Patents Assigned to Merck
  • Polymorphic form of a tachykinin receptor antagonist
    Patent number: 6096742
    Abstract: This invention is concerned with a novel polymorphic form of the compound 2-(R)-(1-(R)-(3,5-bis(trifluoromethyl)-phenyl)-ethoxy)-3-(S)-(4-fluoro)phe nyl-4-(3-(5-oxo-1H,4H-1,2,4-triazolo)methylmorpholine which is a tachykinin receptor antagonist useful in the treatment or prevention of disorders of the central nervous system, inflammatory diseases, pain or migraine, asthma, and emesis. The instant polymorphic form has advantages over the other known forms of 2-(R)-(1-(R)-(3,5-bis(trifluoro-methyl)-phenyl)ethoxy)-3-(S)-(4-fluoro)phe nyl-4-(3-(5-oxo-1H,4H-1,2,4-triazolo)methylmorpholine in terms of thermodynamic stability and suitability for inclusion in pharmaceutical formulations.
    Type: Grant
    Filed: December 15, 1998
    Date of Patent: August 1, 2000
    Assignee: Merck & Co., Inc.
    Inventors: Louis Crocker, James McCauley
  • Polymeric film
    Patent number: 6096241
    Abstract: The invention relates to a polymeric film composed of an optically anisotropic material made from a cross-linked synthetic resin composition comprising a polymer network, being obtainable by copolymerization of a mixture comprising(a) at least one monomer or oligomer, each of said monomers or oligomers having at least two polymerizable functional groups selected from the group consisting of (meth-)acrylate ester, epoxy and vinyl ether,(b) at least one achiral liquid crystalline monomer or oligomer, each of said monomers/oligomers having mesogenic groups and one polymerizable functional group selected from the group consisting of (meth-)acrylate ester, epoxy and vinyl ether.
    Type: Grant
    Filed: January 2, 1998
    Date of Patent: August 1, 2000
    Assignee: Merck Patent Gesellschaft mit beschrankter Haftung
    Inventors: David Coates, Simon Greenfield, Emma Jane Jolliffe
  • Method of improved mixing in roller bottles
    Patent number: 6096544
    Abstract: A method for enhancing the mixing of materials in a roller bottle by the introduction of controlled axial and cross-sectional flow perturbations is disclosed. The effectiveness of the method is demonstrated by achieving higher efficiency in cell culturing and virus propagation in roller bottles by introducing controlled flow perturbations during the process.
    Type: Grant
    Filed: October 26, 1998
    Date of Patent: August 1, 2000
    Assignees: Merck & Co., Inc., Rutgers, The State University of New Jersey
    Inventors: Joye L. Bramble, Fernando J. Muzzio, James A. Searles
  • Inhibitors of farnesyl-protein transferase
    Patent number: 6093737
    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 the farnesylation of the oncogene protein Ras.
    Type: Grant
    Filed: December 23, 1997
    Date of Patent: July 25, 2000
    Assignee: Merck & Co., Inc.
    Inventors: Neville J. Anthony, Robert P. Gomez, Lekhanh O. Tran, Steven D. Young
  • Method of measuring bone resorption activity with a highly enriched population of prefusion osteoclast cells
    Patent number: 6093533
    Abstract: Methods of obtaining enriched populations of osteoclast precursor cells which can be released from tissue culture dishes and used for biochemical studies are described. Osteoblastic cells and bone marrow cells are co-cultured. Next a .alpha..sub.v .beta..sub.3 receptor ligand, such as echistatin is used for cell detachment. The result is a 75-95% pure enriched population of tartrate resistant acid phosphatase (TRAP.sup.+) cells, in high yields (2-3.times.10.sup.6 cells per experiment) can be obtained. These cells are mosty mononucleated and based on their characteristics are considered to be pre-fusion osteoclasts (pOC cells). The precursor osteoclasts can be reseeded onto osteoblasts to obtain an enriched population of mature, multinucleated osteoclast cells.
    Type: Grant
    Filed: November 17, 1997
    Date of Patent: July 25, 2000
    Assignee: Merck & Co., Inc.
    Inventors: Sevgi B. Rodan, Gregg Wesolowski, Gideon A. Rodan
  • Imidazopyridine thrombin inhibitors
    Patent number: 6093717
    Abstract: Compounds of the invention are useful in inhibiting thrombin and associated thrombotic occlusions having the following structure: ##STR1## wherein Y.sup.1 and Y.sup.2 are independently selected from the group consisting ofhydrogen,C.sub.1-4 alkyl,C.sub.1-4 alkoxy,C.sub.
    Type: Grant
    Filed: May 26, 1999
    Date of Patent: July 25, 2000
    Assignee: Merck & Co., Inc.
    Inventors: Philip E. Sanderson, Adel M. Naylor-Olsen
  • Tocolytic oxytocin receptor antagonists
    Patent number: 6090805
    Abstract: This invention relates to certain novel benzoxazinone compounds and derivatives thereof, their synthesis, and their use as oxytocin receptor antagonists. One application of these compounds is in the treatment of preterm labor in mammals, especially humans. The ability of the compounds to relax uterine contractions in mammals also makes them useful for treating dysmenorrhea and stopping labor prior to cesarean delivery.
    Type: Grant
    Filed: June 10, 1998
    Date of Patent: July 18, 2000
    Assignee: Merck & Co., Inc.
    Inventors: Peter D. Williams, Michelle A. Sparks, Ian Bell, Debra S. Perlow, Kenneth Stauffer, Roger M. Freidinger
  • Recombinant human calcium channel .beta..sub.4 subunits
    Patent number: 6090623
    Abstract: Isolated DNA encoding each of human calcium channel .alpha..sub.1 -, .alpha..sub.2 -, .beta.- and .gamma.-subunits, including subunits that arise as splice variants of primary transcripts, is provided. In particular DNA clones encoding each of the .alpha..sub.1A-1, .alpha..sub.1A-2, .alpha..sub.1E-1, .alpha..sub.1C-2, .alpha..sub.1E-3, .beta..sub.3-1, .beta..sub.2C, .beta..sub.2D, .beta..sub.2E and .beta..sub.4 subunits of human calcium channels are provided. Cells and vectors containing the DNA, subunit specific antibodies and nucleic acid probes and methods for identifying compounds that modulate the activity of human calcium channels are also provided.
    Type: Grant
    Filed: October 14, 1997
    Date of Patent: July 18, 2000
    Assignee: Merck & Co., Inc.
    Inventors: Michael M. Harpold, Steven B. Ellis, Mark E. Williams, Ann F. McCue
  • Alkanoic acid derivatives as .alpha.v integrin receptor antagonists
    Patent number: 6090944
    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 .alpha.v.beta.3, .alpha.v.beta.5 and/or .alpha.v.beta.6 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, and tumor growth and metastasis.
    Type: Grant
    Filed: August 10, 1999
    Date of Patent: July 18, 2000
    Assignee: Merck & Co., Inc.
    Inventor: John H. Hutchinson
  • Use of NK-1 receptor antagonists for treating mania
    Patent number: 6090819
    Abstract: A method for the treatment or prevention of mania or hypomania is disclosed comprising administering 3-[2-cyclopropoxy-5-(trifluoromethoxy)phenyl]-6-phenyl-1-oxa-7-aza-spiro[4 .5]decane.
    Type: Grant
    Filed: July 27, 1999
    Date of Patent: July 18, 2000
    Assignee: Merck Sharp & Dohme, Ltd.
    Inventor: Nadia Melanie Rupniak
  • Benzisoxazole-derived antidiabetic compounds
    Patent number: 6090836
    Abstract: The instant invention is concerned with acetylphenols which are useful as antiobesity and antidiabetic compounds. Compositions and methods for the use of the compounds in the treatment of diabetes and obesity and for lowering or modulating triglyceride levels and cholesterol levels or raising high density lipoprotein levels or for increasing gut motility or for treating atherosclerosis are also disclosed.
    Type: Grant
    Filed: January 31, 1997
    Date of Patent: July 18, 2000
    Assignee: Merck & Co., Inc.
    Inventors: Alan D. Adams, Joel P. Berger, Gregory D. Berger, Kenneth J. Fitch, Donald W. Graham, Anthony B. Jones, Derek von Langen, Mark D. Leibowitz, David E. Moller, Arthur A. Patchett, Conrad Santini, Soumya P. Sahoo, Richard L. Tolman, Richard B. Toupence, Thomas F. Walsh
  • Antidiabetic agents
    Patent number: 6090839
    Abstract: The instant invention is concerned with aryl and heteroaryl oxyacetic acid type compounds which are useful antidiabetic compounds. Compositions and methods for the use of the compounds in the treatment of diabetes and related diseases and for lowering triglyceride levels are also disclosed.
    Type: Grant
    Filed: December 19, 1997
    Date of Patent: July 18, 2000
    Assignee: Merck & Co., Inc.
    Inventors: Alan D. Adams, Derek Von Langen, Richard L. Tolman, Hiroo Koyama
  • Direactive mesogenic compounds and intermediates
    Patent number: 6090308
    Abstract: The invention relates to direactive mesogenic compounds or mixtures thereof comprising mesogene-containing molecules, said mesogens having two side chains attached thereto which contain a terminal polymerizable functional group, said mesogens and said functional groups being separated by spacer groups having at least two to twenty spacer atoms, wherein both spacer groups have different chain length.
    Type: Grant
    Filed: August 5, 1997
    Date of Patent: July 18, 2000
    Assignee: Merck Patent Gesellschaft
    Inventors: David Coates, Simon Greenfield
  • Dry mix formulation for bisphosphonic acids
    Patent number: 6090410
    Abstract: Pharmaceutical compositions of bisphosphonic acids, and salts thereof, are prepared by direct compression/dry mix tablet formulation. These pharmaceutical compositions are useful in the treatment of disturbances involving calcium or phosphate metabolism, in particular, the treatment and prevention of diseases involving bone resorption, especially osteoporosis, Paget's disease, malignant hypercalcemia, and metastatic bone disease.
    Type: Grant
    Filed: August 28, 1998
    Date of Patent: July 18, 2000
    Assignee: Merck & Co., Inc.
    Inventors: Simon R. Bechard, Kenneth A. Kramer, Ashok V. Katdare
  • Substituted N-carboxyalkylpeptidyl derivatives as antidegenerative agents
    Patent number: 6090785
    Abstract: Novel N-carboxyalkylpeptidyl compounds represented by the formula ##STR1## which are found to be useful inhibitors of matrix metalloendoproteinases which degrade major components of articular cartilage and basement membranes causing degenerative diseases such as arthritis, periodontal disease, corneal ulceration and the like, and certain cancers, are described.
    Type: Grant
    Filed: October 15, 1992
    Date of Patent: July 18, 2000
    Assignee: Merck & Co., Inc.
    Inventors: Philippe L. Durette, Craig K. Esser, William K. Hagmann, Ihor E. Kopka
  • Inhibitors of farnesyl-protein transferase
    Patent number: 6090948
    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 of inhibiting farnesyl-protein transferase and the farnesylation of the oncogene protein Ras.
    Type: Grant
    Filed: July 27, 1998
    Date of Patent: July 18, 2000
    Assignee: Merck & Co., Inc.
    Inventors: Christopher J. Dinsmore, George D. Hartman
  • Substituted pyrrole derivatives as cell adhesion inhibitors
    Patent number: 6090841
    Abstract: Substituted pyrrole derivatives of Formula I are antagonists of VLA-4 and/or .alpha..sub.4 .beta..sub.7, and as such are useful in the inhibition or prevention of cell adhesion and cell-adhesion mediated pathologies. These compounds may be formulated into pharmaceutical compositions and are suitable for use in the treatment of asthma, allergies, inflammation, multiple sclerosis, and other inflammatory and autoimmune disorders.
    Type: Grant
    Filed: November 9, 1998
    Date of Patent: July 18, 2000
    Assignee: Merck & Co., Inc.
    Inventors: Linda Chang, Malcolm MacCoss, William K. Hagmann
  • Pigment for shielding of ultraviolet radiation
    Patent number: 6086666
    Abstract: An ultraviolet radiation shielding pigment having a high power of shielding of ultraviolet radiation, particularly UV-A, a low cohesive force, and excellent extensibility and adhesiveness as a pigment for cosmetics. A pigment for shielding an ultraviolet radiation which comprises a flaky powder having particle surfaces coated with particles of barium sulfate having an average diameter of 0.1 to 2.0 microns, and with needle crystal particles of zinc oxide having an average major-axis diameter of 0.05 to 1.5 microns, and a process for manufacturing it.
    Type: Grant
    Filed: July 2, 1998
    Date of Patent: July 11, 2000
    Assignee: Merck Patent Gesellschaft mit beschrankter Haftung
    Inventors: Tamio Noguchi, Yukitaka Watanabe
  • Use of NK-1 receptor antagonists for treating stress disorders
    Patent number: 6087348
    Abstract: The present invention provides the use of an orally active, long acting, CNS-penetrant NK-1 receptor antagonist for the manufacture of a medicament adapted for oral administration for the treatment or prevention of stress disorders without concomitant therapy with other anti-stress agents, methods of treatment using such a NK-1 receptor antagonist and pharmaceutical compositions comprising it.
    Type: Grant
    Filed: June 9, 1999
    Date of Patent: July 11, 2000
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Raymond Baker, Neil Roy Curtis, Jason Matthew Elliott, Timothy Harrison, Gregory John Hollingworth, Philip Stephen Jackson, Janusz Jozef Kulagowski, Nadia Melanie Rupniak, Eileen Mary Seward, Christopher John Swain, Brian John Williams
  • Composition of enalapril and losartan
    Patent number: 6087386
    Abstract: The present invention discloses a pharmaceutical composition of enalapril and losartan and a pharmaceutically acceptable carrier.
    Type: Grant
    Filed: June 17, 1997
    Date of Patent: July 11, 2000
    Assignee: Merck & Co., Inc.
    Inventors: Tzyy-Show H. Chen, Bassel Iskandarani, Charles S. Sweet, Kenneth A. Krammer, William Grossman