Patents Represented by Attorney, Agent or Law Firm Melvin Winokur
  • Aryldifluoromethylphosphonic acids with sulfur-containing substituents as PTP-1B inhibitors
    Patent number: 6498151
    Abstract: The invention encompasses the novel class of compounds represented by the formula below, which are inhibitors of the PTP-1B enzyme. The invention also encompasses pharmaceutical compositions and methods of treating or preventing PTP-1B mediated diseases, including diabetes.
    Type: Grant
    Filed: March 21, 2001
    Date of Patent: December 24, 2002
    Assignee: Merck Frosst Canada & Co.
    Inventors: Chun Sing Li, Christopher Bayly, Jacques Yves Gauthier, Yves Leblanc, Cheuk Kun Lau, Patrick Roy, Michel Therien, Zhaoyin Wang, Claude Dufresne, Rejean Fortin
  • Pyrrolidine modulators of chemokine receptor activity
    Patent number: 6498161
    Abstract: The present invention is directed to pyrrolidine compounds of the formula I: (wherein R1, R2, R3, R4, R5, R6 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-5 and/or CCR-3.
    Type: Grant
    Filed: April 4, 2000
    Date of Patent: December 24, 2002
    Assignee: Merck & Co., Inc.
    Inventors: Charles G. Caldwell, Kevin T. Chapman, Jeffrey Hale, Dooseop Kim, Christopher Lynch, Malcolm MacCoss, Sander G. Mills, Christopher Willoughby, Scott Berk, Ronald M. Kim
  • Isoforms of mouse serotonin 5-HT2C receptor
    Patent number: 6495665
    Abstract: The invention includes mouse serotonin 5-HT2c receptor isoforms having amino acid replacements at one or more positions of the natural mouse serotonin 5-HT2c receptor polypeptide sequence, specifically at one or more of positions 157, 159 and 161. The polypeptides are useful for identifying ligands which bind with the serotonin 5-HT2c receptor and modulators of the serotonin 5-HT2c, and for identifying drugs with affinity for 5-HT2 receptors which are used to treat schizophrenia, Parkinsonism, and anxiety disorders.
    Type: Grant
    Filed: March 15, 2000
    Date of Patent: December 17, 2002
    Assignee: Merck & Co., Inc.
    Inventors: Tong M. Fong, Jie Liu, Leonardus H. T. Van Der Ploeg
  • Diketoacid-derivatives as inhibitors of polymerases
    Patent number: 6492423
    Abstract: Diketoacids of Formula (A) are useful as inhibitors of viral polymerases. In particular hepatitis C virus RNA dependent RNA polymerase (HCV RdRp), hepatitis B virus polymerase (HBV pol) and reverse transcriptase of human immunodeficiency virus (HIV RN.) The group R may be broadly chosen and is an organic moiety which contains 2 to 24 carbon atoms and includes an optionally cyclic or heterocyclic group in which the atom directly bonded to the adjacent carbonyl in the diketoacid is part of the ring structure.
    Type: Grant
    Filed: January 26, 2001
    Date of Patent: December 10, 2002
    Assignee: Istituto di Ricerche di Biologia Molecolare Pangeletti SpA
    Inventors: Altamura Sergio, Licia Tomei, Uwe Koch, Philippe Jean Sigfried Neuner, Vincenzo Summa
  • Process for the synthesis of 3,5-bis(trifluoromethyl)benzoic acid
    Patent number: 6489507
    Abstract: The present invention is concerned with a novel process for the preparation of 3,5-bis(trifluoromethyl)benzoic acid (CAS 725-89-3). This compound is useful as an intermediate in the synthesis of compounds which possess pharmacological activity, in particular, as substance P (neurokinin-1) receptor antagonists.
    Type: Grant
    Filed: June 8, 2000
    Date of Patent: December 3, 2002
    Assignee: Merck & Co., Inc.
    Inventors: Raymond Cvetovich, John Leazer
  • Tetrahydropyran derivatives and their use as therapeutic agents
    Patent number: 6489343
    Abstract: The present invention relates to compounds of the formula (I): wherein R1 is fluorine or trifluoromethyl; R2 is fluorine or trifluoromethyl; R3 is methyl or hydroxymethyl; R4 represents a variety of substituents; and n is zero, 1 or 2; and pharmaceutically acceptable salts thereof. The compounds are of particular use in the treatment or prevention of depression, anxiety, pain, inflammation, migaine, emesis or postherpetic neuralgia.
    Type: Grant
    Filed: August 20, 2001
    Date of Patent: December 3, 2002
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Jose Luis Castro Pineiro, Simon Neil Owen, Eileen Mary Seward, Christopher John Swain, Brian John Williams
  • Phenylindole derivatives as 5-HT2A receptor ligands
    Patent number: 6486153
    Abstract: A class of tryptamine analogues bearing an optionally substituted phenyl nucleus at the 2-position are selective antagonists of the human 5-HT2A receptor and are therefore useful as pharmaceutical agents, especially in the treatment and/or prevention of adverse neurological conditions, including psychotic disorders such as schizophrenia.
    Type: Grant
    Filed: March 3, 2000
    Date of Patent: November 26, 2002
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Jose Luis Castro Pineiro, Steven Michael Hutchins, Stephen John Lewis, Michael Rowley, Adrian Leonard Smith, Graeme Irvine Stevenson
  • Phosphonic acid biaryl derivatives as inhibitors of protein tyrosine phosphatase 1B (PTP-1B)
    Patent number: 6486141
    Abstract: The invention encompasses the novel class of compounds represented by formula I which are inhibitors of the PTP-1B enzyme. The invention also encompasses pharmaceutical compositions and methods of treating or preventing PTP-1B mediated diseases, including diabetes, obesity, and diabetes-related conditions.
    Type: Grant
    Filed: December 21, 2000
    Date of Patent: November 26, 2002
    Assignee: Merck Frosst Canada & Co.
    Inventors: Cheuk Kun Lau, Christopher Bayly, Jacques Yves Gauthier, Yves Leblanc, Chun Sing Li, Patrick Roy, Michel Therien, Zhaoyin Wang
  • Phosphonic acid derivatives as inhibitors of protein tyrosine phosphatase 1B (PTP-1B)
    Patent number: 6486142
    Abstract: The invention encompasses the novel class of compounds represented by formula I, which are inhibitors of the PTP-1B enzyme. The invention also encompasses pharmaceutical compositions and methods of treating or preventing PTP-1B mediated diseases, including diabetes, obesity, and conditions related to diabetes.
    Type: Grant
    Filed: December 21, 2000
    Date of Patent: November 26, 2002
    Assignee: Merck Frosst Canada & Co.
    Inventors: Yves Leblanc, Claude Dufresne, Jacques Yves Gauthier, Cheuk Kun Lau, Chun Sing Li, Patrick Roy, Michel Therien, John Scheigetz, Zhaoyin Wang
  • Process for preparing acetonides
    Patent number: 6482952
    Abstract: Acetonides are obtained in a one-step reaction of a carboxylic acid halide, a 1,2-aminoalcohol, and 2-alkoxypropene or 2,2-dialkoxypropane in an ether solvent and in the presence of an inorganic base. Acetonides are also obtained in a two-step reaction scheme in which an acid halide and 1,2-aminoalcohol are reacted in an ether solvent in the presence of LiOH to form a hydroxyamide, which is then reacted with 2-alkoxypropene or 2,2-dialkoxypropane in the presence of acid to form the acetonide. The acetonides resulting from the one-step and two-step protocols can be further reacted with an allylating agent such as an allyl halide in the presence of a strong base to provide the corresponding allyl acetonide. The acetonides and allyl acetonides can serve as intermediates in the production of certain HIV protease inhibitors which are useful for treating HIV infection and AIDS.
    Type: Grant
    Filed: June 18, 2001
    Date of Patent: November 19, 2002
    Assignee: Merck & Co., Inc.
    Inventors: Steven J. Cianciosi, Gregory L. Tewalt, Eric T. Pisk, Ilia A. Zavialov, Glenn A. Hulvey
  • Azabicyclic spiroether derivatives and their use as therapeutic agents
    Patent number: 6479486
    Abstract: The present invention relates compounds of the formula (I): wherein Z is —CR9R10CH2— or —CH2CR9R10—; and R1, R2, R3, R4, R5 and R6 are as defined herein. The compounds are of particular use in the treatment or prevention of depression, anxiety, pain, inflammation, migaine, emesis or postherpetic neuralgia.
    Type: Grant
    Filed: April 1, 2002
    Date of Patent: November 12, 2002
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Ian Thomas Huscroft, Janusz Jozef Kulagowski, Piotr Antoni Raubo
  • Phenylindole derivatives as 5-ht2a receptor ligands
    Patent number: 6479480
    Abstract: Compounds according to Formula (I) or a salt thereof are selective antagonists of the human 5-HT2A receptor useful for treatment of adverse conditions of the central nervous system:
    Type: Grant
    Filed: January 12, 2001
    Date of Patent: November 12, 2002
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Christopher Richard Moyes, Michael Rowley
  • Zwitterionic tachykinin receptor antagonists
    Patent number: 6479518
    Abstract: The present invention is directed to certain novel compounds represented by structural formula I: or a pharmaceutically acceptable salt thereof, wherein R3, R5, R6, R7, R8, R11, R12, R13, Q, W, X, Y and Z are defined herein. The invention is also concerned with pharmaceutical formulations comprising these novel compounds as active ingredients and the use of the novel compounds and their formulations in the treatment of certain disorders. The compounds of this invention are tachykinin receptor antagonists and are useful in the treatment of psychiatric disorders including depression and anxiety.
    Type: Grant
    Filed: September 21, 2001
    Date of Patent: November 12, 2002
    Assignee: Merck & Co., Inc.
    Inventors: Paul E. Finke, Laura C. Meurer, Sander G. Mills, Malcolm MacCoss, Hongbo Qi
  • Triazolo-pyridine derivatives as ligands for GABA receptors
    Patent number: 6479506
    Abstract: Substituted or 6,7-ring fused 1,2,3-triazolo[4,5-b]pyridine derivatives are selective ligands for GABAA receptors useful in the treatment of disorders of the central nervous system.
    Type: Grant
    Filed: November 7, 2000
    Date of Patent: November 12, 2002
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Howard Barff Broughton, Jose Luis Castro Pineiro, Ian James Collins, Leslie Joseph Street
  • 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
  • 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
  • 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
  • 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
  • Substituted triazolo pyridazine derivatives as inverse agonists of the GABAA&agr;5 receptor subtype
    Patent number: 6465462
    Abstract: Compounds of formula (I) or a pharmaceutically acceptable salt thereof are useful in enhancing cognition.
    Type: Grant
    Filed: January 14, 1999
    Date of Patent: October 15, 2002
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: William Robert Carling, Angus Murray MacLeod, Ruth McKernan, Austin John Reeve, Francine Sternfeld, Leslie Joseph Street
  • Aryldifluoromethylphosphonic acids with sulfur-containing substituents as PTP-1B inhibitors
    Patent number: 6465444
    Abstract: The invention encompasses the novel class of compounds represented by the formula below, which are inhibitors of the PTP-1B enzyme. The invention also encompasses pharmaceutical compositions and methods of treating or preventing PTP-1B mediated diseases, including diabetes.
    Type: Grant
    Filed: March 21, 2001
    Date of Patent: October 15, 2002
    Assignees: Merck Frosst Canada & Co., Banyu Pharmaceutical Co., Ltd.
    Inventors: Christopher Bayly, Mitsuru Ohkubo