YH239-EE | 1364489-40-6

• 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: YH239-EE
• 英文别名: Ethyl 3-(2-(tert-butylamino)-1-(N-(4-chlorobenzyl)formamido)-2-oxoethyl)-6-chloro-1H-indole-2-carboxylate；ethyl 3-[2-(tert-butylamino)-1-[(4-chlorophenyl)methyl-formylamino]-2-oxoethyl]-6-chloro-1H-indole-2-carboxylate
• CAS: 1364489-40-6
• 化学式: C₂₅H₂₇Cl₂N₃O₄
• 分子量: 504.413
• InChiKey: OTUBDDRFPQLPKD-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  5.2
• 重原子数：
  34
• 可旋转键数：
  9
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.32
• 拓扑面积：
  91.5
• 氢给体数：
  2
• 氢受体数：
  4

文献信息

• p53-Mdm2 ANTAGONISTS
  申请人：Doemling Alexander

  公开号：US20140005386A1

  公开（公告）日：2014-01-02

  Novel p53-Mdm2 antogonists that conform to Formula I or to Formula II: where the prescribed substituent groups are defined, are useful in treating or preventing cancer. In particular, the compounds and their pharmaceutical compositions are useful for treating relapsed/refractory acute myeloid and lymphoid leukemia and refractory chronic lymphocytic leukemia/small cell lymphocytic lymphomas.

  符合公式I或公式II的新型p53-Mdm2拮抗剂，其中所规定的取代基团，可用于治疗或预防癌症。特别地，这些化合物及其药物组合物对于治疗复发/难治性急性髓系和淋巴系白血病以及难治性慢性淋巴细胞白血病/小细胞淋巴瘤非常有用。
• 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。
• P53-MDM2 ANTAGONISTS
  申请人：University of Pittsburgh - Of The Commonwealth System of Higher Education

  公开号：EP2614051A2

  公开（公告）日：2013-07-17
• METHODS OF TREATING CANCER
  申请人：Kartos Therapeutics, Inc.

  公开号：EP3787625A1

  公开（公告）日：2021-03-10
• METHODS AND COMPOSITIONS OF TREATING AN OPHTHALMIC CONDITION
  申请人：Kartos Therapeutics

  公开号：EP3927344A1

  公开（公告）日：2021-12-29