公开(公告)号：WO2012035057A3

公开(公告)日：2012-08-16

申请号：PCT/EP2011065925

申请日：2011-09-14

Applicant: MEDICHEM SA ,  MANGION BERNARDINO ,  DURAN LOPEZ ERNESTO

Inventor： MANGION BERNARDINO ,  DURAN LOPEZ ERNESTO

IPC: C07D413/14

CPC classification number: C07D413/14 ,  G01N33/15

Abstract: The present invention relates to a process for determining the suitability for distribution of a batch of rivaroxaban or of a pharmaceutical composition thereof. In particular, it also relates to two impurities of rivaroxaban, to their use as reference markers to determine the purity of a sample of rivaroxaban or a composition thereof, to analytical methods for determining the purity of a sample of rivaroxaban or a composition thereof and to a process of preparing rivaroxaban or pharmaceutical compositions thereof which are free or substantially free of such impurities.

Abstract translation: 本发明涉及一种用于确定一批利伐沙班或其药物组合物分布的适用性的方法。 特别地，它还涉及利伐沙班的两种杂质，用作参考标记用于确定利伐沙班或其组合物的样品的纯度，用于测定利伐沙班或其组合物样品的纯度的分析方法，以及 制备游离或基本上不含这些杂质的利伐沙班或其药物组合物的方法。

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：WO2011009873A3

公开(公告)日：2011-05-05

申请号：PCT/EP2010060509

申请日：2010-07-20

Applicant: MEDICHEM SA ,  MASLLORENS LLINAS ESTER ,  DURAN LOPEZ ERNESTO

Inventor： MASLLORENS LLINAS ESTER ,  DURAN LOPEZ ERNESTO

IPC: C07C211/42 ,  A61K31/135 ,  A61P25/16

CPC classification number: C07C211/42 ,  C07C2602/08

Abstract: The invention relates to rasagiline mesylate with improved flowability and compressibility and with advantageously reduced stickiness, to processes for the preparation thereof, and to the use thereof for milling and for preparing pharmaceutical formulations. Also, the invention relates to a method for improving the flowability and / or alleviating the stickiness of rasagiline mesylate having a very poor flowability and / or showing undesirable stickiness.

Abstract translation: 本发明涉及具有改善的流动性和可压缩性以及有利地降低的粘性的甲磺酸雷沙吉兰，其制备方法及其用于研磨和用于制备药物制剂的用途。 此外，本发明涉及一种改善流动性和/或减轻具有非常差的流动性和/或显示不期望的粘性的甲磺酸雷沙吉兰的粘性的方法。

公开(公告)号：WO2008044153A2

公开(公告)日：2008-04-17

申请号：PCT/IB2007/004313

申请日：2007-08-29

Applicant: MEDICHEM, S.A. ,  BENITO VELEZ, Monica ,  WINTER, Stephen ,  DURAN LOPEZ, Ernesto

Inventor： BENITO VELEZ, Monica ,  WINTER, Stephen ,  DURAN LOPEZ, Ernesto

CPC classification number: C07D231/14

Abstract: The invention relates to a process for preparing rimonabant. In particular, the invention relates to minimizing the presence and effects of certain by-products and impurities present in rimonabant occurring during the synthesis of rimonabant.

Abstract translation: 本发明涉及一种制备利莫那班的方法。 特别地，本发明涉及最小化在利莫那班合成期间发生的利莫那班中存在的某些副产物和杂质的存在和影响。

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：WO2011012659A2

公开(公告)日：2011-02-03

申请号：PCT/EP2010/060981

申请日：2010-07-28

Applicant: MEDICHEM S.A. ,  SERRA MIRALLES, Judit ,  DURAN LOPEZ, Ernesto ,  BOSCH I LLADÓ, Jordi

Inventor： SERRA MIRALLES, Judit ,  DURAN LOPEZ, Ernesto ,  BOSCH I LLADÓ, Jordi

IPC: C07C271/28

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-亚苯基二氨基甲酸二乙酯（IV）及其盐，其可用作分析包含瑞替加滨或其盐的样品的参考标记和参考标准。 还公开了制备化合物（IV）及其盐的方法。

公开(公告)号：WO2011101456A2

公开(公告)日：2011-08-25

申请号：PCT/EP2011/052469

申请日：2011-02-18

Applicant: MEDICHEM S.A. ,  DURAN LOPEZ, Ernesto ,  BOSCH I LLADÓ, Jordi ,  SERRA MIRALLES, Judit

Inventor： DURAN LOPEZ, Ernesto ,  BOSCH I LLADÓ, 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。 此外，本发明涉及一种干燥瑞他滨的方法。 此外，本发明涉及稳定的或基本上稳定的固体化的瑞替加滨或包含其的药物制剂。 此外，本发明还涉及一种制备瑞替加滨的改进方法。

公开(公告)号：WO2011061272A2

公开(公告)日：2011-05-26

申请号：PCT/EP2010/067782

申请日：2010-11-18

Applicant: MEDICHEM S.A. ,  SANCHEZ SALGUERO, Laura ,  BOU BOSCH, Raquel ,  BOSCH I LLADÓ, Jordi ,  CAMACHO CARRASCO, Antonio ,  DURAN LOPEZ, Ernesto ,  ANDRES MAGNANI, Pablo

Inventor： SANCHEZ SALGUERO, Laura ,  BOU BOSCH, Raquel ,  BOSCH I LLADÓ, Jordi ,  CAMACHO CARRASCO, Antonio ,  DURAN LOPEZ, Ernesto ,  ANDRES MAGNANI, Pablo

IPC: C07C279/18 ,  C07C277/08

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: 本发明涉及一种减少氯己定中对氯苯胺残留量的方法。 而且，本发明涉及制备无潜在遗传毒性的氯己定或其药学上可接受的盐的方法。 另外，本发明涉及所述没有潜在遗传毒性的氯己定或其药学上可接受的盐。 此外，本发明涉及用于测定氯己定或其药学上可接受的盐样品中潜在遗传毒性杂质的分析HPLC方法。 本发明还涉及在水溶液中无潜在遗传毒性的稳定的氯己定二葡糖酸盐，以及稳定在水溶液中无潜在遗传毒性的氯己定二葡糖酸盐的方法。

公开(公告)号：WO2011039369A2

公开(公告)日：2011-04-07

申请号：PCT/EP2010/064694

申请日：2010-10-01

Applicant: MEDICHEM S.A. ,  BENITO VELEZ, Monica ,  DURAN LOPEZ, Ernesto

Inventor： BENITO VELEZ, Monica ,  DURAN LOPEZ, Ernesto

IPC: A61K9/14

CPC classification number: C07C271/28 ,  A61K9/0019 ,  A61K9/146 ,  A61K9/1694 ,  A61K9/2086 ,  A61K31/27

Abstract: The invention relates to a stable amorphous solid mixture of retigabine and at least one pharmaceutically acceptable carrier, to processes for preparing the same, to solid pharmaceutical formulations comprising the same, and to said mixture or formulation stabilized in a container or packaging.

Abstract translation: 本发明涉及瑞格列宾和至少一种药学上可接受的载体的稳定无定形固体混合物，其制备方法，包含其的固体药物制剂以及稳定在容器或包装中的所述混合物或制剂。