Patents Assigned to Merck Sharp & Dohme
  • Substituted triazolo-pyridazine derivative, pharmaceutical compositions made therefrom
    Patent number: 6630471
    Abstract: 7-(1,1 -Dimethylethyl)-6-(2-ethyl-2H-1,2,4-triazol-3-ylmethoxy)-3-(2-fluorophenyl)-1,2,4-triazolo[4,3-b]pyridazine, and pharmaceutically acceptable salts thereof are selective ligands for GABAA receptors useful in the treatment of disorders of the central nervous system.
    Type: Grant
    Filed: February 1, 2001
    Date of Patent: October 7, 2003
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: William Robert Carling, Jose Luis Castro Pineiro, Cameron John Cowden, Antony John Davies, Andrew Madin, James Francis McCabe, Gareth Edward Pearce, Leslie Joseph Street
  • Spheronized self-emulsifying system for hydrophobic and water-sensitive agents
    Patent number: 6630150
    Abstract: A self-emulsifying system comprises i) microcrystalline cellulose and ii) an oily substance, surfactant, and water is useful for providing solid dosage forms of hydrophobic or water sensitive agents when dried or extruded and spheronized.
    Type: Grant
    Filed: October 15, 2001
    Date of Patent: October 7, 2003
    Assignee: Merck Sharp & Dohme Limited
    Inventors: Steven William Booth, Ashley Clarke, John Michael Newton
  • Imidazo-triazine derivatives as ligands for GABA receptors
    Patent number: 6617326
    Abstract: A class of 7-phenylimidazo[1,2-b][1,2,4]triazine derivatives, substituted at the meta position of the phenyl ring by a (cyano)(fluoro)phenyl moiety, being selective ligands for GABAA receptors, in particular having good affinity for the &agr;2 and/or &agr;3 subunit thereof, are accordingly of benefit in the treatment and/or prevention of adverse conditions of the central nervous system, including anxiety and convulsions.
    Type: Grant
    Filed: July 15, 2002
    Date of Patent: September 9, 2003
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: William Robert Carling, David James Hallett, Michael Geoffrey Neil Russell, Leslie Joseph Street
  • Pentaaza-cyclopental[a]naphthalene derivatives as ligands for GABAa &agr;5 receptors
    Patent number: 6613766
    Abstract: A class of 1,2,3a,4,x-pentaaza-cyclopenta[a]naphthalene compounds (x=6, 7, 8 or 9) is described. The compounds have a high affinity for the GABAA &agr;5 receptors and show inverse agonist activity thereat. The compounds are useful in therapy where cognition enhancement is required.
    Type: Grant
    Filed: May 10, 2001
    Date of Patent: September 2, 2003
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Neil Roy Curtis, Janusz Jozef Kulagowski, Francine Sternfeld
  • Use of NK-1 receptor antagonists for treating major depressive disorders
    Patent number: 6613765
    Abstract: The present invention provides methods for the treatment of major depressive disorders comprising 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: June 11, 1998
    Date of Patent: September 2, 2003
    Assignee: Merck Sharp & Dohme Limited
    Inventors: Raymond Baker, Neil Roy Curtis, Jason Matthew Elliott, Timothy Harrison, Gregory John Hollingworth, Philip Stephen Jackson, Janusz Jozef Kulagowski, Nadia Melanie Rupniak, Eileen May Seward, Christopher John Swain, Brian John Williams
  • 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
  • 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
  • Use of an angiotensin II receptor antagonist for the preparation of drugs to increase the survival rate of renal transplant patients
    Patent number: 6576652
    Abstract: The present invention relates to the use, for the preparation of drugs to increase the survival rate of transplant patients, including renal and heart transplant patients, of a therapeutically effective amount of an angiotension II receptor antagonist compound, such as the class of substituted imidazoles represented by formula (I) and in particular by losartan potassium, 2-butyl-4-chloro-[(2′-tetrazol-5-yl)biphenyl-4-il]methyl]-5-(hydroxymethyl)imidazole potassium salt.
    Type: Grant
    Filed: February 19, 2002
    Date of Patent: June 10, 2003
    Assignee: Merck Sharp & Dohme (Italia) S.p.A.
    Inventor: Giuseppe Remuzzi
  • 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
  • Benzimidazolinyl piperidines as CGRP ligands
    Patent number: 6552043
    Abstract: The present invention relates to benzimidazolinylpiperidine derivatives useful as ligands for CGRP (Calcitonin Gene-Related Peptide) receptors, their use in therapy, pharmaceutical compositions comprising them and methods of treatment using them.
    Type: Grant
    Filed: May 30, 2001
    Date of Patent: April 22, 2003
    Assignees: Merck Sharpe & Dohme Ltd., Merck & Co, Inc.
    Inventors: Arthur A. Patchett, Raymond George Hill, Lihu Yang
  • 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
  • Combination of a selective NMDA NR2B antagonist and an opioid analgesic
    Patent number: 6538008
    Abstract: A combination of a selective NMDA NR2B antagonist and an opioid analgesic is useful in the treatment of pain or nociception.
    Type: Grant
    Filed: August 22, 2000
    Date of Patent: March 25, 2003
    Assignee: Merck Sharpe & Dohme Limited
    Inventor: Susan Boyce
  • 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