Patents by Inventor Jose Luis Castro Pineiro

Jose Luis Castro Pineiro 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: 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
  • Patent number: 6489343
    Abstract: The present invention relates to compounds of the formula (I): wherein R1 is fluorine or trifluoromethyl; R2 is fluorine or trifluoromethyl; R3 is methyl or hydroxymethyl; R4 represents a variety of substituents; and n is zero, 1 or 2; and pharmaceutically acceptable salts 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: August 20, 2001
    Date of Patent: December 3, 2002
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Jose Luis Castro Pineiro, Simon Neil Owen, Eileen Mary Seward, Christopher John Swain, Brian John Williams
  • Patent number: 6486153
    Abstract: A class of tryptamine analogues bearing an optionally substituted phenyl nucleus at the 2-position are selective antagonists of the human 5-HT2A receptor and are therefore useful as pharmaceutical agents, especially in the treatment and/or prevention of adverse neurological conditions, including psychotic disorders such as schizophrenia.
    Type: Grant
    Filed: March 3, 2000
    Date of Patent: November 26, 2002
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Jose Luis Castro Pineiro, Steven Michael Hutchins, Stephen John Lewis, Michael Rowley, Adrian Leonard Smith, Graeme Irvine Stevenson
  • 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
  • Publication number: 20020035132
    Abstract: The present invention relates to compounds of the formula (I): 1
    Type: Application
    Filed: August 20, 2001
    Publication date: March 21, 2002
    Inventors: Jose Luis Castro Pineiro, Simon Neil Owen, Eileen Mary Seward, Christopher John Swain, Brian John Williams
  • 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: 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: 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
  • 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
  • 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
  • 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
  • Patent number: 6110915
    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 thereof, and are accordingly of benefit in the treatment and/or prevention of emesis.
    Type: Grant
    Filed: December 8, 1998
    Date of Patent: August 29, 2000
    Assignee: Merck & Co., Inc.
    Inventors: Jose Luis Castro Pineiro, Frederick David Tattersall
  • 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
  • Patent number: 6063783
    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 thereof, and are accordingly of benefit in the treatment and/or prevention of pain.
    Type: Grant
    Filed: December 10, 1998
    Date of Patent: May 16, 2000
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Jose Luis Castro Pineiro, Raymond George Hill
  • Patent number: 6051572
    Abstract: A class of azetidine, pyrrolidine and piperidine derivatives, substituted by inter alia a phenylmorpholinyl, phenylpiperidinyl or benzimidazolone 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: April 28, 1998
    Date of Patent: April 18, 2000
    Assignee: Merck Sharp & Dohme Ltd.
    Inventor: Jose Luis Castro Pineiro
  • Patent number: 6048878
    Abstract: A compound of formula (I), or a salt or prodrug thereof, is described, wherein G is attached at position 3 or 4 of the piperidine ring and represents halogen or C.sub.1-6 alkoxy; R1 represents C.sub.3-6 alkenyl, C.sub.3-6 alkynyl, aryl(C.sub.1-6)alkyl or heteroaryl (C.sub.1-6)alkyl, any of which groups may be optionally substituted; processes for its preparation and its use in therapy, particularly in the treatment of migraine.
    Type: Grant
    Filed: May 13, 1998
    Date of Patent: April 11, 2000
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Jose Luis Castro Pineiro, Ian James Collins, Angus Murray MacLeod, Christopher Richard Moyes, Michael Rowley, Graham Andrew Showell
  • Patent number: 6025374
    Abstract: A class of substituted azetidine, pyrrolidine and piperidine derivatives 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: May 28, 1997
    Date of Patent: February 15, 2000
    Assignee: Merck Sharp & Dohme, Ltd.
    Inventors: Jose Luis Castro Pineiro, Caroline Henry, Victor Giulio Matassa, Austin John Reeve, Francine Sternfeld, Leslie Joseph Street
  • Patent number: 5998440
    Abstract: A class of substituted azetidine, pyrrolidine and piperidine derivatives, linked by a fluoro-substituted alkylene chain to a fused bicyclic heteroaromatic moiety such as indolyl, are selective agonists of 5-HT.sub.1 -like receptors, being potent agonists of the human 5-HT.sub.1D.alpha. receptor subtype while 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, while eliciting fewer side-effects, notably adverse cardiovascular events, than those associated with non-subtype-selective 5-HT.sub.1D receptor agonists.
    Type: Grant
    Filed: May 8, 1998
    Date of Patent: December 7, 1999
    Assignee: Merck Sharpe & Dohme Ltd.
    Inventors: Jose Luis Castro Pineiro, Angus Murray MacLeod, Monique Bodil Van Niel
  • Patent number: 5977116
    Abstract: A class of N-substituted piperazine, piperidine and tetrahydropyridine derivatives, linked by a fluoro-substituted alkylene chain to a fused bicyclic heteroaromatic moiety such as indolyl, and further substituted at the 4-position by an optionally substituted alkenyl, alkynyl, 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 recptor agonists.
    Type: Grant
    Filed: May 12, 1998
    Date of Patent: November 2, 1999
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Jose Luis Castro Pineiro, Angus Murray MacLeod, Michael Rowley, Monique Bodil Van Niel