Patents Represented by Attorney, Agent or Law Firm Irving Newman
  • Patent number: 6906084
    Abstract: The present invention relates to compounds of formula I, in which R0; R1; R2; R3; R4; R5; R6; R7; Q; V, G and M have the meanings indicated in the claims. The compounds of formula I are valuable pharmacologically active compounds. They exhibit a strong antithrombotic effect and are suitable, for example, for the therapy and prophylaxis of cardiovascular disorders like thromboembolic diseases or restenoses. They are reversible inhibitors of the blood clotting enzymes factor Xa (FXa) and/or factor VIIa (FVIIa), and can in general be applied in conditions in which an undesired activity of factor Xa and/or factor VIIa is present or for the cure or prevention of which an inhibition of factor Xa and/or factor VIIa is indicated. The invention furthermore relates to processes for the preparation of compounds of formula I, their use, in particular as pharmaceuticals for treating the foregoing conditions, and pharmaceutical preparations comprising them.
    Type: Grant
    Filed: November 21, 2002
    Date of Patent: June 14, 2005
    Assignee: Aventis Pharma Deutschland GmbH
    Inventors: Marc Nazaré, Melanie Essrich, David William Will, Hans Matter, Kurt Ritter, Volkmar Wehner
  • Patent number: 6872717
    Abstract: A method of treating or preventing obesity, this method comprising administering to a patient in need of such treatment an effective amount of a compound of formula in which R, R3 and R4 are as defined in the specification.
    Type: Grant
    Filed: September 12, 2002
    Date of Patent: March 29, 2005
    Assignee: Aventis Pharma S.A.
    Inventors: Daniel Achard, Hervé Bouchard, Jean Bouquerel, Bruno Filoche, Serge Grisoni, Augustin Hittinger, Michael R. Myers
  • Patent number: 6858603
    Abstract: Disclosed are azetidine derivatives of formula: their optical isomers, their salts, their preparation and medicaments containing them.
    Type: Grant
    Filed: December 16, 2002
    Date of Patent: February 22, 2005
    Assignee: Aventis Pharma S.A.
    Inventors: Daniel Achard, Hervé Bouchard, Jean Bouquerel, Marc Capet, Serg Grisoni, Jean-Luc Malleron, Serge Mignani, Augustin Hittinger
  • Patent number: 6809177
    Abstract: The invention relates to a process for the conversion of echinocandin class of peptides to their C4-homotyrosine monodeoxy analogues, particularly mulundocandin to deoxymulundocandin, which consists of a single step selective reduction of C4-htyr (homotyrosine) hydroxyl group of echinocandins to their monodeoxy analogues under neutral conditions without prior protection/deprotection of the equally facile C5-Orn (ornithine) hydroxyl group and purification of the monodeoxy compound from the crude reaction mixture.
    Type: Grant
    Filed: March 29, 2001
    Date of Patent: October 26, 2004
    Assignee: Aventis Pharma Deutschland GmbH.
    Inventors: Triptikumar Mukhopadhyay, Kenia Jayvanti, Erra Koteswara Satya Vijaya Kumar
  • Patent number: 6806277
    Abstract: Quinolylpropylpiperidine derivatives of general formula (I) in which: R1 is NH2, alkylamino, dialkylamino, hydroxyamino, alkyl(alkyloxy)amino or alkyloxyamino, R2 is a carboxyl, carboxymethyl or hydroxymethyl radical, R3 is alkyl (1 to 6C) substituted by phenylthio which can itself carry 1 to 3 substituents selected from halogen, OH, alkyl, alkyloxy, CF3, OCF3, COOH, alkyloxycarbonyl, CN and NH2, by cycloalkylthio (3 to 7 members) or by heteroarylthio (5 to 6 members) comprising 1 to 4 heteroatoms selected from N, S and O and optionally itself substituted [by halogen, OH, alkyl, alkyloxy, CF3, OCF3, ═O, COOH, alkyloxycarbonyl, CN or NH2] or R3 is propargyl substituted by phenyl which can itself carry 1 to 3 substituents selected from halogen, OH, alkyl, alkyloxy, CF3, OCF3, COOH, alkyloxycarbonyl, CN and NH2 or substituted by cycloalkyl comprising 3 to 7 members or substituted by 5- to 6-membered heteroaryl comprising 1 to 4 heteroatoms chosen from N, O or S and optionally itself substituted
    Type: Grant
    Filed: July 18, 2003
    Date of Patent: October 19, 2004
    Assignee: Aventis, Pharma S.A.
    Inventors: Eric Bacqué, Jean-Luc Malleron, Serge Mignani, Michel Tabart
  • Patent number: 6800645
    Abstract: This invention is directed to physiologically active compounds of formula (I) wherein represents a bicyclic ring system, of about 10 to about 13 ring members, in which the ring is an azaheterocycle, and the ring represents an azaheteroaryl ring, or an optionally halo substituted benzene ring; R1 represents hydrogen or a straight- or branched-chain alkyl group of 1 to about 4 carbon atoms, optionally substituted by hydroxy or one or more halogen atoms, or when Z1 represents a direct bond R1 may also represent a lower alkenyl or lower alkynyl group, or a formyl group; R2 represents hydrogen, alkenyl, alkoxy, alkyl, alkylsulphinyl, alkylsulphonyl, alkylthio, aryl, arylalkyloxy, arylalkylsulphinyl, arylalkylsulphonyl, arylalkylthio, aryloxy, arylsulphinyl, arylsulphonyl, arylthio, cyano, cycloalkenyl, cycloalkenyloxy, cycloalkyl, cycloalkyloxy, heteroaryl, heteroarylalkyloxy, heteroaryloxy, hydroxy, —SO2NR4R5, —NR4SO2R5, —
    Type: Grant
    Filed: July 7, 2000
    Date of Patent: October 5, 2004
    Assignee: Aventis Pharma Limited
    Inventors: Paul Joseph Cox, Shelley Bower, David John Aldous, Peter Charles Astles, Daniel Gerard McGarry, Christopher Hulme, John Robinson Regan, Fu-Chih Huang, Stevan Wakefield Djuric, Kevin Joseph Moriarty, Rose Mappilakunnel Mathew, Gregory Bernard Poli
  • Patent number: 6753409
    Abstract: The invention is directed to a non-hygroscopic stable crystalline form of the antithrombotic compound N-[N-[N-(4-piperdin-4-yl)butanoyl)-N-ethylglycyl]-(L)-aspartyl]-(L)-&bgr;-cyclohexyl-alanine amide, to processes for preparing said stable crystalline form, to a pharmaceutical composition thereof, and intermediates thereof, and the invention is directed also to processes for preparing a compound of the formula wherein: A, B, Z, E1, E2, G, R, m, n, and p are as defined herein.
    Type: Grant
    Filed: August 15, 2000
    Date of Patent: June 22, 2004
    Assignee: Aventis Pharmaceuticals Inc.
    Inventors: Zofia J. Chrzan, James J. Mencel, David Toledo-Velasquez, Vincent Windisch, Rick G. Woodward, Diane C. Salazar, Narasimha M. Vemuri, Anthony J. Gardetto, Matthew R. Powers, Gregory G. Kubiak, Robert C. Liu, Benoit J. Vanasse, James P. Sherbine, Walter Rodriguez, Adam W. Sledeski
  • Patent number: 6734176
    Abstract: The present invention relates to pharmaceutical compositions containing, as active ingredient, a compound of formula: in which R1 represents a radical —NHCOR4 or —N(R5)—Y—R6, Y is CO or SO2, R4 represents a radical -alk-SO2—R11, -alk-SO2—CH═CH—R11 or Het substituted with —SO2—R11 or a phenyl radical substituted with —SO2—R11 or -alk-SO2—R11, R5 represents a hydrogen atom or an alkyl radical, R6 represents a phenylalkyl, Het or Ar radical, to the novel derivatives of formula (I) and to their preparation, as well s to their use in treating various disorders of the nervous system.
    Type: Grant
    Filed: December 17, 2002
    Date of Patent: May 11, 2004
    Assignee: Aventis Pharma S.A.
    Inventors: Daniel Achard, Hervé Bouchard, Jean Bouquerel, Bruno Filoche, Serge Grisoni, Augustin Hittinger, Michael R. Myers
  • Patent number: 6673834
    Abstract: Compounds of the formula I are suitable for producing pharmaceuticals for the prophylaxis and therapy of diseases in which high blood platelet aggregations occur.
    Type: Grant
    Filed: November 21, 2002
    Date of Patent: January 6, 2004
    Assignee: Aventis Pharma Deutschland GmbH
    Inventors: Michael Kurz, Matthias Herrmann, Luigi Toti, Laszlo Vertesy
  • Patent number: 6617316
    Abstract: The present invention relates to oligosaccharides of formula: to mixtures thereof, to diastereoisomers thereof, to a process for preparing them, to pharmaceutical compositions containing them, and to their use in preventing or treating a disease associated with an inflammatory process involving the production of nitric oxide.
    Type: Grant
    Filed: October 20, 2000
    Date of Patent: September 9, 2003
    Assignee: Aventis Pharma
    Inventors: Pierre Mourier, Elisabeth Perrin, Jean-marie Stutzmann, Christian Viskov, Florence Wahl
  • Patent number: 6608042
    Abstract: The present invention relates to pharmaceutical compositions containing as an active ingredient at least one oligosaccharide of formula: to novel oligosaccharides of formula (I), to mixtures thereof and to methods for their preparation.
    Type: Grant
    Filed: March 26, 2001
    Date of Patent: August 19, 2003
    Assignee: Aventis Pharma, S.A.
    Inventors: Pierre Mourier, Elisabeth Perrin, Christian Viskov
  • Patent number: 6602864
    Abstract: The compounds of formula I herein exhibit useful pharmacological activity and accordingly are incorporated into pharmaceutical compositions and used in the treatment of patients suffering from certain medical disorders. More specifically, they are inhibitors of the activity of Factor Xa. The present invention is directed to compounds of formula I, compositions containing compounds of formula I, and their use, which are for treating a patient suffering from, or subject to, physiological condition which can be ameliorated by the administration of an inhibitor of the activity of Factor Xa.
    Type: Grant
    Filed: June 3, 1998
    Date of Patent: August 5, 2003
    Assignee: Aventis Pharma Deutschland GmbH
    Inventors: Yong Mi Choi-Sledeski, Henry W. Pauls, Jeffrey N. Barton, William R. Ewing, Daniel M. Green, Michael R. Becker, Yong Gong
  • Patent number: 6602877
    Abstract: Compounds of formula (I) are described in which R1 is optionally substituted heteroaryl; R2 is optionally substituted aryl or optionally substituted heteroaryl; R3 is a group —L1—R7 or —L2—R8 [where L1 is an optionally substituted alkylene linkage; R7 is hydrogen, aryl, cyano, cycloalkyl, heteroaryl, heterocycloalkyl, nitro, —S(O)nR9, —NHSO2R9, —C(═Z)OR10, —C(═Z)R10, —OR10, —N(R11)—C(═Z)R9, —NY1Y2, —SO2NY1Y2, —C(═Z)—NY1Y2, —N(R11)—C(═Z)—NY1Y2, —N(OR10)—C(═Z)—NY1Y2, —N(OR10)—C(═Z)R10, —C(═NOR10)R10, —C(═Z)NR10OR12, —N(R11)—C(═NR13)—NY1Y2 or —N(R11)—C(═Z)OR11; L2 is a direct bond or a straight- or branched-carbon chain comprising from 2 to about 6 carbon atoms and contains a double or triple carbon-carbon bond; and R8 is hydrogen, aryl, cycloalkenyl, cycloalkyl, heteroaryl or
    Type: Grant
    Filed: December 8, 1999
    Date of Patent: August 5, 2003
    Assignee: Aventis Pharma Limited
    Inventors: Paul L. Bamborough, Alan J. Collis, Frank Halley, Richard A. Lewis, David J. Lythgoe, Jeffrey M. McKenna, Iain M. McLay, Barry Porter, Andrew J. Ratcliffe, Paul A. Wallace
  • Patent number: 6579858
    Abstract: Cerebral edema is prevented and treated by administering an effective amount of a low molecular weight heparin.
    Type: Grant
    Filed: November 29, 1999
    Date of Patent: June 17, 2003
    Assignee: Aventis Pharma S.A.
    Inventors: Véronique Mary, Jérémy Pratt, Jean-Marie Stutzman, André Uzan, Florence Wahl
  • Patent number: 6569993
    Abstract: This invention is directed to a process for the solid phase, fragment-based synthesis of resin-bound cyclic peptide analogs of parathyroid hormones and analogs of parathyroid hormone-related proteins, which analogs contain at least one bridge between the side chains of two non-adjacent amino acid residues, and to peptide fragments useful therefor.
    Type: Grant
    Filed: November 18, 1999
    Date of Patent: May 27, 2003
    Assignee: Aventis Pharma S.A.
    Inventors: Adam W. Sledeski, James J. Mencel
  • Patent number: 6566356
    Abstract: The present invention relates to pharmaceutical compositions containing, as active ingredient, a compound of formula: in which R1 represents a radical —NHCOR4 or —N(R5)—Y—R6, Y is CO or SO2, R4 represents a radical -alk-SO2—R11, -alk-SO2—CH═CH—R11 or Het substituted with —SO2—R11 or a phenyl radical substituted with —SO2—R11 or -alk-SO2—R11, R5 represents a hydrogen atom or an alkyl radical, R6 represents a phenylalkyl, Het or Ar radical, to the novel derivatives of formula (I) and to their preparation.
    Type: Grant
    Filed: March 2, 2001
    Date of Patent: May 20, 2003
    Assignee: Aventis Pharma S.A.
    Inventors: Daniel Achard, Hervé Bouchard, Jean Bouquerel, Bruno Filoche, Serge Grisoni, Augustin Hittinger, Michael R. Myers
  • Patent number: 6545006
    Abstract: The invention relates to a process for obtaining L-dihydroorotic acid by chromatography on an anionic exchange material in a base water mixture under a pressure from about 1.1 MPa to about 40 MPa. The process can be used to investigate the in vitro and in vivo activity of N-(4-trifluoromethylphenyl)-5-methylisoxazole-4-carboxamide, N-(4-trifluoromethylphenyl)-2-cyano-3-hydroxycrontonamide and similar compounds.
    Type: Grant
    Filed: December 11, 2000
    Date of Patent: April 8, 2003
    Assignee: Aventis Pharma Deutschland GmbH
    Inventors: Ulrike Milbert, Robert Bartlett, Eric Ruuth, Claude Fudali
  • Patent number: 6541505
    Abstract: This invention is directed to an (aminoiminomethyl or aminomethyl)benzoheteroaryl compound of formula I which is useful for inhibiting the activity of Factor Xa by combining said compound with a composition containing Factor Xa. The present invention is also directed to compositions containing compounds of the formula I, methods for their preparation, their use, such as in inhibiting the formation of thrombin or for treating a patient suffering from, or subject to, a disease state associated with a physiologically detrimental excess amount of thrombin.
    Type: Grant
    Filed: June 30, 2000
    Date of Patent: April 1, 2003
    Assignee: Aventis Pharmaceuticals Inc.
    Inventors: William P. Dankulich, Daniel G. McGarry, Christopher Burns, Timothy F. Gallagher, Francis A. Volz
  • Patent number: 6521252
    Abstract: The invention concerns a novel agent for transferring nucleic acids into cells. Said agent is particularly characterised in that it comprises one or several disulphide bonds sensitive to reducing conditions. The invention also concerns compositions comprising such an agent for transferring in vivo, ex vivo or in vitro nucleic acids of interest into different cell types.
    Type: Grant
    Filed: July 6, 2000
    Date of Patent: February 18, 2003
    Assignee: Aventis Pharma S.A.
    Inventors: Gérardo Byk, Catherine Dubertret, Bruno Pitard, Daniel Scherman
  • Patent number: 6518264
    Abstract: Disclosed are azetidine derivatives of formula: their optical isomers, their salts, their preparation and medicaments containing them.
    Type: Grant
    Filed: March 9, 2001
    Date of Patent: February 11, 2003
    Assignee: Aventis Pharma S.A.
    Inventors: Daniel Achard, Hervé Bouchard, Jean Bouquerel, Marc Capet, Serg Grisoni, Jean-Luc Malleron, Serge Mignani, Augustin Hittinger