专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

1. 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。

2. 发明申请

US20090111849A1 CRYSTALLINE SALT OF MONTELUKAST 审中-公开
标题翻译： MONTELUKAST的晶体盐
公开(公告)号：US20090111849A1
公开(公告)日：2009-04-30
申请号：US11965730
申请日：2007-12-27
申请人： Joan Huguet Clotet , Jordi Peirats Masia
发明人： Joan Huguet Clotet , Jordi Peirats Masia
IPC分类号： A61K31/47 , C07D215/18
CPC分类号： C07D215/18
摘要： Cyclopropylamine salt of montelukast in crystalline form and its use for the preparation of highly pure amorphous montelukast sodium.
摘要翻译：结晶形式的孟鲁司特环丙胺盐及其用于制备高纯度无定型孟鲁司特钠的用途。

3. 发明授权

US06455585B1 Esters derived from substituted phennyl-cyclohexyl compounds 失效
标题翻译：衍生自取代的苯基 - 环己基化合物的酯
公开(公告)号：US06455585B1
公开(公告)日：2002-09-24
申请号：US09831177
申请日：2001-05-04
申请人： Juan Carlos Del Castillo Nieto , Joan Huguet Clotet , Elisabet De Ramon Amat , Maria Chalaux Freixa , Marisabel Mourelle Mancini
发明人： Juan Carlos Del Castillo Nieto , Joan Huguet Clotet , Elisabet De Ramon Amat , Maria Chalaux Freixa , Marisabel Mourelle Mancini
IPC分类号： C07C6978
CPC分类号： C07C271/44 , C07B2200/07 , C07C219/28 , C07C219/30 , C07C2601/14 , C07C2601/16 , C07D487/04
摘要： New esters derived from substituted phenyl-cyclohexyl compounds, which are derived from Tramadol, process for obtaining them and their use for preparing a drug with analgesic properties. These new compounds of general formula (I) have a higher analgesic activity, a lower toxicity and a longer effective time period than Tramadol.
摘要翻译：衍生自衍生自曲马多的取代的苯基 - 环己基化合物的新酯，用于获得它们的方法及其用于制备具有止痛性质的药物的用途。这些新的通式（I）化合物与曲马多相比具有较高的镇痛活性，较低的毒性和较长的有效时间。

4. 发明授权

US07741492B2 Method for obtaining a pharmaceutically active compound (Irbesartan) and its synthesis intermediate 有权
标题翻译：获得药物活性化合物（厄贝沙坦）及其合成中间体的方法
公开(公告)号：US07741492B2
公开(公告)日：2010-06-22
申请号：US11909757
申请日：2006-02-23
申请人： Joan Huguet Clotet , Pere Dalmases Barjoan
发明人： Joan Huguet Clotet , Pere Dalmases Barjoan
IPC分类号： C07D257/00
CPC分类号： C07D235/02 , C07D403/10
摘要： It is provided a method for obtaining Irbesartan polymorph A, with few synthesis steps, by coupling the intermediate of formula (II) with the compound of formula (III), neutralising one of its alkaline salts in an aqueous medium and recrystallising the crude product obtained. The utilisation of said method obviates protection and deprotection of the tetrazole ring and is therefore of considerable interest for obtaining Irbesartan on a large industrial scale. The invention also refers to the synthesis intermediate of formula (II).
摘要翻译：提供了一种通过将式（II）的中间体与式（III）的化合物偶联在水性介质中中和其中的一种碱性盐并重结晶得到的粗产物而获得的厄贝沙坦多晶型A几乎没有合成步骤的方法。所述方法的利用消除了四唑环的保护和去保护，因此在大规模工业规模上获得厄贝沙坦是非常有意义的。本发明还涉及式（II）的合成中间体。

5. 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。

6. 发明授权

US07964749B2 Process for obtaining valine derivatives useful for obtaining a pharmaceutically active compound 失效
标题翻译：用于获得可用于获得药学活性化合物的缬氨酸衍生物的方法
公开(公告)号：US07964749B2
公开(公告)日：2011-06-21
申请号：US12090729
申请日：2006-10-19
申请人： Pere Dalmases Barjoan , Joan Huguet Clotet
发明人： Pere Dalmases Barjoan , Joan Huguet Clotet
IPC分类号： C07C233/31 , C07C305/24
CPC分类号： C07D257/04
摘要： The invention provides a method for obtaining the intermediate (II), useful for manufacturing Valsartan and a drug directed to a treatment of arterial hypertension or heart failure. The process comprises a) Imination of the aldehyde group of a compound (VII) by L-Valine (IV) salts with organic or inorganic bases and a polar solvent or water, where X means halogen or an —OSO2R group, where R is CF3, tolyl, methyl or F; to give an imine-type compound (VIII), where B+ is the protonated form of an organic base or an alkaline cation; b) Reduction of the imine group of the compound (VIII) followed by acidification, to give the compound (VI); and c) N-Acylation of the compound (VI) with valeryl chloride to give the compound (II). Steps a) and b) can be performed in a “one pot” reaction.
摘要翻译：本发明提供了获得中间体（II）的方法，其可用于制造缬沙坦和用于治疗动脉高血压或心力衰竭的药物。该方法包括a）用有机或无机碱和极性溶剂或水将L-缬氨酸（Ⅳ）盐与化合物（Ⅶ）的醛基进行偶联，其中X表示卤素或-OSO 2 R基团，其中R为CF 3 ，甲苯基，甲基或F; 得到亚胺型化合物（VIII），其中B +是有机碱或碱性阳离子的质子化形式; b）还原化合物（Ⅷ）的亚胺基，然后酸化，得到化合物（Ⅵ）; 和c）将化合物（VI）与戊酰氯进行N-酰化反应，得到化合物（II）。步骤a）和b）可以在“一锅”反应中进行。

7. 发明授权

US07858821B2 Intermediate compounds useful to prepare dolasetron 失效
标题翻译：可用于制备多拉司琼的中间体化合物
公开(公告)号：US07858821B2
公开(公告)日：2010-12-28
申请号：US12017709
申请日：2008-01-22
申请人： Juan Antonio Pérez Andrés , Pere Dalmases Barjoan , Joan Huguet Clotet
发明人： Juan Antonio Pérez Andrés , Pere Dalmases Barjoan , Joan Huguet Clotet
IPC分类号： C07C69/66
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。

8. 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。

9. 发明申请

US20100240919A1 Process For Obtaining Valine Derivatives Useful For Obtaining A Pharmaceutically Active Compound 失效
标题翻译：获得有用的药物活性化合物的缬氨酸衍生物的方法
公开(公告)号：US20100240919A1
公开(公告)日：2010-09-23
申请号：US12090729
申请日：2006-10-19
申请人： Pere Dalmases Barjoan , Joan Huguet Clotet
发明人： Pere Dalmases Barjoan , Joan Huguet Clotet
IPC分类号： C07C303/26 , C07C227/16
CPC分类号： C07D257/04
摘要： The invention provides a method for obtaining the intermediate (II), useful for manufacturing Valsartan and a drug directed to a treatment of arterial hypertension or heart failure. The process comprises a) Imination of the aldehyde group of a compound (VII) by L-Valine (IV) salts with organic or inorganic bases and a polar solvent or water, where X means halogen or an —OSO2R group, where R is CF3, tolyl, methyl or F; to give an imine-type compound (VIII), where B+ is the protonated form of an organic base or an alkaline cation; b) Reduction of the imine group of the compound (VIII) followed by acidification, to give the compound (VI); and c) N-Acylation of the compound (VI) with valeryl chloride to give the compound (II). Steps a) and b) can be performed in a “one pot” reaction.
摘要翻译：本发明提供了获得中间体（II）的方法，其可用于制造缬沙坦和用于治疗动脉高血压或心力衰竭的药物。该方法包括a）用有机或无机碱和极性溶剂或水将L-缬氨酸（Ⅳ）盐与化合物（Ⅶ）的醛基进行偶联，其中X表示卤素或-OSO 2 R基团，其中R为CF 3 ，甲苯基，甲基或F; 得到亚胺型化合物（VIII），其中B +是有机碱或碱性阳离子的质子化形式; b）还原化合物（Ⅷ）的亚胺基，然后酸化，得到化合物（Ⅵ）; 和c）将化合物（VI）与戊酰氯进行N-酰化反应，得到化合物（II）。步骤a）和b）可以在“一锅”反应中进行。

10. 发明申请

US20090124677A1 Method For Obtaining A Pharmaceutically Active Compound (Irbesartan) And Its Synthesis Intermediate 有权
标题翻译：获得药物活性化合物（厄贝沙坦）及其合成中间体的方法
公开(公告)号：US20090124677A1
公开(公告)日：2009-05-14
申请号：US11909757
申请日：2006-02-23
申请人： Joan Huguet Clotet , Pere Dalmases Barjoan
发明人： Joan Huguet Clotet , Pere Dalmases Barjoan
IPC分类号： A61K31/4178 , C07D403/08 , C07D235/02
CPC分类号： C07D235/02 , C07D403/10
摘要： It is provided a method for obtaining Irbesartan polymorph A, with few synthesis steps, by coupling the intermediate of formula (II) with the compound of formula (III), neutralising one of its alkaline salts in an aqueous medium and recrystallising the crude product obtained. The utilisation of said method obviates protection and deprotection of the tetrazole ring and is therefore of considerable interest for obtaining Irbesartan on a large industrial scale. The invention also refers to the synthesis intermediate of formula (II).
摘要翻译：提供了一种通过将式（II）的中间体与式（III）的化合物偶联在水性介质中中和其中的一种碱性盐并重结晶得到的粗产物而获得的厄贝沙坦多晶型A几乎没有合成步骤的方法。所述方法的利用消除了四唑环的保护和去保护，因此在大规模工业规模上获得厄贝沙坦是非常有意义的。本发明还涉及式（II）的合成中间体。

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式