Patents Represented by Attorney Michael D. Alexander
  • Patent number: 7176213
    Abstract: The present invention relates to adenosine A3 receptor ligands of the general formula (I), within those preferably antagonists, as well as their salts, solvates and isomers, and the pharmaceutical compositions containings them, to the use of the compounds of the general formula (I), as well as their salts, solvates and isomers, to the preparation of the compounds of the general formula (I) and their salts, solvates and isomers, furthermore to the new intermediates of the general formulae (II) and (III) and to the preparation thereof.
    Type: Grant
    Filed: December 17, 2002
    Date of Patent: February 13, 2007
    Assignee: Sanofi-Aventis
    Inventors: Péter Arányi, László Balázs, Mária Balogh, Sándor Bátori, Kinga Boér, Katalin Gerber, Zoltán Kapui, Endre Mikus, Geza Tímári, T. Nagy Lajos, Katalin Urbán-Szabó, Judit Vargáné Szeredi
  • Patent number: 6916838
    Abstract: Tricyclic derivatives of 1-benzylpyrazole-3-carboxylic acid which are antagonists of the cannabinoid CB2 receptors; their method of preparation and pharmaceutical compositions containing them.
    Type: Grant
    Filed: November 2, 2000
    Date of Patent: July 12, 2005
    Assignee: Sanofi-Aventis
    Inventors: Francis Barth, Joseph Millan, Didier Oustric, Murielle Rinaldi, Martine Vernhet
  • Patent number: 6908927
    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.
    Type: Grant
    Filed: February 6, 2003
    Date of Patent: June 21, 2005
    Assignee: Sanofi-Synthelabo
    Inventors: Frédéric Galli, Samir Jegham, Alistair Lochead, Axelle Samson
  • Patent number: 6893659
    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
  • Patent number: 6867220
    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.
    Type: Grant
    Filed: December 14, 2000
    Date of Patent: March 15, 2005
    Assignee: Sanofi-Synthelabo
    Inventor: Roberto Cecchi
  • Patent number: 6858629
    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.
    Type: Grant
    Filed: September 8, 2000
    Date of Patent: February 22, 2005
    Assignee: Sanofi-Synthelabo
    Inventors: Roberto Cecchi, Ambrogio Oliva
  • Patent number: 6852736
    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
  • Patent number: 6844337
    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.
    Type: Grant
    Filed: May 29, 2001
    Date of Patent: January 18, 2005
    Assignee: Sanofi-Synthelabo
    Inventors: Frédéric Galli, Odile Leclerc, Alistair Lochead
  • Patent number: 6835730
    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.
    Type: Grant
    Filed: September 24, 2002
    Date of Patent: December 28, 2004
    Assignee: Sanofi-Synthelabo
    Inventors: Frédéric Galli, Samir Jegham, Odile Leclerc, Alistair Lochead, Alain Nedelec
  • Patent number: 6828448
    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.
    Type: Grant
    Filed: June 10, 2003
    Date of Patent: December 7, 2004
    Assignee: Sanofi-Synthelabo
    Inventors: Noël Fino, Corinne Leroy
  • Patent number: 6828321
    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
  • Patent number: 6806282
    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
  • Patent number: 6800761
    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
  • Patent number: 6794382
    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
  • Patent number: 6767533
    Abstract: A composition containing a peripheral benzodiazepine receptor ligand for topical use in the treatment of cutaneous stress.
    Type: Grant
    Filed: May 14, 2001
    Date of Patent: July 27, 2004
    Assignee: Sanofi-Synthelabo
    Inventors: Pierre Casellas, Jean-Marie Derocq
  • Patent number: 6761879
    Abstract: The invention relates to a titanium-derived compounds, and to processes for preparing the same.
    Type: Grant
    Filed: April 17, 2002
    Date of Patent: July 13, 2004
    Assignee: Sanofi-Synthelabo
    Inventor: Claudine Finidori
  • Patent number: 6730695
    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
  • Patent number: 6713053
    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
  • Patent number: 6710042
    Abstract: Compounds of formula (I) are useful as human NK3 receptor antagonists.
    Type: Grant
    Filed: September 18, 2001
    Date of Patent: March 23, 2004
    Assignee: Sanofi-Synthelabo
    Inventors: Daniel Bichon, Xavier Edmonds-Alt, Patrick Gueule, Vincenzo Proietto, Didier Van Broeck
  • Patent number: 6693118
    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