Patents Assigned to Synthelabo
  • Patent number: 6649627
    Abstract: The invention concerns compounds of formula (Ia) wherein R1a represents hydrogen, an —S(O)z —(C1-C4)Alk group, a —CO(C1-C4)Alk group, an —NHSO2—(C1-C4)Alk group, an NCHl (C1-C4) Alk group, a 2-furyl group or a halogen; R2 represents hydrogen or a (C1-C4)Alk group, a (C1-C4) alkoxyl group, a halogen, —COOH, —COO(C1-C4)Alk, —CN, —CONR3R4, —NO2, —SO2NH2, —NHSO2(C1-C4)Alk; m and n are independently 0, 1 or 2; R3 and R4 independently represent hydrogen or a (C1-C4)Alk group; Z is 1 or 2 and their salts or solvates, the pharmaceutical compositions that contain them, the process for their preparation, and intermediate synthesis products.
    Type: Grant
    Filed: March 26, 2001
    Date of Patent: November 18, 2003
    Assignee: Sanofi-Synthelabo
    Inventors: Roberto Cecchi, Tiziano Croci, Umberto Guzzi, Eric Marsault
  • Patent number: 6642258
    Abstract: The invention relates to the use of a central cannabinoid receptor antagonist for the preparation of medicinal products that are useful in treating and preventing neuroinflammatory pathologies.
    Type: Grant
    Filed: March 21, 2002
    Date of Patent: November 4, 2003
    Assignee: Sanofi-Synthelabo
    Inventors: Bernard Bourrie, Pierre Casellas
  • Patent number: 6642233
    Abstract: The invention relates to the compounds of formula: as well as to the salts thereof with inorganic or organic acids, to solvates thereof and/or to hydrates thereof, which have strong affinity and high selectivity for the human NK1 receptors of substance P. The invention also relates to the process for preparing them, to the intermediate compounds of formula (VII) which are useful for the preparation, to pharmaceutical compositions containing them and to their fuse for the manufacture of medicinal products intended for treating any pathology in which substance P and the human NK1 receptors are involved.
    Type: Grant
    Filed: August 9, 2001
    Date of Patent: November 4, 2003
    Assignee: Sanofi-Synthelabo
    Inventors: Jean-Philippe Ducoux, Xavier Emonds-Alt, Patrick Gueule, Vincenzo Proietto
  • Patent number: 6639083
    Abstract: The invention relates to a process for preparing 2-thienyl-2-ethanol, in which: a) thiophene is metallated using an alkali metal, in the presence of an electron transfer agent, b) the compound obtained is treated with ethylene oxide, c) the thienyl derivative thus formed is hydrolyzed, to give the desired compound. 2-Thienyl-2-ethanol is a synthetic intermediate.
    Type: Grant
    Filed: April 19, 2002
    Date of Patent: October 28, 2003
    Assignee: Sanofi-Synthelabo
    Inventors: Michel Biard, André Bousquet
  • Patent number: 6635645
    Abstract: The invention relates to 2,5-diazabicyclo[2.2.1]heptane derivatives, to pharmaceutical compositions containing them, and to methods for the treatment or prevention of disorders associated with a dysfunction of the nicotinic receptors utilizing them.
    Type: Grant
    Filed: August 16, 2001
    Date of Patent: October 21, 2003
    Assignee: Sanofi-Synthelabo
    Inventors: Alistair Lochead, Samir Jegham, Alain Nedelec, Jean Jeunesse, Frédéric Galli, Luc Even
  • Patent number: 6627649
    Abstract: The invention relates to pharmaceutical compositions containing (2S)-1-{(2R,3S)-5-chloro-3-(2-chlorophenyl)-1-(3,4-dimethoxybenzenesulfonyl)-3-hydroxy-2,3-dihydro-1H-indole-2-carbonyl}pyrrolidine-2-carboxamide, a selective V1a arginine vasopressin receptor antagonist, in combination with the equatorial isomer of 1-{4-(N-tert-butylcarbamoyl)-2-methoxybenzenesulfonyl}-5-ethoxy-3-spiro{4-(2-morpholinoethyloxy)cyclohexane}indol-2-one or one of its salts, a selective V2 arginine vasopressin receptor antagonist. The invention relates to the use of such compositions for the production of medicines designed to treat all diseases for which either arginine vasopressin or the V2 receptors are implicated or to treat all diseases related to a water overlead.
    Type: Grant
    Filed: October 6, 2000
    Date of Patent: September 30, 2003
    Assignee: Sanofi-Synthelabo
    Inventors: Colette Lacour, Dino Nisato
  • Patent number: 6624164
    Abstract: The invention relates to compounds of formula: and their solvates and/or hydrates exhibiting affinity for the arginine-vasopressin V1b receptors or for both V1b and V1a receptors. The invention also relates to their process of preparation, to the intermediate compounds of formula (II) of use for their preparation, to the pharmaceutical compositions comprising them and to their use for the preparation of medicaments.
    Type: Grant
    Filed: November 25, 2002
    Date of Patent: September 23, 2003
    Assignee: Sanofi-Synthelabo
    Inventors: Bruno Schoentjes, Claudine Serradeil-Le Gal, Jean Wagnon
  • Patent number: 6617336
    Abstract: Compounds of general formula (I) in which: A represents a hydrogen atom, a hydroxyl, a C1-3 alkoxy group, a hydroxy(C1-6 alkyl) group, a (C1-3 alkoxy)(C1-3 alkyl) group, a thiol, (C1-6 alkyl)sulfanyl or a halogen; B and D represent, independently of one another, a hydrogen atom, a C1-6 alkyl group, a fluoro(C1-6 alkyl) group or a perfluoro(C1-2 alkyl) group or B and D together from an oxo; R1 represents a phenyl, a naphthyl or a heteroaryl comprising 4 or 5 carbon atoms; R2 and R3 represent, independently of one another, a hydrogen atom, a halogen or a C1-6 alkyl group, R4 represents a hydrogen atom, a hydroxyl or a halogen, and R5 and R6 represent, independently of one another, a hydrogen atom, a C1-6 alkyl group, a C2-6 alkenyl group, a C3-6 cycloalkyl group, a C3-6 cycloalkenyl group, a fluoro(C1-6 alkyl) group or a perfluoro(C1-2 alkyl) group or R5 and R6 together form a C2-6 alkylene chain or a C3-6 alkenylene chain, to give, with the nitrogen to which they are attached, a heteroc
    Type: Grant
    Filed: May 22, 2002
    Date of Patent: September 9, 2003
    Assignee: Sanofi-Synthelabo
    Inventors: Philippe R Bovy, Alain Braun, Christophe Philippo
  • Patent number: 6610882
    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: June 7, 2002
    Date of Patent: August 26, 2003
    Assignee: Sanofi-Synthelabo
    Inventors: Bernard Ferrari, Jean Gougat, Claude Muneaux, Yvette Muneaux, Pierre Perreaut, Claudine Planchenault
  • Publication number: 20030157177
    Abstract: The subject of the invention is pharmaceutical microspheres containing, as active principle, a mixture of valproic acid and of one of its pharmaceutically acceptable salts in combination with a matrix vehicle selected from glycerol esters, hydrogenated oils, esterified polyethylene glycols, waxes and their mixtures.
    Type: Application
    Filed: October 15, 2002
    Publication date: August 21, 2003
    Applicant: Sanofi-Synthelabo, a corporation of France.
    Inventors: Christian Langlois, Jean-Yves Lanne
  • Patent number: 6600039
    Abstract: The invention relates to a process for the preparation of a compound of formula (I) and the salts thereof by reacting the compound of formula (II) with the compound of formula (III), which comprises carrying out the reaction in dimethyl sulfoxide, at a temperature between 10° C. and 40° C., preferably at room temperature and transforming the resulting base of formula (I), if desired, into its salt by a method known per se.
    Type: Grant
    Filed: April 17, 2002
    Date of Patent: July 29, 2003
    Assignee: Sanofi-Synthelabo
    Inventors: Gergely Héja, Éva Csikós, Tünde Erösné Takácsy, Csaba Gönczi, Judit Halász, István Hermecz, Csilla Majláth, Lajos Nagy, Andrea Sántáné Csutor, Péter Sárosi, Kálmán Simon, Tiborné Szomor, Györgyné Szvoboda
  • Patent number: 6596732
    Abstract: The invention relates to compounds of formula: and their solvates and/or hydrates exhibiting an affinity and a selectivity for arginine-vasopressin V1b receptors or for both V1b and V1a receptors.
    Type: Grant
    Filed: August 12, 2002
    Date of Patent: July 22, 2003
    Assignee: Sanofi-Synthelabo
    Inventors: Claudine Serradeil-Le Gal, Bernard Tonnerre, Jean Wagnon
  • Patent number: 6585702
    Abstract: A single-use device for injection includes a pre-filled syringe with a front nose which supports an injection needle which is protected by a protective cap, and a syringe body which accommodates the syringe. The device further includes a joining piece with claws which can be extended radially to cover and grasp the protective cap by penetrating the cap. The syringe body includes a front section, which can be separated, that is delimited by a breakable area. The front section includes a neck that clamps the tabs of the joining piece onto the protective cap.
    Type: Grant
    Filed: February 8, 2000
    Date of Patent: July 1, 2003
    Assignee: Sanofi-Synthelabo
    Inventor: Marc Brunel
  • Patent number: 6586456
    Abstract: Substituted 4-phenyl-2-aminothiazole derivatives, processes for preparing the same, and the use thereof as corticotropin releasing factor (CRF) antagonists.
    Type: Grant
    Filed: April 17, 2002
    Date of Patent: July 1, 2003
    Assignee: Sanofi-Synthelabo
    Inventors: Evelyne Fontaine, Michel Geslin, Danielle Gully, Antoine Pradines, Pierre Roger
  • Patent number: 6575939
    Abstract: The invention concerns a single-use device for injecting a dose of a medicinal product, comprising a syringe (1) and a piston rod (7) provided with a collar (9) housed in a casing formed of two parts, a front part (11) and a rear part (10), fitted inside each other and capable of sliding in relation to each other over a short traverse between two positions, a retracted position and a forward position. This device additionally includes means (35) for supporting the collar (9) of the piston rod (7) arranged so as to permit, on the one hand, injection under the effect of a propulsion spring (50) in the forward position of the parts (10, 11) of the casing and, on the other hand, backward movement of the syringe (1) inside the casing, after injection, in the retracted position of the said parts of the casing. It also includes means (28, 29) for viewing the supporting means (35) at the end of injection.
    Type: Grant
    Filed: August 3, 2000
    Date of Patent: June 10, 2003
    Assignee: Sanofi-Synthelabo
    Inventor: Marc Brunel
  • Patent number: 6573386
    Abstract: The invention relates to a process for the preparation of spiro [(4-cyclohexanone)-[3H]indol]-2′[1′H]-one derivatives of general formula I—wherein R1 and R2 independently stand for hydrogen, C1-4alkyl, C1-4alkoxy, C1-4alkylthio, C1-4polyfluoroalkyl, C1-4polyfluoroalkoxy, C3-7cycloalkyloxy, C3-7cycloalkylthio, phenoxy, benzyloxy or nitro group—, characterized by reacting an indolin-2-one derivative of general formula II—wherein R1 and R2 are as defined above—with a compound capable for introducing a protective group, coupling the compound of general formula III, thus obtained—wherein R1 and R2 are as defined above and A stands for a protective group—with acrylic acid C1-4ester; cyclizing the resulting compound of general formula IV—wherein R1 and R2 are as defined above—with a compound capable for introducing a protective group, coupling the compound of formula III thus obtained,—wherein R1 and R2 are as defined abo
    Type: Grant
    Filed: April 17, 2002
    Date of Patent: June 3, 2003
    Assignee: Sanofi-Synthelabo
    Inventors: Csaba Gönczi, Éva Csikós, István Hermecz, Gergely Héja, Árpád Illár, Lajos Nagy, Andrea Sántáné Csutor, Attila Simon, Kálmán Simon, Ágota Smelkóné Esek, Tiborné Szomor, Györgyné Szvoboda
  • Patent number: 6573281
    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
  • Patent number: 6573381
    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.
    Type: Grant
    Filed: October 6, 2000
    Date of Patent: June 3, 2003
    Assignee: Sanofi-Synthelabo
    Inventors: André Bousquet, Andrée Musolino
  • Patent number: 6548702
    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
  • Patent number: 6541488
    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