Abstract: Methyl (R)-2-(R1OSO2)-2-(2-chlorophenyl)acetates useful as intermediates in the preparation of methyl (S)-2(2-chlorophenyl)-2-(4,5,6,7-tetrahydrothieno[3,2-c]-5-pyridyl)acetate.
Abstract: The present invention relates to the use of saredutant and of its pharmaceutically acceptable salts for the treatment or prevention of adaptation disorders, bipolar disorders, and dysthymic disorders.
Type:
Grant
Filed:
October 9, 2001
Date of Patent:
June 3, 2003
Assignee:
Sanofi-Synthelabo
Inventors:
Xavier Emonds-Alt, Philippe Soubrie, Régis Steinberg
Abstract: The invention relates to a process for the preparation of 2-methoxy-4-(N-t-butylaminocarbonyl)benzenesulfonyl chloride by sulfonating m-hydroxybenzoic acid, methylating the hydroxy group of the resulting sulfonic acid or its salt, transforming the carboxylic acid group and the sulfonic acid group to acid chloride groups and reacting the 4-chlorosulfonyl-3-methoxy-benzoyl chloride with t-butylamine, which comprises carrying out the sulfonation of the 3-methoxy-benzoic acid of general formula (II) with 96% sulfuric acid, separating the resulting 3-hydroxy-4-sulfobenzoic acid of general formula (III) in the form of its salt of general formula (IV), wherein Z stands for alkali metal or ammonium group, methylating the compound of general formula (IV) in the presence of a phase transfer catalyst at a pH value of about 11.
Type:
Grant
Filed:
April 26, 2002
Date of Patent:
April 15, 2003
Assignee:
Sanofi-Synthelabo
Inventors:
Csaba Gönczi, Éva Csikós, Félix Hajdú, István Hermecz, Gergely Héja, Gergelyné Héja, Lajos Nagy, Andrea Sántáné Csutor, Kálmán Simon, Ágota Smelkóné Esek, Tiborné Szomor, Györgyné Szvoboda
Abstract: The invention relates to the use of direct or indirect selective inhibitors of factor Xa acting via antithrombin III, alone or in combination with one or more compounds with anti-platelet aggregation activity, for the preparation of medicines intended to prevent and to treat thromboembolic arterial diseases.
The subject of the invention is also pharmaceutical compositions containing one or more direct or indirect selective inhibitors of factor Xa which act via antithrombin III in combination with one or more compounds with anti-platelet aggregation activity, and optionally one or more pharmaceutically acceptable vehicles.
Type:
Grant
Filed:
February 11, 2000
Date of Patent:
April 1, 2003
Assignees:
Sanofi-Synthelabo, Akzo Nobel
Inventors:
André Bernat, Jean Marc Herbert, Maurice Petitou, Ronald Van Amsterdam
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
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.
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
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
Abstract: The invention relates to a stable fumagillin formulation and to the method of use thereof in treating and/or combating intestinal infections.
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
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
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
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
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
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
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
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.
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
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