2-[(3R)-3-aminopyrrolidin-1-yl]-5,6-dibromo-1-ethylbenzimidazole-4-carbonitrile

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯并咪唑类
• 英文名称: 2-[(3R)-3-aminopyrrolidin-1-yl]-5,6-dibromo-1-ethylbenzimidazole-4-carbonitrile
• 化学式: C₁₄H₁₅Br₂N₅
• 分子量: 413.11
• InChiKey: OZQBQIDAOBZZLL-MRVPVSSYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.6
• 重原子数：
  21
• 可旋转键数：
  2
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.43
• 拓扑面积：
  70.9
• 氢给体数：
  1
• 氢受体数：
  4

文献信息

• Novel Benzimidazole Derivatives as Kinase Inhibitors
  申请人：SELVITA S.A.

  公开号：US20150336967A1

  公开（公告）日：2015-11-26

  The present invention relates to derivatives of benzimidazoles of formula (I) as disclosed herein as well as pharmaceutical compositions comprising said derivatives. The derivates according to the present invention are serine/threonine and tyrosine kinase-inhibitors, particularly of PIM1-3- and DYRK1A-kinases and may particularly be used in the treatment of diseases linked to these kinases, such as e.g. leukemias, lymphomas, solid tumors and autoimmune disorders.

  本发明涉及公式（I）所披露的苯并咪唑衍生物，以及包含该衍生物的药物组合物。根据本发明的衍生物是丝氨酸/苏氨酸和酪氨酸激酶抑制剂，特别是PIM1-3和DYRK1A激酶的抑制剂，可以特别用于治疗与这些激酶相关的疾病，例如白血病、淋巴瘤、实体肿瘤和自身免疫性疾病。
• Benzimidazole derivatives as kinase inhibitors
  申请人：SELVITA S.A.

  公开号：US10174013B2

  公开（公告）日：2019-01-08

  The present invention relates to derivatives of benzimidazoles of formula (I) as disclosed herein as well as pharmaceutical compositions comprising said derivatives. The derivates according to the present invention are serine/threonine and tyrosine kinase-inhibitors, particularly of PIM1-3- and DYRK1A-kinases and may particularly be used in the treatment of diseases linked to these kinases, such as e.g. leukemias, lymphomas, solid tumors and autoimmune disorders.

  本发明涉及本文公开的式 (I) 苯并咪唑的衍生物以及包含上述衍生物的药物组合物。根据本发明的衍生物是丝氨酸/苏氨酸和酪氨酸激酶抑制剂，特别是 PIM1-3- 和 DYRK1A- 激酶的抑制剂，尤其可用于治疗与这些激酶有关的疾病，如白血病、淋巴瘤、实体瘤和自身免疫性疾病。
• NOVEL BENZIMIDAZOLE DERIVATIVES AS KINASE INHIBITORS
  申请人：SELVITA S.A.

  公开号：EP2935244A2

  公开（公告）日：2015-10-28
• US9388192B2
  申请人：——

  公开号：US9388192B2

  公开（公告）日：2016-07-12
• [EN] NOVEL BENZIMIDAZOLE DERIVATIVES AS KINASE INHIBITORS<br/>[FR] NOUVEAUX DÉRIVÉS DE BENZIMIDAZOLE EN TANT QU'INHIBITEURS DE LA KINASE
  申请人：SELVITA S A

  公开号：WO2014096388A2

  公开（公告）日：2014-06-26

  The present invention relates to derivatives of benzimidazoles of formula (I) as disclosed herein as well as pharmaceutical compositions comprising said derivatives. The derivates according to the present invention are serine/threonine and tyrosine kinase-inhibitors, particularly of PIM1-3-and DYRK1A-kinases and may particularly be used in the treatment of diseases linked to these kinases, such as e.g. leukemias, lymphomas, solid tumors and autoimmune disorders.