Patents Assigned to Merck Sharp & Dohme Limited
  • 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
  • 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
  • Patent number: 6395766
    Abstract: Compounds according to Formula (I) or a pharmaceutically acceptable salt thereof are GABA-A Alpha 5 ligands useful for enhancing cognition: where A is C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C3-6cycloalkyl, arylC1-6alkyl, or aryl wherein the aryl group is optionally substituted by halogen, C1-6alkyl, CF3, CN, NO2 or NH2, NR1R10, S(O)pR1, heteroarylC1-6alkyl or heteroaryl where heteroaryl is a 5- or 6-membered heteroaromatic ring as defined for B; and B is phenyl or a 5-membered ring having one or two unsaturations containing 1, 2, 3, or 4 heteroatoms chosen from O, N and S provided that not more than one heteroatom is other than N, a 6-membered heteroaromatic ring containing 1, 2, 3 or 4 nitrogen atoms, each of which rings is optionally substituted by one or more substituents.
    Type: Grant
    Filed: November 6, 2000
    Date of Patent: May 28, 2002
    Assignee: Merck Sharp & Dohme Limited
    Inventors: Howard Barff Broughton, Helen Jane Bryant, Mark Stuart Chambers, Neil Roy Curtis
  • Patent number: 6352994
    Abstract: Compounds according to Formula (I) or a salt thereof are selective ligands for GABAA receptors useful for treatment of disorders of the central nervous system:
    Type: Grant
    Filed: January 4, 2001
    Date of Patent: March 5, 2002
    Assignee: Merck Sharp & Dohme Limited
    Inventors: Ian James Collins, Stephen Robert Fletcher, Timothy Harrison, Paul David Leeson, Christopher Richard Moyes, Alan John Nadin, Michael Rowley, Timothy Jason Sparey, Martin Richard Teall
  • Publication number: 20020019524
    Abstract: 1
    Type: Application
    Filed: September 10, 2001
    Publication date: February 14, 2002
    Applicant: Merck Sharp & Dohme Limited
    Inventors: Ian Frank Cottrell, Ulf H. Dolling, David Hands, Robert Darrin Wilson
  • Patent number: 6323198
    Abstract: A method of treatment for enhancing cognition in the treatment of Alzheimer's disease, for example, employs a specific GABAA Alpha5 receptor ligand.
    Type: Grant
    Filed: July 20, 2000
    Date of Patent: November 27, 2001
    Assignee: Merck Sharp & Dohme Limited
    Inventor: Gerard Raphael Dawson
  • Patent number: 6303597
    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, 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, are useful in the treatment of anxiety and convulsions.
    Type: Grant
    Filed: June 26, 2000
    Date of Patent: October 16, 2001
    Assignee: Merck Sharp & Dohme Limited
    Inventors: William Robert Carling, Kevin William Moore, Leslie Joseph Street
  • Patent number: 6291460
    Abstract: 1,2,4-triazolo[4,3-b]pyridazine derivatives, represented by wherein Z represents cyclobutyl, 1-methylcyclopentyl or pyrrolidin-1-yl, 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: September 18, 2001
    Assignee: Merck Sharp & Dohme Limited
    Inventors: Timothy Harrison, Timothy Jason Sparey, Martin Richard Teall
  • Publication number: 20010018438
    Abstract: Compounds according to Formula (I) or a salt thereof are selective ligands for GABAA receptors useful for treatment of disorders of the central nervous system: 1
    Type: Application
    Filed: January 4, 2001
    Publication date: August 30, 2001
    Applicant: MERCK SHARP & DOHME LIMITED
    Inventors: Ian James Collins, Stephen Robert Fletcher, Timothy Harrison, Paul David Leeson, Christopher Richard Moyes, Alan John Nadin, Michael Rowley, Timothy Jason Sparey, Martin Richard Teall
  • Patent number: 6271230
    Abstract: The present invention provides methods for the treatment or prevention of cognitive disorders which comprises 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: May 24, 1999
    Date of Patent: August 7, 2001
    Assignee: Merck Sharp & Dohme Limited
    Inventors: Raymond Baker, Jason Matthew Elliott, Neil Roy Curtis, Timothy Harrison, Gregory John Hollingworth, Janusz Jozef Kulagowski, Philip Stephen Jackson, Nadia Melanie Rupniak, Eileen Mary Seward, Brian John Williams, Christopher John Swain
  • Patent number: 6262103
    Abstract: A pharamceutical composition comprises a compound of formula (I) or a pharmaceutically acceptable salt thereof, wherein A is C1-6alkyl, C2-6alkenyl, C2-6-alkynyl, C3-6-cycloalkyl, arylC1-6alkyl, aryl, S(O)pR1.
    Type: Grant
    Filed: April 16, 1999
    Date of Patent: July 17, 2001
    Assignee: Merck Sharp & Dohme Limited
    Inventors: Howard Barff Broughton, Mark Stewart Chambers, Sarah Christine Hobbs, Angus Murray MacLeod, Austin John Reeve
  • Patent number: 6255305
    Abstract: Substituted triazolo-pyridazine derivative compounds represented by wherein the variables are disclosed herein are selective ligands for GABA-A receptors, particularly for the &agr;2 and/or &agr;3 subunits.
    Type: Grant
    Filed: November 10, 1998
    Date of Patent: July 3, 2001
    Assignee: Merck Sharp & Dohme Limited
    Inventors: Howard Barff Broughton, William Robert Carling, Jose Luis Castro Pineiro, Alexander Richard Guiblin, Andrew Madin, Kevin William Moore, Michael Geoffrey Russell, Leslie Joseph Street
  • Patent number: 6214846
    Abstract: The present invention relates to compounds of formula (I), wherein R1 represents a fluoroC1-2alkoxy group; and R2 represents a hydrogen or halogen atom or a C1-4alkyl, C1-4alkoxy, fluoroC1-4alkyl or fluoroC1-4alkoxy group; or a pharmaceutically acceptable salt thereof. The compounds are of particular use in the treatment or prevention of pain or inflammation, migraine, emesis, postherpetic neuralgia, depression or anxiety.
    Type: Grant
    Filed: December 9, 1999
    Date of Patent: April 10, 2001
    Assignee: Merck Sharp & Dohme Limited
    Inventor: Jason Matthew Elliott
  • Patent number: 6200975
    Abstract: Substituted 1,2,4-Triazolo[3,4-A]phthalazine derivatives are GABA Alpha 5 ligands and are represented by the formula
    Type: Grant
    Filed: November 12, 1998
    Date of Patent: March 13, 2001
    Assignee: Merck Sharp & Dohme Limited
    Inventors: William Robert Carling, Tamara Ladduwahetty, Angus Murray MacLeod, Kevin John Merchant, Kevin William Moore, Francine Sternfeld, Leslie Joseph Street
  • Patent number: 6180624
    Abstract: This invention relates to methods and compositions for treating pain and nociception in a patient by administering a combination of a morpholine or thiomorpholine tachykinin antagonist and an opioid analgesic.
    Type: Grant
    Filed: February 25, 1999
    Date of Patent: January 30, 2001
    Assignee: Merck Sharp & Dohme Limited
    Inventor: Raymond George Hill
  • Patent number: 6180630
    Abstract: Pyrazolo[4,3-c]pyridazin-3-one analogues, represented by 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: December 8, 1999
    Date of Patent: January 30, 2001
    Assignee: Merck Sharp & Dohme Limited
    Inventors: Peter Blurton, Stephen Robert Fletcher
  • Patent number: 6162805
    Abstract: The present invention relates to the use of an NK-1 receptor antagonist and a selective serotonin reuptake inhibitor for the treatment or prevention of obesity.
    Type: Grant
    Filed: October 22, 1999
    Date of Patent: December 19, 2000
    Assignee: Merck Sharp & Dohme Limited
    Inventor: Franz Fridolin Hefti
  • Patent number: 6156787
    Abstract: The present invention provides compounds of formula (I) or pharmaceutically acceptable salts thereof: ##STR1## where A is C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, C.sub.3-6 cycloalkyl, arylC.sub.1-6 alkyl, aryl, S(O),R.sup.1, OR.sup.1 or NR.sup.1 R.sup.6 ;R.sup.1 is hydrogen; C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, C.sub.3-6 cycloalkyl or C.sub.3-6 cycloalkenyl each of which is optionally substituted by amino, C.sub.1-6 alkylamino, di(C.sub.1-6 alkyl)amino, C.sub.1-6 alkoxy, C.sub.1-6 alkylaminocarbonyl, one, two or three hydroxy groups, one, two or three halogen atoms or a four, five or six-membered saturated heterocyclic ring containing a nitrogen atom and optionally either an oxygen atom or a further nitrogen atom which ring is optionally substituted by C.sub.1-4 alkyl on the further nitrogen atom; aryl, arylC.sub.1-6 alkyl, arylC.sub.2-6 alkenyl or arylC.sub.2-6 alkynyl optionally substituted on the aryl ring by halogen, nitro, cyano, C.sub.
    Type: Grant
    Filed: April 22, 1999
    Date of Patent: December 5, 2000
    Assignee: Merck Sharp & Dohme Limited
    Inventors: Howard Barff Broughton, Mark Stuart Chambers
  • Patent number: 6156749
    Abstract: The present invention provides the use of an orally active, long acting, CNS-penetrant NK-1 antagonist for the manufacture of a medicament for oral administration for the treatment or prevention of movement disorders, methods of treatment using such a NK-1 receptor antagonist and pharmaceutical compositions comprising it.
    Type: Grant
    Filed: June 9, 1999
    Date of Patent: December 5, 2000
    Assignee: Merck Sharp & Dohme Limited
    Inventor: Nadia Melanie Rupniak
  • Patent number: 6143773
    Abstract: The present invention provides compounds of formula (I) and pharmaceutically acceptable salts thereof: ##STR1## wherein A is C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, C.sub.3-6 cycloalkyl, arylC.sub.1-6 alkyl, aryl, S(O).sub.p R.sup.1, OR.sup.1 or NR.sup.1 R.sup.12 ;B is optionally substituted 5- or 6-membered heteroaromatic ring or C(O)NR.sup.10 R.sup.11 ;R.sup.1 is hydrogen, optionally substituted C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, C.sub.3-6 cycloalkyl or C.sub.3-6 cycloalkenyl, optionally substituted aryl, arylC.sub.1-6 alkyl, arylC.sub.2-6 alkenyl or arylC.sub.2-6 alkynyl or an optionally substituted 5- or 6-membered heteroaromatic ring;R.sup.2 and R.sup.3 are hydrogen or C.sub.1-6 alkyl;R.sup.4 is hydrogen, C.sub.1-8 alkyl, C.sub.2-8 alkenyl, C.sub.2-8 alkynyl, aryl or CH.sub.2 (CO).sub.m NR.sup.8 R.sup.9 ;R.sup.5 is NR.sup.6 R.sup.7, C.sub.1-6 alkyl or C.sub.1-6 alkoxy;R.sup.6 is independently as defined for R.sup.4 ;R.sup.
    Type: Grant
    Filed: April 22, 1999
    Date of Patent: November 7, 2000
    Assignee: Merck Sharp & Dohme Limited
    Inventors: Howard Barff Broughton, Mark Stuart Chambers