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.
Abstract: The present invention relates to novel synthetic polysaccharides with antithrombotic activity exhibiting at least one covalent bond with biotin or a biotin derivative and to a process employing avidin or streptavidin which makes it possible to neutralize these polysaccharides.
Type:
Grant
Filed:
September 20, 2001
Date of Patent:
January 18, 2005
Assignee:
Sanofi-Synthelabo
Inventors:
Philippe Duchaussoy, Jean-Marc Herbert, Maurice Petitou, Pierre Savi
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.
Abstract: Compounds of the general formula (I)
in which R1, R2, R3 and R4 each represent a hydrogen or halogen atom or a nitro, amino, trifluoromethyl, cyano, hydroxyl, alkyl or alkoxy group, X represents either a nitrogen atom, in which case Z represents a group of the formula C—R5 or a nitrogen atom, or a group of the formula C—R6, in which case Z represents a nitrogen atom, R5 and R6 each represent a hydrogen or halogen atom or a trifluoromethyl, cyano, hydroxyl, (C1-C6)alkyl or (C1-C6)alkoxy group, and R7 represents a hydrogen atom or a (C1-C6)alkyl group.
Use in therapy.
Abstract: The invention relates to 2-butyl-5-(methanesulfonamido)benzofuran, its preparation and its use.
This compound is a synthesis intermediate, in particular for the preparation of dronedarone.
Abstract: The present invention relates to novel branched substituted amino derivatives of 3-amino-1-phenyl-1H-[1,2,4]triazole, processes for their preparation and pharmaceutical compositions comprising them.
Type:
Grant
Filed:
June 12, 2002
Date of Patent:
October 19, 2004
Assignee:
Sanofi-Synthelabo
Inventors:
Michel Geslin, Danielle Gully, Jean-Pierre Maffrand, Pierre Roger
Abstract: The invention relates to a novel crystalline form of irbesartan, to pharmaceutical compositions containing it, to processes for preparing it, and to a method for treating cardiovascular diseases utilizing it.
Type:
Grant
Filed:
March 12, 2001
Date of Patent:
October 5, 2004
Assignee:
Sanofi-Synthelabo
Inventors:
Bruno Franc, Christian Hoff, San Kiang, Mark D. Lindrud, Olivier Monnier, Chenkou Wei
Abstract: The invention relates to benzimidazole derivatives of general formula
in which
X represents a nitrogen atom or a carbon atom;
and when X represents a nitrogen atom:
R3 represents a hydrogen atom or a C1-C4 alkyl group, or does not exist, to give the compounds of formula (I) comprising a secondary or tertiary amine;
R4 represents a hydrogen atom or a C1-C6 alkyl, C3-C7 cycloalkyl, optionally substituted C3-C7 heterocycloalkyl, —(CH2)p-heteroaryl, heteroaryl-carbonyl, phenylcarbonyl, (C1-C6)alkylcarbonyl, —(CH2)pCOOR, optionally substituted phenylsulphonyl or optionally substituted —(CH2)p-phenyl group,
and, when X represents a carbon atom:
R3 represents a hydrogen atom or a group —NR5R6, —N(R5)3+, —NHCOR7, —CONHR5, —COR7, —NHCONH2, —OH or —CH2OH,
R4 represents a hydrogen atom or an optionally substituted —(CH2)p-phenyl, —(CH2)p-heteroaryl or —(CH2)tNR7R8 group.
Type:
Grant
Filed:
January 30, 2003
Date of Patent:
September 21, 2004
Assignee:
Sanofi-Synthelabo
Inventors:
Francis Barth, Daniel Bichon, Frank Bolkenius, Viviane Van Dorsselaer
Abstract: The invention relates to compounds of formula:
as well as the possible salts thereof with mineral or organic acids, and the solvates and/or hydrates thereof, which have affinity for and selectivity towards the V1b receptors or towards both the V1b and V1a receptors of arginine-vasopressin.
The invention also relates to the process for preparing them, to the intermediate compounds of formula (II) that are useful for preparing them, to pharmaceutical compositions containing them and to their use for the preparation of medicinal products.
Type:
Grant
Filed:
July 24, 2002
Date of Patent:
May 4, 2004
Assignee:
Sanofi-Synthelabo
Inventors:
Richard Roux, Claudine Serradeil-Le Gal, Bernard Tonnerre, Jean Wagnon
Abstract: The use of interleukin 7 or T cells pre-incubated in the presence of IL-7 for preparing a drug or pharmaceutical composition for treating an auto-immune disease, particularly an auto-immune disease induced by a defect in CD4+ T cell immunoregulation, is disclosed.
Type:
Grant
Filed:
August 18, 1998
Date of Patent:
March 30, 2004
Assignee:
Sanofi-Synthelabo
Inventors:
Jean Francois Bach, Jean Marc Gombert, Andre Herbelin, Michel Morre
Abstract: The invention relates to the use of a compound of formula (I):
for the preparation of pharmaceutical compositions for increasing the circulating, cellular and extracellular levels of TGF-&bgr;1.
Type:
Grant
Filed:
November 20, 2001
Date of Patent:
February 17, 2004
Assignee:
Sanofi-Synthelabo
Inventors:
Françoise Bono-Combie, Jacqueline Fournier, Jean Marc Herbert, Isabelle Lamarche, Umberto Guzzi
Abstract: The present invention relates to compounds of formula (I):
in which
R1 represents a hydrogen or halogen atom, or a group CF3;
R2 and R3 represent, independently, a hydrogen atom or a methyl group;
n and n′ each represent, independently, 0 or 1;
* represents the positions of attachment;
A represents N or CH;
X represents a sulfur or oxygen atom;
R4 and R5 represent, independently, a hydrogen atom or a (C1-C6) alkyl group;
and also their salts or solvates, to a method for the preparation thereof and to the pharmaceutical compositions containing them.
Type:
Grant
Filed:
October 15, 2002
Date of Patent:
February 10, 2004
Assignee:
Sanofi-Synthelabo
Inventors:
Marco Baroni, Bernard Bourrie, Rosanna Cardamone, Pierre Casellas
Abstract: The invention relates to lower-alkyl esters of 3-(3,4-dihalophenyl)-2,6-dioxopiperidine-3-propionic acid derivatives, and to processes for preparing the same.
Abstract: Compounds of formula [I]
in which:
W may represent a —(CH2)2—, —(CH2)3—, —CH2—C≡C— or —CH2—CH═CH— group,
R2 may in particular represent a piperidyl group, an optionally substituted 1,2,3,6-tetrahydropyridyl group, a hexahydro-1H-azepinyl group, an optionally substituted piperazinyl group or a morpholinyl group,
R3 may in particular represent a group —COR1,
A may in particular represent an optionally substituted phenyl group, a heterocycle or a cyclopentyl group, and
B may in particular represent a pyridyl group, an aminopyrazinyl group, an aminopyridazinyl group, a pyrimidinyl group optionally substituted with an amino group, piperidyl group or an aminopyridyl group optionally substituted on the pyridine with a (C1-C4)alkyl or (C1-C4)alkoxy group, the amino group possibly also being substituted with a (C1-C4)alkyl group,
their preparation and their therapeutic application.
Abstract: The present invention relates to novel indolin-2-one derivatives of formula:
to the preparation and to the pharmaceutical compositions comprising them.
These compounds have an affinity for oxytocin receptors.
Type:
Grant
Filed:
October 2, 2002
Date of Patent:
January 6, 2004
Assignee:
Sanofi-Synthelabo
Inventors:
Loïc Foulon, Georges Garcia, Claudine Serradeil-Le Gal, Gérard Valette
Abstract: The invention relates to the racemisation process of the optically active [2-(2-thienyl)ethylamino](2-halogenophenyl)acetamides of general formula (VII) by using basic compounds.
The resulting racemic compounds of general formula (VII) can thus be recycled into synthesis of the therapeutically useful compounds of general formula (VI).
Type:
Grant
Filed:
June 18, 2001
Date of Patent:
December 30, 2003
Assignee:
Sanofi-Synthelabo
Inventors:
Mária Bakonyl, Tiborné Bai, Zsolt Dombrády, Katalin Gáspár, Attila Supic
Abstract: Pentasaccharides in acidic form and their pharmaceutically acceptable salts, the anionic form thereof having the formula:
wherein:
R represents hydrogen or an —SO3−, (C1-C3)alkyl or (C2-C3)acyl group;
T represents hydrogen or an ethyl group; and
n represents 1 or 2 for use in the treatment of pathologies associated with a clotting dysfunction.