7,7-difluorospermidine | 117659-32-2

• 分子结构分类: 有机化合物 - 有机氮化合物
• 英文名称: 7,7-difluorospermidine
• 英文别名: 7,7-difluoro-1,8-diamino-4-aza-octane；1,4-Butanediamine, N4-(3-aminopropyl)-2,2-difluoro-；N'-(3-aminopropyl)-2,2-difluorobutane-1,4-diamine
• CAS: 117659-32-2
• 化学式: C₇H₁₇F₂N₃
• 分子量: 181.229
• InChiKey: QOWHBRZUSJBWAI-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -0.7
• 重原子数：
  12
• 可旋转键数：
  7
• 环数：
  0.0
• sp3杂化的碳原子比例：
  1.0
• 拓扑面积：
  64.1
• 氢给体数：
  3
• 氢受体数：
  5

反应信息

• 作为产物：
  描述：

  1,8-Diamino-4-p-toluenesulfonyl-7,7-difluoro-4-aza-octane 在 乙醚 、 氢溴酸 、 2,2-Difluoro-7-hydrazinylheptan-1-amine 、 trihydrobromide 、 丙酮 作用下， 以 氢溴酸 为溶剂， 反应 20.0h， 生成 7,7-difluorospermidine
  参考文献：
  名称：

  Gem-dihalo-1, 8-diamino-4-aza-octanes

  摘要：

  Gem-dihalo-1,8-diamino-4-aza-octane衍生物可用作抗增生或抗肿瘤剂。

  公开号：

  US04914240A1

文献信息

• Use of difluoromethylornithine (DFMO) for the treatment of amyotrophic lateral sclerosis
  申请人：——

  公开号：US20030130350A1

  公开（公告）日：2003-07-10

  The present invention provides methods and compositions for modulating polyamine pathway activity as a means for ameliorating neurodegenarative disorders. In particular, for ameliorating the symptoms or onset of amyotrophic lateral sclerosis (ALS) by modulating the gene and protein products involved the polyamine pathway, such as by inhibiting the enzyme, ornithine decarboxylase (ODC), involved in the synthesis of the polyamine, putrescine. Compositions and methods are disclosed for inhibiting the polyamine pathway producing lower polyamine levels resulting in a beneficial effect on ALS. This can be accomplished by using modulating agents such as analogs, or polyamine analogs, and antiproliferative drugs. In particular, the ODC inhibitor difuoromethylornithine (DFMO) is disclosed as a useful pharmacological agent in the modulation and treatment of ALS. Screening assays for pharmacological agents that are capable of decreasing polyamine levels and/or reducing cell proliferation are also disclosed.

  本发明提供了调节多胺通路活性的方法和组合物，作为改善神经变性疾病的一种手段。特别是，通过调节涉及多胺途径的基因和蛋白质产物，例如通过抑制参与合成多胺--腐胺的酶--鸟氨酸脱羧酶（ODC），来改善肌萎缩性脊髓侧索硬化症（ALS）的症状或发病。已公开的组合物和方法可抑制多胺途径，降低多胺水平，从而对 ALS 产生有益影响。这可以通过使用类似物或多胺类似物等调节剂以及抗增生药物来实现。特别是，ODC 抑制剂二氟甲基鸟氨酸（DFMO）作为一种有用的药理制剂被公开用于 ALS 的调节和治疗。此外，还公开了能够降低多胺水平和/或减少细胞增殖的药剂筛选试验。
• Use of polyamine analogs for amyotrophic lateral sclerosis
  申请人：——

  公开号：US20030130357A1

  公开（公告）日：2003-07-10

  The present invention provides methods and compositions for modulating polyamine pathway activity as a means for ameliorating neurodegenarative disorders. In particular, for ameliorating the symptoms or onset of amyotrophic lateral sclerosis (ALS) by modulating the gene and protein products involved the polyamine pathway, such as by inhibiting the enzyme, ornithine decarboxylase (ODC), involved in the synthesis of the polyamine, putrescine. Compositions and methods are disclosed for inhibiting the polyamine pathway producing lower polyamine levels resulting in a beneficial effect on ALS. This can be accomplished by using modulating agents such as analogs, or polyamine analogs, and antiproliferative drugs. In particular, the polyamine analog N(1),N(11)-diethylnorspermine (DENSPM) is disclosed as a useful modulating agent in the treatment of ALS. Screening assays for pharmacological agents that are capable of decreasing polyamine levels and/or reducing cell proliferation are also disclosed.

  本发明提供了调节多胺通路活性的方法和组合物，作为改善神经变性疾病的一种手段。特别是，通过调节涉及多胺途径的基因和蛋白质产物，例如通过抑制参与合成多胺--腐胺的酶--鸟氨酸脱羧酶（ODC），来改善肌萎缩性脊髓侧索硬化症（ALS）的症状或发病。已公开的组合物和方法可抑制多胺途径，降低多胺水平，从而对 ALS 产生有益影响。这可以通过使用类似物或多胺类似物和抗增生药物等调节剂来实现。特别是，多胺类似物N(1),N(11)-二乙基去甲精胺（DENSPM）被公开为治疗ALS的有用调节剂。此外，还公开了能够降低多胺水平和/或减少细胞增殖的药剂的筛选试验。
• Treatment of neurodegenerative disorders through the modulation of the polyamine pathway
  申请人：——

  公开号：US20030158262A1

  公开（公告）日：2003-08-21

  The present invention provides methods and compositions for modulating polyamine pathway activity as a means for ameliorating neurodegenarative disorders. In particular, for ameliorating the symptoms or onset of amyotrophic lateral sclerosis (ALS) by modulating the gene and protein products involved the polyamine pathway, such as by inhibiting the enzyme, ornithine decarboxylase (ODC), involved in the synthesis of the polyamine, putrescine. Compositions and methods are disclosed for inhibiting the polyamine pathway producing lower polyamine levels resulting in a beneficial effect on ALS. This can be accomplished by using modulating agents such as analogs, or polyamine analogs, and antiproliferative drugs. Screening assays for pharmacological agents that are capable of decreasing polyamine levels and/or reducing cell proliferation are also disclosed.

  本发明提供了调节多胺通路活性的方法和组合物，作为改善神经变性疾病的一种手段。特别是，通过调节涉及多胺途径的基因和蛋白质产物，例如通过抑制参与合成多胺--腐胺的酶--鸟氨酸脱羧酶（ODC），来改善肌萎缩性脊髓侧索硬化症（ALS）的症状或发病。已公开的组合物和方法可抑制多胺途径，降低多胺水平，从而对 ALS 产生有益影响。这可以通过使用类似物或多胺类似物等调节剂以及抗增生药物来实现。此外，还公开了能够降低多胺水平和/或减少细胞增殖的药剂的筛选试验。
• Gem-dihalo-1,8-diamino-4-aza-octanes
  申请人：MERRELL DOW PHARMACEUTICALS INC.

  公开号：EP0215319B1

  公开（公告）日：1991-10-16
• GERHART, FRITZ;MAMONT, PIERRE
  作者：GERHART, FRITZ、MAMONT, PIERRE

  DOI：——

  日期：——