Abstract: A method for the total chemical synthesis of flavipucine employs the condensation of 4-hydroxy-6-methyl-2-pyridone with isobutylglyoxal in alkali alkoxide. The resulting alkali salt is acylated in both the 1' and 4 positions. Treatment of the 1',4-diacyloxy derivative with excess alkaline peroxide yields flavipucine.
Type:
Grant
Filed:
May 19, 1977
Date of Patent:
June 13, 1978
Assignee:
Merck & Co., Inc.
Inventors:
Norman L. Wendler, Narindar N. Girotra, Zbigniew S. Zelawski, deceased
Abstract: 2-R-substituted-1,2,5-thiadiazole-3-ones have broad spectrum antibacterial and antifungal activity. They are especially useful in agriculture to protect plants against diseases such as leaf, stem, and fruit spotting, internal discoloration and decay of fruits and vegetables. These compounds are particularly active against diseases caused by the genera Pseudomonas, Xanthomonas, Erwinia, and Corynebacterium.
Abstract: Novel di-bicyclo[3.1.1] and [2.2.1]heptyl and dibicyclo[3.1.1] and [2.2.1]heptenyl ketones are useful as intermediates for preparing novel polyamines useful as antimicrobial agents, as well as algae inhibitors.
Abstract: Novel diphenyl and loweralkyl substituted diphenyl polyamines are useful antimicrobial agents, as well as algae inhibitors. They are especially useful because of their low toxicity, and as such are advantageously included as the active agent in surgical scrubs, antibacterial soaps, as preservatives in cosmetic preparations, and the like. They also can be used for topical treatment of dermatological conditions having a bacterial origin or implication such as Acne vulgaris.
Type:
Grant
Filed:
February 12, 1976
Date of Patent:
March 14, 1978
Assignee:
Merck & Co., Inc.
Inventors:
Richard A. Dybas, Nathaniel Grier, Bruce E. Witzel
Abstract: This invention relates to novel crystalline dipilocarpinium pamoate useful as an agent, for lowering elevated intraocular pressure in glaucomatous patients, as well as to a process for preparing said compound and novel intermediates thereof.
Abstract: An improved process for the removal of malodorous compounds, especially sulfur-containing compounds, for example H.sub.2 S and methyl mercaptan, from gas streams containing oxygen in which a bed of activated carbon treated with NaOH and moisture is used to remove said compounds. The treatment, which may also be combined with regeneration of the activated carbon, is effected, typically, by applying to the carbon one bed volume of dilute (4-6%) NaOH solution, draining and drying with 50- 100% R.H. air.
Type:
Grant
Filed:
December 20, 1976
Date of Patent:
February 7, 1978
Assignee:
Calgon Corporation
Inventors:
Rabindra Kumar Sinha, Norman J. Wagner, Ronald S. Joyce
Abstract: Novel 6-methoxy and 6-thioalkyl-6-acylamidopenicillanic acids and their non-toxic pharmaceutically-acceptable salts, esters and amides which are useful as antibiotics. The products are prepared by treating an ester of 6-substituted-6-aminopenicillanic acid with an acylating agent followed by removal of the ester group. Also disclosed are novel intermediates.
Abstract: Novel diphenyl and loweralkyl substituted diphenyl polyamines are useful antimicrobial agents, as well as algae inhibitors. They are especially useful because of their low toxicity, and as such are advantageously included as the active agent in surgical scrubs, antibacterial soaps, as preservatives in cosmetic preparations, and the like. They also can be used for topical treatment of dermatological conditions having a bacterial origin or implication such as Acne vulgaris.
Type:
Grant
Filed:
October 16, 1975
Date of Patent:
January 24, 1978
Assignee:
Merck & Co., Inc.
Inventors:
Richard A. Dybas, Nathaniel Grier, Bruce E. Witzel
Abstract: Novel dibicyclo [3.1.1] and [2.2.1] heptyl and dibicyclo [3.1.1] and [2.2.1] heptenyl polyamines are useful antimicrobial agents, as well as algae inhibitors. They are especially useful as hard surface disinfectants and as additives to oil well drilling muds, injection brines and industrial water where bacterial control is desired.
Type:
Grant
Filed:
February 17, 1977
Date of Patent:
December 27, 1977
Assignee:
Merck & Co., Inc.
Inventors:
Nathaniel Grier, Richard A. Dybas, Robert A. Strelitz
Abstract: Novel diphenyl and loweralkyl substituted diphenyl polyamines are useful antimicrobial agents, as well as algae inhibitors. They are especially useful because of their low toxicity, and as such are advantageously included as the active agent in surgical scrubs, antibacterial soaps, as preservatives in cosmetic preparations, and the like. They also can be used for topical treatment of dermatological conditions having a bacterial origin or implication such as Acne vulgaris.
Type:
Grant
Filed:
September 2, 1975
Date of Patent:
December 6, 1977
Assignee:
Merck & Co., Inc.
Inventors:
Richard A. Dybas, Nathaniel Grier, Bruce E. Witzel
Abstract: A composition comprising tris-(hydroxymethyl)aminomethane and dicyclohexyl-, dicyclohexenyl- and cyclohexylcyclohexenyl-alkyl polyamines, their acid addition salts, and mixtures thereof are useful as antibacterial agents. The composition is particularly useful because of the synergistic improvement obtained against strains of the genus Pseudomonas, as well as other genera.
Type:
Grant
Filed:
May 14, 1976
Date of Patent:
November 29, 1977
Assignee:
Merck & Co., Inc.
Inventors:
David P. Jacobus, Eugene L. Dulaney, Nathaniel Grier
Abstract: A composition comprising tris-(hydroxymethyl)aminomethane and dibicyclo [3.1.1] and [2.2.1] heptyl and dibicyclo [3.1.1] and [2.2.1] heptenyl polyamines, their acid addition salts, and mixtures thereof are useful as antimicrobial agents. The composition is particularly useful because of the synergistic improvement obtained against strains of the genus Pseudomonas, as well as other genera.
Type:
Grant
Filed:
May 14, 1976
Date of Patent:
November 15, 1977
Assignee:
Merck & Co., Inc.
Inventors:
David P. Jacobus, Eugene L. Dulaney, Nathaniel Grier
Abstract: A composition comprising tris-(hydroxymethyl)aminomethane and diphenyl and loweralkyl substituted diphenyl polyamines, their acid addition salts, and mixtures thereof are useful as antibacterial agents. The composition is particularly useful because of the synergistic improvement obtained against strains of the genus Pseudomonas, as well as other genera.
Type:
Grant
Filed:
May 14, 1976
Date of Patent:
November 15, 1977
Assignee:
Merck & Co., Inc.
Inventors:
David P. Jacobus, Eugene L. Dulaney, Nathaniel Grier
Abstract: Total synthesis methods employ 7-amino (6-amino in the case of a penicillin derivative) group in the alpha configuration. The instant invention provides a general route for preparing the 7.beta.-amino (or 6.beta.-amino) compound, through the formation of an imino-containing intermediate, followed by hydrolysis to the desired epimer. Novel intermediate products are provided. The compounds having the desired beta epimer can be converted to acylamino-antibiotics.
Abstract: Novel dicyclohexyl, dicyclohexenyl and cyclohexylcyclohexenylalkyl polyamines are useful antimicrobial agents, as well as algae inhibitors. They are especially useful in agriculture to protect plants against diseases such as leaf, stem, and fruit spotting, internal discoloration and decay of fruits and vegetables. These compounds are particularly active against diseases caused by the genera Pseudomonas, Xanthomonas, Erwinia, and Corynebacterium.
Type:
Grant
Filed:
March 8, 1976
Date of Patent:
September 20, 1977
Assignee:
Merck & Co., Inc.
Inventors:
Bruce E. Witzel, Nathaniel Grier, Richard A. Dybas, Robert A. Strelitz
Abstract: An antimicrobial composition for secondary and tertiary oil recovery comprising a flooding composition consisting of displacement and driving fluids having incorporated therein an antimicrobially effective amount of a di-bicyclo[3.1.1] or [2.2.1] heptyl or di-bicyclo[3.1.1] and [2.2.1] heptenyl polyamines or salts thereof.
Type:
Grant
Filed:
May 18, 1976
Date of Patent:
September 20, 1977
Assignee:
Merck & Co., Inc.
Inventors:
Nathaniel Grier, Richard A. Dybas, Robert A. Strelitz
Abstract: Novel dibicyclo [3.1.1] and [2.2.1] heptyl and dibicyclo [3.1.1] and [2.2.1] heptenyl polyamines having a cyclohexylene group in the polyamine moiety are useful antimicrobial agents, as well as algae inhibitors. They are especially useful as hard surface disinfectants and as additives to oil well drilling muds, injection brines and industrial waters where microbial control is desired.
Type:
Grant
Filed:
March 26, 1976
Date of Patent:
July 12, 1977
Assignee:
Merck & Co., Inc.
Inventors:
Nathaniel Grier, Richard A. Dybas, Robert A. Strelitz
Abstract: Novel 6-methoxy and 6-thioalkyl-6-acylamido-penicillanic acids and their non-toxic pharmaceutically-acceptable salts, esters and amides which are useful as antibiotics. The products are prepared by treating an ester of 6-substituted-6-aminopenicillanic acid with an acylating agent followed by removal of the ester group. Also disclosed are novel intermediates.
Abstract: Novel dibicyclo [3.1.1] and [2.2.1] heptyl and dibicyclo [3.1.1] and [2.2.1] heptenylalkyl polyamines are useful antimicrobial agents, as well as algae inhibitors. They are especially useful as hard surface disinfectants and as additives to oil well drilling muds, injection brines and industrial water where bacterial control is desired.
Type:
Grant
Filed:
July 2, 1976
Date of Patent:
July 5, 1977
Assignee:
Merck & Co., Inc.
Inventors:
Nathaniel Grier, Richard A. Dybas, Robert A. Strelitz
Abstract: There is described 2-amino-5,7-disubstituted-naphthyridine and 5,7-disubstituted-naphthyridin-2(1H)-one derivatives with bronchodilating and hypotensive properties prepared by the reaction of 2,6-diaminopyridine with an appropriate .beta.-diketone providing the 2-amino products. The 2-oxo analogs are prepared from the 2-amino products by treatment with nitrous acid.
Type:
Grant
Filed:
December 9, 1975
Date of Patent:
June 21, 1977
Assignee:
Merck Sharp & Dohme (I.A.) Corporation
Inventors:
Hayden Windsor Richard Williams, Clarence Stanley Rooney