Patents by Inventor Alain Merschaert

Alain Merschaert has filed for patents to protect the following inventions. This listing includes patent applications that are pending as well as patents that have already been granted by the United States Patent and Trademark Office (USPTO).

  • Process for preparing lacosamide
    Patent number: 9630908
    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.
    Type: Grant
    Filed: August 17, 2015
    Date of Patent: April 25, 2017
    Assignee: UCB Pharma GmbH
    Inventors: Alain Merschaert, Christophe Joseph Szczepaniak, Joerg Hamann, Ralf Kanzler
  • Process for Preparing Lacosamide
    Publication number: 20160039744
    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.
    Type: Application
    Filed: October 30, 2015
    Publication date: February 11, 2016
    Applicant: UCB PHARMA GMBH
    Inventors: Alain Merschaert, Christophe Joseph Szczepaniak, Joerg Hamann, Ralf Kanzler
  • Process for preparing lacosamide
    Patent number: 9139513
    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.
    Type: Grant
    Filed: November 9, 2011
    Date of Patent: September 22, 2015
    Assignee: UCB Pharma GmbH
    Inventors: Alain Merschaert, Christophe Joseph Szczepaniak, Joerg Hamann, Ralf Kanzler
  • Process for the preparation of amino acid derivatives
    Patent number: 8969620
    Abstract: The present invention relates to a process of manufacture of compounds of formula (B) wherein R1, R2 and R3 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.
    Type: Grant
    Filed: September 29, 2011
    Date of Patent: March 3, 2015
    Assignee: UCB Pharma GmbH
    Inventors: Alain Merschaert, Didier Bouvy, David Vasselin, Nicolas Carly
  • Process for the preparation of amino acid derivatives
    Patent number: 8946476
    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).
    Type: Grant
    Filed: November 6, 2009
    Date of Patent: February 3, 2015
    Assignee: UCB Pharma GmbH
    Inventors: Didier Bouvy, Alain Merschaert, Véronique Pinilla, Joerg Hamann, Ralf Kanzler, Antoine Thomas
  • METHOD OF CARRYING OUT CC-COUPLING REACTIONS USING OXIDE SUPPORTED PD-CATALYSTS
    Publication number: 20140163283
    Abstract: A method of carrying out Suzuki-Miyaura CC-coupling reactions, includes 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.
    Type: Application
    Filed: July 6, 2012
    Publication date: June 12, 2014
    Applicant: UNIVERSITE CATHOLIQUE DE LOUVAIN
    Inventors: Eric Gaigneaux, Marc Jacquemin, Damien Hauwaert, Caroline Cellier, Alain Merschaert, Raquel Mateos Blanco
  • Process for Preparing Lacosamide
    Publication number: 20140018577
    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.
    Type: Application
    Filed: November 9, 2011
    Publication date: January 16, 2014
    Applicant: UCB PHARMA GMBH
    Inventors: Alain Merschaert, Christophe Joseph Szczepaniak, Joerg Hamann, Ralf Kanzler
  • PROCESS FOR THE PREPARATION OF AMINO ACID DERIVATIVES
    Publication number: 20130190533
    Abstract: The present invention relates to a process of manufacture of compounds of formula (B) wherein R1, R2 and R3 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.
    Type: Application
    Filed: September 29, 2011
    Publication date: July 25, 2013
    Applicant: UCB PHARMA GMBH
    Inventors: Alain Merschaert, Didier Bouvy, David Vasselin, Nicolas Carly
  • Novel Process for the Preparation of Amino Acid Derivatives
    Publication number: 20110263899
    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).
    Type: Application
    Filed: November 6, 2009
    Publication date: October 27, 2011
    Applicant: UCB PHARMA GMBH
    Inventors: Didier Bouvy, Alain Merschaert, Véronique Pinilla, Joerg Hamann, Ralf Kanzler, Antoine Thomas
  • PROCESSES FOR THE PREPARATION OF 3,4-SUBSTITUTED-1,2,5-THIADIAZOLES AND INTERMEDIATES THEREOF
    Publication number: 20090156808
    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.
    Type: Application
    Filed: December 7, 2005
    Publication date: June 18, 2009
    Inventors: Alfio Borghese, Vincenzo Mancuso, Alain Merschaert
  • Process for the asymmetric synthesis of duloxetine
    Patent number: 7538232
    Abstract: This invention provides an improved asymmetric process for the synthesis of duloxetine involving arylation of Compounds of Formula I.
    Type: Grant
    Filed: January 19, 2006
    Date of Patent: May 26, 2009
    Assignee: Eli Lilly and Company
    Inventors: Mark Anthony Butchko, Alain Merschaert, Kenneth Philip Moder
  • IMPROVED PROCESS FOR THE ASYMMETRIC SYNTHESIS OF DULOXETINE
    Publication number: 20070167636
    Abstract: This invention provides an improved asymmetric process for the synthesis of duloxetine involving arylation of Compounds of Formula I.
    Type: Application
    Filed: January 19, 2006
    Publication date: July 19, 2007
    Inventors: Mark Butchko, Alain Merschaert, Kenneth Moder
  • Methods for producing amino-substituted chromanes
    Publication number: 20040014804
    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.
    Type: Application
    Filed: July 15, 2003
    Publication date: January 22, 2004
    Inventors: Luc Antoine, Pascal Bouquel, Alfio Borghese, Hugo Gorissen, Michael Martinelli, Alain Merschaert, Gerd Ruhter, Carine Rypens, Robert Scarborough, Theo Schotten, Jean-Pierre Van Hoeck
  • Method for resolving chiral (2s) and (2r) chromanes
    Publication number: 20040014994
    Abstract: Disclosed are processes for resolving chiral (2S) and (2R) benzopyrans, racemizing benzopyrans, and recycling racemized benzopyrans to increase yield of a desired enantiomer to provide purified or substantially purified bicyclic amino substituted benzopyran derivatives. Such benzopyran derivatives are preferably chromans which can be coupled with benzoyl derivatives via an amide bond to produce potent platelet aggregation inhibitors.
    Type: Application
    Filed: July 17, 2003
    Publication date: January 22, 2004
    Inventors: Luc Antoine, Pascal Bouquel, Alfio Borghese, Hugo Gorissen, Vien V. Khau, Michael Martinelli, Alain Merschaert, Gerd Ruhter, Carine Rypens