Patents Represented by Attorney, Agent or Law Firm David L. Rose
  • Amide derivatives as &bgr; 3 agonists
    Patent number: 6291491
    Abstract: Amide derivatives are selective &bgr;3 adrenergic receptor agonists with very little &bgr;1 and &bgr;2 adrenergic receptor activity and as such the compounds are capable of increasing lipolysis and energy expenditure in cells. The compounds thus have potent activity in the treatment of Type II diabetes and obesity. The compounds can also be used to lower triglyceride levels and cholesterol levels or raise high density lipoprotein levels or to decrease gut motility. In addition, the compounds can be used to reduced neurogenic inflammation or as antidepressant agents. Compositions and methods for the use of the compounds in the treatment of diabetes and obesity and for lowering triglyceride levels and cholesterol levels or raising high density lipoprotein levels or for increasing gut motility are also disclosed.
    Type: Grant
    Filed: October 12, 2000
    Date of Patent: September 18, 2001
    Assignee: Merck & Co., Inc.
    Inventors: Ann E. Weber, Emma R. Parmee, Robert Mathvink, Wallace T. Ashton, Elizabeth M. Naylor
  • 2-cyclohexyl benzimidazole NMDA/NR2B antagonists
    Patent number: 6291499
    Abstract: Novel 4-substituted cyclohexanes substituted in the 1-position with 2-benzimidazoles, 2-imidazopyridines, or 4-imidazoles either directly or through a C1-C4alkyl, cycloalkyl, hydroxyalkyl, alkoxy or aminoalkyl chain are effective as NMDA NR2B antagonists useful for relieving pain.
    Type: Grant
    Filed: October 25, 2000
    Date of Patent: September 18, 2001
    Assignee: Merck & Co., Inc.
    Inventors: Wayne Thompson, David A. Claremon, Peter M. Munson, John A. McCauley
  • Synthesis of methylthiophenyl hydroxyketones
    Patent number: 6281391
    Abstract: This invention encompasses a novel process for synthesizing compounds represented by formula A: These compounds are intermediates useful in the preparation of certain agents that are selective COX-2 inhibitors.
    Type: Grant
    Filed: October 27, 1999
    Date of Patent: August 28, 2001
    Assignees: Merck & Co., Inc., Merck Frosst Canada & Co.
    Inventors: Richard D. Tillyer, Ian W. Davies, Robert D. Larsen, Xin Wang, Paul O'Shea, Anthony On-Ping King, Dalian Zhao, Cheng Y. Chen, Edward J. J. Grabowski
  • Biphenylene lactams as prostaglandin receptor ligands
    Patent number: 6277839
    Abstract: The present invention relates to biphenylene lactams of Formula II which are ligands at the prostaglandin receptors, as well as a method for treating prostaglandin mediated diseases comprising administration to a patient in need of such a treatment of a non-toxic therapeutically effective amount of compound of Formula II, and the like.
    Type: Grant
    Filed: October 1, 1999
    Date of Patent: August 21, 2001
    Assignee: Merck Frosst Canada & Co.
    Inventors: Joseph G. Atkinson, Marc Labelle, Patrick Lacombe, Rejean Ruel
  • Alteration of circadian rhythmicity with a tachykinin antagonist
    Patent number: 6274604
    Abstract: A tachykinin antagonist is useful, alone or in conjunction with other agents, for altering circadian rhythmicity and alleviating circadian rhythm disorders and for enhancing and improving the quality of sleep.
    Type: Grant
    Filed: May 5, 1999
    Date of Patent: August 14, 2001
    Assignee: Merck & Co., Inc.
    Inventor: Carl Mendel
  • Use of NK-1 receptor antagonists for treating cognitive disorders
    Patent number: 6271230
    Abstract: The present invention provides methods for the treatment or prevention of cognitive disorders which comprises oral administration of an orally active, long acting, CNS-penetrant NK-1 receptor antagonist and pharmaceutical compositions comprising such a NK-1 receptor antagonist.
    Type: Grant
    Filed: May 24, 1999
    Date of Patent: August 7, 2001
    Assignee: Merck Sharp & Dohme Limited
    Inventors: Raymond Baker, Jason Matthew Elliott, Neil Roy Curtis, Timothy Harrison, Gregory John Hollingworth, Janusz Jozef Kulagowski, Philip Stephen Jackson, Nadia Melanie Rupniak, Eileen Mary Seward, Brian John Williams, Christopher John Swain
  • Cyclic amino acid derivatives as cell adhesion inhibitors
    Patent number: 6271252
    Abstract: Cyclic amino acid derivatives 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 asthma, allergies, inflammation, multiple sclerosis, and other inflammatory and autoimmune disorders.
    Type: Grant
    Filed: May 23, 2000
    Date of Patent: August 7, 2001
    Assignee: Merck & Co., Inc.
    Inventors: Linda Chang, William K. Hagmann, Malcolm MacCoss
  • Eosinophil eotaxin receptor
    Patent number: 6271347
    Abstract: The eosinophil eotaxin receptor has been isolated, cloned and sequenced. This receptor is a human &bgr;-chemokine receptor and has been designated “CC CKR3”. The eosinophil eotaxin receptor may be used to screen and identify compounds that bind to the eosinophil eotaxin receptor. Such compounds would be useful in the treatment and prevention of atopic conditions including allergic rhinitis, dermatitis, conjunctivitis, and particularly bronchial asthma.
    Type: Grant
    Filed: April 24, 1997
    Date of Patent: August 7, 2001
    Assignee: Merck & Co., Inc.
    Inventors: Bruce L. Daugherty, Julie A. Demartino, Salvatore J. Siciliano, Martin S. Springer
  • Thienycyclohexanone derivatives as ligands of the GABAA &agr;5 receptor subtype
    Patent number: 6262103
    Abstract: A pharamceutical composition comprises a compound of formula (I) or a pharmaceutically acceptable salt thereof, wherein A is C1-6alkyl, C2-6alkenyl, C2-6-alkynyl, C3-6-cycloalkyl, arylC1-6alkyl, aryl, S(O)pR1.
    Type: Grant
    Filed: April 16, 1999
    Date of Patent: July 17, 2001
    Assignee: Merck Sharp & Dohme Limited
    Inventors: Howard Barff Broughton, Mark Stewart Chambers, Sarah Christine Hobbs, Angus Murray MacLeod, Austin John Reeve
  • Human neurokinin-3 receptor
    Patent number: 6258943
    Abstract: A recombinant human neurokinin-3 receptor (hereinafter identified as human NK3R) is disclosed which has been prepared by polymerase chain reaction techniques. Also disclosed is the complete sequence of human NK3R complementary DNA; expression systems, including a CHO (chinese hamster ovarian cell line) stable expression system; and an assay using the CHO expression system. Human NK3R can be used in an assay to identify and evaluate entities that bind to the neurokinin-3 receptor.
    Type: Grant
    Filed: July 12, 1993
    Date of Patent: July 10, 2001
    Assignee: Merck & Co., Inc.
    Inventors: Tung Ming Fong, Ruey-Ruey C. Huang, Catherine D. Strader
  • Stabilization of the reagent dimethyl titanocene
    Patent number: 6255550
    Abstract: The present invention is directed to organic solutions of the reagent dimethyl titanocene which further comprise a sterically hindered ester and optionally titanocene dichloride. Stability of the reagent dimethyl titanocene is enhanced by the presence of the sterically hindered ester.
    Type: Grant
    Filed: October 28, 1999
    Date of Patent: July 3, 2001
    Assignee: Merck & Co., Inc.
    Inventor: Mark Huffman
  • Process for the synthesis of 3,5-bis(trifluoromethyl)-bromobenzene
    Patent number: 6255545
    Abstract: The present invention is concerned with a novel process for the preparation of 3,5-bis(trifluoromethyl)bromobenzene (CAS 328-70-1). This compound is useful as an intermediate in the synthesis of compounds which possess pharmacological activity.
    Type: Grant
    Filed: June 8, 2000
    Date of Patent: July 3, 2001
    Assignee: Merck & Co., Inc.
    Inventors: Raymond Cvetovich, Fuh-Rong Tsay
  • Intermediates useful in a process for synthesizing COX-2 inhibitors
    Patent number: 6252116
    Abstract: The invention encompasses a process for making compounds of Formula I useful in the treatment of cyclooxygenase-2 mediated diseases.
    Type: Grant
    Filed: January 21, 2000
    Date of Patent: June 26, 2001
    Assignee: Merck & Co., Inc.
    Inventors: Edward G. Corley, Ian W. Davies, Robert D. Larsen, Philip J. Pye, Kai Rossen
  • Carboxylic acids and acylsulfonamides, compositions containing such compounds and methods of treatment
    Patent number: 6242493
    Abstract: Compounds of formula I: as well as pharmaceutically acceptable salts, hydrates and esters thereof, are disclosed. The compounds are useful for treating or preventing prostaglandin mediated diseases. Pharmaceutical compositions containing such compounds and methods of treatment are also included.
    Type: Grant
    Filed: March 10, 1999
    Date of Patent: June 5, 2001
    Assignee: Merck Frosst Canada & Co.
    Inventors: Yves Gareau, Marc LaBelle, Helene Juteau, Michel Gallant, Nicolas LaChance, Michel Belley
  • Method for treating attention deficit disorder
    Patent number: 6242446
    Abstract: Tachykinin receptor antagonists that are useful for treating or preventing attention deficit disorder, optionally associated with hyperactivity in a patient, are desclosed.
    Type: Grant
    Filed: May 31, 2000
    Date of Patent: June 5, 2001
    Assignee: Merck & Co., Inc.
    Inventors: David L. Glatt, Mark S. Kramer, Nadia Rupniak
  • F-18 radiolabeled neurokinin-1 receptor antagonists
    Patent number: 6241964
    Abstract: The present invention is directed to radiolabeled neurokinin-1 receptor antagonists which are useful for the labeling and diagnostic imaging of neurokinin-1 receptors in mammals.
    Type: Grant
    Filed: September 28, 1999
    Date of Patent: June 5, 2001
    Assignee: Merck & Co., Inc.
    Inventors: H. Donald Burns, Terence G. Hamill, Raymond E. Gibson
  • 3-phenyl-4-(4(methylsulfonyl)phenyl)-2-(5H)-furanone as a cox-2 inhibitor
    Patent number: 6239173
    Abstract: The invention encompasses the novel compound of Formula I useful in the treatment of cyclooxygenase-2 mediated diseases. The invention also encompasses certain pharmaceutical compositions for treatment of cyclooxygenase-2 mediated diseases comprising compounds of Formula I.
    Type: Grant
    Filed: November 18, 1999
    Date of Patent: May 29, 2001
    Assignee: Merck Frosst Canada Inc./Merck Frosst Canada & Co.
    Inventors: Zhaoyin Wang, Michel Therien
  • Morpholine and thiomorpholine tachykinin receptor antagonists
    Patent number: 6235735
    Abstract: Substituted heterocycles of the general structural formula: are tachykinin receptor antagonists useful in the treatment of inflammatory diseases, pain or migraine, asthma and emesis, and calcium channel blockers useful in the treatment of cardiovascular conditions such as angina, hypertension or ischemia.
    Type: Grant
    Filed: March 16, 2000
    Date of Patent: May 22, 2001
    Assignee: Merck & Co., Inc.
    Inventors: Conrad P. Dorn, Jeffrey J Hale, Paul E. Finke, Malcolm Maccoss, Sander G. Mills, Shrenik K. Shah, Mark Stuart Chambers, Tamara Ladduwahetty, Timothy Harrison, Brian John Williams
  • Method for treating or preventing psychosomatic and psychoimmunologic disorders
    Patent number: 6232311
    Abstract: A tachykinin receptor antagonist is useful for treating or preventing a psychosomatic disorder in a patient.
    Type: Grant
    Filed: August 10, 1999
    Date of Patent: May 15, 2001
    Assignee: Merck & Co., Inc.
    Inventors: Nadia Rupniak, Mark S. Kramer
  • Synthesis of 4-[(5-substituted phenyl)-3-substituted-1H-pyrazol-1-yl]benzenesulfonamide
    Patent number: 6232472
    Abstract: This invention encompasses a novel process for synthesizing the compound represented by formula I: These compounds are useful as non-steroidal anti-inflammatory agents.
    Type: Grant
    Filed: September 13, 2000
    Date of Patent: May 15, 2001
    Assignee: Merck Frosst Canada & Co.
    Inventors: Paul O'Shea, Xin Wang, Richard D. Tillyer, Sophie-Dorothee Clas, Chad Dalton