Abstract: Angiotensin I converting enzyme inhibitors A-58365 factors A, B, and C are produced by culturing Streptomyces chromofuscus NRRL 15098 under submerged aerobic fermentation conditions and are isolated and purified from the acidic filtered fermentation broth via chromatography, in particular HPLC. The factors are useful hypotensive agents.
Abstract: Trans-(.+-.) or trans-(-)-2,4-permissibly-substituted-6-alkyl or allyl octahydropyrimido[4,5-g]quinolines and related compounds, ultraviolet light absorbers.
Type:
Grant
Filed:
September 26, 1983
Date of Patent:
March 26, 1985
Assignee:
Eli Lilly and Company
Inventors:
Cynthia L. Nichols, Edmund C. Kornfeld, John M. Schaus
Abstract: A method for stabilizing and selecting host cells containing recombinant DNA which expresses a functional polypeptide and the novel organisms and cloning vectors for the practice thereof. The invention further provides a simple, convenient, and inexpensive method to lyse host cells for purification of intracellular products.
Type:
Grant
Filed:
June 18, 1981
Date of Patent:
March 19, 1985
Assignee:
Eli Lilly and Company
Inventors:
Charles L. Hershberger, Anna K. Radue, Paul R. Rosteck, Jr.
Abstract: Method of preparing compounds of formula 1: ##STR1## by oxidative deamination of a glycopeptide antibiotic of formula 2: ##STR2## the antibiotic being selected from A35512 factors A, B, C, E and H, A35512B pseudoaglycone, actaplanin factors A, B.sub.1, B.sub.2, B.sub.3, C.sub.1a, C.sub.2a, C.sub.3, D.sub.1, D.sub.2, E.sub.1, G, K, L, M, N and O, actaplanin pseudoaglycone, A41030 factors A, B, C, D, E, F and G, A47934, ristocetin A and ristocetin A pseudoaglycone, novel compounds and compositions and methods of increasing feed-utilization efficiency in animals are provided.
Abstract: The present invention discloses multifunctional recombinant DNA cloning vectors for use in Streptomyces, Bacillus, and E. coli. The invention further discloses transformants of the aforementioned vectors.
Type:
Grant
Filed:
February 1, 1982
Date of Patent:
March 5, 1985
Assignee:
Eli Lilly and Company
Inventors:
James R. Miller, Jeffrey T. Fayerman, Steven Kovacevic, Nancy E. Beerman
Abstract: 1-Oxa-beta-lactam antibiotics of the formula ##STR1## are broad spectrum antibiotics especially useful in the treatment of infections attributable to the gram-negative microorganisms such as Pseudomonas or are intermediates to such antibiotics.
Abstract: 7.beta.-[2-Amino-2-(benzothien-4,5,6, and 7-yl)acetylamino]-3-substituted-3-cepham-4-carboxylic acids and 7.beta.-[2-amino-2-(2,3-dihydrobenzothien-4,5,6, and 7 yl)acetylamino]-3H- or 3-substituted-3-cephem-4-carboxylic acids (1), e.g. 7.beta.-[2-amino-2-(benzothien-4-yl)acetylamino]-3-methyl-3-cephem-4-carbo xylic acid, are orally effective antibiotics. Also provided are benzothienyl oximino compounds, the corresponding 2,3-dihydro compounds (2) useful as intermediates to (1) and as antibiotics, as well as 7.beta.-(2,2-dialkyl-5-oxo-4-benzothienyl-1-imidazolidinyl)-3H-(3-substitu ted)-3-cephem-4-carboxylic acids and the corresponding 2,3-dihydro compounds (3) useful as antibiotics, and prepared with (1) by condensation with ketones. Pharmaceutical formulations of antibiotic compounds (1), (2), and (3) are provided.
Abstract: The present invention is directed to the inhibition of nitrosamines in dinitroaniline herbicides by the incorporation of an addition compound of an alkali metal or ammonium bisulfite with an aldehyde or ketone.
Abstract: Cephalosporin compounds substituted in the 7-position by a 2-(5- or 6-membered heterocyclic)-2-oximinoacetylamino group and in the 3-position with a thienopyridinium methyl group or a furopyridinium methyl group are broad spectrum antibiotics highly effective in combating bacterial infections of gram-negative and gram-positive microorganisms. The cephalosporins are best prepared by reacting a silylated 7-[2-(heterocyclic)-2-oximinoacetylamino-3-iodomethyl-3-cephem-4-carboxyli c acid with the thienopyridine or the furopyridine. Pharmaceutical formulations comprising a compound of the invention and a method for treating bacterial infections comprising their use are also provided.
Abstract: Trans-(.+-.)-2-Amino or substituted amino-4-permissibly-substituted 6-lower alkyl or allyl-5,5a,-6,7,8,9,9a,10-octahydropyrimido[4,5-g]quinolines, the corresponding trans-(-)-stereoisomers and salts thereof, useful in treating anxiety, Parkinson's Syndrome, sexual dysfunction, depression, hypertension and elevated prolactin levels, and intermediates useful for the synthesis thereof.
Abstract: A process is described for preparing 2-acetylthiomethyl-5-quanidinopentanoic acid by treating 2-acetylthiomethyl-5-aminopentanoic acid with 1-quanyl-3,5-dimethylpyrazole in a medium comprising a hydroxylated solvent.
Type:
Grant
Filed:
November 12, 1982
Date of Patent:
February 26, 1985
Assignee:
Eli Lilly and Company
Inventors:
Russell L. Barton, Stephen L. Briggs, Gary A. Koppel
Abstract: A stereo-selective preparation of novel sulfonated o-phenylenediamines carrying a trans-.alpha.-alkylidenebenzyl group at the 5-position, which are intermediates in the synthesis of antiviral benzimidazoles.
Abstract: 1-Heterocyclic-2-pyrrolidinone analogs, and intermediates thereof, as aquatic and terrestrial herbicides and aquatic algicides. The compounds and intermediates can also be used together with one or more herbicides to provide useful terrestrial herbicidal combinations.
Abstract: This invention provides for certain novel 2,4,5-triaryl pyrimidine derivatives, their pharmaceutical formulations, and a method of treating pain, fever, thrombosis, inflammation, and arthritis.
Abstract: 4-Fluoroazetidinone antibacterial agents are provided by a process comprising the reaction of an azetidinone-4-sulfinic acid, or a salt thereof, with perchloryl fluoride (FClO.sub.3) at -80.degree. C. to -25.degree. C., e.g., p-nitrobenzyl 3-methyl-2-(2-oxo-4-sulfino-3-phenoxyacetamido-1-azetidinyl-3-butenoate is reacted with FClO.sub.3 to provide corresponding 4-fluoroazetidinone. The latter is isomerized with a tertiary amine to corresponding 2-butenoate which a carboxy group deprotection provides an antibacterial compound.
Type:
Grant
Filed:
December 27, 1982
Date of Patent:
February 19, 1985
Assignee:
Eli Lilly and Company
Inventors:
Wayne A. Spitzer, Theodore Goodson, Jr.
Abstract: N-Acyl-glycopeptide antibiotics having the formula ##STR1## and their salts are useful new antibiotics. The N-acyl actaplanin derivatives also increase feed-utilization efficiency and promote growth in animals and improve milk production in lactating ruminants.