Abstract: This invention encompasses the novel compounds of formula A, which are useful in the treatment of prostaglandin mediated diseases,
or a pharmaceutically acceptable salt, hydrate or ester thereof. The invention also encompasses pharmaceutical compositions and methods for treatment of prostaglandin mediated diseases.
Type:
Grant
Filed:
September 14, 2000
Date of Patent:
April 9, 2002
Assignee:
Merck Frosst Canada & Co.
Inventors:
Patrick Lacombe, Marc Labelle, Rejean Ruel
Abstract: This invention encompasses a novel process for synthesizing compounds represented by formula A:
These compounds are intermediates useful in the preparation of certain agents that are selective COX-2 inhibitors.
Inventors:
Richard D. Tillyer, Ian W. Davies, Robert D. Larsen, Xin Wang, Paul O'Shea, Anthony On-Ping King, Dalian Zhao, Cheng Y. Chen, Edward J. J. Grabowski
Abstract: The present invention relates to biphenylene lactams of Formula II which are ligands at the prostaglandin receptors, as well as a method for treating prostaglandin mediated diseases comprising administration to a patient in need of such a treatment of a non-toxic therapeutically effective amount of compound of Formula II, and the like.
Type:
Grant
Filed:
October 1, 1999
Date of Patent:
August 21, 2001
Assignee:
Merck Frosst Canada & Co.
Inventors:
Joseph G. Atkinson, Marc Labelle, Patrick Lacombe, Rejean Ruel
Abstract: The instant invention provides a drug combination comprised of an HMG-CoA reductase inhibitor in combination with a COX-2 inhibitor, which is useful for treating, preventing, and/or reducing the risk of developing atherosclerosis and atherosclerotic disease events.
Abstract: Compounds of formula I:
as well as pharmaceutically acceptable salts, hydrates and esters thereof, are disclosed.
The compounds are useful for treating or preventing prostaglandin mediated diseases. Pharmaceutical compositions containing such compounds and methods of treatment are also included.
Type:
Grant
Filed:
March 10, 1999
Date of Patent:
June 5, 2001
Assignee:
Merck Frosst Canada & Co.
Inventors:
Yves Gareau, Marc LaBelle, Helene Juteau, Michel Gallant, Nicolas LaChance, Michel Belley
Abstract: This invention encompasses a novel process for synthesizing the compound represented by formula I:
These compounds are useful as non-steroidal anti-inflammatory agents.
Type:
Grant
Filed:
September 13, 2000
Date of Patent:
May 15, 2001
Assignee:
Merck Frosst Canada & Co.
Inventors:
Paul O'Shea, Xin Wang, Richard D. Tillyer, Sophie-Dorothee Clas, Chad Dalton
Abstract: Compounds represented by formula I:
as well as pharmaceutically acceptable salts, esters and hydrates thereof are disclosed along with pharmaceutical compositions and methods of treatment. The compounds are useful as inhibitors of caspase-3, which is implicated in modulating apoptosis.
Type:
Grant
Filed:
March 16, 2000
Date of Patent:
May 1, 2001
Assignee:
Merk Frosst Canada & Co.
Inventors:
Yongxin Han, Andre Giroux, Erich Grimm, Renee Aspiotis, Sebastien Francoeur, Robert Zamboni, Petpiboon Prasit, Christopher Bayly, Dan McKay, Cameron Black
Abstract: The invention encompasses compounds 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:
April 28, 2000
Date of Patent:
April 3, 2001
Assignee:
Merck Frosst Canada & Co.
Inventors:
Cheuk Kun Lau, Chun-Sing Li, Cameron Black, Michel Therien, Jacques Yves Gauthier
Abstract: The invention encompasses the novel class of compounds represented by formula I which are inhibitors of the PTP-1B enzyme.
The invention also encompasses pharmaceutical compositions and methods of treating or preventing PTP-1B mediated diseases.
Type:
Grant
Filed:
September 17, 1999
Date of Patent:
January 16, 2001
Assignee:
Merck Frosst Canada & Co.
Inventors:
Zhaoyin Wang, Claude Dufresne, Yves Leblanc, Chun Sing Li, Jacques Y. Gauthier, Cheuk K. Lau, Michel Therien, Patrick Roy
Abstract: The invention encompasses the novel compound of Formula I useful in the treatment of cyclooxygenase-2 mediated diseases.
The invention also encompasses certain pharmaceutical compositions for treatment of cyclooxygenase-2 mediated diseases comprising compounds of Formula I.
Type:
Grant
Filed:
October 21, 1999
Date of Patent:
January 2, 2001
Assignee:
Merck Frosst Canada & Co.
Inventors:
Michel Belley, Jacques Yves Gauthier, Erich Grimm, Yves LeBlanc, Chun-Sing Li, Michel Therien, Cameron Black, Petpiboon Prasit, Cheuk-Kun Lau, Patrick Roy
Abstract: This invention encompasses a novel process for synthesizing the compound represented by formula I: ##STR1## These compounds are useful as non-steroidal anti-inflammatory agents.
Type:
Grant
Filed:
January 14, 2000
Date of Patent:
November 21, 2000
Assignee:
Merck Frosst Canada & Co.
Inventors:
Paul O'Shea, Richard D. Tillyer, Xin Wang, Sophie-Dorothee Clas, Chad Dalton
Abstract: Described is a process of preparing 3-aryl, 4-aryloxy furan-5-ones which are useful as inhibitors of cyclooxygenase-2 (COX-2). Such compounds are useful as anti-inflammatory agents. The process is directed to an asymmetric synthesis which involves: a trisubstituted styrene derivative preparation via Horner-Wadsworth-Emmons reaction and subsequent one pot trifluoromethylation of the allylic alcohol; preparation of the .alpha.-hydroxyl ketone using Sharpless asymmetric dihydroxylation and Swern oxidation; the esterification of the .alpha.-hydroxyl ketone with the phenoxy acetic acid; and the Dieckman condensation of the resulting ester.
Type:
Grant
Filed:
September 15, 1998
Date of Patent:
October 31, 2000
Assignee:
Merck & Co., Inc.
Inventors:
Cheng Y. Chen, Lushi Tan, Robert D. Larsen
Abstract: The invention encompasses compounds of Formula I as well as a method of treating COX-2 mediated diseases comprising administration to a patient need of such treatment of a non-toxic therapeutically effective amount of a compound of Formula I ##STR1## e.g. (5R)-3-(3,4-difluorophenyl)-5-ethyl-5-methyl-4-[4-(methylsulfonyl)phenyl]- 2,5-dihydro-2-furanone.
Abstract: The invention encompasses a process for making compounds of Formula I useful in the treatment of cyclooxygenase-2 mediated diseases.
Type:
Grant
Filed:
September 18, 1998
Date of Patent:
October 3, 2000
Assignee:
Merck & Co., Inc.
Inventors:
Philip J. Pye, Kai Rossen, Ashok Maliakal, Ralph P. Volante, Jess Sager, Jean-Francois Marcoux, Ian Davies, Edward G. Corley, Daniel Richard Sidler, Robert D. Larsen
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. ##STR1## The invention also encompasses certain pharmaceutical compositions for treatment of COX-2 mediated diseases comprising compounds of Formula I.
Type:
Grant
Filed:
May 17, 1999
Date of Patent:
June 6, 2000
Assignee:
Merck Frosst Canada & Co.
Inventors:
Daniel Dube, Rejean Fortin, Richard Friesen, Zhaoyin Wang, Jacques Yves Gauthier