Abstract: The invention relates to a process for the preparation of spiro[cis-4-(&bgr;-hydroxyethyloxy)cyclohexane-[3H]indol]-2′[1′H]-one derivatives of the formula (I) wherein R1 and R2 are as defined herein, by reduction of a dispiro[(1,3-dioxolane)-2,4′-cyclohexane-1′3′-[3H]indol]-2″[1″H]-one derivative of general formula (II), wherein R1 and R2 are as defined herein, which comprises carrying out the reduction (a) with sodium cyanoborohydride in the presence of a Lewis acid, or (b) with sodium borohydride in the presence of a strong acid.
Type:
Grant
Filed:
April 17, 2002
Date of Patent:
April 1, 2003
Assignee:
Sanofi-Synthelabo
Inventors:
Gergely Héja, Éva Csikós, Csaba Gönczi, Judit Halász, Félix Hajdú, István Hermecz, László Kis, Lajos Nagy, Andrea Sántáné Csutor, Kálmán Simon, Tiborné Szomor, Györgyné Szvoboda
Abstract: The invention relates to pyridopyranoazepine derivatives, to pharmaceutical compositions containing them, to processes 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: A synthetic polysaccharide including an antithrombin III binding domain consisting of a concatenation of five monosaccharides supporting a total of two carboxylic acid functions and at least four sulpho groups, said domain being directly bound at the non-reducing end by a thrombin binding domain including a concatenation of 10-25 monosaccharide units selected from hexoses, pentoses or deoxy sugars of which all the hydroxyl groups are etherified by a C1-6 alkyl group or esterified in the form of sulpho groups, as well as salts and particularly pharmaceutically acceptable salts thereof, are disclosed.
Type:
Grant
Filed:
September 7, 1999
Date of Patent:
March 18, 2003
Assignees:
Sanofi-Synthelabo, Akzo Nobel
Inventors:
Pierre Alexandre Driguez, Philippe Duchaussoy, Jean Marc Herbert, Maurice Petitou, Constant Van Boeckel, Peter Grootenhuis, Johannes Basten, Cornelia Dreef-Tromp
Abstract: The invention relates to a stable fumagillin formulation and to the method of use thereof in treating and/or combating intestinal infections.
Abstract: Novel synthetic polysaccharides for use in the treatment of pathologies associated with a coagulation dysfunction.
Type:
Grant
Filed:
September 5, 2000
Date of Patent:
March 4, 2003
Assignees:
Sanofi-Synthelabo, Akzo Nobel N.V.
Inventors:
Johannes Basten, Cornelia Dreef-Tromp, Pierre Alexandre Driguez, Philippe Duchaussoy, Jean Marc Herbert, Maurice Petitou, Constant Van Boeckel
Abstract: The invention relates to a process for the preparation of Fumagillin by liberation from its salt characterized by reacting Fumagillin dicyclohexylamine salt with an organic acid in alcoholic medium.
Type:
Grant
Filed:
March 5, 2002
Date of Patent:
February 18, 2003
Assignee:
Sanofi-Synthelabo
Inventors:
Gyula Farkas, Andrea Györbiró, István Hermecz, Kálmán Simon, Anna Szabó, Árpádné Vasvári
Abstract: The present invention relates to controlled-release dosage forms of zolpidem or salts thereof adapted to release zolpidem over a predetermined time period, according to a biphasic profile of dissolution, where the first phase is an immediate release phase and the second phase is a prolonged release phase and particular embodiments thereof intended to avoid abuse.
Type:
Grant
Filed:
July 16, 2001
Date of Patent:
February 4, 2003
Assignee:
Sanofi-Synthelabo
Inventors:
Gérard Alaux, Gareth Lewis, Frédéric Andre
Abstract: N-(phenylacetyl)morpholine derivatives useful as NK1 receptor antagonists, a process for the preparation thereof, and pharmaceutical compositions containing them as active principle.
Type:
Grant
Filed:
September 24, 2001
Date of Patent:
January 14, 2003
Assignee:
Sanofi-Synthelabo
Inventors:
Jean-Philippe Ducoux, Xavier Emonds-Alt, Patrick Gueule, Vincenzo Proietto
Abstract: Novel orthorombic polymorph of clopidogrel hydrogen sulfate or hydrogen sulfate of methyl (+)-(S)-&agr;-(2-chlorophenyl)-4,5,6,7-tetrahydrothieno[3,2-c]pyridine-5-acetate and a process for its preparation
Type:
Grant
Filed:
June 21, 2002
Date of Patent:
January 7, 2003
Assignee:
Sanofi-Synthelabo
Inventors:
André Bousquet, Bertrand Castro, Jean Saint-Germain
Abstract: The invention relates to a method of crystallizing a tetrahydropyridine derivative, to the novel crystalline forms thereby obtained and to the pharmaceutical compositions containing said tetrahydropyridine derivative in a given crystalline form as the active principle.
Type:
Grant
Filed:
September 6, 2001
Date of Patent:
December 3, 2002
Assignee:
Sanofi-Synthelabo
Inventors:
Antoine Caron, Bruno Franc, Olivier Monnier
Abstract: The invention concerns compounds of formula (I) wherein A, X, Y, n, R1, R2 and R3 are as defined in claim 1. Said compounds are specifically binding to sigma receptors particularly those of the peripheral nervous system.
Type:
Grant
Filed:
February 27, 2002
Date of Patent:
November 19, 2002
Assignee:
Sanofi-Synthelabo
Inventors:
Robert Boigegrain, Bernard Bourrie, Martine Bourrie, Pierre Casellas, Jean Marc Herbert, Pierre Lair, Dino Nisato, Raymond Paul, Jean Claude Vernieres
Abstract: The invention relates to the use of a synthetic oligosaccharide which is a selective inhibitor of factor Xa acting via antithrombin III, alone or in association with aspirin, for the preparation of medicaments intended for preventing or treating thromboembolic diseases occurring in a mammal which has undergone a percutaneous transluminal angioplasty.
Type:
Application
Filed:
May 28, 2002
Publication date:
October 31, 2002
Applicant:
Sanofi-Synthelabo
Inventors:
Roger Guilcaume Cariou, Jacobus Christianus Johannes Stiekema
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: A toothbrush, of the type in which a brush head is equipped with flexible friction rods which include a lower anchoring foot by fastening the rods to a principal body of the head, the anchoring foot of at least some of the rods is received in an anchoring hole passing through the principal body in such a way that upper and lower ends of the anchoring foot are arranged above and below the upper and lower faces, respectively, of the principal body, an upper end of an anchoring foot is connected to a lower end by a bridge of material which extends outside the anchoring hole and, at the lower and upper ends of the anchoring foot, the bridge of material bears against the lower and upper faces, respectively, of the principal body in order to fasten the rods to the head.
Abstract: The invention concerns compounds of formula (I) in racemic or optically pure form, methods for obtaining them and pharmaceutical compositions containing same. Said compounds are selective NK3 receptor antagonists.
Type:
Grant
Filed:
April 5, 2001
Date of Patent:
October 15, 2002
Assignee:
Sanofi-Synthelabo
Inventors:
Alain Aulombard, Xavier Emonds-Alt, Vincenzo Proietto, Didier Van Broeck
Abstract: 4-Oxo-3,5-dihydro-4H-pyridazino[4,5-b]indole-1-carboxamide derivatives having affinity for the peripheral benzodiazepine receptors are useful for the prevention or treatment of peripheral neuropathies and for the treatment of central neurogenerative diseases.
Type:
Grant
Filed:
July 25, 2001
Date of Patent:
September 17, 2002
Assignee:
Sanofi-Synthelabo
Inventors:
Frank Marguet, Jacques Froissant, Régine Bartsch-Li, Benoît Marabout, Mireille Sevrin
Abstract: The invention relates to an injection device comprising a syringe body (1), which delimits a chamber which is designed to be filled with liquid, and a unit (25) for distributing the liquid, comprising an end piece for closing off the said chamber, which is extended by a base, which supports an injection needle which is protected by a protective cap (35), the said distribution unit being mobile axially between a closing-off position of the chamber, and a position for injection of the liquid. According to the invention, the unit (25) for distributing comprises an intermediate section (31) between the base and the closing-off end piece, and the syringe body (1) comprises a ring (6) which delimits two superimposed compartments (18, 19), which can each accommodate the said intermediate section.
Abstract: The invention relates to an injection device comprising a syringe body (1, 13), which delimits a chamber which is designed to be filled with a liquid, and a unit (17) for distributing the liquid, comprising an end piece (17a) for closing off the chamber, which is extended by a locking male conical connection (17c), and can be displaced axially between a closing-off position of the said chamber and a position for injection of the liquid. According to the invention, the unit (17) for distributing comprises an intermediate connection (20), which is provided between the closing-off end piece (17a) and the male conical connection (17c).