4-Hydroxynipecotic acid | 71609-37-5

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 哌啶类
• 英文名称: 4-Hydroxynipecotic acid
• 英文别名: (3R,4S)-4-hydroxypiperidine-3-carboxylic acid
• CAS: 71609-37-5
• 化学式: C₆H₁₁NO₃
• 分子量: 145.16
• InChiKey: DAMFVOCECLPLSI-UHNVWZDZSA-N

物化性质

• 沸点：
  346.0±42.0 °C(Predicted)
• 密度：
  1.299±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  -2.9
• 重原子数：
  10
• 可旋转键数：
  1
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.83
• 拓扑面积：
  69.6
• 氢给体数：
  3
• 氢受体数：
  4

文献信息

• Dopamine analog amide
  申请人：——

  公开号：US20010056116A1

  公开（公告）日：2001-12-27

  The invention involves the formation of a prodrug from a fatty acid carrier and a neuroactive drug. The prodrug is stable in the environment of both the stomach and the bloodstream and may be delivered by ingestion. The prodrug passes readily through the blood brain barrier. Once in the central nervous system, the prodrug is hydrolyzed into the fatty acid carrier and the drug to release the drug. In a preferred embodiment, the carrier is 4, 7, 10, 13, 16, 19 docosahexa-enoic acid and the drug is dopamine. Both are normal components of the central nervous system. The covalent bond between the drug and the carrier preferably is an amide bond, which bond may survive the conditions in the stomach. Thus, the prodrug may be ingested and will not be hydrolyzed completely into the carrier molecule and drug molecule in the stomach.

  该发明涉及使用脂肪酸载体和神经活性药物形成前药。该前药在胃和血液流动环境中稳定，并可通过口服递送。该前药容易穿过血脑屏障。一旦进入中枢神经系统，前药被水解成脂肪酸载体和药物以释放药物。在首选实施方式中，载体是4,7,10,13,16,19二十二碳六烯酸，药物是多巴胺。两者都是中枢神经系统的正常成分。药物和载体之间的共价键通常是酰胺键，这种键可以在胃的条件下存活。因此，前药可以被摄入，并且不会在胃中完全水解成载体分子和药物分子。
• ARYL PHENYLHETEROCYCLYL SULFIDE DERIVATIVES AND THEIR USE AS CELL ADHESION-INHIBITING ANTI-INFLAMMATORY AND IMMUNE-SUPPRESSIVE AGENTS
  申请人：Wang T. Gary

  公开号：US20070066585A1

  公开（公告）日：2007-03-22

  The present invention relates to novel heterocyclyl-containing diaryl sulfide compounds that are useful for treating inflammatory and immune diseases, to pharmaceutical compositions comprising these compounds, and to methods of inhibiting inflammation or suppressing immune response in a mammal.

  本发明涉及一种新的含杂环基的二芳基硫化物化合物，用于治疗炎症和免疫性疾病，包括包含这些化合物的制药组合物，以及在哺乳动物中抑制炎症或抑制免疫反应的方法。
• COMPOSITIONS FOR TREATING FREQUENT URINATION AND URINARY INCONTINENCE
  申请人：Takeda Chemical Industries, Ltd.

  公开号：EP1142584A1

  公开（公告）日：2001-10-10

  A GABA uptake inhibitor is useful in composition for treating urinary frequency and urinary incontinence.

  GABA 摄取抑制剂可用于治疗尿频和尿失禁。
• A method for treating tension-type headache
  申请人：HEADEXPLORER ApS

  公开号：EP1829539A2

  公开（公告）日：2007-09-05

  Tension-type headache is treated by interacting with neuronal transmission in relation to pain in connection with headache in a way which prevents or decreases sensitization of second order nociceptive neurons. In particular, treatment is performed by administration of an effective amount of a substance which prevents or decreases central sensitization. Important examples of such substances are substances which interact with glutamate neurotransmission, such as glutamate receptor antagonists, such as NMDA receptor antagonists, such as MK-801 or Amitriptylline or Imipramine or Desipramine or Mirtazaprine or Venlafaxine. Other examples are substances which interact with nitric oxide, such as nitric oxide synthase (NOS) inhibitors, such as L-NMMA or L-NAME or L-NIO or L-NNA. According to a broader aspect of the invention tension-type headache is treated by administration of substances which are effective in preventing or decreasing pain in connection with tension-type headache, such as the substances mentioned above. An additional aspect of the invention relates to treatment of tension-type headache by administration of substances which substantially inhibit the activity of nitric oxide synthase (NOS), such as NOS inhibitors, such as L-NMMA or L-NAME or L-NIO or L-NNA.

  治疗紧张型头痛的方法是，与头痛有关的疼痛神经元传递相互作用，防止或减少二阶痛觉神经元的敏化。具体来说，治疗方法是通过施用有效量的物质来防止或减少中枢敏化。这类物质的重要例子是与谷氨酸神经递质相互作用的物质，如谷氨酸受体拮抗剂，如NMDA受体拮抗剂，如MK-801或阿米替林或丙咪嗪或地西普胺或米氮平或文拉法辛。其他例子包括与一氧化氮相互作用的物质，如一氧化氮合酶（NOS）抑制剂，如L-NMMA或L-NAME或L-NIO或L-NNA。根据本发明更广泛的一个方面，治疗紧张型头痛的方法是施用能有效预防或减轻紧张型头痛相关疼痛的物质，如上述物质。本发明的另一个方面涉及通过施用实质上抑制一氧化氮合酶（NOS）活性的物质，如NOS抑制剂，如L-NMMA或L-NAME或L-NIO或L-NNA，来治疗紧张型头痛。
• 頻尿・尿失禁治療組成物
  申请人：武田薬品工業株式会社

  公开号：JP2000264848A

  公开（公告）日：2000-09-26

  (57)【要約】\n【課題】頻尿・尿失禁の予防・治療組成物の提供。\n【解決手段】ＧＡＢＡ取り込み阻害物質を含有してなる頻尿・尿失禁の予防・治療組成物。

  (57) [摘要]n[主题]提供预防和治疗尿频和尿失禁的组合物。\(58) [解决方案]一种用于预防和治疗尿频和尿失禁的组合物，包括一种 GABA 摄取抑制剂。