4-Methyl-11-oxa-4-azatetracyclo[8.6.1.01,12.06,17]heptadeca-6(17),7,9,15-tetraene-9,14-diol

• 分子结构分类: 有机化合物 - 生物碱及其衍生物 - 石蒜科生物碱
• 英文名称: 4-Methyl-11-oxa-4-azatetracyclo[8.6.1.01,12.06,17]heptadeca-6(17),7,9,15-tetraene-9,14-diol
• 化学式: C₁₆H₁₉NO₃
• 分子量: 273.33
• InChiKey: OYSGWKOGUVOGFQ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.5
• 重原子数：
  20
• 可旋转键数：
  0
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.5
• 拓扑面积：
  52.9
• 氢给体数：
  2
• 氢受体数：
  4

文献信息

• CHOLINERGIC ENHANCERS WITH IMPROVED BLOOD-BRAIN BARRIER PERMEABILITY FOR THE TREATMENT OF DISEASES ACCOMPANIED BY COGNITIVE IMPAIRMENT
  申请人：Maelicke Alfred

  公开号：US20090253654A1

  公开（公告）日：2009-10-08

  The present invention refers to compounds that, in addition to enhancing the sensitivity to acetylcholine and choline, and their exogenous agonists, of neuronal cholinergic receptors and/or acting as cholinesterase inhibitors and/or neuroprotective agents, have enhanced blood-brain barrier permeability in comparison to their parent compounds. The compounds are derived (either formally by their chemical structure or directly by chemical synthesis) from natural compounds belonging to the class of amaryllidaceae alkaloids e.g., galantamine, narwedine and lycoramine, or from metabolites of said compounds. The compounds of the present invention can either interact as such with their target molecules, or they can act as “pro-drugs”, in the sense that after reaching their target regions in the body they are converted by hydrolysis or enzymatic attack to the original parent compound and react as such with their target molecules, or both. The compounds of this invention may be used as medicaments.

  本发明涉及化合物，除了增强神经元胆碱能受体及/或作为胆碱酯酶抑制剂和/或神经保护剂的敏感性，还具有与其母体化合物相比增强的血脑屏障通透性。这些化合物是从天仙子科生物碱类天仙子碱、纳尔韦丁和丝兰碱或其代谢物中衍生出来的（无论是通过其化学结构或直接通过化学合成）。本发明的化合物可以直接与其靶分子相互作用，也可以作为“前药”，在到达体内的目标区域后，通过水解或酶攻击被转化为原始母体化合物，并与其靶分子反应，或两者兼有。本发明的化合物可用作药物。
• METHODS OF TREATMENT OF FATTY LIVER DISEASE BY PHARMACOLOGICAL ACTIVATION OF CHOLINERGIC PATHWAYS
  申请人：Pavlov Valentin A.

  公开号：US20120322719A1

  公开（公告）日：2012-12-20

  A method of treating a fatty liver disease in a subject. The method comprises administering to the subject an effective amount of a cholinergic pathway stimulating agent, wherein the fatty liver disease is selected from non-alcoholic fatty liver (NAFL), alcoholic fatty liver (AFL), non-alcoholic steatohepatitis (NASH), alcoholic steatohepatitis (ASH), NASH-associated liver fibrosis, ASH-associated liver fibrosis, non-alcoholic cirrhosis, and alcoholic cirrhosis.
• US8088918B2
  申请人：——

  公开号：US8088918B2

  公开（公告）日：2012-01-03
• US8865641B2
  申请人：——

  公开号：US8865641B2

  公开（公告）日：2014-10-21