Patents Assigned to Merck Sharp & Dohme
  • 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
  • Patent number: 7205434
    Abstract: There is disclosed a novel class of sulphonamido-substituted bridged bicycloalkyl derivatives comprising a substitute on the bridgehead position. The compounds modulate the production of the ?-amyloid precursor protein, and hence are useful in the treatment of Alzheimer's Disease.
    Type: Grant
    Filed: July 31, 2002
    Date of Patent: April 17, 2007
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Joanne Clare Hannam, Timothy Harrison, Andrew Madin, Timothy Jason Sparey
  • 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
  • Patent number: 7176203
    Abstract: A class of imidazo[1,2b][1,2,4]triazine derivatives, substituted at the 7-position by an optionally substituted five-membered or six-membered heteroaromatic ring, being selective ligands for GABAA receptors, in particular having good 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 1, 2003
    Date of Patent: February 13, 2007
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Mark Stuart Chambers, Simon Charles Goodacre, David James Hallett, Robert James Maxey, Michael Geoffrey Neil Russell, Leslie Joseph Street
  • 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
  • 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
  • Patent number: 7157478
    Abstract: Compounds of formula I: wherein X represents a 5-(R-substituted)-1,2,4-oxadiazole-3-yl moiety are inhibitors of gamma-secretase, and hence useful for treating Alzheimer's disease
    Type: Grant
    Filed: April 24, 2003
    Date of Patent: January 2, 2007
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Ian James Collins, Laura Catherine Cooper
  • Patent number: 7157249
    Abstract: The present invention relates to the cloning of novel cDNA sequences encoding the ?4 and ? receptor subunits of the human GABA A receptor; to stably co-transfected eukaryotic cell lines capable of expressing a human GABAA receptor, which receptor comprises at least one of the novel ?4 and ? receptor subunits; and to the use of such cell lines in screening for and designing medicaments which act upon the human GAGAA receptor.
    Type: Grant
    Filed: August 2, 2002
    Date of Patent: January 2, 2007
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Beatrice Le Bourdelles, Paul John Whiting
  • Patent number: 7153868
    Abstract: The present invention provides a method of treatment of a subject suffering from a disease, such as schizophrenia, for which the administration of an NK-3 antagonist is indicated which comprises administering to that subject a therapeutically effective amount of a compound of formula I: wherein, generally, Q is R1 is benzyl, phenyl, thiophene or imidazolyl optionally substituted with C1-4alkyl or halogen, such as methyl, fluorine or bromine; R2 is hydrogen or C1-4alkyl such as methyl; R3 is phenyl; R4 is hydrogen; R5 is hydrogen or C1-6alkylcarbonyl such as methylcarbonyl; X is —SO2— or —C(O)N(R2)SO2— where R2 is preferably hydrogen; Y is a bond, CH2 or Z1 where Z1 is —N(Rf)— in which Rf is C1-6alkylcarbonyl such as ethylcarbonyl; and R6 is phenyl, pyrazolyl, pyridyl, pyrimidinyl or benzimidazolonyl optionally substituted with one or two groups chosen from C1-6alkyl and benzyl, such as methyl, ethyl and benzyl; or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: April 16, 2003
    Date of Patent: December 26, 2006
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Mark Stuart Chambers, Philip Jones, Helen Jane Szekeres
  • Patent number: 7148222
    Abstract: The present invention discloses a compound of formula 1, 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 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; a pharmaceutical composition comprising it; its use in a method of treatment; use of it to manufacture a medicament; and a method of using it to prevent or treat anxiety, convulsions or cognitive disorders.
    Type: Grant
    Filed: October 29, 2003
    Date of Patent: December 12, 2006
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Simon Charles Goodacre, David James Hallett
  • 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
  • Patent number: 7144887
    Abstract: The present invention provides a compound of formula (I) in which R1 is generally hydrogen or CF3, R2 is generally hydrogen, W is a cyclic amine, a heterocycle or a group L-Y—X where L-Y is a linking portion and X is generally an aromatic or non-aromatic heterocycle, alkyl or alkylcarbonyl and Z is generally a heterocycle such as 5-methylisoxazol-3-yl, and pharmaceutically acceptable salts thereof for enhancing cognition in conditions such as Alzheimer's Disease, pharmaceutical compositions comprising them, their use for manufacturing medicaments and methods of treatment using them
    Type: Grant
    Filed: December 11, 2000
    Date of Patent: December 5, 2006
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Helen Jane Bryant, Mark Stuart Chambers, Philip Jones, Angus Murray MacLeod, Robert James Maxey
  • 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
  • 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
  • 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
  • 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
  • Patent number: 7101892
    Abstract: The present invention relates to sulfone derivatives of formula (I): Ar—SO2—CR2R3-L-N(R1)2I wherein Ar, L, R1, R2 and R3 are as defined herein, and pharmaceutically acceptable salts and N-oxides thereof, useful in the treatment of a condition which is susceptible to treatment by modulation of 5-HT7 receptor activity, such as depression or a sleep disorder.
    Type: Grant
    Filed: May 14, 2004
    Date of Patent: September 5, 2006
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Sylvie Bourrain, Peter Alan Hunt, Ian Thomas Huscroft, Janusz Jozef Kulagowski, Clare London, Elizabeth Mary Naylor, Piotr Antoni Raubo, Eileen Mary Seward
  • Patent number: 7060710
    Abstract: The present invention provides compounds of formula I: in which: one of X and Y is a nitrogen atom substituted by a group R6? and the other is a carbon atom substituted by an isoxazole group substituted on its carbon atoms by groups R3 and R4; one of R6 and R6? is hydrogen; either all of W1, W2, W3 and W4 are carbon or one of W1, W2, W3 and W4 is nitrogen and the rest are carbon; and R1 and R2 are, independently, a small group, heteroaromatic ring or a 4–7 membered cyclic amine ring; processes for making them; pharmaceutical composition containing them; their use in therapy, particularly for enhancing cognition in conditions such as Alzheimer's Disease; and methods of treatment using them.
    Type: Grant
    Filed: November 22, 2002
    Date of Patent: June 13, 2006
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Tamara Ladduwahetty, Angus Murray MacLeod, Kevin John Merchant, Francine Sternfeld
  • Patent number: 7049296
    Abstract: Urea derivatives of formula I are disclosed: The compounds are inhibitors of ?-secretase, and hence useful in the treatment or prevention of Alzheimer's Disease
    Type: Grant
    Filed: February 28, 2001
    Date of Patent: May 23, 2006
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Jose Luis Castro Pineiro, Adrian Leonard Smith, Graeme Irvine Stevenson
  • Patent number: 7041689
    Abstract: Compounds of formula I are disclosed: in which X is a 5-membered heteroaryl ring and R is as defined herein.
    Type: Grant
    Filed: April 24, 2003
    Date of Patent: May 9, 2006
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Ian James Collins, Laura Catherine Cooper, Timothy Harrison, Linda Elizabeth Keown, Andrew Madin, Mark Peter Ridgill