公开(公告)号：WO0194331A8

公开(公告)日：2003-11-06

申请号：PCT/US0118014

申请日：2001-06-01

Applicant: LILLY CO ELI ,  COR THERAPEUTICS INC ,  ANTOINE LUC ,  BOQUEL PASCAL ,  BORGHESE ALFIA ,  GORISSEN HUGO ,  MARTINELLI MICHAEL ,  MERSCHAERT ALAIN ,  RUHTER GERD ,  RYPENS CARINE ,  SCARBOROUGH ROBERT ,  SCHOTTEN THEO ,  VAN HOECK JEAN-PIERRE

Inventor： ANTOINE LUC ,  BOQUEL PASCAL ,  BORGHESE ALFIA ,  GORISSEN HUGO ,  MARTINELLI MICHAEL ,  MERSCHAERT ALAIN ,  RUHTER GERD ,  RYPENS CARINE ,  SCARBOROUGH ROBERT ,  SCHOTTEN THEO ,  VAN HOECK JEAN-PIERRE

IPC: C07D311/58 ,  C07D311/70 ,  A61K31/353 ,  A61P7/02

CPC classification number: C07D311/58

Abstract: Disclosed are processes for producing benzopyran compounds, reduced 2-(chroman-2-yl) acetic acid compounds and 2-(6-aminochroman-2-yl)acetic acid esters which are intermediates for producing platelet aggregation inhibitors and/or are themselves potent platelet aggregation inhibitors.

Abstract translation: 公开了制备苯并吡喃化合物，还原的2-（色满-2-基）乙酸化合物和2-（6-氨基苯并二氢吡喃-2-基）乙酸酯的方法，其为制备血小板聚集抑制剂的中间体和/或本身是有效的 血小板聚集抑制剂。

公开(公告)号：WO2012041986A1

公开(公告)日：2012-04-05

申请号：PCT/EP2011/067038

申请日：2011-09-29

Applicant: UCB PHARMA GmbH ,  MERSCHAERT, Alain ,  BOUVY, Didier ,  VASSELIN, David ,  CARLY, Nicolas

Inventor： MERSCHAERT, Alain ,  BOUVY, Didier ,  VASSELIN, David ,  CARLY, Nicolas

IPC: C07C231/02 ,  C07C231/12 ,  C07C231/18 ,  C07C237/22

CPC classification number: C07C231/02 ,  C07B2200/07 ,  C07C231/12 ,  C07C231/16 ,  C07C231/18 ,  C07C237/22

Abstract: The present invention relates to a process of manufacture of compounds of formula (B) wherein R 1 , R 2 and R 3 are as defined for compounds of formula (A), which process comprises hydrogenation of compounds of general formula (A). In particular, the present invention relates to an improved process for the manufacture of Lacosamide (LCM), (R)-2-acetamido-N-benzyl-3-methoxypropion-amide (B1), which is useful as an anticonvulsive drug.

Abstract translation: 本发明涉及式（B）化合物的制备方法，其中R1，R2和R3如式（A）化合物所定义，该方法包括通式（A）化合物的氢化。 特别地，本发明涉及一种用于制造可用作抗惊厥药物的拉科酰胺（LCM），（R）-2-乙酰氨基-N-苄基-3-甲氧基丙酰胺（B1）的改进方法。

公开(公告)号：WO0194333A3

公开(公告)日：2002-06-06

申请号：PCT/US0117765

申请日：2001-06-01

Applicant: LILLY CO ELI ,  ANTOINE LUC ,  BOUQUEL PASCAL ,  BORGHESE ALFIO ,  FISHER MATTHEW ,  GORISSEN HUGO ,  JAKUBOWSKI JOSEPH A ,  KHAU VIEN V ,  MARTINELLI MICHAEL ,  MERSCHAERT ALAIN ,  PAAL MICHAEL ,  RUHTER GERD ,  RYPENS CARINE ,  SCHOTTEN THEO ,  STENZEL WOLFGANG ,  HOECK JEAN PIERRE VAN

Inventor： ANTOINE LUC ,  BOUQUEL PASCAL ,  BORGHESE ALFIO ,  FISHER MATTHEW ,  GORISSEN HUGO ,  JAKUBOWSKI JOSEPH A ,  KHAU VIEN V ,  MARTINELLI MICHAEL ,  MERSCHAERT ALAIN ,  PAAL MICHAEL ,  RUHTER GERD ,  RYPENS CARINE ,  SCHOTTEN THEO ,  STENZEL WOLFGANG ,  VAN HOECK JEAN-PIERRE

IPC: A61K31/353 ,  A61P7/02 ,  A61P9/08 ,  A61P9/10 ,  C07B57/00 ,  C07C257/18 ,  C07D311/58 ,  A61K31/35

CPC classification number: C07D311/58

Abstract: Disclosed are processes for coupling amino substituted 2-chromanyl derivatives and benzoyl derivatives via an amide bond, and intermediates for producing platelet aggregation inhibitors and for producing potent platelet aggregation inhibitors. Also disclosed are processes for producing such compounds from chiral intermediates to provide desired enantiomers, and methods for using the compounds as platelet aggregation inhibitors.

Abstract translation: 公开了通过酰胺键偶联氨基取代的2-苯并二氢吡喃衍生物和苯甲酰基衍生物的方法，以及用于产生血小板聚集抑制剂和产生有效的血小板聚集抑制剂的中间体。 还公开了由手性中间体制备这些化合物以提供所需对映异构体的方法，以及使用该化合物作为血小板聚集抑制剂的方法。

公开(公告)号：WO2010052011A1

公开(公告)日：2010-05-14

申请号：PCT/EP2009/007962

申请日：2009-11-06

Applicant: UCB PHARMA, S.A. ,  BOUVY, Didier ,  MERSCHAERT, Alain ,  PINILLA, Véronique ,  HAMANN, Joerg ,  KANZLER, Ralf ,  THOMAS, Antoine

Inventor： BOUVY, Didier ,  MERSCHAERT, Alain ,  PINILLA, Véronique ,  HAMANN, Joerg ,  KANZLER, Ralf ,  THOMAS, Antoine

IPC: C07C231/20 ,  C07C237/22 ,  C07C237/06 ,  C07C237/52

CPC classification number: C07C231/20 ,  C07C231/18 ,  C07C237/22

Abstract: The present patent application relates to an alternative process for the preparation of amino derivatives. In particular, the present application relates to an improved process for the manufacture of Lacosamide (LCM) , (R)-2-acetamido-N-benzyl-3-methoxypropion-amide, which is useful as an anticonvulsive drug. In a particular aspect, the present invention relates to a process of manufacture of optically enriched (R)-2-acetamido-N-benzyl-3-methoxypropion-amide (I) comprising resolution of 2-acetamido-N-benzyl-3-methoxypropion-amide (II).

Abstract translation: 本专利申请涉及氨基衍生物的制备方法。 特别地，本申请涉及制造用作抗惊厥药物的拉科酰胺（LCM），（R）-2-乙酰氨基-N-苄基-3-甲氧基丙酰胺的改进方法。 在特定方面，本发明涉及制备光学富集的（R）-2-乙酰氨基-N-苄基-3-甲氧基丙酰胺（I）的方法，其包括拆分2-乙酰氨基-N-苄基-3- 甲氧基丙酰胺（II）。

公开(公告)号：WO2006068821A2

公开(公告)日：2006-06-29

申请号：PCT/US2005/044117

申请日：2005-12-07

Applicant: ELI LILLY AND COMPANY ,  BORGHESE, Alfio ,  MANCUSO, Vincenzo ,  MERSCHAERT, Alain

Inventor： BORGHESE, Alfio ,  MANCUSO, Vincenzo ,  MERSCHAERT, Alain

CPC classification number: C07D285/01 ,  C07D471/08

Abstract: The present invention relates to intermediate compounds useful for the preparation of 1,2,5-thiadiazole compounds, including unsymmetrically substituted compounds such as 4-(3-secondary amino-2-hydroxy-propoxy)-1,2,5-thiadiazole compounds and azacyclic or azabicyclic 1,2,5-thiadiazole compounds and to processes for making the same.

Abstract translation: 本发明涉及用于制备1,2,5-噻二唑化合物的中间体化合物，其包括非对称取代的化合物，例如4-（3-仲氨基-2-羟基 - 丙氧基） - 1,2,5-噻二唑化合物和氮杂环或氮杂双环1,2,5-噻二唑化合物及其制备方法。

公开(公告)号：WO2001094331A3

公开(公告)日：2001-12-13

申请号：PCT/US2001/018014

申请日：2001-06-01

Applicant: ELI LILLY & COMPANY ,  COR THERAPEUTICS, INC. ,  ANTOINE, Luc ,  BOQUEL, Pascal ,  BORGHESE, Alfia ,  GORISSEN, Hugo ,  MARTINELLI, Michael ,  MERSCHAERT, Alain ,  RUHTER, Gerd ,  RYPENS, Carine ,  SCARBOROUGH, Robert ,  SCHOTTEN, Theo ,  VAN HOECK, Jean-Pierre

Inventor： ANTOINE, Luc ,  BOQUEL, Pascal ,  BORGHESE, Alfia ,  GORISSEN, Hugo ,  MARTINELLI, Michael ,  MERSCHAERT, Alain ,  RUHTER, Gerd ,  RYPENS, Carine ,  SCARBOROUGH, Robert ,  SCHOTTEN, Theo ,  VAN HOECK, Jean-Pierre

IPC: C07D311/70

Abstract: Disclosed are processes for producing benzopyran compounds, reduced 2-(chroman-2-yl) acetic acid compounds and 2-(6-aminochroman-2-yl)acetic acid esters which are intermediates for producing platelet aggregation inhibitors and/or are themselves potent platelet aggregation inhibitors.

公开(公告)号：WO0194331A2

公开(公告)日：2001-12-13

申请号：PCT/US0118014

申请日：2001-06-01

Applicant: LILLY CO ELI ,  COR THERAPEUTICS INC ,  ANTOINE LUC ,  BOUQUEL PASCAL ,  BORGHESE ALFIA ,  GORISSEN HUGO ,  MARTINELLI MICHAEL ,  MERSCHAERT ALAIN ,  RUHTER GERD ,  RYPENS CARINE ,  SCARBOROUGH ROBERT ,  SCHOTTEN THEO ,  HOECK JEAN PIERRE VAN

Inventor： ANTOINE LUC ,  BOUQUEL PASCAL ,  BORGHESE ALFIA ,  GORISSEN HUGO ,  MARTINELLI MICHAEL ,  MERSCHAERT ALAIN ,  RUHTER GERD ,  RYPENS CARINE ,  SCARBOROUGH ROBERT ,  SCHOTTEN THEO ,  VAN HOECK JEAN-PIERRE

IPC: C07D311/58 ,  C07D311/00

CPC classification number: C07D311/58

Abstract: Disclosed are processes for producing benzopyran compounds, reduced 2-(chroman-2-yl) acetic acid compounds and 2-(6-aminochroman-2-yl)acetic acid esters which are intermediates for producing platelet aggregation inhibitors and/or are themselves potent platelet aggregation inhibitors.

Abstract translation: 公开了制备苯并吡喃化合物，还原的2-（色满-2-基）乙酸化合物和2-（6-氨基苯并二氢吡喃-2-基）乙酸酯的方法，其为制备血小板聚集抑制剂的中间体和/或本身是有效的 血小板聚集抑制剂。

公开(公告)号：WO2013189920A1

公开(公告)日：2013-12-27

申请号：PCT/EP2013/062605

申请日：2013-06-18

Applicant: UCB PHARMA S.A. ,  ATES, Célal ,  MERSCHAERT, Alain ,  SIEW, Eugene

Inventor： ATES, Célal ,  MERSCHAERT, Alain ,  SIEW, Eugene

IPC: C07D453/04 ,  C07C205/04

CPC classification number: C07D453/04 ,  B01D61/02 ,  B01D61/022 ,  B01D61/58 ,  B01D65/08 ,  B01D2311/04 ,  B01D2311/06 ,  B01D2311/08 ,  B01D2311/25 ,  C07C201/12 ,  C07C201/16 ,  C07D307/54 ,  C07C205/53 ,  C07C205/56

Abstract: The present invention relates to compound of formula (1) and its use as a catalyst in the asymmetric Michael addition reactions.

Abstract translation: 本发明涉及式（1）化合物及其在不对称迈克尔加成反应中作为催化剂的用途。

公开(公告)号：WO2013004814A1

公开(公告)日：2013-01-10

申请号：PCT/EP2012/063238

申请日：2012-07-06

Applicant: UNIVERSITE CATHOLIQUE DE LOUVAIN ,  GAIGNEAUX, Eric ,  JACQUEMIN, Marc ,  HAUWAERT, Damien ,  CELLIER, Caroline ,  MERSCHAERT, Alain ,  MATEOS BLANCO, Raquel

Inventor： GAIGNEAUX, Eric ,  JACQUEMIN, Marc ,  HAUWAERT, Damien ,  CELLIER, Caroline ,  MERSCHAERT, Alain ,  MATEOS BLANCO, Raquel

IPC: C07C2/68 ,  C07B37/04 ,  C07C15/14

CPC classification number: C07C1/321 ,  C07B37/04 ,  C07C2521/06 ,  C07C2523/44 ,  C07C15/14

Abstract: The present invention is directed to a method of carrying out Suzuki- Miyaura CC-coupling reactions, comprising reacting an aryl halide with an aryl boronic acid in an organic solvent in the presence of an oxide supported palladium catalyst and a base, characterized in that the base is added in the form of an aqueous solution with a constant flow rate within a predetermined period of time at the beginning of the reaction.

Abstract translation: 本发明涉及一种进行Suzuki- Miyaura CC-偶联反应的方法，包括在氧化物负载型钯催化剂和碱的存在下，使芳基卤与芳基硼酸在有机溶剂中反应，其特征在于， 碱在反应开始时在预定时间内以恒定流速的水溶液的形式加入。

公开(公告)号：WO2012065891A1

公开(公告)日：2012-05-24

申请号：PCT/EP2011/069721

申请日：2011-11-09

Applicant: UCB PHARMA GMBH ,  MERSCHAERT, Alain ,  SZCZEPANIAK, Christophe Joseph ,  HAMANN, Joerg ,  KANZLER, Ralf

Inventor： MERSCHAERT, Alain ,  SZCZEPANIAK, Christophe Joseph ,  HAMANN, Joerg ,  KANZLER, Ralf

IPC: C07C237/22 ,  C07C229/22 ,  C07C233/47

CPC classification number: C07C231/02 ,  C07B2200/07 ,  C07C227/18 ,  C07C227/34 ,  C07C231/14 ,  C07C237/22 ,  C12P13/04 ,  C12P13/06 ,  C12P41/007 ,  C07C229/22 ,  C07C233/47

Abstract: The present invention provides a process for the preparation of lacosamide in substantially optically pure form, which in one aspect comprises the following steps: (i) resolution of O -methyl-D,L-serine to provide O -methyl-D-serine in substantially optically pure form; (ii) acetylation of O -methyl-D-serine thereby obtained to provide the N -acetyl 10 derivative thereof in substantially optically pure form; (iii) activating the carboxy group of the compound thereby obtained; and (iv) reacting the compound thereby obtained with benzylamine.

Abstract translation: 本发明提供了基本上光学纯的形式制备漆酶的方法，其一方面包括以下步骤：（i）拆分O-甲基-D，L-丝氨酸以提供O-甲基-D-丝氨酸 基本上光学纯的形式; （ii）由此得到的O-甲基-D-丝氨酸的乙酰化，以提供其基本上光学纯的形式的N-乙酰基10衍生物; （iii）活化所得化合物的羧基; 和（iv）使由此获得的化合物与苄胺反应。