Patents Assigned to Merck
  • Pyrazolo-triazine derivatives as ligands for GABA receptors
    Patent number: 6476030
    Abstract: Compounds according to Formula (I): or a salt or prodrug thereof, have good affinity as ligands for the alpha2 and/or alpha3 subunit of the human GABAA receptor and are useful for treatment of disorders of the central nervous system, including anxiety and convulsions.
    Type: Grant
    Filed: June 8, 2001
    Date of Patent: November 5, 2002
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: William Robert Carling, Andrew Mitchinson, Kevin William Moore, Michael Geoffrey Russell, Gayle Scott, Leslie Joseph Street
  • Cyclic amine modulators of chemokine receptor activity
    Patent number: 6476054
    Abstract: The present invention is directed to cyclic amines of the formula I: (wherein R1, R2, R3, m and n 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-1, CCR-2, CCR-2A, CCR-2B, CCR-3, CCR-4, CCR-5, CXCR-3, and/or CXCR-4.
    Type: Grant
    Filed: October 17, 2000
    Date of Patent: November 5, 2002
    Assignee: Merck & Co., Inc.
    Inventors: Charles G. Caldwell, Paul E. Finke, Malcolm Maccoss, Sander G. Mills, Bryan Oates, Dooseop Kim, Shankaran Kothandaraman, Liping Wang
  • Azaindole derivatives and their use as therapeutic agents
    Patent number: 6476045
    Abstract: The present invention relates to compounds of the formula (I): wherein: Het represents a heterocyclic residue selected from: where the dotted line in (b) represents an optional double bond; A completes a fused pyridine ring; and B completes a fused benzene or pyridine ring. The compounds are of particular use in the treatment or prevention of depression, anxiety, pain, inflammation, migaine, emesis or postherpetic neuralgia.
    Type: Grant
    Filed: July 11, 2001
    Date of Patent: November 5, 2002
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Kevin Dinnell, Jason Matthew Elliott, Gregory John Hollingworth, Duncan Edward Shaw
  • Direactive mesogenic compounds and intermediates
    Patent number: 6475574
    Abstract: The present invention generally relates to a direactive compound which is of the formula IV A R1—(CH2)mO—MG—O—(CH2)n—R2  (IVA) wherein R1, R2, m, n, and MG are defined herein.
    Type: Grant
    Filed: May 22, 2000
    Date of Patent: November 5, 2002
    Assignee: Merck Patent Geselleschaft mit beschranhkter Haftung
    Inventors: David Coates, Simon Greenfield
  • 1,4 substituted piperidinyl NMDA/NR2B antagonists
    Patent number: 6476041
    Abstract: Novel piperidinyl compounds substituted in the 1- and 4-positions are effective as NMDA NR2B antagonists useful for relieving pain.
    Type: Grant
    Filed: October 25, 2000
    Date of Patent: November 5, 2002
    Assignee: Merck & Co., Inc.
    Inventors: Wayne Thompson, David A. Claremon, Peter M. Munson, Janusz Kulagowski, Willie Whitter, Ian Huscroft
  • Fluorocyclohexene derivatives, and liquid-crystalline medium
    Patent number: 6475595
    Abstract: Fluorocyclohexene derivatives of formula I R1—(A1—Z1)n—A—(Z2—A2)m—Z3—B—(Z4—A3)p—R2  I, in which n, m, p, R1, R2, Z1, Z2, Z3, Z4, A1, A2, A3, A and B are as defined herein, are suitable for use in liquid crystal mediums. Also, difluorocyclohexanes of formula III R3—A*—(Z6—A7)m—Z7—Qr—R7  III, where R3, A*, Z6, A7, m, Z7, Q, r, and R4 are as defined herein, are suitable for use in liquid crystal mediums.
    Type: Grant
    Filed: March 31, 2000
    Date of Patent: November 5, 2002
    Assignee: Merck GmbH
    Inventors: Matthias Bremer, Detlef Pauluth, Joachim Krause, Michael Heckmeier, Peer Kirsch
  • Borate salts for use in electrochemical cells
    Publication number: 20020160261
    Abstract: The invention relates to borate salts and to their use in electro-chemical cells.
    Type: Application
    Filed: January 24, 2002
    Publication date: October 31, 2002
    Applicant: Merck GmbH
    Inventors: Michael Schmidt, Andreas Kuhner, Klaus-Dieter Franz, Gerd-Volker Roschenthaler, German Bissky, Alexander Kolomeitsev, Alexander Kadyrov
  • Electrooptical liquid crystal system
    Publication number: 20020158227
    Abstract: The invention relativ to an electroptical system
    Type: Application
    Filed: March 18, 2002
    Publication date: October 31, 2002
    Applicant: Merck Patent GmbH
    Inventors: David Coates, Owain Parri, Simon Greenfield, Martin Tillin, Mark Goulding, Patrick Nolan
  • Pigment preparation
    Publication number: 20020157574
    Abstract: The present invention relates to a pigment preparation comprising BiOCl pigments, one or more luster pigments and spherical particles, and to the use thereof in printing inks, security printing inks, surface coatings, paints, plastics and in cosmetic formulations.
    Type: Application
    Filed: April 29, 2002
    Publication date: October 31, 2002
    Applicant: Merck Patent GmbH
    Inventors: Joachim Weitzel, Wolfgang Hechler
  • Protein elongation factor 2 as a target for antifungal and antiparasitic agents
    Publication number: 20020160441
    Abstract: Inhibition of protein elongation factor 2 provides a target for identifying potential antifungal and antiparasitic compounds. EF2 inhibitors are useful as therapeutic agents against fungal and parasitic infections.
    Type: Application
    Filed: April 24, 2002
    Publication date: October 31, 2002
    Applicant: Merck & Co., Inc.
    Inventors: Jennifer Nielsen-Kahn, Michael C. Justice, Dennis M. Schmatz, Ming-Jo Hsu, Theresa W. Ku
  • &agr;V integrin receptor antagonists
    Patent number: 6472403
    Abstract: The present invention relates to novel imidazolidinone derivatives thereof, their synthesis, and their use as &agr;v integrin receptor antagonists. More particularly, the compounds of the present invention are antagonists of the integrin receptors &agr;v&bgr;3 and/or &agr;v&bgr;5 and are useful for inhibiting bone resorption, treating and preventing osteoporosis, and inhibiting vascular restenosis, diabetic retinopathy, macular degeneration, angiogenesis, atherosclerosis, inflammation, inflammatory arthritis, viral disease, cancer, and metastatic tumor growth.
    Type: Grant
    Filed: January 19, 2001
    Date of Patent: October 29, 2002
    Assignee: Merck & Co., Inc.
    Inventors: Mark E. Duggan, Wasyl Halczenko, John H. Hutchinson, Aiwen Li, Robert S. Meissner, James J. Perkins, Thomas G. Steele, Jiabing Wang, Michael A. Patane
  • Spiropiperidine derivatives as melanocortin receptor agonists
    Patent number: 6472398
    Abstract: Certain novel spiropiperidine derivatives of structural formula Ia wherein the substituents are as defined herein are agonists of the human melanocortin receptor(s) and, in particular, are selective agonists of the human melanocortin-4 receptor (MC-4R). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the activation of MC-4R, such as obesity, diabetes, sexual dysfunction, including erectile dysfunction and female sexual dysfunction.
    Type: Grant
    Filed: March 20, 2001
    Date of Patent: October 29, 2002
    Assignee: Merck & Co., Inc.
    Inventors: Brenda L. Palucki, Ravi P. Nargund
  • N-cyclopentyl modulators of chemokine receptor activity
    Patent number: 6472410
    Abstract: The present invention is directed to compounds of the formula I: (wherein R1, R3, R4, R5, R6, 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: October 29, 2002
    Assignee: Merck & Co., Inc.
    Inventors: Paul E. Finke, Kevin T. Chapman, Malcolm Maccoss, Sander G. Mills, Jennifer L. Loebach, Bryan Oates
  • DNA vaccine formulations
    Publication number: 20020156037
    Abstract: This invention relates to novel methods and formulations of nucleic acid pharmaceutical products, specifically formulations of nucleic acid vaccine products and nucleic acid gene therapy products. The formulations of the disclosure stabilize the conformation of DNA pharmaceutical products.
    Type: Application
    Filed: September 7, 2001
    Publication date: October 24, 2002
    Applicant: Merck & Co., Inc.
    Inventors: David B. Volkin, Robert K. Evans, Mark Bruner
  • Lactonization process
    Publication number: 20020156298
    Abstract: Crystalline 3-hydroxylactone-containing products can be prepared in high yield and purity in a one-pot process by treating the corresponding 3,5-dihydroxy acid with a strong mineral acid in a cold, aprotic, water-miscible solvent to effect lactonization, followed by addition of excess acid to effect crystallization of the lactonized product from the reaction mixture.
    Type: Application
    Filed: April 5, 2002
    Publication date: October 24, 2002
    Applicant: Merck & Co., Inc.
    Inventors: James McManus, Nicholas Anousis, John F. Genus, Christopher Hancock
  • Human N-methyl-D-aspartate receptor subunits, nucleic acids encoding same and uses therefor
    Patent number: 6469142
    Abstract: In accordance with the present invention, there are provided nucleic acids encoding human NMDA receptor protein subunits and the proteins encoded thereby. The NMDA receptor subunits of the invention comprise components of NMDA receptors that have cation-selective channels and bind glutamate and NMDA. In one aspect of the invention, the nucleic acids encode NMDAR1 and NMDAR2 subunits of human NMDA receptors. In a preferred embodiment, the invention nucleic acids encode NMDAR1, NMDAR2A, NMDAR2B, NMDAR2C and NMDAR2D subunits of human NMDA receptors. In addition to being useful for the production of NMDA receptor subunit proteins, these nucleic acids are also useful as probes, thus enabling those skilled in the art, without undue experimentation, to identify and isolate related human receptor subunits.
    Type: Grant
    Filed: August 28, 2000
    Date of Patent: October 22, 2002
    Assignee: Merck & Co., Inc.
    Inventors: Lorrie P. Daggett, Chin-Chun Lu
  • Process for the preparation of chemical compounds
    Patent number: 6469172
    Abstract: An improved and efficient synthesis for the preparation of 2-amino-6-[(4-aminopiperidin-1-yl]methyl]pyridine, an intermediate compound in the preparation of muscarinic M3 receptor antagonists, includes as a final step the removal of trimethylacetyl and an amino protecting group from 2-trimethylacetyl-amino-6-[(4-protected aminopiperidin-1-yl)methyl]pyridine.
    Type: Grant
    Filed: March 5, 2001
    Date of Patent: October 22, 2002
    Assignee: Merck & Co., Inc.
    Inventors: Peter E. Maligres, Jaemoon Lee
  • Vinylene and ethyl compounds
    Patent number: 6468608
    Abstract: Vinyldene and ethyl compounds of the formula I in which R1, R2, A1, Z1, Z2, Z3, m, n and R are as defined herein, where at least one of Z1 to Z3 is wherein L1 to L6 are each H or F and at least one of L1 to L2 is F or at least one of L3 to L6 is F, are suitable as components of liquid-crystalline media.
    Type: Grant
    Filed: September 25, 2000
    Date of Patent: October 22, 2002
    Assignee: Merck Patent GmbH
    Inventors: Matthias Bremer, Detlef Pauluth, Kazuaki Tarumi, Joachim Krause, Michael Heckmeier
  • Angiogenesis assay
    Patent number: 6468735
    Abstract: The present invention relates to assays and kits using porcine carotid arteries for screening compounds to identify modulators of angiogenesis. In particular, an assay for rapidly screening compounds that inhibit angiogenesis is provided.
    Type: Grant
    Filed: February 26, 2001
    Date of Patent: October 22, 2002
    Assignee: Merck & Co., Inc.
    Inventor: Janet Stiffey-Wilusz
  • Process for the synthesis of (2R, 2-alpha-R)-4-benzyl-2-[1-(3,5-bis (trifluoromethyl)phenyl)ethoxy]-1,4-oxazine-3-one
    Patent number: 6469164
    Abstract: The present invention is concerned with novel processes for the preparation of (2R, 2-alpha-R)-4-benzyl-2-[1-[3,5-bis(trifluoromethyl)phenyl]ethoxy-1,4-oxazin-3-one. This compound is useful as an intermediate in the synthesis of compounds which possess pharmacological activity.
    Type: Grant
    Filed: June 8, 2001
    Date of Patent: October 22, 2002
    Assignee: Merck & Co., Inc.
    Inventors: Karel M. Jos Brands, Joseph F. Payack, Philip J. Pye