Patents Examined by Deborah Hung
  • Patent number: 5286650
    Abstract: Starting from 5-alkylidene or 5-benzylidenetetramic acid, optically-active 4-amino-3-hydroxy-carboxylic acids are produced in the (rel-3R,4R) configuration, especially statine. The synthesis process includes the O-acylation of the tetramic acid to the corresponding 4-acyloxy-3-pyrrolin-2-one, a stereoselective hydrogenation to (rel-4R,5R)-4-acyloxy-5-alkyl or 5-benzylpyrrolidin-2-one and an enantioselective enzymatic hydrolysis of the (4R,5R)-enantiomer to the corresponding 4-hydroxypyrrolidin-2-one. The nonhydrolyzed enantiomer is separated and converted into the target compound with (3S,4S) configuration by hydrolytic cleavage of the lactam ring and the ester function and optionally introduction of an amino protective group. Analogously the (3R,4R)-enantiomer can be obtained from the 4-hydroxypyrrolidin-2-one from the enzymatic hydrolysis. The 4-amino-3-hydroxycarboxylic acids producible according to the invention are the structural elements of enzyme inhibitors.
    Type: Grant
    Filed: August 20, 1992
    Date of Patent: February 15, 1994
    Assignee: Lonza Ltd.
    Inventors: Markus Banziger, John McGarrity, Thomas Meul
  • Patent number: 5278067
    Abstract: The invention is directed to a biologically pure culture of the microorganism Phoma sp. IMI 332962 or a mutant thereof.
    Type: Grant
    Filed: January 8, 1992
    Date of Patent: January 11, 1994
    Assignee: Glaxo Group Limited
    Inventors: Michael J. Dawson, Allan Baxter, Robert M. Tait, Nigel S. Watson, David Noble, Alan Shuttleworth, Howard G. Wildman, Michael V. Hayes
  • Patent number: 5266468
    Abstract: .beta.-Hydroxy-.alpha.-amino acids are obtained via serine hydroxymethyltransferase catalyzed condensation of aldehydes with glycine. The predominant product with most aldehydes is the L-erythro diastereomer. For example, succinic semialdehyde methylester is condensed with glycine in the process to provide L-erythro .alpha.-amino hydroxy adipic acid mono methyl ester.
    Type: Grant
    Filed: July 22, 1992
    Date of Patent: November 30, 1993
    Assignee: University of Notre Dame du Lac
    Inventor: Marvin J. Miller
  • Patent number: 5264355
    Abstract: Described is a new enzyme, 31-O-desmethyl-FK-506 O-methyltransferase (FKMT) and its N-terminal amino acid sequence. This enzyme can specifically and preferentially methylate the C-31 hydroxy group in 31-O-desmethyl FK-506/FR-900506 and other 31-O-desmethyl analogs of FK-506/FR-900506 and related compounds such as 31-O-desmethyl immunomycin type molecules, also designated FK-520 and FR-900520 by Fujisawa. The enzyme can be isolated from a FK-506 producing microorganism Streptomyces sp. (Merck Culture Collection No. MA 6858) ATCC No. 55098. Employing the enzyme in its active form, supplemented with Mg.sup.+2 ion, in the presence of the methyl donor, S-adenosyl methionine (SAM), derivatives of 31-O-desmethyl FK-506, 31-O-desmethyl FK-520 and related 31-O-desmethyl compounds may be prepared.
    Type: Grant
    Filed: July 2, 1992
    Date of Patent: November 23, 1993
    Assignee: Merck & Co., Inc.
    Inventors: Ali Shafiee, Patricia M. Cameron, David A. Boulton, Louis Kaplan, Haideh Motamedi
  • Patent number: 5250435
    Abstract: Novel strains of Aspergillus terreus have been discovered which provide fermentation production of at least 5.2 g/L of 7-[1,2,6,7,8,8a(R)-hexahydro-2(S),6(R)-dimethyl-8(S)-hydroxy-1(S)-naphthyl ]-3(R),5(R)-dihydroxyheptanoic acid (triol acid, I), but with production of not more than 0.85 g/L of (triol acid)-related side products and specifically less than 0.10 mg/liter of lovastatin. The predominant fermentation product triol acid, may be converted in a straightforward manner to its lactone form, in which it is an inhibitor of HMG-CoA reductase and thus useful as an antihypercholesterolemic agent, and in which it may also serve as an intermediate for preparation of other HMG-CoA reductase inhibitors.
    Type: Grant
    Filed: June 4, 1991
    Date of Patent: October 5, 1993
    Assignee: Merck & Co., Inc.
    Inventors: William H. Cover, Rebecca L. Dabora, Anderson Hong, Christopher Reeves, Robert W. Stieber, Victor A. Vinci
  • Patent number: 5213815
    Abstract: A method of treating ascites in poultry comprising administering Eyebright herb and Brewer's yeast to poultry in need thereof. The Brewer's yeast and eyebright quantities ingested by the birds can be varied judiciously to suit the poultry breed, the severity of the environmental conditions and the severity of the diseased condition of the stricken birds.
    Type: Grant
    Filed: October 10, 1991
    Date of Patent: May 25, 1993
    Inventor: Gerard T. O'Brien