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1. 发明申请

WO2012098075A1 PROCESS FOR THE PREPARATION OF RETIGABINE 审中-公开
标题翻译：制剂的制备方法
公开(公告)号：WO2012098075A1
公开(公告)日：2012-07-26
申请号：PCT/EP2012/050559
申请日：2012-01-16
申请人： GLAXO GROUP LIMITED , FITZGERALD, Russ, N , MILLAR, Alan , TOCZKO, Jennifer, Fell
发明人： FITZGERALD, Russ, N , MILLAR, Alan , TOCZKO, Jennifer, Fell
IPC分类号： C07C269/04 , C07C269/06 , C07C271/28
CPC分类号： C07C269/06 , C07C269/04 , C07C271/28
摘要： This invention relates to a novel chemical process for the synthesis of 2-ethyoxycarbonylamino-5-(4-fluorobenzylamino)-nitrobenzene and its use in the preparation of 2-amino-4-(4-fluorobenzylamino)-1-ethoxycarbonylaminobenzene (retigabine/ezogabine) and its polymorphic forms thereof.
摘要翻译：本发明涉及一种用于合成2-乙氧基羰基氨基-5-（4-氟苄基氨基） - 硝基苯的新型化学方法及其在制备2-氨基-4-（4-氟苄基氨基）-1-乙氧基羰基氨基苯（瑞替加滨/ 依佐胺）及其多晶型。

2. 发明申请

WO2012166916A1 METHOD OF SEPARATION OF LIPID AND BIOLOGICAL MOLECULAR SPECIES USING HIGH PURITY CHROMATOGRAPHIC MATERIALS 审中-公开
标题翻译：使用高纯度色谱材料分离脂质和生物分子物种的方法
公开(公告)号：WO2012166916A1
公开(公告)日：2012-12-06
申请号：PCT/US2012/040205
申请日：2012-05-31
申请人： WATERS TECHNOLOGIES CORPORATION , ISAAC, Giorgis , MCDONALD, Stephen , MILLAR, Alan , FOUNTAIN, Kenneth , SHOCKCOR, John
发明人： ISAAC, Giorgis , MCDONALD, Stephen , MILLAR, Alan , FOUNTAIN, Kenneth , SHOCKCOR, John
IPC分类号： B01D15/04
CPC分类号： B01D15/327 , B01D15/36 , B01D15/3847 , G01N30/482
摘要： The present invention provides methods of separating, profiling and analyzing molecular species contained within a biological sample using a high purity chromatographic material (HPCM) comprising a chromatographic surface wherein the chromatographic surface comprises a hydrophobic surface group and one or more ionizable modifiers with the proviso that when the ionizable modifier does not contain a Zwitterion, the ionizable modifier does not contain a quaternary ammonium ion moiety.
摘要翻译：本发明提供了使用包含色谱表面的高纯度色谱材料（HPCM）分离，分析和分析生物样品中所含的分子种类的方法，其中色谱表面包含疏水表面基团和一个或多个可离子化改性剂，条件是当可离子化改性剂不含有两性离子时，电离改性剂不含有季铵离子部分。

3. 发明申请

WO2006003429A3 MASS SPECTROMETER 审中-公开
公开(公告)号：WO2006003429A3
公开(公告)日：2006-01-12
申请号：PCT/GB2005/002610
申请日：2005-07-01
申请人： MICROMASS UK LIMITED , CASTRO-PEREZ, Jose , MILLAR, Alan , PLUMB, Robert
发明人： CASTRO-PEREZ, Jose , MILLAR, Alan , PLUMB, Robert
IPC分类号： H01J49/00
摘要： A method of searching for potentially unknown metabolites of pharmaceutical compounds is disclosed. The accurate mass of a pharmaceutical compound will generally be known and can be rendered in the form of an integer nominal mass or mass to charge ratio component and a decimal mass or mass to charge ratio component. Possible metabolites are searched for on the basis of having a decimal mass or mass to charge ratio component which is substantially very similar to the decimal mass or mass to charge ratio of the parent pharmaceutical compound.

4. 发明申请

WO0246207A3 PROCESS 审中-公开
标题翻译：处理
公开(公告)号：WO0246207A3
公开(公告)日：2003-03-20
申请号：PCT/US0148173
申请日：2001-11-02
申请人： GLAXO GROUP LTD , DAVIS ROMAN , MILLAR ALAN , STERBENZ JEFFREY THOMAS
发明人： DAVIS ROMAN , MILLAR ALAN , STERBENZ JEFFREY THOMAS
IPC分类号： C12N9/99 , C07J73/00 , C07J75/00
CPC分类号： C07J75/00
摘要： An improved process for preparing steroids, such as 3-oxo-4-azasteroids, is described. Compounds of this type are known to be useful in the preparation of compounds having 5a-reductase inhibitor activity. The process comprises the hydrogenation of the corresponding steroid alkene in the presence of ammonium acetate, ammonium formate, and/or ammonium propionate and an appropriate catalyst.
摘要翻译：描述了一种用于制备类固醇的改进方法，例如3-氧代-4-氮杂甾族化合物。已知这种化合物可用于制备具有5α-还原酶抑制剂活性的化合物。该方法包括在乙酸铵，甲酸铵和/或丙酸铵和适当的催化剂存在下氢化相应的类固醇烯烃。

5. 发明申请

WO1989007598A2 IMPROVED PROCESS FOR TRANS-6-[2-(SUBSTITUTED-PYRROL-1-YL)ALKYL]PYRAN-2-ONE INHIBITORS OF CHOLESTEROL SYNTHESIS 审中-公开
标题翻译：改进方法TRANS-6- [2-（取代的吡咯-1-基）烷基]吡喃-2-酮抑制剂胆固醇的合成
公开(公告)号：WO1989007598A2
公开(公告)日：1989-08-24
申请号：PCT/US1989000719
申请日：1989-02-22
申请人： WARNER-LAMBERT COMPANY , BUTLER, Donald, Eugene , DEERING, Carl, Francis , MILLAR, Alan , NANNINGA, Thomas, Norman , ROTH, Bruce, David
发明人： WARNER-LAMBERT COMPANY
IPC分类号： C07D405/06
CPC分类号： C07D319/08 , C07C235/80 , C07D207/34 , C07D319/06 , C07D405/06
摘要： An improved process for the preparation of trans-6-[2-(substituted-pyrrol-1-yl)alkyl]pyran-2-ones by a novel synthesis is described where 1,6-heptadien-4-ol is converted in eight operations to the desired products, as well as an improved process for the preparation of (2R-trans) and trans-(U)-5-(4-fluoro-phenyl)-2-(1-methylethyl)-N,4-diphenyl-1-[2-(tetrahydro-4-hydroxy-6-oxo-2H-pyran-2-yl)ethyl]-1H-pyrrole-3-carboxamide by a novel synthesis where 4-methyl-3-oxo-N-phenylpentanamide is converted in eight operations to the desired product or alternatively 4-fluoro-alpha-[2-methyl-1-oxopropyl]-gamma-oxo-N,beta-diphenylbenzenebutaneamide is converted in one step to the desired product, and additionally, a process for preparing (2R-trans)-5-(4-fluorophenyl)-2-(1-methylethyl)-N,4-diphenyl-1-[2-(tetrahydro-4-hydroxy-6-oxo-2H-pyran-2-yl)ethyl]-1H-pyrrole-3-carboxamide from (R)-4-cyano-3-[[(1,1-dimethylethyl)dimethylsilyl]oxy]butanoic acid, as well as other valuable intermediates used in the processes.
摘要翻译：它已经开发了一种改进的方法，用于反式-6-的制备[2-（取代的吡咯-1-基）烷基]吡喃-2-酮由一个新的合成装置，用于将1,6-heptadiène- 在所需产品中进行8次操作。制备（2R-反式）和反式 - （U）-5-（4-氟 - 苯基）-2-（1-甲基乙基）-N，4-二苯基-1的改进方法也被开发出来。 [2-（四氢-4-羟基-6-氧代-2H-吡喃-2-基）乙基]使用新的合成用于将4-甲基-3-氧代-1H-吡咯-3-甲酰胺 -N苯基戊酰胺在八个操作中，期望的产物或在另一个实施方案中变换4-氟-α-[2-甲基-1-氧代丙基〕-gamma氧代-N，β-diphénylbenzènebutaneamide在一个步骤中在期望的产品中。已经进一步开发出一种方法，用于制备式（2R-反式）-5-（4-flurophényle）-2-（1-甲基乙基）-N，4-二苯基-1- [2-（四氢 4-羟基-6-氧代-2H-吡喃-2-基）乙基]从（R）-4-氰基-3- -1H-吡咯-3-甲酰胺 - [[（1,1-二甲乙基）二甲基甲硅烷 ]氧]丁酸，以及在该方法中使用的其他有价值的中间体。

6. 发明申请

WO2006003429A2 MASS SPECTROMETER 审中-公开
标题翻译：质谱仪
公开(公告)号：WO2006003429A2
公开(公告)日：2006-01-12
申请号：PCT/GB2005002610
申请日：2005-07-01
申请人： MICROMASS LTD , CASTRO-PEREZ JOSE , MILLAR ALAN , PLUMB ROBERT
发明人： CASTRO-PEREZ JOSE , MILLAR ALAN , PLUMB ROBERT
IPC分类号： H01J49/00
CPC分类号： H01J49/0031 , G01N33/15 , G06F19/703 , H01J49/004 , H01J49/26 , Y10T436/24
摘要： A method of searching for potentially unknown metabolites of pharmaceutical compounds is disclosed. The accurate mass of a pharmaceutical compound will generally be known and can be rendered in the form of an integer nominal mass or mass to charge ratio component and a decimal mass or mass to charge ratio component. Possible metabolites are searched for on the basis of having a decimal mass or mass to charge ratio component which is substantially very similar to the decimal mass or mass to charge ratio of the parent pharmaceutical compound.
摘要翻译：公开了一种搜索潜在未知的药物化合物代谢物的方法。药物化合物的精确质量通常是已知的，并且可以以整数标称质量或质荷比组分和十进制质量或质荷比组分的形式提供。基于具有基本上非常相似于母体药物化合物的十进制质量或质荷比的十进制质量或质荷比成分来搜索可能的代谢物。

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