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公开(公告)号：US20100190726A1
公开(公告)日：2010-07-29
申请号：US12642877
申请日：2009-12-21
CPC分类号： A61K36/47
摘要： A method is described for producing an extract of Phyllanthus comprising the steps of: (a) extracting Phyllanthus components with a solvent; (b) fractionating the extract obtained in the preceding step on the basis of hydrophobicity; (c) collecting and combining fractions that correspond in hydrophobicity to elute fractions resulting from 10-50% methanol elution steps, wherein the elute fractions are obtained by low pressure vacuum liquid chromatography (VLC) using a C18 reversed-phase lipophilic column and a water/methanol gradient system, wherein the gradient system is based on an initial elution step of loading the column with 100% water, on intermediate elution steps with gradually decreasing water content and on a terminal elution step loading the column with 100% methanol; and (d) optionally drying the extract obtained in step (c). The invention also relates to an extract of Phyllanthus obtainable or obtained by the method or a fraction thereof and a Phyllanthus extract or fraction thereof comprising repandusinic acid, wherein the repandusinic acid is present at a concentration of at least 42 mg/g.
摘要翻译： 描述了用于生产叶酸提取物的方法，包括以下步骤：（a）用溶剂萃取叶酸成分; （b）基于疏水性对前述步骤中获得的提取物进行分级; （c）将从疏水性对应的级分与从10-50％甲醇洗脱步骤得到的洗脱级分进行收集并合并，其中洗脱级分通过使用C18反相亲油柱和水的低压真空液相色谱（VLC）获得 /甲醇梯度系统，其中梯度系统基于在具有逐渐降低的水含量的中间洗脱步骤的情况下以100％水加载柱的初始洗脱步骤，以及在100％甲醇下加载柱的末端洗脱步骤; 和（d）任选地干燥步骤（c）中获得的提取物。 本发明还涉及通过该方法或其一部分获得或获得的珍珠提取物，以及含有还原性酸的叶酸提取物或其级分，其中所述还原性酸以至少42mg / g的浓度存在。
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公开(公告)号：US08366935B2
公开(公告)日：2013-02-05
申请号：US12642877
申请日：2009-12-21
IPC分类号： B01D15/08
CPC分类号： A61K36/47
摘要： A method is described for producing an extract of Phyllanthus comprising the steps of: (a) extracting Phyllanthus components with a solvent; (b) fractionating the extract obtained in the preceding step on the basis of hydrophobicity; (c) collecting and combining fractions that correspond in hydrophobicity to elute fractions resulting from 10-50% methanol elution steps, wherein the elute fractions are obtained by low pressure vacuum liquid chromatography (VLC) using a C18 reversed-phase lipophilic column and a water/methanol gradient system, wherein the gradient system is based on an initial elution step of loading the column with 100% water, on intermediate elution steps with gradually decreasing water content and on a terminal elution step loading the column with 100% methanol; and (d) optionally drying the extract obtained in step (c). The invention also relates to an extract of Phyllanthus obtainable or obtained by the method or a fraction thereof and a Phyllanthus extract or fraction thereof comprising repandusinic acid, wherein the repandusinic acid is present at a concentration of at least 42 mg/g.
摘要翻译： 描述了一种用于生产叶酸提取物的方法，包括以下步骤：（a）用溶剂萃取珍珠花成分; （b）基于疏水性对前述步骤中获得的提取物进行分级; （c）将从疏水性对应的级分与从10-50％甲醇洗脱步骤得到的洗脱级分进行收集并合并，其中洗脱级分通过使用C18反相亲油柱和水的低压真空液相色谱（VLC）获得 /甲醇梯度系统，其中梯度系统基于在具有逐渐降低的水含量的中间洗脱步骤的情况下以100％水加载柱的初始洗脱步骤，以及在100％甲醇下加载柱的末端洗脱步骤; 和（d）任选地干燥步骤（c）中获得的提取物。 本发明还涉及通过该方法或其一部分获得或获得的珍珠提取物，以及含有还原性酸的叶酸提取物或其级分，其中所述还原性酸以至少42mg / g的浓度存在。
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公开(公告)号：US20140038168A1
公开(公告)日：2014-02-06
申请号：US13881835
申请日：2011-10-27
申请人： Andrey Vinnik , Peter Fedichev , Maxim Kholin , Christopher Molloy , Aron Katz
发明人： Andrey Vinnik , Peter Fedichev , Maxim Kholin , Christopher Molloy , Aron Katz
IPC分类号： C12N7/00 , C07C237/40 , C07K14/005 , G06F19/16
CPC分类号： G01N33/566 , A61K31/00 , C07C231/12 , C07C237/40 , C07C237/42 , C07C2601/14 , C07K14/005 , C07K16/1063 , C07K2317/14 , C12N7/00 , C12Q1/703 , C40B30/02 , G01N33/50 , G01N2333/162 , G01N2333/70514 , G01N2500/00 , G01N2500/02 , G06F19/16 , G06F19/706
摘要： The present invention relates to a method of designing an inhibitor of the binding of HIV (human immunodeficiency virus) glycoprotein (gp)120 to a CD4-receptor or to the integrin alpha4 beta7 (a4b7). The inhibitor interacts with at least two amino acid residues comprised in six motifs within the 3-dimensional structure of gp120. Also provided are compounds, pharmaceutical compositions thereof and uses thereof in the development of an inhibitor of the binding of a HIV gp120 to a CD4-receptor or an integrin alpha4 beta7 (a4b7). The inhibitors are useful for the prevention or treatment of an HIV infection and/or diseases associated with an HIV infection.
摘要翻译： 本发明涉及一种设计HIV（人类免疫缺陷病毒）糖蛋白（gp）120与CD4受体或整联蛋白α4β7（a4b7）结合的抑制剂的方法。 抑制剂与gp120的三维结构内的六个基序中包含的至少两个氨基酸残基相互作用。 还提供了化合物，其药物组合物及其在开发HIV gp120与CD4受体或整联蛋白α4β7（a4b7）结合的抑制剂中的用途。 抑制剂可用于预防或治疗HIV感染和/或与HIV感染相关的疾病。
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公开(公告)号：US09422527B2
公开(公告)日：2016-08-23
申请号：US13881835
申请日：2011-10-27
申请人： Andrey Vinnik , Peter Fedichev , Maxim Kholin , Christopher Molloy , Aron Katz
发明人： Andrey Vinnik , Peter Fedichev , Maxim Kholin , Christopher Molloy , Aron Katz
IPC分类号： C12N7/00 , A61K31/00 , C12Q1/70 , C40B30/02 , G01N33/50 , G06F19/16 , G06F19/00 , C07C237/40 , C07K14/005 , C07K16/10
CPC分类号： G01N33/566 , A61K31/00 , C07C231/12 , C07C237/40 , C07C237/42 , C07C2601/14 , C07K14/005 , C07K16/1063 , C07K2317/14 , C12N7/00 , C12Q1/703 , C40B30/02 , G01N33/50 , G01N2333/162 , G01N2333/70514 , G01N2500/00 , G01N2500/02 , G06F19/16 , G06F19/706
摘要： The present invention relates to a method of designing an inhibitor of the binding of HIV (human immunodeficiency virus) glycoprotein (gp)120 to a CD4-receptor or to the integrin alpha4 beta7 (a4b7). The inhibitor interacts with at least two amino acid residues comprised in six motifs within the 3-dimensional structure of gp120. Also provided are compounds, pharmaceutical compositions thereof and uses thereof in the development of an inhibitor of the binding of a HIV gp120 to a CD4-receptor or an integrin alpha4 beta7 (a4b7). The inhibitors are useful for the prevention or treatment of an HIV infection and/or diseases associated with an HIV infection.
摘要翻译： 本发明涉及一种设计HIV（人类免疫缺陷病毒）糖蛋白（gp）120与CD4受体或整联蛋白α4β7（a4b7）结合的抑制剂的方法。 抑制剂与gp120的三维结构内的六个基序中包含的至少两个氨基酸残基相互作用。 还提供了化合物，其药物组合物及其在开发HIV gp120与CD4受体或整联蛋白α4β7（a4b7）结合的抑制剂中的用途。 抑制剂可用于预防或治疗HIV感染和/或与HIV感染相关的疾病。
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