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

US20100010265A1 PROCESS FOR THE PREPARATION OF AROMATIC DERIVATIVES OF 1-ADAMANTANE 审中-公开
标题翻译：制备1-亚氨酸的芳族衍生物的方法
公开(公告)号：US20100010265A1
公开(公告)日：2010-01-14
申请号：US12563579
申请日：2009-09-21
申请人： Alexander Christian Comely , Marta Marfil Sanchez , Llorenc Rafecas Jane , Xavier Verdaguer Espaulella
发明人： Alexander Christian Comely , Marta Marfil Sanchez , Llorenc Rafecas Jane , Xavier Verdaguer Espaulella
IPC分类号： C07F5/02
CPC分类号： C07C43/225 , C07C51/15 , C07C2603/74 , C07C65/26
摘要： Process for the obtaining of 1-adamantane (tricycle[3.3.1.1 (3,7)]decane) derivatives, or of a pharmaceutically acceptable salt thereof, based on a carboxylation reaction, via metallation, of a precursor compound with an adequate leaving group. It also comprises the preparation of the precursor compound by means of a selective coupling of the corresponding boron, magnesium or zinc derivative with the corresponding disubstitute aromatic derivative. It is especially useful for the obtaining of Adapalene at industrial scale with good yield and high purity.
摘要翻译：基于前体化合物与足够的离去基团的金属化的羧基化反应获得1-金刚烷（三环[3.3.1.1（3,7）]癸烷）衍生物或其药学上可接受的盐的方法。它还包括通过相应的硼，镁或锌衍生物与相应的取代芳族衍生物的选择性偶联制备前体化合物。特别适用于以高产率和高纯度获得工业规模的阿达帕林。

2. 发明申请

US20080171869A1 Process For The Preparation Of An 11-(4-Substituted-I- Piperazinyl)Dibenzo[B,F][1,4:rsqb; Thiazepine Derivative 失效
标题翻译：制备11-（4-取代的 - 哌嗪基）二苯并[B，F] [1,4：rsqb; 噻吩衍生物
公开(公告)号：US20080171869A1
公开(公告)日：2008-07-17
申请号：US11817884
申请日：2005-12-21
申请人： Alexander Christian Comely , Francesc Xavier Verdaguer Espaulella , Llorenc Rafecas Jane , Antonio Domingo Coto
发明人： Alexander Christian Comely , Francesc Xavier Verdaguer Espaulella , Llorenc Rafecas Jane , Antonio Domingo Coto
IPC分类号： C07D281/16
CPC分类号： C07D281/16
摘要： A process for the preparation of an 11-(4-substituted-1-piperazinyl)dibenzo[b,f][1,4]thiazepine derivative, of general Formula (I), where A is hydrogen or a —(CH2)2—OH group or a —(CH2)2-0-(CH2)2—OH group, or of a salt thereof, comprises a step in which 10H-dibenzo[b,f][1,4]thiazepin-11-one is reacted with a piperazine derivative in the presence of a titanium alkoxide of general formula Ti(OR)4, where R is a straight or branched alkyl group, having from one to eight carbon atoms to obtain said Formula I derivative or a salt thereof. Where A is —CH2)2-0-(CH2)2—OH, then the piperazine derivative is 1-(2-(2-hydroxyethoxy)ethyl)piperazine and the 11-(4-substituted-1-piperazinyl)dibenzo[b,f][1,4]thiazepine is quetiapine, (11-(4-(2-(2-hydroxyethoxy)ethyl)-1-piperazinyl)dibenzo[b,f][1,4]thiazepine). The process may comprise an additional step of reacting the quetiapine with fumaric acid to obtain quetiapine hemifumarate.
摘要翻译：制备通式（I）的11-（4-取代-1-哌嗪基）二苯并[b，f] [1,4]硫杂吗啉衍生物的方法，其中A是氢或 - （CH

3. 发明申请

US20090137841A1 PROCESS FOR THE PREPARATION OF AROMATIC DERIVATIVES OF 1-ADAMANTANE 失效
标题翻译：制备1-亚氨酸的芳族衍生物的方法
公开(公告)号：US20090137841A1
公开(公告)日：2009-05-28
申请号：US12095376
申请日：2006-12-01
申请人： Alexander Christian Comely , Marta Marfil Sanchez , Llorenc Rafecas Jane , Xavier Verdaguer Espaulella
发明人： Alexander Christian Comely , Marta Marfil Sanchez , Llorenc Rafecas Jane , Xavier Verdaguer Espaulella
IPC分类号： C07C63/34
CPC分类号： C07C43/225 , C07C51/15 , C07C2603/74 , C07C65/26
摘要： Process for the obtaining of 1-adamantane (tricycle[3.3.1.1 (3,7)]decane) derivatives, or of a pharmaceutically acceptable salt thereof, based on a carboxylation reaction, via metallation, of a precursor compound with an adequate leaving group. It also comprises the preparation of the precursor compound by means of a selective coupling of the corresponding boron, magnesium or zinc derivative with the corresponding disubstitute aromatic derivative. It is especially useful for the obtaining of Adapalene at industrial scale with good yield and high purity.
摘要翻译：基于前体化合物与足够的离去基团的金属化的羧基化反应获得1-金刚烷（三环[3.3.1.1（3,7）]癸烷）衍生物或其药学上可接受的盐的方法。它还包括通过相应的硼，镁或锌衍生物与相应的取代芳族衍生物的选择性偶联制备前体化合物。特别适用于以高产率和高纯度获得工业规模的阿达帕林。

4. 发明申请

US20060142376A1 Method for obtaining an antiepileptic agent 失效
标题翻译：获得抗癫痫剂的方法
公开(公告)号：US20060142376A1
公开(公告)日：2006-06-29
申请号：US10544967
申请日：2004-02-06
申请人： Juan Jose Surroca , Llorenc Rafecas Jane , Lourdes Garriga Sanahuja , Miquel Pericas Brondo , Lluis Carandell
发明人： Juan Jose Surroca , Llorenc Rafecas Jane , Lourdes Garriga Sanahuja , Miquel Pericas Brondo , Lluis Carandell
IPC分类号： A61K31/4015 , C07D207/24
CPC分类号： C07D207/27 , A61K31/4015
摘要： A process for obtaining the pharmaceutical active ingredient, levetiracetam, by means of deaminomethylation of a sufficiently pure enantiomer intermediate (S)-(II), or by means of deaminomethylation of an addition salt thereof with an acid, wherein R1 and R2 are either the same or different (C1-C6)-alkyl radicals, or else R1 and R2 together with the nitrogen atom to which they are bonded form a radical selected from the group consisting of 1-pyrrolidinyl, 1-piperidinyl, 1-morpholinyl, 1-piperazinyl and 1-[4-(C1-C4)-alkylpiperazinyl]. The invention also comprises preparing the sufficiently pure enantiomer intermediate (S)-(II) by treating the corresponding chemically new racemic intermediate (II) with an amine resolving agent, followed by selective crystallisation of a diastereoisomeric salt thereof. It is useful for obtaining levetiracetam on an industrial scale and involves neither hydrogenation nor chromatography.
摘要翻译：通过使足够纯的对映异构体中间体（S） - （II）的脱氨基甲基化或通过其加成盐与酸的脱氨基甲基化获得药物活性成分左乙拉西坦的方法，其中R 1，或者R 2或R 2相同或不同（C 1 -C 6 -C 6 - ） - 烷基，或者R 1， 1和R 2与它们所键合的氮原子一起形成选自以下的基团：1-吡咯烷基，1-哌啶基，1-吗啉基，1-哌嗪基和 1- [4-（C 1 -C 4 - 烷基哌嗪基）]。本发明还包括通过用胺拆分剂处理相应的化学新外消旋中间体（II），然后选择性结晶其非对映异构体盐，来制备足够纯的对映异构体中间体（S） - （II）。在工业规模上获得左乙拉西坦是有用的，既不涉及氢化也不涉及色谱。

5. 发明申请

US20090036677A1 Preparation of Delmopinol 有权
标题翻译：德莫酚的制备
公开(公告)号：US20090036677A1
公开(公告)日：2009-02-05
申请号：US12161593
申请日：2007-01-10
申请人： Alexander Comely , Llorenc Rafecas Jane , Nicolas Tesson , Atoni Riera Escale
发明人： Alexander Comely , Llorenc Rafecas Jane , Nicolas Tesson , Atoni Riera Escale
IPC分类号： C07D265/30 , C07D263/04 , C07C215/06 , C07D303/04 , C07C11/02 , C07C19/075
CPC分类号： C07D263/06 , C07C11/02 , C07C17/16 , C07C19/075 , C07D265/08 , C07D309/04
摘要： It comprises a preparation process of delmopinol or a pharmaceutically acceptable salt and/or a solvate thereof, by submitting the compound of formula (II) where R1 and R2 are the same or different, independently selected from the group consisting of H, (C1-C6)-alkyl or, alternatively, R1 and R2 form, together with the carbon atom to which they are attached, a (C5-C6)-cycloalkyl radical; and R3 is a radical selected from the group consisting of CF3, (C1-C4)-alkyl, phenyl, and phenyl mono- or disubstituted by a radical selected from the group consisting of (C1-C4)-alkyl, halogen and nitro to a deprotection and cyclisation reaction. The process is useful to prepare delmopinol or its salts on an industrial scale. The compound of formula (II) is new and also forms part of the present invention, as well as its preparation process and other new intermediates of said preparation process.
摘要翻译：它包括德米莫酚或其药学上可接受的盐和/或其溶剂化物的制备方法，其中R 1和R 2相同或不同，式（II）化合物独立地选自H，（C1- C 6） - 烷基，或者，R 1和R 2与它们所连接的碳原子一起形成（C 5 -C 6） - 环烷基; 并且R 3是选自以下的基团：CF 3，（C 1 -C 4） - 烷基，苯基和被选自（C 1 -C 4） - 烷基，卤素和硝基的基团单或双取代的苯基，脱保护和环化反应。该工艺可用于在工业规模上制备德莫莫醇或其盐。式（II）化合物是新的，也是本发明的一部分，以及其制备方法和所述制备方法的其它新中间体。

6. 发明申请

US20090124577A1 Intermediate Compounds for the Preparation of an Angiotensin II Receptor Antagonist 审中-公开
标题翻译：用于制备血管紧张素II受体拮抗剂的中间体化合物
公开(公告)号：US20090124577A1
公开(公告)日：2009-05-14
申请号：US11722640
申请日：2005-12-22
申请人： Llorenc Rafecas Jane , Antoni Riera Escale , Marta Ecija Queralt , Albert Moyano Baldoire , Alex Comely , Irene Casalprim Castella
发明人： Llorenc Rafecas Jane , Antoni Riera Escale , Marta Ecija Queralt , Albert Moyano Baldoire , Alex Comely , Irene Casalprim Castella
IPC分类号： A61K31/69 , C07F5/04
CPC分类号： C07D257/04 , C07F5/025
摘要： It comprises new substituted 4-valinylmethylphenyl boronic acids of formula (II) and their derivatives and also its preparation process. It also comprises a preparation process of Valsartan (I) from such intermediates. The process comprises the reaction of the new 4-valinylmethylphenyl boronic compounds with a (halophenyl)tetrazole compound which proceeds with high yields. The process is particularly advantageous in its practical industrial realization because it avoids the use of azide derivatives and also the use of expensive biphenyl intermediates.
摘要翻译：它包括式（II）的新的取代的4-缬氨基甲基苯基硼酸及其衍生物及其制备方法。它还包括从这样的中间体制备缬沙坦（I）的制备方法。该方法包括新的4-缬烯基甲基苯基硼化合物与以高产率进行的（卤代苯基）四唑化合物的反应。该方法在其实际的工业实现中是特别有利的，因为它避免了使用叠氮化物衍生物以及使用昂贵的联苯中间体。

7. 发明申请

US20090099367A1 Process for preparing a leukotriene antagonist 审中-公开
标题翻译：制备白细胞三烯拮抗剂的方法
公开(公告)号：US20090099367A1
公开(公告)日：2009-04-16
申请号：US12281947
申请日：2007-03-05
申请人： Jordi Bessa Bellmunt , Llorenc Rafecas Jane , Mireia Pasto Aguila , Xavier Verdaguer Espaulella , Esther Gordo Campon
发明人： Jordi Bessa Bellmunt , Llorenc Rafecas Jane , Mireia Pasto Aguila , Xavier Verdaguer Espaulella , Esther Gordo Campon
IPC分类号： C07D215/18 , C07C321/20
CPC分类号： C07D215/18 , C07C319/14 , C07C323/53 , C07C2601/02
摘要： Process for preparing montelukast or a pharmaceutically acceptable salt thereof, especially its sodium salt, that comprises the condensation of an aldehyde and 7-chloro-2-methylquinoline. Moreover, novel intermediates useful for the synthesis of montelukast are described as well as their preparation.
摘要翻译：制备孟鲁司特或其药学上可接受的盐，特别是其钠盐的方法，其包括醛与7-氯-2-甲基喹啉的缩合。此外，描述了可用于合成孟鲁司特的新型中间体及其制备方法。

8. 发明申请

US20080300411A1 Process for the Preparation of the (S)-Enantiomer of Omeprazole 失效
标题翻译：制备奥美拉唑（S） - 对映异构体的方法
公开(公告)号：US20080300411A1
公开(公告)日：2008-12-04
申请号：US12159565
申请日：2006-12-18
申请人： Antonio Domingo Coto , Alexander Comely , Xavier Verdaguer Espaulella , Llorenc Rafecas Jane
发明人： Antonio Domingo Coto , Alexander Comely , Xavier Verdaguer Espaulella , Llorenc Rafecas Jane
IPC分类号： C07D401/12
CPC分类号： C07D401/12
摘要： A process for the preparation of (S)-omeprazole from racemic omeprazole via the formation of an inclusion complex with (S)-1,1,2-triphenyl-1,2-ethanediol. (S)-Omeprazole is recovered in a substantially optically pure form either in neutral form or as a pharmaceutically acceptable salt or as its solvates including hydrates. The (S)-omeprazole 2[(S)-1,1,2-triphenyl-1,2-ethanediol] inclusion complex is new. This resolution process proceeds with high yields and high optical purity.
摘要翻译：通过与（S）-1,1,2-三苯基-1,2-乙二醇形成包合络合物从外消旋奥美拉唑制备（S） - 奥美拉唑的方法。（S） - 奥美拉唑以中性形式或作为药学上可接受的盐或作为其溶剂化物包括水合物的基本光学纯的形式回收。（S） - 梅拉唑2 [（S）-1,1,2-三苯基-1,2-乙二醇]包合物是新的。该分解方法以高产率和高的光学纯度进行。

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