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 diarrhea, hypertension, angina, platelet aggregation, cerebral spasm, premature labor, spontaneous abortion, dysmenorrhea, and migraine.
Type:
Grant
Filed:
September 25, 1992
Date of Patent:
May 3, 1994
Assignee:
Merck Frosst Canada, Inc.
Inventors:
John W. Gillard, John H. Hutchinson, Richard Frenette, Michel Therien
Abstract: Substituted quinazolinones and pyridopyrimidines of structural formula 1 ##STR1## are angiotensin II antagonists useful in the treatment of disorders related to the renin-angiotensin system (RAS) such as hypertension, congestive heart failure, ocular hypertension and certain CNS disorders.
Type:
Grant
Filed:
July 22, 1993
Date of Patent:
May 3, 1994
Assignees:
Merck & Co., Inc., E. I. Du Pont de Nemours and Co.
Abstract: Conformationally constrained tricyclic derivatives of the thienodiazocine and thienothiadiazocine classes of compounds and ring homologs thereof are topically effective carbonic anhydrase inhibitors useful in the treatment of ocular hypertension and glaucoma associated therewith.
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:
August 27, 1992
Date of Patent:
May 3, 1994
Assignee:
Merck Frosst Canada, Inc.
Inventors:
Yves Girard, Daniel Delorme, Rejean Fortin, Daniel Dube, Pierre Hamel, Carol Lepine, Yves Ducharme
Abstract: Inhibition of renal cancer, melanoma, colon cancer, lung cancer and leukemia cells by administration of compounds from the bafilomycin and hygrolidin groups of compounds.
Abstract: The present invention concerns a fluid pharmaceutical composition intended to be brought into contact with a physiological fluid, characterized in that it contains, as active principle, at least one 4-quinolone derivative complexed with a divalent metal ion selected from Cu.sup.++, Zn.sup.++ and Mg.sup.++, the said complex being in the form of particles of a size compatible with parenteral or ophthalmic administration, in suspension in a fluid dispersant and not being subject to a crystalline growth phenomenon during storage of the said composition; the invention also provides a process for preparing a pharmaceutical composition of this type.
Abstract: An organism of the Sporormiella species produces a compound having the formula ##STR1## which is useful. The compound is useful as an antifungal agent.
Abstract: The present invention is directed to farnesyl pyrophosphate analogs which inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention, and methods for inhibiting farnesyl-protein transferase and the farnesylation of the oncogene protein Ras.
Type:
Grant
Filed:
September 27, 1991
Date of Patent:
March 29, 1994
Assignee:
Merck & Co., Inc.
Inventors:
Neville J. Anthony, Ta-Jyh Lee, Robert L. Smith, Gerald E. Stokker
Abstract: Macrocyclic compounds of general Structure I: ##STR1## Wherein M is C or N are angiotensin II receptor (A-II) antagonists useful in the treatment of certain cardiovascular dysfunctions and ocular hypertension.
Type:
Grant
Filed:
August 18, 1992
Date of Patent:
March 8, 1994
Assignee:
Merck & Co., Inc.
Inventors:
Stephen E. deLaszlo, Tomasz Glinka, Robert B. Nachbar, Eric E. Allen, Kristine Prendergast
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 diarrhea, hypertension, angina, platelet aggregation, cerebral spasm, premature labor, spontaneous abortion, dysmenorrhea, and migraine.
Type:
Grant
Filed:
September 25, 1992
Date of Patent:
March 1, 1994
Assignee:
Merck Frosst Canada, Inc.
Inventors:
John W. Gillard, John H. Hutchinson, Michel Therien
Abstract: There is disclosed a series of macrolides isolated from the fermentation broth of microorganisms identified as MA-6825, MA-6864 and MA-6865. The structure of the novel compounds isolated from the microorganisms is presented based upon analytical studies. The compounds are highly potent antiparasitic, insecticidal, and anthelmintic agents and are related to the class of macrolides known as milbemycins. Compositions for such uses are also disclosed.
Type:
Grant
Filed:
April 13, 1992
Date of Patent:
March 1, 1994
Assignee:
Merck & Co., Inc.
Inventors:
Robert T. Goegelman, Elvira Munguira, Maria T. Diez Matas, Ruth S. Sykes, Yu L. Kong, Jerrold M. Liesch, Gregory L. Helms, E. Tracy Turner Jones
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:
October 26, 1992
Date of Patent:
January 25, 1994
Assignee:
Merck Frosst Canada, Inc.
Inventors:
Robert N. Young, Yves Girard, John W. Gillard, Laird A. Trimble, John Scheigetz, James A. Yergey, Yves Ducharme, Deborah A. Nicoll-Griffith, John H. Hutchinson
Abstract: Compounds of general formula: ##STR1## are topically effective carbonic anhydrase inhibitors useful in the treatment of ocular hypertension and related disorders such as glaucoma.
Type:
Grant
Filed:
September 9, 1992
Date of Patent:
January 4, 1994
Assignee:
Merck & Co., Inc.
Inventors:
John J. Baldwin, Jacob M. Hoffman, Jr., James H. Jones, Clarence S. Rooney, Anthony M. Smith
Abstract: Substituted hexahydrobenzopyran derivatives of the Formulae A, B, or C are useful as angiotensin II antagonists: ##STR1##
Type:
Grant
Filed:
October 16, 1992
Date of Patent:
January 4, 1994
Assignee:
Merck & Co., Inc.
Inventors:
Maria T. Diez, Michael A. Goetz, Robert A. Giacobbe, Otto D. Hensens, Leeyan Huang, Isabel Martin, E. Tracy T. Jones, Siobhan Stevens-Miles, Yu L. Kong
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 diarrhea, hypertension, angina, platelet aggregation, cerebral spasm, premature labor, spontaneous abortion, dysmenorrhea, and migraine.
Type:
Grant
Filed:
September 25, 1992
Date of Patent:
December 28, 1993
Assignee:
Merck Frosst Canada Inc.
Inventors:
Richard Frenette, Michel Therien, John H. Hutchinson
Abstract: An improved synthesis is described for producing a quinolinylmethoxyphenyl hydrazine which is an intermediate in the preparation of quinolinylmethoxyindoles useful as inhibitors of leukotriene biosynthesis. The improved process eliminates two isolation steps and yields a product of high purity.
Abstract: Various cyproheptadine derivatives sensitize multidrug resistant cells to certain chemotherapeutic agents. As such, these cyproheptadine derivatives are useful as adjuncts in the reversal of multidrug resistance in mammalian tumor cells either as compounds, pharmaceutically acceptable salts, or pharmaceutical composition ingredients in combination with anticancer chemotherapeutic agents or compounds.
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 diarrhea, hypertension, angina, platelet aggregation, cerebral spasm, premature labor, spontaneous abortion, dysmenorrhea, and migraine.
Type:
Grant
Filed:
December 14, 1992
Date of Patent:
December 21, 1993
Assignee:
Merck Frosst Canada, Inc.
Inventors:
Petpiboon Prasit, Rejean Fortin, John H. Hutchinson, Michel L. Belley, Serge Leger, Richard Frenette, John Gillard