Patents Represented by Attorney, Agent or Law Firm John P. Parise
  • Patent number: 5891900
    Abstract: Compounds of the formula ##STR1## wherein R.sup.1 is lower-alkyl, cycloalkyl or phenyl,R.sup.2 is H, OH or C(O)O--A, wherein A is lower-alkyl, cycloalkyl or phenyl, andR.sup.3,R.sup.4 and R.sup.5 are either methyl or R.sup.3 is H and R.sup.4 and R.sup.5 taken together are trimethyleneas well as hydrates or solvates and physiologically usable salts thereof can be used for the production of medicaments for the treatment or prophylaxis of illnesses which are caused by thrombin-induced platelet aggregation or fibrinogen clotting in blood plasma.
    Type: Grant
    Filed: July 8, 1997
    Date of Patent: April 6, 1999
    Assignee: Hoffman-La Roche Inc
    Inventors: Fran.cedilla.ois Diederich, Ulrike Obst, Lutz Weber
  • Patent number: 5883254
    Abstract: The present invention provides a process for the manufacture of pyrimidines of formula I: ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 each independently represent hydrogen, C.sub.1-7 -alkyl, or C.sub.1-7 -alkoxy,A signifies --CN,a carbanionic R.sup.4 -alkynyl residue, in which R.sup.4 is hydrogen or C.sub.1-7 -alkyl, ora carbanionic residue of the malonic acid derivative of formula III ##STR2## in which B and B' independently represent --CN, --COOR.sup.5, or --C(O)R.sup.5, wherein R.sup.5 is alkyl or aryl.
    Type: Grant
    Filed: October 16, 1997
    Date of Patent: March 16, 1999
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Wolfgang Gohring
  • Patent number: 5866583
    Abstract: Compounds of formula I ##STR1## wherein R.sup.1 is lower-alkoxy, R.sup.2 is bromine, lower-alkoxy or hydroxy, R.sup.3 is hydrogen, lower-alkyl, cycloalkyl, aryl, heterocyclyl, aralkyl, heterocyclyl-lower-alkyl or cyano, R.sup.4 and R.sup.5 each independently are hydrogen, lower-alkyl, lower-alkoxy, halogen, hydroxy, amino, di(lower alkyl)amino, cyano or nitro and Q is ethynylene or vinylene, or pharmaceutically usable salts thereof, the use of these compounds and their salts as therapeutically active substances; medicaments based on these substances and their production; the use of these substances as medicaments and for the production of antibacterially-active medicaments; as well as the manufacture of the compounds of formula I and their pharmaceutically acceptable salts and intermediates for their manufacture.
    Type: Grant
    Filed: April 24, 1997
    Date of Patent: February 2, 1999
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Philippe Guerry, Henri Stalder, Pierre-Charles Wyss
  • Patent number: 5856503
    Abstract: Aminoalkyl-substituted benzo-heterocyclic compounds of the formula ##STR1## wherein M, Q, R and T are as defined in the specification, as well as acid addition salts thereof. These compounds are useful as cholesterol level lowering agents and as antimycotic agents.
    Type: Grant
    Filed: December 6, 1996
    Date of Patent: January 5, 1999
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Johannes Aebi, Henrietta Dehmlow, Jacques Himber, Hans-Peter Marki, Hans Lengsfeld, Olivier Morand, Gerard Schmid, Yu-Hua Ji
  • Patent number: 5854238
    Abstract: 9-methyl-4-phenyl-6H-thieno?3,2-f!-s-triazolo?4,3-a!?1,4!diazepine for the treatment and prevention of illnesses which are caused by low plasma apolipoprotein A-I levels as coronary coronary disease.
    Type: Grant
    Filed: February 23, 1998
    Date of Patent: December 29, 1998
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Herman Kempen
  • Patent number: 5848990
    Abstract: A device for introducing an active substance solution into a patient and with means for fastening to the skin and a cannula. The cannula is held in a withdrawn position by a retaining and releasing mechanism before use and, after release, is propelled into the patient's skin. A connector connected to the rear of the cannula serves to connect the cannula to an active substance reservoir.
    Type: Grant
    Filed: August 14, 1997
    Date of Patent: December 15, 1998
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Giorgio Cirelli, Benno Rothenhausler, Hans Steffen
  • Patent number: 5847144
    Abstract: A process for the manufacture of the .alpha.,.alpha.'-diaminoalcohol of formula ##STR1## is via N-protected L-phenylalanine lower alkyl esters, corresponding N-protected .alpha.-amino-.alpha.'-haloketones, and .alpha.-amino-.alpha.'-haloalcohols.
    Type: Grant
    Filed: July 25, 1997
    Date of Patent: December 8, 1998
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Hans Hilpert
  • Patent number: 5837708
    Abstract: Compounds of the formula ##STR1## wherein the variables are hereinbelow defined. The compounds of formula I are inhibitors for endothelin receptors. They can be used for the treatment of disorders which are associated with endothelin activities, especially circulatory disorders such as hypertension, ischaemia, vasospasms and angina pectoris.
    Type: Grant
    Filed: October 15, 1996
    Date of Patent: November 17, 1998
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Volker Breu, Kaspar Burri, Jean-Marie Cassal, Martine Clozel, Georges Hirth, Bernd-Michael Loffler, Marcel Muller, Werner Neidhart, Henri Ramuz
  • Patent number: 5817838
    Abstract: A process for the manufacture of 4,4-disubstituted 5-methylene-1,3-dioxolan-2-ones ("cyclocarbonates") of the formula: ##STR1## wherein R.sup.1 and R.sup.2 each independently signify a saturated or olefinically-unsaturated aliphatic group or an aromatic group, or R.sup.1 and R.sup.2 together form tetra- or pentamethylene, by reacting a corresponding 3,3-disubstituted prop-1-yn-3-ol of the formula HC.tbd.C--C(R.sup.1)(R.sup.2)--OH (II) with carbon dioxide in the presence of a quaternary ammonium or phosphonium salt as the catalyst comprises using a silver salt as a further catalyst. An alkali metal or quaternary ammonium or phosphonium salt of a carboxylic acid can also be used to increase the catalytic performance of the silver salt catalyst. Moreover, the addition of triphenylphosphine serves to accelerate the reaction to some extent. The silver salts catalyze this process significantly better than the previously utilized copper salts.
    Type: Grant
    Filed: October 8, 1997
    Date of Patent: October 6, 1998
    Assignee: Roche Vitamins Inc.
    Inventors: Hansjorg Grundler, Hans-Jurgen Hansen
  • Patent number: 5814613
    Abstract: The invention provides an antibiotic designated LL-E19020 Gamma which is derived from the microorganism Streptomyces lydicus ssp. tanzanius NRRL 18036.
    Type: Grant
    Filed: September 9, 1991
    Date of Patent: September 29, 1998
    Assignee: Roche Vitamins Inc.
    Inventors: Guy Thomas Carter, David R. Williams, Joseph D. Korshalla
  • Patent number: 5814615
    Abstract: The invention provides an antibiotic designated LL-E19020 Alpha.sub.1 which is derived from the micro-organism Streptomyces lydicus ssp. tanzanius NRRL 18036.
    Type: Grant
    Filed: September 9, 1991
    Date of Patent: September 29, 1998
    Assignee: Roche Vitamins Inc.
    Inventors: Guy Thomas Carter, David R. Williams, Joseph D. Korshalla
  • Patent number: 5808029
    Abstract: The present invention is concerned with non-soluble proteins and soluble or insoluble fragments thereof, which bind TNF, in homogeneous form, as well as their physiologically compatible salts, especially those proteins having a molecular weight of about 55 or 75 kD (non-reducing SDS-PAGE conditions), a process for the isolation of such proteins, antibodies against such proteins, DNA sequences which code for non-soluble proteins and soluble or non-soluble fragments thereof, which bind TNF, as well as those which code for proteins comprising partly of a soluble fragment, which binds TNF, and partly of all domains except the first of the constant region of the heavy chain of human immunoglobulins and the recombinant proteins coded thereby as well as a process for their manufacture using transformed pro- and eukaryotic host cells.
    Type: Grant
    Filed: May 19, 1995
    Date of Patent: September 15, 1998
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Manfred Brockhaus, Zlatko Dembic, Reiner Gentz, Werner Lesslauer, Hansruedi Lotscher, Ernst-Jurgen Schlaeger
  • Patent number: 5795547
    Abstract: An apparatus for automatic performance of temperature cycles in a number of test tubes in which each test tube is closed by a closure and contains a predetermined volume of a liquid reaction mixture. The apparatus includes a holder, a computer-controlled automatic control system, and a device for cyclic alteration of the holder temperature. The holder has an arrangement of chambers for holding test tubes with each chamber being adapted to receive one test tube. The holder is constructed of a material of high thermal conductivity, and has an upper surface, a bottom surface and a cylindrical outer wall. Each chamber has an opening located in the upper surface of the holder. The device for cyclic alteration of the temperature of the holder is actuated by the automatic control system. By reducing the dimensions of the device and the power required to operate it, numerous advantages are realized.
    Type: Grant
    Filed: October 23, 1996
    Date of Patent: August 18, 1998
    Assignee: Roche Diagnostic Systems, Inc.
    Inventors: Rolf Moser, Lukas Birrer
  • Patent number: 5777141
    Abstract: A process for the recovery of unsaturated fatty acids with at least 16 carbon atoms in the molecule or a derivative of such a fatty acid from a mixture of fatty acids and/or fatty acid derivatives by column chromatography with supercritical or liquid carbon dioxide as the mobile phase comprises using aluminum oxide, optionally pretreated with alkali, as the stationary phase. The pre-treatment of the aluminum oxide is conveniently effected by contacting the particulate aluminum oxide with an aqueous solution of an alkali metal or alkaline earth metal hydroxide, optionally supplemented with a water-miscible or water-soluble organic solvent, in the pH range of about 10 to about 13 over several hours. The unsaturated fatty acids or fatty acid derivatives produced chromatographically in this manner are suitable as valuable active agents in the fields of nutrition and medicine.
    Type: Grant
    Filed: August 16, 1996
    Date of Patent: July 7, 1998
    Assignee: Roche Vitamins Inc.
    Inventors: Gerd Brunner, Frank Reichmann
  • Patent number: 5770458
    Abstract: Binding assays are effected by introducing a specific binding reagent through a top absorbant membrane in parallel contact with a main absorbant membrane. By providing a parallel flow of liquid in the two membranes, and by controlling the flow of the diluted reagent from the top absorbant membrane into the main absorbant membrane, a controlled, uniform dilution of the reagent is obtained, leading to more accurate assay results.
    Type: Grant
    Filed: June 17, 1997
    Date of Patent: June 23, 1998
    Assignee: Roche Diagnostics Systems, Inc.
    Inventors: Alexei Dmitri Klimov, Shiow-Chuan Jane Tsai
  • Patent number: 5767268
    Abstract: Compounds of formulas ##STR1## wherein, B is lower alkylene or an optionally substituted aromatic ring system;G.sup.1, G.sup.2 and G.sup.3 each independently signify a residue of a glycopyranoside, a glycopyranose or a derivative thereof, with at least one hydroxy group of residue G.sup.1, G.sup.2 or G.sup.3 being esterified with sulfuric acid, and pharmaceutically usable salts thereof, are useful for the treatment of disorders which are characterized by excessive or destructive proliferation of smooth muscle cells.
    Type: Grant
    Filed: April 26, 1996
    Date of Patent: June 16, 1998
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Alexander Chucholowski, Jurgen Fingerle, Niggi Iberg, Hans Peter Marki, Rita Muller, Michael Pech, Marianne Rouge, Gerard Schmid, Thomas Tschopp, Hans Peter Wessel
  • Patent number: 5763651
    Abstract: A process for the manufacture of polyene esters or polyene acids comprises reacting a polyene O,O-dialkylacetal of di(O,O-dialkylacetal) with a vinylketene acetal or analogue thereof in the presence of a Lewis acid, hydrolyzing the reaction mixture depending on the vinylketene acetal used, subsequently cleaving alcohol under strongly basic conditions from the polyene derivative produced at this stage and, where the desired ester or carboxy group is still not present, performing the respective conversion. Certain intermediates in this process form a further aspect of the invention. The final products are primarily carotenoids which can be used appropriately, e.g. as colorants and pigments for foodstuffs, animal products etc.
    Type: Grant
    Filed: May 29, 1997
    Date of Patent: June 9, 1998
    Assignee: Roche Vitamins Inc.
    Inventor: August Ruttimann
  • Patent number: 5762872
    Abstract: The analytical device comprises a conveyor for conveying cuvettes to one or more stations for processing samples for analysis in the cuvettes. The processing stations comprise means for removing individual cuvettes from the conveyor, transferring the cuvettes to a processing position and returning the cuvettes to the conveyor after processing.
    Type: Grant
    Filed: July 23, 1997
    Date of Patent: June 9, 1998
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Jurg Buhler, Andreas Greter
  • Patent number: 5762923
    Abstract: An aqueous interferon composition which comprises an amount of interferon-alpha dissolved in water with a non-ionic detergent and benzyl alcohol in amounts sufficient to stabilize the amount of interferon-alpha, which composition contains an amount of acidic buffer which provides a pH of 4.5 to 6.0, and may also contain an isotonizing agent.
    Type: Grant
    Filed: April 4, 1996
    Date of Patent: June 9, 1998
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Gunter Gross, Sabino Del Terzo, Saran Kandakuri Kumar
  • Patent number: 5763436
    Abstract: Compounds of the formula ##STR1## wherein L, M, R, T and X are set forth in the description, as well as hydrates or solvates thereof, which inhibit thrombin-induced platelet aggregation and clotting of fibrinogen in plasma, are described. The compounds of formula I are prepared by amidination or, depending on whether L is NH or O, by amide formation or esterification.
    Type: Grant
    Filed: September 17, 1996
    Date of Patent: June 9, 1998
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Jean Ackermann, David Banner, Klaus Gubernator, Paul Hadvary, Kurt Hilpert, Klaus Muller, Ludvik Labler, Gerard Schmid, Thomas B. Tschopp, Hans Peter Wessel, Beat Wirz