3-(2-Methyl-5-nitro-imidazol-1-yl)-N-(2,2,2-trichloro-1-phenylamino-ethyl)-propionamide

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 唑类
• 英文名称: 3-(2-Methyl-5-nitro-imidazol-1-yl)-N-(2,2,2-trichloro-1-phenylamino-ethyl)-propionamide
• 英文别名: N-(1-anilino-2,2,2-trichloroethyl)-3-(2-methyl-5-nitroimidazol-1-yl)propanamide
• 化学式: C15H16Cl3N5O3
• 分子量: 420.7
• InChiKey: JGLRKOAHBXAHCU-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4
• 重原子数：
  26
• 可旋转键数：
  6
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.33
• 拓扑面积：
  105
• 氢给体数：
  2
• 氢受体数：
  5

文献信息

• METHOD FOR DETERMINING PARP INHIBITOR RESPONSIVENESS AND IMPROVING PARP INHIBITOR THERAPY
  申请人：Universität Zürich

  公开号：EP3822637A1

  公开（公告）日：2021-05-19

  The invention relates to a method for determining the responsiveness of a patient's tumour disease to treatment by administration of a PARP inhibitor. The method comprising the steps of determining a level of TRIP12 protein and/or a level of an mRNA encoding TRIP12 protein, or the presence of a TRIP12 mutation, and comparing the TRIP12 expression level and/or the TRIP12 activity level with a threshold value, and assigning to said tumour disease a likelihood of responsiveness. The invention further relates to a PARP inhibitor for use in treatment of a tumour disease associated with a level of TRIP12 expression lower than a threshold, or to a PARP inhibitor for use in treatment of a tumour disease administered concomitant with or after administration of an ubiquitin ligase inhibitor and/or a nucleic acid agent capable of decreasing or inhibiting or blocking TRIP12 expression.

  本发明涉及一种确定患者肿瘤疾病对给予 PARP 抑制剂治疗的反应性的方法。该方法包括以下步骤：确定TRIP12蛋白的水平和/或编码TRIP12蛋白的mRNA的水平，或TRIP12突变的存在，以及将TRIP12表达水平和/或TRIP12活性水平与阈值进行比较，并给所述肿瘤疾病分配反应性的可能性。 本发明进一步涉及一种用于治疗与TRIP12表达水平低于阈值相关的肿瘤疾病的PARP抑制剂，或涉及一种用于治疗肿瘤疾病的PARP抑制剂，该PARP抑制剂与泛素连接酶抑制剂和/或能够降低或抑制或阻断TRIP12表达的核酸制剂同时给药或在给药后给药。
• [EN] METHOD FOR DETERMINING PARP INHIBITOR RESPONSIVENESS, AND IMPROVED PARP INHIBITOR THERAPY<br/>[FR] MÉTHODE DE DÉTERMINATION DE LA RÉACTIVITÉ D'UN INITIATEUR DE PARP, ET TRAITEMENT AMÉLIORÉ D'UN INITIATEUR DE PARP
  申请人：UNIV ZUERICH

  公开号：WO2021094426A1

  公开（公告）日：2021-05-20

  The invention relates to a method for determining the responsiveness of a patient's tumour disease to treatment by administration of a PARP inhibitor. The method comprising the steps of determining an expression level of TRIP12 biomarker protein and/or a level of an mRNA encoding biomarker protein, or the presence of a TRIP12 mutation, and comparing the TRIP12 biomarker expression and/or activity level with a threshold value, and assigning to said tumour disease a likelihood of responsiveness. The invention further relates to a PARP inhibitor for use in treatment of a tumour disease associated with a level of TRIP12 expression lower than a threshold, or to a PARP inhibitor for use in treatment of a tumour disease administered concomitant with or after administration of an ubiquitin ligase inhibitor and/or a nucleic acid agent capable of decreasing or inhibiting or blocking TRIP12 expression.