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: 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.
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: 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:
August 9, 2001
Date of Patent:
November 4, 2003
Assignee:
Sanofi-Synthelabo
Inventors:
Jean-Philippe Ducoux, Xavier Emonds-Alt, Patrick Gueule, Vincenzo Proietto
Abstract: The invention relates to a process for preparing 2-thienyl-2-ethanol, in which:
a) thiophene is metallated using an alkali metal, in the presence of an electron transfer agent,
b) the compound obtained is treated with ethylene oxide,
c) the thienyl derivative thus formed is hydrolyzed, to give the desired compound.
2-Thienyl-2-ethanol is a synthetic intermediate.
Abstract: The invention relates to pharmaceutical compositions containing (2S)-1-{(2R,3S)-5-chloro-3-(2-chlorophenyl)-1-(3,4-dimethoxybenzenesulfonyl)-3-hydroxy-2,3-dihydro-1H-indole-2-carbonyl}pyrrolidine-2-carboxamide, a selective V1a arginine vasopressin receptor antagonist, in combination with the equatorial isomer of 1-{4-(N-tert-butylcarbamoyl)-2-methoxybenzenesulfonyl}-5-ethoxy-3-spiro{4-(2-morpholinoethyloxy)cyclohexane}indol-2-one or one of its salts, a selective V2 arginine vasopressin receptor antagonist.
The invention relates to the use of such compositions for the production of medicines designed to treat all diseases for which either arginine vasopressin or the V2 receptors are implicated or to treat all diseases related to a water overlead.
Abstract: The invention relates to compounds of formula:
and their solvates and/or hydrates exhibiting affinity for the arginine-vasopressin V1b receptors or for both V1b and V1a receptors.
The invention also relates to their process of preparation, to the intermediate compounds of formula (II) of use for their preparation, to the pharmaceutical compositions comprising them and to their use for the preparation of medicaments.
Type:
Grant
Filed:
November 25, 2002
Date of Patent:
September 23, 2003
Assignee:
Sanofi-Synthelabo
Inventors:
Bruno Schoentjes, Claudine Serradeil-Le Gal, Jean Wagnon
Abstract: Compounds of general formula (I)
in which:
A represents a hydrogen atom, a hydroxyl, a C1-3 alkoxy group, a hydroxy(C1-6 alkyl) group, a (C1-3 alkoxy)(C1-3 alkyl) group, a thiol, (C1-6 alkyl)sulfanyl or a halogen;
B and D represent, independently of one another, a hydrogen atom, a C1-6 alkyl group, a fluoro(C1-6 alkyl) group or a perfluoro(C1-2 alkyl) group or B and D together from an oxo;
R1 represents a phenyl, a naphthyl or a heteroaryl comprising 4 or 5 carbon atoms;
R2 and R3 represent, independently of one another, a hydrogen atom, a halogen or a C1-6 alkyl group,
R4 represents a hydrogen atom, a hydroxyl or a halogen, and
R5 and R6 represent, independently of one another, a hydrogen atom, a C1-6 alkyl group, a C2-6 alkenyl group, a C3-6 cycloalkyl group, a C3-6 cycloalkenyl group, a fluoro(C1-6 alkyl) group or a perfluoro(C1-2 alkyl) group or R5 and R6 together form a C2-6 alkylene chain or a C3-6 alkenylene chain, to give, with the nitrogen to which they are attached, a heteroc
Type:
Grant
Filed:
May 22, 2002
Date of Patent:
September 9, 2003
Assignee:
Sanofi-Synthelabo
Inventors:
Philippe R Bovy, Alain Braun, Christophe Philippo
Abstract: The invention relates to compounds of formula
in which R1 to R9, R16 and R17 are as defined in claim 1.
These compounds are pharmacologically active.
Type:
Grant
Filed:
June 7, 2002
Date of Patent:
August 26, 2003
Assignee:
Sanofi-Synthelabo
Inventors:
Bernard Ferrari, Jean Gougat, Claude Muneaux, Yvette Muneaux, Pierre Perreaut, Claudine Planchenault
Abstract: The invention relates to a process for the preparation of a compound of formula (I) and the salts thereof by reacting the compound of formula (II) with the compound of formula (III), which comprises carrying out the reaction in dimethyl sulfoxide, at a temperature between 10° C. and 40° C., preferably at room temperature and transforming the resulting base of formula (I), if desired, into its salt by a method known per se.
Type:
Grant
Filed:
April 17, 2002
Date of Patent:
July 29, 2003
Assignee:
Sanofi-Synthelabo
Inventors:
Gergely Héja, Éva Csikós, Tünde Erösné Takácsy, Csaba Gönczi, Judit Halász, István Hermecz, Csilla Majláth, Lajos Nagy, Andrea Sántáné Csutor, Péter Sárosi, Kálmán Simon, Tiborné Szomor, Györgyné Szvoboda
Abstract: The invention relates to compounds of formula:
and their solvates and/or hydrates exhibiting an affinity and a selectivity for arginine-vasopressin V1b receptors or for both V1b and V1a receptors.
Type:
Grant
Filed:
August 12, 2002
Date of Patent:
July 22, 2003
Assignee:
Sanofi-Synthelabo
Inventors:
Claudine Serradeil-Le Gal, Bernard Tonnerre, Jean Wagnon
Abstract: Substituted 4-phenyl-2-aminothiazole derivatives, processes for preparing the same, and the use thereof as corticotropin releasing factor (CRF) antagonists.
Type:
Grant
Filed:
April 17, 2002
Date of Patent:
July 1, 2003
Assignee:
Sanofi-Synthelabo
Inventors:
Evelyne Fontaine, Michel Geslin, Danielle Gully, Antoine Pradines, Pierre Roger
Abstract: The invention relates to the use of 5HT2A AND 5HT2A/C receptor antagonists for the treatment of snoring and upper airway high resistance syndrome.
Abstract: The invention relates to a process for the preparation of spiro [(4-cyclohexanone)-[3H]indol]-2′[1′H]-one derivatives of general formula I—wherein R1 and R2 independently stand for hydrogen, C1-4alkyl, C1-4alkoxy, C1-4alkylthio, C1-4polyfluoroalkyl, C1-4polyfluoroalkoxy, C3-7cycloalkyloxy, C3-7cycloalkylthio, phenoxy, benzyloxy or nitro group—, characterized by reacting an indolin-2-one derivative of general formula II—wherein R1 and R2 are as defined above—with a compound capable for introducing a protective group, coupling the compound of general formula III, thus obtained—wherein R1 and R2 are as defined above and A stands for a protective group—with acrylic acid C1-4ester; cyclizing the resulting compound of general formula IV—wherein R1 and R2 are as defined above—with a compound capable for introducing a protective group, coupling the compound of formula III thus obtained,—wherein R1 and R2 are as defined abo
Type:
Grant
Filed:
April 17, 2002
Date of Patent:
June 3, 2003
Assignee:
Sanofi-Synthelabo
Inventors:
Csaba Gönczi, Éva Csikós, István Hermecz, Gergely Héja, Árpád Illár, Lajos Nagy, Andrea Sántáné Csutor, Attila Simon, Kálmán Simon, Ágota Smelkóné Esek, Tiborné Szomor, Györgyné Szvoboda
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 present invention relates to the use of saredutant and of its pharmaceutically acceptable salts for the treatment or prevention of adaptation disorders, bipolar disorders, and dysthymic disorders.
Type:
Grant
Filed:
October 9, 2001
Date of Patent:
June 3, 2003
Assignee:
Sanofi-Synthelabo
Inventors:
Xavier Emonds-Alt, Philippe Soubrie, Régis Steinberg
Abstract: The invention relates to a process for the preparation of 2-methoxy-4-(N-t-butylaminocarbonyl)benzenesulfonyl chloride by sulfonating m-hydroxybenzoic acid, methylating the hydroxy group of the resulting sulfonic acid or its salt, transforming the carboxylic acid group and the sulfonic acid group to acid chloride groups and reacting the 4-chlorosulfonyl-3-methoxy-benzoyl chloride with t-butylamine, which comprises carrying out the sulfonation of the 3-methoxy-benzoic acid of general formula (II) with 96% sulfuric acid, separating the resulting 3-hydroxy-4-sulfobenzoic acid of general formula (III) in the form of its salt of general formula (IV), wherein Z stands for alkali metal or ammonium group, methylating the compound of general formula (IV) in the presence of a phase transfer catalyst at a pH value of about 11.
Type:
Grant
Filed:
April 26, 2002
Date of Patent:
April 15, 2003
Assignee:
Sanofi-Synthelabo
Inventors:
Csaba Gönczi, Éva Csikós, Félix Hajdú, István Hermecz, Gergely Héja, Gergelyné Héja, Lajos Nagy, Andrea Sántáné Csutor, Kálmán Simon, Ágota Smelkóné Esek, Tiborné Szomor, Györgyné Szvoboda
Abstract: The invention relates to the use of direct or indirect selective inhibitors of factor Xa acting via antithrombin III, alone or in combination with one or more compounds with anti-platelet aggregation activity, for the preparation of medicines intended to prevent and to treat thromboembolic arterial diseases.
The subject of the invention is also pharmaceutical compositions containing one or more direct or indirect selective inhibitors of factor Xa which act via antithrombin III in combination with one or more compounds with anti-platelet aggregation activity, and optionally one or more pharmaceutically acceptable vehicles.
Type:
Grant
Filed:
February 11, 2000
Date of Patent:
April 1, 2003
Assignees:
Sanofi-Synthelabo, Akzo Nobel
Inventors:
André Bernat, Jean Marc Herbert, Maurice Petitou, Ronald Van Amsterdam