ALE 0540 | 234779-34-1

• 分子结构分类: 有机化合物 - 苯类化合物 - 萘
• 英文名称: ALE 0540
• 英文别名: 1H-Benz(de)isoquinoline-1,3(2H)-dione, 2-((2-hydroxyethyl)amino)-5-nitro-；2-(2-hydroxyethylamino)-5-nitrobenzo[de]isoquinoline-1,3-dione
• CAS: 234779-34-1
• 化学式: C₁₄H₁₁N₃O₅
• 分子量: 301.258
• InChiKey: SURCGQGDUADKBL-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.1
• 重原子数：
  22
• 可旋转键数：
  3
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.14
• 拓扑面积：
  116
• 氢给体数：
  2
• 氢受体数：
  6

反应信息

• 作为产物：
  描述：

  2-肼基乙醇 、 3-硝基-1,8-萘二甲酸酐 以 甲苯 为溶剂， 生成 ALE 0540
  参考文献：
  名称：

  Neurotrophin antagonist compositions

  摘要：

  一种药物组合物，包括I1式化合物，其中R1从以下选项中选择，包括烷基，芳基-低烷基，杂环-低烷基，低烷氧基羰基；可选择取代氨基；苯并咪唑-2-基；可选择取代的苯基；低烷基-(R5)(R6)其中R5和R6中的一个选择自H和另一个选择自羧基，羧基-低烷基和低烷氧羰基；NHCH2CH2OX其中X代表体内可水解的酯；R2和R3独立选择自H，NO2，卤素，二（低烷基）氨基，氰基，C（O）OH，苯基-S—，低烷基和Z（O）OR7其中Z选择自C和S，R7选择自H，低烷基氨基和芳基氨基；或其药学上可接受的盐或体内可水解的酯或酰胺，在有效抑制神经营养因子介导的活性的量和适当的载体中进行描述。该组合物可用于抑制某些神经退行性疾病状态中发生的神经元突起生长等不良神经营养因子介导的活性。

  公开号：

  US20020169182A1

文献信息

• Methods of modulating neurotrophin-mediated activity
  申请人：Babinski Kazimierz

  公开号：US20070093474A1

  公开（公告）日：2007-04-26

  Disclosed are compositions which modulate the interaction with nerve growth factor and precursors thereof with neurotrophic receptors. Also disclosed are methods of using the compositions of the invention, including methods of administration.

  本发明涉及一种调节神经生长因子及其前体与神经营养受体相互作用的组合物。本发明还涉及使用该组合物的方法，包括给药方法。
• NEUROTROPHIN ANTAGONISTS FOR THE TREATMENT OF EPILEPSY, ALZHEIMER'S DISEASE AND PAIN
  申请人：Allelix Biopharmaceuticals Inc.

  公开号：EP0930883B1

  公开（公告）日：2006-01-11
• NEUROTROPHIN ANTAGONIST COMPOSITIONS
  申请人：Allelix Biopharmaceuticals Inc.

  公开号：EP0930883A1

  公开（公告）日：1999-07-28
• METHODS OF MODULATING NEUROTROPHIN-MEDIATED ACTIVITY
  申请人：PainCeptor Pharma Corp.

  公开号：EP1931637A2

  公开（公告）日：2008-06-18
• PHARMACEUTICAL COMBINATIONS FOR IMMUNOTHERAPY
  申请人：Technische Universitat Dresden

  公开号：US20170189522A1

  公开（公告）日：2017-07-06

  The present invention relates generally to a method for regulating immune reactions and test substances useful for same. Specifically, the method of the present invention relates to the modulation of the nerve growth factor receptor p75 NTR , which is expressed by plasmacytoid dendritic cells. More specifically, the invention relates to a combination comprising at least one modulator of p75 NTR signalling selected from a p75 NTR antagonist or p75 NTR agonist and at least one TLR receptor agonist selected from an agonist of TLR7 and/or TLR9. The invention further relates to the use of a combination of antagonists and agonists of p75 NTR signalling and agonists of TLR7 and/or TLR9 as vaccine adjuvants and the invention provides vaccine compositions comprising antagonists and agonists of p75 NTR signalling and agonists of TLR7 and/or TLR9. The agonists and antagonists of p75 NTR signalling are useful in the manufacture of drugs for controlling cytokine function, antigen presentation, activation and proliferation of lymphocytes, which is important for the treatment of a range of conditions including cancer, inflammatory conditions, immunological disorders, growth disorders, infections and any other conditions involving p75 NTR signal transduction. The invention provides assays to screen for a range of agonists and antagonists of p75 NTR useful in modulating cytokine function, activation and proliferation of lymphocytes. The present invention further provides, therefore, screening assays for agonists and antagonists of p75NTR-modulated immune responses.