Patents Assigned to Synthelabo
  • 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: 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: 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: 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: 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: 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
  • Patent number: 6056944
    Abstract: Polar lipid composition of plant origin for conveying an active agent and/or making it penetrate into a target cell, the composition being characterized in that it is comprised of an injectable, intra-articular, topical or ingestable aqueous emulsion of a polar lipid mixture rich in phospholipids, in glycolipids and in ceramides, having a composition which is substantially similar to that of the polar lipids constituents of lipid cytomembranes of cells and obtained from a plant compound such as cereal flour or an extract such as bran or lipids extracted from cereals by means of chlorinated solvants.
    Type: Grant
    Filed: June 8, 1998
    Date of Patent: May 2, 2000
    Assignee: Synthelabo
    Inventor: Claudine Finidori
  • Patent number: 6020352
    Abstract: The use of polyamine site antagonists in treating ischemic disorders of the retina and optic nerve head are disclosed. Especially preferred are certain 1-phenyl-2-piperidinoalkanol derivatives, such as eliprodil and ifenprodil.
    Type: Grant
    Filed: November 18, 1997
    Date of Patent: February 1, 2000
    Assignee: Synthelabo
    Inventors: Michael A. Kapin, Louis Desantis, Jr., Bernard Scatton, Salomon Langer
  • Patent number: 5969146
    Abstract: Compounds derived from oxazolidin-2-one of formula (I) ##STR1## in which: R.sub.1 represents a hydrogen atom, an alkyl group, a hydroxyalkyl group, a fluoroalkyl group, a hydroxyfluoroalkyl group, a cyanoalkyl group, a substituted or unsubstituted phenyl group, a substituted or unsubstituted phenylmethyl group or an R.sub.3 A- group in which R.sub.3 is a cycloalklyl or cyclooxyalkyl group which is unsubstituted or substituted by a hydroxyl group and A is a --CH.sub.2 or --CH.sub.2 --CH.sub.2 radical,R.sub.2 represents a hydrogen atom or a methyl group,X represents an oxygen or sulphur atom or an NR.sub.4 group where R.sub.4 is an alkyl group or a hydrogen atom, andZ represents an oxygen atom or a --CH.dbd.CH or --CH.sub.2 --CH.sub.2 group,their process of preparation and their applications in therapeutics.
    Type: Grant
    Filed: April 13, 1998
    Date of Patent: October 19, 1999
    Assignee: Synthelabo
    Inventors: Samir Jegham, Frederic Puech, Philippe Burnier, Danielle Berthon, Odile Leclerc
  • Patent number: 5958924
    Abstract: Compounds of formula (I) ##STR1## in which A represents a 4-(thieno?3,2-c! pyridin-4-yl)-1-piperazinyl or 4-(4-fluorobenzoyl)-1-piperidyl group, R.sub.1 and R.sub.2 each represent, independently of one another, either a hydrogen or halogen atom, or an amino, hydroxyl, nitro, cyano, (C.sub.1 -C.sub.6)alkyl, (C.sub.1 -C.sub.6)alkoxy, trifluoromethyl, trifluoromethoxy or --COOH group, a group --COOR.sub.4, a --CONH.sub.2 group or a group --CONHR.sub.4, --CONR.sub.4 R.sub.5, --SR.sub.4, --SO.sub.2 R.sub.4, --NHCOR.sub.4, --NHS0.sub.2 R.sub.4 or --N(R.sub.4).sub.2, where R.sub.4 and R.sub.5 are each a (C.sub.1 -C.sub.4)alkyl group, R.sub.3 represents either a hydrogen atom, or a (C.sub.1 -C.sub.4)alkyl group, or a group --(CH.sub.2)OH, --(CH.sub.2).sub.p NH.sub.2, --(CH.sub.2).sub.n COOH, --(CH.sub.2).sub.n COOR.sub.4, --(CH.sub.2).sub.n CONH.sub.2, --(CH.sub.2).sub.n CONHOH, --(CH.sub.2).sub.p SH, --(CH.sub.2).sub.n SO.sub.3 H, --(CH.sub.2).sub.n SO.sub.2 NH.sub.2, --(CH.sub.2).sub.n SO.sub.2 NHR.sub.4, --(CH.
    Type: Grant
    Filed: February 4, 1998
    Date of Patent: September 28, 1999
    Assignee: SYNTHELABO
    Inventors: Gary McCort, Christian Hoornaert, Genevieve Dellac, Michel Aletru
  • Patent number: 5929089
    Abstract: Compounds corresponding to the general formula (I) ##STR1## in which R.sub.1 represents a (C.sub.1 -C.sub.4)alkyl or (C.sub.3 -C.sub.7)cycloalkylmethyl group, X.sub.1 represents a hydrogen or halogen atom or a (C.sub.1 -C.sub.4)alkoxy group or else OR.sub.1 and X.sub.1 together represent a group of formula -OCH.sub.2 O-, -O(CH.sub.2).sub.2 -, -O(CH.sub.2).sub.3 -, -O(CH.sub.2).sub.2 O- or -O(CH.sub.2).sub.3 O-, X.sub.2 represents a hydrogen atom or an amino group, X.sub.3 represents a hydrogen or halogen atom, and R.sub.2 represents either a hydrogen atom or an optionally substituted (C.sub.1 -C.sub.6) alkyl group or a phenyl (C.sub.1 -C.sub.4) alkyl group which is optionally substituted on the phenyl ring or a phenyl (C.sub.2 -C.sub.3) alkenyl group or a phenoxy (C.sub.2 -C.sub.4) alkyl group or a cyclo (C.sub.3 -C.sub.7) alkylmethyl group or a 2,3-dihydro-1H-inden-1-yl or 2,3-dihydro-1H-inden-2-yl group or a group of general formula -(CH.sub.2).sub.
    Type: Grant
    Filed: May 8, 1998
    Date of Patent: July 27, 1999
    Assignee: Synthelabo
    Inventors: Samir Jegham, Alistair Lochead, Frederic Galli, Alain Nedelec, Axelle Solignac, Laurence De Cruz
  • Patent number: 5929078
    Abstract: Compounds corresponding to the general formula (I): ##STR1## in which X represents a hydrogen atom, a hydroxyl group, a C.sub.1 -C.sub.3 alkoxy group or a cyclopropylmethoxy group and Y represents a hydrogen atom, a hydroxyl group or a methoxy group and salts and bases thereof. The compounds may exists in the form of a pure enantiomer or as a mixture of enantiomers. Additionally, the compounds of formula (I) are useful for the treatment of diseases associated with serotoninergic receptors, particularly anxiety and/or depression.
    Type: Grant
    Filed: February 3, 1998
    Date of Patent: July 27, 1999
    Assignee: Synthelabo
    Inventors: Pascal George, Mireille Sevrin, Philippe Manoury, Michel Peynot, Daniele De Peretti, Jean Fran.cedilla.ois Gibert, Arlette Tixidre, David Machnik
  • Patent number: 5925662
    Abstract: Derivatives of oxazolidin-2-one of general formula (I) ##STR1## in which: n is equal to 0 or 1,R.sub.1 represents a cyano group, an alkyl group or a fluoroalkyl group,R.sub.2 represents a hydrogen atom or a hydroxyl group, andR.sub.3 represents a hydrogen atom or a methyl group.Application in therapeutics.
    Type: Grant
    Filed: May 8, 1998
    Date of Patent: July 20, 1999
    Assignee: Synthelabo
    Inventors: Samir Jegham, Frederic Puech, Philippe Burnier, Danielle Berthon
  • Patent number: 5922739
    Abstract: Compounds of general formula (I) ##STR1## in which R.sub.1 represents a hydrogen atom or a (C.sub.1 -C.sub.4)alkyl, (C.sub.3 -C.sub.6)cycloalkylmethyl or phenyl-(C.sub.1 -C.sub.3)alkyl group optionally substituted on the phenyl ring with one or more atoms or groups chosen from halogens and methyl, trifluoromethyl, methoxy and cyano groups, R.sub.2 represents a hydroxyl or alkoxy group or a group of general formula NR.sub.3 R.sub.4 in which R.sub.3 and R.sub.4 each represent a hydrogen atom, an alkyl group, a cycloalkyl group, a cycloalkylmethyl group, a phenyl group, a phenylmethyl group or a pyridyl group, or alternatively R.sub.3 and R.sub.4 form, together with the nitrogen atom, a pyrrolidine or piptzidine ring, and n represents the number 1, 2 or 3.Application in therapy.
    Type: Grant
    Filed: June 8, 1998
    Date of Patent: July 13, 1999
    Assignee: Synthelabo
    Inventors: Gihad Dargazanli, Yannick Evanno, Jonathan Frost, Patrick Lardenois, Mireille Sevrin, Pascal George
  • Patent number: 5891884
    Abstract: Use of a compound represented by the following general formula (I) ##STR1## where X is a group --CH-- or a nitrogen atom; R.sub.1 is a hydrogen atom, a benzyl group, a substituted benzyl group; a non-substituted heterocyclic methyl group wherein the heterocyclic part is a pyridyl, thienyl or furyl; or a substituted heterocyclic methyl group;R.sub.2 is a hydrogen atom or (C.sub.1-4) alkyl group;R.sub.3 is a hydrogen atom or hydroxy group;R.sub.4 is a hydrogen atom or (C.sub.1-4) alkyl group, its tautomer whenR.sub.3 is an hydroxy group, their pharmaceutically permissible acid addition salts, or any of their hydrates for preventing and/or treating rhinitis.
    Type: Grant
    Filed: September 24, 1997
    Date of Patent: April 6, 1999
    Assignee: Synthelabo
    Inventors: Noboru Yamada, Fumiko Sano
  • Patent number: 5869518
    Abstract: Azacyloalkane derivatives of general formula ##STR1## in which: R.sub.1 and R.sub.2 represent a hydrogen atom, an alkyl group or a phenyl group, or R.sub.1 and R.sub.2 together form an oxo group, R.sub.3 represents a hydrogen atom or an alkyl group, or alternatively R.sub.3 forms a methylene group, R.sub.4 represents an aromatic group or, when R.sub.3 forms a methylene group, R.sub.4 represents a phenylene group in which one carbon atom is linked to Y and another carbon atom, adjacent to the preceding one, is linked to the said methylene group, R.sub.5 is either a group OR.sub.7, where R.sub.7 is a hydrogen atom or a benzyl group, or an N.sup.4 -methylpiperazinyl group, or alternatively a group NHR.sub.8 where R.sub.8 is a hydroxyl, pyridylmethyl or phenylmethyl group, A is an optionally substituted aromatic ring, n is equal to 1 or 2, X is CH, O or N, and Y is CH.sub.2, O or S, the process for preparing them and their applications in therapy.
    Type: Grant
    Filed: October 31, 1997
    Date of Patent: February 9, 1999
    Assignee: SYNTHELABO
    Inventors: Manuel Bedoya Zurita, Juan Antonio Diaz Martin, Gregorio del Sol Moreno, Ulpiano Martin Escudero Perez, Maria Dolores Jimenez Bargueno, Magali Romanach Ferrer
  • Patent number: D414937
    Type: Grant
    Filed: August 26, 1997
    Date of Patent: October 12, 1999
    Assignee: Synthelabo
    Inventors: Jean-Michel Cornu, Veronique Malcourant
  • Patent number: D423784
    Type: Grant
    Filed: March 2, 1999
    Date of Patent: May 2, 2000
    Assignee: Synthelabo
    Inventor: Olivier Joulin