Abstract: This invention describes an amidation process whereby amino acids of the Formulae IIA or IIB can be activated and treated with an amine in the presence of a base to yield amides of the Formula (I), without loss of optical purity.
Abstract: The present invention relates to piperidine-based renin inhibitor compounds having carboxylate or carboxylic acid terminal groups, and their use in treating cardiovascular events and renal insufficiency.
Type:
Application
Filed:
May 23, 2008
Publication date:
May 13, 2010
Applicant:
MERCK FROSST CANADA LTD.
Inventors:
Tom Yao-Hsiang Wu, Helene Juteau, Michel Gallant, Daniel Dube, Patrick Roy, Renee Aspiotis, Erich L. Grimm, Sebastien Laliberte, Austin Chen
Abstract: The invention is directed to naphthalene and quinoline sulfonylurea derivatives as EP4 receptor antagonists useful for the treatment of EP4 mediated diseases or conditions, such as acute and chronic pain, osteoarthritis, rheumatoid arthritis and cancer. Pharmaceutical compositions and methods of use are also included.
Type:
Application
Filed:
March 25, 2008
Publication date:
April 29, 2010
Applicant:
MERCK FROSST CANADA LTD.
Inventors:
Jason Burch, Julie Farand, Yongxin Han, Claudio Sturino
Abstract: The invention is directed to indoline amide derivatives of formula I as EP4 receptor ligands, antagonists or agonists, useful for the treatment of EP4 mediated diseases or conditions, such as acute and chronic pain, osteoarthritis, rheumatoid arthritis, cancer and glaucoma. Pharmaceutical compositions and methods of use are also included.
Abstract: Compounds according to formula (I) wherein the radicals R1, R2 and R3 are as herein defined, and wherein Ar represents an aryl group or heteroaryl group, preferably phenyl, n is 1 or 2, and the radical X represents a group selected from —C(Ra)(Rb)—, —C(Ra)(Rb)—C(Ra)(Rb)—, —C(Ra)?C(Ra)—, OC(Ra)(Rb)— or SC(Ra)(Rb)—. These compounds and their pharmaceutical acceptable salts are used in pharmaceutical compositions as prostaglandine D2 receptor antagonists useful in the treatment of CRTH2-mediated diseases such as respiratory, inflammatory or allergic conditions among others.
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: Compounds of formula (I): are found to be selective inhibitors of cathepsin B, and hence useful in treating a variety of pathological conditions.
Type:
Application
Filed:
September 24, 2007
Publication date:
February 25, 2010
Applicant:
MERCK FROSST CANADA LTD, Merk & Co., Inc.
Inventors:
Jacques Yves Gauthier, Vouy-Linh Truong
Abstract: Cyclic amine derivatives of structural formula (I) are selective inhibitors of stearoyl-coenzyme A delta-9 desaturase (SCD1) relative to other known stearoyl-coenzyme A desaturases. The compounds of the present invention are useful for the prevention and treatment of conditions related to abnormal lipid synthesis and metabolism, including cardiovascular disease; atherosclerosis; obesity; diabetes; neurological disease; metabolic syndrome; insulin resistance; and liver steatosis.
Abstract: Azacycloalkane derivatives of structural formula (I) are selective inhibitors of stearoyl-coenzyme A delta-9 desaturase (SCD1) relative to other known stearoyl-coenzyme A desaturases. The compounds of the present invention are useful for the prevention and treatment of conditions related to abnormal lipid synthesis and metabolism, including cardiovascular disease, such as atherosclerosis; obesity; diabetes; neurological disease; metabolic syndrome; insulin resistance; and liver steatosis.
Type:
Application
Filed:
October 18, 2007
Publication date:
January 7, 2010
Applicant:
MERCK FROSST CANADA LTD.
Inventors:
Renata M. Oballa, Denis Deschenes, Marc Gagnon, Yves Leblanc, David Powell, Yeeman K. Ramtohul
Abstract: Azacycloalkane derivatives of structural formula I are selective inhibitors of stearoyl-coenzyme A delta-9 desaturase (SCD1) relative to other known stearoyl-coenzyme A desaturases. The compounds of the present invention are useful for the prevention and treatment of conditions related to abnormal lipid synthesis and metabolism, including cardiovascular disease, such as atherosclerosis; obesity; diabetes; neurological disease; metabolic syndrome; insulin resistance; and liver steatosis. Formula (I).
Abstract: The instant invention provides compounds of formula: (I) which are 5-lipoxygenase activating protein inhibitors: formula (I). Compounds of formula (I) are useful as anti-atherosclerotic, anti-asthmatic, anti-allergic, anti-inflammatory and cyto-protective agents.
Inventors:
Lin Chu, Mark T. Goulet, Feroze Ujjainwalla, Linda Chang, Richard Frenette, Yves Girard, Michel Therien, Dwight Macdonald, John H. Hutchinson
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: Pyridopyrrolizine and pyridoindolizine derivatives are prostaglandin receptor antagonists useful for the treatment of prostaglandin-mediated diseases such as allergic rhinitis, nasal congestion and asthma.
Type:
Grant
Filed:
October 28, 2003
Date of Patent:
November 17, 2009
Assignee:
Merck Frosst Canada Ltd.
Inventors:
Yves Leblanc, Claude Dufresne, Patrick Roy
Abstract: Fluoro substituted cycloalkanoindole derivatives are antagonists of prostaglandins, and as such are useful for the treatment of prostaglandin mediated diseases.
Type:
Grant
Filed:
July 23, 2007
Date of Patent:
November 17, 2009
Assignee:
Merck Frosst Canada Ltd.
Inventors:
Carl Berthelette, Nicolas Lachance, Lianhai Li, Claudio Sturino, Zhaoyin Wang
Abstract: Azacycloalkane derivatives of structural formula I are selective inhibitors of stearoyl-coenzyme A delta-9 desaturase (SCD1) relative to other known stearoyl-coenzyme A desaturases. The compounds of the present invention are useful for the prevention and treatment of conditions related to abnormal lipid synthesis and metabolism, including cardiovascular disease, such as atherosclerosis; obesity; diabetes; neurological disease; metabolic syndrome; insulin resistance; and liver steatosis.
Type:
Grant
Filed:
January 25, 2008
Date of Patent:
September 1, 2009
Assignee:
Merck Frosst Canada L.L.C.
Inventors:
Yves Leblanc, David Powell, Yeeman K. Ramtohul, Serge Léger
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: The instant invention provides compounds of Formula Ia which are leukotriene biosynthesis inhibitors. Compounds of Formula Ia are useful as anti-atherosclerotic, anti-asthmatic, anti-allergic, anti-inflammatory and cytoprotective agents.
Type:
Grant
Filed:
March 21, 2006
Date of Patent:
June 30, 2009
Assignee:
Merck Frosst Canada Ltd.
Inventors:
Marc Blouin, Erich L. Grimm, Yves Gareau, Marc Gagnon, Helene Juteau, Sebastien Laliberte, Bruce MacKay, Richard Friesen
Abstract: Heteroaromatic compounds of structural formula (I) are selective inhibitors of stearoyl-coenzyme A delta-9 desaturase (SCD1) relative to other known stearoyl-coenzyme A desaturases. The compounds of the present invention are useful for the prevention and treatment of conditions related to abnormal lipid synthesis and metabolism, including cardiovascular disease; atherosclerosis; lipid disorders; obesity; diabetes; neurological disease; metabolic syndrome; insulin resistance; and fatty liver disease.
Type:
Application
Filed:
July 18, 2006
Publication date:
May 7, 2009
Applicant:
MERCK FROSST CANADA LTD.
Inventors:
Cameron Black, Denis Deschenes, Marc Gagnon, Nicolas Lachance, Yves LeBlanc, Serge Leger, Chun Sing Li, Renata M. Oballa
Abstract: The present invention provides compounds of formula I which are inhibitors of cathepsin S and as such are useful in the prevention and treatment of cathepsin S dependent diseases and conditions including, but not limited to, chronic obstructive pulmonary disease (COPD) and pain.