Patents Assigned to Synthelabo
  • Patent number: 6165507
    Abstract: A sustained-release pharmaceutical formulation containing mizolastine, a core formed of a sustained-release table containing mizolastine combined with a fatty matrix and an organic acid, the tablet being coated.
    Type: Grant
    Filed: August 26, 1998
    Date of Patent: December 26, 2000
    Assignee: Synthelabo
    Inventors: Maryvonne Chariot, Gareth Lewis, Jean Montel
  • Patent number: 6162923
    Abstract: The present invention relates to a process for the preparation of a compound of general formula (I), ##STR1## wherein R.sup.1 represents a hydrogen atom or an alkyl group of 1-6 carbon atoms, and their salts, wherein the compound of formula (II): ##STR2## is reacted with a compound of formula (III): ##STR3## wherein R represents an alkyl group of 1-4 carbon atoms and R.sup.1 is the same as defined above, by heating their neutral pH mixtures at the boiling temperature of the mixture, and the resulting compound of general formula (IV): ##STR4## wherein R and R.sup.1 are the same as defined above, is cyclized into the compound of general formula (I) by further elevating the temperature of the neutral mixture, and if desired, the compounds of general formula (I) are transformed into their salts, or the compounds of general formula (I) are liberated from their salts.
    Type: Grant
    Filed: April 26, 2000
    Date of Patent: December 19, 2000
    Assignee: Sanofi-Synthelabo
    Inventors: Csaba Huszar, Attila Kis-Tamas, Attila Nemeth, Antal Gajary, Lajosne Pali
  • Patent number: 6156301
    Abstract: Mammalian Interleukin-7 proteins (IL-7s), DNAs and expression vectors encoding mammalian IL-7s, and processes for producing mammalian IL-7s as products of cell culture, including recombinant systems, are disclosed.
    Type: Grant
    Filed: May 12, 1999
    Date of Patent: December 5, 2000
    Assignee: Sanofi-Synthelabo
    Inventors: Anthony E. Namen, Raymond G. Goodwin, Stephen D. Lupton, Diane Y. Mochizuki
  • Patent number: 6153610
    Abstract: Disclosed are: aqueous parenteral formulations for the treatment of cancer tumors comprising 1,2,4-benzotriazine 1,4-dioxides in a citrate buffer; and method of cancer tumor treatment.
    Type: Grant
    Filed: September 21, 1998
    Date of Patent: November 28, 2000
    Assignee: Sanofi-Synthelabo Inc.
    Inventors: Stephen Brown, Edward Baker
  • Patent number: 6149940
    Abstract: Pharmaceutical tablet which consists of:a) a first layer having the property of swelling considerably and quickly on contact with aqueous biological fluids, the first layer being produced by compression of a mixture or of a granulate comprising hydrophilic polymers, andb) a second layer adjacent to the first layer being formulated with hydrophilic polymers and with other auxiliary substances in order to give the preparation suitable properties of compressibility and in order to allow the release of alfuzosin hydrochloride within a predetermined time period.
    Type: Grant
    Filed: April 26, 1999
    Date of Patent: November 21, 2000
    Assignees: Synthelabo, Jagotec AB
    Inventors: Lauretta Maggi, Ubaldo Conte, Pascal Grenier, Guy Vergnault, Alain Dufour, Fran.cedilla.ois Xavier Jarreau, Clemence Rauch-Desanti
  • Patent number: 6143761
    Abstract: Compounds corresponding to the general formula (I) ##STR1## in which R.sub.1 represents a hydrogen atom, a (C.sub.1 -C.sub.6)alkyl group or a phenyl(C.sub.1 -C.sub.4)alkyl group, R.sub.2 represents a hydrogen atom or a (C.sub.1 -C.sub.6)alkyl group and R.sub.3, R.sub.4 and R.sub.5 each represent, independently of one another, a hydrogen or halogen atom or a trifluoromethyl, cyano, hydroxyl, (C.sub.1 -C.sub.6)alkyl or (C.sub.1 -C.sub.6)alkoxy group. Application in therapeutics.
    Type: Grant
    Filed: September 15, 1999
    Date of Patent: November 7, 2000
    Assignee: Sanofi-Synthelabo
    Inventors: Alistair Lochead, Samir Jegham, Frederic Galli, Thierry Gallet
  • Patent number: 6143772
    Abstract: Compounds derived from 3-(benzofuran-5-yl) oxazolidin-2-one, of general formula (I) ##STR1## in which: R.sub.1 represents a phenyl group, a phenylmethyl group, an alkyl group or a fluoroalkyl group, and R.sub.2 represents a hydrogen atom or a methyl group. Application in therapeutics.
    Type: Grant
    Filed: May 8, 1998
    Date of Patent: November 7, 2000
    Assignee: Synthelabo
    Inventors: Samir Jegham, Frederic Puech, Philippe Burnier, Danielle Berthon
  • Patent number: 6143792
    Abstract: The invention relates to the use of a specific 5HT2 receptor antagonist for the preparation of medicines useful in the treatment of the sleep apnea syndrome.
    Type: Grant
    Filed: March 27, 2000
    Date of Patent: November 7, 2000
    Assignee: Sanofi-Synthelabo
    Inventor: Fran.cedilla.oise Cattelin
  • Patent number: 6140335
    Abstract: The invention concerns the use of mizolastine and the pharmaceutically acceptable salts thereof for making a medicine for treating inflammatory diseases or inflammatory constituents of some other diseases related to the 5-lipoxygenase route.
    Type: Grant
    Filed: November 19, 1999
    Date of Patent: October 31, 2000
    Assignee: Sanofi-Synthelabo
    Inventors: Itzchak Angel, Sonia Arbilla, Luc Even, Jonathon Marc Goldhill, Philippe Pichat, Nigel Oliver Roome
  • Patent number: 6124318
    Abstract: The invention relates to compounds of the formula ##STR1## in which: Y is --CH-- or --N--;R.sub.1 is a halogen or a CF.sub.3, (C.sub.1 -C.sub.4)alkyl or (C.sub.1 -C.sub.4)alkoxy group;R.sub.2 and R.sub.3 are each hydrogen or a (C.sub.1 -C.sub.3)alkyl;n is 0 or 1; andPh.sub.1 and Ph.sub.2 are each independently an unsubstituted, monosubstituted or polysubstituted phenyl group;to a process for their preparation and to the pharmaceutical compositions containing them.These compounds have neurotrophic and neuroprotective activity.
    Type: Grant
    Filed: July 27, 1999
    Date of Patent: September 26, 2000
    Assignee: Sanofi-Synthelabo
    Inventors: Marco Baroni, Rosanna Cardamone, Jacqueline Fournier, Umberto Guzzi
  • Patent number: 6118025
    Abstract: The invention concerns a method for preparing an optically active alcohol of formula (I) in which the carbon atom indicated by the symbol * can have the configuration (R) or (S) and X represents a non-substituted amino group or a mono- or di-(C.sub.1 -C.sub.4)alkylamino group optionally salified from corresponding ketones by catalytic hydrogenation in the presence of a rhodium complex.
    Type: Grant
    Filed: December 27, 1999
    Date of Patent: September 12, 2000
    Assignee: Sanofi-Synthelabo
    Inventors: Francine Agbossou, Marc Devocelle, Jean-Robert Dormoy, Andre Mortreux
  • Patent number: 6118006
    Abstract: The invention relates to a method for the preparation of 1-[2-(2-naphthyl)ethyl]-4-(3-trifluoromethylphenyl)-1,2,3,6-tetrahydropyri dine and its pharmaceutically acceptable salts by reacting 2-(2-bromoethyl)naphthalene with 4-(3-trifluoromethylphenyl)-1,2,3,6-tetrahydropyridine or one of its salts, and to a universal method for the preparation of the same product and its salts by the reduction of naphthylacetic acid, treatment of the resulting 2-naphthylethanol with hydrobromic acid and treatment of the 2-(2-bromoethyl)naphthalene with 4-(3-trifluoromethylphenyl)-1,2,3,6-tetrahydropyridine or one of its salts.
    Type: Grant
    Filed: June 22, 1999
    Date of Patent: September 12, 2000
    Assignee: Sanofi-Synthelabo
    Inventors: Michel Buj, Robert Filhol
  • Patent number: 6100278
    Abstract: The invention relates compounds of formula ##STR1## in which R.sub.1 to R.sub.9, R.sub.16 and R.sub.17 are as defined in claim 1.These compounds are pharmacologically active.
    Type: Grant
    Filed: November 4, 1999
    Date of Patent: August 8, 2000
    Assignee: Sanofi-Synthelabo
    Inventors: Bernard Ferrari, Jean Gougat, Claude Muneaux, Yvette Muneaux, Pierre Perreaut, Claudine Planchenault
  • Patent number: 6090818
    Abstract: The invention relates to compounds with formula (I), a process for their preparation and pharmaceutical compositions containing them.
    Type: Grant
    Filed: June 14, 1999
    Date of Patent: July 18, 2000
    Assignee: Sanofi-Synthelabo
    Inventors: Loic Foulon, Claudine Serradeil-Le Gal, Gerard Valette
  • Patent number: 6080875
    Abstract: The present invention relates to a process for the preparation of 2-thienylethylamine derivatives of general formula: ##STR1## as well as their acid addition salts, in which R represents a halogen atom and R.sub.1 represents a C.sub.1 -C.sub.4 alkyl group, characterized in that a thienylglycidic derivative of general formula: ##STR2## in which M represents an alkali metal atom or a fraction of an alkaline-earth metal atom, is reacted with a phenylglycine ester, optionally in the form of a strong acid salt, of general formula: ##STR3## in which R and R.sub.1 have the same meaning as above, in the presence of an alkali metal borchydride of general formula:X--Y IVin which X represents an alkali metal atom and Y represents a group of formula:--BH.sub.3 CN or --BH.sub.(4-w) Z.sub.win which Z represents a carboxylic acid residue and optionally in the presence of a C.sub.1 -C.sub.
    Type: Grant
    Filed: September 2, 1999
    Date of Patent: June 27, 2000
    Assignee: Sanofi-Synthelabo
    Inventors: Bertrand Castro, Jean-Robert Dormoy, Aldo Previero
  • Patent number: 6075021
    Abstract: Compounds of general formula (I) ##STR1## in which the variables are as defined in the specification, their preparation and their application in therapeutics.
    Type: Grant
    Filed: April 7, 1999
    Date of Patent: June 13, 2000
    Assignee: Synthelabo
    Inventors: Yannick Evanno, Mireille Sevrin, Christian Maloizel, Odette Legalloudec, Pascal George
  • Patent number: 6069165
    Abstract: A pharmaceutical composition, comprising a lipophilic phase and, as active principle, at least one compound selected froman optically active isomer or a racemate of amisulpride;an optically active isomer or a racemate of a pharmaceutically acceptable acid addition salt of amisulpride;an optically active isomer or a racemate of a quaternary ammonium salt of amisulpride; andan optically active isomer or a racemate of an oxide of amisulpride.
    Type: Grant
    Filed: March 16, 1999
    Date of Patent: May 30, 2000
    Assignee: Synthelabo
    Inventors: Veronique Andrieu, Alain Cuine, Jean Montel
  • Patent number: 6063780
    Abstract: In accordance with the present invention there is provided a method of treating a mammal having a solid tumor, the method comprising:a) administering to the mammal an effective amount of 3-amino-1,2,4-benzotriazine 1,4-dioxide;b) administering to the mammal an effective amount of paclitaxel; andc) administering to the mammal an effective amount of a platinum complex.The method provides unexpected synergistic efficacy. The invention further provides a kit for treatment of a mammalian tumor comprising 3-amino-1,2,-benzotriazine 1,4-dioxide, paclitaxel and a platinum complex.
    Type: Grant
    Filed: February 27, 1998
    Date of Patent: May 16, 2000
    Assignee: Sanofi-Synthelabo Inc.
    Inventors: Daniel L. Dexter, Paul E. Juniewicz, James B. Rake, Daniel D. Von Hoff
  • Patent number: 6063810
    Abstract: Compounds of formula (I), wherein A is a hydrogen atom or a hydroxyl group; B is a hydrogen atom or a C.sub.1-8 alkyl, C.sub.1-8 alkenyl, C.sub.1-8 fluoroalkyl or C.sub.1-8 perfluoroalkyl group; each of R.sub.1, R.sub.2 and R.sub.5, which are the same or different, is a hydrogen atom, a halogen such as chlorine, bromine or fluorine, a C.sub.1-8 alkyl, C.sub.1-8 alkenyl, C.sub.3-8 cycloalkyl, C.sub.3-8 cycloalkenyl, C.sub.6, C.sub.10 or C.sub.14 aryl, C.sub.1-6 alkoxycarbonyl, C.sub.1-6 hydroxyalkyl, C.sub.1-6 alkoxyalkyl, C.sub.1-6 alkoxy, C.sub.1-8 fluoroalkyl or C.sub.1-8 perfluoroalkyl group, or R.sub.1 and R.sub.2 taken together form a C.sub.3-8 cycloalkyl, C.sub.3-8 cycloalkenyl or C.sub.6, C.sub.10 or C.sub.14 aryl ring, except for compounds in which R.sub.1 and R.sub.2 are both hydrogen; each of R.sub.3 and R.sub.4, which are the same or different, is a hydrogen atom or a C.sub.1-8 alkyl, C.sub.1-8 alkenyl, C.sub.3-8 cycloalkyl or C.sub.3-8 cycloalkenyl group, or R.sub.3 and R.sub.
    Type: Grant
    Filed: August 31, 1998
    Date of Patent: May 16, 2000
    Assignee: Synthelabo
    Inventors: Christophe Philippo, Gilles Courtemanche, Eykmar Fett, Marie Claire Orts, Philippe Bovy, Stephen Eric O'Connor, Anne Marie Galzin
  • Patent number: 6060508
    Abstract: Compounds of general formula (I) ##STR1## in which: A represents either a hydrogen atom, a hydroxyl, a C.sub.1-6 hydroxyalkyl group, a thiol, a C.sub.1-6 alkylsulphanyl group, an amino group, a C.sub.1-6 alkylamino group, a di(C.sub.1-6 alkyl)amino group, a C.sub.1-6 alkylhydroxylamine group, a C.sub.1-6 alkoxy group, a hydroxylamine group, an N,O-di(C.sub.1-6 alkyl)hydroxylamine group, an azido or a halogen such as fluorine, chlorine or bromine, B represents a hydrogen atom, a linear or branched C.sub.1-6 alkyl group, a C.sub.2-6 alkenyl group, a C.sub.1-6 fluoroalkyl group, a C.sub.1-2 perfluoroalkyl group, a C.sub.1-6 alkoxy group, a phenyl group or an oxo group, X represents an oxygen or sulphur atom.Application in therapeutics.
    Type: Grant
    Filed: February 26, 1999
    Date of Patent: May 9, 2000
    Assignee: Synthelabo
    Inventors: Christophe Philippo, Marie Claire Orts, Olivier Crespin, Philippe R. Bovy