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1. 发明授权

US09073899B2 Solid forms of dabigatran etexilate mesylate and processes for their preparation 有权
标题翻译：达比加群酯的甲磺酸固体形式及其制备方法
公开(公告)号：US09073899B2
公开(公告)日：2015-07-07
申请号：US14376834
申请日：2013-02-21
申请人： ESTEVE QUÍMICA, S.A.
发明人： Martí Bartra Sanmartí , Rosa Maria Espinosa Ferrer , Maria del Pilar Lupon Roses , Stephen Benedict David Winter , Silvia Donnici Garcia
IPC分类号： C07D401/12 , A61K31/4439
CPC分类号： C07D401/12 , C07B2200/13
摘要： It relates to solid forms of dabigatran etexilate mesylate, in particular dabigatran etexilate mesylate in crystalline Form A, and in amorphous form; to processes for their preparation, and to pharmaceutical compositions comprising them. It also relates to a crystalline form of dabigatran etexilate base (Form A), and to a process for its preparation.
摘要翻译：它涉及甲磺酸达比加群酯的固体形式，特别是结晶形式A的达比加群酯甲磺酸盐和无定形形式; 制备方法和包含它们的药物组合物。它还涉及达比加群酯结晶形式（A型）的结晶形式及其制备方法。

2. 发明申请

US20120309976A1 PREPARATION PROCESS OF THE SODIUM SALT OF ESOMEPRAZOLE 失效
标题翻译：异辛醚钠盐的制备方法
公开(公告)号：US20120309976A1
公开(公告)日：2012-12-06
申请号：US13577827
申请日：2011-02-11
申请人： Marti Bartra Sanmartí , Ramón Berenguer Maimó , Joan Gabriel Solsona Rocabert
发明人： Marti Bartra Sanmartí , Ramón Berenguer Maimó , Joan Gabriel Solsona Rocabert
IPC分类号： C07D401/12
CPC分类号： C07D401/12
摘要： A preparation process of esomeprazole sodium substantially free of sulfone impurity including the steps of: a) combining either esomeprazole with a (C3-C8)-ketone or a mixture thereof, a sodium alkoxide, and a (C1-C5)-alcohol, or esomeprazole sodium with a (C3-C8)-ketone or a mixture thereof and a (C1-C5)-alcohol; and b) recovering the esomeprazole sodium formed from the reaction media by filtration.
摘要翻译：一种基本上不含砜杂质的艾美拉唑钠的制备方法，包括以下步骤：a）将埃索美拉唑与（C 3 -C 8） - 酮或其混合物，醇钠和（C1-C5） - 醇或具有（C 3 -C 8） - 酮或其混合物和（C 1 -C 5） - 醇的艾美拉唑钠; 和b）通过过滤回收由反应介质形成的埃索美拉唑钠。

3. 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。

4. 发明授权

US09035070B2 Process for the preparation of 1-aryl-pyrazol-3-one intermediates useful in the synthesis of sigma receptors inhibitors 有权
标题翻译：用于合成西格玛受体抑制剂的1-芳基 - 吡唑-3-酮中间体的制备方法
公开(公告)号：US09035070B2
公开(公告)日：2015-05-19
申请号：US13704148
申请日：2011-07-28
申请人： Martí Bartra Sanmarti , Ramon Berenguer Maimo , Jorge Medrano Ruperez , Jorge Garcia Gomez , Javier Ariza Piquer
发明人： Martí Bartra Sanmarti , Ramon Berenguer Maimo , Jorge Medrano Ruperez , Jorge Garcia Gomez , Javier Ariza Piquer
IPC分类号： C07D231/20 , C07D207/36 , C07D317/30
CPC分类号： C07D207/36 , C07D231/20 , C07D317/30
摘要： The invention relates to a process for preparing 1-aryl-pyrazol-3-one intermediates, tautomers, and salts thereof, to novel intermediates, and to the use of the intermediates in the preparation of sigma receptor inhibitors.
摘要翻译：本发明涉及一种制备1-芳基 - 吡唑-3-酮中间体，互变异构体及其盐，新中间体以及中间体在制备σ受体抑制剂中的用途的方法。

5. 发明申请

US20100041883A1 Process for the preparation of abacavir 失效
标题翻译：制备阿巴卡韦的方法
公开(公告)号：US20100041883A1
公开(公告)日：2010-02-18
申请号：US12520510
申请日：2007-12-20
申请人： Jorge Medrano Rupérez , Julio Campon Pardo , Laia Elías Rius , Ramón Berenguer Maimó
发明人： Jorge Medrano Rupérez , Julio Campon Pardo , Laia Elías Rius , Ramón Berenguer Maimó
IPC分类号： C07D473/16
CPC分类号： C07D473/00
摘要： Process for the preparation of abacavir, or its salts or its solvates comprising the step of reacting a compound (IV) where R1 is a (C1-C4)-alkyl radical with anhydrous hydrochloric acid/(C1-C6)-alcohol, and then with tri(C1-C4)-alkyl orthoformate, in the absence of water. The preparation process may include further steps of reacting the compound obtained with cyclopropylamine and subsequently hydrolysis to yield abacavir.
摘要翻译：制备阿巴卡韦或其盐或其溶剂合物的方法，包括使R1为（C1-C4） - 烷基的化合物（Ⅳ）与无水盐酸/（C 1 -C 6） - 醇反应的步骤，然后与三（C1-C4）烷基原甲酸酯，在没有水的情况下。制备方法可以包括使获得的化合物与环丙胺反应并随后水解以产生阿巴卡韦的进一步的步骤。

6. 发明申请

US20130296558A1 PREPARATION PROCESS OF AN ANTIVIRAL DRUG (ENTECAVIR) AND INTERMEDIATES THEREOF 审中-公开
标题翻译：抗病毒药物（ENTECAVIR）及其中间体的制备方法
公开(公告)号：US20130296558A1
公开(公告)日：2013-11-07
申请号：US13996545
申请日：2011-12-22
申请人： Martí Bartra Sanmartí , Ramón Berenguer Maimó , Javier Velasco Turbau , Javier Ariza Piquer , Jaime Farrás Soler , Jorge García Gómez
发明人： Martí Bartra Sanmartí , Ramón Berenguer Maimó , Javier Velasco Turbau , Javier Ariza Piquer , Jaime Farrás Soler , Jorge García Gómez
IPC分类号： C07D473/18 , C07F7/08 , C07F7/18
CPC分类号： C07D473/18 , C07D303/14 , C07D303/16 , C07F7/081 , C07F7/1804
摘要： It comprises a preparation process of entecavir comprising: submitting a (1S,3R)-3-(tert-butyldimethylsilyloxy)-1-(oxiran-2-yl)pent-4-yn-1-ol (VIII) to a double esterification and to a radicalary cyclization, yielding a compound of formula (V), where either a compound of formula (VIII) is submitted to a first esterification reaction, then to a catalytic radicalary cyclization using titanocene dichloride as catalyst in the presence of Mn/2,4,6-collidine HCl or Zn/2,4,6-collidine/trimethylsilyl chloride, and finally to a second esterification reaction or, alternatively, the compound of formula (VIII) is submitted first to a catalytic radicalary cyclization, and then to an esterification reaction. Entecavir can be obtained by submitting compound (V) to a desilylation reaction to remove the TBS group and then to a Mitsunobu coupling with 2-amino-6-chloroguanine, followed by hydrolysis. It also relates to some new intermediates of the process.
摘要翻译：其包括恩替卡韦的制备方法，其包括：将（1S，3R）-3-（叔丁基二甲基甲硅烷氧基）-1-（环氧乙烷-2-基）戊-4-炔-1-醇（VIII）和式（Ⅴ）化合物反应，其中式（Ⅷ）化合物进行第一次酯化反应，然后在二氯甲烷二氯化物作催化剂存在下，在Mn / 2存在下进行催化自由基环化，4,6-可可丁HCl或Zn / 2,4,6-可力丁/三甲基甲硅烷基氯，最后进行第二次酯化反应，或者，将式（Ⅷ）化合物首先进行催化活性环化，然后进行酯化反应。恩替卡韦可以通过将化合物（V）提交到脱甲硅烷基化反应中以除去TBS基团，然后与2-氨基-6-氯鸟嘌呤进行Mitsunobu偶联，随后水解。它也涉及到一些新的中间体的过程。

7. 发明申请

US20100029945A1 Process for the purification of Montelukast 审中-公开
标题翻译：蒙特鲁卡斯净化工艺
公开(公告)号：US20100029945A1
公开(公告)日：2010-02-04
申请号：US12376773
申请日：2007-08-07
申请人： Yolanda Gasanz Guillén , Pedro Talavera Escasany , Montserrat Monsalvatje Llagostera
发明人： Yolanda Gasanz Guillén , Pedro Talavera Escasany , Montserrat Monsalvatje Llagostera
IPC分类号： C07D215/04
CPC分类号： C07D215/18
摘要： It relates to a process for the purification of Montelukast, or pharmaceutically salts thereof, or solvates thereof, including stereoisomers or mixture thereof which comprises carrying out a specific set of selective solvent extractions of Montelukast or its impurities in a mixture of an organic solvent and water at specific ranges of pH and temperature which depend on the type of impurities to remove. In particular, it comprises at least one wash of an aqueous phase containing crude Montelukast in salt form with an organic solvent, at a pH comprised between 12.0 and 13.5; and optionally one or more washes of the resulting aqueous phase with an organic solvent at a pH comprised between 8.5 and 10.0. Montelukast is recovered by acidification at a pH comprised between 4.5 and 8.0 and solvent extraction, and is isolated either as acid or in salt form.
摘要翻译：本发明涉及纯化Montelukast或其药学上可接受的盐或其溶剂化物，包括立体异构体或其混合物的方法，其包括在有机溶剂和水的混合物中进行特定的选择性溶剂萃取孟鲁司特或其杂质在特定的pH和温度范围内，这取决于要除去的杂质的类型。特别地，其包含至少一次含有盐形式的粗壮孟鲁司特与有机溶剂的水相洗涤，pH在12.0和13.5之间; 并且任选地用pH为8.5至10.0的有机溶剂一次或多次洗涤所得水相。通过在4.5至8.0之间的pH下酸化回收孟鲁司特并进行溶剂萃取，并以酸或盐形式分离。

8. 发明申请

US20100004446A1 Process for the Preparation of Abacavir 有权
标题翻译：阿巴卡韦制备方法
公开(公告)号：US20100004446A1
公开(公告)日：2010-01-07
申请号：US12443378
申请日：2007-09-27
申请人： Jorge Medrano Rupérez , Julio Campon Pardo , Laia Elías Rius , Ramón Berenguer Maimó
发明人： Jorge Medrano Rupérez , Julio Campon Pardo , Laia Elías Rius , Ramón Berenguer Maimó
IPC分类号： C07D473/16
CPC分类号： C07D473/00 , Y02P20/55
摘要： Process for removal of the amino protective group of a N-acylated [(1S,4R)-4-[2-amino-6-(cyclopropylamino)-9H-purin-9-yl]-cyclopent-2-enyl]methanol of formula (II) where R═H or a (C1-C4)-alkyl, using an inorganic base in a mixture of water and alcohol, to yield abacavir or its salts. The process proceeds very fast and the product can be obtained in high yield and purity.
摘要翻译：去除N-酰化的[（1S，4R）-4- [2-氨基-6-（环丙基氨基）-9H-嘌呤-9-基] - 环戊-2-烯基]甲醇的氨基保护基的方法式（II）其中RH或（C1-C4） - 烷基，使用水和醇的混合物中的无机碱产生阿巴卡韦或其盐。该方法进行得非常快，可以高产率和纯度获得产品。

9. 发明申请

WO2012085209A1 PREPARATION PROCESS OF AN ANTIVIRAL DRUG (ENTECAVIR) AND INTERMEDIATES THEREOF 审中-公开
标题翻译：抗病毒药物（ENTECAVIR）及其中间体的制备方法
公开(公告)号：WO2012085209A1
公开(公告)日：2012-06-28
申请号：PCT/EP2011/073800
申请日：2011-12-22
申请人： ESTEVE QUÍMICA, S.A. , BARTRA SANMARTÍ, Martí , BERENGUER MAIMÓ, Ramón , VELASCO TURBAU, Javier , ARIZA PIQUER, Javier , FARRÀS SOLER, Jaime , GARCÍA GÓMEZ, Jorge
发明人： BARTRA SANMARTÍ, Martí , BERENGUER MAIMÓ, Ramón , VELASCO TURBAU, Javier , ARIZA PIQUER, Javier , FARRÀS SOLER, Jaime , GARCÍA GÓMEZ, Jorge
IPC分类号： C07D473/18 , C07D303/14 , C07D303/16 , C07C13/11 , C07F7/08
CPC分类号： C07D473/18 , C07D303/14 , C07D303/16 , C07F7/0818 , C07F7/1852 , C07F7/1856 , C07F7/1868
摘要： It comprises a preparation process of entecavir comprising: submitting a (1S, 3R)-3-(tert-butyldimethylsilyloxy)-1 -(oxiran-2-yl)pent-4-yn-1-ol (VIII) to a double esterification and to a radicalary cyclization, yielding a compound of formula (V), where either a compound of formula (VIII) is submitted to a first esterification reaction, then to a catalytic radicalary cyclization using titanocene dichloride as catalyst in the presence of Mn/2,4,6-collidine HCI or Zn/2,4,6-collidine/trimethylsilyl chloride, and finally to a second esterification reaction or, alternatively, the compound of formula (VIII) is submitted first to a catalytic radicalary cyclization, and then to an esterification reaction. Entecavir can be obtained by submitting compound (V) to a desilylation reaction to remove the TBS group and then to a Mitsunobu coupling with 2- amino-6-chloroguanine, followed by hydrolysis. It also relates to some new intermediates of the process.
摘要翻译：其包括恩替卡韦的制备方法，其包括：将（1S，3R）-3-（叔丁基二甲基甲硅烷氧基）-1-（环氧乙烷-2-基）戊-4-炔-1-醇（VIII）和式（Ⅴ）化合物反应，其中式（Ⅷ）化合物进行第一次酯化反应，然后在二氯甲烷二氯化物作催化剂存在下，在Mn / 2存在下进行催化自由基环化，4,6-可力丁HCl或Zn / 2,4,6-可力丁/三甲基甲硅烷基氯，最后进行第二次酯化反应，或者，将式（Ⅷ）化合物首先进行催化活性环化，然后进行酯化反应。恩替卡韦可以通过将化合物（V）提交到脱甲硅烷基化反应中以除去TBS基团，然后与2-氨基-6-氯鸟嘌呤进行Mitsunobu偶联，然后水解。它也涉及到一些新的中间体的过程。

10. 发明申请

WO2012013755A1 PROCESS FOR THE PREPARATION OF 1-ARYL-PYRAZOL-3-ONE INTERMEDIATES USEFUL IN THE SYNTHESIS OF SIGMA RECEPTORS INHIBITORS 审中-公开
标题翻译：制备1-ARYL-PYRAZOL-3-ONE中间体在合成SIGMA受体抑制剂中有用的方法
公开(公告)号：WO2012013755A1
公开(公告)日：2012-02-02
申请号：PCT/EP2011/063020
申请日：2011-07-28
申请人： ESTEVE QUÍMICA, S.A. , BARTRA SANMARTÍ, Martí , BERENGUER MAIMÓ, Ramon , MEDRANO RUPÉREZ, Jorge , GARCÍA GÓMEZ, Jorge , ARIZA PIQUER, Javier
发明人： BARTRA SANMARTÍ, Martí , BERENGUER MAIMÓ, Ramon , MEDRANO RUPÉREZ, Jorge , GARCÍA GÓMEZ, Jorge , ARIZA PIQUER, Javier
IPC分类号： C07C59/125 , C07C69/96 , C07D231/20 , C07D317/30
CPC分类号： C07D207/36 , C07D231/20 , C07D317/30
摘要： The invention relates to a process for preparing 1-aryl-pyrazol-3-one intermediates, tautomers, and salts thereof, to novel intermediates, and to the use of the intermediates in the preparation of sigma receptor inhibitors.
摘要翻译：本发明涉及一种制备1-芳基 - 吡唑-3-酮中间体，互变异构体及其盐，新中间体以及中间体在制备σ受体抑制剂中的用途的方法。

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