Piperazine, 1-methyl-4-[4-(phenylmethyl)phenyl]- | 831226-51-8

• 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: Piperazine, 1-methyl-4-[4-(phenylmethyl)phenyl]-
• 英文别名: 1-(4-benzylphenyl)-4-methylpiperazine
• CAS: 831226-51-8
• 化学式: C₁₈H₂₂N₂
• 分子量: 266.4
• InChiKey: UDPPHFGUOMVFNH-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.8
• 重原子数：
  20
• 可旋转键数：
  3
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.33
• 拓扑面积：
  6.5
• 氢给体数：
  0
• 氢受体数：
  2

文献信息

• Small molecule toll-like receptor (TLR) antagonists
  申请人：Lipford B. Grayson

  公开号：US20070232622A1

  公开（公告）日：2007-10-04

  The invention provides methods and compositions useful for modulating signaling through Toll-like receptors. The methods involve contacting a TLR-expressing cell with a small molecule having a core structure including at least two rings. Certain of the compounds are 4-primary amino quinolines. Many of the compounds and methods are useful specifically for inhibiting immune stimulation involving at least one of TLR9, TLR8, TLR7, and TLR3. The methods may have use in the treatment of autoimmunity, inflammation, allergy, asthma, graft rejection, graft versus host disease, infection, sepsis, cancer, and immunodeficiency.

  本发明提供了用于调节通过Toll样受体信号传导的方法和组合物。该方法涉及使用一个包含至少两个环的核心结构的小分子接触TLR表达的细胞。其中某些化合物是4-主氨基喹啉。许多化合物和方法特别适用于抑制至少一个TLR9、TLR8、TLR7和TLR3的免疫刺激。该方法可能在治疗自身免疫、炎症、过敏、哮喘、移植排斥、移植物抗宿主病、感染、败血症、癌症和免疫缺陷方面有用。
• COMPOSITIONS AND METHODS FOR TREATING NEURODEGENERATIVE DISEASE
  申请人：Catalano Susan M.

  公开号：US20140378460A1

  公开（公告）日：2014-12-25

  This invention relates to the use sigma-2 receptor antagonists, and of pharmaceutical compositions comprising such compounds, in methods for inhibiting Abeta-associated synapse loss or synaptic dysfunction in neuronal cells, modulating an Abeta-associated membrane trafficking change in neuronal cells, and treating cognitive decline associated with Abeta pathology and more broadly treating with such compounds and compositions neurodegenerative diseases and disorders associated with Abeta pathology. This invention also relates to methods for screening compounds for activity in inhibiting cognitive decline on the basis of their ability to bind to a sigma-2 receptor.

  本发明涉及使用sigma-2受体拮抗剂及包含这种化合物的药物组合物，用于抑制神经元细胞中Abeta相关突触丢失或突触功能障碍，调节神经元细胞中Abeta相关的膜转运变化，以及治疗与Abeta病理相关的认知衰退，更广泛地使用这种化合物和组合物治疗与Abeta病理相关的神经退行性疾病和障碍。本发明还涉及通过它们与sigma-2受体结合的能力来筛选具有抑制认知衰退活性的化合物的方法。
• Biphenylderivatives, process for their preparation and their use as medicaments
  申请人：Eisai Co., Ltd.

  公开号：EP0675118B1

  公开（公告）日：2002-10-09
• US7410975B2
  申请人：——

  公开号：US7410975B2

  公开（公告）日：2008-08-12
• [EN] COMPOSITIONS AND METHODS FOR TREATING NEURODEGENERATIVE DISEASE<br/>[FR] COMPOSITIONS ET MÉTHODES DE TRAITEMENT DE MALADIES NEURODÉGÉNÉRATIVES
  申请人：COGNITION THERAPEUTICS INC

  公开号：WO2013029060A2

  公开（公告）日：2013-02-28

  This invention relates to the use sigma-2 receptor antagonists, and of pharmaceutical compositions comprising such compounds, in methods for inhibiting Abeta- associated synapse loss or synaptic dysfunction in neuronal cells, modulating an Abeta-associated membrane trafficking change in neuronal cells, and treating cognitive decline associated with Abeta pathology and more broadly treating with such compounds and compositions neurodegenerative diseases and disorders associated with Abeta pathology. This invention also relates to methods for screening compounds for activity in inhibiting cognitive decline on the basis of their ability to bind to a sigma-2 receptor.