Patents by Inventor Simon Charles Goodacre

Simon Charles Goodacre 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: 7030128
    Abstract: A class of imidazo[1,2-?]pyrimidine derivatives, substituted at the 3-position by an optionally substituted five-membered or six-membered heteroaromatic ring, are selective ligands for GABAA receptors, in particular having good affinity for the ?2 and/or ?3 and/or ?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: Grant
    Filed: March 19, 2002
    Date of Patent: April 18, 2006
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Wesley Peter Blackaby, Jose Luis Castro Pineiro, Mark Stuart Chambers, Simon Charles Goodacre, David James Hallett, Philip Jones, Richard Thomas Lewis, Angus Murray MacLeod, Robert James Maxey, Kevin William Moore, Leslie Joseph Street
  • Patent number: 7005431
    Abstract: A class of 7-phenylimidazo[1,2-b][1,2,4]triazine 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 substituted on the phenyl ring by one or two further substituents as defined herein, 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 28, 2006
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Michela Bettati, Mark Stuart Chambers, Simon Charles Goodacre, David James Hallett, Michael Geoffrey Neil Russell, Leslie Jospeh Street
  • Patent number: 6969716
    Abstract: The present invention provides a compound of formula I, or an N-oxide thereof or a pharmaceutically acceptable salt thereof: wherein X1 represents hydrogen, halogen, C1-6 alkyl, trifluoromethyl or C1-6 alkoxy; X2 represents hydrogen or halogen; Z represents hydrogen, halogen, cyano, cyanomethyl, trifluoromethyl, nitro, hydroxy, hydroxy(C1-6)alkyl, C1-6 alkoxy, C1-6 alkoxy(C1-6)alkyl, trifluoromethoxy, trifluoromethylthio, trifluoromethanesulfinyl, formyl, C2-6 alkoxycarbonyl, oxopyrrolidinyl, or an optionally substituted aryl, heteroaryl or heteroaryl(C1-6)alkoxy group; and R1 represents aryl or heteroaryl, either of which groups may be optionally substituted; pharmaceutical compositions comprising it, its use in therapy and methods of treatment of anxiety and/or depression using it.
    Type: Grant
    Filed: January 30, 2004
    Date of Patent: November 29, 2005
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Wesley Peter Blackaby, Simon Charles Goodacre, David James Hallett, Andrew Jennings, Richard Thomas Lewis, Leslie Joseph Street, Kevin Wilson
  • Patent number: 6914063
    Abstract: A class of imidazo[1,2-?]pyrazine analogues substituted in the 3-position by a substituted phenyl ring, being selective ligands for GABAA receptors which interact more favourably with the ?2 and/or ?3 subunit than with the ?1 subunit, are accordingly of benefit in the treatment and/or prevention of a variety of disorders of the central nervous system, including anxiety and convulsions, with a reduced propensity to cause sedation.
    Type: Grant
    Filed: July 18, 2001
    Date of Patent: July 5, 2005
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Simon Charles Goodacre, David James Hallett, Leslie Joseph Street
  • Patent number: 6914060
    Abstract: The present invention relates to imidazo[2,1-f]triazin-4-one analogues which are substituted in the 7-position by a substituted phenyl ring, being ligands for GABAA receptors and accordingly of benefit in the therapy of deleterious neurological disorders.
    Type: Grant
    Filed: May 18, 2004
    Date of Patent: July 5, 2005
    Assignee: Merck Sharp & Dohme Ltd.
    Inventor: Simon Charles Goodacre
  • Patent number: 6900215
    Abstract: A class of 3-phenylimidazo[1,2-?]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 ?2 and/or ?3 and/or ?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: Grant
    Filed: March 19, 2002
    Date of Patent: May 31, 2005
    Assignee: Merck Sharp & Dohme Ltd.
    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: 6887885
    Abstract: A compound of formula I, 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 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 including the compound and methods for treating anxiety, convulsions and cognitive disorders are disclosed.
    Type: Grant
    Filed: October 30, 2003
    Date of Patent: May 3, 2005
    Assignee: Merck Sharp & Dohme Ltd
    Inventor: Simon Charles Goodacre
  • Patent number: 6872731
    Abstract: A class of 3-phenylimidazo[1,2-a]pyridine 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, are selective ligands for GABAA receptors, in particular having high affinity for the ?2 and/or ?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: Grant
    Filed: May 23, 2002
    Date of Patent: March 29, 2005
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: James Michael Crawforth, Simon Charles Goodacre, Timothy Harrison, David James Hallett, Andrew Pate Owens, Michael Rowley, Martin Richard Teall
  • Publication number: 20040235844
    Abstract: The present invention relates to imidazo[2,1-f]triazin-4-one analogues which are substituted in the 7-position by a substituted phenyl ring, being ligands for GABAA receptors and accordingly of benefit in the therapy of deleterious neurological disorders.
    Type: Application
    Filed: May 18, 2004
    Publication date: November 25, 2004
    Inventor: Simon Charles Goodacre
  • Publication number: 20040192692
    Abstract: The present invention provides a compound of formula I, or an N-oxide thereof or a pharmaceutically acceptable salt thereof: 1
    Type: Application
    Filed: January 30, 2004
    Publication date: September 30, 2004
    Inventors: Wesley Peter Blackaby, Simon Charles Goodacre, David James Hallett, Andrew Jennings, Richard Thomas Lewis, Leslie Joseph Street, Kevin Wilson
  • Publication number: 20040132767
    Abstract: A compound of formula I, or a pharmaceutically acceptable salt thereof: 1
    Type: Application
    Filed: October 30, 2003
    Publication date: July 8, 2004
    Inventor: Simon Charles Goodacre
  • Publication number: 20040092533
    Abstract: A class of imidazo[1,2-&agr;]pyrimidine derivatives, substituted at the 3-position by an optionally substituted five-membered or six-membered heteroaromatic ring, 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: September 19, 2003
    Publication date: May 13, 2004
    Inventors: Wesley Peter Blackaby, Jose Luis Castro Pineiro, Mark Stuart Chambers, Simon Charles Goodacre, David James Hallett, Philip Jones, Richard Thomas Lewis, Angus Murray MacLeod, Robert James Maxey, Kevin William Moore, Leslie Joseph Street
  • Patent number: 6730681
    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 &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: Grant
    Filed: June 14, 2002
    Date of Patent: May 4, 2004
    Assignee: Merck Sharp & Dohme Ltd.
    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: 20040019057
    Abstract: A class of imidazo[1,2-&agr;]pyrazine analogues substituted in the 3-position by a substituted phenyl ring, being selective ligands for GABAA receptors which interact more favourably with the &agr;2 and/or &agr;3 subunit than with the &agr;1 subunit, are accordingly of benefit in the treatment and/or prevention of a variety of disorders of the central nervous system, including anxiety and convulsions, with a reduced propensity to cause sedation.
    Type: Application
    Filed: January 22, 2003
    Publication date: January 29, 2004
    Inventors: Simon Charles Goodacre, David James Hallett, Leslie Joseph Street
  • Patent number: 6642229
    Abstract: A class of 3-phenylimidazo(1,2-a)pyrimidine derivatives (of Formula I, or salt or prodrug thereof: I) wherein 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.
    Type: Grant
    Filed: November 22, 2002
    Date of Patent: November 4, 2003
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Wesley Peter Blackaby, Simon Charles Goodacre, David James Hallett, Andrew Jennings, Richard Thomas Lewis, Kevin William Moore, Leslie Joseph Street
  • Publication number: 20030176449
    Abstract: A class of 3-phenylimidazo(1,2-&agr;) pyrimidine derivatives (of Formula I, or salt or prodrug thereof: I) wherein 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.
    Type: Application
    Filed: November 22, 2002
    Publication date: September 18, 2003
    Inventors: Wesley Peter Blackaby, Simon Charles Goodacre, David James Hallett, Andrew Jennings, Richard Thomas Lewis, Kevin William Moore, 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: 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
  • Publication number: 20020188000
    Abstract: A class of 3-phenylimidazo[1,2-a]pyridine 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, 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: May 23, 2002
    Publication date: December 12, 2002
    Inventors: James Michael Crawforth, Simon Charles Goodacre, Timothy Harrison, David James Hallett, Andrew Pate Owens, Michael Rowley, Martin Richard Teall