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1. 发明申请

US20080306270A1 Process for the Preparation of a Leukotriene Antagonist and Intermediates Thereof 审中-公开
标题翻译：制备白三烯拮抗剂及其中间体的方法
公开(公告)号：US20080306270A1
公开(公告)日：2008-12-11
申请号：US12092554
申请日：2006-11-03
申请人： Laura Coppi , Marti Bartra Sanmarti , Yolanda Gasanz Guillen , Montserrat Monsalvatje Llagostera , Pedro Talavera Escasany
发明人： Laura Coppi , Marti Bartra Sanmarti , Yolanda Gasanz Guillen , Montserrat Monsalvatje Llagostera , Pedro Talavera Escasany
IPC分类号： C07D215/18
CPC分类号： C07D215/18
摘要： It comprises a preparation process of Montelukast from a new intermediate compound of formula (VI), which is previously prepared by reaction of the corresponding sulfonate with 1-(mercaptomethyl)cyclopropyl)methanol. Compound (VI) is reacted with a Grignard reactant to convert the ester group into a tertiary alcohol, followed by conversion of the primary alcohol into a sulfonate, substitution of the sulfonate group by a cyano group, and finally transforming the cyano compound to the carboxilic acid compound by a hydrolysis reaction to afford Montelukast. Montelukast can also be prepared by a hydrolysis reaction of the corresponding amide. It also comprises new intermediate compounds useful in such preparation process.
摘要翻译：它包括由新的式（VI）中间体化合物制备Montelukast的制备方法，其通过相应的磺酸酯与1-（巯基甲基）环丙基）甲醇反应而制备。使化合物（VI）与格氏反应物反应，将酯基转化为叔醇，然后将伯醇转化成磺酸盐，用磺酰基取代氰基，最后将氰基化合物转化为羧酸酸化合物通过水解反应得到蒙特鲁卡斯特。孟鲁司特也可以通过相应酰胺的水解反应制备。它还包括在这种制备过程中有用的新的中间体化合物。

2. 发明授权

US06967248B2 Crystalline forms of meloxicam and processes for their preparation and interconversion 失效
标题翻译：美洛昔康的结晶形式及其制备和相互转化的方法
公开(公告)号：US06967248B2
公开(公告)日：2005-11-22
申请号：US10314542
申请日：2002-12-09
申请人： Laura Coppi , Marti Bartra Sanmarti , Montserrat Closa Clavo
发明人： Laura Coppi , Marti Bartra Sanmarti , Montserrat Closa Clavo
IPC分类号： C07D417/02 , A61K31/5415 , A61P29/00 , A61P43/00 , C07D417/12
CPC分类号： C07D417/12
摘要： The invention relates to the new crystalline forms II, III and V of meloxicam; to the processes for obtaining the crystalline forms I, II, III and V; and, finally, to the interconversion processes of the forms II, III, IV and V into the form I.
摘要翻译：本发明涉及美洛昔康的新结晶形式II，III和V; 涉及获得晶型I，II，III和V的方法; 最后是形式二，三，四和五的互换过程形式为一。

3. 发明申请

US20070249684A1 Solid Forms of the Magnesium Salt of S-Omeprazole and Processes for Their Preparation 有权
标题翻译： S-奥美拉唑的镁盐的固体形式及其制备方法
公开(公告)号：US20070249684A1
公开(公告)日：2007-10-25
申请号：US11571564
申请日：2005-06-29
申请人： Ramon Berenguer Maimo , Laura Coppi , Yolanda Gasanz Guillen , Jorge Medrano Ruperez
发明人： Ramon Berenguer Maimo , Laura Coppi , Yolanda Gasanz Guillen , Jorge Medrano Ruperez
IPC分类号： A61K31/4439 , A61P1/00 , C07D401/12
CPC分类号： C07D401/12
摘要： New solid forms of the active ingredient magnesium salt of S-omeprazole, obtainable by a preparation process including: a) crystallizing a magnesium salt of S-omeprazole from a solution of a magnesium salt of S-omeprazole in a solvent system that includes a mixture of methanol/water with an amount of water equal to or greater than about 0.01 ml/g of the magnesium salt of S-omeprazole starting material; b) isolating the magnesium salt of S-omeprazole that appears in the prior operation; c) separating the free organic solvent from the magnesium salt of S-omeprazole obtained or, alternatively, separating both the free solvent and the solvation solvent. The new solid forms are obtained by a reproducible and robust process, with high yield and elevated optical purity, which is useful for the preparation of pharmaceutical products that contain said active ingredient.
摘要翻译： S-奥美拉唑的活性成分镁盐的新固体形式，其可通过制备方法获得，所述制备方法包括：a）将S-奥美拉唑的镁盐从包含混合物的溶剂体系中的S-奥美拉唑的镁盐溶液中结晶的甲醇/水，其量为等于或大于约0.01ml / g的S-奥美拉唑起始材料的镁盐; b）分离在先前操作中出现的S-奥美拉唑镁盐; c）从所获得的S-奥美拉唑的镁盐中分离游离有机溶剂，或者分离游离溶剂和溶剂化溶剂两者。新的固体形式通过可重复且可靠的方法获得，具有高产率和高的光学纯度，其可用于制备含有所述活性成分的药物产品。

4. 发明授权

US06635773B2 Process for preparing citalopram 失效
公开(公告)号：US06635773B2
公开(公告)日：2003-10-21
申请号：US10351289
申请日：2003-01-24
申请人： Laura Coppi , Yolanda Gasanz Guillen , Julio Campon Pardo
发明人： Laura Coppi , Yolanda Gasanz Guillen , Julio Campon Pardo
IPC分类号： C07D30787
CPC分类号： C07D307/87
摘要： Process for preparing purified citalopram or one of its salts that comprises the purification of citalopram by selective extractions of citalopram or of its impurities with organic solvents and water under specific conditions of pH and temperature. The crude citalopram can be prepared by a process that comprises reacting 1-[3-(dimethylamine)propyl]-1-(4-fluorophenyl)-1,3-dihydro-5-bromoisobenzofuran with copper cyanide.

5. 发明授权

US06603009B2 Method for oxidizing a thioether group into a sulfoxide group 失效
标题翻译：将硫醚基氧化成亚砜基的方法
公开(公告)号：US06603009B2
公开(公告)日：2003-08-05
申请号：US10204506
申请日：2002-08-20
申请人： Ramon Berenguer Maimo , Julio Campon Pardo , Laura Coppi
发明人： Ramon Berenguer Maimo , Julio Campon Pardo , Laura Coppi
IPC分类号： A61K314439
CPC分类号： C07D401/12 , C07C315/02
摘要： The present invention relates to a procedure for the oxidation of a thioether group to a sulfoxide group, with aqueous sodium percarbonate in the presence of a molybdenum salt as a catalyst. The procedure is of application to oxidize the thioether group of a compound (I), where R1 is a C1-C6 alkyl, a halogenated C1-C6 alkyl, or —(CH2)n—OR9, where n is an integer between 1 and 6 and R9 is H or a C1-C6 alkyl; R2, R3, R4, R5, R6 and R8, independently form each other represent H, a C1-C6 alkyl, or C1-C6 alkoxy; and R7 is H, a C1-C6 alkyl, a C1-C6 alkoxy or a C1-C6 fluorinated alkoxy, in order to obtain the sulfinyl derivative (II).
摘要翻译：本发明涉及在钼盐作为催化剂存在下，用过碳酸钠水溶液将硫醚基氧化成亚砜基的方法。该方法用于氧化化合物（I）的硫醚基团，其中R 1是C 1 -C 6烷基，卤代C 1 -C 6烷基或 - （CH 2）n OR 9，其中n是介于1和 6和R9是H或C1-C6烷基; R2，R3，R4，R5，R6和R8彼此独立地表示H，C1-C6烷基或C1-C6烷氧基; 并且R 7为H，C 1 -C 6烷基，C 1 -C 6烷氧基或C 1 -C 6氟化烷氧基，以获得亚磺酰基衍生物（II）。

6. 发明授权

US5312975A Process for the preparation of 5-(2,4-difluorophenyl)-salicylic acid 失效
标题翻译： 5-（2,4-二氟苯基） - 水杨酸的制备方法
公开(公告)号：US5312975A
公开(公告)日：1994-05-17
申请号：US813661
申请日：1991-12-27
申请人： Claudio Giordano , Laura Coppi , Francesco Minisci
发明人： Claudio Giordano , Laura Coppi , Francesco Minisci
IPC分类号： B01J27/10 , B01J27/128 , B01J31/12 , C07B61/00 , C07C37/055 , C07C39/367 , C07C41/18 , C07C43/225 , C07C51/00 , C07C51/15 , C07C51/363 , C07C65/05 , C07F5/02 , C07C41/01 , C07C41/24
CPC分类号： C07F5/027 , C07C37/00 , C07C37/055 , C07C51/15
摘要： A process for the preparation of 5-(2,4-difluorophenyl)-salicylic acid comprising the reaction of an organometallic derivative with a suitable substituted benzene in the presence of a transition-metal based catalyst is described.
摘要翻译：描述了在过渡金属基催化剂存在下包含有机金属衍生物与合适的取代苯的反应的5-（2,4-二氟苯基） - 水杨酸的制备方法。

7. 发明授权

US07902370B2 Solid forms of the magnesium salt of S-omeprazole and processes for their preparation 有权
标题翻译： S-奥美拉唑镁盐的固体形式及其制备方法
公开(公告)号：US07902370B2
公开(公告)日：2011-03-08
申请号：US11571564
申请日：2005-06-29
申请人： Ramón Berenguer Maimó , Laura Coppi , Yolanda Gasanz Guillén , Jorge Medrano Rupérez
发明人： Ramón Berenguer Maimó , Laura Coppi , Yolanda Gasanz Guillén , Jorge Medrano Rupérez
IPC分类号： C07D401/12
CPC分类号： C07D401/12
摘要： New solid forms of the active ingredient magnesium salt of S-omeprazole, obtainable by a preparation process including: a) crystallizing a magnesium salt of S-omeprazole from a solution of a magnesium salt of S-omeprazole in a solvent system that includes a mixture of methanol/water with an amount of water equal to or greater than about 0.01 ml/g of the magnesium salt of S-omeprazole starting material; b) isolating the magnesium salt of S-omeprazole that appears in the prior operation; c) separating the free organic solvent from the magnesium salt of S-omeprazole obtained or, alternatively, separating both the free solvent and the solvation solvent. The new solid forms are obtained by a reproducible and robust process, with high yield and elevated optical purity, which is useful for the preparation of pharmaceutical products that contain said active ingredient.
摘要翻译： S-奥美拉唑的活性成分镁盐的新固体形式，其可通过制备方法获得，所述制备方法包括：a）将S-奥美拉唑的镁盐从包含混合物的溶剂体系中的S-奥美拉唑的镁盐溶液中结晶的甲醇/水，其量为等于或大于约0.01ml / g的S-奥美拉唑起始材料的镁盐; b）分离在先前操作中出现的S-奥美拉唑镁盐; c）从所获得的S-奥美拉唑的镁盐中分离游离有机溶剂，或者分离游离溶剂和溶剂化溶剂两者。新的固体形式通过可重复且可靠的方法获得，具有高产率和高的光学纯度，其可用于制备含有所述活性成分的药物产品。

8. 发明申请

US20080167473A1 Process for the Preparation of Optically Active Derivatives of 2-(2-Pyridylmethylsulfinyl)-Benzimidazole Via Inclusion Complex with 1,1'-Binaphthalene-2, 2'Diol 有权
标题翻译： 2-（2-吡啶基甲基亚磺酰基） - 苯并咪唑与1,1'-联萘-2,2'-二醇的包合配合物的光学活性衍生物的制备方法
公开(公告)号：US20080167473A1
公开(公告)日：2008-07-10
申请号：US11817624
申请日：2006-02-22
申请人： Laura Coppi , Ramon Berenguer Maimo , Yolanda Gasanz Guilen , Jorge Medrano Ruperez
发明人： Laura Coppi , Ramon Berenguer Maimo , Yolanda Gasanz Guilen , Jorge Medrano Ruperez
IPC分类号： C07D401/12
CPC分类号： C07D401/12
摘要： Process for the preparation of optically active derivatives of 2-(2-piridylmethylsulfinyl)-benzimidazole, or salts thereof, by resolution of the corresponding racemic derivatives of 2-(2-piridylmethylsulfinyl)-benzimidazole. The resolution is performed through the formation of inclusion complexes with (S)-(−) or (R)-(+)-[1,1′-Binaphthalene]-2,2′-diol in the presence of an amine, followed by the break of the inclusion complex by treatment with an hydroxide of an alkaline metal. The enantiomer of the derivative of 2-(2-piridylmethylsulfinyl)-benzimidazole may be obtained by extractions at a particular pH with a suitable organic solvent. The process allows to perform the resolution with high yields and high optical purity, without using neither toxic solvents nor chromatography.
摘要翻译：通过拆分2-（2-吡啶基甲基亚磺酰基） - 苯并咪唑的相应外消旋衍生物，制备2-（2-吡啶基甲基亚磺酰基） - 苯并咪唑的光学活性衍生物或其盐的方法。通过在胺的存在下与（S） - （ - ）或（R） - （+） - [1,1'-联萘] -2,2'-二醇形成包合络合物进行分辨率，随后通过用碱金属的氢氧化物处理破坏包合物。 2-（2-吡啶基甲基亚磺酰基） - 苯并咪唑衍生物的对映异构体可以通过用合适的有机溶剂在特定pH下萃取而获得。该方法允许以高产率和高光学纯度执行分辨率，而不使用有毒溶剂或色谱。

9. 发明授权

US5412143A Process for the preparation of 5-(2,4-difluorophenyl)-salicylic acid 失效
标题翻译： 5-（2,4-二氟苯基） - 水杨酸的制备方法
公开(公告)号：US5412143A
公开(公告)日：1995-05-02
申请号：US174316
申请日：1993-12-30
申请人： Claudio Giordano , Laura Coppi , Francesco Minisci
发明人： Claudio Giordano , Laura Coppi , Francesco Minisci
IPC分类号： B01J27/10 , B01J27/128 , B01J31/12 , C07B61/00 , C07C37/055 , C07C39/367 , C07C41/18 , C07C43/225 , C07C51/00 , C07C51/15 , C07C51/363 , C07C65/05 , C07F5/02 , C07F5/04
CPC分类号： C07F5/027 , C07C37/00 , C07C37/055 , C07C51/15
摘要： A process for the preparation of 5-(2,4-difluorophenyl)-salicylic acid comprising the reaction of an organometallic derivative with a suitable substituted benzene in the presence of a transition-metal based catalyst is described.
摘要翻译：描述了在过渡金属基催化剂存在下包含有机金属衍生物与合适的取代苯的反应的5-（2,4-二氟苯基） - 水杨酸的制备方法。

10. 发明授权

US07777044B2 Process for the preparation of optically active derivatives of 2-(2-pyridylmethylsulfinyl)-benzimidazole via inclusion complex with 1,1′-binaphthalene-2,2′diol 有权
标题翻译：通过与1,1'-联萘-2,2'-二醇的包合络合物制备2-（2-吡啶基甲基亚磺酰基） - 苯并咪唑的光学活性衍生物的方法
公开(公告)号：US07777044B2
公开(公告)日：2010-08-17
申请号：US11817624
申请日：2006-02-22
申请人： Laura Coppi , Ramón Berenguer Maimó , Yolanda Gasanz Guillén , Jorge Medrano Rupérez
发明人： Laura Coppi , Ramón Berenguer Maimó , Yolanda Gasanz Guillén , Jorge Medrano Rupérez
IPC分类号： C07D401/12
CPC分类号： C07D401/12
摘要： Process for the preparation of optically active derivatives of 2-(2-piridylmethylsulfinyl)-benzimidazole, or salts thereof, by resolution of the corresponding racemic derivatives of 2-(2-piridylmethylsulfinyl)-benzimidazole. The resolution is performed through the formation of inclusion complexes with (S)-(−) or (R)-(+)-[1,1′-Binaphthalene]-2,2′-diol in the presence of an amine, followed by the break of the inclusion complex by treatment with an hydroxide of an alkaline metal. The enantiomer of the derivative of 2-(2-piridylmethylsulfinyl)-benzimidazole may be obtained by extractions at a particular pH with a suitable organic solvent. The process allows to perform the resolution with high yields and high optical purity, without using neither toxic solvents nor chromatography.
摘要翻译：通过拆分2-（2-吡啶基甲基亚磺酰基） - 苯并咪唑的相应外消旋衍生物，制备2-（2-吡啶基甲基亚磺酰基） - 苯并咪唑的光学活性衍生物或其盐的方法。通过在胺的存在下与（S） - （ - ）或（R） - （+） - [1,1'-联萘] -2,2'-二醇形成包合络合物进行分辨率，随后通过用碱金属的氢氧化物处理破坏包合物。 2-（2-吡啶基甲基亚磺酰基） - 苯并咪唑衍生物的对映异构体可以通过用合适的有机溶剂在特定pH下萃取而获得。该方法允许以高产率和高光学纯度执行分辨率，而不使用有毒溶剂或色谱。

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