Patents Assigned to Merck Sharp & Dohme Ltd.
  • Imidazo-pyrimidine derivatives as ligands for gaba receptors
    Patent number: 6900215
    Abstract: A class of 3-phenylimidazo[1,2-?]pyrimidine derivatives, substituted at the meta position of the phenyl ring by an optionally substituted aryl or heteroaryl group which is directly attached or bridged by an oxygen atom or a —NH— linkage, and further substituted on the phenyl ring by alkyl, trifluoromethyl, alkoxy or one or two halogen atoms, especially fluoro, are selective ligands for GABAA receptors, in particular having good affinity for the ?2 and/or ?3 and/or ?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: March 19, 2002
    Date of Patent: May 31, 2005
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Mark Stuart Chambers, Simon Charles Goodacre, David James Hallett, Andrew Jennings, Philip Jones, Richard Thomas Lewis, Kevin William Moore, Michael Geoffrey Neil Russell, Leslie Joseph Street, Helen Jane Szekeres
  • Imidazo[4,5-c]pyridin-4-one analogues as GABAA receptor ligands
    Patent number: 6887885
    Abstract: A compound of formula I, or a pharmaceutically acceptable salt thereof: wherein X1 represents hydrogen, halogen, C1-6 alkyl, trifluoromethyl or C1-6 alkoxy; X2 represents hydrogen or halogen; Y represents a chemical bond, an oxygen atom, or a —NH— linkage; Z represents an optionally substituted aryl or heteroaryl group; R1 represents hydrocarbon, a heterocyclic group, trifluoromethyl, —SO2Ra, —SO2NRaRb, —CORa, —CO2Ra or —CONRaRb; and Ra and Rb independently represent hydrogen, hydrocarbon or a heterocyclic group; pharmaceutical compositions including the compound and methods for treating anxiety, convulsions and cognitive disorders are disclosed.
    Type: Grant
    Filed: October 30, 2003
    Date of Patent: May 3, 2005
    Assignee: Merck Sharp & Dohme Ltd
    Inventor: Simon Charles Goodacre
  • Pyrazolo-triazine derivatives as ligands for gaba receptors
    Patent number: 6872720
    Abstract: A class of substituted pyrazolo[1,5-d][1,2,4]triazine derivatives, possessing an optionally substituted cycloalkyl, phenyl or heteroaryl substituent at the 7-position, an alkyl group at the 4-position, and a substituted alkoxy moiety at the 2-position, are selective ligands for GABAA receptors, in particular having high affinity for the ?2 and/or ?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: April 4, 2001
    Date of Patent: March 29, 2005
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: William Robert Carling, Andrew Mitchinson, Michael Geoffrey Russell, Leslie Joseph Street
  • Imidazo-pyridine derivatives as ligands for GABA receptors
    Patent number: 6872731
    Abstract: A class of 3-phenylimidazo[1,2-a]pyridine derivatives, substituted at the meta position of the phenyl ring by an optionally substituted aryl or heteroaryl group which is directly attached or bridged by an oxygen atom or a —NH-linkage, are selective ligands for GABAA receptors, in particular having high affinity for the ?2 and/or ?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: May 23, 2002
    Date of Patent: March 29, 2005
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: James Michael Crawforth, Simon Charles Goodacre, Timothy Harrison, David James Hallett, Andrew Pate Owens, Michael Rowley, Martin Richard Teall
  • Phenylsulphonylipiperazinyl derivatives as 5-HT receptor ligands
    Patent number: 6852718
    Abstract: A class of phenylsulphonyl derivatives wherein the sulphonyl moiety is also attached to an N-arylalkyl-substituted piperazine 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 other psychotic disorders.
    Type: Grant
    Filed: March 30, 2001
    Date of Patent: February 8, 2005
    Assignee: Merck Sharp & Dohme Ltd
    Inventors: Frank Burkamp, Susan Koon-Fung Cheng, Stephen Robert Fletcher
  • Triazolo-pyridazine derivatives as ligands for GABA receptors
    Patent number: 6828322
    Abstract: A class of substituted 1,2,4-triazolo[4,3-b]pyridazine derivatives, possessing a fluoro-substituted phenyl ring at the 3-position and a heteroaryl-methoxy 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, 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: June 17, 2003
    Date of Patent: December 7, 2004
    Assignee: Merck Sharp & Dohme Ltd.
    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
  • Tetrahydropyranyl cyclopentyl tetrahydropyridopyridine modulators of chemokine receptor activity
    Patent number: 6812234
    Abstract: The present invention is directed to compounds of the formula I: (wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, X, n and the dashed line are defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptor CCR-2.
    Type: Grant
    Filed: April 29, 2003
    Date of Patent: November 2, 2004
    Assignees: Merck & Co., Inc., Merck Sharp & Dohme Ltd.
    Inventors: Richard Jiao, Gregori Morriello, Lihu Yang, Stephen D. Goble, Sander G. Mills, Alexander Pasternak, Changyou Zhou, Gabor Butora, Shankaran Kothandaraman, Deodialsingh Guiadeen, Christopher Moyes, Cheng Tang
  • Phenylsulphonyl derivatives as 5-HT receptor ligands
    Patent number: 6777430
    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: April 1, 2003
    Date of Patent: August 17, 2004
    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
  • Pyrazino-pyridazine derivatives as ligands for GABA receptors
    Patent number: 6730676
    Abstract: A class of pyrazino[2,3-d]pyridazine derivatives, possessing an optionally substituted cycloalkyl, phenyl or heteroaryl substituent at the 5-position, a substituted alkoxy moiety at the 3-position, and a range of substituents at the 2-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: June 18, 2002
    Date of Patent: May 4, 2004
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Wesley Peter Blackaby, Richard Thomas Lewis, Leslie Joseph Street
  • Triazolo-pyrimidine derivatives as ligands for gaba receptors
    Patent number: 6730681
    Abstract: A class of substituted or 6,7-ring fused [1, 2, 3]triazolo[1,5-&agr;]-pyrimidine derivatives, possessing an optionally substituted cycloalkyl, phenyl or heteroaryl substituent at the 3-position and an amino moiety at the 5-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: June 14, 2002
    Date of Patent: May 4, 2004
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Mark Stuart Chambers, Ian James Collins, Simon Charles Goodacre, David James Hallett, Philip Jones, Linda Elizabeth Keown, Robert James Maxey, Leslie Joseph Street
  • Azabicyclic ether derivatives and their use as therapeutic agents
    Patent number: 6727249
    Abstract: The present invention relates compounds of the formula (I): wherein X represents hydrogen, C1-4alkyl optionally substituted by a hydroxy, methoxy or benzyloxy group, or CO2(C1-2alkyl); 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: April 27, 2004
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Neil Roy Curtis, Ian Thomas Huscroft, Janusz Jozef Kulagowski, Piotr Antoni Raubo
  • Imidazo-pyridine derivatives as ligands for GABA receptors
    Patent number: 6723735
    Abstract: The present invention is directed to 3-phenylimidazol[4,5-b]pyridine derivatives, that are selective ligands for GABAA receptors. These compounds are useful in the treatment and prevention of disorders of the central nervous system, including anxiety and convulsions.
    Type: Grant
    Filed: February 25, 2002
    Date of Patent: April 20, 2004
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: David James Hallett, Michael Rowley
  • Triazolo-pyridazine derivatives as ligands for GABA receptors
    Patent number: 6699859
    Abstract: 1,2,4-triazolo[4,3-b]pyridazine derivatives, possessing an optionally substituted cycloalkyl, phenyl or heteroaryl substituent at the 3-position, a substituted alkoxy moiety at the 6-position, an optionally substituted N-linked nitrogen-containing aliphatic ring at the 7-position, and a chloro at the 8-position are selective ligands for GABAZA 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 26, 2000
    Date of Patent: March 2, 2004
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: William Robert Carling, Andrew Mitchinson, Leslie Joseph Street
  • Process for the preparation of 1,2,4-triazolin-5-one derivatives
    Patent number: 6673939
    Abstract: The present invention relates to a process for the preparation of a compound of formula (I) wherein R represents hydrogen, C1-10alkyl, haloC1-10alkyl or aryl; which are useful intermediates in the preparation of morpholine derivatives of formula (A). Compounds of formula (A) are useful as therapeutic agents.
    Type: Grant
    Filed: February 5, 2003
    Date of Patent: January 6, 2004
    Assignee: Merck Sharp & Dohme Ltd.
    Inventor: Cameron John Cowden
  • Use of a NK-1 receptor antagonist and an antidepressant and/or an anti-anxiety agent for treatment of depression or anxiety
    Patent number: 6649614
    Abstract: The present invention relates to the treatment of depression and/or anxiety by the administration of a combination of a specific class of NK-1 receptor antagonists and an antidepressant or anti-anxiety agent.
    Type: Grant
    Filed: October 16, 2001
    Date of Patent: November 18, 2003
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Emma Joanne Carlson, Nadia Melanie Rupniak
  • 3-Phenyl-imidazo-pyrimidine derivatives as ligands for GABA receptors
    Patent number: 6642229
    Abstract: A class of 3-phenylimidazo(1,2-a)pyrimidine derivatives (of Formula I, or salt or prodrug thereof: I) wherein Y represents a chemical bond, an oxygen atom, or a —NH— linkage; Z represents an optionally substituted aryl or heteroaryl group; R1 represents hydrogen, hydrocarbon, a heterocyclic group, halogen, cyano trifluoromethyl, nitro, —ORa, —SRa, —SORa, —SO2Ra, —SO2NRaRb, —NRaRb, —NRaCORb, —NRaCO2Rb, —CORa, CO2Ra, —CONRaRb or —CRa═NORb; and Ra and Rb independently represent hydrogen, hydrocarbon or a heterocyclic group.
    Type: Grant
    Filed: November 22, 2002
    Date of Patent: November 4, 2003
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Wesley Peter Blackaby, Simon Charles Goodacre, David James Hallett, Andrew Jennings, Richard Thomas Lewis, Kevin William Moore, Leslie Joseph Street
  • 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
  • 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
  • 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