Abstract: The invention relates to an intact cell assay for direct quantitation of protein tyrosine phosphatase (PTP) activity using the baculovirus expression system. A PTP expressed in transformed host insect cells is processed and localized in their predicted subcellular compartments. Assays are performed on the PTP expressing host cells challenged with a substrate such as, p-nitrophenyl phosphate. This substrate is hydrolysed to p-nitrophenol by expressed phosphatase activity. Emergence of p-nitrophenol is determined spectrophotometrically and is a measure of PTP activity.
Further, the assay and transformed host cells of this invention are particularly useful in a screening method for selecting potential inhibitors to PTPs. Basically, transformed host cells are pre-incubated with or without inhibitors and the assay conducted as described. This invention relates to an intact cell assay with a direct readout of PTP activity that is useful in a cell-based screening method for selecting inhibitors of PTPs.
Abstract: The invention encompasses the novel compound of Formula I as well as a method of treating cyclooxygenase-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 cyclooxygenase-2 mediated diseases comprising compounds of Formula I.
Type:
Grant
Filed:
February 25, 1997
Date of Patent:
December 11, 2001
Assignee:
Merck Frosst Canada & Co.
Inventors:
Petpiboon Prasit, Daniel Guay, Zhaoyin Wang, Serge Leger, Michel Therien
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: 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 provides a method of treating a neurodegenerative disease and in particular Alzheimers disease which comprises administering to a human in need thereof a therapeutically effective amount of a non-steroid COX-II inhibitor.
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: 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: 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.
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: The invention encompasses the novel compound of Formula (I) as well as a method of treating cyclooxygenase-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 cyclooxygenase-2 mediated diseases comprising compounds of Formula (I).
Type:
Grant
Filed:
June 12, 1997
Date of Patent:
April 24, 2001
Assignee:
Merck Frosst Canada & Co.
Inventors:
Cameron Black, Erich Grimm, Serge Leger, Petpiboon Prasit, Zhaoyin Wang
Abstract: A novel human DP 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:
April 28, 1999
Date of Patent:
April 10, 2001
Assignee:
Merck Frosst Canada & Co.
Inventors:
Mark Abramovitz, Yves Boie, Kathleen Metters, Nicole Sawyer, Deborah M. Slipetz
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: Compounds and methods for treating prostaglandin mediated diseases, and certain pharmaceutical compositions thereof are disclosed. The compounds are represented by formula II:
Ar1—W—Ar2—X—Q II
The compounds of the invention are structurally different from NSAIDs and opiates, and are antagonists of the pain and inflammatory effects of E-type prostaglandins.
Type:
Grant
Filed:
October 4, 1999
Date of Patent:
April 3, 2001
Assignee:
Merck Frosst Canada & Co.
Inventors:
Michel Belley, Marc Labelle, Nicholas Lachance, Michel Gallant, Nathalie Chauret, Laird A. Trimble, Chun Li
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: Leukotriene C4 synthase polypeptide identified by photoaffinity labelling, and purification of leukotriene C4 synthase to homogeneity is described.
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: The present invention relates to a transgenic nonhuman animal lacking native amyloid precursor protein. The transgenic mouse of the invention may be used in the study of Alzheimer's Disease and disorders involving the central nervous system.
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