Abstract: Histone deacetylase inhibition provides a target for identifying potential antiprotozoal compounds. Histone deacetylase inhibitors are useful as therapeutic agents against protozoal infections.
Type:
Grant
Filed:
April 22, 1999
Date of Patent:
August 6, 2002
Assignee:
Merck & Co.
Inventors:
Paula M. Dulski, Robert W. Myers, Anne M. Gumett, Sandra J. Rattray, Dennis M. Schmatz
Abstract: The present invention relates to a method of enhancing cognition without producing convulsions which method comprises administering to a subject in need thereof a cognition enhancing amount of a compound which is a GABAa selective alpha5 receptor inverse agonist.
Abstract: 2-lithio-5-halopyridine is formed as a predominant component of a reaction mixture by reacting BuLi with 2,5-dihalopyridine in a non-coordinating solvent.
Type:
Grant
Filed:
February 27, 2001
Date of Patent:
July 16, 2002
Assignees:
Merck & Co., Inc., Merck Frosst Canada & Co
Abstract: There are disclosed compounds of formula (I)
and pharmaceutically acceptable salts thereof which exhibit utility for the treatment of cytokine mediated diseases such as arthritis.
Type:
Grant
Filed:
June 12, 2000
Date of Patent:
June 11, 2002
Assignee:
Merck & Co., Inc.
Inventors:
Nigel J. Liverton, David A. Claremon, John W. Butcher, Cory R. Theberge
Abstract: A pharmaceutical product comprising an SSRI and a non-sedating anxiolytic compound, which is a modulator of the benzodiazepine binding site of the human GABAA receptor, having a binding affinity for the &agr;3 subunit of the human GABAA receptor of 10 nM or less, which elicits at least a 40% potentiation of the GABA EC20 response in stably transfected recombinant cell lines expressing the &agr;3 subunit of &agr;3 and which elicits at most a 30% potentiation of the GABA EC20 response in stably transfected cell lines expressing the &agr;1 subunit of the human GABAA receptor is disclosed for simultaneous, separate or sequential administration.
Abstract: 9a-Azalides, and pharmaceutical compositions containing them, are useful in the treatment and prevention of bacterial respiratory and enteric infections in livestock animals, particularly in cattle and swine.
Type:
Grant
Filed:
May 11, 2000
Date of Patent:
January 15, 2002
Assignee:
Merck & Co., Inc.
Inventors:
Helmut Kropp, Daniel Farrington, Jeffrey Clark, Ronald Ratcliffe, Robert Wilkening
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
Abstract: Compounds represented by formula I:
or a pharmaceutically acceptable salt or hydrate thereof, are disclosed.
Pharmaceutical compositions and methods of treatment are also included.
Type:
Grant
Filed:
May 4, 2000
Date of Patent:
November 20, 2001
Assignee:
Merck & Co., Inc.
Inventors:
Christopher F. Claiborne, Nigel J. Liverton, Brian Libby, Neil R. Curtis, Janusz Kulagowski
Abstract: 1,2,4-triazolo[4,3-b]pyridazine derivatives, represented by
wherein Z represents an optionally substituted tetrahydropyridinyl substituent, 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.
Abstract: In accordance with the present invention, a novel class of substituted aryl compounds (containing ether, ester, amide, ketone or thioether substitution) that promote the release of ligands involved in neurotransmission have been discovered. In a particular aspect, compounds of the present invention are capable of modulating acetylcholine receptors. The compounds of the present invention are capable of displacing one or more acetylcholine receptor ligands, e.g., 3H-nicotine, from mammalian neuronal membrane binding sites. Invention compounds may act as agonists, partial agonists, antagonists or allosteric modulators of acetylcholine receptors.
Abstract: An assay for emetic activity among inhibitors of type 4 phosphodiesterase (PDE 4) is disclosed. The assay comprises:
(A) administering to a test mammal an anesthetic compound in an amount sufficient to cause an anesthetic effect;
(B) administering to the test mammal a test compound that has PDE 4 inhibitory activity;
(C) observing the test mammal for changes in the anesthetic effect, and
(D) correlating any change in the anesthetic effect observed in the anesthetized test mammal to a standard.
Type:
Grant
Filed:
February 24, 2000
Date of Patent:
November 13, 2001
Assignee:
Merck Frosst Canada & Co.
Inventors:
Annette Robichaud, Chantal Savoie, Chi Chung Chang
Abstract: The invention encompasses the novel compound of Formula I useful in the treatment of diseases, including asthma, by raising the level of cyclic adenosine-3′,5′-monophosphate (cAMP) through the inhibition of phosphodiesterase IV (PDE 4).
The invention also encompasses pharmaceutical compositions and methods for treatment.
Type:
Grant
Filed:
April 17, 2000
Date of Patent:
November 13, 2001
Assignee:
Merck Frosst Canada & Co.
Inventors:
Richard Frenette, Yves Ducharme, Sylvie Prescott
Abstract: The present invention relates to novel nodulosporic acid derivatives, which are acaricidal, antiparasitic, insecticidal and anthelmintic agents.
Type:
Grant
Filed:
March 17, 1999
Date of Patent:
April 24, 2001
Assignee:
Merck & Co., Inc.
Inventors:
Peter T. Meinke, Thomas L. Shih, Michael H. Fisher
Abstract: The invention encompasses compounds of Formula I useful in the treatment of diseases, including asthma, by raising the level of cyclic adenosine-3′,5′-monophosphate (cAMP) through the inhibition of phosphodiesterase IV (PDE IV).
The invention also encompasses certain pharmaceutical compositions and methods for treatment of diseases by inhibition of PDE IV, resulting in an elevation of cAMP, comprising the use of compounds of Formula I.
Type:
Grant
Filed:
February 25, 2000
Date of Patent:
March 20, 2001
Assignee:
Merck Frosst Canada & Co.
Inventors:
Richard Friesen, Yvbes Ducharme, Daniel Dube, Yves Girard, Richard Frenette, Chun Li, Marc Blouin, Nathalie Chauret, Laird Trimble
Abstract: Substituted 1,2,4-Triazolo[3,4-A]phthalazine derivatives are GABA Alpha 5 ligands and are represented by the formula
Type:
Grant
Filed:
November 12, 1998
Date of Patent:
March 13, 2001
Assignee:
Merck Sharp & Dohme Limited
Inventors:
William Robert Carling, Tamara Ladduwahetty, Angus Murray MacLeod, Kevin John Merchant, Kevin William Moore, Francine Sternfeld, Leslie Joseph Street
Abstract: The invention encompasses the novel compound of Formula I useful in the treatment of diseases, including asthma, by raising the level of cyclic adenosine-3′,5′-monophosphate (cAMP) through the inhibition of phosphodiesterase IV (PDE 4).
or a pharmaceutically acceptable salt or hydrate thereof.
The invention also encompasses pharmaceutical compositions and methods for treatment.
Type:
Grant
Filed:
April 17, 2000
Date of Patent:
March 13, 2001
Assignee:
Merck Frosst Canada & Co.
Inventors:
Bernard Cote, Richard Friesen, Richard Frenette, Mario Girard, Yves Girard, Cedrickx Godbout, Daniel Guay, Pierre Hamel, Marc Blouin, Yves Ducharme, Sylvie Prescott
Abstract: In accordance with the present invention, there is provided a class of pyridine compounds which are modulators of acetylcholine receptors. The compounds of the invention displace acetylcholine receptor ligands from their binding sites.
Type:
Grant
Filed:
December 22, 1998
Date of Patent:
February 27, 2001
Assignee:
Merck & Co., Inc.
Inventors:
Nicholas D. Cosford, Jean-Michel Vernier
Abstract: Pyrazolo[4,3-c]pyridazin-3-one analogues, represented by
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.
Abstract: The invention encompasses the novel compound of Formula I useful in the treatment of diseases, including asthma, by raising the level of cyclic adenosine-3′,5′-monophosphate (cAMP) through the inhibition of phosphodiesterase IV (PDE 4).
The invention also encompasses pharmaceutical compositions and methods for treatment.
Type:
Grant
Filed:
March 14, 2000
Date of Patent:
January 30, 2001
Assignee:
Merck Frosst Canada & Co.
Inventors:
Richard Frenette, Richard Friesen, Mario Girard, Yves Girard, Cedrickx Godbout, Daaniel Guay, Pierre Hamel, Helene Perrier