Patents Assigned to Merck Frosst Canada, Inc.
  • 4,7-diacyloxybenzofuran derivatives
    Patent number: 4912131
    Abstract: 4,7-Diacyloxybenzofuran derivatives of Formula I, are disclosed. These compounds are useful as inhibitors of mammalian leukotriene biosynthesis. As such, these compounds are useful therapeutic agents for treating allergic conditions, asthma, cardiovascular disorders, inflammation, psoriasis and allergic conjunctivitis. The compounds are also useful as analgesics and as cytoprotective agents.
    Type: Grant
    Filed: October 11, 1988
    Date of Patent: March 27, 1990
    Assignee: Merck Frosst Canada, Inc.
    Inventors: Julian Adams, Yvan Guindon
  • Cyclohept[b]indoleakanoic acids, pharmaceutical compositions and use
    Patent number: 4906654
    Abstract: Cyclohept[b]indolealkanoic acids and acid derivatives are disclosed. The compounds act as prostaglandin and thromboxane antagonists and are useful in treating asthma, diarrhea, hypertension, angina, platelet aggregation, cerebral spasm, premature labor, spontaneous abortion, dysmenorrhea and nephrotoxicity caused by cyclosporin A and as cytoprotective agents.
    Type: Grant
    Filed: June 27, 1988
    Date of Patent: March 6, 1990
    Assignee: Merck Frosst Canada, Inc.
    Inventors: John W. Gillard, Howard E. Morton, Yvan Guindon, Yves Girard, Christiane Yoakim
  • Fluoro-sulfones
    Patent number: 4906658
    Abstract: Compounds of Formula I ##STR1## the pharmaceutically acceptable salts, and the gamma-lactone form thereof are described. They are antagonists of leukotrienes and SRS-A.
    Type: Grant
    Filed: April 21, 1987
    Date of Patent: March 6, 1990
    Assignee: Merck Frosst Canada, Inc.
    Inventors: Haydn W. R. Williams, Robert N. Young
  • Benzo[a]phenothiazines and hydro-derivatives for inhibiting leukotriene biosynthesis
    Patent number: 4876246
    Abstract: Pharmaceutical compositions containing a compound of Formula I: ##STR1## wherein X is O, S, SO or SO.sub.2 and R.sub.2, R.sub.3, R.sub.4 and R.sub.5 may be positioned anywhere on the structure, or a pharmaceutically-acceptable salt thereof and certain novel benzo[a]phenothiazines, which compositions and compounds are useful in treating allergic conditions, asthma, cardiovascular disorders, inflammation and pain and are useful as cytoprotective agents.
    Type: Grant
    Filed: April 20, 1988
    Date of Patent: October 24, 1989
    Assignee: Merck Frosst Canada, Inc.
    Inventors: Yvan Guindon, Yves Girard, Cheuk K. Lau, Rejean Fortin, Joshua Rokach, Christiane Yoakim
  • Leukotriene antagonists
    Patent number: 4871756
    Abstract: Compounds having the formula: ##STR1## are antagonists of leukotrienes of C.sub.4, D.sub.4, E.sub.4 and the slow reacting substance of anaphylaxis.As such, these compounds will be useful as anti-asthmatic, anti-allergic, anti-inflammatory and cytoprotective agents.
    Type: Grant
    Filed: February 17, 1987
    Date of Patent: October 3, 1989
    Assignee: Merck Frosst Canada, Inc.
    Inventors: John Gillard, Joshua Rokach, Patrice C. Belanger
  • Benzofuran derivatives useful as inhibitors of mammalian leukotriene biosynthesis
    Patent number: 4863958
    Abstract: Benzofuran derivatives, pharmaceutical compositions and methods of treatment are disclosed. These compounds are useful as inhibitors of mammalian leukotriene biosynthesis. As such, these compounds are useful therapeutic agents for treating allergic conditions, asthma, cardiovascular disorders, inflammation. The compounds ar also useful as analgesics and as cytoprotective agents.
    Type: Grant
    Filed: April 20, 1988
    Date of Patent: September 5, 1989
    Assignee: Merck Frosst Canada, Inc.
    Inventors: Patrice C. Belanger, John Scheigetz, Joshua Rokach
  • Pharmaceutical compositions of phenothiazone derivatives and analogs
    Patent number: 4859667
    Abstract: Phenothiazone derivatives and analogs thereof, pharmaceutical compositions and methods of treatment are disclosed. These compounds are useful as inhibitors of mammalian leukotriene biosynthesis. As such, these compounds are useful therapeutic agents for treating allergic conditions, asthma, cardiovascular disorders and inflammation.
    Type: Grant
    Filed: January 14, 1987
    Date of Patent: August 22, 1989
    Assignee: Merck Frosst Canada, Inc.
    Inventors: Cheuk K. Lau, Christiane Yoakim, Joshua Rokach, Rejean Fortin, Yvan Guindon
  • Stereoselective synthesis of leukotriene antagonists
    Patent number: 4857659
    Abstract: The present invention relates to a stereo-selective synthesis of leukotriene antagonists. More particularly, this invention relates to the stereo-selective synthesis of (.beta.S,.gamma.R) and (.beta.R,.gamma.S)-4-((3-(4-acetyl-3-hydroxy-2-propyl(phenoxy)propyl)-thio -.gamma.-hydroxy-.beta.-methylbenzenebutanoic acid, and related compounds. These compounds are useful therapeutic agents for treating allergic conditions, asthma, cardiovascular, disorders, inflammation and pain in mammals, especially humans. The compounds are also useful for inducing cytoprotection in mammals, especially humans.
    Type: Grant
    Filed: April 15, 1987
    Date of Patent: August 15, 1989
    Assignee: Merck Frosst Canada, Inc.
    Inventors: Richard Frenette, Jacques-Yves Gauthier, Robert N. Young, Robert Zamboni, Masatoshi Kakushima, Thomas R. Verhoeven
  • Process for the preparation of HMG-CoA reductase inhibitors and intermediate compounds employed therein
    Patent number: 4855481
    Abstract: An intermediate compound of the formula ##STR1## wherein Y is chloro or bromo: Pr is a protecting group selected from benzoyl, acetyl, triphenylsilyl or t-butyldiphenylsilyl:R.sup.5 is C.sub.1-5 alkyl or benzyl; andR.sup.7 is C.sub.1-5 alkyl, benzyl, C.sub.2-5 alkoxyalkyl or C.sub.3-5 alkoxyalkoxyalkyl,useful for the preparation of certain HMG-CoA reductase inhibitors.
    Type: Grant
    Filed: April 4, 1988
    Date of Patent: August 8, 1989
    Assignee: Merck Frosst Canada, Inc.
    Inventors: Yvan Guindon, Christiane Yoakim, Howard E. Morton
  • 2-substituted quinoline dioic acids and pharmaceutical compositions
    Patent number: 4851409
    Abstract: Compounds having the formula: ##STR1## are antagonists of leukotrienes and inhibitors of their biosynthesis. These compounds are useful as anti-asthmatic, anti-allergic, anti-inflammatory, and cytoprotective agents.
    Type: Grant
    Filed: February 5, 1987
    Date of Patent: July 25, 1989
    Assignee: Merck Frosst Canada Inc.
    Inventors: Robert N. Young, Robert Zamboni, Serge Leger
  • Method of inhibiting mammalian leukotriene biosynthesis
    Patent number: 4845083
    Abstract: Phenothiazine derivatives and analogs thereof having the Formula I are useful as inhibitors of the biosynthesis of mammalian leukotrienes. As such, these compounds are useful therapeutic agents for treating allergic conditions, asthma, cardiovascular disorders and inflammation, and are useful as cytoprotective agents.
    Type: Grant
    Filed: January 9, 1987
    Date of Patent: July 4, 1989
    Assignee: Merck Frosst Canada, Inc.
    Inventors: Rejean Fortin, Cheuk K. Lau, Yvan Guindon, Joshua Rokach, Christiane Yoakim
  • Certain pyridyl derivatives useful as leukotriene antagonists
    Patent number: 4845108
    Abstract: Compounds having the formula: ##STR1## are antagonists of leukotrines of C.sub.4, D.sub.4 and E.sub.4, the slow reacting substance of anaphylaxis. These compounds are useful as anti-asthmatic, anti-allergic and anti-inflammatory agents.
    Type: Grant
    Filed: February 17, 1987
    Date of Patent: July 4, 1989
    Assignee: Merck Frosst Canada, Inc.
    Inventors: Robert N. Young, Joshua Rokach
  • Benzofuran 2-carboxylic acid hydrazides useful as inhibitors of leukotriene biosynthesis
    Patent number: 4822803
    Abstract: Compounds of the Formula I: ##STR1## and pharmaceutically acceptable salts thereof are inhibitors of leukotriene biosynthesis. These compounds inhibit the mammalian 5-lipoxygenase enzyme, thus preventing the metabolism of arachidonic acid to the leukotrienes. These compounds are thus useful in the treatment of asthma, allergic disorders, inflammation, skin diseases and certain cardiovascular disorders.
    Type: Grant
    Filed: February 4, 1988
    Date of Patent: April 18, 1989
    Assignee: Merck Frosst Canada, Inc.
    Inventors: Joseph G. Atkinson, Yvan Guindon, Cheuk K. Lau
  • Phenoxypropoxy halophenylacetic acids as leukotriene antagonists
    Patent number: 4820867
    Abstract: Compounds of the formula: ##STR1## are antagonists of leukotrienes of C.sub.4, D.sub.4 and E.sub.4, the slow reacting substance of anaphylaxis. These compounds are useful as anti-asthmatic, anti-allergic and anti-inflammatory agents.
    Type: Grant
    Filed: April 22, 1986
    Date of Patent: April 11, 1989
    Assignee: Merck Frosst Canada, Inc.
    Inventors: Patrice Belanger, Rejean Fortin, Yvan Guindon, Christiane Yoakim, Joshua Rokach
  • 4,7-diacetoxy-2-(4-methoxybenzyl)-3,5,6-trimethylbenzofuran
    Patent number: 4800228
    Abstract: 4,7-Diacyloxybenzofuran derivatives of Formula I, are disclosed. These compounds are useful as inhibitors of mammalian leukotriene biosynthesis. As such, these compounds are useful therapeutic agents for treating allergic conditions, asthma, cardiovascular disorders, inflammation, psoriasis and allergic conjunctivitis. The compounds are also useful as analgesics and as cytoprotective agents.
    Type: Grant
    Filed: June 18, 1987
    Date of Patent: January 24, 1989
    Assignee: Merck Frosst Canada, Inc.
    Inventors: Julian Adams, Yvan Guindon
  • Conjugates of leukotrienes with proteins
    Patent number: 4767745
    Abstract: Leukotrienes may be conjugated with various proteins such as Bovine Serum Albumin (BSA) and Hemocyanin from Giant Keyhole Limpets (KLH) using 1,5-difluoro-2,4-dinitrobenzene or 6-N-maleimidohexanoic acid chloride as coupling agents.These conjugates are useful as reagents in a newly developed immunoassay for leukotrienes, as well as having potential utility as chemical immunotherapeutic agents in the treatment of various allergic and chronic inflammatory diseases of the skin, lung, and airways, including asthma, allergic rhinitis, rheumatoid arthritis, and skin diseases such as psoriasis and eczema.
    Type: Grant
    Filed: May 5, 1986
    Date of Patent: August 30, 1988
    Assignees: Merck Frosst Canada, Inc., Merck & Co., Inc.
    Inventors: Robert N. Young, Joshua Rokach, Edward C. Hayes
  • Leukotriene antagonists
    Patent number: 4761425
    Abstract: Compounds having the formula: ##STR1## are antagonists of leukotrienes of C.sub.4, D.sub.4 and E.sub.4, the slow reacting substance of anaphylaxis. These compounds are useful as anti-asthmatic, anti-allergic, anti-inflammatory agents, and cytoprotective agents.
    Type: Grant
    Filed: December 24, 1984
    Date of Patent: August 2, 1988
    Assignee: Merck Frosst Canada, Inc.
    Inventors: Yves Girard, Joshua Rokach
  • 5-lipoxygenease inhibitors
    Patent number: 4749699
    Abstract: Compounds of the Formula I: ##STR1## are inhibitors of the mammalian 5-lipoxygenase enzyme system of the arachidonic acid cascade. As such, these compounds are useful therapeutic agents for treating allergic conditions, asthma, cardiovascular disorders and inflammation.
    Type: Grant
    Filed: July 21, 1986
    Date of Patent: June 7, 1988
    Assignee: Merck Frosst Canada, Inc.
    Inventors: Joseph G. Atkinson, Yvan Guindon, Patrice C. Belanger, Joshua Rokach
  • Benzyl esters of benzofuran-2-carboxylic acids useful as inhibitors of leukotriene biosynthesis
    Patent number: 4745127
    Abstract: Compounds of the Formula I: ##STR1## and pharmaceutically acceptable salts thereof are inhibitors of leukotriene biosynthesis. These compounds inhibit the mammalian 5-lipoxygenase enzyme, thus preventing the metabolism of arachidonic acid to the leukotrienes. These compounds are thus useful in the treatment of asthma, allergic disorders, inflammation, skin diseases and certain cardiovascular disorders.
    Type: Grant
    Filed: January 7, 1987
    Date of Patent: May 17, 1988
    Assignee: Merck Frosst Canada, Inc.
    Inventors: Joseph G. Atkinson, Yvan Guindon, Cheuk K. Lau
  • Leukotriene antagonists
    Patent number: 4720505
    Abstract: Compounds having the formula: ##STR1## are antagonists of leukotrienes of C.sub.4, D.sub.4 and E.sub.4, the slow reacting substance of anaphylaxis. These compounds are useful as anti-asthmatic, anti-allergic and anti-inflammatory agents.
    Type: Grant
    Filed: November 13, 1984
    Date of Patent: January 19, 1988
    Assignee: Merck Frosst Canada, Inc.
    Inventors: Patrice C. Belanger, John W. Gillard, Joshua Rokach