Abstract: The present invention is directed to compounds of Formula (I): where variables A1, A2, B, J, K, m, n, R4, R5a, R5b, R5c and X are as defined herein useful as antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, such as headache, migraine and cluster headache. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.
Type:
Grant
Filed:
September 6, 2005
Date of Patent:
August 2, 2011
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Ian M. Bell, Craig A. Stump, Cory R. Theberge
Abstract: Compounds of formula I: inhibit gamma-secretase and hence find use in treatment or prevention of Alzheimer's disease.
Type:
Grant
Filed:
May 7, 2004
Date of Patent:
August 12, 2008
Assignee:
Merck Sharp & Dohme Ltd.
Inventors:
Kevin Dinnell, Karl Richard Gibson, Timothy Harrison, Richard Alexander Jelley, Alan John Nadin, Paul Joseph Oakley, Andrew Pate Owens, Duncan Edward Shaw, Brian John Williams
Abstract: The present invention encompasses compounds of Formula I: (I) or pharmaceutically acceptable salts or hydrates thereof, which are useful as selective glucocorticoid receptor ligands for treating a variety of autoimmune and inflammatory diseases or conditions. Pharamaceutical compositions and methods of use are also included.
Type:
Grant
Filed:
April 8, 2003
Date of Patent:
October 16, 2007
Assignee:
Merck & Co., Inc.
Inventors:
Amjad Ali, James M. Balkovec, Donald W. Graham, Christopher F. Thompson, Nazia Quraishi
Abstract: The present invention encompasses compounds of Formula (I): as well as the pharmaceutically acceptable salts and hydrates thereof. The compounds are useful for treating immune mediated diseases and conditions, such as bone marrow, organ and tissue transplant rejection. Pharmaceutical compositions and methods of use are included.
Type:
Grant
Filed:
December 16, 2003
Date of Patent:
May 22, 2007
Assignee:
Merck & Co., Inc.
Inventors:
George A. Doherty, Jeffrey J. Hale, Sander G. Mills
Abstract: The present invention is directed to certain hydroisoindoline compounds which are useful as neurokinin-1 (NK-1) receptor antagonists, and inhibitors of tachykinin and in particular substance P. The invention is also concerned with pharmaceutical formulations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including emesis, urinary incontinence, depression, and anxiety.
Type:
Grant
Filed:
January 26, 2005
Date of Patent:
May 15, 2007
Assignee:
Merck & Co., Inc.
Inventors:
Jaime Lynn Bunda, Robert J. DeVita, Jinlong Jiang, Sander G. Mills
Abstract: The present invention encompasses compounds of Formula I: as well as the pharmaceutically acceptable salts and hydrates thereof. The compounds are useful for treating immune mediated diseases and conditions, such as bone marrow, organ and tissue transplant rejection. Pharmaceutical compositions and methods of use are included.
Type:
Grant
Filed:
June 16, 2003
Date of Patent:
April 3, 2007
Assignee:
Merck & Co., Inc.
Inventors:
Weirong Chen, Jeffrey J. Hale, Zhen Li, Christopher L. Lynch, Sander G. Mills, William E. Neway, III
Abstract: The invention encompasses novel compounds of Formula I, which are nitric oxide-releasing prodrugs of diaryl-2-(5H) furanones useful in the treatment of cyclooxygenase-2 mediated diseases. The invention also encompasses certain pharmaceutical compositions and methods for treatment of cyclooxygenase-2 mediated diseases comprising the use of compounds of Formula I.
Type:
Grant
Filed:
July 24, 2003
Date of Patent:
April 3, 2007
Assignee:
Merck Frosst Company
Inventors:
Carl Berthelette, Nicholas Lachance, Lianhai Li, Claudio Sturino, Zhaoyin Wang, Robert N. Young, Claude Dufresne
Abstract: The present invention is directed to certain lactam compounds which are useful as neurokinin-1 (NK-1) receptor antagonists, and inhibitors of tachykinin and in particular substance P. The invention is also concerned with pharmaceutical formulations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including emesis, urinary incontinence, depression, and anxiety.
Type:
Grant
Filed:
May 23, 2005
Date of Patent:
March 27, 2007
Assignee:
Merck & Co., Inc.
Inventors:
Paul E. Finke, Laura C. Meurer, Sander G. Mills
Abstract: The invention encompasses novel compounds of Formula I, which are nitric oxide-releasing prodrugs of diaryl-2-(5H) furanones useful in the treatment of cyclooxygenase-2 mediated diseases. The invention also encompasses certain pharmaceutical compositions and methods for treating cyclooxygenase-2 mediated diseases comprising the use of compounds of Formula I. The above compounds may be used as a combination therapy with low-dose aspirin to treat chronic cyclooxygenase-2 mediated diseases or conditions while also reducing the risk of thrombotic cardiovascular events.
Type:
Grant
Filed:
March 1, 2004
Date of Patent:
January 30, 2007
Assignee:
Merck Frosst Company
Inventors:
Carl Berthelette, Lianhai Li, Claudio Sturino, Zhaoyin Wang
Abstract: The invention encompasses the novel compound of Formula I as well as a method of treating COX-2 mediated diseases comprising administration to a patient in need of such treatment of a non-toxic therapeutically effective amount of a compound of Formula I. The invention also encompasses certain pharmaceutical compositions for treatment of COX-2 mediated diseases comprising compounds of Formula I.
Type:
Grant
Filed:
August 11, 2004
Date of Patent:
June 13, 2006
Assignee:
Merck Frosst Canada Ltd.
Inventors:
Daniel Dube, Rejean Fortin, Richard Friesen, Zhaoyin Wang, Jacques Yves Gauthier
Abstract: Polymorphic, amorphous and hydrated forms of the title compound having the following structure: are disclosed. The compound is a potent and selective cyclooxygenase-2 (COX-2)inhibitor.
Abstract: The invention encompasses the novel compound of Formula I as well as a method of treating COX-2 mediated diseases comprising administration to a patient in need of such treatment of a non-toxic therapeutically effective amount of a compound of Formula I.
The invention also encompasses certain pharmaceutical compositions for treatment of COX-2 mediated diseases comprising compounds of Formula I.
Type:
Grant
Filed:
March 24, 2003
Date of Patent:
November 2, 2004
Assignee:
Merck Frosst Canada and Co.
Inventors:
Daniel Dube, Rejean Fortin, Richard Friesen
Abstract: This invention encompasses a pharmaceutical composition comprising the compound of formula A:
in combination with a pharmaceutically acceptable carrier, said compound being comprised of about 1-50%, 1-20% or 1-10% of the polymorphic form which is designated Form V and the remainder of the compound being comprised of at least one polymorphic form selected from the group consisting of: Form I, Form II, Form III and Form IV.
Type:
Grant
Filed:
September 21, 2001
Date of Patent:
October 5, 2004
Assignee:
Merck & Co., Inc.
Inventors:
Loius S. Crocker, Ian W. Davies, Richard G. Osifchin, Andrew Kotliar
Abstract: Compounds represented by formula I:
as well as pharmaceutically acceptable salts, esters, N-oxides and hydrates thereof are disclosed. Pharmaceutical compositions and methods of use are also included. The compounds are active against the caspase-3 enzyme, and thus are useful to treat caspase-3 mediated diseases and conditions.
Type:
Grant
Filed:
July 25, 2002
Date of Patent:
March 2, 2004
Assignee:
Merck & Co., Inc.
Inventors:
Yongxin Han, Andre Giroux, Robert Zamboni, Daniel J. McKay, Christopher I. Bayly, Erich L. Grimm, John Colucci
Abstract: This invention encompasses the Form V polymorph of Compound A of structural formula:
which is useful in the treatment of cyclooxygenase-2 mediated diseases. The invention encompasses certain pharmaceutical compositions for treatment of cyclooxygenase-2 mediated diseases comprising the Form V polymorph of Compound A. The invention also encompasses a process for synthesizing the Form V polymorph of Compound A.
Type:
Grant
Filed:
January 14, 2003
Date of Patent:
January 6, 2004
Assignee:
Merck & Co., Inc.
Inventors:
Louis S. Crocker, Ian W. Davies, Richard G. Osifchin, Andrew Kotliar
Abstract: This invention is directed to a method of retarding or preventing the transformation of a colonic adenoma to a colonic adenocarcinoma comprising the administration to a patient with FAP or a patient with one or more of said adenomas a non-toxic therapeutically effective amount of NSAID, said amount effective to inhibit the PGHS-2 in said adenoma. The preferred method comprises the administration of a specific PGHS-2 inhibiting agent as defined herein.
Abstract: This invention encompasses a method for the treatment or prevention of prostaglandin mediated diseases comprising administering to a mammalian patient a compound of formula I:
in an amount that is effective to treat or prevent said prostaglandin mediated disease. Novel compounds are also disclosed.
Type:
Grant
Filed:
April 24, 2001
Date of Patent:
September 30, 2003
Inventors:
Michel Gallant, Nicolas Lachance, Marc Labelle, Robert Zamboni, Helene Juteau, Yves Gareau, Patrick Lacombe
Abstract: The invention encompasses the novel compound of Formula I as well as a method of treating COX-2 mediated diseases comprising administration to a patient in need of such treatment of a non-toxic therapeutically effective amount of a compound of Formula I.
The invention also encompasses certain pharmaceutical compositions for treatment of COX-2 mediated diseases comprising compounds of Formula I.
Type:
Grant
Filed:
October 30, 2001
Date of Patent:
July 22, 2003
Assignee:
Merck & Co., Inc.
Inventors:
Daniel Dube, Rejean Fortin, Richard Friesen, Zhaoyin Wang, Jacques Yves Gauthier
Abstract: This invention is directed to a method of retarding or preventing the transformation of a colonic adenoma to a colonic adenocarcinoma comprising the administration to a patient with FAP or a patient with one or more of said adenomas a non-toxic therapeutically effective amount of NSAID, said amount effective to inhibit the PGHS-2 in said adenoma. The preferred method comprises the administration of a specific PGHS-2 inhibiting agent as defined herein.
Type:
Grant
Filed:
October 12, 2001
Date of Patent:
July 15, 2003
Inventors:
Stacia Kargman, Jilly Evans, Thomas J. Simon
Abstract: The invention encompasses the novel class of compounds represented by formula I, which are caspase-3 inhibitors.
The invention also encompasses certain pharmaceutical compositions for treatment of caspase-3 mediated diseases comprising compounds of formula I.
Type:
Grant
Filed:
December 2, 1999
Date of Patent:
April 22, 2003
Assignee:
Merck Frosst Canada & Co.
Inventors:
Erich L. Grimm, Johanne Renaud, Renee Aspiotis, Christopher I. Bayly, Robert Zamboni, Shawn Black