GLN-0979 | 934162-94-4

• 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: GLN-0979
• 英文别名: (4aS,6R,8aS)-4a,5,9,10,11,12-hexahydro-3-methoxy-11-methyl-6H-benzofuro[3a,3,2-ef][2]benzazepin-6-ol 2-methyl-propanoate；[(1S,12S,14R)-9-methoxy-4-methyl-11-oxa-4-azatetracyclo[8.6.1.01,12.06,17]heptadeca-6(17),7,9,15-tetraen-14-yl] 2-methylpropanoate
• CAS: 934162-94-4
• 化学式: C₂₁H₂₇NO₄
• 分子量: 357.45
• InChiKey: SYLQDIWQGQNPIH-WJPUGNRLSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.5
• 重原子数：
  26
• 可旋转键数：
  4
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.57
• 拓扑面积：
  48
• 氢给体数：
  0
• 氢受体数：
  5

反应信息

• 作为反应物：
  描述：

  GLN-0979 在 盐酸 作用下， 以 乙酸乙酯 为溶剂， 以97%的产率得到(4aS,6R,8aS)-4a,5,9,10,11,12-hexahydro-3-methoxy-11-methyl-6H-benzofuro[3a,3,2-ef][2]benzazepin-6-ol 2-methyl-propanoate hydrochloride
  参考文献：
  名称：

  [EN] DERIVATIVES OF GALANTAMINE AS PRO-DRUGS FOR THE TREATMENT OF HUMAN BRAIN DISEASES
  [FR] DÉRIVÉS DE GALANTAMINE COMME PROMÉDICAMENTS POUR LE TRAITEMENT DE MALADIES DU CERVEAU HUMAIN

  摘要：

  本发明涉及选择的加兰他敏衍生物，在治疗人类脑部疾病方面具有高效性和低副作用。

  公开号：

  WO2009127218A1

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。
• US9763953B2
  申请人：——

  公开号：US9763953B2

  公开（公告）日：2017-09-19
• [EN] DERIVATIVES OF GALANTAMINE AS PRO-DRUGS FOR THE TREATMENT OF HUMAN BRAIN DISEASES<br/>[FR] DÉRIVÉS DE GALANTAMINE COMME PROMÉDICAMENTS POUR LE TRAITEMENT DE MALADIES DU CERVEAU HUMAIN
  申请人：GALANTOS PHARMA GMBH

  公开号：WO2009127218A1

  公开（公告）日：2009-10-22

  The present invention refers to selected galantamine derivatives having high efficacy in treatment of human brain diseases and low side effects.

  本发明涉及选择的加兰他敏衍生物，在治疗人类脑部疾病方面具有高效性和低副作用。