Patents Assigned to Merck Sharp & Dohme Limited
  • 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
  • Gamma-secretase inhibitors
    Patent number: 7183303
    Abstract: Compounds of formula I: inhibit gamma-secretase and hence find use in treatment of Alzheimer's disease.
    Type: Grant
    Filed: November 5, 2004
    Date of Patent: February 27, 2007
    Assignee: Merck Sharp & Dohme Limited
    Inventors: Jose Luis Castro Pineiro, Ian James Collins, Timothy Harrison
  • Tetrahydropyranyl cyclopentyl tetrahydroisoquinoline modulators of chemokine receptor activity
    Patent number: 7166614
    Abstract: The present invention is directed to compounds of the formula I: 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.
    Type: Grant
    Filed: April 25, 2003
    Date of Patent: January 23, 2007
    Assignees: Merck & Co., Inc., Merck Sharp & Dohme Limited
    Inventors: Richard Jiao, Stephen D. Goble, Sander G. Mills, Gregori Morriello, Alexander Pasternak, Lihu Yang, Changyou Zhou, Gabor Butora, Shankaran Kothandaraman, Deodialsingh Guiadeen, Christopher Moyes
  • Sulphones for inhibition of gamma secretase
    Patent number: 7161006
    Abstract: The invention provides compounds of formula I: which are inhibitors of ?-secretase and hence useful in the treatment or prevention of Alzheimer's disease.
    Type: Grant
    Filed: September 25, 2003
    Date of Patent: January 9, 2007
    Assignee: Merck Sharp & Dohme Limited
    Inventors: James Michael Crawforth, Jason Matthew Elliott, Andrew Pate Owens, Francine Sternfeld
  • Gamma-secretase inhibitors
    Publication number: 20060293373
    Abstract: Compounds of formula I: are potent inhibitors of gamma-secretase and hence find use in treatment or prevention of diseases associated with deposition of ?-amyloid.
    Type: Application
    Filed: September 16, 2004
    Publication date: December 28, 2006
    Applicant: MERCK SHARP & DOHME LIMITED
    Inventors: Ian Collins, Joanne Hannam, Andrew Madin, Mark Ridgill
  • Sulfonamides, sulfamates and sulfamides as gamma-secretase inhibitors
    Patent number: 7144910
    Abstract: Compounds of formula I: inhibit the processing of APP by gamma-secretase, and hence are useful in treating or preventing Alzheimer's disease.
    Type: Grant
    Filed: October 29, 2003
    Date of Patent: December 5, 2006
    Assignee: Merck Sharp & Dohme Limited
    Inventors: Andrew Madin, Mark Peter Ridgill
  • Sulfamides as gamma-secretase inhibitors
    Patent number: 7138400
    Abstract: Novel sulfamides of formula (I) are disclosed. The compounds exert an inhibitory action on the processing of APP by gamma-secretase, and are therefore useful in the treatment or prevention of Alzheimer's disease.
    Type: Grant
    Filed: October 29, 2001
    Date of Patent: November 21, 2006
    Assignee: Merck Sharp & Dohme Limited
    Inventors: Ian James Collins, Joanne Claire Hannam, Timothy Harrison, Stephen John Lewis, Andrew Madin, Timothy Jason Sparey, Brian John Williams
  • Cyclohexane derivatives and their use as therapeutic agents
    Patent number: 7105507
    Abstract: The present invention relates compounds of formula (I), wherein ring A is a phenyl or pyridyl ring; X represents a linker selected from the group consisting of formulae: (a), (b), (c), (d), and (e); and R1, R2, R3, R4, R5, R6, R7, R13, R14, R15, R16, R17, R21a and R21b are as defined herein. The compounds are of particular use in the treatment or prevention of depression, anxiety, pain, inflammation, migraine, emesis or postherpetic neuralgia.
    Type: Grant
    Filed: May 16, 2001
    Date of Patent: September 12, 2006
    Assignee: Merck Sharp & Dohme Limited
    Inventors: Jose Luis Castro Pineiro, Kevin Dinnell, Jason Matthew Elliott, Gregory John Hollingworth, Duncan Edward Shaw, Christopher John Swain
  • Benzodiazepine derivatives as APP modulators
    Patent number: 7105509
    Abstract: A novel class of 1,4- and 1,5-benzodiazepines of formula (I) is disclosed.
    Type: Grant
    Filed: May 21, 2001
    Date of Patent: September 12, 2006
    Assignee: Merck Sharp & Dohme Limited
    Inventors: Jose Luis Castro Pineiro, Ian Churcher, Alexander Richard Guiblin, Timothy Harrison, Sonia Kerrard, Andrew Madin, Alan John Nadin, Andrew Pate Owens, Timothy Jason Sparey, Martin Richard Teall, Susannah Williams
  • Cyclohexyl sulphone derivatives as gamma-secretase inhibitors
    Patent number: 7101895
    Abstract: Compounds of formula I: wherein Ar1 and Ar2 are optionally substituted aryl or heteroaryl, L is a bond, ?CH— or —(CHRa)n—, and X is SCN, SR1, S(O)R1, (CRaRb)mSO2R1, SO2N(R2)2, SO2NHCOR1, SO2NHN(R2)2, OSO2N(R2)2, OS(O)N(R2)2, OSO2NHCOR1, COR4, NHCOR1, NHCO2R1, NHCON(R2)2, NHSO2R1 or NHSO2N(R2)2, inhibit the processing of APP by gamma secretase, and hence are useful in treatment of Alzheimer's disease.
    Type: Grant
    Filed: October 6, 2003
    Date of Patent: September 5, 2006
    Assignee: Merck Sharp & Dohme Limited
    Inventors: Ian Churcher, Timothy Harrison, Sonia Kerrad, Paul Joseph Oakley, Duncan Edward Shaw, Martin Richard Teall, Susannah Williams
  • Process for synthesising useful intermediates for the preparation of avss3 receptor antagonists
    Publication number: 20060149069
    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. The compounds of formula (A) are useful as ???3 receptor antagonists.
    Type: Application
    Filed: March 4, 2004
    Publication date: July 6, 2006
    Applicant: MERCK SHARP & DOHME LIMITED
    Inventors: Brian Bishop, Karel Marie Brands, Ian Cottrell, Cameron Cowden, Anthony Davies, Stephen Keen, David Lieberman, Gavin Stewart
  • Benzodiazepine derivatives as inhibitors of gamma secretase
    Patent number: 6995155
    Abstract: Compounds of formula (I) are disclosed. The compounds inhibit the action of gamma secretase, and hence find use in the treatment and prevention of Alzheimer's disease.
    Type: Grant
    Filed: August 8, 2001
    Date of Patent: February 7, 2006
    Assignee: Merck Sharp & Dohme Limited
    Inventors: Ian Churcher, Alan John Nadin, Andrew Pate Owens
  • Cyclohexyl sulphones
    Patent number: 6984663
    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: August 20, 2002
    Date of Patent: January 10, 2006
    Assignee: Merck Sharp & Dohme Limited
    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
  • Inhibitors of Akt activity
    Patent number: 6958334
    Abstract: The present invention is directed to compounds comprising a triazolo[4,3-b]pyridazine moiety which inhibit the activity of Akt, a serine/threonine protein kinase.
    Type: Grant
    Filed: April 8, 2002
    Date of Patent: October 25, 2005
    Assignees: Merck & Co., Inc., Merck Sharp & Dohme Limited
    Inventors: Andrew Pate Owens, Stanley F. Barnett
  • Cyclohexyl derivatives and their use as therapeutic agents
    Patent number: 6953792
    Abstract: The present invention relates compounds of the formula (I): wherein ring A is a phenyl or pyridyl ring; X represents a linker selected from the group consisting of: (a), (b), (c), (d), (e), (f), (g), (h), (i), (j), (k), (l) and R1, R2, R3, R4, R5, R6, R7, R13, R14, R15, R16, R?17, R18, R19, R21a and R21b are as defined herein. The compounds are of particular use in the treatment or prevention of depression, anxiety, pain, inflammation, migraine, emesis or postherpetic neuralgia.
    Type: Grant
    Filed: May 16, 2001
    Date of Patent: October 11, 2005
    Assignees: Merck Sharp & Dohme Limited, Merck & Co., Inc.
    Inventors: Jose Luis Castro Pineiro, Kevin Dinnell, Jason Matthew Elliot, Gregory John Hollingworth, Duncan Edward Shaw, Christopher John Swain, Lihu Yang
  • Cyclohexyl sulphones as gamma-secretase inhibitors
    Patent number: 6890956
    Abstract: Compounds of formula I: inhibit the processing of APP by gamma-secretase, and hence are useful in treating or preventing Alzheimer's disease.
    Type: Grant
    Filed: October 6, 2003
    Date of Patent: May 10, 2005
    Assignee: Merck Sharp & Dohme Limited
    Inventors: Ian Churcher, Timothy Harrison, Sonia Kerrad, Alan John Nadin, Andrew Pate Owens, Duncan Edward Shaw, Joanne Thomson, Susannah Williams
  • Gamma-secretase inhibitors
    Patent number: 6756511
    Abstract: Gamma-secretase inhibitors, useful in the treatment or prevention of Alzheimer's disease, are disclosed. The preferred compounds have, as the central portion of the molecule, the structure (a) and are di-astereoisomers of known protease inhibitors.
    Type: Grant
    Filed: July 18, 2002
    Date of Patent: June 29, 2004
    Assignee: Merck Sharp & Dohme Limited
    Inventors: Jose Luis Castro Pineiro, Timothy Harrison, Peter Alan Hunt, Alan John Nadin
  • 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
  • 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