Abstract: Renin inhibitory peptides of the formula ##STR1## and analogs thereof inhibit renin and are useful for treating various forms of renin-associated hypertension and hyperaldosteronism.
Type:
Grant
Filed:
April 4, 1984
Date of Patent:
May 5, 1987
Assignee:
Merck & Co., Inc.
Inventors:
Mark G. Bock, Joshua S. Boger, Stephen F. Brady, Daniel F. Veber
Abstract: Renin inhibitory peptides of the formula ##STR1## and analogs thereof inhibit renin and are useful for treating various forms of renin-associated hypertension and hyperaldosteronism.
Abstract: The (5-R-2-oxo-1,3-dioxolen-4-yl)methyl moiety: ##STR1## wherein R is loweralkyl of 1-6 carbon atoms, especially methyl or t-butyl; when utilized as an ester on a pharmaceutical having a carboxylic acid functionality, enhances oral absorption of the pharmaceutical. This effect is applicable to a broad range of pharmaceutically active substances, including antibiotics, and antihypertensives as well as other classes of therapeutic agents.
Abstract: A container for storing and dispensing small objects, such as capsules or pills containing medicament, one at a time, consists of a receptacle containing, within itself, a delivery mechanism including a funnel-shaped exit port for capsules and a capsule or pill delivery tube at the end of said funnel-shaped exit designed to accommodate no more than one pill or capsule. This funnel divides the outer receptacle into an upper storage compartment and a lower delivery compartment. The receptacle also contains between the exit end of the receptacle and the delivery tube a resilient gate member positioned to prevent or allow escape of a capsule or pill from the delivery tube. The inner end of the receptacle is pressed into or twisted in the user's hand which moves the resiliently mounted gate members, thus opening the delivery tube and delivering a single small object to the user.
Type:
Grant
Filed:
June 27, 1985
Date of Patent:
March 31, 1987
Assignee:
Merck & Co., Inc.
Inventors:
Kenneth J. Gibilisco, Stephen Degnen, Richard Borders
Abstract: Renin inhibitory peptides of the formula ##STR1## and analogs thereof inhibit renin and are useful for treating various forms of renin-associated hypertension and hyperaldosteronism.
Type:
Grant
Filed:
March 27, 1984
Date of Patent:
January 13, 1987
Assignee:
Merck & Co., Inc.
Inventors:
Mark G. Bock, Robert M. DiPardo, Joshua S. Boger, Ben E. Evans, Roger Freidinger
Abstract: The present invention provides an improved process for producing 3-acylamino benzodiazepines of the formula: ##STR1## wherein: R is loweralkyl of from 1-6 carbon atoms, aryl such as phenyl and halophenyl, aralkyl, alkyloxy, aralkyloxy, indolyl or substituted indolyl;R' is hydrogen, loweralkyl of from 1-6 carbon atoms, carboxymethyl or carbalkoxymethyl wherein the alkoxy groups contain from 1-4 carbon atoms;X is hydrogen or halogen;Y is hydrogen or halogen.These compounds are useful because of their activity as cholecystokinin (CCK) inhibitors.
Type:
Grant
Filed:
January 2, 1986
Date of Patent:
December 9, 1986
Assignee:
Merck & Co., Inc.
Inventors:
Mark G. Bock, Daniel F. Veber, Robert M. DiPardo
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 and cytoprotective agents.
Abstract: Purines and pyrimidines having a fused cyclopropane ring in the side chain and the heterocyclic isosteres of said purines and pyrimidines have antiviral activity, especially against viruses of the herpes class.
Type:
Grant
Filed:
April 10, 1984
Date of Patent:
October 14, 1986
Assignee:
Merck & Co., Inc.
Inventors:
Wallace Ashton, Edward Walton, Richard L. Tolman
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.
Abstract: Disclosed are compounds of the formula: ##STR1## and the pharmaceutically acceptable salts thereof wherein R.sup.1 and R.sup.2 are independently alkyl, haloalkyl, alkenyl, haloalkenyl, alkynyl or haloalkynyl, each having 1 to 19 carbon atoms, or R.sup.2 is hydrogen; R.sup.3 is hydrogen, alkyl having 1 to 6 carbon atoms or hydroxyalkyl having 1 to 6 carbon atoms; R.sup.4 is hydrogen, halogen, amino or alkyl having 1 to 4 carbon atoms; R.sup.5, R.sup.6 and R.sup.7 are independently selected from hydrogen, hydroxy, alkyl having 1 to 6 carbon atoms, acyloxy having 1 to 8 carbon atoms, alkoxy having 1 to 6 carbon atoms, hydroxyalkyl having 1 to 6 carbon atoms, acyloxyalkyl having 1 to 12 carbon atoms, amino, alkylamino of 1 to 6 carbon atoms and --PO.sub.3.sup.=, or two of R.sup.5, R.sup.6 and R.sup.7 taken together form a group --OPO.sub.2 O.sup.- --, --CH.sub.2 OPO.sub.2 O.sup.- --, --CH.sub.2 OPO.sub.2 OPO.sub.2 O.sup.= --, or --OPO.sub.2 OPO.sub.2 O.sup.= --; A is O, S or CH.sub.
Type:
Grant
Filed:
April 6, 1984
Date of Patent:
April 1, 1986
Assignee:
Merck & Co., Inc.
Inventors:
Malcolm MacCoss, Richard L. Tolman, Robert A. Strelitz
Abstract: Novel quinazolino-1,4-benzodiazepin-5,13-diones, which have been found to be antagonists of the function of cholecystokinins (CCK), to the preparation of these compounds from compounds prepared by aerobic fermentation of certain Aspergillus alliaceus strains, and to the use of these compounds to antagonize the function of CCK, which antagonism is useful, e.g., for the treatment and prevention of disorders of the gastrointestinal, central nervous and appetite-regulatory systems of mammals, especially of humans.
Type:
Grant
Filed:
January 25, 1985
Date of Patent:
January 7, 1986
Assignee:
Merck & Co., Inc.
Inventors:
Mark G. Bock, Roger M. Freidinger, Ben E. Evans, George D. Hartman
Abstract: Novel indol-3-yl-quinazolino-1,4-benzodiazepin-5,13-diones, which are antagonists of the function of cholecystokinins (CCK), to the preparation of these compounds from compounds prepared by aerobic fermentation of certain Aspergillus alliaceus strains, and to the use of these compounds to antagonize the function of CCK, which antagonism is useful, e.g., for the treatment and prevention of disorders of the gastrointestinal, central nervous and appetite-regulatory systems of mammals, especially of humans.
Type:
Grant
Filed:
January 25, 1985
Date of Patent:
December 17, 1985
Assignee:
Merck & Co., Inc.
Inventors:
Mark G. Bock, Roger M. Freidinger, Ben E. Evans
Abstract: Novel quinazolino-1,4-benzodiazepin-5,13-dione derivatives, which are soluble in aqueous media and which have been found to be antagonists of the function of cholecystokinins (CCK), to the preparation of these compounds from compounds prepared by aerobic fermentation of certain Aspergillus alliaceus strains, and to the use of these compounds to antagonize the function of CCK, which antagonism is useful, e.g., for the treatment and prevention of disorders of the gastrointestinal, central nervous and appetite-regulatory systems of mammals, especially of humans.
Type:
Grant
Filed:
January 25, 1985
Date of Patent:
December 17, 1985
Assignee:
Merck & Co., Inc.
Inventors:
Mark G. Bock, Roger M. Freidinger, Ben E. Evans
Abstract: A herpes simplex type I subunit vaccine is prepared from infected chick embryo cells by ultra extraction of the virus while the infected cells are still attached to the growth surface.
Type:
Grant
Filed:
July 23, 1981
Date of Patent:
September 10, 1985
Assignee:
Merck & Co., Inc.
Inventors:
Alexander U. Bertland, George P. Lampson
Abstract: Chiral N-protected, N-substituted .alpha.-amino acids are described. These compounds are prepared by condensation of an N-protected .alpha.-amino acid with an aldehyde followed by the selective reductive cleavage of an oxazolidinone intermediate.
Abstract: Novel dibenzo[b,f]thiepin-3-carboxaldehydes and derivatives are prepared and employed in the treatment and control of allergic conditions such as allergic asthma.
Abstract: ADP-Ribosylating toxins are rendered enzymatically inactive by reactions with photolabile affinity reagents. The toxoids retain the antigenic and immunogenic properties of the original toxins. These bacterial toxoids can be used as immunogens to protect against the specific disease that the precursor toxins cause or, in the case of P. aeruginosa, the toxoid can be used in combination with E. coli J-5 vaccine to protect against gram-negative bacteremia in general.
Type:
Grant
Filed:
October 26, 1983
Date of Patent:
December 18, 1984
Assignee:
Merck & Co., Inc.
Inventors:
Richard L. Tolman, Stephen Marburg, Lynn T. Callahan, III
Abstract: Haemophilus influenzae type B polysaccharide is coupled through a spacer to a serotype outer membrane protein from Neisseria meningitidis. This conjugate has enhanced antigenicity and immunogenicity relative to the unconjugated polysaccharide.
Type:
Grant
Filed:
January 31, 1983
Date of Patent:
July 10, 1984
Assignee:
Merck & Co., Inc.
Inventors:
Maurice R. Hilleman, Joseph Y. Tai, Richard L. Tolman, Philip P. Vella