Patents Assigned to Hoechst Marion Roussel
  • Cyclic nitrones
    Patent number: 5962469
    Abstract: The present invention is directed to novel cyclic nitrones and their use in the prevention of oxidation tissue damage by free radicals, their use in the treatment of a number of disease states in which radicals either damage or destroy tissues via oxidation, and pharmaceutical compositions containing these cyclic nitrones.
    Type: Grant
    Filed: November 26, 1997
    Date of Patent: October 5, 1999
    Assignee: Hoechst Marion Roussel Inc.
    Inventors: Craig E. Thomas, Thomas L. Fevig, Stephen M. Bowen, Robert A. Farr, Albert A. Carr, David A. Janowick
  • Method of lowering serum cholesterol levels with 2,6-di-alkyl-4-silyl-phenols
    Patent number: 5962435
    Abstract: A method of lowering plasma cholesterol level in a patient with hypercholesterolemia, by administration of a compound of formula (1) ##STR1## wherein: R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are each independently a C.sub.1 -C.sub.6 alkyl group;Z is a thio, oxy or methylene group;A is a C.sub.1 -C.sub.4 alkylene group; andR.sub.5 is a C.sub.1 -C.sub.6 alkyl or --(CH.sub.2).sub.n --(Ar)wherein n is an integer 0, 1, 2 or 3; and Ar is phenyl or napthyl unsubstituted or substituted with one to three substituents selected from the group consisting of hydroxy, methoxy, ethoxy, chloro, fluoro or C.sub.1 -C.sub.6 alkyl.
    Type: Grant
    Filed: May 12, 1997
    Date of Patent: October 5, 1999
    Assignee: Hoechst Marion Roussel, Inc.
    Inventors: Simon J. T. Mao, Mark T. Yates, Roger A. Parker
  • Tricyclic compounds
    Patent number: 5959146
    Abstract: Novel tricyclic compounds of formula I as defined in the specification, a process for their preparation and their use for the preparation of optically active or racemic colchicine and thiocolchicine derivatives.
    Type: Grant
    Filed: December 13, 1996
    Date of Patent: September 28, 1999
    Assignee: Hoechst Marion Roussel
    Inventors: Francis Brion, Bernadette Chappert, Christian Diolez, Christian Marie, Alain Mazurie, Michel Middendorp, Didier Pronine, Edmond Toromanoff
  • Process for preparing 6-0-monoesters of castanospermine
    Patent number: 5959111
    Abstract: The present invention relates to a process for preparing a compound of formula (I): ##STR1## wherein R is C.sub.1 -C.sub.10 alkyl, phenyl or substituted phenyl, comprising treating a compound of formula (II): ##STR2## with bis(tributyltin) oxide in an organic solvent selected from the group consisting of o-xylene, m-xylene, p-xylene and mixed xylenes;and subsequently treating the reaction mixture with a compound of formula (III): ##STR3## wherein X is halogen and R is defined as above.
    Type: Grant
    Filed: May 14, 1998
    Date of Patent: September 28, 1999
    Assignee: Hoechst Marion Roussel, Inc.
    Inventors: Christian T. Goralski, Sandra K Stolz-Dunn, James E. Hitt, David H. Louks, Brian D. Scherzer, Mark A. Nitz
  • Imidazolidines substituted with a heterocycle
    Patent number: 5958936
    Abstract: Novel imidazoles of the formula ##STR1## wherein the substituents are as defined in the disclosure and their non-toxic, pharmaceutically acceptable addition salts with acids and bases having antiandrogenic activity.
    Type: Grant
    Filed: September 23, 1997
    Date of Patent: September 28, 1999
    Assignee: Hoechst Marion Roussel
    Inventors: Andre Claussner, Francois Goubet, Jean-Georges Teutsch
  • Sulfonamide-substituted chromans, processes for their preparation, their use as a medicament or diagnostic, and pharmaceutical preparations comprising them
    Patent number: 5955607
    Abstract: Compounds of the formula I ##STR1## having the meanings of the substituents indicated in the claims are outstandingly efficacious substances for producing medicaments for the prophylaxis and for the therapy of cardiovascular disorders, in particular arrhythmias, for the treatment of ulcers of the gastrointestinal region or for the treatment of diarrheal disorders.
    Type: Grant
    Filed: September 25, 1998
    Date of Patent: September 21, 1999
    Assignee: Hoechst Marion Roussel Deutschland
    Inventors: Joachim Brendel, Uwe Gerlach, Hans Jochen Lang, Klaus Weidmann
  • Use of non-peptide bradykinin antagonists for the treatment or prevention of Alzheimer's disease
    Patent number: 5952346
    Abstract: The invention relates to the use of non-peptide bradykinin antagonists for the production of pharmaceuticals for the prevention and treatment of Alzheimer's disease. Suitable Compounds are non-peptide bradykinin antagonists which inhibit the actions of the Alzheimer's protein amyloid (.beta./A4) in isolated endothelial cells, such as for example, fused heterobicyclic fluoroalkyl derivatives.
    Type: Grant
    Filed: October 14, 1997
    Date of Patent: September 14, 1999
    Assignee: Hoechst Marion Roussel Deutschland GmbH
    Inventors: Holger Heitsch, Klaus Wirth, Gabriele Wiemer
  • Pyridiniminyl-1,2-benzisoxazoles and -benzisothiazoles
    Patent number: 5948798
    Abstract: Novel pyridiniminyl-1,2-benzisoxazoles and -benzisothiazoles, intermediates and processes for the preparation thereof, and methods of relieving memory dysfunction and treating depression utilizing the 1,2-benzisoxazoles and -benzisothiazoles and intermediates, or compositions thereof are disclosed.
    Type: Grant
    Filed: October 30, 1997
    Date of Patent: September 7, 1999
    Assignee: Hoechst Marion Roussel, Inc.
    Inventors: David M. Fink, Barbara E. Kurys, Gregory M. Shutske, John D. Tomer, IV
  • Acylated enol derivatives of .alpha.-ketoesters and .alpha.-ketoamides
    Patent number: 5948886
    Abstract: This invention relates to acylated enol derivatives of .alpha.-ketoesters and .alpha.-ketoamides. The compounds of this invention are either prodrugs of known elastase inhibitors or are elastase inhibitors in their own right and are useful in the treatment of various inflammatory diseases, including cystic fibrosis and emphysema.
    Type: Grant
    Filed: November 25, 1997
    Date of Patent: September 7, 1999
    Assignee: Hoechst Marion Roussel, Inc.
    Inventors: Norton P. Peet, Joseph P. Burkhart, Shujaath Mehdi
  • 17,20-epoxy steroid intermediates
    Patent number: 5945530
    Abstract: A compound of the formula ##STR1## wherein the A.sub.1 and B.sub.1 rings are as defined by the specification. The compounds are intermediates in the preparation of oxoetiocholenic acid.
    Type: Grant
    Filed: November 5, 1997
    Date of Patent: August 31, 1999
    Assignee: Hoechst Marion Roussel
    Inventors: Patrick Roussel, Michel Vivat
  • Pesticidal paste compositions
    Patent number: 5945113
    Abstract: A readily, water-dispersible pesticide formulation in the form of a thick paste containing 1 to 80% by weight of the pesticide, 0.30 to 2.0% by weight of a micropore-generating agent and 30 to 50% by weight of effervescent agents the percentages being based on the total weight of the formulation.
    Type: Grant
    Filed: September 26, 1996
    Date of Patent: August 31, 1999
    Assignee: Hoechst Marion Roussel
    Inventors: Colette Meinard, Jean-Claude Suglia
  • Acid pyrazole derivatives, preparation method therefor, use thereof as drugs, novel use therefor, and pharmaceutical compositions containing such derivatives
    Patent number: 5942622
    Abstract: The subject of the invention is the products of formula (I): in which one of A and B represents a nitrogen atom and the other one of A and B represents a methine radical, such that:A represents either nitrogen substituted in particular by alkyl,or methine substituted in particular by phenyl, thienyl or pyridyl,B represents either nitrogen substituted in particular by cyclohexylalkyl,or methine substituted in particular by alkylthio,R.sub.1 represents in particular carboxy,R represents in particular halogen,as well as the isomers and salts of said products of formula(I).
    Type: Grant
    Filed: April 22, 1998
    Date of Patent: August 24, 1999
    Assignee: Hoechst Marion Roussel
    Inventors: Stanislas Didierlaurent, Michel Fortin, Jidong Zhang
  • Substituted N-methyl-N-(4-(4-(1H-benzimidazol-2-yl) {1,4}diazepan-1-yl)-2-(aryl) butyl) benzamides useful for the treatment of allergic diseases
    Patent number: 5932571
    Abstract: The present invention relates to novel N-methyl-N-(4-(4-(1H-benzimidazol-2-yl)?1,4!diazepan-1-yl)-2-(aryl)butyl)b enzamide derivatives of the formula: ##STR1## stereoisomers thereof, and pharmaceutically acceptable salts thereof which are useful as histamine receptor antagonists and tachykinin receptor antagonists. Such antagonists are useful in the treatment of allergic rhinitis, including seasonal rhinitis and sinusitis; inflammatory bowel diseases, including Crohn's disease and ulcerative colitis; asthma; bronchitis; and emesis.
    Type: Grant
    Filed: March 6, 1998
    Date of Patent: August 3, 1999
    Assignee: Hoechst Marion Roussel, Inc.
    Inventors: George D. Maynard, John M. Kane, Christopher R. Dalton, Braulio Santiago, Elizabeth M. Kudlacz, Larry D. Bratton
  • Imidazole-5-carboxylic acid compounds
    Patent number: 5932741
    Abstract: The invention relates to the use and the products of formula (I): ##STR1## in which: R.sub.1 =represents hydroxyl, alkyl, alkenyl, alkynyl, alkoxy, alkylthio, formyl, cycloalkyl, optionally interrupted by heteroatoms,R.sub.2, R.sub.3 represent in particular halogen, mercapto, acyl, carboxy, nitro, cyano, amino, carbamoyl, R.sub.4, --OR.sub.4 with R.sub.4 representing in particular hydrogen, alkyl, alkenyl, alkynyl, acyl, amino, --(CH.sub.2).sub.m1 --S(o).sub.m2 --X--R.sub.10 with m1=0 to 4, m2=0 to 2, X represents a single bond or --NH--, --NH--CO--, --NH--CO--NH--, and R.sub.10 represents alkyl, alkenyl or aryl,and Y represents optionally substituted aryl,these products being in all the isomer forms and the salts, as medicaments.
    Type: Grant
    Filed: June 29, 1998
    Date of Patent: August 3, 1999
    Assignee: Hoechst Marion Roussel
    Inventors: Bertrand Heckmann, Jean-Paul Vevert, Jidong Zhang
  • Pharmaceutical composition for piperidinoalkanol compounds
    Patent number: 5932247
    Abstract: The invention provides a pharmaceutical composition in solid unit dosage form, comprising, a) a therapeutically effective amount of a piperidinoalkanol compound or a pharmaceutically acceptable salt thereof; and, b) at least one inert ingredient.
    Type: Grant
    Filed: October 9, 1997
    Date of Patent: August 3, 1999
    Assignee: Hoechst Marion Roussel, Inc.
    Inventors: Thomas T. Ortyl, Paul F. Skultety, Kristen C. Mitchell, Deepak S. Phadke, Faraneh Attarchi, Marguerite L. Pierce, Aaron W. Schoeneman, Joseph M. Schnitz
  • Trans cyclopentanyl azaadenyl analogs useful as immunosuppressants
    Patent number: 5929079
    Abstract: This invention relates to Trans cyclopentanyl purine analogs of the formula (1) ##STR1## wherein the substituent in the 3-position on the cyclopentanyl ring is in the Trans configuration relative to the bicyclic substituent,Y.sub.3, Y.sub.5, Y.sub.7, Y.sub.8 and Y.sub.9 are each nitrogen,R is a hydrogen, a C.sub.1 -C.sub.7 alkyl acyl or aryl acyl,Q is NH.sub.2, halogen or hydrogen,Z is hydrogen, halogen, or NH.sub.2 ;or a pharmaceutically-acceptable salt thereof, and to their use as immunosuppressants.
    Type: Grant
    Filed: November 20, 1997
    Date of Patent: July 27, 1999
    Assignee: Hoechst Marion Roussel, Inc.
    Inventors: David R. Borcherding, Carl K. Edwards, III, Ronald E. Esser, Douglas L. Cole
  • Substituted 3-(aminoalkylamino)-1, 2-benzisoxazoles and related compounds
    Patent number: 5925766
    Abstract: This application relates to compounds of the formula ##STR1## wherein R.sup.1, X, Y and n are as defined in the specification; and pharmaceutically acceptable addition salts thereof and optical and geometric isomers or racemic mixtures thereof; which compounds are useful or the treatment of various memory dysfunctions characterized by a decreased cholinergic function such as Alzheimer's disease. Compounds of this invention also inhibit monoamine oxidase and hence are useful as antidepressants.
    Type: Grant
    Filed: March 18, 1997
    Date of Patent: July 20, 1999
    Assignee: Hoechst Marion Roussel, Inc.
    Inventors: Gerard J. O'Malley, Mark G. Palermo
  • Substituted N-methyl-N-(4-(4-(1H-Benzimidazol-2-YL-amino) piperidin-1-YL)-2-(arlyl) butyl) benzamides useful for the treatment of allergic diseases
    Patent number: 5922737
    Abstract: The present invention relates to novel substituted N-methyl-N-(4-(4-(1H-benzimidazol-2-yl-amino)piperidin-1-yl)-2-(aryl)butyl )benzamide derivatives of the formula: ##STR1## stereoisomers thereof, and pharmaceutically acceptable salts thereof which are useful as histamine receptor antagonists and tachykinin receptor antagonists. Such antagonists are useful in the treatment of allergic rhinitis, including seasonal rhinitis and sinusitis; inflammatory bowel diseases, including Crohn's disease and ulcerative colitis; asthma; bronchitis; and emesis.
    Type: Grant
    Filed: January 6, 1997
    Date of Patent: July 13, 1999
    Assignee: Hoechst Marion Roussel, Inc.
    Inventors: George Daniel Maynard, John Michael Kane, Braulio Santiago, Elizabeth Mary Kudlacz, Larry Don Bratton, Christopher Robin Dalton
  • 4-heteroaryl-1-piperidinealkanols and derivatives thereof and their therapeutic utility
    Patent number: 5919798
    Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. The compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: July 6, 1999
    Assignee: Hoechst Marion Roussel, Inc.
    Inventors: Joseph T. Strupczewski, Grover C. Helsley, Edward J. Glamkowski, Yulin Chiang, Kenneth J. Bordeau, Peter A. Nemoto, John J. Tegeler
  • Method of determining the degree of aggregation of the .beta.-A4 peptide
    Patent number: 5919631
    Abstract: A method of determining the degree of aggregation of the .beta.A4 peptide is disclosed. The method comprises reacting the protein with a suitable binding agent which is capable of binding the .beta.A4 peptide only in its non-aggregated state to form an amount of protein bound binding reagent. The amount of protein bound binding agent is then measured.
    Type: Grant
    Filed: July 17, 1996
    Date of Patent: July 6, 1999
    Assignee: Hoechst Marion Roussel, Inc.
    Inventors: Shefali Goyal, Joseph W. Paul, Norbert G. Riedel, Sudhir R. Sahasrabudhe