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1. 发明授权

US07728021B2 Process for the preparation of Valsartan and precursors thereof 失效
标题翻译：制备缬沙坦及其前体的方法
公开(公告)号：US07728021B2
公开(公告)日：2010-06-01
申请号：US11568054
申请日：2005-04-18
申请人： Pere Dalmases Barjoan , Jordi Bessa Belmunt , Joan Huguet Clotet , Juan Antonio Perez Andres
发明人： Pere Dalmases Barjoan , Jordi Bessa Belmunt , Joan Huguet Clotet , Juan Antonio Perez Andres
IPC分类号： A61K31/41 , C07D257/00
CPC分类号： C07D257/04
摘要： This invention relates to a process for preparing intermediates useful in preparing Valsartan and to a process for preparing the latter, together with synthesis intermediates of formula (IV), (V) and (VI), useful for manufacturing a medicament for the treatment of arterial hypertension or heart failure. The process for preparing Valsartan permits it to be prepared on an industrial scale with high yields and without racemisation problems, in addition to using simple and available starting products. The invention also provides a process for preparing the intermediate of formula (VI), from an intermediate of formula (V) that does not require protection of the carboxylic acid prior to N-acylation.
摘要翻译：本发明涉及一种制备用于制备缬沙坦的中间体的方法及其制备方法，以及用于制备用于治疗动脉的药物的式（IV），（V）和（VI）的合成中间体高血压或心力衰竭。制备缬沙坦的过程允许以高产量和无外消旋化问题，以工业规模进行准备，除了使用简单和可用的起始产品。本发明还提供了从N-酰化之前不需要保护羧酸的式（Ⅴ）中间体制备式（Ⅵ）中间体的方法。

2. 发明申请

US20090221836A1 PROCESS FOR THE PREPARATION OF VALSARTAN AND PRECURSORS THEREOF 失效
标题翻译：制备VALSARTAN及其前驱物的方法
公开(公告)号：US20090221836A1
公开(公告)日：2009-09-03
申请号：US11568054
申请日：2005-04-18
申请人： Jordi Bessa Bellmunt , Joan Huguet Clotet , Juan Antonio Perez Andres , Pere Dalmases Barjoan
发明人： Jordi Bessa Bellmunt , Joan Huguet Clotet , Juan Antonio Perez Andres , Pere Dalmases Barjoan
IPC分类号： C07D257/04 , C07C229/00
CPC分类号： C07D257/04
摘要： This invention relates to a process for preparing intermediates useful in preparing Valsartan and to a process for preparing the latter, together with synthesis intermediates of formula (IV), (V) and (VI), useful for manufacturing a medicament for the treatment of arterial hypertension or heart failure. The process for preparing Valsartan permits it to be prepared on an industrial scale with high yields and without racemisation problems, in addition to using simple and available starting products. The invention also provides a process for preparing the intermediate of formula (VI), from an intermediate of formula (V) that does not require protection of the carboxylic acid prior to N-acylation.
摘要翻译：本发明涉及一种制备用于制备缬沙坦的中间体的方法及其制备方法，以及用于制备用于治疗动脉的药物的式（IV），（V）和（VI）的合成中间体高血压或心力衰竭。制备缬沙坦的过程允许以高产量和无外消旋化问题，以工业规模进行准备，除了使用简单和可用的起始产品。本发明还提供了从N-酰化之前不需要保护羧酸的式（Ⅴ）中间体制备式（Ⅵ）中间体的方法。

3. 发明申请

US20090124807A1 INTERMEDIATE COMPOUNDS USEFUL TO PREPARE DOLASETRON 失效
标题翻译：中间体化合物有助于制备DOLASETRON
公开(公告)号：US20090124807A1
公开(公告)日：2009-05-14
申请号：US12017709
申请日：2008-01-22
申请人： Juan Antonio Perez Andres , Pere Dalmases Barjoan , Joan Huguet Clotet
发明人： Juan Antonio Perez Andres , Pere Dalmases Barjoan , Joan Huguet Clotet
IPC分类号： C07D471/18 , C07C69/708 , C07D453/02
CPC分类号： C07C67/313 , C07C67/32 , C07C67/343 , C07C69/708 , C07D451/14 , C07D471/18 , C07D471/22 , C07C69/716
摘要： The present invention relates to intermediates useful in the synthesis of Dolasetron and synthetic precursors thereof, as well as to processes for obtaining them. In addition, it refers to the hydrochloric salt of Dolasetron and polymorphic forms of Dolasetron and precursors thereof.
摘要翻译：本发明涉及可用于合成杜拉司琼及其合成前体的中间体以及获得它们的方法。此外，它是指多沙司琼的盐酸盐和多沙司琼的多晶型物及其前体。

4. 发明申请

US20080194825A1 PROCESS FOR OBTAINING MONTELUKAST 审中-公开
标题翻译：获取MONTELUKAST的过程
公开(公告)号：US20080194825A1
公开(公告)日：2008-08-14
申请号：US11736912
申请日：2007-04-18
申请人： Juan Antonio Perez Andres , Juan Huguet Clotet , Pere Dalmases Barjoan
发明人： Juan Antonio Perez Andres , Juan Huguet Clotet , Pere Dalmases Barjoan
IPC分类号： C07D215/18 , C07C69/76
CPC分类号： C07D215/18
摘要： The present invention refers to a process for the synthesis of (1-{1-(R)-(E)-{3-[2-(7-chloro-quinolin-2-yl)-vinyl]-phenyl}-3-[2-(1-hydroxy-1-methyl-ethyl)-phenyl]-propylsulfanylmethyl}-cyclopropyl)-acetic acid or its salts, comprising the reaction between 7-Chloro-2-vinyl-quinoline and a compound of formula (I) wherein X is a halogen atom or a group of formula —OSO2R, wherein R is selected from the group consisting of CF3, tolyl, methyl and F; in the presence of a palladium based catalyst. The invention is also directed to intermediates compounds of the process.
摘要翻译：本发明涉及合成（1- {1-（R） - （E） - {3- [2-（7-氯 - 喹啉-2-基） - 乙烯基] - 苯基} -3 - [2-（1-羟基-1-甲基 - 乙基） - 苯基] - 丙基硫烷基甲基} - 环丙基） - 乙酸或其盐，包括7-氯-2-乙烯基 - 喹啉与式 I）其中X是卤素原子或式-OSO 2 R R基团，其中R选自CF 3，甲苯基，甲基和F; 在钯基催化剂的存在下。本发明还涉及该方法的中间体化合物。

5. 发明授权

US07745628B2 Method for obtaining a pharmaceutically active compound, synthesis intermediates thereof and methods for obtaining them 有权
标题翻译：获得药物活性化合物的方法，其合成中间体及其获得方法
公开(公告)号：US07745628B2
公开(公告)日：2010-06-29
申请号：US11994667
申请日：2006-06-26
申请人： Juan Antonio Perez Andres , Pere Dalmases Barjoan
发明人： Juan Antonio Perez Andres , Pere Dalmases Barjoan
IPC分类号： C07D221/22 , C07D451/00 , C07D453/00 , C07D455/00
CPC分类号： C07D451/06 , Y02P20/55
摘要： The present invention relates to a method for obtaining Dolasetron that comprises: a) Esterification of the alcohol of formula (IV) with indole-3-carboxylic acid (compound (III)) or a reactive derivative thereof, to give a compound of formula (V), followed by step b) which includes Dieckmann reaction of the intermediate (V), by reaction with a strong organic or inorganic base, to give the intermediate (VI), and step c) which comprises dealcoxycarbonylation of the intermediate (VI) to give Dolasetron base and, if desired, a pharmaceutically acceptable salt thereof, hydrates or solvates of the base of said salt. The invention also relates to the intermediates (V) and (VI), and methods for obtaining them. With the method of the present invention Dolasetron is obtained at industrial scale with good yields, with decreased use of reactants and solvents, while said method is also of greater atomic efficiency.
摘要翻译：本发明涉及一种获得杜拉司琼的方法，该方法包括：a）式（Ⅳ）的醇与吲哚-3-羧酸（化合物（Ⅲ））或其活性衍生物酯化，得到式 V），然后是步骤b），其包括中间体（V）的Dieckmann反应，通过与强有机或无机碱反应得到中间体（VI），和步骤c），其包括中间体（VI）的反式羟基羰基化反应，给予多沙司琼碱，以及如果需要，其药学上可接受的盐，所述盐的碱的水合物或溶剂合物。本发明还涉及中间体（V）和（VI）及其获得方法。利用本发明的方法，以工业规模获得了具有良好产率的Dolasetron，反应物和溶剂的使用减少，而所述方法也具有更高的原子效率。

6. 发明申请

US20080194824A1 Method For Obtaining A Pharmaceutically Active Compound, Synthesis Intermediates Thereof And Methods For Obtaining Them 有权
标题翻译：获得药物活性化合物的方法，其合成中间体及其获得方法
公开(公告)号：US20080194824A1
公开(公告)日：2008-08-14
申请号：US11994667
申请日：2006-06-26
申请人： Juan Antonio Perez Andres
发明人： Juan Antonio Perez Andres
IPC分类号： C07D451/00
CPC分类号： C07D451/06 , Y02P20/55
摘要： The present invention relates to a method for obtaining Dolasetron that comprises: a) Esterification of the alcohol of formula (IV) with indole-3-carboxylic acid (compound (III)) or a reactive derivative thereof, to give a compound of formula (V), followed by step b) which includes Dieckmann reaction of the intermediate (V), by reaction with a strong organic or inorganic base, to give the intermediate (VI), and step c) which comprises dealcoxycarbonylation of the intermediate (VI) to give Dolasetron base and, if desired, a pharmaceutically acceptable salt thereof, hydrates or solvates of the base of said salt. The invention also relates to the intermediates (V) and (VI), and methods for obtaining them. With the method of the present invention Dolasetron is obtained at industrial scale with good yields, with decreased use of reactants and solvents, while said method is also of greater atomic efficiency.
摘要翻译：本发明涉及一种获得杜拉司琼的方法，该方法包括：a）式（Ⅳ）的醇与吲哚-3-羧酸（化合物（Ⅲ））或其活性衍生物酯化，得到式 V），然后是步骤b），其包括中间体（V）的Dieckmann反应，通过与强有机或无机碱反应得到中间体（VI），和步骤c），其包括中间体（VI）的反式羟基羰基化反应，给予多沙司琼碱，以及如果需要，其药学上可接受的盐，所述盐的碱的水合物或溶剂合物。本发明还涉及中间体（V）和（VI）及其获得方法。利用本发明的方法，以工业规模获得了具有良好产率的Dolasetron，反应物和溶剂的使用减少，而所述方法也具有更高的原子效率。

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