Patents Represented by Attorney, Agent or Law Firm Richard C. Billups
  • (methylsulfonyl)phenyl-2-(5H)-furanones with oxygen link as COX-2 inhibitors
    Patent number: 6071954
    Abstract: The invention encompasses the novel compound of Formula I useful in the treatment of cyclooxygenase-2 mediated diseases. ##STR1## The invention also encompasses certain pharmaceutical compositions for treatment of cyclooxygenase-2 mediated diseases comprising compounds of Formula I.
    Type: Grant
    Filed: March 13, 1998
    Date of Patent: June 6, 2000
    Assignee: Merk Frosst Canada, Inc.
    Inventors: Yves LeBlanc, Patrick Roy, Serge Leger, Erich Grimm, Zhaoyin Wang
  • 3,4-Diaryl-2-hydroxy-2,5-dihydrofurans as prodrugs to cox-2 inhibitors
    Patent number: 6057319
    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 2, 1998
    Date of Patent: May 2, 2000
    Assignee: Merck Frosst Canada & Co.
    Inventors: Cameron Black, Serge Leger, Petpiboon Prasit, Zhaoyin Wang, Pierre Hamel, Yongxin Han, Gregory Hughes
  • 2,3,5-trisubstituted pyridines as inhibitors of cyclooxygenase-2
    Patent number: 6046217
    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. ##STR1## The invention also encompasses certain pharmaceutical compositions for treatment of cyclooxygenase-2 mediated diseases comprising compounds of Formula I.
    Type: Grant
    Filed: September 11, 1998
    Date of Patent: April 4, 2000
    Assignee: Merck Frosst Canada & Co.
    Inventors: Richard Friesen, Rejean Fortin, Daniel Dube, Denis Deschenes
  • Hexahydro-5-imino-1,4-heteroazepine derivatives as inhibitors of nitric oxide synthases
    Patent number: 6043358
    Abstract: Disclosed herein are compounds of Formula I and pharmaceutically acceptable salts thereof which have been found useful in the treatment of nitric oxide synthase mediated diseases and disorders, including neurodegenerative disorders, disorders of gastrointestinal motility and inflammation.
    Type: Grant
    Filed: September 25, 1996
    Date of Patent: March 28, 2000
    Assignee: Merck & Co., Inc.
    Inventors: Charles G. Caldwell, William K. Hagmann, Malcolm Maccoss, Shrenik K. Shah, Kothandaraman Shankaran, Karla L. Furman
  • Process for synthesizing COX-2 inhibitors
    Patent number: 6040319
    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 23, 1999
    Date of Patent: March 21, 2000
    Assignee: Merck & Co., Inc.
    Inventors: Edward G. Corley, Ian W. Davies, Robert D. Larsen, Philip J. Pye, Kai Rossen
  • Process for making diaryl pyridines useful as cox-2-inhibitors
    Patent number: 6040450
    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 15, 1998
    Date of Patent: March 21, 2000
    Assignee: Merck & Co., Inc.
    Inventors: Ian W. Davies, Michel Journet, Linda Gerena, Robert D. Larsen, Philip J. Pye, Kai Rossen
  • Mur D inhibiting compounds, compositions containing such compounds and methods of use
    Patent number: 6030996
    Abstract: The present invention addresses compounds which inhibit Mur D. The compounds are represented by structural formula 1: ##STR1## wherein: X represents OH, OC.sub.1-6 alkyl, O-aryl, O-Har, uridinyl, 5-iodouridinyl or O--Y.sup.+, wherein Y.sup.+ represents a charge balancing group; R.sup.1 and R.sup.2 independently represent H or C.sub.1-6 alkyl, or R.sup.1 and R.sup.2 taken together represent C.sub.1-6 alkylene unsubstituted or substituted with from 1-2 aryl or Har groups; W represents H, aryl, C.sub.1-6 alkyl or a charge balancing group; each M independently represents a member selected from the group consisting of: H, a charge balancing group and a protecting group.Salts and hydrates thereof are included.Also included are pharmaceutical compositions and methods of treatment.
    Type: Grant
    Filed: March 11, 1998
    Date of Patent: February 29, 2000
    Assignee: Merch & Co., Inc.
    Inventor: Laura D. Gegnas
  • Somatostatin agonists
    Patent number: 6025372
    Abstract: Somatostatin agonist compounds of formula I are disclosed: ##STR1## including pharmaceutically acceptable salts and hydrates thereof These compounds are useful in the treatment of diabetes, cancer, acromegaly, restenosis, depression, irritable bowel syndrome and pain. The compounds are potent with high selectivity toward the receptor subtype 2.Pharmaceutical compositions and methods of treatment are also included.
    Type: Grant
    Filed: April 1, 1998
    Date of Patent: February 15, 2000
    Assignee: Merck & Co., Inc.
    Inventors: Lihu Yang, Arthur A. Patchett, Alexander Pasternak, Kevin Chapman, James R. Tata, Liangqin Guo
  • Method of treating diabetes and related disease states
    Patent number: 6020382
    Abstract: The instant invention is concerned with acetylphenols which are useful as antiobesity and antidiabetic compounds. Compositions and methods for the use of the compounds in the treatment of diabetes and obesity and for lowering or modulating triglyceride levels and cholesterol levels or raising high density lipoprotein levels or for increasing gut motility or for treating atherosclerosis are also disclosed.
    Type: Grant
    Filed: January 4, 1999
    Date of Patent: February 1, 2000
    Assignee: Merck & Co., Inc.
    Inventors: Thomas W. Doebber, Joel P. Berger, Gregory D. Berger, Mark D. Leibowitz, David E. Moller, John T. Olson, Arthur A. Patchett, Richard B. Toupence
  • (Methylsulfonyl)phenyl-2-(5H)-furanones as COX-2 inhibitors
    Patent number: 6020343
    Abstract: The invention encompasses the novel compound of Formula I useful in the treatment of cyclooxygenase-2 mediated diseases. ##STR1## The invention also encompasses certain pharmaceutical compositions for treatment of cyclooxygenase-2 mediated diseases comprising compounds of Formula I.
    Type: Grant
    Filed: June 15, 1998
    Date of Patent: February 1, 2000
    Assignee: Merck Frosst Canada, Inc.
    Inventors: Michel Belley, Jacques Yves Gauthier, Erich Grimm, Yves LeBlanc, Chun-Sing Li, Michel Therien, Cameron Black, Petpiboon Prasit, Cheuk-Kun Lau, Patrick Roy
  • Spiro-substituted azacycles as neurokinin antagonists
    Patent number: 6013652
    Abstract: Disclosed are spiro-substituted azacycles of formula I are tachykinin receptor antagonists useful in the treatment of inflammatory diseases, pain or migraine, and asthma. In particular compounds of formula I are shown to be neurokinin antagonists.
    Type: Grant
    Filed: December 4, 1997
    Date of Patent: January 11, 2000
    Assignee: Merck & Co., Inc.
    Inventors: Malcolm Maccoss, Sander G. Mills, Shrenik K. Shah, Yuan-Ching P. Chiang, Patrick T. Dunn, Hiroo Koyama
  • 2-aminopyridines as inhibitors of cyclooxygenase-2
    Patent number: 6004950
    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. ##STR1## The invention also encompasses certain pharmaceutical compositions for treatment of cyclooxygenase-2 mediated diseases comprising compounds of Formula I.
    Type: Grant
    Filed: September 11, 1998
    Date of Patent: December 21, 1999
    Assignee: Merck Frosst Canada, Inc.
    Inventors: Richard Friesen, Daniel Dube, Denis Deschenes
  • Pyridazinones as inhibitors of cyclooxygenase-2
    Patent number: 6004960
    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. ##STR1## The invention also encompasses certain pharmaceutical compositions for treatment of cyclooxygenase-2 mediated diseases comprising compounds of Formula I.
    Type: Grant
    Filed: March 13, 1998
    Date of Patent: December 21, 1999
    Assignee: Merck Frosst Canada, Inc.
    Inventors: Chun Sing Li, Jacques Y. Gauthier, Cheuk K. Lau, Michel Therien
  • Substituted pyridines as selective cyclooxygenase-2 inhibitors
    Patent number: 6001843
    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: October 29, 1998
    Date of Patent: December 14, 1999
    Assignee: Merck & Co., Inc.
    Inventors: Daniel Dube, Rejean Fortin, Richard Friesen, Zhaoyin Wang, Jacques Yves Gauthier
  • Antibiotic synthesis
    Patent number: 5998612
    Abstract: A method of preparing intermediates for carbapenem antibiotics characterized by treating a N-deprotected acetoxy conpound of the formula: ##STR1## in the presence of a Lewis acid or a silylating agent to yeild an intermediate; and cyclizing the intermediate in the presence of rhodium (II) acetate to form a bicyclic ketoester.
    Type: Grant
    Filed: June 12, 1992
    Date of Patent: December 7, 1999
    Inventors: Paul J. Reider, Edward J. J. Grabowski
  • Bisaryl COX-2 inhibiting compounds, compositions and methods of use
    Patent number: 5994379
    Abstract: The present invention relates to inhibitors of COX-2, compositions which contain such compounds and methods of use. The compounds are represented by formula I: ##STR1## and include pharmaceutically acceptable salts and esters thereof.
    Type: Grant
    Filed: February 9, 1999
    Date of Patent: November 30, 1999
    Assignee: Merck Frosst Canada, Inc.
    Inventors: Christopher I. Bayly, Cameron Black, Nathalie Ouimet, David Percival, Serge Leger, Marc Ouellet
  • Homoerythromycin A derivatives modified at the 4"-and 8A-positions
    Patent number: 5985844
    Abstract: Compounds of the formula: ##STR1## where R is hydrogen, hydroxyl, alkyl or acyl, R' and R" together are oxo, hydroxyimino or alkoxyimino, and R' and R" independently are hydrogen, hydroxyl, acyloxy, or amino substituted by any of hydrogen, alkylcarbonyl, arylcarbonyl, aralkylcarbonyl, alkoxycarbonyl, aralkoxycarbonyl, alkylsulfonyl or arylsulfonyl, and n is 0 or 1, and the pharmaceutically acceptable salts thereof. The compounds are macrolide antibiotics and are also useful as intermediates to the synthesis of other macrolide antibiotics. Pharmaceutical compositions and methods of their use are also provided for.
    Type: Grant
    Filed: March 26, 1992
    Date of Patent: November 16, 1999
    Assignee: Merck & Co., Inc.
    Inventors: James V. Heck, William J. Leanza, Ronald W. Ratcliffe, Thomas N. Salzmann, Kothandaraman Shankaran, Michael J. Szymonifka, Robert R. Wilkening
  • (Methylsulfonyl)phenyl-2-(5H)-furanones as COX-2 inhibitors
    Patent number: 5981576
    Abstract: The invention encompasses the novel compound of Formula A that is useful in the treatment of cyclooxygenase-2 mediated diseases. ##STR1## The invention also encompasses certain pharmaceutical compositions for treatment of cyclooxygenase-2 mediated diseases comprising compounds of Formula A.
    Type: Grant
    Filed: June 15, 1998
    Date of Patent: November 9, 1999
    Assignee: Merck Frosst Canada, Inc.
    Inventors: Michel Belley, Jacques Yves Gauthier, Erich Grimm, Yves LeBlanc, Chun-Sing Li, Michel Therien, Cameron Black, Petpiboon Prasit, Cheuk-Kun Lau, Patrick Roy
  • Substituted 2-aminopyridines as inhibitors of nitric oxide synthase
    Patent number: 5972975
    Abstract: Substituted 2-aminopyridine compounds of Formula (I) and pharmaceutically acceptable salts which have been found useful in the treatment of nitric oxide synthase mediated diseases and disorders.
    Type: Grant
    Filed: May 22, 1997
    Date of Patent: October 26, 1999
    Assignee: Merck & Co., Inc.
    Inventors: Craig Esser, William Hagmann, William Hoffman, Shrenik Shah, Kenny Wong, Renee Chabin, Ravindra Guthikonda, Malcolm Maccoss, Charles Caldwell, Philippe Durette
  • 5-Methanesulfonamido-3H-isobenzofuran-1-ones as inhibitors of cyclooxygenase-2
    Patent number: 5968958
    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. ##STR1## The invention also encompasses certain pharmaceutical compositions for treatment of cyclooxygenase-2 mediated diseases comprising compounds of Formula I.
    Type: Grant
    Filed: June 19, 1997
    Date of Patent: October 19, 1999
    Assignee: Merck Frosst Canada, Inc.
    Inventors: Daniel Guay, Chun-Sing Li, Nathalie Ouimet