Patents Assigned to Merck Sharp & Dohme Ltd.
  • 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
  • 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
  • Phenylsulphonyl derivatives as 5-HT receptor ligands
    Patent number: 6559166
    Abstract: A class of phenylsulphonyl derivatives wherein the sulphonyl moiety is also attached to an N-arylalkyl-substituted azetidine, pyrrolidine or piperidine ring 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 conditions of the central nervous system, including schizophrenia and depression.
    Type: Grant
    Filed: September 27, 2001
    Date of Patent: May 6, 2003
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Peter Blurton, Frank Burkamp, Susan Koon-Fung Cheng, Stephen Robert Fletcher, Angus Murray MacLeod, Daniel Spinks, Monique Bodil Van Niel
  • 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
  • Human theta subunit of the GABAa receptor
    Patent number: 6555341
    Abstract: This invention concerns the cloning of a novel cDNA sequence encoding a particular subunit of the human GABAA receptor. In addition, the invention relates to a stable cell line capable of expressing said cDNA and to the use of the cell line in a screening technique for the design and development of subtype-specific medicaments.
    Type: Grant
    Filed: October 25, 1999
    Date of Patent: April 29, 2003
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Timothy Peter Bonnert, Paul John Whiting
  • 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
  • Delta subunit of human GABAA receptor
    Publication number: 20030013158
    Abstract: The present invention relates to the cloning of novel cDNA sequences encoding the &agr;4 and &dgr; receptor subunits of the human GABAA receptor; to stably co-transfected eukaryotic cell lines capable of expressing a human GABAA receptor, which receptor comprises at least one of the novel &agr;4 and &dgr; receptor subunits; and to the use of such cell lines in screening for and designing medicaments which act upon the human GAGAA receptor.
    Type: Application
    Filed: August 2, 2002
    Publication date: January 16, 2003
    Applicant: Merck Sharp & Dohme, Ltd.
    Inventors: Beatrice Le Bourdelles, Paul John Whiting
  • 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
  • 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
  • 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
  • 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
  • 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
  • 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
  • Tetrahydropyran derivatives and their use as therapeutic agents
    Patent number: 6458830
    Abstract: The present invention relates to compounds of the formula (I): wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10 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 10, 2001
    Date of Patent: October 1, 2002
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Simon Neil Owen, Eileen Mary Seward, Christopher John Swain, Brian John Williams
  • Human &agr;4 receptor subunit of the GABA-A receptor
    Patent number: 6455276
    Abstract: The present invention provides nucleotide sequences encoding the &agr;4 and &dgr; subunits of the human GABAA receptor, preparations of &agr;4 and &dgr; receptor subunit proteins, preparations of receptors including &agr;4 or &dgr; polypeptides, expression vectors including the nucleotide sequences, stably co-transfected eukaryotic cells and methods of their preparation and methods of screening for and designing medicaments which act upon the GABAA receptor.
    Type: Grant
    Filed: June 19, 1997
    Date of Patent: September 24, 2002
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Beatrice Le Bourdelles, Paul John Whiting
  • Combination of a GABAA &agr;5 inverse agonist and a muscarinic agonist
    Patent number: 6455552
    Abstract: A combination of a muscarinic agonist and an inverse agonist of the GABAA &agr;5 receptor subtype useful in treating neurodegenerative conditions such as Alzheimer's Disease is disclosed.
    Type: Grant
    Filed: August 24, 2000
    Date of Patent: September 24, 2002
    Assignee: Merck Sharp & Dohme Ltd.
    Inventor: Gerard Raphael Dawson