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.
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.
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
Abstract: This invention relates to a slimming cosmetic composition containing at least one compound inducing the production of IL-6 by the adipocytes in the form of a mixture with an NPY antagonist and/or an ?2 antagonist and with an excipient for a cosmetic preparation.
Type:
Application
Filed:
July 28, 2005
Publication date:
December 22, 2005
Applicant:
Sanfoi-Synthelabo
Inventors:
Pierre Casellas, Jean-Marie Derocq, Joelle Guesnet
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
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
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
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.
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
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.
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
Abstract: The pharmaceutical compositions for oral administration according to the invention contain 0.5% to 20% of N-piperidino-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methylpyrazole-3-carboxamide in microcrystalline form, and pharmaceutical excipients; they are formulated by wet granulation.
Type:
Grant
Filed:
May 1, 2002
Date of Patent:
May 17, 2005
Assignee:
Sanoti-Synthelabo
Inventors:
Bernard Abramovici, Christian Condamine, Jean-Claude Gromenil
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.
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.
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
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
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.
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
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.