N-[6-Cyano-1,2,3,4-tetrahydro-1-(1H-imidazol-4-ylmethyl)-3-quinolinyl]-N-[(2,5-dimethylphenyl)methyl]benzenesulfonamide monohydrochloride | 219861-97-9

• 分子结构分类: 有机化合物 - 苯类化合物 - 四氢化萘
• 英文名称: N-[6-Cyano-1,2,3,4-tetrahydro-1-(1H-imidazol-4-ylmethyl)-3-quinolinyl]-N-[(2,5-dimethylphenyl)methyl]benzenesulfonamide monohydrochloride
• 英文别名: N-[6-cyano-1,2,3,4-tetrahydro-1-(1H-imidazol-4-ylmethyl)-3-quinolinyl]-N-[(2,5-dimethylphenyl)methyl]benzenesulfonamide hydrochloride；N-[6-cyano-1-(1H-imidazol-5-ylmethyl)-3,4-dihydro-2H-quinolin-3-yl]-N-[(2,5-dimethylphenyl)methyl]benzenesulfonamide;hydrochloride
• CAS: 219861-97-9
• 化学式: C₂₉H₂₉N₅O₂S*ClH
• 分子量: 548.108
• InChiKey: YQBUEWAYUFCCNF-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  5.14
• 重原子数：
  38
• 可旋转键数：
  7
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.24
• 拓扑面积：
  102
• 氢给体数：
  2
• 氢受体数：
  6

文献信息

• Methods for the treatment of synucleinopathies
  申请人：Lansbury T. Peter

  公开号：US20050272722A1

  公开（公告）日：2005-12-08

  Methods are provided of treating synucleinopathies, such as Parkinson's Disease, Diffuse Lewy Body Disease and Multiple System Atrophy, comprising administering to a synucleinopathic subject a farnesyl transferase inhibitor compound.

  提供了一种治疗突触核蛋白病的方法，例如帕金森病、弥漫性Lewy体病和多系统萎缩症，包括向突触核蛋白病患者施用一种法尼酰转移酶抑制剂化合物。
• 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。
• EP0994856A4
  申请人：——

  公开号：EP0994856A4

  公开（公告）日：2000-12-06
• INHIBITORS OF FARNESYL PROTEIN TRANSFERASE
  申请人：BRISTOL-MYERS SQUIBB COMPANY

  公开号：EP0994856A1

  公开（公告）日：2000-04-26
• TREATMENT OF LYSOSOMAL STORAGE DISEASES
  申请人：Link Medicine Corporation

  公开号：EP2155197A2

  公开（公告）日：2010-02-24