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1. 发明授权

US07812042B2 Pharmaceutical compositions and therapeutic applications for the use of a novel vitamin B12 derivative, N-acetyl-L-cysteinylcobalamin 有权
标题翻译：用于使用新型维生素B12衍生物，N-乙酰基-L-半胱氨酰钴胺素的药物组合物和治疗应用
公开(公告)号：US07812042B2
公开(公告)日：2010-10-12
申请号：US11903066
申请日：2007-09-20
申请人： Nicola E. Brasch , Catherine Stephanie Birch , John Henry Howatson Williams
发明人： Nicola E. Brasch , Catherine Stephanie Birch , John Henry Howatson Williams
IPC分类号： A61K31/4184 , A61K31/28 , C07D235/08 , C07F15/06
CPC分类号： A61K31/7042
摘要： Therapeutic applications, such as prevention, treatment and supplementation, for the use of novel and other thiolatocobalamins to protect human cells against the effects of oxidative stress. In particular, this invention relates to the use of a novel synthetic thiolatocobalamin, N-acetyl-L-cysteinylcobalamin (NACCbl) to protect animal cells against oxidative stress damage. This invention also relates to the use of thiolatocobalamins, such as NACCbl, in lieu of current, commercially available forms of vitamin B12 for the treatment and prevention of conditions associated with oxidative stress damage and for dietary supplementation.
摘要翻译：治疗应用，如预防，治疗和补充，用于使用新型和其他硫胺素类维生素来保护人类细胞免受氧化应激的影响。特别地，本发明涉及一种新的合成硫胺素一精胺N-乙酰基-L-半胱氨酰钴胺素（NACCbl）用于保护动物细胞免受氧化应激损伤的用途。本发明还涉及硫胺素类维生素如NACCbl的用途，代替目前市售的维生素B12形式用于治疗和预防与氧化应激损伤和膳食补充相关的病症。

2. 发明授权

US07777046B2 Method of synthesis of a salt of N-acetyl-L-cysteinylcobalamin 有权
标题翻译：合成N-乙酰基-L-半胱氨酰钴胺素盐的方法
公开(公告)号：US07777046B2
公开(公告)日：2010-08-17
申请号：US11725861
申请日：2007-03-20
申请人： Nicola E Brasch , Edward Suarez-Moreira
发明人： Nicola E Brasch , Edward Suarez-Moreira
IPC分类号： C07F15/06
CPC分类号： C07F15/065
摘要： The invention provides a method for preparing the sodium salt of the novel thiol derivative of vitamin B12, N-acetyl-L-cysteinylcobalamin (Na[NACCbl]). The method involves carrying out the reaction in aqueous solvent with a relatively small excess of ligand reactant, specifically from one to less than four molar equivalents. The cobalamin derivative formed is precipitated from the aqueous solvent, preferably by the addition of a precipitate inducing solvent. This provides a product in acceptable purity without the need for an additional chromatographic purification step.
摘要翻译：本发明提供了制备维生素B12，N-乙酰基-L-半胱氨酰钴胺素（Na [NACCbl]）的新型硫醇衍生物的钠盐的方法。该方法包括在水溶剂中用相对小的过量配体反应物，特别是1至小于4摩尔当量进行反应。形成的钴胺素衍生物从水性溶剂中析出，优选通过加入沉淀引发溶剂。这提供了可接受纯度的产品，而不需要额外的色谱纯化步骤。

3. 发明授权

US07030105B2 Method of synthesis of β-thiolato cobalamin compounds 失效
标题翻译： β-硫醇钴钴胺化合物的合成方法
公开(公告)号：US07030105B2
公开(公告)日：2006-04-18
申请号：US10430468
申请日：2003-05-06
申请人： Nicola E. Brasch , Ling Xia
发明人： Nicola E. Brasch , Ling Xia
IPC分类号： A61K31/40 , A61K31/155 , A61B5/055 , A61B10/00 , C07B47/00
CPC分类号： C07H23/00
摘要： The invention provides a method for preparing glutathionylcobalamin (GluSCbl) which involves running the reaction in an aqueous solvent with a relatively small excess of glutathione, i.e. GluSH, specifically from one to less than four molar equivalents of GluSH. The formed GluSCbl is precipitated from the aqueous solvent, preferably by the addition of a precipitate inducing solvent. This provides GluSCbl in acceptable purity without the need for an additional chromatographic purification step. Additionally, it has been found that the reaction can be run to an acceptable level of purity by using very high concentrations of the reactants, i.e. around saturation concentrations for aquocobalamin. This has the advantage of eliminating the need for air-free conditions.
摘要翻译：本发明提供了一种制备谷胱甘肽钴胺素（GluSCbl）的方法，其包括在具有相对小量过量谷胱甘肽（即GluSH），特别是1至小于4摩尔当量的GluSH的水性溶剂中进行反应。形成的GluSCb1从水性溶剂中沉淀出来，优选通过加入沉淀引发溶剂。这提供了可接受纯度的GluSCbl，而不需要额外的色谱纯化步骤。此外，已经发现，通过使用非常高浓度的反应物，即水溶胆固醇的饱和浓度，反应可以达到可接受的纯度水平。这具有消除对无空气条件的需要的优点。

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