Patents Assigned to Merck Frosst Canada, Inc.
  • Process for the preparation of radiolabeled meta-halobenzylguanidine
    Patent number: 5565185
    Abstract: The present invention provides a no-carrier-added synthesis of radiolabeled meta-halobenzylguanidine by halodestannylation which comprises reacting a meta-trialkylstannylbenzylguanidine with a source of radionuclide of a halogen. The present invention also provides meta-trialkylstannylbenzylguanidine as intermediates in the afore-mentioned process.
    Type: Grant
    Filed: July 20, 1994
    Date of Patent: October 15, 1996
    Assignee: Merck Frosst Canada, Inc.
    Inventors: Duncan H. Hunter, Alok Goel, Richard J. Flanagan
  • Unsaturated hydroxyalkylquinoline acids as leukotriene antagonists
    Patent number: 5565473
    Abstract: Compounds having the formula I: ##STR1## are leukotriene antagonists and inhibitors of leukotriene biosynthesis. These compounds are useful as anti-asthmatic, anti-allergic, anti-inflammatory, and cytoprotective agents. They are also useful in treating angina, cerebral spasm, glomerular nephritis, hepatitis, endotoxemia, uveitis, and allograft rejection.
    Type: Grant
    Filed: February 23, 1995
    Date of Patent: October 15, 1996
    Assignee: Merck Frosst Canada, Inc.
    Inventors: Michel L. Belley, Serge Leger, Marc Labelle, Patrick Roy, Yi B. Xiang, Daniel Guay
  • TC or RE radionuclide labelled chelate, hexapeptide complexes useful for diagnostic or therapeutic applications
    Patent number: 5556939
    Abstract: Technetium or rhenium radionuclide labelled chelate-hexapeptide complexes are useful for the selective detection or treatment of tumors with somatostatin receptors. In particular, compounds of formula: ##STR1## (wherein R, R.sup.1, R.sup.3 and A are as defined herein) incorporating an N3S2 chelate may be labelled with a radionuclide. The resulting complexes are useful as radioimaging agents or as radiopharmaceuticals for the treatment of certain tumors.
    Type: Grant
    Filed: October 13, 1994
    Date of Patent: September 17, 1996
    Assignee: Merck Frosst Canada, Inc.
    Inventors: Richard J. Flanagan, Jean-Marc Dufour, Keith T. Hogan
  • DNA encoding precursor of interleukin-1 beta converting enzyme - related cysteine proteinase III (ice rel-III)
    Patent number: 5552536
    Abstract: A complementary DNA (cDNA) encoding full length form of ICE.sub.rel -III is identified, sequenced and isolated. The cDNA is cloned into expression vectors for expression in recombinant hosts. The cDNA is useful to produce recombinant full length ICE.sub.rel -III. The cDNA and the recombinant ICE.sub.rel -III protein derived therefrom are useful in diagnostic kits, laboratory reagents and assays. The cDNA and the recombinant ICE.sub.rel -III protein may be used to identify compounds that affect ICE.sub.rel -III function, inflammation and cell apoptosis. ICE.sub.rel -III function, inflammation and cell apoptosis may also be modulated by ICE.sub.rel -III antisense or gene therapy.
    Type: Grant
    Filed: April 8, 1994
    Date of Patent: September 3, 1996
    Assignee: Merck Frosst Canada, Inc.
    Inventors: Donald W. Nicholson, Ambereen Ali, Neil A. Munday, John P. Vaillancourt
  • Aryl substituted 5,5 fused aromatic nitrogen compounds as anti-inflammatory agents
    Patent number: 5552422
    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: January 11, 1995
    Date of Patent: September 3, 1996
    Assignee: Merck Frosst Canada, Inc.
    Inventors: Jacques Y. Gauthier, Cheuk K. Lau, Yves LeBlanc, Chun-Sing Li, Patrick Roy, Michel Therien, Zhaoyin Wang
  • Bisarylcarbinol derivatives as inhibitors of leukotriene biosynthesis
    Patent number: 5552437
    Abstract: Compounds having the Formula I:R.sup.1 R.sup.2 C(OR.sup.3)--Ar.sup.1 --X--Ar.sup.2 --Ar.sup.3Ire inhibitors of leukotriene biosynthesis. These compounds are useful as anti-asthmatic, anti-allergic, anti-inflammatory, and cytoprotective agents. They are also useful in treating angina, cerebral spasm, glomerular nephritis, hepatitis, endotoxemia, uveitis, and allograft rejection and in preventing the formation of atherosclerotic plaques.
    Type: Grant
    Filed: October 27, 1994
    Date of Patent: September 3, 1996
    Assignee: Merck Frosst Canada, Inc.
    Inventors: Daniel Delorme, Daniel Dub e, Yves Ducharme, Erich L. Grimm, Richard Friesen, Carole Lepine
  • Phenyl heterocycles as cox-2 inhibitors
    Patent number: 5550142
    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: May 8, 1995
    Date of Patent: August 27, 1996
    Assignee: Merck Frosst Canada Inc.
    Inventors: Yves Ducharme, Jacques Y. Gauthier, Petpiboon Prasit, Yves Leblanc, Zhaoyin Wang, Serge Leger, Michel Therien
  • Human cyclooxygenase-2 cDNA and assays for evaluating cyclooxygenase-2 activity
    Patent number: 5543297
    Abstract: The invention discloses a human cyclooxygenase-2 cDNA, a human cyclooxygenase-2 and assays for preferentially and independently measuring cyclogenase-2 or cyclooxygenase-1 activity present in a given sample.
    Type: Grant
    Filed: May 6, 1993
    Date of Patent: August 6, 1996
    Assignee: Merck Frosst Canada, Inc.
    Inventors: Wanda A. Cromlish, Brian P. Kennedy, Gary O'Neill, Philip J. Vickers, Elizabeth Wong, Joseph A. Mancini
  • High affinity chelates containing isothiocyanate groups, useful for coupling with peptides and proteins
    Patent number: 5539138
    Abstract: The ligands HBED-SCN, HBPD-SCN, and HTDD-SCN are provided which have enhanced ease of reaction with peptides or proteins and which are suitable for chelating with radioisoptopes, especially Indium-.sup.III and Gallium-.sup.67.
    Type: Grant
    Filed: July 28, 1994
    Date of Patent: July 23, 1996
    Assignee: Merck Frosst Canada, Inc.
    Inventors: Richard J. Flanagan, Keith T. Hogan, Jean-Marc Dufour, F. Peter Charleson
  • Phenyl heterocycles as COX-2 inhibitors
    Patent number: 5536752
    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: May 8, 1995
    Date of Patent: July 16, 1996
    Assignee: Merck Frosst Canada Inc.
    Inventors: Yves Ducharme, Jacques Y. Gauthier, Petpiboon Prasit, Yves Leblanc, Zhaoyin Wang, Serge Leger, Michel Therien
  • Indole derivatives with affinity for the cannabinoid receptor
    Patent number: 5532237
    Abstract: Disclosed are indole derivatives having activity on the cannabinoid receptors and the methods of their preparation. The compounds are useful for lowering ocular intra ocular pressure and treating glaucoma because of the activity on the cannabinoid receptor.
    Type: Grant
    Filed: February 15, 1995
    Date of Patent: July 2, 1996
    Assignee: Merck Frosst Canada, Inc.
    Inventors: Michel Gallant, Yves Gareau, Daniel Guay, Marc Labelle, Petpiboon Prasit
  • Bisarylcarbinol cinnamic acids as inhibitors of leukotriene biosynthesis
    Patent number: 5527827
    Abstract: Compounds having the Formula I:R.sup.1 R.sup.2 C(OR.sup.3)--Ar.sup.1 --X--Ar.sup.2 --C(Ar.sup.3).dbd.CHCO.sub.2 H Iare inhibitors of leukotriene biosynthesis. These compounds are useful as anti-asthmatic, anti-allergic, anti-inflammatory, and cytoprotective agents. They are also useful in treating angina, cerebral spasm, glomerular nephritis, hepatitis, endotoxemia, uveitis, and allograft rejection and in preventing the formation of atherosclerotic plaques.
    Type: Grant
    Filed: October 27, 1994
    Date of Patent: June 18, 1996
    Assignee: Merck Frosst Canada, Inc.
    Inventors: Daniel Delorme, Yves Ducharme, Richard Friesen, Erich L. Grimm, Carole Lepine
  • Diaryl bicyclic heterocycles as inhibitors of cyclooxygenase-2
    Patent number: 5521213
    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: August 29, 1994
    Date of Patent: May 28, 1996
    Assignee: Merck Frosst Canada, Inc.
    Inventors: Petpiboon Prasit, Daniel Guay, Zhaoyin Wang, Serge Leger, Michel Therien
  • DNA encoding prostaglandin receptor IP
    Patent number: 5516652
    Abstract: A novel 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: October 6, 1993
    Date of Patent: May 14, 1996
    Assignee: Merck Frosst Canada Inc.
    Inventors: Mark Abramovitz, Yves Boie, Richard Grygorczyk, Kathleen Metters, Thomas H. Rushmore, Deborah M. Slipetz
  • N-benzyl-3-indoleacetic acids as antiinflammatory drugs
    Patent number: 5510368
    Abstract: The invention encompasses the novel compound of Formula I as well as a method of treating inflammation and, in particular, 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 inflammation and, in particular, cyclooxygenase-2 mediated diseases comprising compounds of Formula I.
    Type: Grant
    Filed: May 22, 1995
    Date of Patent: April 23, 1996
    Assignee: Merck Frosst Canada, Inc.
    Inventors: Cheuk K. Lau, Cameron Black, Michel Belley
  • Pyridine-substituted benzyl alcohols as leukotriene antagonists
    Patent number: 5506227
    Abstract: Compounds having the formula I: ##STR1## are antagonists of the actions of leukotrienes. These compounds are useful as anti-asthmatic, anti-allergic, anti-inflammatory, and cytoprotective agents. They are also useful in treating angina, cerebral spasm, glomerular nephritis, hepatitis, endotoxemia, uveitis, and allograft rejection.
    Type: Grant
    Filed: April 13, 1992
    Date of Patent: April 9, 1996
    Assignee: Merck Frosst Canada, Inc.
    Inventors: Robert Zamboni, Daniel Guay, Jacques-Yves Gauthier
  • Phenyl heterocycles as cox-2 inhibitors
    Patent number: 5474995
    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: January 10, 1994
    Date of Patent: December 12, 1995
    Assignee: Merck Frosst Canada, Inc.
    Inventors: Yves Ducharme, Jacques Y. Gauthier, Petpiboon Prasit, Yves Leblanc, Zhaoyin Wang, Serge Leger, Michel Therien
  • Diaryl 5,6-fused heterocyclic acids as leukotriene antagonists
    Patent number: 5472964
    Abstract: Compounds having the formula I: ##STR1## are antagonists of the actions of leukotrienes. These compounds are useful as anti-asthmatic, anti-allergic, anti-inflammatory, and cytoprotective agents. They are also useful in treating angina, cerebral spasm, glomerular nephritis, hepatitis, endotoxemia, uveitis, and allograft rejection.
    Type: Grant
    Filed: June 16, 1994
    Date of Patent: December 5, 1995
    Assignee: Merck Frosst Canada, Inc.
    Inventors: Robert N. Young, Marc Labelle, Yves Leblanc, Yi B. Xiang, Cheuk K. Lau, Claude Dufresne, Yves Gareau
  • Peptide sequences and antipeptide antisera for detecting human cyclooxygenase-1 and cyclooxygenase-2 proteins
    Patent number: 5459239
    Abstract: This invention discloses novel immunogenic peptide sequences, derived from the human cyclooxygenase-1 and cyclooxygenase-2 cDNAs which elicit specific non cross-reactive antibody responses. Assays are also disclosed for selectively and independently detecting cyclooxygenase-1 or cyclooxygenase-2 proteins present in a given biological sample.
    Type: Grant
    Filed: January 24, 1994
    Date of Patent: October 17, 1995
    Assignee: Merck Frosst Canada Inc.
    Inventors: Gary O'Neill, Philip J. Vickers, Stacia Kargman, Jillian F. Evans
  • Arylbicyclooctanes as inhibitors of leukotriene biosynthesis
    Patent number: 5459271
    Abstract: Compounds having the formula I: ##STR1## are inhibitors of leukotriene biosynthesis. These compounds are useful as anti-asthmatic, anti-allergic, anti-inflammatory, and cytoprotective agents. They are also useful in treating angina, cerebral spasm, glomerular nephritis, hepatitis, endotoxemia, uveitis and allograft rejection and in preventing the formation of atherosclerotic plaques.
    Type: Grant
    Filed: July 20, 1993
    Date of Patent: October 17, 1995
    Assignee: Merck Frosst Canada, Inc.
    Inventors: Richard W. Friesen, Yves Girard, Daniel Dube