2-(3-pyridyl)-N-(2,2-diphenyl-ethyl)-N-((cis)-3-sulfanylpyrrolidin-2-ylmethyl)acetamide

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: 2-(3-pyridyl)-N-(2,2-diphenyl-ethyl)-N-((cis)-3-sulfanylpyrrolidin-2-ylmethyl)acetamide
• 英文别名: N-(2,2-diphenylethyl)-2-pyridin-3-yl-N-[[(2S,3S)-3-sulfanylpyrrolidin-2-yl]methyl]acetamide
• 化学式: C₂₆H₂₉N₃OS
• 分子量: 431.602
• InChiKey: WQNXJGZWLMGOST-DQEYMECFSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.8
• 重原子数：
  31
• 可旋转键数：
  8
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.31
• 拓扑面积：
  46.2
• 氢给体数：
  2
• 氢受体数：
  4

文献信息

• 3-Mercaptopyrrolidines as farnesyl protein transferase inhibitors
  申请人：Boyle Thomas Francis

  公开号：US20050209217A1

  公开（公告）日：2005-09-22

  The present invention relats to inhibitors of ras farnesylation of Formula (I) wherein: R 1 is for example H and further values as defined in the specification; R 2 is for example H and further values as defined in the specification; R 3 is for example H or a substituent having values as defined in the specification; p is 0-3 in which R 3 values can be the same or different; L is a linking moiety for example —CH 2 —NH— and further values as defined in the specification; A is selected from phenyl; naphthyl; a 5-10 membered monocyclic or bicyclic heteroaryl ring containing up to 5 heteroatoms where the heteroatoms are independently selected from O, N and S; or a —S—S— dimer thereof when R 2 =H; or a N-oxide or a pharmaceutically-acceptable salt, prodrug or solvate thereof. Processes for their preparation, their use as therapeutic agents and pharmaceutical compositions containing them. A particular use is in cancer therapy.

  本发明涉及 Formula (I) 的 ras 泛酰化抑制剂，其中：R1 例如为 H，以及在规范中定义的进一步数值；R2 例如为 H，以及在规范中定义的进一步数值；R3 例如为 H 或具有在规范中定义的数值的取代基；p 为 0-3，其中 R3 的数值可以相同也可以不同；L 是一个连接基团，例如 —CH2—NH—，以及在规范中定义的进一步数值；A 选自苯基；萘基；一个含有最多 5 个杂原子的 5-10 成员单环或双环杂芳基环，其中杂原子独立地选自 O、N 和 S；或者当 R2=H 时的一个 —S—S— 二聚体；或者其 N-氧化物或药用可接受的盐、前药或溶剂。它们的制备方法，作为治疗剂的用途以及含有它们的药物组合物。一个特定用途是在癌症治疗中。
• Compounds which inhibits protein prenylation ( e.g. geranylgeranyltransferase or farnesyltransferase inhibitors) for treating Parkinson's disease
  申请人：Exonhit Therapeutics SA

  公开号：EP1656931A1

  公开（公告）日：2006-05-17

  The invention relates to compounds and their uses, particularly in the pharmaceutical industry. The invention more specifically relates to new uses of compounds that inhibit the prenylation of proteins, in particular the geranylgeranyl and/or farnesyl modifications of proteins, for treating neurodegeneration involving oxidative stress and, more particularly, Parkinson's disease. The invention also relates to corresponding methods of treatment, and can be used in human subjects for preventive or curative treatment, either alone or in combination with other active agents or treatments.

  本发明涉及化合物及其用途，尤其是在制药业中的用途。本发明更具体地涉及抑制蛋白质的前酰化，特别是抑制蛋白质的香叶基和/或法呢基修饰的化合物的新用途，用于治疗涉及氧化应激的神经变性，特别是帕金森病。本发明还涉及相应的治疗方法，可用于人体的预防或治疗，可单独使用，也可与其他活性剂或治疗方法联合使用。
• 3-MERCAPTOPYRROLIDINES AS FARNESYL PROTEIN TRANSFERASE INHIBITORS
  申请人：ZENECA LIMITED

  公开号：EP0923545A1

  公开（公告）日：1999-06-23
• COMPOUNDS WHICH INHIBITS PROTEIN PRENYLATION E.G. GERANYLGERANYLTRANSFERASE OR FARNESYLTRANSFERASE INHIBITORS FOR TREATING PARKINSON'S DISEASE
  申请人：Exonhit Therapeutics SA

  公开号：EP1811984A1

  公开（公告）日：2007-08-01
• Compounds Which Inhibits Protein Prenylation E.G. Geranylgeransferse or Farnesyltransferase Inhibitors for Treating Parkinson's Disease
  申请人：Schweighoffer Fabien

  公开号：US20080153758A1

  公开（公告）日：2008-06-26

  The invention relates to compounds and their uses, particularly in the pharmaceutical industry. The invention more specifically relates to new uses of compounds that inhibit the prenylation of proteins, in particular the geranylgeranyl and/or farnesyl modifications of proteins, for treating neurodegeneration involving oxidative stress and, more particularly, Parkinson's disease. The invention also relates to corresponding methods of treatment, and can be used in human subjects for preventive or curative treatment, either alone is or in combination with other active agents or treatments.