Patents Assigned to Sanofi-Synthelabo
  • Patent number: 8535721
    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: Grant
    Filed: February 21, 2006
    Date of Patent: September 17, 2013
    Assignee: Sanofi-Synthelabo
    Inventors: Christian Langlois, Jean-Yves Lanne
  • Patent number: 7427615
    Abstract: A pyrimidone derivative represented by formula (I) or a salt thereof, or a solvate thereof or a hydrate thereof having inhibitory activity against tau protein kinase 1: wherein R1 represents a C1-C12 alkyl group which may be substituted; R represents, for example, a group represented by the following formula (II): wherein R2 and R3 independently represent a hydrogen atom or a C1-C8 alkyl group; R4 represents a benzene ring which may be substituted, a naphthalene ring which may be substituted, an indan ring which may be substituted, a tetrahydronaphthalene ring which may be substituted, or an optionally substituted heterocyclic ring having 1 to 4 hetero atoms selected from the group consisting of oxygen atom, sulfur atom and nitrogen atom, and having 5 to 10 ring-constituting atoms in total.
    Type: Grant
    Filed: September 20, 2002
    Date of Patent: September 23, 2008
    Assignees: Mitsubishi Pharma Corporation, Sanofi-Synthelabo
    Inventors: Fumiaki Uehara, Keiichi Aritomo, Aya Shoda, Shinsuke Hiki, Masahiro Okuyama, Yoshihiro Usui, Mitsuru Ooizumi, Kazutoshi Watanabe, Koichi Yamakoshi
  • Patent number: 6979683
    Abstract: The invention relates to benzimidazole derivatives of general formula (I) in which X represents a nitrogen atom or a carbon atom; and when X represents a nitrogen atom R3 represents in particular a hydrogen atom or a (C1-C4)alkyl group, R4 represents in particular a hydrogen atom; a (C1-C6)alkyl; (C3-C7)cycloalkyl; 4-piperidyl; —(CH2)p—NR5R6; —(CH2)p—CONR5R6; —CO—(CH2)p—NR5R6; —(CH2)p-phenyl; —(CH2)p-morpholinyl; —(CH2)p-pyrrolidinyl; —(CH2)p-tetrahydroisoquinoline; —(CH2)p-heteroaryl; heteroarylcarbonyl; phenylcarbonyl; (C1-C6)alkylcarbonyl; —(CH2)p—COOR?; or phenylsulphonyl group; and when X represents a carbon atom R3 represents a hydrogen atom; a group —NR5R6; —NHCOR7; —CONHR5; —COR7; —NHCONH2; —OH or —CH2OH, R4 represents in particular a hydrogen atom; an optionally substituted group —(CH2)p-phenyl; a group —(CH2)p-heteroaryl; or a group —(CH2)tNR7R8. Preparation process and therapeutic application.
    Type: Grant
    Filed: November 21, 2001
    Date of Patent: December 27, 2005
    Assignee: Sanofi-Synthelabo
    Inventors: Francis Barth, Daniel Bichon, Frank Bolkenius, Viviane Van Dorsselaer
  • Patent number: 6949583
    Abstract: The invention relates to benzofuran or benzothiophene derivatives, to processes for preparing them, to pharmaceutical compositions comprising them, and to the method of use thereof in the treatment of pathological syndromes of the cardiovascular system.
    Type: Grant
    Filed: August 21, 2001
    Date of Patent: September 27, 2005
    Assignee: Sanofi-Synthelabo
    Inventors: Jean-Louis Assens, Claude Bernhart, Frédérique Cabanel-Haudricourt, Patrick Gautier, Dino Nisato
  • Publication number: 20050202089
    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: Application
    Filed: January 3, 2005
    Publication date: September 15, 2005
    Applicant: SANOFI-SYNTHELABO
    Inventors: Maryvonne Chariot, Gareth Lewis, Jean Montel
  • Publication number: 20050182104
    Abstract: This invention discloses and claims a compound conforming to the general formula (I): Wherein R1, R2, R?2, R3, R4 and R5 are as described herein. The compounds of the present invention exhibit an inhibitory effect on the production of ?-amyloid peptide (?-A4) by inhibition of gamma protease. Therefore, the compounds of the present invention are useful in the treatment of pathologies such as senile dementia, Alzheimer's disease, Down's syndrome, Parkinson's disease, amyloid angiopathy and/or cerebrovascular disorders.
    Type: Application
    Filed: January 14, 2005
    Publication date: August 18, 2005
    Applicant: Sanofi-Synthelabo
    Inventors: Sylvie Balter, Bruno Schoentjes, Viviane Van Dorsselaer
  • Patent number: 6918889
    Abstract: A single-use injection device, includes a pre-filled syringe (1), a syringe body (5) which is integral with the said syringe, and a protective case (10), the syringe body and protective case being provided with elements (9, 14, 15, 21) for relative locking in translation, which permit their relative displacement between a position of injection and a position of protection after use. The injection device includes a locking ring (23), which is provided with digital support elements (24), and locking units (25), which can lock the syringe body (5) and the protective case (10), in their position of injection, during injection, and can be displaced axially, such as to permit relative displacement of the syringe body and protective case, towards their position of protection after use, under the effect of the action of resilient member (27), only when the plunger (4) has reached its end of travel.
    Type: Grant
    Filed: May 25, 2000
    Date of Patent: July 19, 2005
    Assignee: Sanofi-Synthelabo
    Inventor: Marc Brunel
  • Patent number: 6916929
    Abstract: The invention relates to a process for preparing a 4-alkoxycarbonylamino-1-benzyl-4-phenylpiperidine of formula (I) via hydrolysis of 1-benzyl-4-cyano-4-phenylpiperidine (II) in acidic medium and treatment of the 1-benzyl-4-phenyl-4-piperidinecarboxamide (III) thus obtained with bromine in the presence of an alkali metal alkoxide. The invention also relates to a process for preparing 4-methylamino-4-phenylpiperidine from compound (II).
    Type: Grant
    Filed: July 15, 2002
    Date of Patent: July 12, 2005
    Assignee: Sanofi-Synthelabo
    Inventors: Gilles Anne-Archard, Patrick Gros-Claude
  • Patent number: 6908914
    Abstract: The invention relates to benzene derivatives, to pharmaceutical compositions containing them, to processes for preparing them, and to the method of use thereof in the treatment of psychotic disorders.
    Type: Grant
    Filed: June 27, 2000
    Date of Patent: June 21, 2005
    Assignee: Sanofi-Synthelabo
    Inventors: Robert Boigegrain, Martine Bourrie, Pierre Lair, Raymond Paul, Martine Poncelet, Jean Claude Vernieres
  • Patent number: 6908927
    Abstract: The invention relates to pyridopyranoazepine derivatives, to pharmaceutical compositions containing them, to process 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.
    Type: Grant
    Filed: February 6, 2003
    Date of Patent: June 21, 2005
    Assignee: Sanofi-Synthelabo
    Inventors: Frédéric Galli, Samir Jegham, Alistair Lochead, Axelle Samson
  • Patent number: 6894186
    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: April 29, 2003
    Date of Patent: May 17, 2005
    Assignee: Sanofi-Synthelabo
    Inventors: André Bousquet, Andrée Musolino
  • Patent number: 6867220
    Abstract: The invention relates to compounds of formula (I) where R1 represents a hydrogen or halogen atom or an —S(O)z—(C1-C4)alkyl, —S(O)z—(C1-C4)R3, —SO2—NH—(C1-C4)alkyl, —NHCO(C1-C4) alkyl, —CO(C1-C4)alkyl or —NHSO2—(C1-C4)alkyl group; m and n independently represent 0, 1 or 2; A represents a group of formula (a) or (b): where X is N or CH; R2 represents an —SO2—R3, —CO—R3 or —CO—(C1-C4)—alkyl group; R3 represents a phenyl group, optionally substituted by a (C1-C4)alkyl or (C1-C4)alkoxy group, one or two halogen atoms or a heterocycle; R4 represents a hydrogen or halogen atom or a (C1-C6)alkyl, (C1-C4)alkoxy, —COOH, —COO(C1-C4)alkyl, —CN, —CONR5R6, —NO2, —NHSO2(C1-C4)alkyl or —SO2NR5R6 group; z is 1 or 2; R5 and R6 independently represent a hydrogen atom or a (C1-C4)alkyl, phenyl or phenyl (C1-C4)alkyl group; and their salts or solvates, to a process for their preparation, to synthetic intermediates and to the pharmaceutical compositions comprising them.
    Type: Grant
    Filed: December 14, 2000
    Date of Patent: March 15, 2005
    Assignee: Sanofi-Synthelabo
    Inventor: Roberto Cecchi
  • Patent number: 6864277
    Abstract: The invention relates to compounds of formula: and to solvates and/or hydrates thereof, with affinity for and selectivity towards the Vreceptors or both the V1b and V1a receptors of arginine-vasopressin. The invention also relates to a process for preparing them, to the intermediate compounds of formula (II) which are useful for preparing them, to pharmaceutical compositions containing them and to their use for preparing medicinal products.
    Type: Grant
    Filed: June 19, 2001
    Date of Patent: March 8, 2005
    Assignee: Sanofi-Synthelabo
    Inventors: Richard Roux, Claudine Serradeil-Le Gal, Jean Wagnon
  • Patent number: 6861072
    Abstract: The invention concerns a pharmaceutical composition with gastric residence and controlled release, characterized in that it comprises two or three layers and contains (a) an active principle associated with a excipient modifying its release; (b) a system generating carbon dioxide in a swelling polymer hydrophilic matrix; (a) and (b) capable of being included in a common layer or in separate layers.
    Type: Grant
    Filed: October 12, 1999
    Date of Patent: March 1, 2005
    Assignee: Sanofi-Synthelabo
    Inventors: Gérard Alaux, Frédéric Andre, Alain Cuine, Gareth Lewis
  • Patent number: 6858629
    Abstract: Compounds of formula (I): where X is N or CH; A represents a group of formula (a) or (b) R1 represents hydrogen or an —NH2, —NR3R4, —NR3CO(C1-C4)Alk or —NR3SO2(C1-C4)Alk group; R2 represents hydrogen, a halogen or a (C1-C4)Alk, (C1-C4)alkoxy, —COOH, —COO(C1-C4)Alk, —CN, —CONR3R4, —NO2, —SO2NR3R4 or —NHSO2(C1-C4)Alk; m and n each represent 0, 1 or 2; R3 and R4 each represent hydrogen or a (C1-C4)Alk group; Y1 and Y2 each represent NH or O; and their salts or solvates, a process for their preparation and the pharmaceutical compositions comprising them.
    Type: Grant
    Filed: September 8, 2000
    Date of Patent: February 22, 2005
    Assignee: Sanofi-Synthelabo
    Inventors: Roberto Cecchi, Ambrogio Oliva
  • Patent number: 6852736
    Abstract: The invention concerns phenoxypropanolamines of formula (I) in which R1 represents a hydrogen, a group —S(O)z—(C1-C4)alk-R?, (R? being H, phenyl or (C1-C4)alkoxy), —NHSO2—(C1-C4)alk or NHCO(C1-C4)alk; m and n are each independently 0, 1 or 2; R2 and R3 independently represent a hydrogen, a (C5-C6)alkyl, (C3-C6)cycloalkyl, (C1-C4)alkoxy, hydrogen(C1-C4)alkoxy-(C1-C4)alkyl, mono- or di(C1-C4)alkamino(C1-C4)alkyl, pyrrolidino(C1-C4)alkyl, phenylamino or (C2-C4)alkenyl group, an aromatic or heteroaromatic group optionally substituted with a group R4, an aralkyl or heteroaralkyl group optionally substituted with a group R4, R2 and R3 can also together constitute a saturated or unsaturated ring of 3 to 8 atoms possibly bearing a (C1-C4)alkyl, amino (C1-C4)alkyl, carbamoyl or benzyl substituent; R4 represents a hydrogen or a halogen, or a group —CO(C1-C4)alk or a group —NHSO2—(C1-C4)alk; a group (C1-C4)alk, a group (C1-C4)alkoxy, a halogen, —COOH, —COO(C1-C4)alk, —CN, —CONR3R4, —NO2, —SO2NH2 or —NHSO2(C1-C4)alk;
    Type: Grant
    Filed: December 15, 2000
    Date of Patent: February 8, 2005
    Assignee: Sanofi-Synthelabo
    Inventors: Philippe R. Bovy, Roberto Cecchi, Olivier Venier
  • Patent number: 6846936
    Abstract: The invention relates to 2-butyl-3-(4-[3-(dibutylamino)propoxy]benzoyl-5-nitrobenzofuran hydrochloride, to its preparation and to its use as synthetic intermediate, in particular in preparing 2-butyl-3-(4-[3-(dibutylamino)propoxy]benzoyl)-5-nitrobenzofuran, itself an intermediate for dronedarone.
    Type: Grant
    Filed: December 10, 2001
    Date of Patent: January 25, 2005
    Assignee: Sanofi-Synthelabo
    Inventor: Michel Biard
  • Patent number: 6844337
    Abstract: Compounds corresponding to general formula (I) in which R1, R2, R3, R4 and R5 each represent, independently of one another, a hydrogen or halogen atom or a nitro, amino, trifluoromethyl, trifluoromethoxy, cyano, hydroxy, (C1-C6)alkyl, (C1-C6)alkoxy or phenyl group, it also being possible for two of these substituents in adjacent positions together to represent a methylenedioxy group, and R6 represents a hydrogen atom or a (C1-C6)alkyl group. Application in therapeutics.
    Type: Grant
    Filed: May 29, 2001
    Date of Patent: January 18, 2005
    Assignee: Sanofi-Synthelabo
    Inventors: Frédéric Galli, Odile Leclerc, Alistair Lochead
  • Patent number: 6844335
    Abstract: A pyrimidone derivative represented by formula (I) or a salt thereof: Wherein: R1 represents a hydrogen atom or a C1-6 alkyl group which may be substituted by a C6,10 aryl group; R2 represents a C1-10 alkyl group which may be substituted, a C2-6 alkenyl group which may be substituted, a C3-6 alkynyl group which may be substituted, a C3-6 cycloalkyl group which may be substituted, or a C6-10 ARYL group which may be substituted; or R1 and R2 form together a C2-6 alkylene group which may be substituted; or R1 and R2 form together a chain of formula —(CH2)2—X—(CH2)2— or —(CH2)2—X—(CH2)3— where X represents a oxygen atom, a sulfur atom, or a nitrogen atom which may be substituted; R3 represents a 2, 3 or 4-pyridyl group optionally substituted by a C1-4 alkyl group, C1-4 alkoxy group or halogen atom; and R4 represents a C1-10 alkyl group optionally substituted by a hydroxyl group, amino, C1-6 monoalkylamino group, C2-12 dialkylamino group or C6,10 aryl group which may be substituted.
    Type: Grant
    Filed: March 22, 2001
    Date of Patent: January 18, 2005
    Assignees: Sanofi-Synthelabo, Mitsubishi Pharma Corporation
    Inventors: Antonio Almario Garcia, Ryoichi Ando, Keiichi Arimoto, Fumiaki Uehara, Adrien Tak Li, Aya Shoda, Jonathan Reid Frost, Kazutoshi Watanabe
  • Patent number: D505320
    Type: Grant
    Filed: April 14, 2003
    Date of Patent: May 24, 2005
    Assignee: Sanofi-Synthelabo
    Inventors: Hervé Gattefosse, Patrick Sivera