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 general formula (I) and one or more compounds of general formula (I*) in which R, R1*, R2*, A1, Z1, Y, L, L1*, L2*, m, x and y are as defined in claim 1.
Abstract: Thienopyrimidines of the formula I
and their physiologically acceptable salts,
in which
R1, R2 and X have the meanings indicated in claim 1, exhibit phosphodiesterase V inhibition and can be employed for the treatment of disorders of the cardiovascular system and for the treatment and/or therapy of potency disorders.
Type:
Grant
Filed:
May 10, 2002
Date of Patent:
September 7, 2004
Assignee:
Merck Patent Gesellschaft mit beschränkter
Haftung
Inventors:
Rochus Jonas, Pierre Schelling, Franz-Werner Kluxen, Maria Christadler
Abstract: An adenoviral vector is described which carries a codon-optimized gag gene, along with a heterologous promoter and transcription terminator. This viral vaccine can effectively prevent HIV infection when administered to humans either alone or as part of a prime and boost regime also with a vaccine plasmid.
Type:
Grant
Filed:
March 27, 2001
Date of Patent:
September 7, 2004
Assignee:
Merck & Co., Inc.
Inventors:
Ling Chen, John W. Shiver, Andrew J. Bett, Danilo R. Casimiro, Michael J. Caulfield, Michael A. Chastain, Emilio A. Emini
Abstract: The invention relates to a process for the preparation of compounds having at least one —CF2O— bridge in the molecule, which comprises initially reacting a bis(alkylthio)carbenium salt with a compound containing at least one hydroxyl group in the presence of a base followed by oxidative fluorination, preferably in situ, with a fluorinating agent and an oxidizing agent to form the compound having at least one —CF2O— bridge in the molecule.
Type:
Grant
Filed:
September 3, 2002
Date of Patent:
September 7, 2004
Assignee:
Merck Patent GmbH
Inventors:
Peer Kirsch, Andreas Taugerbeck, Detlef Pauluth, Matthias Bremer
Abstract: Process for the production of hydrophobic layers on optical substrates which have an alkaline earth metal fluoride or alkali metal fluoride layer as the outermost layer or consist of alkaline earth metal fluorides or alkali metal fluorides, by thermal vapor deposition with polyfluorohydrocarbons in a high vacuum.
Type:
Grant
Filed:
November 14, 2001
Date of Patent:
August 31, 2004
Assignee:
Merck Patent GmbH
Inventors:
Uwe Anthes, Reiner Dombrowski, Martin Friz
Abstract: To provide a high-chromatic flaky pigment with good colorability, and to provide a method for producing the flaky pigment in a simple and inexpensive plant. A high-chromatic flaky pigment of which the entire surface of the flaky substrate coated with a metal oxide having an interference color is further coated with a semi-transparent thin metal film to enhance the interference color of the pigment.
Abstract: The present invention relates to compounds and derivatives thereof, their synthesis, and their use as integrin receptor antagonists. More particularly, the compounds of the present invention are antagonists of the integrin receptors &agr;v&bgr;3, &agr;v&bgr;5, and/or &agr;v&bgr;6 and are useful for inhibiting bone resorption, treating and preventing osteoporosis, and inhibiting vascular restenosis, diabetic retinopathy, macular degeneration, angiogenesis, atherosclerosis, inflammation, wound healing, viral disease, tumor growth, and metastasis.
Type:
Grant
Filed:
July 27, 2001
Date of Patent:
August 31, 2004
Assignee:
Merck & Co., Inc.
Inventors:
Ben C. Askew, Paul J. Coleman, Mark E. Duggan, Wasyl Halczenko, George D. Hartman, Cecilia A. Hunt, John H. Hutchinson, Robert S. Meissner, Michael A. Patane, Garry R. Smith, Jiabing Wang
Abstract: The present invention relates to a liquid crystal electro-optical switching member that comprises at least one polariser and a liquid crystal layer having an initial orientation in which the liquid crystal molecules are oriented so as to be essentially parallel to the substrates and to each other. The change of orientation of the liquid crystals, from their initial orientation that is substantially parallel to the substrates, is induced by a corresponding electric field which is oriented so as to be practically parallel to the substrates in the case liquid crystal with a negative dielectric anisotropy and so as to be practically perpendicular to the substrates in the case liquid crystal with a positive dielectric anisotropy. The liquid crystal layer has an optical delay [(d&Dgr;n) LC?] of between 0.06 and 0.43 &mgr;m. The present invention also relates to a liquid crystal display system that comprises said liquid crystal switching members.
Type:
Grant
Filed:
January 22, 2002
Date of Patent:
August 24, 2004
Assignee:
Merck Patent GmbH
Inventors:
Michael Heckmeier, Brigitte Schuler, Achim Götz, Herbert Plach
Abstract: The invention relates to liquid-crystalline compounds of the formula I
in which
R1, R2, A1, A2, A3, A4, Z1, Z2, a, b and c are as defined in claim 1, and to liquid-crystalline media comprising at least compound of the formula I and to electro-optical displays containing a liquid-crystalline medium of this type.
Type:
Grant
Filed:
June 12, 2003
Date of Patent:
August 24, 2004
Assignee:
Merck Patent GmbH
Inventors:
Peer Kirsch, Detlef Pauluth, Joachim Krause, Michael Heckmeier, Georg Lüssem, Dagmar Klement
Abstract: Thienopyrimidines of the formula (I) and their physiologically acceptable salts, in which R1, R2 and X are as defined in claim 1, exhibit phosphodiesterase V inhibition and can be employed for the treatment of illnesses of the cardiovascular system and for the treatment and/or therapy of impotence.
Type:
Grant
Filed:
March 3, 2003
Date of Patent:
August 24, 2004
Assignee:
Merck Patent GmbH
Inventors:
Rochus Jonas, Hans-Michael Eggenweiler, Pierre Schelling, Maria Christadler, Norbert Beier
Abstract: The present invention relates to multilayer pigments based on platelet-shaped metal substrates coated with two or more metal oxide layers by a one-pot process in an exclusively aqueous medium. The invention further relates to the use of the multilayer pigments in paints, varnishes, printing inks, including security printing inks, plastics, ceramic materials and cosmetic and for the laser formulations marking of plastics.
Type:
Grant
Filed:
June 4, 2003
Date of Patent:
August 17, 2004
Assignee:
Merck Patent Gesellschaft MIT Beschrankter Haftung
Inventors:
Stephanie Andes, Sabine George, Margarete Herbski, Peter Reynders, Reiner Vogt, Johann Dietz, Helge Kniess, Elke Steudel
Abstract: The invention encompasses the novel class of compounds represented by formula I, which are inhibitors of the PTP-1B enzyme.
The invention also encompasses pharmaceutical compositions and methods of treating or preventing PTP-1B mediated diseases, including diabetes, obesity, and diabetes-related diseases.
Type:
Grant
Filed:
June 28, 2002
Date of Patent:
August 17, 2004
Assignee:
Merck Frosst Canada & Co.
Inventors:
Yves Leblanc, Claude Dufresne, Jacques Yves Gauthier, Robert Young
Abstract: The present invention provides nucleoside compounds and certain derivatives thereof which are inhibitors of RNA-dependent RNA viral polymerase. These compounds are inhibitors of RNA-dependent RNA viral replication and are useful for the treatment of RNA-dependent RNA viral infection. They are particularly useful as inhibitors of hepatitis C virus (HCV) NS5B polymerase, as inhibitors of HCV replication, and/or for the treatment of hepatitis C infection. The invention also describes pharmaceutical compositions containing such nucleoside compounds alone or in combination with other agents active against RNA-dependent RNA viral infection, in particular HCV infection. Also disclosed are methods of inhibiting RNA-dependent RNA polymerase, inhibiting RNA-dependent RNA viral replication, and/or treating RNA-dependent RNA viral infection with the nucleoside compounds of the present invention.
Type:
Grant
Filed:
January 18, 2002
Date of Patent:
August 17, 2004
Assignees:
Merck & Co., Inc., Isis Pharmaceuticals, Inc.
Inventors:
Balkrishen Bhat, Neelima Bhat, Anne B. Eldrup, Thazha P. Prakash, Marija Prhavc, Quanlai Song, Phillip Dan Cook, Steven S. Carroll, Malcolm Maccoss, David B. Olsen
Abstract: Pyrazolo[4,3-d]pyrimidines of the formula I
and their physiologically acceptable salts,
in which
R1, R2, R3, R4 and X have the meanings indicated in Claim 1, exhibit phosphodiesterase V inhibition and can be employed for the treatment of disorders of the cardiovascular system and for the treatment and/or therapy of potency disorders.
Type:
Grant
Filed:
July 29, 2002
Date of Patent:
August 17, 2004
Assignee:
Merck Patent GmbH
Inventors:
Rochus Jonas, Hans-Michael Eggenweiler, Pierre Schelling, Maria Christadler, Norbert Beier
Abstract: A class of phenylsulphonyl derivatives wherein the sulphonyl moiety is also attached to an N-arylalkyl-substituted azetidine, pyrrolidine or piperidine ring are selective antagonists of the human 5-HT2A receptor and are therefore useful as pharmaceutical agents, especially in the treatment and/or prevention of adverse conditions of the central nervous system, including schizophrenia and depression.
Type:
Grant
Filed:
April 1, 2003
Date of Patent:
August 17, 2004
Assignee:
Merck Sharp & Dohme Ltd.
Inventors:
Peter Blurton, Frank Burkamp, Susan Koon-Fung Cheng, Stephen Robert Fletcher, Angus Murray MacLeod, Daniel Spinks, Monique Bodil Van Niel
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.
Abstract: The present invention relates to pigment mixtures consisting of at least two components, component A being SiO2 flakes coated with one or more metal oxides and/or metals and component B being special-effect pigments, and to their use in varnishes, paints, printing inks, masterbatches, plastics and cosmetic formulations.
Type:
Grant
Filed:
March 24, 2003
Date of Patent:
August 10, 2004
Assignee:
Merck Patent GmbH
Inventors:
Sabine Schoen, Reiner Vogt, Norbert Schül, Karl Osterried, Johann Munz
Abstract: A naturally occurring protein isolated from the saliva of the medicinal leech Hirudo medicinalis is described which strongly binds to collagen thus acting as an inhibitor of natural platelet adhesion to collagen. The protein has a molecular weight of about 12,000, an acidic isoelectric point and contains six cysteins. The protein was sequenced and the gene was cloned from a H. medicinalis cDNA-library. Procedures for producing such polypeptide by recombinant techniques are disclosed. The recombinant and the natural occurring proteins are potent inhibitors of collagen-dependent platelet adhesion and therefore useful for the therapeutic treatment of various conditions related to heart disease and diseases of the circulation system. Furthermore, the protein is useful for coating natural or artificial collagen surfaces in order to render them nonadhesive for cells and prevent the activation of cells.
Type:
Grant
Filed:
September 17, 2001
Date of Patent:
August 10, 2004
Assignee:
Merck Patent GmbH
Inventors:
Wolfgang Strittmatter, Detlef Güssow, Uwe Hofmann, Jürgen Hemberger, Zisi Fotev, Bernhard Scheuble
Abstract: In accordance with the present invention, there is provided a novel class of heterocyclic compounds. Compounds of the invention contain a substituted, unsaturated five, six or seven membered heterocyclic ring that includes at least one nitrogen atom and at least one carbon atom. The ring additionally includes three, four or five atoms independently selected from carbon, nitrogen, sulfur and oxygen atoms. The heterocyclic ring has at least one substituent located at a ring position adjacent to a ring nitrogen atom. This mandatory substituent of the ring includes a moiety (B), linked to the heterocyclic ring via a carbon-carbon double bond, a carbon-carbon triple bond or an azo group. The mandatory substituent is positioned adjacent to the ring nitrogen atom. Invention compounds are capable of a wide variety of uses. For example heterocyclic compounds can act to modulate physiological processes by functioning as agonists and antagonists of receptors in the nervous system.
Type:
Grant
Filed:
August 13, 2002
Date of Patent:
August 10, 2004
Assignee:
Merck & Co., Inc.
Inventors:
Nicholas David Peter Cosford, Leo Solomon Bleicher, Jean-Michel Andre Vernier, Rowena V. Cube, Edwin Schweiger, Ian McDonald