Abstract: Phenoxyphenylacetic acids and derivatives of general structural formula I ##STR1## have endothelin antagonist activity and are therefore useful in treating cardiovascular disorders, such as hypertension, congestive heart failure, postischemic renal failure, vasospasm, cerebral and cardiac ischemia, myocardial infarction, inflammatory diseases, Raynaud's disease, and endotoxic shock, and asthma.
Type:
Grant
Filed:
March 19, 1993
Date of Patent:
December 20, 1994
Assignee:
Merck & Co., Inc.
Inventors:
Daljit S. Dhanoa, Kenneth J. Fitch, Daniel F. Veber, Thomas F. Walsh, David L. Williams, Jr.
Abstract: The present invention is a procedure for preparing cooked foods which involve the use of a gellan gum batter to coat a food substrate to impart qualities which are typically associated with fried foods, including crispness and juiciness. The coated food is then fried and frozen. Food products resulting from the procedure of the present invention contain low levels of fat and yet have the desirable qualities of fried foods.
Type:
Grant
Filed:
January 15, 1993
Date of Patent:
December 13, 1994
Assignee:
Merck & Co., Inc.
Inventors:
William F. Chalupa, George R. Sanderson
Abstract: Carbapenems of the formula ##STR1## are useful antibacterial agents. Compositions containing such compounds and methods of use are also disclosed.
Abstract: A conjugate immunogen, having polysaccharide moieties derived from bacterial sources, provides a multivalent vaccine with a low protein to polysaccharide ratio. The vaccine reduces complications associated with injection of protein immunogens due to pyrogenic responses, such as swelling and pain, and is particularly suitable for administration to infants.
Abstract: The present invention is directed to water-soluble derivatives of antibiotic lipopeptides having the formula. ##STR1## wherein R is H or OH and R' is a phosphono, sulfo or acyl radical possessing a charged group at neutral pH.The derivatives are esters but having a charged group, have good solubility properties in aqueous medium, rendering them more useful as therapeutic agents.
Type:
Grant
Filed:
March 15, 1991
Date of Patent:
November 29, 1994
Assignee:
Merck & Co., Inc.
Inventors:
Milton L. Hammond, James M. Balkovec, David J. Mathre
Abstract: Sustained release tablet comprising a microbially produced alginate-type polysaccharide and an active ingredient to be delivered in controlled fashion.
Abstract: This invention relates to compounds of structural formula (I): ##STR1## which are squalene synthase inhibitors and thus useful as cholesterol lowering agents and antifungal agents. These compounds are also inhibitors of farnesyl protein transferase and farnesylation of the oncogene protein Ras and thus useful in treating cancer.
Type:
Grant
Filed:
March 19, 1993
Date of Patent:
November 29, 1994
Assignee:
Merck & Co., Inc.
Inventors:
Gregory D. Berger, James D. Bergstrom, Tesfaye Biftu, Robert L. Bugianesi, Robert M. Burk, Narindar N. Girotra, C. H. Kuo, William H. Parsons, Mitree M. Ponpipom, Lori L. Whiting
Abstract: A new antibiotic cyclic lipopeptide having the formula ##STR1## wherein R is H or OH and a method of producing is described. The agent has very high activity against human pathogens and is of very low mammalian toxicity.
Type:
Grant
Filed:
May 21, 1993
Date of Patent:
November 22, 1994
Assignee:
Merck & Co., Inc.
Inventors:
Robert E. Schwartz, Prakash S. Masurekar, David F. Sesin, Jerrold M. Liesch, Thomas C. Hallada, Otto D. Hensens
Abstract: A device for the controlled delivery of a beneficial agent as a gelatinous dispersion consisting of (i) a core which contains a beneficial agent, a polymer which forms gelatinous microscopic particles upon hydration and if desired an agent to modulate the hydration of the polymer; and (ii) an impermeable, insoluble coating which adheres to and surrounds the core and contains apertures which provide an area for the hydration and release of a dispersion comprising gelatinous microscopic particles.
Abstract: Incubation of ##STR1## with a preparation from mammalian organ yields as biotransformation products the 5-(1-hydroxy)ethyl pyridinone analog as well as the 5-(1-hydroxy)ethyl pyridyl and the 5-(2-hydroxy)ethyl pyridyl derivatives.
Type:
Grant
Filed:
February 24, 1992
Date of Patent:
November 15, 1994
Assignee:
Merck & Co., Inc.
Inventors:
Suresh K. Balani, Laura R. Kauffman, Anthony D. Theoharides
Abstract: This invention relates to compounds of structural formula (I) isolated from an aerobic fermentation of Trichoderma viride MF5628, ATCC 74084: ##STR1## which are squalene synthase inhibitors and thus useful as cholesterol lowering agents. These compounds are also potent antifungal agents. Additionally, they inhibit farnesyl protein transferase and farnesylation of the oncogene protein Ras and are thus useful in treating cancer. This invention also relates to a process for obtaining compounds of structural formula (I).
Type:
Grant
Filed:
February 9, 1993
Date of Patent:
November 15, 1994
Assignee:
Merck & Co., Inc.
Inventors:
Guy H. Harris, Deborah Zink, E. Tracy T. Jones, Yu L. Kong
Abstract: New substituted cephalosporin sulfones are found to be potent elastase inhibitors and thereby useful anti-inflammatory/antidegenerative agents.
Type:
Grant
Filed:
May 1, 1992
Date of Patent:
November 15, 1994
Assignee:
Merck & Co., Inc.
Inventors:
James B. Doherty, Raymond A. Firestone, Paul E. Finke, William K. Hagmann, Shrenik K. Shah, Kevan R. Thompson
Abstract: A flexible fluid dispensing bottle is provided which conveniently meters out its contents in several small controlled doses. The device is designed to specifically provide multiple extended outlets to facilitate access beneath the fur of an animal ("comb effect") and to better spread treatment. In addition, the device uses a combination of bottle geometry, and internal ribs and cores to control capacity as well as volume displaced during individual pump strokes of the squeeze bottle.
Abstract: An improved process for formation of a 5-oxime on avermectin derivatives comprises the treatment of the oxo compound with O-(trimethylsilyl)hydroxylamine in the presence of a Lewis acid.
Abstract: A liquid carrier fluid that is used as a carrier system to suspend and deliver water soluble polymers which act to adjust the rheological properties of the aqueous systems to which they are added.
Type:
Grant
Filed:
October 14, 1992
Date of Patent:
November 8, 1994
Assignee:
Merck & Co., Inc.
Inventors:
Bryan Skaggs, Mike O'Brien, James M. Seheult, John M. Swazey
Abstract: A 4"-oxoavermectin intermediate is reductively aminated using hexa- or heptamethyldisilazane and sodium borohydride to produce a 4"-amino (or methylamino)avermectin. The 4"- aminoavermectin is a useful intermediate in the preparation of N-acyl derivatives. The compounds are useful as agricultural and animal health insecticides and parasiticides.
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:
June 18, 1993
Date of Patent:
November 8, 1994
Assignee:
Merck & Co., Inc.
Inventors:
Neville J. Anthony, Ta-Jyh Lee, Robert L. Smith, Gerald E. Stokker