Abstract: The invention encompasses the novel compounds of Formula I, which are useful in the treatment of cyclooxygenase-2 mediated diseases.
The invention also encompasses certain pharmaceutical compositions comprising compounds of Formula I as well as methods of treating cyclooxygenase-2 mediated diseases comprising administering to a patient in need of such treatment a non-toxic therapeutically effective amount of a compound of Formula I.
Type:
Grant
Filed:
June 27, 2001
Date of Patent:
October 15, 2002
Assignee:
Merck Frosst Canada & Co.
Inventors:
Chun-Sing Li, Cheuk Kun Lau, Michel Therien, Petpiboon Prasit
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, including diabetes, obesity, and diabetes-related diseases.
Type:
Grant
Filed:
December 21, 2000
Date of Patent:
September 10, 2002
Assignee:
Merck Frosst Canada & Co.
Inventors:
Yves Leblanc, Claude Dufresne, Jacques Yves Gauthier, Robert Young
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 fin caspase-3 mediated diseases and conditions.
Type:
Grant
Filed:
July 19, 2000
Date of Patent:
September 3, 2002
Assignee:
Merck Frosst Canada & Co.
Inventors:
Yongxin Han, Andre Giroux, Robert Zamboni, Daniel J. McKay, Christopher I. Bayly, Erich L. Grimm, John Colucci
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: Compounds represented by formula I:
as well as pharmaceutically acceptable salts and hydrates thereof are disclosed as useful for treating or preventing diseases and conditions mediated by PDE-IV.
Pharmaceutical compositions and methods of treatment are also included.
Type:
Grant
Filed:
March 1, 2001
Date of Patent:
August 20, 2002
Assignee:
Merck Frosst Canada & Co.
Inventors:
Marc Labelle, Claudio Sturino, Nicolas Lachance, Dwight Macdonald
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: The present invention relates to methods for inhibiting bone resorption in a mammal comprising administering to a mammal in need thereof a therapeutically effective amount of an EP4 receptor subtype antagonist.
Type:
Grant
Filed:
October 13, 1999
Date of Patent:
July 2, 2002
Assignees:
Merck Frosst Canada & Co., Merck & Co., Inc.
Inventors:
Shun-ichi Harada, Gideon A. Rodan, Mohamed Machwate, Marc LaBelle, Kathleen Metters, Robert N. Young
Abstract: Substituted cyclopentanoindole derivatives are antagonists of prostaglandins, and as such are useful for the treatment of prostaglandin mediated diseases.
Type:
Grant
Filed:
July 20, 2001
Date of Patent:
June 25, 2002
Assignee:
Merck Frosst Canada & Co.
Inventors:
Marc Labelle, Claudio Sturino, Bruno Roy, Carl Berthelette, Michael Boyd, Nicolas Lachance, John Scheigetz
Abstract: Novel substituted 8-arylquinolines, wherein the aryl group at the 8-position contains a substituent substituted-alkenyl group, are PDE4 inhibitors.
Type:
Grant
Filed:
December 20, 2000
Date of Patent:
June 25, 2002
Assignee:
Merck Frosst Canada & Co.
Inventors:
Denis Deschenes, Daniel Dube, Michel Gallant, Yves Girard, Patrick Lacombe, Dwight MacDonald, Anthony Mastracchio, Helene Perrier
Abstract: Novel ethanes substituted with i) a phenyl, ii) a thiazole, and iii) a pyridyl moiety are PDE4 inhibitors.
Type:
Grant
Filed:
March 16, 2001
Date of Patent:
June 4, 2002
Assignee:
Merck Frosst Canada & Co.
Inventors:
Richard Freisen, Yves Ducharme, Bernard Cote, Marc Blouin, Evelyn Martins, Daniel Guay, Pierre Hamel, Mario Girard, Richard Frenette, Sebastien Laliberte
Abstract: A human prostaglandin receptor has been identified and DNA encoding the receptor has been isolated, purified, sequenced and expressed in host cells. This DNA encoding the human prostaglandin receptor and host cells expressing the receptor are used to identify modulators of the prostaglandin receptor.
Type:
Grant
Filed:
June 20, 2000
Date of Patent:
May 28, 2002
Assignee:
Merck Frosst Canada & Co.
Inventors:
Mark Abramovitz, Kathleen Metters, Yves Boie, Nicole Sawyer, Deborah M. Slipetz
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 certain pharmaceutical compositions and methods for treatment of prostaglandin mediated diseases comprising the use of compounds of formula A.
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 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: A novel prostaglandin receptor has been identified and DNA encoding the receptor has been isolated, purified, sequenced and expressed in host cells. This DNA encoding the novel prostaglandin receptor and host cells expressing the receptor are used to identify modulators of the prostaglandin receptor.
Type:
Grant
Filed:
March 16, 1998
Date of Patent:
April 2, 2002
Assignee:
Merck Frosst Canada & Co.
Inventors:
Mark Abramovitz, Yves Boie, Richard Grygorczyk, Kathleen Metters, Thomas H. Rushmore, Deborah M. Slipetz
Abstract: The invention encompasses compounds represented by formula I:
as well as compositions and methods of treatment. The compounds are inhibitors of the PTP-1B enzyme.
Type:
Grant
Filed:
May 12, 2000
Date of Patent:
April 2, 2002
Assignee:
Merck Frosst Canada & Co.
Inventors:
Yves Leblanc, Claude Dufresne, Patrick Roy, Zhaoyin Wang
Abstract: The invention discloses a cDNA consisting of human cyclooxygenase-2 cDNA attached to 3′ flanking sequence of human cyclooxygenase-1 methods for increasing the expression of human cyclooxygenase-2 in transformed cells and assays for preferentially and independently measuring cyclogenase-2 in samples.
Abstract: A novel prostaglandin receptor has been identified and DNA encoding the receptor has been isolated, purified, sequenced and expressed in host cells. This DNA encoding the novel prostaglandin receptor and host cells expressing the receptor are used to identify modulators of the prostaglandin receptor.
Type:
Grant
Filed:
November 21, 1997
Date of Patent:
March 19, 2002
Assignee:
Merck Frosst Canada & Co.
Inventors:
Mark Abramovitz, Richard Grygorczyk, Kathleen Metters, Truyen Nguyen, Thomas H. Rushmore, Deborah Slipetz
Abstract: Disclosed are new ligands for use in a binding assay for proteases and phosphatases, which contain cysteine in their binding sites or as a necessary structural component for enzymatic binding. The sulfhydryl group of cysteine is the nucleophilic group in the enzyme's mechanistic proteolytic and hydrolytic properties. The assay can be used to determine the ability of new, unknown ligands and mixtures of compounds to competitively bind with the enzyme versus a known binding agent for the enzyme, e.g., a known enzyme inhibitor. By the use of a mutant form of the natural or native wild-type enzyme, in which serine, or another amino acid, e.g., alanine, replaces cysteine, the problem of interference from extraneous oxidizing and alkylating agents in the assay procedure is overcome. The interference arises because of oxidation or alkylation of the sulfhydryl, —SH (or —S−), in the cysteine, which then adversely affects the binding ability of the enzyme.
Type:
Grant
Filed:
April 29, 1998
Date of Patent:
February 19, 2002
Assignee:
Merck Frosst Canada & Co.
Inventors:
Sylvie Desmarais, Robert Zamboni, Richard Friesen, Yves LeBlanc, Claude Dufresne, Robert N. Young, Patrick Roy
Abstract: The present invention relates to a whole cell assay for cathepsin K. The present invention is useful for determining cathepsin K activity in a mammalian cell systems and for identifying and evaluating inhibitors of cathepsin K.
Type:
Grant
Filed:
April 20, 2000
Date of Patent:
February 12, 2002
Assignee:
Merck Frosst Canada & Co.,
Inventors:
Joseph Mancini, Denis Riendeau, David Claveau