Abstract: Compounds of structural formula: ##STR1## wherein Ar is an aromatic ring, B is a cyclic moiety fused to Ar of 5-7 members, X and Y are bridging groups, Q is a nitrogen containing heterocycle, R.sup.2 and R.sup.3 are H, substituted or unsubtituted C.sub.1-3 alkyl, C.sub.1-3 alkoxy, N(R).sub.2, halogen, CF.sub.3 or R.sup.5 and R.sup.1 is H or an aryl group.
Type:
Grant
Filed:
July 15, 1991
Date of Patent:
June 1, 1993
Assignee:
Merck & Co., Inc.
Inventors:
John J. Baldwin, David A. Claremon, Jason M. Elliott, Gerald S. Ponticello, David C. Remy, Harold G. Selnick
Abstract: Pharmaceutical compositions containing aromatic 2-benzazepines with fused 5- or 6-membered heterocyclic rings are disclosed which are useful in the treatment of panic disorder or anxiety disorder.
Type:
Grant
Filed:
May 16, 1991
Date of Patent:
May 11, 1993
Assignee:
Merck & Co., Inc.
Inventors:
Mark G. Bock, Ben E. Evans, Roger M. Freidinger
Abstract: Pharmaceutical compositions containing benzodiazepines of the formula: ##STR1## are disclosed which are useful in the treatment of panic disorder or anxiety disorder.
Type:
Grant
Filed:
May 14, 1991
Date of Patent:
April 27, 1993
Assignee:
Merck & Co., Inc.
Inventors:
Roger M. Freidinger, Mark G. Bock, Ben E. Evans
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:
February 5, 1991
Date of Patent:
April 20, 1993
Assignee:
Merck Frosst Canada, Inc.
Inventors:
Petpiboon Prasit, Rejean Fortin, John H. Hutchinson, Michel L. Belley, Serge Leger, John Gillard, Richard Frenette
Abstract: Compounds of the formula ##STR1## are disclosed. These compounds inhibit the angiotensinogen-cleaving action of the natural proteolytic enzyme, renin, are useful in treating, preventing or managing renin-associated hypertension, hyperaldosteronism, congestive heart failure, and glaucoma.
Type:
Grant
Filed:
June 11, 1991
Date of Patent:
March 16, 1993
Assignee:
Merck & Co., Inc.
Inventors:
William J. Greenlee, Ralph A. Rivero, Ann E. Weber, Lihu Yang
Abstract: Pharmaceutical compositions containing Virginiamycin M.sub.1 having the Formula: ##STR1## and Virginiamycin M.sub.1 analogs having the Formulae I-IV: ##STR2## are disclosed which are useful in the treatment of panic disorder or anxiety disorder.
Type:
Grant
Filed:
June 3, 1991
Date of Patent:
February 23, 1993
Assignee:
Merck & Co., Inc.
Inventors:
Roger M. Freidinger, Mark G. Bock, Yiu-Kuen T. Lam, Raymond S. Chang, Otto D. Hensens, Cheryl D. Schwartz, Deborah L. Zink
Abstract: Pharmaceutical compositions containing Triazolobenzodiazepines of the formula: ##STR1## are disclosed which are useful in the treatment of panic disorder or anxiety disorder.
Type:
Grant
Filed:
May 14, 1991
Date of Patent:
February 9, 1993
Assignee:
Merck & Co., Inc.
Inventors:
Roger M. Freidinger, Mark G. Bock, Ben E. Evans
Abstract: Pharmaceutical compositions containing 6-membered heterocyclic rings are disclosed which are useful in the treatment of panic disorder or anxiety disorder.
Type:
Grant
Filed:
June 17, 1991
Date of Patent:
January 5, 1993
Assignee:
Merck & Co., Inc.
Inventors:
Roger M. Freidinger, Ben E. Evans, Mark G. Bock
Abstract: This invention is directed to diamino isothiazole -1-oxides and -1,1-dioxides and related compounds as well as pharmaceutical compositions and methods useful in the treatment of gastric secretion in mammals.
Type:
Grant
Filed:
November 12, 1991
Date of Patent:
December 15, 1992
Assignee:
Merck & Co., Inc.
Inventors:
Susan F. Britcher, William C. Lumma, Jr.
Abstract: Aromatic 2-benzazepines with fused 5- or 6-membered heterocyclic rings which are antagonists of cholecystokinins and/or gastrin, and are useful in the treatment or prevention of CCK-related and/or gastrin-related disorders of the gastrointestinal, central nervous and appetite regulatory systems; compositions comprising these compounds; and methods of treatment of mammals or of increasing food intake of animals employing these compounds.
Type:
Grant
Filed:
March 11, 1991
Date of Patent:
November 24, 1992
Assignee:
Merck & Co., Inc.
Inventors:
Roger M. Freidinger, Ben E. Evans, Mark G. Bock
Abstract: Disclosed herein are /.sup.35 S/-labelled compound of the formula (I):(C.sub.6 H.sub.5).sub.3 C.sup.35 SHand processes therefor. This Compound (I) is useful as an intermediate for the introduction of sulfur isotope into a variety of compounds. For example, it is useful in the introduction of sulfur isotope into important compounds such as 6-mercaptopurine, 5-[3-(2-(7-chloroquinolin-2-yl)ethenyl)phenyl]-8-dimethylcarbamyl-4,6-dith ioactanoic acid, a potent antagonist of leukotriene D.sub.4 ; thiophosphoric acid derivatives, photo-affinity reagents and the like.
Type:
Grant
Filed:
October 19, 1990
Date of Patent:
June 2, 1992
Assignee:
Merck Frosst Canada, Inc.
Inventors:
Haydn W. R. Williams, Robert N. Young, Robert J. Zamboni
Abstract: Compounds of the formula: ##STR1## which are potent inhibitors of human renin and are useful for treating various forms of renin-associated hypertension, hyperaldosteronism and congestive heart failure; compositions containing these renin-inhibitory compounds, optionally with other antihypertensive agents; and methods of treating hypertension, hyperaldosteronism or congestive heart failure or of establishing renin as a causative factor in these conditions which employ these novel compounds.
Type:
Grant
Filed:
September 9, 1991
Date of Patent:
May 19, 1992
Assignee:
Merck & Co., Inc.
Inventors:
Wallace T. Ashton, Christine L. Cantone, Richard L. Tolman
Abstract: Analogs of glutamic acid and related amino acids and pharmaceutically-acceptable salts thereof which antagonize the function of cholecystokinins and gastrin disease states in animals and compositions for and methods of preventing or treating disorders of the gastrointestinal, central nervous and appetite regulatory systems of mammals, especially of humans.
Abstract: Renin-inhibitory di-, tri-, and tetrapeptides of the formula I:A-B-E-G-T-Jin whichA is heterocyclic, substituted heterocyclic etc;B is --N(A.sup.1)CH[(CH.sub.2).sub.2 R.sup.3 ]CO--,E is absent or is --N(A.sup.2)CH[(CH.sub.2).sub.2 R.sup.4 ]CO--;G is ##STR1## and J is --Y--(CH.sub.2).sub.x [CH(R.sup.5)].sub.y --(CH.sub.2).sub.z --R.sup.10and pharmaceutically acceptable salts thereof are disclosed. These compounds inhibit renin and are useful for treating various forms of renin-associated hypertension, hyperaldosteronism and congestive heart failure; compositions containing these renin-inhibitory peptides, optionally with other antihypertensive agents; and methods of treating hypertension, hyperaldosteronism or congestive heart failure or of establishing renin as a causative factor in these problems which employ these novel peptides.
Abstract: Peptides of the formula: ##STR1## which comprise novel elements replacing the Phe(8)-His(9) sequence in renin-inhibitory peptides based on substrate analogy, which inhibit the substrate-cleaving action of renin and have improved bioavailability; compositions containing these renin-inhibitory peptides, optionally with other antihypertensive agents; and methods of treating hypertension or congestive heart failure or of establishing renin as a causative factor in these problems which employ the novel peptides.
Type:
Grant
Filed:
March 8, 1989
Date of Patent:
August 13, 1991
Assignee:
Merck & Co., Inc.
Inventors:
Arthur A. Patchett, William H. Parsons, William J. Greenlee, Prasun K. Chakravarty