Patents Represented by Attorney, Agent or Law Firm David L. Rose
  • 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
  • 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
  • Patent number: 6465509
    Abstract: The invention encompasses the novel compounds of Formula I, which are useful in the treatment of cyclooxygenase-2 mediated diseases. The invention also encompasses certain pharmaceutical compositions comprising compounds of Formula I as well as methods of treating cyclooxygenase-2 mediated diseases comprising administering to a patient in need of such treatment a non-toxic therapeutically effective amount of a compound of Formula I.
    Type: Grant
    Filed: June 27, 2001
    Date of Patent: October 15, 2002
    Assignee: Merck Frosst Canada & Co.
    Inventors: Chun-Sing Li, Cheuk Kun Lau, Michel Therien, Petpiboon Prasit
  • Patent number: 6455548
    Abstract: The present invention is directed to pyrrolidine compounds of the formula I: (wherein R1, R2, R3, R4c, R4d, and R4f 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-3 and/or CCR-5.
    Type: Grant
    Filed: February 27, 2001
    Date of Patent: September 24, 2002
    Assignee: Merck & Co., Inc.
    Inventors: Jennifer Chee, Jill N. Johanson, Frank Kayser, William H. Parsons, Kathleen M. Rupprecht
  • Patent number: 6448274
    Abstract: A PDE4 inhibiting compound is represented by
    Type: Grant
    Filed: May 24, 2001
    Date of Patent: September 10, 2002
    Assignee: Merck Frosst Canada & Co.
    Inventors: Richard Friesen, Yves Ducharme, Yves Girard, Chun Li, Annette Robichoud
  • Patent number: 6444811
    Abstract: Compounds represented by formula I: as well as pharmaceutically acceptable salts, esters, N-oxides and hydrates thereof are disclosed. Pharmaceutical compositions and methods of use are also included. The compounds are active against the caspase-3 enzyme, and thus are useful to treat fin caspase-3 mediated diseases and conditions.
    Type: Grant
    Filed: July 19, 2000
    Date of Patent: September 3, 2002
    Assignee: Merck Frosst Canada & Co.
    Inventors: Yongxin Han, Andre Giroux, Robert Zamboni, Daniel J. McKay, Christopher I. Bayly, Erich L. Grimm, John Colucci
  • Patent number: 6440967
    Abstract: Combinations of a GABAA alpha 5 inverse agonist and a COX-2 inhibitor, NSAID, estrogen or vitamin E are disclosed for treating neurodegenerative conditions such as Alzheimer's Disease.
    Type: Grant
    Filed: November 10, 1999
    Date of Patent: August 27, 2002
    Assignee: Merck & Co., Inc.
    Inventors: Gilbert A. Block, Christopher R. Lines
  • Patent number: 6441002
    Abstract: Polymorphic, amorphous and hydrated forms of the title compound having the following structure: are disclosed. The compound is a potent and selective cyclooxygenase-2 (COX-2) inhibitor.
    Type: Grant
    Filed: November 28, 2000
    Date of Patent: August 27, 2002
    Assignees: Merck & Co., Inc., Merck Frosst Canada & Co.
    Inventors: Sophie Dorothee Clas, Louis S. Crocker, James A. McCauley, Ian Davies, Chad Dalton
  • Patent number: 6440976
    Abstract: Compounds described by the chemical structural formula or a pharmaceutically acceptable salt thereof, are useful in the treatment of pain, migraine, depression, anxiety, schizophrenia, Parkinson's disease, stroke, and in the treatment of neuropathies including postherpetic neuralgia, central pain from spinal cord injury, and phantom limb pain.
    Type: Grant
    Filed: June 25, 2001
    Date of Patent: August 27, 2002
    Assignee: Merck & Co., Inc.
    Inventors: David A. Claremon, John A. McCauley, Nigel J. Liverton, Cory R. Theberge
  • Patent number: 6436965
    Abstract: Compounds represented by formula I: as well as pharmaceutically acceptable salts and hydrates thereof are disclosed as useful for treating or preventing diseases and conditions mediated by PDE-IV. Pharmaceutical compositions and methods of treatment are also included.
    Type: Grant
    Filed: March 1, 2001
    Date of Patent: August 20, 2002
    Assignee: Merck Frosst Canada & Co.
    Inventors: Marc Labelle, Claudio Sturino, Nicolas Lachance, Dwight Macdonald
  • Patent number: 6436395
    Abstract: Disclosed is a method for controlling phytopathogenic fungi using pure strains of Rosellinia subiculata ATCC 74386 and fungus ATCC 74387. Further, methods of producing a sordarin compound are disclosed. The method includes cultivating each strain separately in a nutrient medium containing assimilable sources of carbon and nitrogen and recovering the compound. A sordarin compound of formula I is also disclosed. Also an antifungal composition containing a sordarin compound is also disclosed.
    Type: Grant
    Filed: June 23, 1999
    Date of Patent: August 20, 2002
    Assignee: Merck & Co., Inc.
    Inventors: Gerald F. Bills, Anne W. Dombrowski, Wendy S. Horn, Richard K. Jansson, Mark Rattray, Dennis Schmatz, Robert E. Schwartz
  • Patent number: 6437165
    Abstract: Immunoregulatory compounds are disclosed of the formula: as well as the pharmaceutically acceptable salts and hydrates thereof, are disclosed. The compounds are useful for treating immune mediated diseases and conditions, such as bone marrow, organ and tissue transplant rejection. Pharmaceutical compositions and methods of use are included.
    Type: Grant
    Filed: August 30, 2001
    Date of Patent: August 20, 2002
    Assignee: Merck & Co., Inc.
    Inventors: Suzanne Mandala, James Bergstrom, Richard Hajdu, Hugh Rosen, William Parsons, Deborah J. Card, Malcolm Maccoss, Rupprecht Kathleen
  • Patent number: 6432976
    Abstract: Novel 3-substituted 8-aza-bicyclo[3.2.1]octanes (commonly known as “tropanes”) substituted in the 8-position are effective as NMDA NR2B antagonists useful for relieving pain.
    Type: Grant
    Filed: October 25, 2000
    Date of Patent: August 13, 2002
    Assignee: Merck & Co., Inc.
    Inventors: Wayne Thompson, David A. Claremon, Peter M. Munson, Brian Phillips
  • Patent number: 6432980
    Abstract: Trisubstituted pyrroles are antiprotozoal agents useful in the treatment and prevention of protozoal diseases in human and animals, including the control of coccidiosis in poultry.
    Type: Grant
    Filed: November 10, 2000
    Date of Patent: August 13, 2002
    Assignee: Merck & Co., Inc.
    Inventors: Tesfaye Biftu, Danqing D. Feng, Gui-Bai Liang, Mitree M. Ponpipom, Xiaoxia Qian, Narindar Girotra, Michael H. Fischer, Matthew J. Wyvratt
  • Patent number: 6428983
    Abstract: Histone deacetylase inhibition provides a target for identifying potential antiprotozoal compounds. Histone deacetylase inhibitors are useful as therapeutic agents against protozoal infections.
    Type: Grant
    Filed: April 22, 1999
    Date of Patent: August 6, 2002
    Assignee: Merck & Co.
    Inventors: Paula M. Dulski, Robert W. Myers, Anne M. Gumett, Sandra J. Rattray, Dennis M. Schmatz
  • Patent number: 6420565
    Abstract: 2-lithio-5-halopyridine is formed as a predominant component of a reaction mixture by reacting BuLi with 2,5-dihalopyridine in a non-coordinating solvent.
    Type: Grant
    Filed: February 27, 2001
    Date of Patent: July 16, 2002
    Assignees: Merck & Co., Inc., Merck Frosst Canada & Co
    Inventors: Paul O'Shea, Xin Wang, Richard Tillyer
  • Patent number: 6420418
    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: August 14, 2000
    Date of Patent: July 16, 2002
    Assignee: Merck & Co., Inc.
    Inventors: William K. Hagmann, Stephen E. Delaszlo, George Doherty, Linda L. Chang, Ginger X. Yang
  • Patent number: 6410583
    Abstract: Substituted cyclopentanoindole derivatives are antagonists of prostaglandins, and as such are useful for the treatment of prostaglandin mediated diseases.
    Type: Grant
    Filed: July 20, 2001
    Date of Patent: June 25, 2002
    Assignee: Merck Frosst Canada & Co.
    Inventors: Marc Labelle, Claudio Sturino, Bruno Roy, Carl Berthelette, Michael Boyd, Nicolas Lachance, John Scheigetz
  • 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
  • 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