Patents Assigned to Merck Sharp & Dohme Ltd.
  • Spiro-azacyclic derivatives and their use as therapeutic agents
    Patent number: 6225320
    Abstract: Substituted spiro-azacyclic derivatives of structural formula I are tachykinin receptor antagonists of use, for example, in the treatment of pain, inflammation, migraine, emesis and posttherpetic neuralgia Wherein A is a pyridyl, X is —CH2—, Y is —CH2— or —CH═ and q is 2.
    Type: Grant
    Filed: November 18, 1999
    Date of Patent: May 1, 2001
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Janusz Jozef Kulagowski, Piotr Antoni Raubo, Christopher John Swain, Christopher George Thomson
  • Aminocyclohexane derivatives as 5-HT receptor agonists
    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
  • Indole and indoline derivatives as 5-HT6 selective ligands
    Patent number: 6187805
    Abstract: Three classes of indole and indoline derivatives are disclosed as ligands selective for the 5-HT6 receptors, and hence of value in the treatment or prevention of CNS disorders, including Alzheimer's disease, Parkinson's disease, schizophrenia, depression and anxiety. A particular class, 1-substituted-4-(&ohgr;-N,N-dialkyl-aminoalkyl)indoles, are claimed as novel compounds.
    Type: Grant
    Filed: September 9, 1999
    Date of Patent: February 13, 2001
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Jose Luis Castro Pineiro, George Mc Allister, Michael Geoffrey Neil Russel
  • Antipsychotic use of triazolo-pyridazine derivatives
    Patent number: 6174886
    Abstract: A class of substituted or 7,8-ring fused 1,2,4-triazolo[4,3-b]pyridazine derivatives, possessing an optionally substituted cycloalkyl, phenyl or heteroaryl substituent at the 3-position and a substituted alkoxy moiety at the 6-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 psychotic disorders including schizophrenia.
    Type: Grant
    Filed: November 12, 1998
    Date of Patent: January 16, 2001
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Jose Luis Castro Pineiro, Ruth McKernan, Paul John Whiting
  • Spiro-azacyclic derivatives and their use as therapeutic agents
    Patent number: 6172077
    Abstract: The present invention is directed to substituted spiro-azacyclic derivatives of the formula (I): (wherein R1, R2, R3, R4, R5, R6, R9, R10, X, Y, p and q are defined herein) which are tachykinin antagonists and are useful, for example, in the treatment or prevention of pain, inflammation, migraine, emesis and postherpetic neuralgia.
    Type: Grant
    Filed: October 22, 1999
    Date of Patent: January 9, 2001
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Neil Roy Curtis, Jason Matthew Elliott, Gregory John Hollingworth, Philip Stephen Jackson, Janusz Jozef Kulagowski, Eileen Mary Seward, Christopher John Swain, Brian John Williams
  • Diazabicyclo-octane derivatives as 5-HT receptor ligands
    Patent number: 6150391
    Abstract: Compounds having formula I, or pharmaceutically acceptable salts or prodrugs thereof: ##STR1## are selective agonists of the 5-HT.sub.1D.alpha. receptor and are useful in the treatment of migraine and associated conditions.
    Type: Grant
    Filed: July 21, 1998
    Date of Patent: November 21, 2000
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Jose Luis Castro Pineiro, Michael Geoffrey Russell
  • Use of a tachykinin antagonist and a muscarinic antagonist and/or an antihistamine to treat motion sickness
    Patent number: 6140324
    Abstract: The present invention relates to the use of a tachykinin antagonist and a muscarinic antagonist and/or an antihistamine for the treatment or prevention of motion sickness. There is also provided pharmaceutical compositions and products comprising a tachykinin antagonist and a muscarinic antagonist and/or an antihistamine.
    Type: Grant
    Filed: December 18, 1997
    Date of Patent: October 31, 2000
    Assignee: Merck Sharp & Dohme Ltd.
    Inventor: Frederick David Tattersall
  • Azetidine, pyrrolidine and piperidine derivatives as 5-HT receptor agonists
    Patent number: 6140347
    Abstract: A class of compounds of formula (I) wherein Z, E, Q, T, U, V, W, M, R.sup.1, R.sup.7 and R.sup.8 are as defined herein; are selective agonists of 5-HT.sub.1 -like receptors, being potent agonists of the human 5-HT.sub.1D.alpha. receptor subtype whilst possessing at least a 10-fold selective affinity for the 5-HT.sub.1D.alpha. receptor subtype relative to the 5-HT.sub.1D.beta. 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-HT.sub.1D receptors is indicated, whilst eliciting fewer side-effects, notably adverse cardiovascular events, than those associated with non-subtype-selective 5-HT.sub.1D receptor agonists.
    Type: Grant
    Filed: October 14, 1998
    Date of Patent: October 31, 2000
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Jose Luis Castro Pineiro, Andrew Madin, Joseph George Neduvelil, Graham Andrew Showell, Leslie Joseph Street, Monique Bodil Van Niel
  • 1-piperidinyl-propan-2-derivatives and their use as therapeutic agents
    Patent number: 6136824
    Abstract: The present invention relates compounds of the formula (I): ##STR1## wherein R.sup.1 and R.sup.2 each independently represents a phenyl group optionally substituted by a variety of substituents;R.sup.3 represents a variety of substituents;R.sup.4, R.sup.5, R.sup.6, and R.sup.7 each independently represents hydrogen or C.sub.1-6 alkyl;A represents --O-- or --S--;B represents --O--, --S--, --NR.sup.a -- or --CHR.sup.a --; andn is zero, 1, 2, 3, 4 or 5;or a pharmaceutically acceptable salt or a prodrug thereof.The compounds are of particular use in the treatment or prevention of depression, anxiety, pain, inflammation, migaine, emesis or postherpetic neuralgia.
    Type: Grant
    Filed: February 22, 2000
    Date of Patent: October 24, 2000
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Angus Murray MacLeod, Christopher John Swain, Monique Bodil van Niel
  • Chemical synthesis of a chiral 1,4-oxazin-2-one
    Patent number: 6130331
    Abstract: The present invention relates to a process for the preparation of substantially pure N-((S)-(-)-.alpha.-methylbenzyl)-3-(S)-(4-fluorophenyl)-1,4-oxazin-2-one hydrochloride, which comprises selectively crystallising the (S,S)-diastereomer as the hydrochloride salt from a mixture of the (S,R)- and (S,S)-diastereomers in an organic solvent, and collecting the resultant crystalline product.
    Type: Grant
    Filed: September 8, 1999
    Date of Patent: October 10, 2000
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Michael Stewart Ashwood, Ian Frank Cottrell, Brian Christopher Bishops, John Simon Edwards
  • Human NMDA R2A receptor subunit and isoforms of the human NMDA-R1 receptor subunit and encoding cDNAs
    Patent number: 6130058
    Abstract: The present invention relates to a stably co-transfected eukaryotic cell line that expresses an N-methyl-D-aspartate (NMDA) receptor, particularly a human NMDA receptor, which receptor comprises at least one R1 subunit isoform, or at least one R1 subunit isoform and one or two R2 subunits. Additionally, the cell line can be used to design and develop NMDA receptor subtype-selective compounds. The invention also relates to cloning of novel cDNA sequences encoding the human NMDAR 2A subunit and various isoforms of the human NMDA R1 subunit.
    Type: Grant
    Filed: May 10, 1995
    Date of Patent: October 10, 2000
    Assignee: Merck Sharpe & Dohme Ltd.
    Inventors: Beatrice Le Bourdelles, Janice Ann Myers, Paul John Whiting
  • Spiro-ketal derivatives and their use as therapeutic agents
    Patent number: 6127365
    Abstract: The present invention is directed to compounds of the formula (I): ##STR1## (wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.9a, R.sup.9b, m and n are as defined herein) which are tachykinin antagonists and which are particularly useful in the treatment of pain, inflammation, migraine, emesis and postherpetic neuralgia.
    Type: Grant
    Filed: August 13, 1998
    Date of Patent: October 3, 2000
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Jason Matthew Elliott, Fintan Kelleher, Christopher John Swain
  • Azetidine, pyrrolidine and piperidine derivatives as 5-HT.sub.1D receptor agonists
    Patent number: 6127388
    Abstract: A class of substituted azetidine, pyrrolidine and piperidine derivatives of Formula I are selective agonists of 5-HT.sub.1 -like receptors, being potent agonists of the human 5-HT.sub.1D.alpha. receptor subtype whilst possessing at least a 10-fold selective affinity for the 5-HT.sub.1D.alpha. receptor subtype relative to the 5-HT.sub.1D.beta. 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-HT.sub.1D receptors is indicated, whilst eliciting fewer side-effects, notably adverse cardiovascular events, than those associated with non-subtype-selective 5-HT.sub.1D receptor agonists.
    Type: Grant
    Filed: October 26, 1998
    Date of Patent: October 3, 2000
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Sylvie Bourrain, Angus Murray MacLeod, Graham Andrew Showell, Leslie Joseph Street
  • Use of a NK-1 receptor antagonist and an antidepressant and/or an anti-anxiety agent
    Patent number: 6117855
    Abstract: The present invention relates to the treatment or prevention of depression and/or anxiety by the administration of a combination of CNS-penetrant NK-1 receptor antagonists and an antidepressant or anti-anxiety agent.
    Type: Grant
    Filed: December 19, 1997
    Date of Patent: September 12, 2000
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Emma Joanne Carlson, Nadia Melanie Rupniak
  • Use of NK-1 receptor antagonists for treating major depressive disorders with anxiety
    Patent number: 6114315
    Abstract: The present invention provides methods for the treatment or prevention of major depressive disorder with anxiety without concomitant therapy with other anti-depressant or anti-anxiety agents which comprises 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 5, 2000
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Raymond Baker, Neil Roy Curtis, Jason Matthew Elliott, Timothy Harrison, Gregory John Hollingworth, Philip Stephen Jackson, Janusz Jozef Kulagowski, Nadia Melanie Rupniak, Eileen Mary Seward, Christopher John Swain, Brian John Williams
  • Neuroprotective use of triazolo-pyridazine derivatives
    Patent number: 6107296
    Abstract: A class of substituted 7,8-ring fused 1,2,4-triazolo[4,3-b]pyridazine derivatives as shown in Formula I, possessing an optionally substituted cycloalkyl, phenyl or heteroaryl substituent at the 3-position and a substituted alkoxy moiety at the 6-position, are selective ligands for GABA.sub.A receptors, in particular having high affinity for the .alpha.2 and/or .alpha.3 subunit therof, and are accordingly of benefit in the treatment and/or prevention of neurodegeneration arising from cerebral ischemia.
    Type: Grant
    Filed: December 7, 1998
    Date of Patent: August 22, 2000
    Assignee: Merck Sharp & Dohme, Ltd.
    Inventor: Jose Luis Castro Pineiro
  • Diazabicyclooctane derivatives having selective 5-HT.sub.1Dalpha agonist activity
    Patent number: 6107321
    Abstract: A class of 3-substituted 3,7-diazabicyclo[3.3.0]octane derivatives, further substituted at the 7-position by an optionally substituted alkenyl, alkynyl, arylcarbonyl, aryl-alkyl or heteroaryl-alkyl moiety, are selective agonists of 5-HT.sub.1 -like receptors, being potent agonists of the human 5-HT.sub.1D.alpha. receptor subtype whilst possessing at least a 10-fold selective affinity for the 5-HT.sub.1D.alpha. receptor subtype relative to the 5-HT.sub.1D.beta. 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-HT.sub.1D receptors is indicated, whilst eliciting fewer side-effects, notably adverse cardiovascular events, than those associated with non-subtype-selective 5-HT.sub.1D receptor agonists.
    Type: Grant
    Filed: March 9, 1998
    Date of Patent: August 22, 2000
    Assignee: Merck Sharp & Dohme Ltd.
    Inventor: Andrew Madin
  • Use of NK-1 receptors antagonists for treating schizophrenic disorders
    Patent number: 6100256
    Abstract: The present invention provides a method for the treatment or prevention of schizophrenic disorders using 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: August 8, 2000
    Assignee: Merck Sharp & Dohme Ltd.
    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
  • Use of NK-1 receptor antagonists for treating amnestic disorders
    Patent number: 6096729
    Abstract: The present invention provides methods for the treatment or prevention of amnestic disorders which comprises oral administration of an orally active, long acting, CNS-penetrant NK-1 receptor antagonist.
    Type: Grant
    Filed: December 1, 1997
    Date of Patent: August 1, 2000
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Raymond Baker, Neil Roy Curtis, Jason Matthew Elliott, Timothy Harrison, Gregory John Hollingworth, Philip Stephen Jackson, Janusz Jozef Kulagowski, Nadia Melanie Rupniak, Eileen Mary Seward, Christopher John Swain, Brian John Williams
  • 3-benzylaminopiperidines as tachykinin receptor antagonists
    Patent number: 6096766
    Abstract: The present invention relates to certain 3-benzylaminopiperidines which are tachykinin receptor antagonists and are useful in the treatment or prevention of pain, inflammation, migraine, emesis and postherpetic neuralgia.
    Type: Grant
    Filed: June 9, 1998
    Date of Patent: August 1, 2000
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Raymond Baker, Jason Matthew Elliott, Christopher John Swain