Patents Represented by Attorney Edmunde D. Riedl
  • Patent number: 4031085
    Abstract: This invention relates to the preparation of 3-hydroxymethyl-7.beta.-aminoadipoyl-7.alpha.-methoxy-3-cephem-4-carboxyli c acid from 3-(.alpha.-methoxy-p-sulfo-oxycinnamoyloxymethyl)-7.beta.-aminoadipoyl-7.a lpha.-methoxy-3-cephem-4-carboxylic acid or 3-(.alpha.-methoxy-p-hydroxycinnamoyloxymethyl)-7.beta.-aminoadipoyl-7.alp ha.-methoxy-3-cephem-4-carboxylic acid by treatment at 60.degree. C. and pH 3.5-6.5 for about 1 hour. The starting compounds are isolated as fermentation products produced by various Streptomyces species.
    Type: Grant
    Filed: February 17, 1976
    Date of Patent: June 21, 1977
    Assignee: Merck & Co., Inc.
    Inventors: Seemon H. Pines, Matthew A. Kozlowski
  • Patent number: 4011236
    Abstract: This invention relates to compositions containing N-(benzimidazol-2-yl)arylcarboxamides as ultraviolet (UV) light absorbers. The compounds are useful to protect UV sensitive materials, particularly plastic compositions, or ingredients thereof such as dyes, anti-microbial agents, or plasticizers from attack by ultraviolet light. The compositions are suitable for those uses where UV protection is required only for short periods of time, for example in sun tan lotions, as well as for uses which require protection for extended periods of time.
    Type: Grant
    Filed: May 27, 1975
    Date of Patent: March 8, 1977
    Assignee: Merck & Co., Inc.
    Inventor: Nathaniel Grier
  • Patent number: 4010176
    Abstract: Novel substituted nitroimidazoles are provided, for example, 2-(4,5-substituted-isoxazol-3-yl)-1-substituted-5-nitroimidazole; 2-(4,5-disubstituted-.DELTA..sup.2 -isoxazolin-3-yl)-1-substituted-5-nitroimidazole; or 2-(4,5-disubstituted-2-loweralkyl-isoxazolidin-3-yl)-1-substituted-5-nitro imidazole. These compounds have antibacterial and antiprotozoal activity, especially against human and animal trypanosomiasis and trichomoniasis.
    Type: Grant
    Filed: July 30, 1975
    Date of Patent: March 1, 1977
    Assignee: Merck & Co., Inc.
    Inventors: Peter Kulsa, Clarence S. Rooney
  • Patent number: 4003934
    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.
    Type: Grant
    Filed: September 2, 1975
    Date of Patent: January 18, 1977
    Assignee: Merck & Co., Inc.
    Inventors: Nathaniel Grier, Richard A. Dybas
  • Patent number: 3995039
    Abstract: Novel pyrazolo [1,5-a] [1,3,5] triazines are provided which are active agents to inhibit bronchial constriction with very low chronotropic effects. The novel compounds are prepared by the reaction of an appropiately substituted 1-amidino-5-amino pyrazole with an appropriately substituted trialkyl orthoester. Suitable compositions for utilizing this bronchodilating activity by administration to humans are also disclosed.
    Type: Grant
    Filed: May 27, 1975
    Date of Patent: November 30, 1976
    Assignee: Merck & Co., Inc.
    Inventors: Clarence Stanley Rooney, Haydn Windsor Richard Williams
  • Patent number: 3993656
    Abstract: There is described 1,8-naphthyridin-2(1H)-one compounds with bronchodilating and hypotensive properties prepared by reaction of 2,6-diaminopyridine with an appropriate .beta.-diketone providing a 2-aminonaphthyridine compound which upon treatment with nitrous acid is converted to the 2-oxo product. Alternatively, an appropriate .beta.-diketone can be reacted with an alkyl alkoxycarbonylacetimidate, the alkyl 2-aminonicotinate thus formed converted to the hydrazide, which upon treatment with a sulfonyl halide forms the N-sulfonyl hydrazide derivative. This intermediate is reacted with an alkali metal carbonate to provide the 2-aminonicotinaldehyde which upon reaction with an ester of a substituted aliphatic carboxylic acid provides the desired product. In some cases the aminonicotinaldehyde is generated in situ in the presence of the ester thereby giving the desired product in one step from the N-sulfonyl hydrazide derivative.
    Type: Grant
    Filed: February 20, 1975
    Date of Patent: November 23, 1976
    Assignee: Merck & Co., Inc.
    Inventors: Clarence Stanley Rooney, Haydn Windsor Richard Williams, Burton Kendall Wasson
  • Patent number: 3962262
    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: June 7, 1974
    Date of Patent: June 8, 1976
    Assignee: Merck & Co., Inc.
    Inventors: Haydn Windsor Richard Williams, Clarence Stanley Rooney
  • Patent number: 3944560
    Abstract: 3-Hydroxy-3-(substituted-aminoalkyl-3,4-dihydro-2H-1,5-benzodioxepin products are described that exhibit .sym.-advenergic stimulating properties and are therefore suitable for use as bronchodilating agents. The products are prepared essentially by four principal routes from 3-oxo-3,4-dihydro-2H-1,5-benzodioxepins. By one route the 3-oxobenzodioxepin is treated with a nitroalkane to give a 3-hydroxy-3-nitroalkyl-benzodioxepin the nitro group of which is reduced to an amine and the resulting compound reacted with an aldehyde or ketone under hydrogenating conditions to introduce the desired substituent into the amino function.
    Type: Grant
    Filed: November 21, 1973
    Date of Patent: March 16, 1976
    Assignee: Merck & Co., Inc.
    Inventors: Burton K. Wasson, Haydn W. R. Williams