公开(公告)号：WO2011101456A3

公开(公告)日：2011-10-27

申请号：PCT/EP2011052469

申请日：2011-02-18

Applicant: MEDICHEM SA ,  DURAN LOPEZ ERNESTO ,  BOSCH I LLADO JORDI ,  SERRA MIRALLES JUDIT

Inventor： DURAN LOPEZ ERNESTO ,  BOSCH I LLADO JORDI ,  SERRA MIRALLES JUDIT

IPC: A61K9/00 ,  A61K31/27

CPC classification number: C07C271/28 ,  A61K31/27

Abstract: The invention relates to retigabine with improved color quality, and to processes for preparing the same. In addition, the invention relates to a process for drying wet retigabine. Also, the invention relates to stabilized or substantially stabilized retigabine in solid state or pharmaceutical formulation comprising the same. Further, the invention also relates to an improved process for preparing retigabine.

Abstract translation: 本发明涉及具有改善的颜色质量的瑞替加滨及其制备方法。 另外，本发明涉及用于干燥瑞替加滨的方法。 而且，本发明涉及稳定的或基本上稳定的固体状瑞替加滨或包含其的药物制剂。 此外，本发明还涉及制备瑞替加滨的改进方法。

公开(公告)号：WO2011012659A3

公开(公告)日：2011-03-31

申请号：PCT/EP2010060981

申请日：2010-07-28

Applicant: MEDICHEM SA ,  SERRA MIRALLES JUDIT ,  DURAN LOPEZ ERNESTO ,  BOSCH I LLADO JORDI

Inventor： SERRA MIRALLES JUDIT ,  DURAN LOPEZ ERNESTO ,  BOSCH I LLADO JORDI

IPC: C07C271/28 ,  A61K31/27 ,  A61P25/08

CPC classification number: C07C271/28 ,  A61K31/27

Abstract: Disclosed are diethyl 4-(4-fluorobenzylamino)-l,2-phenylenedicarbamate (IV) and salts thereof, which are useful as reference markers and reference standards for analyzing samples comprising retigabine or salts thereof. Also disclosed is a process for preparing a compound (IV) and salts thereof.

Abstract translation: 公开了4-（4-氟苄基氨基）-1,2-亚苯基二氨基甲酸酯（IV）及其盐，其可用作用于分析包含瑞替加滨或其盐的样品的参考标准和参考标准。 还公开了制备化合物（IV）及其盐的方法。

公开(公告)号：WO2007141593A3

公开(公告)日：2008-02-28

申请号：PCT/IB2006004081

申请日：2006-12-22

Applicant: MEDICHEM SA ,  ARNALOT AGUILAR CARMEN ,  BOSCH I LLADO JORDI

Inventor： ARNALOT AGUILAR CARMEN ,  BOSCH I LLADO JORDI

IPC: C07C213/02 ,  A61K31/135 ,  A61P9/10 ,  A61P9/12 ,  C07C213/08 ,  C07C217/32

CPC classification number: C07C213/02 ,  C07C213/08 ,  C07C213/10 ,  C07C217/32

Abstract: The invention relates to an improved process for preparing metoprolol and its salts.

Abstract translation: 本发明涉及一种制备美托洛尔及其盐的改进方法。

公开(公告)号：WO2011158194A1

公开(公告)日：2011-12-22

申请号：PCT/IB2011/052607

申请日：2011-06-15

Applicant: MEDICHEM, S.A. ,  BOSCH I LLADO, Jordi ,  DURAN LOPEZ, Ernesto

Inventor： BOSCH I LLADO, Jordi ,  DURAN LOPEZ, Ernesto

IPC: C12P13/02

CPC classification number: C12P41/006 ,  C12P13/02 ,  C12P41/007 ,  C12Y301/01003

Abstract: The present invention is concerned with a process of preparing (R)-lacosamide. The process comprises providing an (R,S)-lacosamide precursor and contacting the same with at least an enzyme in the presence of a solvent. The enzyme either stereoselectively hydrolyzes or acetylates an (R)- or (S)-enantiomer of the (R,S)-lacosamide precursor. The process further comprises where appropriate also concurrently, or successively, employing one or more reagents capable of converting the hydrolysed or acetylated (R)- or (S)-enantiomer to (R)- lacosamide.

Abstract translation: 本发明涉及制备（R） - 肉豆蔻酰胺的方法。 该方法包括提供（R，S） - 可可酰胺前体，并在溶剂存在下使其与至少一种酶接触。 该酶可立即选择性地水解或乙酰化（R，S） - 酰胺前体的（R） - （S） - 对映异构体。 该方法还在适当的情况下还同时或相继地使用一种或多种能够将水解或乙酰化的（R） - 或（S） - 对映异构体转化为（R） - 拉诺卡胺的试剂。

公开(公告)号：WO2011061272A3

公开(公告)日：2011-11-10

申请号：PCT/EP2010067782

申请日：2010-11-18

Applicant: MEDICHEM SA ,  SANCHEZ SALGUERO LAURA ,  BOU BOSCH RAQUEL ,  BOSCH I LLADO JORDI ,  CAMACHO CARRASCO ANTONIO ,  DURAN LOPEZ ERNESTO ,  ANDRES MAGNANI PABLO

Inventor： SANCHEZ SALGUERO LAURA ,  BOU BOSCH RAQUEL ,  BOSCH I LLADO JORDI ,  CAMACHO CARRASCO ANTONIO ,  DURAN LOPEZ ERNESTO ,  ANDRES MAGNANI PABLO

IPC: C07C279/18 ,  C07C277/08 ,  C07C279/26

CPC classification number: C07C279/265 ,  C07C277/08

Abstract: The invention relates to a process for reducing the residual amount of p-chloroaniline in chlorhexidine. Also, the invention relates to a process for preparing chlorhexidine, or a pharmaceutically acceptable salt thereof, which is free of potential genotoxicity. In addition, the invention refers to the said chlorhexidine, or a pharmaceutically acceptable salt thereof, which is free of potential genotoxicity. Further, the invention relates to an analytical HPLC method for the determination of potentially genotoxic impurities in samples of chlorhexidine, or of a pharmaceutically acceptable salt thereof. The invention also relates to stabilized chlorhexidine digluconate salt free of potential genotoxicity in aqueous solution, and to a method for stabilizing chlorhexidine digluconate salt free of potential genotoxicity in aqueous solution.

Abstract translation: 本发明涉及减少氯己定中对氯苯胺残留量的方法。 此外，本发明涉及一种不含潜在遗传毒性的氯己定或其药学上可接受的盐的制备方法。 此外，本发明涉及没有潜在遗传毒性的所述氯己定或其药学上可接受的盐。 此外，本发明涉及用于测定洗必太或其药学上可接受的盐样品中潜在遗传毒性杂质的分析型HPLC方法。 本发明还涉及在水溶液中没有潜在的遗传毒性的稳定的氯己定二葡萄糖酸盐，以及在水溶液中不含潜在遗传毒性的氯己定二葡糖酸盐的稳定化方法。

公开(公告)号：WO2009141737A3

公开(公告)日：2009-11-26

申请号：PCT/IB2009/006471

申请日：2009-05-21

Applicant: MEDICHEM, S.A. ,  BOSCH I LLADO, Jordi ,  BURGAROLAS MONTERO, Maria Carmen ,  MASLLORENS LLINAS, Judit

Inventor： BOSCH I LLADO, Jordi ,  BURGAROLAS MONTERO, Maria Carmen ,  MASLLORENS LLINAS, Judit

IPC: C07C209/86 ,  C07C209/84

Abstract: The invention relates to processes for preparing rasagiline mesylate that avoid the use of alcohol solvents, thereby producing rasagiline mesylate free of any alkyl mesylates, including isopropyl mesylate. The invention further relates to processes for purifying rasagiline mesylate to obtain a product free of alkyl mesylates, and to the thus obtained rasagiline mesylate.

公开(公告)号：WO2008152497A1

公开(公告)日：2008-12-18

申请号：PCT/IB2008/001542

申请日：2008-06-13

Applicant: MEDICHEM, S.A. ,  SOLDEVILLA MADRID, Nuria ,  BOSCH I LLADO, Jordi

Inventor： SOLDEVILLA MADRID, Nuria ,  BOSCH I LLADO, Jordi

IPC: C07B57/00 ,  B01D15/38 ,  G01N30/68

CPC classification number: G01N30/88 ,  B01D15/3833 ,  G01N30/02 ,  G01N2030/884 ,  G01N2030/8877

Abstract: The present invention relates to a method for differentiating and quantifying the enantiomers, thereby determining the enantiomeric purity, of darifenacin and its intermediate compounds and salts thereof. In addition, the invention relates to a method for differentiating and quantifying the enantiomers, thereby determining the enantiomeric purity of compounds of formula (I): wherein Y is hydrogen or a substituent of the formula (II): including the differentiation and quantification of compounds of formula (I) of varying enantiomeric purity from their corresponding enantiomers. The invention further relates to a process for preparing enantiomerically pure darifenacin using enantiomerically pure starting compounds which have been previously differentiated and quantified according to the method of the invention.

Abstract translation: 本发明涉及用于分离和定量对映异构体的方法，从而确定达曲他辛及其中间体化合物及其盐的对映体纯度。 此外，本发明涉及用于分离和定量对映异构体的方法，从而测定式（I）化合物的对映体纯度：其中Y是氢或式（II）的取代基：包括化合物的分化和定量 从其相应的对映异构体改变对映体纯度的式（I）化合物。 本发明还涉及使用已经根据本发明的方法预先分化和定量的对映体纯的起始化合物来制备对映体纯的达赖芬那诺的方法。

公开(公告)号：WO2007010412A2

公开(公告)日：2007-01-25

申请号：PCT/IB2006/002875

申请日：2006-05-03

Applicant: MEDICHEM, S.A ,  TOJO SUAREZ, Gabriel ,  DURAN LOPEZ, Ernesto ,  BOSCH I LLADO, Jordi

Inventor： TOJO SUAREZ, Gabriel ,  DURAN LOPEZ, Ernesto ,  BOSCH I LLADO, Jordi

CPC classification number: C07D491/10

Abstract: The present invention relates to a process for preparing racemic narwedine (which can be can be kinetically resolved to yield (-)-narwedine and which is the biogenic precursor of (-)- galanthamine) and the use thereof as a starting material for producing (-)-galanthamine. The invention further includes processes for preparing (-)-galanthamine and (-)-galanthamine hydrobromide, as well as related novel compounds.

Abstract translation: 本发明涉及一种制备外消旋纳诺酮的方法（其可以动力学拆分以产生（ - ） - 诺华定，其为（ - ） - 雪花胺的生物前体）及其用作制备（ - ） - 加兰他敏。 本发明还包括制备（ - ） - 雪花胺和（ - ） - 加兰他宁氢溴酸盐以及相关新化合物的方法。

公开(公告)号：WO2008090465A3

公开(公告)日：2008-09-12

申请号：PCT/IB2008000472

申请日：2008-01-22

Applicant: MEDICHEM SA ,  BOSCH I LLADO JORDI

Inventor： BOSCH I LLADO JORDI

IPC: C07C213/08 ,  C07C215/64

CPC classification number: C07C213/08 ,  C07C2601/14 ,  C07C215/64

Abstract: The invention relates to a process for manufacturing desvenlafaxine free base and salts or solvates thereof, comprising O-demethylating venlafaxine by treatment with 2- (diethylamino) ethanethiol free base or its hydrochloride salt.

Abstract translation: 本发明涉及一种通过用2-（二乙基氨基）乙硫醇游离碱或其盐酸盐处理而制备去甲文拉法辛游离碱及其盐或溶剂化物的方法，其中包括O-去甲基化文拉法辛。

公开(公告)号：WO2007010412A3

公开(公告)日：2007-08-30

申请号：PCT/IB2006002875

申请日：2006-05-03

Applicant: MEDICHEM SA ,  TOJO SUAREZ GABRIEL ,  DURAN LOPEZ ERNESTO ,  BOSCH I LLADO JORDI

Inventor： TOJO SUAREZ GABRIEL ,  DURAN LOPEZ ERNESTO ,  BOSCH I LLADO JORDI

IPC: C07D491/10

CPC classification number: C07D491/10

Abstract: The present invention relates to a process for preparing racemic narwedine (which can be can be kinetically resolved to yield (-)-narwedine and which is the biogenic precursor of (-)- galanthamine) and the use thereof as a starting material for producing (-)-galanthamine. The invention further includes processes for preparing (-)-galanthamine and (-)-galanthamine hydrobromide, as well as related novel compounds.

Abstract translation: 本发明涉及一种制备外消旋Narwedine（其可以动力学拆分得到（ - ） - narwedine并且是（ - ） - 加兰他敏的生物学前体）的制备方法及其作为制备 - ） - 加兰他敏。 本发明进一步包括制备（ - ） - 加兰他敏和（ - ） - 氢溴酸加兰他敏的方法以及相关的新化合物。