Abstract: 3-Fluoro-D-alanine, its pharmacologically acceptable esters, and pharmacologically acceptable salts of the foregoing, as well as other pharmacologically acceptable derivatives of 3-fluoro-D-alanine which, when administered clinically, are effective in releasing 3-fluoro-D-alanine in vivo, are potent antibacterial agents, and are prepared by fluorination of D-alanine with fluoroxyperfluoroalkanes or fluoroxypentasulfur in the presence of a free radical initiator followed by esterification and/or treatment with acids or bases.
Abstract: 3-Fluoro-L-alanine is transformed by asymmetric conversion, via an intermediate L-2-(halo)-3-fluoropropionic acid, to 3-fluoro-D-alanine. The 3-fluoro-D-alanine thus obtained is a potent antibacterial agent.
Abstract: The antibiotic thienamycin is active against both gram-positive and gram-negative bacteria. The antibiotic is produced by growing a newly-found and hitherto undescribed species of Streptomyces on suitable fermentation media.
Type:
Grant
Filed:
November 25, 1974
Date of Patent:
April 13, 1976
Assignee:
Merck & Co., Inc.
Inventors:
Jean S. Kahan, Frederick M. Kahan, Edward O. Stapley, Robert T. Goegelman, Sebastian Hernandez
Abstract: Novel cephalosporin compounds having a 3'-.alpha.-methyl, a 3-aryl or 3-heterocycle substituent are prepared by total synthesis. The novel cephalosporin compounds are active against gram-negative and gram-positive microorganisms.
Type:
Grant
Filed:
August 27, 1973
Date of Patent:
March 30, 1976
Assignee:
Merck & Co., Inc.
Inventors:
Burton G. Christensen, Ronald W. Ratcliffe
Abstract: Novel amorphous magnesia-silica complexes containing from about 0.001 to 2.0 percent by weight of an alkali metal oxide, wherein the mole ratio of MgO:SiO.sub.2 of said complexes is from about 1:25 to 14:1.
Type:
Grant
Filed:
April 21, 1975
Date of Patent:
March 2, 1976
Assignee:
Merck & Co., Inc.
Inventors:
Leonard S. Lee, Yoshio Uyeda, Samuel W. Sopp
Abstract: Novel amorphous magnesia-silica complexes containing from about 0.001 to 2.0 percent by weight of an alkali metal oxide, wherein the mole ratio of MgO:SiO.sub.2 of said complexes is from about 1:25 to 14:1.
Type:
Grant
Filed:
October 7, 1974
Date of Patent:
January 13, 1976
Assignee:
Merck & Co., Inc.
Inventors:
Leonard S. Lee, Yoshio Uyeda, Samuel W. Sopp
Abstract: New ampicillin derivatives, probenecidoxymethyl and 1-ethyl esters of ampicillin and their pharmaceutically acceptable salts, useful as antibiotics. A method for preparing these antibiotics by condensing probenecidoxymethyl or 1-ethyl halide with an acid salt of 6[D(-)-.alpha.-azidophenylacetamido] penicillanic acid, hydrogenating the azido group and isolating the product as a pharmaceutically acceptable salt of an acid. Pharmaceutical preparations containing the new antibiotics.
Type:
Grant
Filed:
July 30, 1974
Date of Patent:
January 6, 1976
Assignee:
Merck & Co., Inc.
Inventors:
Burton G. Christensen, William J. Leanza