Patents Assigned to Merck
  • &agr;v integrin receptor antagonists
    Patent number: 6410526
    Abstract: The present invention relates to novel nonanoic acid derivatives, 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 &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: May 31, 2000
    Date of Patent: June 25, 2002
    Assignee: Merck & Co., Inc.
    Inventors: Mark E. Duggan, George D. Hartman, Robert S. Meissner, James J. Perkins
  • Substituted 8-arylquinoline phosphodiesterase-4 inhibitors
    Patent number: 6410563
    Abstract: Novel substituted 8-arylquinolines, wherein the aryl group at the 8-position contains a substituent substituted-alkenyl group, are PDE4 inhibitors.
    Type: Grant
    Filed: December 20, 2000
    Date of Patent: June 25, 2002
    Assignee: Merck Frosst Canada & Co.
    Inventors: Denis Deschenes, Daniel Dube, Michel Gallant, Yves Girard, Patrick Lacombe, Dwight MacDonald, Anthony Mastracchio, Helene Perrier
  • Process for the preparation of recombinant proteins in E. coli by high cell density fermentation
    Patent number: 6410270
    Abstract: The invention relates to a fed-batch fermentation process which uses special E. coli host/vector systems for the purpose of efficiently forming recombinant proteins, in particular recombinant antibody molecules, preferably antibody fragments such as miniantibodies. Under the given conditions, the E. coli cells are able to grow at a maximum specific growth rate up to very high cell densities. After the recombinant product formation has been switched on, it is only the formed product which restricts growth; there is no growth restriction due to substrates or metabolic by-products. High space-time yields of recombinant proteins can be achieved in this manner.
    Type: Grant
    Filed: November 16, 1998
    Date of Patent: June 25, 2002
    Assignee: Merck Patent Gesellschaft
    Inventors: Wolfgang Strittmatter, Siegfried Matzku, Dieter Riesenberg, Uwe Horn, Uwe Knüpeer, Marian Kujau, Rolf Wenderoth, Andreas Plückthun, Anke Krebber
  • Spiropiperidine derivatives as melanocortin receptor agonists
    Patent number: 6410548
    Abstract: Certain novel spiropiperidine compounds are agonists of melanocortin receptor(s) and are useful for the treatment, control or prevention of diseases and disorders responsive to the activation of melanocortin receptors. The compounds of the present invention are therefore useful for treatment of diseases and disorders such as obesity, diabetes, sexual dysfunction including erectile dysfunction and female sexual dysfunction.
    Type: Grant
    Filed: February 12, 2001
    Date of Patent: June 25, 2002
    Assignee: Merck & Co., Inc.
    Inventors: Ravi P. Nargund, Zhixiong Ye, Brenda L. Palucki, Raman K. Bakshi, Arthur A. Patchett, Leonardus H. T. Van Der Ploeg
  • Inhibitors of prenyl-protein transferase
    Patent number: 6410534
    Abstract: The present invention is directed to peptidomimetic macrocyclic compounds which inhibit prenyl-protein transferase and the prenylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting prenyl-protein transferase and the prenylation of the oncogene protein Ras.
    Type: Grant
    Filed: June 29, 1999
    Date of Patent: June 25, 2002
    Assignee: Merck & Co., Inc.
    Inventors: Christopher J. Dinsmore, Ian M. Bell, Douglas C. Beshore, Theresa M. Williams
  • Surface-modified conductive pigment
    Patent number: 6409815
    Abstract: Surface-modified conductive pigment obtainable by partial coating of a conductive pigment with an organic modifying agent. The modifying agent is an organometallic compound of the elements silicon, tin, titanium, zirconium or aluminum. The pigment is prepared by dispersing a conductive pigment, subsequently adding the modifying agent, if appropriate as a mixture with a solvent, to the pigment dispersion, and in particular in an amount such that the powder electrical conductance of the partly coated conductive pigment is in the range between 80% of the starting value and 10−7 S, removing the solvent present, if appropriate, with further agitation and heating of the pigment to 100° C. and finally drying the partly coated pigment.
    Type: Grant
    Filed: April 5, 1995
    Date of Patent: June 25, 2002
    Assignee: Merck Patent Gesellschaft mit beschraenkter Haftung
    Inventors: Alfred Hennemann, Manfred Kieser
  • Polysaccharide precipitation process
    Patent number: 6410025
    Abstract: Bacterial polysaccharides which are used to produced vaccines are isolated then precipitated with a long chain detergent. The precipitated polysaccharides are soluble in organic solvents and can be further derivatized and processed to form the vaccine.
    Type: Grant
    Filed: June 1, 1998
    Date of Patent: June 25, 2002
    Assignee: Merck & Co., Inc.
    Inventor: Russel J. Lander
  • Combination therapy for the treatment of benign prostatic hyperplasia
    Patent number: 6410554
    Abstract: This invention relates to combination therapy for the treatment of benign prostatic hyperplasia comprising an alpha-1a antagonist and an endothelin antagonist. More specifically, the use of a selective alpha-1a adrenergic receptor antagonist in combination with a subtype non-selective endothelin antagonist provides relief of lower urinary tract symptoms in patients with symptomatic prostatism or benign prostatic hyperplasia. This combination therapy improves lower urinary tract symptoms including increasing urine flow rate, decreasing residual urine volume and improving overall obstructive and irritative symptoms in patients with benign prostatic hyperplasia or symptomatic prostatism.
    Type: Grant
    Filed: March 23, 1999
    Date of Patent: June 25, 2002
    Assignee: Merck & Co., Inc.
    Inventors: Theodore P. Broten, Peter K. S. Siegl, Steven A. Nichtberger
  • Chemical synthesis of 1,2,4-triazolinone derivative
    Patent number: 6407255
    Abstract: The present invention relates to a process for the preparation of morpholine derivatives of formula (I) which are useful as a therapeutic agents.
    Type: Grant
    Filed: September 10, 2001
    Date of Patent: June 18, 2002
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Ian Frank Cottrell, Ulf H Dolling, David Hands, Robert Darrin Wilson
  • Cloning and expression of dog gonadotropin releasing hormone receptor
    Patent number: 6407222
    Abstract: The dog GnRH receptor has been isolated, cloned and sequenced. The dog GnRH receptor may be used to screen and identify compounds which bind to the GnRH receptor. Such identified compounds may be used in the treatment of sex hormone related conditions such as endometriosis, uterine fibroids, polycystic ovarian disease, hirsutism, precocious puberty, gonadal steroid-dependent neoplasias such as cancers of the prostate, breast and ovary, gonadotrophe pituitary adenomas, sleep apnea, irritable bowel syndrome, premenstrual syndrome and benign prostatic hypertrophy. The receptor proteins and polypeptides, nucleic acids, cells and assays of this invention are useful in drug screening and development, diagnosis and therapeutic applications.
    Type: Grant
    Filed: May 31, 2000
    Date of Patent: June 18, 2002
    Assignee: Merck & Co., Inc.
    Inventors: Jisong Cui, Jane-Ling Lo, George R. Mount
  • Liquid-crystalline medium
    Patent number: 6406761
    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 in claim 1.
    Type: Grant
    Filed: July 26, 2000
    Date of Patent: June 18, 2002
    Assignee: Merck Patents Gesellschaft mit beschraenkter Haftung
    Inventors: Kazuaki Tarumi, Brigitte Schuler, Michael Schwarz, Hideo Ichinose, Yasuyoshi Namiki, Akiko Takashima, Hiroshi Numata
  • Process and intermediates for the preparation of imidazolidinone &agr;v integrin antagonists
    Patent number: 6407241
    Abstract: A novel process is provided for the preparation of imidazolidinone &agr;v&bgr;3/&agr;v&bgr;5 integrin antagonists, and the useful intermediates obtained therein. These compounds are antagonists of &agr;v&bgr;3/&agr;v&bgr;5 integrin receptors and thus useful for inhibiting bone resorption and treating and preventing osteoporosis. Also disclosed is 3-{2-oxo-3-[3-(5,6,7,8-tetrahydro-[1,8]naphthyridin-2-yl)-propyl]imidazolidin-1-yl}-3(S)-(6-methoxy-pyridin-3-yl)-propionic acid in the form of a hemihydrate.
    Type: Grant
    Filed: November 7, 2000
    Date of Patent: June 18, 2002
    Assignee: Merck & Co., Inc.
    Inventors: Mark S Jensen, Michael Palucki, Nelo R. Rivera, Kenneth M. Wells, Yi Xiao, Yaling Wang, Chunhua Yang, Nobuyoshi Yasuda
  • Cloned and expressed human bradykinin BK-2 receptor
    Patent number: 6407207
    Abstract: The present invention is a cloned human BK-2 bradykinin receptor cloned from a human lung fibroblast cell line. A cDNA clone, also part of the instant invention, encodes a novel 364 amino acid protein (the BK-2 receptor) that has the characteristics of a seven transmembrane domain G-protein coupled receptor. The invention is used to express a BK-2 bradykinin receptor in a host mammalian cell to screen for pharmaceutical antagonists or agonists which bind to or interact with the BK-2 bradykinin receptor protein.
    Type: Grant
    Filed: November 8, 1993
    Date of Patent: June 18, 2002
    Assignee: Merck & Co., Inc.
    Inventors: Joseph A. Borkowski, John W. Hess, Catherine D. Strader, Richard W. Ransom
  • Dry mix formulation for bisphosphonic acids
    Patent number: 6406714
    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: October 17, 2000
    Date of Patent: June 18, 2002
    Assignee: Merck & Co., Inc.
    Inventors: Simon R. Bechard, Kenneth A. Kramer, Ashok V. Katdare
  • Substituted pyridones having cytokine inhibitory activity
    Patent number: 6403596
    Abstract: There are disclosed compounds of formula (I) and pharmaceutically acceptable salts thereof which exhibit utility for the treatment of cytokine mediated diseases such as arthritis.
    Type: Grant
    Filed: June 12, 2000
    Date of Patent: June 11, 2002
    Assignee: Merck & Co., Inc.
    Inventors: Nigel J. Liverton, David A. Claremon, John W. Butcher, Cory R. Theberge
  • Method for treating chronic prostatitis or chronic pelvic pain syndrome
    Patent number: 6403640
    Abstract: The use of a COX-2 selective inhibitor for the treatment of chronic prostatitis or chronic pelvic pain syndrome is disclosed.
    Type: Grant
    Filed: August 24, 2000
    Date of Patent: June 11, 2002
    Assignees: Merck & Co., Inc., Temple University of the Commonwealth of Higher Ed.
    Inventors: Elizabeth Stoner, Joanne Waldstreicher, Curtis J. Nickel, Michel A. Pontari
  • TN and HTN liquid-crystal display
    Patent number: 6403171
    Abstract: TN and HTN liquid-crystal displays having very short response times and good steepness values and angle dependencies, are obtained using nematic liquid-crystal mixtures which comprise compounds of formula IA in combination with compounds of the formula IC: in which R1 to R3, L1, Z, and C are defined herein.
    Type: Grant
    Filed: November 29, 1999
    Date of Patent: June 11, 2002
    Assignee: Merck GmbH
    Inventors: Harald Hirschmann, Marcus Reuter
  • Rotavirus vaccine formulations
    Patent number: 6403098
    Abstract: The present invention provides novel liquid and lyophilized formulations of vaccines against rotavirus infection and methods of their preparation. The formulations include buffering agents appropriate for oral administration of rotavirus vaccines. The formulations also include compounds to stabilize of the vaccine compositions against loss of potency.
    Type: Grant
    Filed: August 3, 1999
    Date of Patent: June 11, 2002
    Assignee: Merck & Co., Inc.
    Inventors: Carl J. Burke, David B. Volkin
  • Combination therapy for reducing the risks associated with cardiovascular disease
    Patent number: 6403571
    Abstract: The instant invention involves a combination therapy and pharmaceutical compositions comprised of a therapeutically effective amount of a cholesterol reducing agent such as an HMG-CoA reductase inhibitor in combination with a platelet aggregation inhibitor which is useful for inhibiting platelet aggregation, for inhibiting the formation of thrombotic occlusions, and for treating, preventing and reducing the risk of occurrence of cardiovascular and cerebrovascular events and related vaso-occlusive disorders.
    Type: Grant
    Filed: January 18, 2001
    Date of Patent: June 11, 2002
    Assignee: Merck & Co., Inc.
    Inventors: Robert J. Gould, Steven A. Nichtberger, Patricia A. Rhymer, Lars Olofsson
  • Substituted nipecotyl derivatives as inhibitors of cell adhesion
    Patent number: 6403584
    Abstract: Compounds of Formula I are antagonists of VLA-4 and/or &agr;4&bgr;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 AIDS-related dementia, allergic conjunctivitis, allergic rhinitis, Alzheimer's disease, asthma, atherosclerosis, autologous bone marrow transplantation, certain types of toxic and immune-based nephritis, contact dermal hypersensitivity, inflammatory bowel disease including ulcerative colitis and Crohn's disease, inflammatory lung diseases, inflammatory sequelae of viral infections, meningitis, multiple sclerosis, multiple myeloma, myocarditis, organ transplantation, psoriasis, pulmonary fibrosis, restenosis, retinitis, rheumatoid arthritis, septic arthritis, stroke, tumor metastasis, uveititis, and type I diabetes.
    Type: Grant
    Filed: June 15, 2001
    Date of Patent: June 11, 2002
    Assignee: Merck & Co., Inc.
    Inventors: Stephen E. de Laszlo, Clare E. Gutteridge, William K. Hagmann, Theodore M. Kamenecka