Patents by Inventor Leslie Joseph Street

Leslie Joseph Street has filed for patents to protect the following inventions. This listing includes patent applications that are pending as well as patents that have already been granted by the United States Patent and Trademark Office (USPTO).

  • 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
  • Publication number: 20030060467
    Abstract: A class of substituted pyrazolo[1,5-d][1,2,4]triazine derivatives, possessing an optionally substituted cycloalkyl, phenyl or heteroaryl substituent at the 7-position, an alkyl group at the 4-position, and a substituted alkoxy moiety at the 2-position, are selective ligands for GABAA receptors, in particular having high affinity for the &agr;2 and/or &agr;3 subunit thereof, and are accordingly of benefit in the treatment and/or prevention of disorders of the central nervous system, including anxiety and convulsions.
    Type: Application
    Filed: October 7, 2002
    Publication date: March 27, 2003
    Inventors: William Robert Carling, Andrew Mitchinson, Michael Geoffrey Russell, Leslie Joseph Street
  • Publication number: 20030055060
    Abstract: A class of 7-phenylimidazo[1,2-b][1,2,4]triazine derivatives, substituted at the meta position of the phenyl ring by a (cyano)(fluoro)phenyl moiety, being selective ligands for GABAA receptors, in particular having good affinity for the &agr;2 and/or &agr;3 subunit thereof, are accordingly of benefit in the treatment and/or prevention of adverse conditions of the central nervous system, including anxiety and convulsions.
    Type: Application
    Filed: July 15, 2002
    Publication date: March 20, 2003
    Inventors: William Robert Carling, David James Hallett, Michael Geoffrey Neil Russell, Leslie Joseph Street
  • Publication number: 20030045532
    Abstract: A class of substituted or 6,7-ring fused [1, 2, 3]triazolo[1,5-&agr;]-pyrimidine derivatives, possessing an optionally substituted cycloalkyl, phenyl or heteroaryl substituent at the 3-position and an amino moiety at the 5-position, are selective ligands for GABAA receptors, in particular having high affinity for the &agr;2 and/or ◯subunit thereof, and are accordingly of benefit in the treatment and/or prevention of disorders of the central nervous system, including anxiety and convulsions.
    Type: Application
    Filed: June 14, 2002
    Publication date: March 6, 2003
    Inventors: Mark Stuart Chambers, Ian James Collins, Simon Charles Goodacre, David James Hallett, Philip Jones, Linda Elizabeth Keown, Robert James Maxey, Leslie Joseph Street
  • Publication number: 20030013716
    Abstract: A class of pyrazino[2,3-d]pyridazine derivatives, possessing an optionally substituted cycloalkyl, phenyl or heteroaryl substituent at the 5-position, a substituted alkoxy moiety at the 3-position, and a range of substituents at the 2-position, are selective ligands for GABAA receptors, in particular having high affinity for the &agr;2 and/or &agr;3 and/or &agr;5 subunit thereof, and are accordingly of benefit in the treatment and/or prevention of adverse conditions of the central nervous system, including anxiety, ceonvulsions and cognitive disorders.
    Type: Application
    Filed: June 18, 2002
    Publication date: January 16, 2003
    Inventors: Wesley Peter Blackaby, Richard Thomas Lewis, Leslie Joseph Street
  • Publication number: 20030004180
    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: Application
    Filed: June 14, 2002
    Publication date: January 2, 2003
    Inventors: Ian James Collins, Linda Elizabeth Keown, Leslie Joseph Street
  • Patent number: 6500828
    Abstract: 1,2,4-triazolo[4,3-b]pyridazine derivatives, possessing a difluoro-or tri-fluoro-substituted phenyl ring at the 3-position, a triazolyl moiety at the 6-position, and a tert-butyl group 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, and are useful in the treatment of anxiety and convulsions.
    Type: Grant
    Filed: July 23, 2001
    Date of Patent: December 31, 2002
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: William Robert Carling, Jose Luis Castro Pineiro, Richard Thomas Lewis, Kevin William Moore, Leslie Joseph Street
  • Publication number: 20020193385
    Abstract: A class of 3-phenylimidazo[1,2-&agr;]pyrimidine derivatives, substituted at the meta position of the phenyl ring by an optionally substituted aryl or heteroaryl group which is directly attached or bridged by an oxygen atom or a —NH— linkage, and further substituted on the phenyl ring by alkyl, trifluoromethyl, alkoxy or one or two halogen atoms, especially fluoro, are selective ligands for GABAA receptors, in particular having good affinity for the &agr;2 and/or &agr;3 and/or &agr;5 subunit thereof, and 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: Application
    Filed: March 19, 2002
    Publication date: December 19, 2002
    Inventors: Mark Stuart Chambers, Simon Charles Goodacre, David James Hallett, Andrew Jennings, Philip Jones, Richard Thomas Lewis, Kevin William Moore, Michael Geoffrey Neil Russell, Leslie Joseph Street, Helen Jane Szekeres
  • Patent number: 6479506
    Abstract: Substituted or 6,7-ring fused 1,2,3-triazolo[4,5-b]pyridine derivatives are selective ligands for GABAA receptors useful in the treatment of disorders of the central nervous system.
    Type: Grant
    Filed: November 7, 2000
    Date of Patent: November 12, 2002
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Howard Barff Broughton, Jose Luis Castro Pineiro, Ian James Collins, Leslie Joseph Street
  • Patent number: 6476030
    Abstract: Compounds according to Formula (I): or a salt or prodrug thereof, have good affinity as ligands for the alpha2 and/or alpha3 subunit of the human GABAA receptor and are useful for treatment of disorders of the central nervous system, including anxiety and convulsions.
    Type: Grant
    Filed: June 8, 2001
    Date of Patent: November 5, 2002
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: William Robert Carling, Andrew Mitchinson, Kevin William Moore, Michael Geoffrey Russell, Gayle Scott, Leslie Joseph Street
  • Patent number: 6465462
    Abstract: Compounds of formula (I) or a pharmaceutically acceptable salt thereof are useful in enhancing cognition.
    Type: Grant
    Filed: January 14, 1999
    Date of Patent: October 15, 2002
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: William Robert Carling, Angus Murray MacLeod, Ruth McKernan, Austin John Reeve, Francine Sternfeld, Leslie Joseph Street
  • Patent number: 6448249
    Abstract: A substituted triazolopyridazine derivative, its use in cognition enhancement therapy, compositions containing it and processes for its manufacture.
    Type: Grant
    Filed: July 24, 2000
    Date of Patent: September 10, 2002
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: William Robert Carling, Tamara Ladduwahetty, Angus Murray MacLeod, Kevin John Merchant, Kevin William Moore, Francine Sternfeld, Leslie Joseph Street
  • Patent number: 6444666
    Abstract: A compound of formula I, or a salt or prodrug thereof: wherein: Z represents C1-6 alkyl, C3-7 cycloalkyl, C4-7 cycloalkenyl, aryl, C3-7 heterocycloalkyl, heteroaryl or di(C1-6)alkylamino, any of which groups may be optionally substituted; R1 represents an optionally substituted five-membered heteroaromatic ring selected from oxazole, thiazole, isoxazole, isothiazole, imidazole, pyrazole, oxadiazole, thiadiazole, triazole and tetrazole; or R1 represents an optionally substituted six-membered heteroaromatic ring selected from pyrazine, pyrimidine and pyridazine; and R2 represents cyano(C1-6)alkyl, hydroxy(C1-6)alkyl, C3-7 cycloalkyl(C1-6)alkyl, propargyl, C3-7 heterocycloalkylcarbonyl(C1-6)alkyl, aryl(C1-6)alkyl or heteroaryl(C1-6)alkyl, any of which groups may be optionally substituted; its use in treating anxiety and pharmaceutical compositions comprising it; a subclass of compounds which are useful in enhancing cognition, such as Alzheimer's Disease, is also disclosed.
    Type: Grant
    Filed: August 27, 1998
    Date of Patent: September 3, 2002
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Tamara Ladduwahetty, Kevin John Merchant, Francine Sternfeld, Leslie Joseph Street
  • Patent number: 6337331
    Abstract: Substituted or 6,7-ring fused 1,2,3-triazolo[1,5-&agr;]-pyrimidine derivatives are selective ligands for GABAA receptors useful in the treatment of disorders of the central nervous system, including anxiety and convulsions.
    Type: Grant
    Filed: November 8, 2000
    Date of Patent: January 8, 2002
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Howard Barff Broughton, Jose Luis Castro Pineiro, Ian James Collins, Karl Richard Gibson, Michael Rowley, Leslie Joseph Street
  • Patent number: 6333336
    Abstract: Pyrazolo[4,3-c]pyridin-3-one derivatives substituted at the 2-position by an optionally substituted aryl or heteroaryl moiety, and having pendant substituents at the 7-position and optionally also at the 6-position, are selective ligands for GABAA receptors, particularly having high affinity for the &agr;2 and/or &agr;3 subunit, and are useful in the treatment and/or prevention of disorders of the central nervous system, including anxiety and convulsions.
    Type: Grant
    Filed: August 23, 2000
    Date of Patent: December 25, 2001
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Wesley Peter Blackaby, Jose Luis Castro Pineiro, Richard Thomas Lewis, Michael Geoffrey Neil Russell, Leslie Joseph Street
  • Patent number: 6310203
    Abstract: Substituted 1,2,4-Triazolo[3,4-A]phthalazine derivatives that are GABA Alpha 5 ligands are prepared from compounds represented by the formula: in which R1 is hydrogen, halogen, CF3, OCF3, CN or an optionally substituted C1-4alkyl, C2-4alkenyl, C2-4alkynyl, C1-4alkoxy, C2-4alkenyloxy or C2-4alkynyloxy group; R2 is hydrogen, halogen, CF3, OCF3, CN or an optionally substituted C1-4alkyl, C2-4alkenyl, C2-4alkynyl, C1-4alkoxy, C2-4alkenyloxy or C2-4alkynyloxy group; Z is an optionally substituted 5-membered or 6-membered heteroaromatic ring; and G is a leaving group.
    Type: Grant
    Filed: April 11, 2000
    Date of Patent: October 30, 2001
    Assignee: Merck Sharpe & Dohme Limited
    Inventors: William Robert Carling, Tamara Ladduwahetty, Angus Murray MacLeod, Kevin John Merchant, Kevin William Moore, Francine Sternfeld, Leslie Joseph Street
  • 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: 6297235
    Abstract: A compound of formula I, or a salt or prodrug thereof: wherein: Z represents C1-6 alkyl, C3-7 cycloalkyl, C4-7 cycloalkenyl, aryl, C3-7 heterocycloalkyl, heteroaryl or di(C1-6)alkylamino, any of which groups may be optionally substituted; R1 represents an optionally substituted five-membered heteroaromatic ring selected from oxazole, thiazole, isoxazole, isothiazole, imidazole, pyrazole, oxadiazole, thiadiazole, triazole and tetrazole; or R1 represents an optionally substituted six-membered heteroaromatic ring selected from pyrazine, pyrimidine and pyridazine; and R2 represents cyano(C1-6)alkyl, hydroxy(C1-6)alkyl, C3-7 cycloalkyl(C1-6)alky, propargyl, C3-7 heterocycloalkylcarbonyl(C1-6)alkyl, aryl(C1-6)alkyl or heteroaryl(C1-6)alkyl, any of which groups may be optionally substituted; its use in treating anxiety and pharmaceutical compositions comprising it; a subclass of compounds which are useful in enhancing cognition, such as Alzheimer's Disease, is also disclosed.
    Type: Grant
    Filed: November 12, 1998
    Date of Patent: October 2, 2001
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Tamara Ladduwahetty, Kevin John Merchant, Francine Sternfeld, Leslie Joseph Street
  • 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: 6211219
    Abstract: A class of substituted aminocyclohexane derivatives are selective agonists of 5-HT1-like receptors, being potent agonists of the human 5-HT1D&agr; receptor subtype while possessing at least a 10-fold selective affinity for the 5-HT1D&agr; receptor subtype relative to the 5-HT1D&bgr; subtype; they are therefore useful in the treatment and/or prevention of clinical conditions, in particular migraine and associated disorders, for which a subtype-selective agonist of 5-HT1D receptors is indicated, while eliciting fewer side-effects, notably adverse cardiovascular events, than those associated with non-subtype-selective 5-HT1D receptor agonists.
    Type: Grant
    Filed: January 4, 1999
    Date of Patent: April 3, 2001
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Angus Murray MacLeod, Graham Andrew Showell, Leslie Joseph Street