Abstract: This invention relates to a novel class of compounds which are cysteine protease inhibitors, including but not limited to, inhibitors of cathepsins K, L, S and B. These compounds are useful for treating diseases in which inhibition of bone resorption is indicated, such as osteoporosis.
Type:
Grant
Filed:
December 9, 2004
Date of Patent:
March 30, 2010
Assignee:
Merck Frosst Canada & Co.
Inventors:
Michael Boyd, Cheuk Lau, Christophe Mellon, Bruno Roy, John Scheigetz, Vouy Linh Truong
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:
January 25, 2005
Date of Patent:
November 24, 2009
Assignee:
Merck Frosst Canada & Co.
Inventors:
Carl Berthelette, Lianhai Li, Christian Beaulieu, Zhaoyin Wang, Claudio F. Sturino
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, Formula (I). The invention also encompasses certain pharmaceutical compositions and methods for treating cyclooxygenase-2 mediated diseases comprising the use of compounds of Formula 1. 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:
January 25, 2005
Date of Patent:
November 24, 2009
Assignee:
Merck Frosst Canada & Co.
Inventors:
Claude Dufresne, Carl Berthelette, Lianhai Li, Daniel Guay, Michel Gallant, Patrick Lacombe, Renee Aspiotis, Zhaoyin Wang, Claudio F. Sturino
Abstract: The invention provides novel polymorphic form of montelukast sodium, as well as methods of using and pharmaceutical compositions containing saud novel form. Also provided are montelukast sodium: acetonitrile solvates, which are intermediates in the formation of crystalline montelukast sodium.
Abstract: This invention relates to a novel class of compounds which are cysteine protease inhibitors, including but not limited to, inhibitors of cathepsins K, L, S and B. These compounds are useful for treating diseases in which inhibition of bone resorption is indicated, such as osteoporosis.
Type:
Grant
Filed:
November 18, 2005
Date of Patent:
August 5, 2008
Assignee:
Merck Frosst Canada & Co.
Inventors:
Jacques Yves Gauthier, Chun Sing Li, Christophe Mellon
Abstract: This invention relates to a class of compounds having the general formula (I) which are cysteine protease inhibitors, including but not limited to, inhibitors of cathepsins K, L, S and B. These compounds are useful for treating diseases in which inhibition of bone resorption is indicated, such as osteoporosis.
Type:
Grant
Filed:
June 28, 2004
Date of Patent:
July 29, 2008
Assignee:
Merck Frosst Canada & Co.
Inventors:
Christopher Bayly, Cameron Black, Sheldon Crane, Daniel J. McKay, Renata Oballa, Joel Robichaud
Abstract: This invention relates to a novel class of compounds which are cysteine protease inhibitors, including but not limited to, inhibitors of cathepsins K, L, S and B. These compounds are useful for treating diseases in which inhibition of bone resorption is indicated, such as osteoporosis.
Inventors:
Christopher I. Bayly, Cameron Black, Serge Leger, Chun Sing Li, Dan McKay, Christophe Mellon, Jacques Yves Gauthier, Vouy-Linh Truong, Cheuk Lau, Michel Therien
Abstract: The present invention is directed to novel cyanoalkylamino derivatives that are inhibitors of cysteine protease such as cathepsins K, S, B and L, in particular cathepsin K Pharmaceutical composition comprising these compounds, method of treating diseases mediated by unregulated cysteine protease activity, in particular cathepsin K utilizing these compounds and methods of preparing these compounds are also disclosed.
Type:
Grant
Filed:
November 13, 2002
Date of Patent:
May 13, 2008
Assignee:
Merck Frosst Canada & Co.
Inventors:
Cameron Black, Sheldon N. Crane, Dana Davis, Eduardo L. Setti
Abstract: A class of compounds is disclosed, comprising sulphonamido-substituted bridged bicycloalkyl structures. The compounds are inhibitors of gamma-secretase, and hence are useful in the treatment of and/or prevention of Alzheimer's disease.
Inventors:
Patrice Charles Belanger, Ian James Collins, Joanne Claire Hannam, Timothy Harrison, Stephen John Lewis, Andrew Madin, Edward Giles McIver, Alan John Nadin, Joseph George Neduvelil, Mark Steven Shearman, Adrian Leonard Smith, Timothy Jason Sparey, Graeme Irvine Stevenson, Martin Richard Teall
Abstract: This invention encompasses a method for treating a prostaglandin E mediated disease or condition comprising administering to a mammalian patient in need of such treatment a compound of Formula (A) in an amount that is effective to treat the prostaglandin E mediated disease or condition
Type:
Grant
Filed:
December 11, 2002
Date of Patent:
March 25, 2008
Assignee:
Merck Frosst Canada & Co.
Inventors:
Daniel Dube, Denis Deschenes, Rejean Fortin, Yves Girard
Abstract: Fluoro substituted cycloalkanoindole derivatives are antagonists of prostaglandins, and as such are useful for the treatment of prostaglandin mediated diseases.
Type:
Grant
Filed:
January 22, 2003
Date of Patent:
January 8, 2008
Assignee:
Merck Frosst Canada & Co.
Inventors:
Carl Berthelette, Nicolas Lachance, Lianhai Li, Claudio Sturino, Zhaoyin Wang
Abstract: This invention relates to class of compounds which are cysteine protease inhibitors, including but not limited to, inhibitors of cathepsins K, L, S and B. These compounds are useful for treating diseases in which inhibition of bone resorption is indicated, such as osteoporosis.
Type:
Grant
Filed:
September 3, 2003
Date of Patent:
October 9, 2007
Assignee:
Merck Frosst Canada & Co.
Inventors:
Michael Boyd, Marc Gagnon, Cheuk Lau, Christophe Mellon, John Scheigetz
Abstract: The invention encompasses the novel class of compounds represented by the formula below, which are inhibitors of the PTP-1B enzyme. The invention also encompasses pharmaceutical compositions which include the compounds shown above and methods of treating or preventing PTP-1B mediated diseases, including diabetes.
Type:
Grant
Filed:
June 19, 2002
Date of Patent:
January 16, 2007
Assignee:
Merck Frosst Canada & Co.
Inventors:
Claude Dufresne, Yves Leblanc, Cheuk K. Lau, Patrick Roy, Chun Sing Li
Abstract: Dihydropyrroloindoles and tetrahydropyridoindoles are prostaglandin receptor antagonists useful for the treatment of prostaglandin-mediated diseases such as allergic rhinitis, nasal congestion and asthma.
Type:
Grant
Filed:
May 22, 2002
Date of Patent:
December 5, 2006
Assignee:
Merck Frosst Canada & Co.
Inventors:
Zhaoyin Wang, Christian Beaulieu, Claude Dufresne, Daniel Guay, Yves LeBlanc
Abstract: The present invention provides substituted tetrahydrocarbazole and cyclopentanoindole derivatives as antagonists of DP receptor, and as such are useful for the treatment of prostaglandin D2 mediated diseases such as rhinitis, asthma and nasal congestion.
Type:
Grant
Filed:
December 8, 2004
Date of Patent:
March 28, 2006
Assignee:
Merck Frosst Canada & Co.
Inventors:
Christian Beaulieu, Daniel Guay, Zhaoyin Wang, Robert Zamboni
Abstract: 8-arylquinolines of formula (I) wherein the aryl group at the 8-position contains a meta two atom bridge to an optionally substituted phenyl or pyridyl group, are PDE4 inhibitors useful to treat asthma, chronic bronchitis, chronic obstructive pulmonary disease, arthritis, respiratory distress syndrome, allergic rhinitis, neurogenic inflammation, pain, rheumatoid arthritis, and other diseases. R1-R7 and Ar are as in claim 1.
Type:
Grant
Filed:
June 26, 2002
Date of Patent:
July 19, 2005
Assignee:
Merck Frosst Canada & Co.
Inventors:
Daniel Dube, Yves Girard, Dwight MacDonald, Anthony Mastracchio, Michel Gallant, Patrick Lacombe, Denis Deschenes
Abstract: Novel ethanes substituted with i) a phenyl, ii) a thiazole, and iii) a pyridyl moiety are PDE4 inhibitors.
Type:
Grant
Filed:
March 20, 2002
Date of Patent:
January 11, 2005
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: This invention relates to a novel class of compounds which are cysteine protease inhibitors, including but not limited to, inhibitors of Cathepsins K and L. These compounds are useful for treating diseases in which inhibition of bone resorption is indicated, such as osteoporosis.
Type:
Grant
Filed:
August 23, 2002
Date of Patent:
December 28, 2004
Assignees:
Merck Frosst Canada & Co., Banyu Pharmaceutical Co., Ltd., Axys Pharmaceuticals, Inc.
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