
  申请人：Brzozka Krzysztof

  公开号：US20110230481A2

  公开（公告）日：2011-09-22

  A derivative of tetrabromobenzimidazole, a process for the preparation thereof, a pharmaceutical composition, a method for using the same, a method for modulating or regulating serine/threonine kinases, and a serine/threonine kinases modulating agent. The invention relates to novel small-molecule compounds with kinase inhibitory activity, having superior properties as pharmaceutical agents, production method thereof and uses thereof. In particular, this invention relates to new derivatives of tetrabromobenzimidazole with Pim kinases inhibitory properties, which exhibits superior pharmacological actions, and can be useful for the treatment of disease conditions, especially cancers depending on Pim kinases, such as leukemias and prostate cancer.

  一种四溴苯并咪唑衍生物，其制备方法，制药组合物，使用方法，调节/调控丝氨酸/苏氨酸激酶的方法和丝氨酸/苏氨酸激酶调节剂。本发明涉及具有激酶抑制活性的新型小分子化合物，具有优越的药物特性，其生产方法和用途。特别是，本发明涉及四溴苯并咪唑的新衍生物，具有Pim激酶抑制性质，表现出优越的药理作用，并可用于治疗疾病，特别是依赖于Pim激酶的癌症，如白血病和前列腺癌。
• A COMPOUND, A PROCESS FOR ITS PREPARATION, A PHARMACEUTICAL COMPOSITION, USE OF A COMPOUND, A METHOD FOR MODULATING OR REGULATING SERINE/THREONINE KINASES AND A SERINE/THREONINE KINASES MODULATING AGENT
  申请人：SELVITA S.A.

  公开号：EP2499117B1

  公开（公告）日：2015-10-21
• COMPOUND, A PROCESS FOR ITS PREPARATION, A PHARMACEUTICAL COMPOSITION, USE OF A COMPOUND, A METHOD FOR MODULATING OR REGULATING SERINE/THREONINE KINASES AND A SERINE/THREONINE KINASES MODULATING AGENT
  申请人：BRZÓZKA Krzysztof

  公开号：US20120184535A1

  公开（公告）日：2012-07-19

  A compound, a process for its preparation, a pharmaceutical composition, use of a compound, a method for modulating or regulating serine/threonine and tyrosine kinases and a serine/threonine and tyrosine kinases modulating agent. Novel small-molecule compounds with kinase inhibitory activity, having superior properties as pharmaceutical agents, production method thereof and uses thereof. In particular, new derivatives of tetrahalogenated benzimidazole with serine/threonine and tyrosine kinases inhibitory properties, preferably selected from the group of PIM, HIPK, DYRK, CLK, CDK, FLT, PKG, Haspin, MER, TAO, MNK, TRK kinases which exhibit superior pharmacological actions, and can be useful for the treatment of disease conditions, especially cancers depending on serine/threonine and tyrosine kinases, such as but not limited to leukemias and solid tumors.