Abstract: A cyclohexapeptide base which is the nucleus of closely related antibiotics obtained by culturing Zalerion arboricola and its salts are described. They are useful intermediates for the preparation of new semisynthetic compounds having antimicrobial activity.
Type:
Grant
Filed:
March 12, 1990
Date of Patent:
May 10, 1994
Assignee:
Merck & Co., Inc.
Inventors:
Dennis M. Schmatz, Jan S. Tkacz, Robert E. Schwartz, Mervyn Turner
Abstract: O-Heteroaryl, O-alkylheteroaryl, O-alkenylheteroaryl and O-alkynylheteroarylrapamycin derivatives of the general structural Formula I: ##STR1## have been prepared from suitable precursors by alkylation and/or arylation at C-42 and/or C-31. These compounds are useful in a mammalian host for the treatment of autoimmune diseases and diseases of inflammation, infectious diseases, the prevention of rejection of foreign organ transplants and the treatment of solid tumors.
Type:
Grant
Filed:
March 5, 1993
Date of Patent:
May 10, 1994
Assignee:
Merck & Co., Inc.
Inventors:
William H. Parsons, Peter J. Sinclair, Frederick Wong, Matthew J. Wyvratt
Abstract: New Zaragozic acids have been isolated from a culture of MF5465. These compounds and their derivatives are active as squalene synthetase inhibitors and are useful in the treatment of hypercholesterolemia.
Type:
Grant
Filed:
September 2, 1992
Date of Patent:
May 10, 1994
Assignee:
Merck & Co., Inc.
Inventors:
Claude Dufresne, Prakash S. Masurekar, Leslie A. Ferrell, Deborah L. Zink, Margaret S. Sosa
Abstract: There are disclosed certain novel compounds identified as benzo-fused lactams which promote the release of growth hormone in humans and animals. This property can be utilized to promote the growth of food animals to render the production of edible meat products more efficient, and in humans, to increase the stature of those afflicted with a lack of a normal secretion of natural growth hormone. Growth promoting compositions containing such benzo-fused lactams as the active ingredient thereof are also disclosed.
Type:
Grant
Filed:
February 2, 1993
Date of Patent:
May 10, 1994
Assignee:
Merck & Co., Inc.
Inventors:
Michael H. Fisher, William R. Schoen, Matthew J. Wyvratt, Robert J. DeVita
Abstract: Method for the preparing biphenyltetrazole compounds which are angiotensin II receptor antagonists or which are useful intermediates to prepare angiotensin II receptor antagonists. An illustrative biphenyl tetrazole compound is 2-n-butyl-4-chloro-1-[(2'-(tetrazol-5-yl)-1,1'-biphenyl-4-yl)methyl]-1H-im idazole-5-methanol, potassium salt.
Type:
Grant
Filed:
July 10, 1992
Date of Patent:
May 10, 1994
Assignees:
E. I. Du Pont de Nemours and Company, Merck & Co., Inc.
Inventors:
Young S. Lo, Lucius T. Rossano, Robert D. Larsen, Anthony O. King
Abstract: Antifungal and antiparasital lipopeptide compounds stable in aqueous media are described. Stability in aqueous media render lipopeptides more useful for compositions for therapeutic applications.
Abstract: Imidazolidyl rapamycin derivatives of the general structural Formula I: ##STR1## have been prepared from suitable precursors by alkylation and/or arylation at C-42 and/or C-31. These compounds are useful in a mammalian host for the treatment of autoimmune diseases and diseases of inflammation, infectious diseases, the prevention of rejection of foreign organ transplants and the treatment of solid tumors.
Type:
Grant
Filed:
March 5, 1993
Date of Patent:
May 10, 1994
Assignee:
Merck & Co., Inc.
Inventors:
Mark Goulet, William H. Parsons, Matthew J. Wyvratt
Abstract: 4-Substituted-1,4-dihydropyridines are prepared by a cycloaddition reaction in which the cyclization is driven to completion, after thermal reaction, by addition of an acid. Felodipine, a vasodilator, is prepared by a cycloaddition reaction of ethyl 3-aminocrotonate with a suitably substituted dichlorobenzylidine under reaction conditions whereby the product crystallizes out of the reaction solution and may be directly isolated by filtration.
Abstract: A vaccine strain of varicella-zoster virus (VZV), tested in clinical trials, is capable of preventing chickenpox in children. This virus has been modified by the introduction into its genome of heterologous DNA which encodes an immunogenic polypeptide of another human pathogen. This heterologous polypeptide is expressed in cells infected by the recombinant virus. Such recombinant VZV is useful as a vaccine for chickenpox as well as for heterologous pathogens.
Type:
Grant
Filed:
February 27, 1992
Date of Patent:
May 10, 1994
Assignee:
Merck & Co., Inc.
Inventors:
Ronald W. Ellis, Elliott Kieff, Edward M. Scolnick, Robert S. Lowe
Abstract: Novel aminopyridones inhibit HIV reverse transcriptase, and are useful in the prevention or treatment of infection by HIV and the treatment of AIDS, either as compounds, pharmaceutically acceptable salts, pharmaceutical composition ingredients, whether or not in combination with other antivirals, anti-infectives, immunomodulators, antibiotics or vaccines. Methods of treating AIDS and methods of preventing or treating infection by HIV are also described.
Type:
Grant
Filed:
November 4, 1992
Date of Patent:
May 3, 1994
Assignee:
Merck & Co., Inc.
Inventors:
Jacob M. Hoffman, Jr., Walfred S. Saari, Clarence S. Rooney, John S. Wai
Abstract: Substituted quinazolinones and pyridopyrimidines of structural formula 1 ##STR1## are angiotensin II antagonists useful in the treatment of disorders related to the renin-angiotensin system (RAS) such as hypertension, congestive heart failure, ocular hypertension and certain CNS disorders.
Type:
Grant
Filed:
July 22, 1993
Date of Patent:
May 3, 1994
Assignees:
Merck & Co., Inc., E. I. Du Pont de Nemours and Co.
Abstract: Conformationally constrained tricyclic derivatives of the thienodiazocine and thienothiadiazocine classes of compounds and ring homologs thereof are topically effective carbonic anhydrase inhibitors useful in the treatment of ocular hypertension and glaucoma associated therewith.
Abstract: Thieno[2,3-b]thiopyran-2-sulfonamides and ring homologs with a hydrophilic substituted-alkyl group adjacent to the thiopyran sulfur are carbonic anhydrase inhibitors topically effective in lowering intraocular pressure.
Type:
Grant
Filed:
June 16, 1992
Date of Patent:
May 3, 1994
Assignee:
Merck & Co., Inc.
Inventors:
John J. Baldwin, Gerald S. Ponticello, Charles N. Habecker, Harold G. Selnick
Abstract: A new antibiotic cyclic lipopeptide having the formula ##STR1## wherein R is H SEQ ID NO:1 or OH SEQ ID NO:2 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:
December 19, 1990
Date of Patent:
April 26, 1994
Assignee:
Merck & Co., Inc.
Inventors:
Robert E. Schwartz, David F. Sesin, Prakash S. Masurekar, Jerrold M. Liesch, Thomas C. Hallada, Otto D. Hensens
Abstract: A gene of varicella-zoster virus (VZV) which encodes immunogenic outer surface viral proteins has been identified by DNA sequence analysis. Antibodies directed against peptides imputed from the DNA sequence can react with the glycoprotein, which itself is reactive with neutralizing antibodies. The amino-terminal sequence of the purified glycoprotein is identical to a portion of the amino acid sequence imputed from the DNA sequence. This glycoprotein is useful for the preparation of a vaccine against VZV.
Type:
Grant
Filed:
June 9, 1992
Date of Patent:
April 26, 1994
Assignee:
Merck & Co., Inc.
Inventors:
Paul M. Keller, Mark W. Riemen, Ronald W. Ellis, Andrew J. Davison, Robert S. Lowe
Abstract: Inhibition of renal cancer, melanoma, colon cancer, lung cancer and leukemia cells by administration of compounds from the bafilomycin and hygrolidin groups of compounds.
Abstract: An organism of the Sporormiella species produces a compound having the formula ##STR1## which is useful. The compound is useful as an antifungal agent.
Abstract: Compounds of Structural Formula (I) ##STR1## are produced by directed biosynthesis. These compounds are squalene synthetase inhibitors and thus useful as cholesterol lowering agents, antifungal agents and cancer treatment agents.
Type:
Grant
Filed:
October 6, 1992
Date of Patent:
April 12, 1994
Assignee:
Merck & Co., Inc.
Inventors:
Kevin M. Byrne, Shieh-Shung T. Chen, Louis Kaplan, John G. MacConnell, Brian R. Petuch, Raymond F. White, Byron H. Arison