galantamine gluconate | 807362-22-7

• 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: galantamine gluconate
• 英文别名: (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-ol;(2R,3S,4R,5R)-2,3,4,5,6-pentahydroxyhexanoic acid
• CAS: 807362-22-7
• 化学式: C₆H₁₂O₇*C₁₇H₂₁NO₃
• 分子量: 483.516
• InChiKey: TWHCYCWGDRWDIE-FGNKIXEOSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -1.64
• 重原子数：
  34
• 可旋转键数：
  6
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.61
• 拓扑面积：
  180
• 氢给体数：
  7
• 氢受体数：
  11

文献信息

• Carboxylate salts of galantamine and their pharmaceutical use
  申请人：Nastech Pharmaceutical Company Inc.

  公开号：US20040254146A1

  公开（公告）日：2004-12-16

  Disclosed are novel carboxylate salts of galantamine including galantamine gluconate, galantamine lactate, galantamine citrate and galantamine glucarate. These salts of galantamine have more than a 5 fold increase in solubility compared to galantamine hydrobromide. These galantamine salts can be administered to an individual to inhibit acetylcholinesterase in the treatment of such diseases as Alzheimer's disease, atony of the smooth muscle of the intestinal tract and urinary bladder, glaucoma, myasthenia gravis, and termination of the effects of competitive neuromuscular blocking drugs.

  本发明涉及新型加兰他敏的羧酸盐，包括加兰他敏葡萄糖酸盐、加兰他敏乳酸盐、加兰他敏柠檬酸盐和加兰他敏葡萄糖醛酸盐。与加兰他敏溴化物相比，这些加兰他敏盐的溶解度增加了5倍以上。这些加兰他敏盐可用于治疗阿尔茨海默病、肠道和膀胱平滑肌无力、青光眼、重症肌无力以及终止竞争性神经肌肉阻滞药的作用。可以将这些加兰他敏盐用于个体中，以抑制乙酰胆碱酯酶。
• Compositions and methods using acetylcholinesterase (ACE) inhibitors to treat central nervous system (CNS) disorders in mammals
  申请人：Quay C. Steven

  公开号：US20060003989A1

  公开（公告）日：2006-01-05

  Methods and compositions of the invention employ acetylcholinesterase (ACE) inhibitors to prevent and treat diseases and other disorders of the central nervous system (CNS), including Alzheimer's disease. ACE inhibitors are administered for targeted delivery to the CNS, for example by intranasal delivery. The methods and compositions of the present invention yield therapeutic concentrations of ACE inhibitors in a CNS tissue or compartment without the attendant disadvantages, risks and side effects of oral or injection delivery. Exemplary ACE inhibitors for use within the invention include galantamine and various salts and derivatives of galantamine. Carboxylate salts of galantamine (e.g., galantamine gluconate, galantamine lactate, galantamine citrate and galantamine glucarate) described herein exhibit a significant increase in solubility compared to other forms of galantamine, such as galantamine hydrobromide.

  本发明的方法和组合物采用乙酰胆碱酯酶（ACE）抑制剂来预防和治疗中枢神经系统（CNS）的疾病和其他失调，包括阿尔茨海默病。乙酰胆碱酯酶抑制剂可定向递送至中枢神经系统，例如通过鼻内递送。本发明的方法和组合物能在中枢神经系统组织或区块中产生治疗浓度的 ACE 抑制剂，而不会产生口服或注射给药的缺点、风险和副作用。用于本发明的典型 ACE 抑制剂包括加兰他敏和加兰他敏的各种盐及衍生物。与其他形式的加兰他敏（如氢溴酸加兰他敏）相比，本文所述的加兰他敏羧酸盐（如葡萄糖酸加兰他敏、乳酸加兰他敏、柠檬酸加兰他敏和葡萄糖酸加兰他敏）的溶解度显著增加。
• GALANTAMINE SALTS, METHOD OF PRODUCING IT AND NASAL COMPOSITION THEREOF
  申请人：Nastech Pharmaceutical Company Inc.

  公开号：EP1753397A2

  公开（公告）日：2007-02-21
• [EN] COMPOSITIONS AND METHODS USING ACETYLCHOLINESTERASE (ACE) INHIBITORS TO TREAT CENTRAL NERVOUS SYSTEM (CNS) DISORDERS IN MAMMALS<br/>[FR] COMPOSITIONS ET PROCEDES D'UTILISATION D'INHIBITEURS D'ACETYLCHOLINESTERASE (ACE) POUR TRAITER LES TROUBLES DU SYSTEME NERVEUX CENTRAL CHEZ DES MAMMIFERES
  申请人：NASTECH PHARM CO

  公开号：WO2005102275A2

  公开（公告）日：2005-11-03

  Methods and compositions of the invention employ acethylcholinesterase (ACE) inhibitors to prevent and treat diseases and other disorders of the central nervous system (CNS), including Alzheimer’s disease. ACE inhibitors are administered for targeted delivery to the CNS, for example by intranasal delivery. The methods and compositions of the present invention yield therapeutic concentrations of ACE inhibitors in a CNS tissue or compartment without the attendant disadvantages, risks and side effects of oral or injection delivery. Exemplary ACE inhibitors for use within the invention include galantamine and various salts and derivatives of galantamine. Carboxylate salts of galantamine (e.g., galantamine gluconate, galantamine lactate, galantamine citrate and galantamine glucarate) described herein exhibit a significant increase in solubility compared to other forms of galantamine, such as galantamine hydrobromide.
• [EN] GALANTAMINE SALTS, METHOD OF PRODUCING IT AND NASAL COMPOSITION THEREOF<br/>[FR] COMPOSITIONS ET PROCEDES D'UTILISATION D'INHIBITEURS D'ACETYLCHOLINESTERASE (ACE) POUR TRAITER LES TROUBLES DU SYSTEME NERVEUX CENTRAL CHEZ DES MAMMIFERES
  申请人：NASTECH PHARM CO

  公开号：WO2005102275A3

  公开（公告）日：2006-03-30

  [EN] Methods and compositions of the invention employ acethylcholinesterase (ACE) inhibitors to prevent and treat diseases and other disorders of the central nervous system (CNS), including Alzheimer's disease. ACE inhibitors are administered for targeted delivery to the CNS, for example by intranasal delivery. The methods and compositions of the present invention yield therapeutic concentrations of ACE inhibitors in a CNS tissue or compartment without the attendant disadvantages, risks and side effects of oral or injection delivery. Exemplary ACE inhibitors for use within the invention include galantamine and various salts and derivatives of galantamine. Carboxylate salts of galantamine (e.g., galantamine gluconate, galantamine lactate, galantamine citrate and galantamine glucarate) described herein exhibit a significant increase in solubility compared to other forms of galantamine, such as galantamine hydrobromide.
  [FR] L'invention porte sur des méthodes et sur des compositions qui utilisent des inhibiteurs d'acéthylcholinestérase (ACE) pour prévenir et traiter des maladies et autres troubles du système nerveux central (SNC) tels que la maladie d'Alzheimer. Les inhibiteurs d'ACE sont administrés au système nerveux central de manière ciblée, par exemple par voie intranasale. Les méthodes et les compositions de cette invention génèrent des concentrations thérapeutiques d'inhibiteurs d'ACE dans un tissu ou une partie du SNC sans les désavantages, risques et effets secondaires concomitants de l'administration par voie buccale ou par injection. Les inhibiteurs d'ACE destinés à être utilisés dans cette invention sont la galantamine et divers sels et dérivés de la galantamine. Des sels de carboxylate de la galantamine (tels que le gluconate de galantamine, le lactate de galantamine, le citrate de galantamine et le glucarate de galantamine) présentent une solubilité bien supérieure comparé à d'autres formes de la galantamine telles que l'hydrobromure de galantamine.