Patents Represented by Attorney, Agent or Law Firm J. Eric Thies
  • Imidazo-triazine derivatives as ligands for GABA receptors
    Patent number: 6608062
    Abstract: A class of substituted 1,2,4-triazolo[4,3-]pyridazine derivatives, possessing an optionally substituted cycloalkyl, phenyl or heteroaryl substituent at the 3-position, a substituted alkoxy moiety at the 6-position, and an optionally substituted bicycloalkyl ring system at the 7-position, are selective ligands for GABAA receptors, in particular having high affinity for the &agr;2 and/or &agr;3 subunit thereof, and are accordingly of benefit in the treatment and/or prevention of disorders of the central nervous system, including anxiety and convulsions.
    Type: Grant
    Filed: February 19, 2002
    Date of Patent: August 19, 2003
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: William Robert Carling, Alexander Richard Guiblin, Kevin William Moore, Christopher Richard Moyes, Michael Rowley, Leslie Joseph Street
  • Process for the synthesis of (2R, 2-alpha-R, 3A)-2-[1-(3,5-bis(trifluoromethyl)phenyl)ethoxy]-3-(4-fluorophenyl)-1, 4-oxazine
    Patent number: 6600040
    Abstract: The present invention is concerned with novel processes for the preparation of (2R, 2-alpha-R, 3a)-2-[1-[3,5-bis(trifluoromethyl)phenyl]ethoxy-3-(4-fluorophenyl)-1,4-oxazine. 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: July 29, 2003
    Assignee: Merck & Co., Inc.
    Inventors: Karel M. Jos Brands, Fuh-Rong Tsay, Karen M. Conrad, Matthew M. Zhao
  • Pyrido-pyridazine derivatives as ligands for GABA receptors
    Patent number: 6593325
    Abstract: A class of pyrido[2,3-d]pyridazine derivatives, possessing an optionally substituted cycloalkyl, phenyl or heteroaryl substituent at the 8-position, a substituted alkoxy moiety at the 2-position, and a range of substituents at the 3-position, are selective ligands for GABAA receptors, in particular having high affinity for the &agr;2 and/or &agr;3 and/or &agr;5 subunit thereof, and are accordingly of benefit in the treatment and/or prevention of adverse conditions of the central nervous system, including anxiety, convulsions and cognitive disorders.
    Type: Grant
    Filed: February 20, 2002
    Date of Patent: July 15, 2003
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: William Robert Carling, Jose Luis Castro Pineiro, Andrew Mitchinson, Leslie Joseph Street
  • Polymorphic form of a tachykinin receptor antagonist
    Patent number: 6583142
    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)phenyl-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)phenyl-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: August 12, 2002
    Date of Patent: June 24, 2003
    Assignee: Merck & Co.
    Inventors: Louis Crocker, James McCauley
  • Triazolo-pyridazine derivatives as ligands for GABA receptors
    Patent number: 6579875
    Abstract: 1,2,4-triazolo[4,3-b]pyridazine derivatives, possessing a fluoro-substituted phenyl ring at the 3-position and a heteroaryl-alkoxy moiety at the 6-position, are selective ligands for GABAA receptors, in particular having high affinity for the &agr;2 and/or &agr;3 subunit thereof, are useful in the treatment of anxiety and convulsions.
    Type: Grant
    Filed: June 28, 2000
    Date of Patent: June 17, 2003
    Assignee: Merck Sharp & Dohme Limited
    Inventors: William Robert Carling, Jose Luis Castro Pineiro, Ian James Collins, Alexander Richard Guiblin, Timothy Harrison, Andrew Madin, Kevin William Moore, Michael Geoffrey Russell, Gayle Scott, Leslie Joseph Street
  • Method for treating or preventing psychosomatic and psychoimmunologic disorders
    Patent number: 6573261
    Abstract: This invention relates to the use of a tachykinin receptor antagonist for treating a psychosomatic or a psychoimmunological disorder in a patient.
    Type: Grant
    Filed: May 15, 2001
    Date of Patent: June 3, 2003
    Assignee: Merck & Co., Inc.
    Inventors: Nadia Rupniak, Mark S. Kramer
  • Azabicyclic amine derivatives and their use as therapeutic agents
    Patent number: 6555552
    Abstract: The present invention relates compounds of the formula (I): wherein X represents hydrogen or a C1-4alkyl group optionally substituted by a hydroxy group; Y represents hydrogen, C1-6alkyl or C3-7cycloalkyl; Z is —CR9R10CH2— or —CH2CR9R10—; R represents hydrogen, fluorine, hydroxy, C1-6alkyl or C1-6alkoxy; and R1, R2, R3, R4, R5 and R6 are as defined herein. The compounds are of particular use in the treatment of depression, anxiety, pain, inflammation, migraine, emesis or postherpetic neuralgia.
    Type: Grant
    Filed: April 1, 2002
    Date of Patent: April 29, 2003
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Janusz Jozef Kulagowski, Piotr Antoni Raubo, Christopher George Thomson
  • Pyrazolo-pyridine derivatives as ligands for GABA receptors
    Patent number: 6541484
    Abstract: A class of substituted and/or ring-fused pyrazolo[3,4-b]pyridine derivatives, possessing an optionally substituted cycloalkyl, phenyl or heteroaryl substituent on the pyrazole nitrogen atom adjacent the pyridine nucleus, and an optionally substituted cycloalkyl-alkoxy, aryl-alkoxy or heteroaryl-alkoxy substituent on the carbon atom adjacent the pyridine ring nitrogen atom, are selective ligands for GABAA receptors, in particular having high affinity for the &bgr;2 and/or &bgr;3 subunit thereof, and are accordingly of benefit in the treatment and/or prevention of adverse neurological disorders, including anxiety and convulsions.
    Type: Grant
    Filed: June 14, 2002
    Date of Patent: April 1, 2003
    Assignee: Merck Sharp & Dohme Limited
    Inventors: Ian James Collins, Linda Elizabeth Keown, Leslie Joseph Street
  • 4-Benzyl-2-hydroxy-1,4-oxazine-3-one and polymorphic forms thereof
    Patent number: 6538134
    Abstract: The present invention is concerned with 4-benzyl-2-hydroxy-1,4-oxazin-3-one, and novel processes for the preparation therof. 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: March 25, 2003
    Assignee: Merck & Co., Inc.
    Inventors: Louis S. Crocker, Karel M. Jos Brands, Todd D. Nelson, Philip J. Pye, Jonathan D. Rosen, Kai Rossen
  • Therapeutic polymorphs of a GABA-A alpha-5 inverse agonist and pamoate formulations of the same
    Patent number: 6534505
    Abstract: There is disclosed 3-(5-methylisoxazol-3-yl)-6-(1-methyl-1,2,3-triazol-4-yl)methyloxy-1,2,4-triazolo[3,4-a]phthalazine in the form of a dihydrate, a dehydrate of the dihydrate and a pentahydrate, pharmaceutical compositions comprising the forms, the use of the forms for enhancing cognition, processes for producing the forms, their incorporation in pharmaceutical compositions comprising pamoate ions and the use of such ions for solubilizing neutral molecules.
    Type: Grant
    Filed: November 30, 2000
    Date of Patent: March 18, 2003
    Assignee: Merck & Co., Inc.
    Inventors: Michael J. Kaufman, Daniel J. Rush
  • Prevention or treatment of insomnia with a neurokinin-1 receptor antagonist
    Patent number: 6525073
    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: October 16, 2001
    Date of Patent: February 25, 2003
    Assignee: Merck & Co. Inc.
    Inventors: Carl M. Mendel, Joanne Waldstreicher
  • 2-aryl indole derivative as antagonists of tachykinins
    Patent number: 6518273
    Abstract: The present invention relates to compounds of the formula (I): wherein R1a, R1b, R2, R3, R4, R5, X and n are defined herein. The compounds are of particular use in the treatment or prevention of depression, anxiety, pain, inflammation, migraine, emesis and postherpetic neuralgia.
    Type: Grant
    Filed: September 4, 2001
    Date of Patent: February 11, 2003
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Kevin Tyler Chapman, Kevin Dinnell, Jason Matthew Elliott, Gregory John Hollingworth, Steven Michael Hutchins, Duncan Edward Shaw, Christopher Alan Willoughby
  • Chemical synthesis of spirocyclic piperidines by double ring-closing metathesis
    Patent number: 6515126
    Abstract: The present invention relates to a process for the preparation of a compound of formula (I) wherein Ts is a tosylate group and R is an alkyl group, an unsubstituted phenyl or substituted phenyl ring, or a benzyl or substituted benzyl group; which comprises: (i) cyclising a compound of formula (II) in the presence of a suitable catalyst; and (ii) purifying and collecting the resultant compound of formula (I).
    Type: Grant
    Filed: February 27, 2001
    Date of Patent: February 4, 2003
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Michael Stewart Ashwood, Ian Frank Cottrell, Cameron John Cowden, Debra Jane Wallace
  • Cyclopentyl modulators of chemokine receptor activity
    Patent number: 6506777
    Abstract: The present invention is directed to compounds of the formula I: (wherein R1, R2, R3, R4, R5, R7, R8, X, n, x and y 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: June 8, 2000
    Date of Patent: January 14, 2003
    Assignee: Merck & Co., Inc.
    Inventors: Paul E. Finke, Jennifer L. Loebach, Malcolm Maccoss, Sander G. Mills
  • Process for the synthesis of (R)-1-(3,5-bis(trifluoromethyl)-phenyl)ethan-1-ol by asymmetric transfer hydrogenation
    Patent number: 6504066
    Abstract: The present invention is concerned with novel processes for the preparation of (R)-1-(3,5-bis(trifluoromethyl)phenyl)ethan-1-ol. This compound is useful as an intermediate in the synthesis of compounds which possess pharmacological activity.
    Type: Grant
    Filed: June 30, 2000
    Date of Patent: January 7, 2003
    Assignee: Merck & Co. Inc.
    Inventors: Paul Devine, Hansen Karl
  • Cyclopentyl modulators of chemokine receptor activity
    Patent number: 6500844
    Abstract: The present invention is directed to compounds of the formula I: (wherein R1, R2, R3, R7, R8, X, Y, Z, x and y 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: June 8, 2000
    Date of Patent: December 31, 2002
    Assignee: Merck & Co., Inc.
    Inventors: Paul E. Finke, Kevin T. Chapman, Malcolm Maccoss, Sander G. Mills, Bryan Oates
  • Triazolo-pyridazine derivatives as ligands for gaba receptors
    Patent number: 6500828
    Abstract: 1,2,4-triazolo[4,3-b]pyridazine derivatives, possessing a difluoro-or tri-fluoro-substituted phenyl ring at the 3-position, a triazolyl moiety at the 6-position, and a tert-butyl group at the 7-position, are selective ligands for GABAA receptors, in particular having high affinity for the &agr;2 and/or &agr;3 subunit thereof, and are useful in the treatment of anxiety and convulsions.
    Type: Grant
    Filed: July 23, 2001
    Date of Patent: December 31, 2002
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: William Robert Carling, Jose Luis Castro Pineiro, Richard Thomas Lewis, Kevin William Moore, Leslie Joseph Street
  • 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
  • 3-alkyl substituted pyrrolidine modulators of chemokine receptor activity
    Patent number: 6489354
    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: March 1, 2000
    Date of Patent: December 3, 2002
    Assignee: Merck & Co., Inc.
    Inventors: Jianming Bao, Robert K. Baker, William H. Parsons, Kathleen Rupprecht
  • 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