Patents Assigned to Merck
  • Process for preparing 3-hydroxymethyl-4-(aryl or heterocyclic)-cyclopentanones
    Patent number: 6506908
    Abstract: Processes are disclosed for preparing 3-hydroxymethylcyclopentanone compounds, which are useful as intermediates in the preparation of HIV chemokine CCR-5 receptor antagonists. A process is described in which the compounds are prepared by opening the cyclopropyl ring of a (1-alkoxycarbonyl-2-oxo)-trans-bicyclo[3.1.0]hexane compound by addition of a nucleophile to the cyclopropyl ring, and then decarboxylating the resulting 2-alkoxycarbonyl-3-(Nu-methyl)-cyclopentanone (Nu=the added nucleophilic group) via base solvolysis. Also described is a process for preparing the bicyclo[3.1.0]hexane precursors by the catalyzed cyclopropanation of a suitable alpha-diazo-beta-ketoester. The preparation of the alpha-diazo-beta-ketoesters and precursors thereto are also disclosed.
    Type: Grant
    Filed: April 20, 2001
    Date of Patent: January 14, 2003
    Assignee: Merck & Co., Inc.
    Inventors: Nobuyoshi Yasuda, Michael Palucki, Joann M. Um, David Alan Conlon, Barry M. Trost
  • Cyclopentyl modulators of chemokine receptor activity
    Patent number: 6506777
    Abstract: The present invention is directed to compounds of the formula I: (wherein R1, R2, R3, R4, R5, R7, R8, X, n, x and y are defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptors CCR-5 and/or CCR-3.
    Type: Grant
    Filed: June 8, 2000
    Date of Patent: January 14, 2003
    Assignee: Merck & Co., Inc.
    Inventors: Paul E. Finke, Jennifer L. Loebach, Malcolm Maccoss, Sander G. Mills
  • Liquid crystalline medium
    Patent number: 6506462
    Abstract: The invention relates to a liquid-crystalline medium based on a mixture of polar compounds having positive dielectric anisotropy, characterized in that it comprises one or more compounds of the general formula I in which R, Y and L1 are as defined therein.
    Type: Grant
    Filed: January 30, 1998
    Date of Patent: January 14, 2003
    Assignee: Merck Patent Gesellschaft mit Beschrankter Haftung
    Inventors: Kazuaki Tarumi, Brigitte Schuler, Michael Schwarz, Hideo Ichinose, Yasuyoshi Namiki, Akiko Takashima, Hiroshi Numata
  • Liquid-crystal compound, liquid-crystal medium comprising same, and electro-optical liquid- crystal display
    Publication number: 20030006399
    Abstract: The present invention relates to compounds containing a cyclobutanone group of the formula I 1
    Type: Application
    Filed: September 24, 2001
    Publication date: January 9, 2003
    Applicant: Merck Patent GmbH
    Inventors: Marcus Reuter, Michael Heckmeier, Volker Reiffenrath
  • Multilayered luster pigments
    Publication number: 20030005859
    Abstract: The invention relates to multilayered luster pigments based on metallic substrates, which are completely surrounded by a plurality of layers, where these layers comprise at least one layer pack (A) having a colorless dielectric layer of a material with a refractive index n of ≦1.8, and a colorless dielectric layer of a material with a refractive index n of >1.8, and a selectively or non-selectively absorbent layer (B), and to a process for their production, and to their use.
    Type: Application
    Filed: June 12, 2002
    Publication date: January 9, 2003
    Applicant: Merck Patent GmbH
    Inventors: Stephanie Andes, Gerald Fuchs-Pohl, Martin Friz, Gerhard Pfaff, Siegfried Raabe, Michael Uhlig
  • Multilayered systems having optical properties
    Publication number: 20030008120
    Abstract: Multilayered systems having optical properties based on metallic substrates comprise both a layer (A) of at least two dielectric materials of different refractive index, where the refractive index at the lower side and the refractive index at the upper side of layer (A) are different, and a selectively or non-selectively absorbent layer (B).
    Type: Application
    Filed: June 12, 2002
    Publication date: January 9, 2003
    Applicant: Merck Patent GmbH
    Inventors: Stephanie Andes, Gerald Fuchs-Pohl, Martin Friz, Ute Honeit, Gerhard Pfaff, Michael Uhlig
  • Catalytic titanium (IV) oxide, mediated geminal symmetric dialkylation of carboxamides
    Publication number: 20030009029
    Abstract: The present invention relates to a process preparing compounds of the general formula (I) 1
    Type: Application
    Filed: June 5, 2002
    Publication date: January 9, 2003
    Applicant: Merck Patent GmbH
    Inventors: Herwig Buchholz, Urs Welz-Biermann
  • Process for the synthesis of (R)-1-(3,5-bis(trifluoromethyl)-phenyl)ethan-1-ol by asymmetric transfer hydrogenation
    Patent number: 6504066
    Abstract: The present invention is concerned with novel processes for the preparation of (R)-1-(3,5-bis(trifluoromethyl)phenyl)ethan-1-ol. This compound is useful as an intermediate in the synthesis of compounds which possess pharmacological activity.
    Type: Grant
    Filed: June 30, 2000
    Date of Patent: January 7, 2003
    Assignee: Merck & Co. Inc.
    Inventors: Paul Devine, Hansen Karl
  • Decarboxylation process for synthesizing carbapenem antibiotics
    Patent number: 6504027
    Abstract: A process for the direct crystallization of a compound of the formula I: or a pharmaceutically acceptable salt thereof, is disclosed, wherein R1 and R2 represent H, C1-10 alkyl, aryl or heteroaryl, or substituted C1-10 alkyl, aryl or heteroaryl and X+ represents a charge balancing group, comprising extracting a solution containing a crude compound of formula I or Ia: or a pharmaceutically acceptable salt thereof, wherein each X+ is a charge balancing group, and R1 and R2 are as described above with a C4-10 alcohol, collecting and crystallizing the resulting aqueous phase to produce a crystalline compound of formula I.
    Type: Grant
    Filed: January 19, 2000
    Date of Patent: January 7, 2003
    Assignee: Merck & Co., Inc.
    Inventors: John M. Williams, Karel M. J. Brands, Renato T. Skerlj, Peter Houghton
  • Liquid-crystalline medium
    Publication number: 20030001137
    Abstract: A liquid-crystalline medium based on a mixture of polar compounds of positive dielectric anisotropy, characterized in that it comprises one or more compounds of the general formula IA and/or IB 1
    Type: Application
    Filed: October 11, 2001
    Publication date: January 2, 2003
    Applicant: Merck Patent Gesellschaft mit beschrankter Haftung
    Inventors: Michael Heckmeier, Matthias Bremer
  • Effer-vescent bisphosphonate formulation
    Publication number: 20030003147
    Abstract: An effervescent formulation of alendronate contains an acid source, a carbonate source, a binder, a lubricant and optionally, flavoring agents, colorants and sweeteners.
    Type: Application
    Filed: July 9, 2002
    Publication date: January 2, 2003
    Applicant: Merck & Co., Inc.
    Inventors: Ashok V. Katdare, Colin R. Gardner, Kenneth A. Kramer
  • Inhibitors of farnesyl-protein transferase
    Patent number: 6500841
    Abstract: The present invention is directed to compounds which inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting farnesyl-protein transferase and treatment of cancer.
    Type: Grant
    Filed: September 12, 1996
    Date of Patent: December 31, 2002
    Assignee: Merck & Co., Inc.
    Inventors: S. Jane deSolms, Samuel L. Graham
  • Sun-protection formulations active against herpes simplex viruses
    Patent number: 6500869
    Abstract: The invention relates to sun-protection formulations in solid or liquid form, containing organic and/or inorganic sunscreen filters having a prophylactic action against herpetic diseases of the skin, and to the use of said sun-screen formulations.
    Type: Grant
    Filed: September 12, 2000
    Date of Patent: December 31, 2002
    Assignee: Merck Patent Gesellschaft
    Inventors: Hansjürgen Driller, Sabine Hitzel
  • Method and apparatus for handling bulk bags
    Patent number: 6499584
    Abstract: There is disclosed an apparatus and method for evenly dispersing the contents of powder filled bulk bags, in order to create a flat, even, horizontal bulk bag surface for efficient attachment to the suction head of a vacuum lift.
    Type: Grant
    Filed: October 16, 2000
    Date of Patent: December 31, 2002
    Assignee: Merck & Co., Inc.
    Inventors: Wendy M. Keim, John E. DelGigante
  • Triazolo-pyridazine derivatives as ligands for gaba receptors
    Patent number: 6500828
    Abstract: 1,2,4-triazolo[4,3-b]pyridazine derivatives, possessing a difluoro-or tri-fluoro-substituted phenyl ring at the 3-position, a triazolyl moiety at the 6-position, and a tert-butyl group at the 7-position, are selective ligands for GABAA receptors, in particular having high affinity for the &agr;2 and/or &agr;3 subunit thereof, and are useful in the treatment of anxiety and convulsions.
    Type: Grant
    Filed: July 23, 2001
    Date of Patent: December 31, 2002
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: William Robert Carling, Jose Luis Castro Pineiro, Richard Thomas Lewis, Kevin William Moore, Leslie Joseph Street
  • Cyclopentyl modulators of chemokine receptor activity
    Patent number: 6500844
    Abstract: The present invention is directed to compounds of the formula I: (wherein R1, R2, R3, R7, R8, X, Y, Z, x and y are defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptors CCR-5 and/or CCR-3.
    Type: Grant
    Filed: June 8, 2000
    Date of Patent: December 31, 2002
    Assignee: Merck & Co., Inc.
    Inventors: Paul E. Finke, Kevin T. Chapman, Malcolm Maccoss, Sander G. Mills, Bryan Oates
  • Multi-coated interference pigments
    Patent number: 6500251
    Abstract: Multilayer interference pigment consisting of plateletlike titanium dioxide as carrier material, coated with alternating layers of metal oxides of low and high refractive index, the difference in the refractive indices being at least 0.1, which is obtainable by solidification and hydrolysis of an aqueous solution of a thermally hydrolyzable titanium compound on a continuous belt, detachment of the resulting coat, coating of the resulting titanium dioxide platelets, with or without drying in between, by a wet method with, alternately, a metal oxide hydrate of high refractive index and a metal oxide hydrate of low refractive index by hydrolysis of the corresponding, water-soluble metal compounds, separation, drying and, if desired, calcining of the material obtained.
    Type: Grant
    Filed: March 9, 1999
    Date of Patent: December 31, 2002
    Assignee: Merck Patent Gesellschaft mit beschrankter Haftung
    Inventors: Stephanie Andes, Gerd Bauer, Günter Brenner, Dieter Brückner, Michael Schmelz, Andrea Heyland, Matthias Kuntz, Karl Osterried, Gerhard Pfaff
  • Cyclopeptide derivatives
    Publication number: 20020198142
    Abstract: Compounds of the formula I
    Type: Application
    Filed: June 28, 2002
    Publication date: December 26, 2002
    Applicant: Merck Patent GmbH
    Inventors: Jorg Meyer, Alfred Jonczyk, Berthold Nies, Horst Kessler, Dirk Finsinger, Martin Kantlehner
  • Polymorphic, amorphous and hydrated forms of 5-chloro-3-(4-methanesulfonylphenyl)-6'-methyl-[2,3']bipyridinyl
    Publication number: 20020198238
    Abstract: Polymorphic, amorphous and hydrated forms of the title compound having the following structure: 1
    Type: Application
    Filed: June 26, 2002
    Publication date: December 26, 2002
    Applicant: Merck & Co., Inc.
    Inventor: Louis S. Crocker
  • Nematic liquid-crystal composition
    Patent number: 6497828
    Abstract: The invention relates to nematic liquid-crystal compositions comprising bisalkenyl compounds of the formula Ia. in which R1 and R2, are each independently alkenyl having 2 to 8 carbon atoms, and Z2 is a single bond, —(CH2)2— or trans-CH═CH—. and to their use in plasma-addressed LCDs.
    Type: Grant
    Filed: July 24, 2000
    Date of Patent: December 24, 2002
    Assignee: Merck Patent GmbH
    Inventors: Harald Hirschmann, Sven Schüpfer, Marcus Reuter