Patents Represented by Attorney Paul E. Dupont

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  • Process for the preparation of spiro[cis-4-(&bgr;-hydroxyethyloxy)cyclohexane-[3h]indol]-2?[1?H]one derivatives
    Patent number: 6541643
    Abstract: The invention relates to a process for the preparation of spiro[cis-4-(&bgr;-hydroxyethyloxy)cyclohexane-[3H]indol]-2′[1′H]-one derivatives of the formula (I) wherein R1 and R2 are as defined herein, by reduction of a dispiro[(1,3-dioxolane)-2,4′-cyclohexane-1′3′-[3H]indol]-2″[1″H]-one derivative of general formula (II), wherein R1 and R2 are as defined herein, which comprises carrying out the reduction (a) with sodium cyanoborohydride in the presence of a Lewis acid, or (b) with sodium borohydride in the presence of a strong acid.
    Type: Grant
    Filed: April 17, 2002
    Date of Patent: April 1, 2003
    Assignee: Sanofi-Synthelabo
    Inventors: Gergely Héja, Éva Csikós, Csaba Gönczi, Judit Halász, Félix Hajdú, István Hermecz, László Kis, Lajos Nagy, Andrea Sántáné Csutor, Kálmán Simon, Tiborné Szomor, Györgyné Szvoboda
  • Pyridopyranoazepine derivatives, their preparation and their therapeutic application
    Patent number: 6538003
    Abstract: The invention relates to pyridopyranoazepine derivatives, to pharmaceutical compositions containing them, to processes for preparing them, and to the method of use thereof in the treatment or prevention of disorders associated with a dysfunction of the nicotine receptors.
    Type: Grant
    Filed: August 17, 2001
    Date of Patent: March 25, 2003
    Assignee: Sanofi-Synthelabo
    Inventors: Frédéric Galli, Samir Jegham, Alistair Lochead, Axelle Samson
  • Synthetic polysaccharides, preparation method therefor and pharmaceutical compositions containing same
    Patent number: 6534481
    Abstract: A synthetic polysaccharide including an antithrombin III binding domain consisting of a concatenation of five monosaccharides supporting a total of two carboxylic acid functions and at least four sulpho groups, said domain being directly bound at the non-reducing end by a thrombin binding domain including a concatenation of 10-25 monosaccharide units selected from hexoses, pentoses or deoxy sugars of which all the hydroxyl groups are etherified by a C1-6 alkyl group or esterified in the form of sulpho groups, as well as salts and particularly pharmaceutically acceptable salts thereof, are disclosed.
    Type: Grant
    Filed: September 7, 1999
    Date of Patent: March 18, 2003
    Assignees: Sanofi-Synthelabo, Akzo Nobel
    Inventors: Pierre Alexandre Driguez, Philippe Duchaussoy, Jean Marc Herbert, Maurice Petitou, Constant Van Boeckel, Peter Grootenhuis, Johannes Basten, Cornelia Dreef-Tromp
  • Synthetic polysaccharides, their method of production and pharmaceutical compositions containing same
    Patent number: 6528497
    Abstract: Novel synthetic polysaccharides for use in the treatment of pathologies associated with a coagulation dysfunction.
    Type: Grant
    Filed: September 5, 2000
    Date of Patent: March 4, 2003
    Assignees: Sanofi-Synthelabo, Akzo Nobel N.V.
    Inventors: Johannes Basten, Cornelia Dreef-Tromp, Pierre Alexandre Driguez, Philippe Duchaussoy, Jean Marc Herbert, Maurice Petitou, Constant Van Boeckel
  • Stable formulation containing fumagillin
    Patent number: 6528539
    Abstract: The invention relates to a stable fumagillin formulation and to the method of use thereof in treating and/or combating intestinal infections.
    Type: Grant
    Filed: October 15, 2001
    Date of Patent: March 4, 2003
    Assignee: Sanofi-Synthelabo
    Inventors: Bernard Abramovici, Jean-Luc Dubois
  • Process for the preparation of fumagillin
    Patent number: 6521764
    Abstract: The invention relates to a process for the preparation of Fumagillin by liberation from its salt characterized by reacting Fumagillin dicyclohexylamine salt with an organic acid in alcoholic medium.
    Type: Grant
    Filed: March 5, 2002
    Date of Patent: February 18, 2003
    Assignee: Sanofi-Synthelabo
    Inventors: Gyula Farkas, Andrea Györbiró, István Hermecz, Kálmán Simon, Anna Szabó, Árpádné Vasvári
  • Controlled-release dosage forms comprising zolpidem or a salt thereof
    Patent number: 6514531
    Abstract: The present invention relates to controlled-release dosage forms of zolpidem or salts thereof adapted to release zolpidem over a predetermined time period, according to a biphasic profile of dissolution, where the first phase is an immediate release phase and the second phase is a prolonged release phase and particular embodiments thereof intended to avoid abuse.
    Type: Grant
    Filed: July 16, 2001
    Date of Patent: February 4, 2003
    Assignee: Sanofi-Synthelabo
    Inventors: Gérard Alaux, Gareth Lewis, Frédéric Andre
  • Phenyl- and pyridyl-tetrahydro-pyridines having TNF inhibiting activity
    Patent number: 6509351
    Abstract: The present invention relates to compounds of formula (I): as well as the salts or solvates thereof, to pharmaceutical compositions containing them, to a process for preparing them and to synthetic intermediates in this process.
    Type: Grant
    Filed: April 19, 2002
    Date of Patent: January 21, 2003
    Assignee: Sanofi-Syntelabo
    Inventors: Marco Baroni, Bernard Bourrie, Rosanna Cardamone, Pierre Casellas, Umberto Guzzi
  • Morpholine derivatives, method for the production thereof and pharmaceutical preparations containing said derivatives
    Patent number: 6506750
    Abstract: N-(phenylacetyl)morpholine derivatives useful as NK1 receptor antagonists, a process for the preparation thereof, and pharmaceutical compositions containing them as active principle.
    Type: Grant
    Filed: September 24, 2001
    Date of Patent: January 14, 2003
    Assignee: Sanofi-Synthelabo
    Inventors: Jean-Philippe Ducoux, Xavier Emonds-Alt, Patrick Gueule, Vincenzo Proietto
  • Polymorphic form of clopidogrel hydrogen sulphate
    Patent number: 6504030
    Abstract: Novel orthorombic polymorph of clopidogrel hydrogen sulfate or hydrogen sulfate of methyl (+)-(S)-&agr;-(2-chlorophenyl)-4,5,6,7-tetrahydrothieno[3,2-c]pyridine-5-acetate and a process for its preparation
    Type: Grant
    Filed: June 21, 2002
    Date of Patent: January 7, 2003
    Assignee: Sanofi-Synthelabo
    Inventors: André Bousquet, Bertrand Castro, Jean Saint-Germain
  • Method for the crystallization of a tetrahydropyridin derivative and resulting crystalline forms
    Patent number: 6489334
    Abstract: The invention relates to a method of crystallizing a tetrahydropyridine derivative, to the novel crystalline forms thereby obtained and to the pharmaceutical compositions containing said tetrahydropyridine derivative in a given crystalline form as the active principle.
    Type: Grant
    Filed: September 6, 2001
    Date of Patent: December 3, 2002
    Assignee: Sanofi-Synthelabo
    Inventors: Antoine Caron, Bruno Franc, Olivier Monnier
  • Benzene derivatives, preparation method and pharmaceutical compositions containing same
    Patent number: 6482986
    Abstract: The invention concerns compounds of formula (I) wherein A, X, Y, n, R1, R2 and R3 are as defined in claim 1. Said compounds are specifically binding to sigma receptors particularly those of the peripheral nervous system.
    Type: Grant
    Filed: February 27, 2002
    Date of Patent: November 19, 2002
    Assignee: Sanofi-Synthelabo
    Inventors: Robert Boigegrain, Bernard Bourrie, Martine Bourrie, Pierre Casellas, Jean Marc Herbert, Pierre Lair, Dino Nisato, Raymond Paul, Jean Claude Vernieres
  • Alkyl esters of 3-(3,4-dihalogenophenyl)-2,6-dioxopiperidine-3-propionic acid of use as intermediates
    Patent number: 6469173
    Abstract: The invention relates to lower-alkyl esters of 3-(3,4-dihalophenyl)-2,6-dioxopiperidine-3-propionic acid derivatives, and to processes for preparing the same.
    Type: Grant
    Filed: June 12, 2001
    Date of Patent: October 22, 2002
    Assignee: Sanofi-Synthelabo
    Inventors: Bertrand Castro, Jean-Robert Dormoy, Alain Rabion
  • Ureidopiperidine derivatives as selective human NK3 receptor antagonists
    Patent number: 6465489
    Abstract: The invention concerns compounds of formula (I) in racemic or optically pure form, methods for obtaining them and pharmaceutical compositions containing same. Said compounds are selective NK3 receptor antagonists.
    Type: Grant
    Filed: April 5, 2001
    Date of Patent: October 15, 2002
    Assignee: Sanofi-Synthelabo
    Inventors: Alain Aulombard, Xavier Emonds-Alt, Vincenzo Proietto, Didier Van Broeck
  • 3-phenyl-2,6-dioxopiperidin-3-ylpropionamide derivatives and method for preparing same
    Patent number: 6452012
    Abstract: This invention relates to 3-(3-phenyl-2,6-dioxopiperidin-3-yl) propionamide derivatives, and to processes for preparing the same.
    Type: Grant
    Filed: November 13, 2001
    Date of Patent: September 17, 2002
    Assignee: Sanofi-Synthelabo
    Inventors: Bertrand Castro, Hélène Mattras, Aldo Previero
  • 4-oxo-3,5-dihydro-4H-pyridazino[4,5-b]indole-1-carboxamide derivatives, preparation and therapeutic use
    Patent number: 6451795
    Abstract: 4-Oxo-3,5-dihydro-4H-pyridazino[4,5-b]indole-1-carboxamide derivatives having affinity for the peripheral benzodiazepine receptors are useful for the prevention or treatment of peripheral neuropathies and for the treatment of central neurogenerative diseases.
    Type: Grant
    Filed: July 25, 2001
    Date of Patent: September 17, 2002
    Assignee: Sanofi-Synthelabo
    Inventors: Frank Marguet, Jacques Froissant, Régine Bartsch-Li, Benoît Marabout, Mireille Sevrin
  • N-(arylsulphonyl) amino acid derivatives, process for their preparation and pharmaceutical compositions containing them
    Patent number: 6433185
    Abstract: The invention relates to compounds of formula in which R1 to R9, R16 and R17 are as defined in claim 1. These compounds are pharmacologically active.
    Type: Grant
    Filed: September 6, 2001
    Date of Patent: August 13, 2002
    Assignee: Sanofi-Synthelabo
    Inventors: Bernard Ferrari, Jean Gougat, Claude Muneaux, Yvette Muneaux, Pierre Perreaut, Claudine Planchenault
  • Pyrazolecarboxylic acid derivatives, their preparation, pharmaceutical compositions containing them
    Patent number: 6432984
    Abstract: N-Piperidino-5-(4-bromophenyl)-1-(2,4-dichlorophenyl)-4-ethylpyrazole-3-carboxamide and its salts and solvates are powerful antagonists of the CB1 cannabinoid receptors. They are prepared by reacting a functional derivative of 5-(4-bromophenyl)-1-(2,4-dichlorophenyl)-4-ethylpyrazole-3-carboxylic acid with 1-aminopiperidine, optionally followed by salification.
    Type: Grant
    Filed: July 27, 2001
    Date of Patent: August 13, 2002
    Assignee: Sanofi-Synthelabo
    Inventors: Francis Barth, Philippe Camus, Serge Martinez, Murielle Rinaldi
  • Polymorphic clopidogrel hydrogenesulphate form
    Patent number: 6429210
    Abstract: Novel orthorombic polymorph of clopidogrel hydrogen sulfate or hydrogen sulfate of methyl (+)-(S)-&agr;-(2-chlorophenyl)-4,5,6,7-tetrahydrothieno[3,2-c]pyridine-5-acetate and a process for its preparation.
    Type: Grant
    Filed: April 5, 2001
    Date of Patent: August 6, 2002
    Assignee: Sanofi-Synthelabo
    Inventors: André Bousquet, Bertrand Castro, Jean Saint-Germain
  • Osanetant in the treatment of depression and depressive disorders
    Patent number: 6420388
    Abstract: The invention relates to a method for the treatment of mood disorders utilizing osanetant or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: October 5, 2001
    Date of Patent: July 16, 2002
    Assignee: Sanofi-Synthelabo
    Inventors: Xavier Emonds-Alt, Philippe Soubrie, Régis Steinberg