Abstract: Compounds having the formula I: ##STR1## are inhibitors of 5-lipoxygenase 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, psoriasis, uveitis, and allograft rejection and in preventing the formation of atherosclerotic plaques.
Type:
Grant
Filed:
November 19, 1992
Date of Patent:
May 24, 1994
Assignee:
Merck Frosst Canada, Inc.
Inventors:
Yves Girard, John H. Hutchinson, Michel Therien, Daniel Delorme
Abstract: Compounds having the formula I: ##STR1## are inhibitors of the 5-lipoxygenase enzyme 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, psoriasis, uveitis, and allograft rejection and in preventing the formation of atherosclerotic plaques.
Type:
Grant
Filed:
June 29, 1992
Date of Patent:
May 24, 1994
Assignees:
Merck & Co., Inc., Merck Frosst Canada Inc.
Inventors:
John Y. L. Chung, Robert A. Reamer, Yves Girard, Pierre Hamel
Abstract: The LTD.sub.4 receptor has been defined by radioligand binding studies as a member of the family of G-protein coupled receptors. A photoactivable azido derivative of LTD.sub.4 ([.sup.125 I]Azido-LTD.sub.4) has been synthesized for use as a photoaffinity probe. Photoactivation of ([.sup.125 I]Azido-LTD.sub.4 under equilibrium binding conditions revealed the selective radiolabeling of a 45 kDa protein in guinea-pig lung membranes, as visualized by SDS-PAGE and autoradiography.
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: 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: Benzalkonium chloride and benzethorium chloride are each useful in radiopharmaceutical preparations (optionally in the presence of a polymyxin or a polymyxin derivative) as bacteriostatic agents which are compatible with anti-oxidants.
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: 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 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: 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
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:
April 10, 1992
Date of Patent:
December 14, 1993
Assignee:
Merck Frosst Canada, Inc.
Inventors:
Robert Zamboni, Daniel Guay, Marc LaBelle
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:
October 10, 1991
Date of Patent:
November 30, 1993
Assignee:
Merck Frosst Canada, Inc.
Inventors:
Michel L. Belley, Yves LeBlanc, Marc Labelle
Abstract: A form of 3-[N-(p-chlorobenzyl)-3-(t-butylthio)-5-(quinolin-2-ylmethoxy)indol-2-yl]- 2,2-dimethylpropanoic acid sodium salt, obtained by freeze or spray drying, is more soluble in water than the crystalline form thereof. The compound is useful as an anti-asthmatic, anti-allergic, anti-inflammatory, or cytoprotective agent. It is also useful in treating diarrhea, hypertension, angina, platelet aggregation, cerebral spasm, premature labor, spontaneous abortion, dysmenorrhea, and migraine.
Abstract: A complex of cyclodextrin and 3-[N-(p-chlorobenzyl)-3-(t-buthylthio)-5-(quinolin-2-ylmethoxy)indol-2-yl] -2,2-dimethylpropanoic acid, sodium salt is more soluble in water than the sodium salt alone. The complex is useful as an anti-asthmatic, anti-allergic, anti-inflammatory, or cytoprotective agent. It is also useful in treating diarrhea, hypertension, angina, platelet aggregation, cerebral spasm, premature labor, spontaneous abortion, dysmenorrhea, and migraine.
Abstract: This invention relates to compounds having the formula I: ##STR1## wherein R.sup.1 is H, F or MeO, which 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.
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:
October 12, 1993
Assignee:
Merck Frosst Canada, Inc.
Inventors:
Yves Girard, Rejean Fortin, Daniel Delorme, Daniel Dube, Pierre Hamel, Yves Ducharme, John W. Gillard
Abstract: Derivatives of synthetic fragments of mammalian atrial natriuretic factor (ANF) in which a chelate molecule is attached to the N-terminal of the peptide are described. The chelate component allows the facile labelling of these peptides with metallic isotopes such as Tc-99m, Ga-67, In-111 and others. These radioactive chelates are useful in determining the in vivo behavior and fate of derivatives of ANF.
Type:
Grant
Filed:
February 27, 1992
Date of Patent:
September 28, 1993
Assignee:
Merck Frosst Canada, Inc.
Inventors:
Richard J. Flanagan, F. Peter Charleson
Abstract: Compounds having the formula: ##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:
October 28, 1991
Date of Patent:
August 3, 1993
Assignee:
Merck Frosst Canada, Inc.
Inventors:
Robert Zamboni, Petpiboon Prasit, Robert N. Young
Abstract: Benzalkonium chloride and benzethonium chloride are each useful in radiopharmaceutical preparations as bacteriostatic agents which are compatible with anti-oxidants.
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:
July 13, 1993
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