Patents Assigned to Merck Sharp & Dohme Limited
  • Patent number: 7759492
    Abstract: An enantioselective route to compounds of formula I is disclosed: The compounds of formula I are key intermediates in the synthesis of compounds useful in treatment of Alzheimer's disease.
    Type: Grant
    Filed: August 17, 2005
    Date of Patent: July 20, 2010
    Assignee: Merck Sharp & Dohme Limited
    Inventors: Stephen Philip Keen, Steven Fraser Oliver, Gavin William Stewart
  • Patent number: 7655675
    Abstract: Compounds of formula I: inhibit the processing of APP by gamma-secretase and hence find use in treatment of Alzheimer's disease.
    Type: Grant
    Filed: October 1, 2004
    Date of Patent: February 2, 2010
    Assignee: Merck Sharp & Dohme Limited
    Inventors: Alan John Nadin, Andrew Pate Owens, Martin Richard Teall
  • Patent number: 7655644
    Abstract: The present invention provides compounds of formula (I), wherein both p's are one or two, R1 is generally heteroaryl or cycloalkyl, R2 is C3-6cycloalkyl or phenyl and R3 is heteroaryl, and pharmaceutically acceptable salts thereof, as GlyT1 inhibitors for treating schizophrenia, pharmaceutical compositions comprising the same and methods for their preparation.
    Type: Grant
    Filed: December 21, 2005
    Date of Patent: February 2, 2010
    Assignee: Merck Sharp & Dohme Limited
    Inventors: Wesley Peter Blackaby, Stephen Robert Fletcher, Andrew Jennings, Richard Thomas Lewis, Elizabeth Mary Naylor, Leslie Joseph Street, Joanne Thomson
  • Patent number: 7626056
    Abstract: The present invention provides compounds of formula I: wherein R1 is an alkyl, phenyl, heterocyclyl, cycloalkyl, alkoxy, ester, amino or amide group; R2 is a phenyl, heterocyclyl, alkyl, cycloalkyl or cycloalkylalkyl group; R3 is an alkyl, cycloalkyl, cycloalkylalkyl, amino or heterocyclyl group; R4 and R5 are hydrogen or alkyl or form a cycloalkyl ring; A is O or N; and m is zero or one; as inhibitors of GlyT1 and thus as useful for treating or preventing diseases such as schizophrenia; with the provision of pharmaceutical compositions, first and second medical uses and methods of treatment.
    Type: Grant
    Filed: June 5, 2006
    Date of Patent: December 1, 2009
    Assignee: Merck Sharp & Dohme Limited
    Inventors: Wesley Peter Blackaby, Jose Luis Castro Pineiro, Richard Thomas Lewis, Elizabeth Mary Naylor, Leslie Joseph Street
  • Publication number: 20090270451
    Abstract: The present invention is directed to piperidine compounds that inhibit the glycine transporter GlyT1 and which are useful in the treatment of neurological and psychiatric disorders associated with glycinergic or glutamatergic neurotransmission dysfunction and diseases in which the glycine transporter GlyT1 is involved.
    Type: Application
    Filed: October 27, 2006
    Publication date: October 29, 2009
    Applicants: MERCK & CO., INC., MERCK SHARP & DOHME LIMITED
    Inventors: David Hallett, Craig W. Lindsley, Elizabeth M. Naylor, Zhijian Zhao, Cory R. Theberge, Scott E. Wolkenberg, M. Brad Nolt
  • Patent number: 7598386
    Abstract: Novel sulphones of Formula I are disclosed: wherein A completes a 4-7 membered ring optionally comprising up to two heteroatoms. The compounds modulate the action of ?-secretase and are therefore useful in the treatment or prevention of Alzheimer's disease.
    Type: Grant
    Filed: April 23, 2007
    Date of Patent: October 6, 2009
    Assignee: Merck Sharp & Dohme Limited
    Inventors: Jose Luis Castro Pineiro, Ian Churcher, Kevin Dinnell, Timothy Harrison, Sonia Kerrad, Alan John Nadin, Paul Joseph Oakley, Andrew Pate Owens, Duncan Edward Shaw, Martin Richard Teall, Susannah William, Brian John Williams
  • Patent number: 7595344
    Abstract: Disclosed are sulphones which modulate the action of gamma-secretase. The compounds are useful in the treatment or prevention of Alzheimer's disease.
    Type: Grant
    Filed: May 6, 2008
    Date of Patent: September 29, 2009
    Assignee: Merck Sharp & Dohme Limited
    Inventors: Jose Luis Castro Pineiro, Ian Churcher, Kevin Dinnell, Timothy Harrison, Sonia Kerrad, Alan John Nadin, Paul Joseph Oakley, Andrew Pate Owens, Duncan Edward Shaw, Martin Richard Teall, Susannah William, Brian John Williams
  • Patent number: 7592456
    Abstract: Compounds of formula (I) are potent and selective 5-HT2A antagonists, useful in treatment of a variety of adverse conditions of the CNS.
    Type: Grant
    Filed: November 28, 2005
    Date of Patent: September 22, 2009
    Assignee: Merck Sharp & Dohme Limited
    Inventors: Mark Stuart Chambers, Neil Roy Curtis, Emanuela Gancia, Myra Gilligan, Alexander Charles Humphries, Tamara Ladduwahetty, Robert James Maxey, Kevin John Merchant
  • Patent number: 7572792
    Abstract: The present invention is directed to azetidine compounds that inhibit the glycine transporter GlyT1 and which are useful in the treatment of neurological and psychiatric disorders associated with glycinergic or glutamatergic neurotransmission dysfunction and diseases in which the glycine transporter GlyT1 is involved.
    Type: Grant
    Filed: April 25, 2005
    Date of Patent: August 11, 2009
    Assignees: Merck & Co., Inc., Merck Sharp & Dohme Limited
    Inventors: Craig W Lindsley, David Hallett, Scott E. Wolkenberg
  • Publication number: 20090186919
    Abstract: Compounds of formula (I) modulate the activity of gamma secretase and hence find use in treatment or prevention of Alzheimer's disease and related conditions.
    Type: Application
    Filed: April 2, 2007
    Publication date: July 23, 2009
    Applicant: MERCK SHARP & DOHME LIMITED
    Inventors: Andrew Madin, Mark Peter Ridgill, Janusz Josef Kulagowski
  • Patent number: 7485640
    Abstract: The present invention discloses a compound of formula I, or a pharmaceutically acceptable salt thereof: (I) wherein —U—V— represents —CH?CH—, or —CH2—CH2—, —N?CH— or —CH?N—; 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— or —OCH2— 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 comprising it; its use in methods of treatment; use of it in the manufacture of a medicament for treating and/or preventing anxiety; convulsions or a cognitive disorder; and methods of treatment using it.
    Type: Grant
    Filed: October 29, 2003
    Date of Patent: February 3, 2009
    Assignee: Merck Sharp & Dohme Limited
    Inventors: William Robert Carling, Jose Luis Castro Pineiro, Simon Charles Goodacre, David James Hallett, Leslie Joseph Street
  • Patent number: 7452899
    Abstract: Compounds of Formula (I): inhibit the processing of APP by gamma-secretase, and hence are useful for treatment or prevention of Alzheimer's disease.
    Type: Grant
    Filed: July 29, 2004
    Date of Patent: November 18, 2008
    Assignee: Merck Sharp & Dohme Limited
    Inventors: Michela Bettati, Amanda Louise Boase, Ian Churcher, Tamara Ladduwahetty, Kevin John Merchant, Abdul Quddus
  • Patent number: 7427621
    Abstract: Compounds of formula I: inhibit the processing of AP by gamma-secretase, and hence are useful for treatment or prevention of Alzheimer's disease.
    Type: Grant
    Filed: October 31, 2003
    Date of Patent: September 23, 2008
    Assignee: Merck Sharp & Dohme Limited
    Inventors: Ian James Collins, Joanne Clare Hannam, Timothy Harrison, Andrew Madin, Mark Peter Ridgill
  • Patent number: 7329659
    Abstract: The present invention provides a compound of formula (I): in which Ar and R1 are phenyl or a heteroaromatic group, R2 is generally hydrogen, R3 is hydrogen or alkyl and X, Y and Z are generally CH or N as VR-1 antagonists; or a pharmaceutically acceptable salt thereof; pharmaceutical compositions comprising it; its use in therapy; use of it to manufacture medicaments to treat pain or inflammation; and methods of treating pain or inflammation
    Type: Grant
    Filed: April 5, 2004
    Date of Patent: February 12, 2008
    Assignee: Merck Sharp & Dohme Limited
    Inventors: Peter Blurton, Frank Burkamp, Stephen Robert Fletcher, A. Brian Jones, Edward Giles McIver
  • Patent number: 7285393
    Abstract: There is provided an assay for identifying compounds which interact with the ?-secretase complex, in particular compounds that lower the production of A?42.
    Type: Grant
    Filed: December 18, 2003
    Date of Patent: October 23, 2007
    Assignee: Merck Sharp & Dohme Limited
    Inventor: D. Beher
  • Patent number: 7282513
    Abstract: Compounds of formula I are disclosed: in which X is a 5-membered heteroaryl ring and R is as defined herein. The compounds are inhibitors of the processing of APP by gamma-secretase, and hence are useful in the treatment or prevention of Alzheimer's disease.
    Type: Grant
    Filed: March 2, 2006
    Date of Patent: October 16, 2007
    Assignee: Merck Sharp & Dohme Limited
    Inventors: Ian James Collins, Laura Catherine Cooper, Timothy Harrison, Linda Elizabeth Keown, Andrew Madin, Mark Peter Ridgill
  • Patent number: 7279580
    Abstract: A class of 8-fluoro-3-phenylimidazo[1,2-?]pyridine derivatives, substituted at the meta position of the phenyl ring by an optionally substituted aryl or heteroaryl group, or by a pyrrolidinonyl group, which is directly attached or bridged by an oxygen atom or by a —NH— or —OCH2— linkage, being selective ligands for GABAA receptors, in particular having high affinity for the ?2 and/or ?3 and/or ?5 subunit thereof, 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: May 23, 2003
    Date of Patent: October 9, 2007
    Assignee: Merck Sharp & Dohme Limited
    Inventors: Simon Charles Goodacre, David James Hallett, Alexander Charles Humphries, Philip Jones, Sarah Margaret Kelly, Kevin John Merchant, Kevin William Moore, Michael Reader
  • Patent number: 7276637
    Abstract: A novel process for preparing cyclohexanone derivatives of formula (I) is described. The products are useful as gamma secretase inhibitors, or as intermediates in the synthesis of other gamma secretase inhibitors.
    Type: Grant
    Filed: July 30, 2003
    Date of Patent: October 2, 2007
    Assignees: Merck Sharp & Dohme Limited, Merck & Co., Inc.
    Inventors: Karel Marie Joseph Brands, Antony John Davies, Paul Joseph Oakley, Jeremy Peter Scott, Duncan Edward Shaw, Martin Richard Teall
  • Patent number: 7276607
    Abstract: Substituted carbocyclic sulphonamide derivatives of formula (I), in which n is 0 or 1 and the other variables are as defined in the claims, are selective 5-HT7 receptor antagonists and are thereby effective in the treatment of a variety of neurological conditions, including depression and sleep disorders.
    Type: Grant
    Filed: November 29, 2002
    Date of Patent: October 2, 2007
    Assignee: Merck Sharp & Dohme Limited
    Inventors: Neil Roy Curtis, Peter Alan Hunt, Janusz Jozef Kulagowski
  • Patent number: 7265110
    Abstract: The present invention relates compounds of the formula (I); wherein R1, R2, R3, R4, R5, R6, R7, R8, and R10 represent a variety of substituents; A represents NR9 or O; B represents a bond, CH2, NR9 or O, wherein one or both hydrogen atoms in said CH2 moiety may be replaced with one or both of R7 and R8, or alternatively, one of the hydrogen atoms in said CH2 moiety together with a hydrogen atom from an adjacent carbon are replaced by a double bond; with the proviso that when A is O, then B is NR9; n is zero, 1 or 2; and pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: September 6, 2002
    Date of Patent: September 4, 2007
    Assignee: Merck Sharp & Dohme Limited
    Inventors: Jose Luis Castro Pineiro, Duncan Edward Shaw, Brian John Williams