Patents Assigned to Merck Sharp
  • Pyridazine derivatives as ligands for GABA receptors
    Patent number: 7381725
    Abstract: A class of pyridazine derivatives, substituted in the 4-position by an optionally substituted heteroaromatic ring, 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: August 4, 2003
    Date of Patent: June 3, 2008
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Stephen Robert Fletcher, Angus Murray MacLeod, Monique Bodil Van Niel, Kevin Wilson
  • Alkenyl-substituted spirocyclic sulfamides as inhibitors of gamma-secretase
    Patent number: 7371771
    Abstract: Compounds of formula (I) are disclosed: wherein R4 is an alkenyl group of defined structure. The compounds inhibit gamma-secretase, and hence are useful for treatment of Alzheimer's disease.
    Type: Grant
    Filed: April 24, 2003
    Date of Patent: May 13, 2008
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Jose Luis Castro Pineiro, Joanne Claire Hannam, Timothy Harrison, Andrew Madin, Mark Peter Ridgill
  • Sulphonamido-substituted bridged bicycloalkyl derivatives
    Patent number: 7365196
    Abstract: A class of compounds is disclosed, comprising sulphonamido-substituted bridged bicycloalkyl structures. The compounds are inhibitors of gamma-secretase, and hence are useful in the treatment of and/or prevention of Alzheimer's disease.
    Type: Grant
    Filed: March 15, 2001
    Date of Patent: April 29, 2008
    Assignees: Merck Sharp & Dohme Ltd., Merck Frosst Canada & Co.
    Inventors: Patrice Charles Belanger, Ian James Collins, Joanne Claire Hannam, Timothy Harrison, Stephen John Lewis, Andrew Madin, Edward Giles McIver, Alan John Nadin, Joseph George Neduvelil, Mark Steven Shearman, Adrian Leonard Smith, Timothy Jason Sparey, Graeme Irvine Stevenson, Martin Richard Teall
  • Substituted-1-phthalazinamines as vr-1 antagonists
    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
  • Piperidines and Related Compounds for Treatment of Alzheimer's Disease
    Publication number: 20080021043
    Abstract: Compounds of formula I: selectively inhibit production of A?(1-42) and hence are useful in treatment or prevention of disease associated with deposition of ?-amyloid in the brain.
    Type: Application
    Filed: October 20, 2005
    Publication date: January 24, 2008
    Applicant: MERCK SHARP & DOHME LTD.
    Inventors: Joanne Hannam, Janusz Kulagowski, Andrew Madin, Mark Ridgill, Eileen Seward
  • Cyclohexyl sulphones
    Patent number: 7304094
    Abstract: Novel sulphones of formula I are disclosed: The compounds modulate the processing of amyloid precursor protein by gamma-secretase, and hence are useful in the treatment or prevention of Alzheimer's disease.
    Type: Grant
    Filed: October 28, 2005
    Date of Patent: December 4, 2007
    Assignee: Merck Sharp + Dohme
    Inventors: Ian Churcher, Kevin Dinnell, Timothy Harrison, Sonia Kerrad, Alan John Nadin, Paul Joseph Oakley, Duncan Edward Shaw, Martin Richard Teall, Susannah Williams, Brian John Williams
  • Method and materials for treatment of Alzheimer's disease
    Patent number: 7300955
    Abstract: The invention provides the combined use of an inhibitor of formation or release of ?-amyloid and a nitric oxide releaser for the treatment or prevention of Alzheimer's disease.
    Type: Grant
    Filed: February 27, 2004
    Date of Patent: November 27, 2007
    Assignee: Merck Sharp + Dohme Ltd.
    Inventor: Jose Luis Castro Pineiro
  • ? v integrin receptor antagonists
    Patent number: 7288655
    Abstract: The present invention relates to the synthesis of intermediates for the preparation of compounds of formula (A): wherein n is 2 or 3 and various salt forms of these compounds.
    Type: Grant
    Filed: March 4, 2004
    Date of Patent: October 30, 2007
    Assignees: Merck & Co., Inc., Merck Sharp & Dohme Ltd.
    Inventors: Brian Christopher Bishop, Karel Marie Joseph Brands, Ian Frank Cottrell, Cameron John Cowden, Antony John Davies, Stephen Philip Keen, David Ross Lieberman, Gavin William Stewart
  • Assay for modulation of ? secretase
    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
  • Heteroaryl substituted spirocyclic sulfamides for inhibition of gamma secretase
    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
  • Imidazo-pyridine derivatives as ligands for GABA receptors
    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
  • 5-HTreceptor antagonists
    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
  • Synthesis of cyclohexanone derivatives
    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
  • Pyrazole derivatives as gamma-secretase inhibitors useful in the treatment of Alzheimer's disease
    Patent number: 7271191
    Abstract: The compounds of formula I: inhibit gamma secretase and hence are of utility in the treatment or prevention of Alzheimer's Disease.
    Type: Grant
    Filed: April 1, 2004
    Date of Patent: September 18, 2007
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Michela Bettati, Mark Stuart Chambers, Peter Alan Hunt, Philip Jones, Angus Murray MacLeod, Helen Jane Szekeres, Martin Richard Teall
  • Tetrahydropyran derivatives and their use as therapeutic agents
    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
  • Polymorphic forms of a GABAagonist
    Patent number: 7262300
    Abstract: Two new crystalline monhydrates and two new crystalline anhydrates of gaboxadol are disclosed together with methods for preparing them.
    Type: Grant
    Filed: January 28, 2005
    Date of Patent: August 28, 2007
    Assignee: Merck Sharp & Dohme Ltd.
    Inventor: Vincent Brett Cooper
  • Process for preparing peptide intermediates
    Patent number: 7262169
    Abstract: The present invention is directed to the improved synthesis of compounds of formula (I) an intermediate compound which is useful in the synthesis of the anticancer agents known as PSA conjugates.
    Type: Grant
    Filed: October 18, 2000
    Date of Patent: August 28, 2007
    Assignees: Merck & Co., Inc., Merck Sharp & Dohme Limited
    Inventors: Michael Stewart Ashwood, Brian Christopher Bishop, Ian Frank Cottrell, Khateeta Moneek Emerson, David Hands, Guo Jie Ho, Joseph Edward Lynch, Yao Jun Shi, Robert Darrin Wilson
  • Gem-disubstituted cyclohexane derivatives and their use as therapeutic agents
    Patent number: 7253205
    Abstract: The present invention relates compounds of the formula (I): wherein R1, R2, R3, R4, R5, R6, R7, R8, R9 and R10 represent a variety of substituents, ring A is a phenyl or pyridyl ring; d is zero, 1 or 2; and pharmaceutically acceptable salts and N-oxides thereof.
    Type: Grant
    Filed: June 10, 2002
    Date of Patent: August 7, 2007
    Assignee: Merck Sharp & Dohme Limited
    Inventors: Jose Luis Castro Pineiro, Kevin Dinnell, Jason Matthew Elliott, Gregory John Hollingworth, Duncan Edward Shaw, Christopher John Swain
  • 8-fluoroimidazo 1,2-a pyridine derivatives as ligands for GABA receptors
    Patent number: 7226926
    Abstract: A class of 8-fluoroimidazo[1,2-?]pyridine derivatives, substituted at the 3-position by an optionally substituted five-membered or six-membered heteroaromatic ring, 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: June 5, 2007
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Wesley Peter Blackaby, Jose Luis Castro Pineiro, Simon Charles Goodacre, David James Hallett, Alexander Charles Humphries, Philip Jones, Kevin John Merchant, Michael Reader
  • Imidazo[1,2-b]pyridazine analogues as anxiolytics and cognition enhancers
    Patent number: 7226922
    Abstract: The present invention provides a compound of formula I: 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 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; pharmaceutical compositions comprising this compound and methods of treating and/or preventing anxiety and convulsions using it.
    Type: Grant
    Filed: October 7, 2003
    Date of Patent: June 5, 2007
    Assignee: Merck Sharp & Dohme Ltd.
    Inventor: David James Hallett