Patents Represented by Attorney, Agent or Law Firm Richard C. Billups
  • Process for making diaryl pyridines useful as cox-2 inhibitors
    Patent number: 6369275
    Abstract: The invention encompasses a process for making compounds of Formula I useful in the treatment of cyclooxygenase-2 mediated diseases.
    Type: Grant
    Filed: November 17, 2000
    Date of Patent: April 9, 2002
    Assignee: Merck & Co., Inc.
    Inventors: Ian W. Davies, Michel Journet, Linda Gerena, Robert D. Larsen, Philip J. Pye, Kai Rossen
  • Carboxylic acids and acylsulfonamides, compositions containing such compounds and methods of treatment
    Patent number: 6369082
    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
  • Synthesis of methylthiophenyl hydroxyketones
    Patent number: 6281391
    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.
    Type: Grant
    Filed: October 27, 1999
    Date of Patent: August 28, 2001
    Assignees: Merck & Co., Inc., Merck Frosst Canada & Co.
    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
  • Biphenylene lactams as prostaglandin receptor ligands
    Patent number: 6277839
    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
  • Combination therapy for reducing the risks associated with cardio-and-cerebrovascular disease
    Patent number: 6245797
    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.
    Type: Grant
    Filed: October 20, 1998
    Date of Patent: June 12, 2001
    Assignee: Merck & Co., Inc.
    Inventor: Melvin Winokur
  • Carboxylic acids and acylsulfonamides, compositions containing such compounds and methods of treatment
    Patent number: 6242493
    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
  • Synthesis of 4-[(5-substituted phenyl)-3-substituted-1H-pyrazol-1-yl]benzenesulfonamide
    Patent number: 6232472
    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
  • Gamma-ketoacid dipeptides as inhibitors of caspase-3
    Patent number: 6225288
    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
  • Diphenyl-1,2,3-thiadiazol-3-oxides, compositions and methods of use
    Patent number: 6211210
    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
  • Process for making diaryl pyridines useful as COX-2 inhibitors
    Patent number: 6204387
    Abstract: The invention encompasses a process for making compounds of Formula I useful in the treatment of cyclooxygenase-2 mediated diseases.
    Type: Grant
    Filed: March 23, 2000
    Date of Patent: March 20, 2001
    Assignee: Merck & Co., Inc.
    Inventors: Ian W. Davies, Linda Gerena, Michel Journet, Robert D. Larsen, Philip J. Pye, Kai Rossen
  • Phosphonic acids derivatives as inhibitors of protein tyrosine phosphate 1B (PTP-1B)
    Patent number: 6174874
    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
  • (Methylsulfonyl)phenyl-2-(5H)-furanones as COX-2 inhibitors
    Patent number: 6169188
    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
  • Intermediates for making heterocycles useful as COX-2 inhibitors
    Patent number: 6153787
    Abstract: The invention encompasses a process for making compounds of Formula I or Ia useful in the treatment of cyclooxygenase-2 mediated diseases.
    Type: Grant
    Filed: December 4, 1998
    Date of Patent: November 28, 2000
    Assignee: Merck & Co., Inc.
    Inventors: Kai Rossen, Guo-Jie Ho, Ralph P. Volante, Roger N. Farr, David J. Mathre
  • Synthesis of 4-[5-substituted or unsubstituted phenyl)-3-substituted-1H-pyrazol-1-yl]benzenesulfonamides
    Patent number: 6150534
    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
  • Process of making 3-aryloxy, 4-aryl furan-2-ones useful as inhibitors of COX-2
    Patent number: 6140515
    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
  • Diaryl-5-alkyl-5-methyl-2-(5H)-furanones as selective cyclooxygenase-2-inhibitors
    Patent number: 6133292
    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.
    Type: Grant
    Filed: October 16, 1998
    Date of Patent: October 17, 2000
    Assignee: Merck Frosst Canada & Co.
    Inventors: Zhaoyin Wang, Erich Grimm, Serge Leger
  • Process for making 2-aryl-3-aryl-5-halo pyridines useful as COX-2 inhibitors
    Patent number: 6130334
    Abstract: The invention encompasses a process for making compounds of Formula I useful in the treatment of cyclooxygenase-2 mediated diseases.
    Type: Grant
    Filed: April 15, 1998
    Date of Patent: October 10, 2000
    Assignee: Merck & Co., Inc.
    Inventors: Philip J. Pye, Ashok Maliakal, Kai Rossen, Ralph P. Volante, Jess Sager
  • Process for making 2-aryl-3-aryl-5-halo pyridines useful as COX-2 inhibitors
    Patent number: 6127545
    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
  • Process for making phenyl heterocycles useful as COX-2 inhibitors
    Patent number: 6080876
    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 17, 1998
    Date of Patent: June 27, 2000
    Assignee: Merck & Co., Inc.
    Inventors: Ilias Dorziotis, Ioannis Houpis, Kan K. Eng
  • Substituted pyridines as selective cyclooxygenase-2 inhibitors
    Patent number: 6071936
    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