Patents Assigned to Synthelabo
  • Patent number: 6242607
    Abstract: The invention relates to glutarimides of formula (I): in which Ar represents a phenyl non substituted or substituted one or more times with one of the substituents selected from a halogen atom, a hydroxyl, a (C1-C4)alkoxy, a trifluoromethyl, a (C1-C4)alkyl, said substituents being identical or different; a pyridyl group; a thienyl group and X is methylene or ethylene, their salts and their enantiomers, as well as their method of preparation and their use for the preparation of the corresponding 3,3-disubstituted piperidines.
    Type: Grant
    Filed: November 10, 1999
    Date of Patent: June 5, 2001
    Assignee: Sanofi-Synthelabo
    Inventors: Philippe Camus, Marcel Descamps, Joël Radisson
  • Patent number: 6242637
    Abstract: The invention relates to compounds of the formula in which: A is a divalent radical selected from: A1) —O—CO— A2) —CH2—O—CO— A3) —O—CH2—CO— A4) —O—CH2—CH2— A5) —N(R1)—CO— A6) —N(R1)—CO—CO— A7) —N(R1)—CH2—CH2— A8) —O—CH2— in which: R1 is a hydrogen or a (C1-C4)-alkyl; and Am is a nitrogen-containing heterocycle.
    Type: Grant
    Filed: October 20, 1998
    Date of Patent: June 5, 2001
    Assignee: Sanofi-Synthelabo
    Inventors: Xavier Emonds-Alt, Isabelle Grossriether, Patrick Gueule, Vincenzo Proietto, Didier Van Broeck
  • Patent number: 6239286
    Abstract: Process for the preparation of compounds of formula (I) wherein R means hydrogen atom, or C1-6 alkyl group, or C7-12 aralkyl group or phenyl group, characterised in that: a) the compound of formula (III) is reacted with a compound of formula (IV) wherein X means halogen atom or C1-5 alkoxy group or hydroxyl group and the resulting compound of formula (II) is transformed in the presence of an oxidising agent in a reaction medium with pH above 7, into the compound of formula (I), or b) the compound of formula (III) is reacted with an anhydride of general formula (V) and the resulting compound of formula (II) transformed in the presence of an oxidising agent, in a reaction medium with pH above 7, into the compound of formula (I), or c) a compound of formula (II) is transformed in the presence of an oxidising agent, in a reaction medium with pH above 7, into the compound of formula (I), and if desired, the resulting compounds of formula (I), before or after isolation, are transformed into acid addition salts, or
    Type: Grant
    Filed: May 15, 2000
    Date of Patent: May 29, 2001
    Assignee: Sanofi-Synthelabo
    Inventors: Attila Kis-Tamás, Csaba Huszár, Bertrand Castro, Attila Németh, Péter Aranyosi, Károly Gyüre, István Mészáros, Ilona Dervalicsné Zrínyi, Katalin Dubovszki, Lajosné Páli, Antal Gajáry, Attila Supic, Zsuzsanna Nád, Zoltán Makovi, Endre Kollár, Zsuzsanna Csetriné Hári, Ágnes Kunsztné Kárász, Erzsébet Bognár
  • Patent number: 6235793
    Abstract: The invention relates to the use of &bgr;3-adrenergic receptor agonists for the preparation of healing drugs and to the pharmaceutical compositions for said use.
    Type: Grant
    Filed: July 15, 1999
    Date of Patent: May 22, 2001
    Assignee: Sanofi-Synthelabo
    Inventors: André Bernat, Jean-Marc Herbert, Michèle Arnone
  • Patent number: 6235791
    Abstract: The present invention relates to the use of compounds capable of displacing tritiated cis-N-cyclohexyl-N-ethyl [3-(3-chloro-4-cyclohexylphenyl)-allyl]amine from its receptors for the preparation of pharmaceutical compositions intended to combat cell proliferation.
    Type: Grant
    Filed: April 12, 1999
    Date of Patent: May 22, 2001
    Assignee: Sanofi-Synthelabo
    Inventors: Jean Claude Breliere, Pascual Ferrara, Christine Lebouteiller, Raymond Paul, Jorge Rosenfeld, Didier Van Broeck
  • Patent number: 6221879
    Abstract: Compounds of general formula (I) in which U represents a group of general formula (A) or (B) in which formulae V represents a hydrogen or halogen atom, a (C1-C3)alkyl group or one or two (C1-C3)alkoxy groups, W and X each represent, respectively, either two oxygen atoms, or an oxygen atom and a CH2 group, or a CH2 group and an oxygen atom, or an oxygen atom and a CO group, n represents the number 0 or 1, R represents either a propyl group when U represents a group of general formula (A), or a hydrogen atom or a (C1-C3)alkyl group when U represents a group of general formula (B), Y represents one or more atoms or groups chosen from the following: hydrogen, halogen, (C1-C3)alkyl and (C1-C3)alkoxy, Z represents two hydrogen atoms or an oxygen atom.
    Type: Grant
    Filed: July 14, 2000
    Date of Patent: April 24, 2001
    Assignee: Sanofi-Synthelabo
    Inventors: Benoit Marabout, Mireille Sevrin, Pascal George, Jean-Pierre Merly, Daniele De Peretti, Jocelyne Roy, David Machnik
  • Patent number: 6218403
    Abstract: The present invention relates to a pharmaceutical composition containing: (a) a thienopyridine derivative of formula  in which R is hydrogen or a (C1-C4)alkoxycarbonyl group, or one of its pharmaceutically acceptable salts; and (b) an HMG-CoA reductase inhibitor.
    Type: Grant
    Filed: January 22, 1999
    Date of Patent: April 17, 2001
    Assignee: Sanofi-Synthelabo
    Inventors: Georges Daste, Jean Marc Herbert
  • Patent number: 6214999
    Abstract: The present invention relates to a process for the preparation of 4′-bromomethyl-biphenyl derivatives of the formula: by reacting a 4′-methyl-biphenyl derivative of the formula: with a brominating agent a in a hydrobromic acid/alkali metal bromate system in a two-phase medium, and under photo-iradiation, where R is as defined in the specification.
    Type: Grant
    Filed: July 14, 2000
    Date of Patent: April 10, 2001
    Assignee: Sanofi-Synthelabo
    Inventors: Michel Biard, Bertrand Castro
  • Patent number: 6215005
    Abstract: A process for the preparation of [2-(2-thienyl)-ethylamino]-(2-halogenophenyl)-acetonitriles of general formula (I) starting from 2-(2-thienyl)-ethyl-amine, alkalicyanide and o-halogeno-benzaldehyde. Compounds of general formula (I) are valuable intermediates.
    Type: Grant
    Filed: May 3, 2000
    Date of Patent: April 10, 2001
    Assignee: Sanofi-Synthelabo
    Inventors: Alain Heymes, Bertrand Castro, Mária Bakonyi, Marianna Csatáriné Nagy, Leventéné Molnár
  • Patent number: 6214882
    Abstract: Benzenesulphonamide compounds of general formula (I), wherein R1 is a hydrogen or halogen atom such as chlorine or fluorine, or a straight or branched C1-4 alkyl or C1-4 alkoxy group, each of R2, R3 and R4, which are the same or different, is a hydrogen atom or a straight, branched or cyclic C1-4 alkyl group, and R1 is a hydrogen atom or a C1-2 alkyl, C1-2 fluoroalkyl or C1-2 perfluoroalkyl group, in the form of enantiomers, diastereoisomers or mixtures thereof, including racemic mixtures, as well as pharmaceutically acceptable acid addition salts thereof, are provided for therapeutical use.
    Type: Grant
    Filed: January 16, 1998
    Date of Patent: April 10, 2001
    Assignee: Synthelabo
    Inventors: Thomas Purcell, Christophe Philippo
  • Patent number: 6211382
    Abstract: Process for the preparation of compounds of formula (I) wherein R means hydrogen atom, or C1-6 alkyl group, or C7-12 aralkyl group or phenyl group, characterised in that a) the compound of formula (III) is reacted with a compound of formula (IV) wherein X means halogen atom or C1-5 alkoxy group or hydroxyl group, and the resulting compound of formula (II) is transformed, in a reaction medium with pH above 7, into the compound of formula (I) or b) the compound of formula (III) is reacted with an anhydride of general formula (V) and the resulting compound of formula (II) transformed, in a reaction medium with pH above 7, into the compound of formula (I), or c) a compound of formula (II) is transformed, in a reaction medium with pH above 7, into the compound of formula (I), and if desired, the resulting compounds of formula (I), before or after isolation, are transformed into acid addition salts, or the compounds of formula (I) are liberated from their acid addition salts.
    Type: Grant
    Filed: April 13, 2000
    Date of Patent: April 3, 2001
    Assignee: Sanofi-Synthelabo
    Inventors: Csaba Huszár, Attila Kis-Tamás, Attila Németh, Zsuzsanna Nád, Zoltán Makovi, Antal Gajáry, Endre Kollár, Péter Aranyosi, Károly Gyüre, István Mészáros, Zsuzsanna Csetriné Hári, Attila Supic, Ilona Dervalicsne Zrinyi, Katalin Dubovszki, Lajosné Páli, Ágnes Kunsztné Kárász, Erzsébet Bognár
  • Patent number: 6200991
    Abstract: A compound of formula (I) the process of preparing compounds of formula (I), their pharmaceutical compositions, and the method of treating diseases associated with M3 muscarinic and/or S—HT4 serotoninergic receptors.
    Type: Grant
    Filed: June 19, 2000
    Date of Patent: March 13, 2001
    Assignee: Sanofi-Synthelabo
    Inventors: Gilles Courtemanche, Gérard DeFosse, Olivier Crespin, Philippe Bovy
  • Patent number: 6197787
    Abstract: A method for preparing pharmaceutical formulations of poorly soluble drug substances in the form of concentrated solutions for filling soft gelatin capsules and solid dispersions and suspensions for filling hard gelatin capsules and compressing into tablets is provided. Pharmaceutical formulations of poorly soluble drug substances are also disclosed. The formulations include the sodium salt of the poorly soluble drug substance, a conversion aid such as PEG, polysorbate, a sugar alcohol (e.g. mannitol or xylitol), propylene glycol or transcutol, and, in some cases an excipient, such as dicalcium phosphate dihydrate, lactose monohydrate, or microcrystalline cellulose.
    Type: Grant
    Filed: October 1, 1999
    Date of Patent: March 6, 2001
    Assignee: Sanofi-Synthelabo
    Inventors: Nancy M. Franson, Micael A. Guillot, Sharon M. Laughlin, William L. Rocco
  • Patent number: 6191137
    Abstract: The present invention relates to an aqueous solution containing 1-[2-(2-naphthyl)ethyl]-4-(3- trifluoromethylphenyl)-1,2,3,6-tetrahydropyridine hydrochloride (hydrochloride of SR 57746), also comprising &bgr;-cyclodextrin (&bgr;-CD) and a pharmaceutically acceptable acid or buffer to give a pH of less than or equal to 3.
    Type: Grant
    Filed: June 16, 2000
    Date of Patent: February 20, 2001
    Assignee: Sanofi-Synthelabo
    Inventors: Claude Aleman, Philippe Bastard, Marielle Bonnel, Thierry Breul
  • Patent number: 6187807
    Abstract: A composition of (S)(−)-amisulpride or a pharmaceutically acceptable salt thereof exhibit antipsychotic properties and are therefore useful in the treatment of certain mental disorders. The mental disorders include positive, negative, affective or cognitive symptoms of schizophrenia, dysthymia, autism, tardive dyskinesia induced by neuroleptics, Tourette disease, manic or depressive symptoms in patients with bipolar disorders, sudden attacks of delirium, migraine or drug addition. A composition of the D-(−)-tartrate of (S)-(−)-anisulpride is useful for the treatment of certain mental disorders.
    Type: Grant
    Filed: December 29, 1999
    Date of Patent: February 13, 2001
    Assignee: Sanofi-Synthelabo
    Inventors: Ghislaine Perrault, Hans Schoemaker, Joël Miget
  • Patent number: 6186980
    Abstract: The invention relates to a single-use device for injection, which comprises a conventional syringe (1) and a device for protection of the injection needle (2) of this syringe (1) after use, comprising a protective sheath (7) which consists of two, rear (9) and front (8) bodies, which are designed to be rendered integral, one in the extension of the other, and a ring (24) which is accommodated in the rear body (9) and is provided with means (29, 31) for locking the syringe (1), the said ring being designed to be displaced between a first position, for injection, and a second position, for protection after use of the injection needle (2), by means of a spring (42) which is kept compressed in the position for injection, and is released when injection is completed.
    Type: Grant
    Filed: February 8, 2000
    Date of Patent: February 13, 2001
    Assignee: Sanofi-Synthelabo
    Inventor: Marc Brunel
  • Patent number: 6184229
    Abstract: Compound corresponding to the general formula (I) in which R1 represents a hydrogen atom, a (C1-C4)alkyl group or a phenyl(C1-C4)alkyl group, R2 represents a hydrogen atom or a (C1-C4) alkyl group, and R3, R4 and R5 each represent a hydrogen or halogen atom or a trifluoromethyl, cyano, hydroxyl, (C1-C6)alkyl or (C1-C6) alkoxy group.
    Type: Grant
    Filed: January 7, 2000
    Date of Patent: February 6, 2001
    Assignee: Sanofi-Synthelabo
    Inventors: Alistair Lochead, Samir Jegham, Frédéric Galli
  • Patent number: 6180793
    Abstract: The present invention relates to a process for the preparation of the racemic or optically active compounds of general formula (VI): wherein the meaning of X is a halogen atom, or their salts, characterized in that, a racemic or optically active new compound of general formula (VII): wherein the meaning of X is a halogen atom, is transformed into the racemic or optically active compound of general formula (VIII):
    Type: Grant
    Filed: November 12, 1999
    Date of Patent: January 30, 2001
    Assignee: Sanofi-Synthelabo
    Inventors: M{acute over (a)}ria Bakonyi, Marianna Csat{acute over (a)}ri n{acute over (e)}e Nagy, Erzs{acute over (e)}bet Moln{acute over (a)}r n{acute over (e)}e Bak{acute over (o)}, Antal Gaj{acute over (a)}ry, Edit Alatty{acute over (a)}ni
  • Patent number: 6170113
    Abstract: The invention concerns a toothbrush (10) with bristles (12) at the top and a handle (14) including a structure for maintaining the brush in a vertical storage position, characterized in that the brush handle (14) is longitudinally divided in its upper part into at least two branches (16,18,20) articulated between an open position for storage wherein the free ends (22,24,26) of the branches (16,18,20), mutually spaced, form support points for the brush (10) on a horizontal surface, and a closed position wherein the branches are brought together for the toothbrush (10) to be used.
    Type: Grant
    Filed: June 22, 1999
    Date of Patent: January 9, 2001
    Assignee: Sanofi-Synthelabo
    Inventors: Jean-Michel Cornu, Veronique Malcourant
  • Patent number: 6169094
    Abstract: A composition is provided comprising an antipsychotic effective amount of (S)(−)-amisulpride, (S)-(−)-4-amino-N-[(1-ethylpyrrolidin-2-yl)methyl]-5-ethylsulfonyl)-2-methoxybenzamide. A preferred composition comprises the (D)-tartrate salt of (S)(−)-amisulpride. The (S)(−) enantiomer exhibits antipsychotic properties and administration of the specific enantiomer reduces adverse side effects by reducing toxicity.
    Type: Grant
    Filed: July 14, 1998
    Date of Patent: January 2, 2001
    Assignee: Sanofi-Synthelabo
    Inventors: Ghislaine Perrault, Hans Schoemaker, Jo{umlaut over (e)}l Miget