(S)-N-((S)-1-cyclohexyl-2-{(S)-2-[4-(4-fluoro-benzoyl)pyridin-2-yl]pyrrolidin-1-yl}-2-oxo-ethyl)-2-methylamino-propionamide | 1005342-68-6

• 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: (S)-N-((S)-1-cyclohexyl-2-{(S)-2-[4-(4-fluoro-benzoyl)pyridin-2-yl]pyrrolidin-1-yl}-2-oxo-ethyl)-2-methylamino-propionamide
• 英文别名: (S)-N-((S)-1-cyclohexyl-2-((S)-2-(4-(4-fluorobenzoyl)pyridin-2-yl)pyrrolidin-1-yl)-2-oxoethyl)-2-(methylamino)propanamide；(2S)-N-[(1S)-1-cyclohexyl-2-[(2S)-2-[4-(4-fluorobenzoyl)pyridin-2-yl]pyrrolidin-1-yl]-2-oxoethyl]-2-(methylamino)propanamide
• CAS: 1005342-68-6
• 化学式: C₂₈H₃₅FN₄O₃
• 分子量: 494.609
• InChiKey: UGFVRQRAWJKTLV-WDNCENIBSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.9
• 重原子数：
  36
• 可旋转键数：
  8
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.5
• 拓扑面积：
  91.4
• 氢给体数：
  2
• 氢受体数：
  6

文献信息

• Organic Compounds
  申请人：CHEN Zhuoliang

  公开号：US20110065726A1

  公开（公告）日：2011-03-17

  The present invention is directed to a compound of the formula: or pharmaceutically acceptable salts thereof and use of such compounds for treating proliferative diseases such as cancer, in mammals.

  本发明涉及一种化合物，其化学式为：或其药用可接受的盐，并且利用这些化合物来治疗哺乳动物中的增殖性疾病，如癌症。
• Organic compounds
  申请人：Novartis AG

  公开号：EP2537846A1

  公开（公告）日：2012-12-26

  The present invention is directed to compounds of the following formulae, which are intermediates in the synthesis of Smac peptidomimetics useful as IAP inhibitors: and

  本发明涉及以下式子的化合物，它们是合成可用作 IAP 抑制剂的 Smac 拟肽物的中间体： 和
• Immunomodulation by IAP Inhibitors
  申请人：Novartis AG

  公开号：EP2698158A1

  公开（公告）日：2014-02-19

  The present invention is directed to immune adjuvants containing IAP inhibitors, including Smac mimetics. The invention further provides pharmaceutical compositions and vaccines containing an IAP inhibitor and an antigen. Methods of enhancing an immune response by administration of an IAP inhibitor, methods of treating or preventing cancer, methods of treating or preventing infections, methods of treating autoimmune disorders, and methods of potentiating cytokine or antibody production are also provided.

  本发明涉及含有 IAP 抑制剂的免疫佐剂，包括 Smac 模仿剂。 本发明进一步提供了含有 IAP 抑制剂和抗原的药物组合物和疫苗。 本发明还提供了通过施用 IAP 抑制剂增强免疫反应的方法、治疗或预防癌症的方法、治疗或预防感染的方法、治疗自身免疫性疾病的方法以及增强细胞因子或抗体产生的方法。
• IMMUNOMODULATION BY IAP INHIBITORS
  申请人：Novartis AG

  公开号：EP3701947A1

  公开（公告）日：2020-09-02

  The present invention is directed to immune adjuvants containing IAP inhibitors, including Smac mimetics. The invention further provides pharmaceutical compositions and vaccines containing an IAP inhibitor and an antigen. Methods of enhancing an immune response by administration of an IAP inhibitor, methods of treating or preventing cancer, methods of treating or preventing infections, methods of treating autoimmune disorders, and methods of potentiating cytokine or antibody production are also provided.

  本发明涉及含有 IAP 抑制剂的免疫佐剂，包括 Smac 模仿剂。 本发明进一步提供了含有 IAP 抑制剂和抗原的药物组合物和疫苗。 本发明还提供了通过施用 IAP 抑制剂增强免疫反应的方法、治疗或预防癌症的方法、治疗或预防感染的方法、治疗自身免疫性疾病的方法以及增强细胞因子或抗体产生的方法。
• NOL3 is a predictor of patient outcome
  申请人：DANA-FARBER CANCER INSTITUTE, INC.

  公开号：US10329626B2

  公开（公告）日：2019-06-25

  The present invention features a method for determining the prognosis for survival of a cancer patient. Methods for measuring the level of NOL3 expression in a cancer cell-containing sample from a patient, and comparing the level of NOL3 expression in the sample to a reference level of NOL3 expression are also included. A higher level of NOL3 relative to the reference level correlates with decreased survival of the patient, and an equivalent or lower level of NOL3 relative to the reference level correlates with increased survival of the patient.

  本发明的特点是确定癌症患者生存预后的方法。还包括测量患者含癌细胞样本中 NOL3 表达水平的方法，以及将样本中 NOL3 表达水平与 NOL3 表达参考水平进行比较的方法。相对于参考水平较高的 NOL3 表达水平与患者存活率降低有关，而相对于参考水平较低的 NOL3 表达水平与患者存活率提高有关。