Abstract: The present invention relates to compounds of formula (I): in which X represents N or CH; R1 represents a hydrogen or halogen atom or a CF3 group; R2 and R3 independently represent a hydrogen atom or a methyl group; n is 0 or 1; A represents an optionally substituted nitrogenous heterocycle; and to their N-oxides and to their salts or solvates, to the pharmaceutical compositions and the medicaments comprising them, and to a process for their preparation.
Type:
Grant
Filed:
April 19, 2002
Date of Patent:
March 6, 2007
Assignee:
Sanofi-Aventis
Inventors:
Marco Baroni, Bernard Bourrie, Pierre Casellas
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 the compounds of formula: as well as to the salts thereof with inorganic or organic acids, to solvates thereof and/or to hydrates thereof, which have strong affinity and high selectivity for the human NK1 receptors of substance P. The invention also relates to the process for preparing them, to the intermediate compounds of formula (VII) which are useful for the preparation, to pharmaceutical compositions containing them and to their fuse for the manufacture of medicinal products intended for treating any pathology in which substance P and the human NK1 receptors are involved.
Type:
Grant
Filed:
September 16, 2003
Date of Patent:
October 4, 2005
Assignee:
Sanofi-Aventis
Inventors:
Jean-Philippe Ducoux, Xavier Emonds-Alt, Patrick Gueule, Vincenzo Proietto
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: 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: 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.
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: 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: A method of using 1,2,4-benzotriazine oxides, some of which are novel compounds, as radiosensitizers and selective cytotoxic agents is disclosed. These compounds are shown to specifically radiosensitize hypoxic tumor cells. Some are additionally disclosed to be useful as specific cytotoxic agents for these cells. They also show an unexpected ability to radiosensitize aerobic cells following or preceding a hypoxic incubation of the cells with the drug. This provides a basis for selective radiosensitization of tumors compared to normal cells. A novel method for preparing the 1,2,4-benzotriazine oxides is also disclosed.
Type:
Grant
Filed:
December 17, 2001
Date of Patent:
December 7, 2004
Assignee:
SRI International
Inventors:
William W. Lee, J. Martin Brown, Edward W. Grange, Abelardo P. Martinez, Michael Tracy, Daniel J. Pollart
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