2E5Qzb8rzj | 345915-21-1

• 分子结构分类: 有机化合物 - 苯丙烷和聚酮 - 二苯乙烯类
• 英文名称: 2E5Qzb8rzj
• 英文别名: (2S)-2-[[2-[2-(4-fluorophenyl)ethyl]-5-[[(2S,4S)-4-sulfanylpyrrolidin-2-yl]methylamino]benzoyl]amino]-4-methylsulfanylbutanoic acid
• CAS: 345915-21-1
• 化学式: C₂₅H₃₂FN₃O₃S₂
• 分子量: 505.7
• InChiKey: DFWZXAKLXQQLPG-FUDKSRODSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2
• 重原子数：
  34
• 可旋转键数：
  12
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.44
• 拓扑面积：
  117
• 氢给体数：
  5
• 氢受体数：
  8

文献信息

• Farnesyl transferase inhibitors
  申请人：——

  公开号：US20030083348A1

  公开（公告）日：2003-05-01

  1 This invention relates to compounds of formula (1) that inhibit farnesylation of gene products through inhibition of the enzyme farnesyl-protein transferase (FPTase). The invention also relates to methods of manufacturing the compounds, pharmaceutical compositions and methods of treating diseases, especially cancer, which are mediated through farnesylation.

  这项发明涉及抑制法尼基化酶（FPTase）从而抑制基因产物法尼基化的公式（1）化合物的制备方法。该发明还涉及制造这些化合物、药物组合物以及治疗特别是通过法尼基化介导的癌症等疾病的方法。
• TREATMENT OF PROTEINOPATHIES USING A FARNESYL TRANSFERASE INHIBITOR
  申请人：Lansbury, JR. Peter T.

  公开号：US20110294794A1

  公开（公告）日：2011-12-01

  Methods and pharmaceutical compositions comprising a low dose of a farnesyl transferase inhibitor useful in the treatment of proteinopathies are provided. These low doses are below the doses used in oncological treatments for which these compounds were initially designed. The treatment includes administering to a subject in need thereof a therapeutically effective amount of a farnesyl transferase inhibitor, wherein the amount is effective to inhibit the farnesylation of a non-Ras FTase substrate involved in the autophagy pathway without substantially affecting the farnesylation of Ras or other oncology related substrates. Treatments in accordance with the present invention may also include an acetylcholinesterase inhibitor, an activator of neurotrophic receptors, an NMDA anatagonist, an amyloid deposit inhibitor, an antipsychotic agent, an antidepressant, an anxiolytic, or an antioxidant.

  本发明提供了一种低剂量法尼醇转移酶抑制剂及其制药组合物，用于治疗蛋白病。这些低剂量低于最初设计这些化合物用于肿瘤治疗所使用的剂量。治疗包括向需要治疗的受体中注射治疗有效量的法尼醇转移酶抑制剂，其中该量能够有效抑制参与自噬通路的非Ras FTase底物的法尼酰化，而不会对Ras或其他与肿瘤相关的底物的法尼酰化产生明显影响。按照本发明的治疗方法还可以包括乙酰胆碱酯酶抑制剂、神经营养因子受体激活剂、NMDA拮抗剂、淀粉样沉积抑制剂、抗精神病药物、抗抑郁药物、抗焦虑药物或抗氧化剂。
• FARNESYL TRANSFERASE INHIBITORS
  申请人：AstraZeneca AB

  公开号：EP1255733B1

  公开（公告）日：2006-01-18
• Treatment of Lysosomal Storage Diseases
  申请人：Grammatopoulos Tom

  公开号：US20100184803A1

  公开（公告）日：2010-07-22

  Methods and compositions useful in the treatment or prevention of lysosomal storage diseases, such as Pompe's disease, Fabry's disease, Gaucher's disease, and Niemann-Pick disease, are provided. The treatment includes administering to a subject a farnesyl transferase inhibitor compound. The treatment may also include enzyme replacement therapy or gene therapy.
• Treatment of Synucleinopathies
  申请人：Justman Craig J.

  公开号：US20110136867A1

  公开（公告）日：2011-06-09

  Methods and compositions useful in the treatment or prevention of synucleinopathies, such as Parkinson's Disease, Diffuse Lewy Body Disease, and Multiple System Atrophy, or other neurodegenerative diseases are provided. The treatment including administering to a subject a farnesyl transferase inhibitor compound.