(4S)-2-[2,4-bis(trideuteriomethoxy)pyrimidin-5-yl]-5-(5-chloro-1-methyl-2-oxopyridin-3-yl)-4-(4-chlorophenyl)-3-[(2R)-1-methoxypropan-2-yl]-4H-pyrrolo[3,4-d]imidazol-6-one

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 羧酸及其衍生物
• 英文名称: (4S)-2-[2,4-bis(trideuteriomethoxy)pyrimidin-5-yl]-5-(5-chloro-1-methyl-2-oxopyridin-3-yl)-4-(4-chlorophenyl)-3-[(2R)-1-methoxypropan-2-yl]-4H-pyrrolo[3,4-d]imidazol-6-one
• 化学式: C27H26Cl2N6O5
• 分子量: 591.5
• InChiKey: XFVPAUGALMSDDA-NLTVXINZSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.1
• 重原子数：
  40
• 可旋转键数：
  8
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.3
• 拓扑面积：
  112
• 氢给体数：
  0
• 氢受体数：
  8

文献信息

• IMIDAZOPYRROLIDINONE COMPOUNDS
  申请人：NOVARTIS AG

  公开号：US20140011798A1

  公开（公告）日：2014-01-09

  The invention relates to compounds of formula (I): as described herein, pharmaceutical preparations comprising such compounds, uses and methods of use for such compounds in the treatment of a disorder or a disease mediated by the activity of MDM2 and/or MDM4, and combinations comprising such compounds.

  本发明涉及式（I）的化合物，如本文所述，包括这些化合物的药物制剂，以及在治疗由MDM2和/或MDM4活性介导的疾病或疾病中使用这些化合物的用途和使用方法，以及包含这些化合物的组合物。
• GDF-15 as a haematological toxicity biomarker
  申请人：Novartis AG

  公开号：US10935540B2

  公开（公告）日：2021-03-02

  The present disclosure relates to use of GDF-15 as a safety biomarker for determining a toxicological effect of a Mdm2 inhibitor; an ex vivo method for determining a toxicological effect of a Mdm2 inhibitor in a subject, in particular for determining a likelihood of developing thrombocytopenia in a subject in response to administration of a dose of a Mdm2 inhibitor; methods of using a Mdm2 inhibitor in the treatment of cancer in a subject; a kit for use in predicting the likelihood that a patient having cancer will develop thrombocytopenia in response to a treatment with a dose of a Mdm2 inhibitor; a kit for use in treating a patient having cancer and related disclosure embodiments.

  本公开涉及使用GDF-15作为确定Mdm2抑制剂毒理学效应的安全性生物标志物；一种用于确定Mdm2抑制剂对受试者的毒理学效应的体内外方法，特别是用于确定受试者因服用一定剂量的Mdm2抑制剂而发生血小板减少症的可能性；使用Mdm2抑制剂治疗受试者癌症的方法；用于预测癌症患者在接受一定剂量的Mdm2抑制剂治疗后发生血小板减少的可能性的试剂盒；用于治疗癌症患者的试剂盒以及相关的公开实施方案。
• Dose and regimen for HDM2-p53 interaction inhibitors
  申请人：Novartis AG

  公开号：US10966978B2

  公开（公告）日：2021-04-06

  The present invention relates to HDM2-p53 interaction inhibitors for use in the treatment of cancer, wherein the drug is administered by a high dose intermittent dosing regimen. The present invention relates in particular to the HDM2-p53 interaction inhibitor HDM20I and the dosing regimen di, d8 of a 4 week cycle.

  本发明涉及用于治疗癌症的HDM2-p53相互作用抑制剂，其中通过大剂量间歇给药方案给药。本发明尤其涉及HDM2-p53相互作用抑制剂HDM20I和4周周期的di、d8给药方案。
• INTERMITTENT DOSING OF MDM2 INHIBITOR
  申请人：Novartis AG

  公开号：EP3160463B1

  公开（公告）日：2020-10-21
• GDF-15 AS A HAEMATOLOGICAL TOXICITY BIOMARKER
  申请人：Novartis AG

  公开号：EP3332252A1

  公开（公告）日：2018-06-13