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:
June 27, 1995
Assignee:
Merck Frosst Canada, Inc.
Inventors:
Yves Ducharme, John W. Gillard, Rejean Fortin, Daniel Dube, Yves Girard, Pierre Hamel, Daniel Delorme
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.
Abstract: An improved process for formation of a 5-oxime on avermectin derivatives comprises the treatment of the oxo-compound with hydroxylamine in aqueous isopropanol at pH 1.8-2.1.
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:
April 25, 1995
Assignee:
Merck Frosst Canada, Inc.
Inventors:
Rick Friesen, Robert N. Young, Yves Girard, Marc Blouin, Daniel Dube
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:
February 14, 1995
Assignee:
Merck Frosst Canada, Inc.
Inventors:
Richard Frenette, John W. Gillard, John H. Hutchinson, Petpiboon Prasit, 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 diarrhea, hypertension, angina, platelet aggregation, cerebral spasm, premature labor, spontaneous abortion, dysmenorrhea, and migraine.
Type:
Grant
Filed:
December 16, 1993
Date of Patent:
January 10, 1995
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 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, glomemlar nephritis, hepatitis, endotoxemia, uveitis, and allograft rejection and in preventing the formation of atherosclerotic plaques.
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:
June 23, 1993
Date of Patent:
November 1, 1994
Assignee:
Merck Frosst Canada, Inc.
Inventors:
Rejean Fortin, Yves Girard, Erich Grimm, John Hutchinson, John Scheigetz
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.
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.
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.
Abstract: The present invention relates to intermediates, pradimic acids and pradimic acid amides of the formula (II) ##STR1## wherein R is OH or NH.sub.2 ; R.sup.1 is hydrogen or a group of the formula ##STR2## with the proviso that when R is OH, R.sup.1 is not hydrogen; Y is OH or NR.sup.2 R.sup.3 ; R.sup.2 is hydrogen or methyl; R.sup.3 is hydrogen, C.sub.1-5 alkyl, or an amino protecting group; R.sup.4 is hydrogen, hydroxy protecting group, or .beta.-D-xylosyl. The invention relates also to novel processes for the preparation of pradimic acids and pradimic acid amides, as well as novel pradimicin derivatives prepared therefrom.
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: 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: An antibiotic designated BMY-42448 is produced by fermentation of Micromonospora narashinoensis strain C39217-R109-7 (ATCC-53791). BMY-42448 exhibits both in vitro and in vivo antitumor activity.
Type:
Grant
Filed:
October 10, 1991
Date of Patent:
December 14, 1993
Assignee:
Bristol-Myers Squibb Company
Inventors:
Daniel R. Schroeder, Kin S. Lam, Grace A. Hesler, Donald R. Gustavson, Koji Tomita, Ronald L. Berry
Abstract: The present invention relates to an arylsulfatase of microbial origin. The enzyme may be linked to an antibody against a tumor-associated antigen and the resulting conjugate used in conjuction with a sulfated prodrug of a 4'-demethylepipodophyllotoxin glucoside derivative, particularly etoposide in cancer chemotherapy.
Abstract: The present invention relates to 10-desacetoxy-11,12-dihydrotaxol-10,12(18)-diene derivatives which are useful as antitumor agents and as intermediates for the preparation of 10-desacetoxytaxol. Also disclosed is a novel process for the preparation of 10-desacetoxytaxol which comprises treating hydroxy protected 10-deacetyltaxol with 1,1,2-trifluoro-2-chlorotriethylamine followed by catalytic hydrogenation.
Abstract: 3-Fluorosulfonyloxyceph-3-ems having a protected amino or acylamino group in the 7-position are subject to carbon-carbon bond formation at the 3-position by means of a palladium catalyzed coupling reaction with substituted organostannanes. A process for preparing cefprozil is disclosed.
Type:
Grant
Filed:
October 31, 1990
Date of Patent:
September 14, 1993
Assignee:
Bristol-Myers Squibb Company
Inventors:
Stephen R. Baker, Chester Sapino, Jr., Gregory P. Roth
Abstract: The present invention provides pradimicin analogs which exhibit improved water solubility relative to parent compounds. These novel agents are useful in treatment of fungal infections.
Type:
Grant
Filed:
December 3, 1991
Date of Patent:
July 13, 1993
Assignee:
Bristol-Myers Squibb Company
Inventors:
Hajime Kamachi, Seiji Iimura, Satsuki Okuyama, Shimpei Aburaki, Takayuki Naito, Yasutsugu Ueda, Leonard B. Crast, Jr., Amarendra B. Mikkilineni
Abstract: The present invention relates to a novel .alpha.-glucosidase inhibitor, pradimicin Q, having the following formula ##STR1## and its pharmaceutically acceptable base salts.