Abstract: Disclosed are antibiotic 6-(substituted methyl) penicillins, derivatives and nuclear analogues thereof; wherein the methyl substituent is, inter alia, hydroxyl, ketonic oxygen, imino nitrogen, amino or thio. Also disclosed are processes for the preparation of such compounds and their pharmaceutically acceptable salt, ester and amide derivatives; pharmaceutical compositions comprising such compounds; and methods of treatment comprising administering such compounds and compositions when an antibiotic effect is indicated.
Type:
Grant
Filed:
May 1, 1978
Date of Patent:
June 10, 1980
Assignee:
Merck & Co., Inc.
Inventors:
Thomas R. Beattie, Frank P. Dininno, Burton G. Christensen
Abstract: Disclosed are 6- and 1-substituted-1-carbadethiapen-2-em-3-carboxylic acids of the following structure: ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 are, inter alia, independently selected from the group consisting of hydrogen, alkyl, aryl, and aralkyl. Such compounds as well as their pharmaceutically acceptable salt, ester and amide derivatives are useful as antibiotics. Also disclosed are processes for the preparation of such compounds, pharmaceutical compositions comprising such compounds and methods of treatment comprising administering such compounds and compositions when an antibiotics effect is indicated.
Abstract: Hepatitis B e antigen or hepatitis B e antibody are separated from human biological fluid by centrifugation in a density gradient and isolated in the 1.04-1.15 g/cc density region.
Abstract: A process is disclosed for preparing antibiotic 6- and 2-substituted-1-carbadethiapen-2-em-3-carboxylic acids and their pharmaceutically acceptable salts and esters (I) ##STR1## wherein: R.sup.1 and R.sup.2 are selected from hydrogen, alkyl aryl, and aralkyl; and R.sup.3 is hydrogen, --R, --OR, or --SR, wherein R is hydrogen, alkyl, aryl or aralkyl. The process comprises complexing an appropriately substituted .delta.,.omega.-unsaturated amino acid with a transition metal carbonyl complex, followed by oxidatively induced ligand transfer and ring closure: ##STR2## wherein: F.sub.p =.eta..sup.5 --C.sub.5 H.sub.5 Fe(CO).sub.2 and F.sub.p (isobutene.sup..sym. represents a cationic complex between F.sub.p and an olefin such as isobutene, which complex cation is employed in the initial ligand exchange reaction; R.sup.4 is lower alkyl or phenyl; R.sup.5 is a readily removable blocking group or pharmaceutically acceptable ester radical; and R.sup.1, R.sup.2 and R.sup.3 are as defined above.
Abstract: The antibiotic A43F is active against a variety of plant pathogenic fungi. The antibiotic A43F is produced by growing an as yet unclassified species of fungus (ATCC No. 20529) on suitable fermentation media and isolating the bioactive component therefrom.
Type:
Grant
Filed:
March 12, 1979
Date of Patent:
May 6, 1980
Assignee:
Merck & Co., Inc.
Inventors:
Janet C. Onishi, Gerald L. Rowin, John E. Miller, Jr.
Abstract: The outer membrane of influenza virus is attached to a liposome by two different techniques. In addition, one of the techniques allows the entrapment of intact virus, usually one virus per liposome. The techniques can be performed with either influenza virus A or B.
Abstract: Subunit viral or bacterial antigens are incorporated into liposomes containing a positively charged amino-containing surfactant. The resulting complex is antigenically more active than the free antigen.
Abstract: Fermentation broths or impure solutions containing thienamycin, a substance having antibiotic activity against gram-negative and gram-positive microorganisms, are purified using a sequence of ion exchange resins, starting with an anion exchange resin of the polystyrene-trimethylammonium type in the HCO.sub.3 -cycle, and ending with absorption on and elution from a polymeric cross-linked polystyrene-type resin adsorbent. Variations in the intermediate steps, e.g. different resins and eluates are possible and are illustrated within.
Abstract: The invention provides an improved process for the growth of lymphoblastoid cells in a medium supplemented with human albumin. The invention further provides for the production of interferon by viral infection of these lymphoblastoid cells in a medium also supplemented with human albumin. This invention eliminates the necessity for adding animal proteins.
Type:
Grant
Filed:
March 30, 1979
Date of Patent:
April 15, 1980
Assignee:
Merck & Co., Inc.
Inventors:
Alfred A. Tytell, Edgar Scattergood, Arthur K. Field
Abstract: Disclosed are 6-(.alpha.-hydroxyethyl)-7-oxo-1-azabicyclo[3.2.0]hept-2-ene-2-carboxylic acid and its 2,3-dihydro analogue, 6-(.alpha.-hydroxyethyl)-7-oxo-1-azabicyclo[3.2.0]heptane-2-carboxylic acid. Such compounds and their pharmaceutically acceptable salt, ester, ether and aide derivatives (derivatives involving both the secondary alcohol and the carboxyl group) are useful as antibiotics. Also disclosed are processes for the preparation of such compounds, pharmaceutical compositions comprising such compounds and methods of treatment comprising administering such compounds and compositions when an antibiotic effect is indicated.
Abstract: Cephamycin C is concentrated and purified by subjecting a fermentation broth which contains Cephamycin C to the following sequence of steps: filtration at acidic pH, passage through a methylene sulfonic acid cation ion exchange resin, washing with an aqueous stream having a low concentration of Cephamycin C, and elution using the above aqueous stream from the previous step, recirculated and maintained at an elevated pH.
Abstract: Disclosed are substituted N-methylene derivatives of thienamycin which may be represented by the following structural formula: ##STR1## wherein X and Y are selected from the group consisting of hydrogen, R, OR, SR, and NR.sup.1 R.sup.2 wherein, inter alia, R is substituted or unsubstituted: alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl, aryl, aralkyl, heteroaryl, heteroaralkyl, heterocyclyl, and heterocyclylalkyl; R.sup.1 and R.sup.2 are hydrogen or R. Such compounds and their pharmaceutically acceptable salt, ether, ester and amide derivatives are useful as antibiotics. Also disclosed are processes for the preparation of such compounds; pharmaceutical compositions comprising such compounds; and methods of treatment comprising administering such compounds and compositions when an antibiotic effect is indicated.
Type:
Grant
Filed:
November 17, 1977
Date of Patent:
March 18, 1980
Assignee:
Merck & Co., Inc.
Inventors:
Burton G. Christensen, William J. Leanza, Kenneth J. Wildonger
Abstract: Uniform starch particles prepared from one or more starches selected from tapioca, corn, waxy maize, potato, sago, arrowroot and cereal; and one or more gelling hydrocolloids selected from sodium alginate, sodium pectate, hydroxypropylcellulose, methylcellulose, methylhydroxypropylcellulose, methylethylcellulose, carrageenan, furcellaran, agar, gelatin, a mixture of xanthan gum and locust bean gum, and curdlan; by adding water, extruding, cutting and drying; useful in preparing retorted or aseptically packaged, tapioca-style pudding and other improved, edible texturized starch products.
Abstract: Disclosed are N-derivatives of thienamycin having structures I and II. ##STR1## wherein: the bifunctional radical may contain additional unsaturation in the ring; and wherein n is an integer selected from 1-6; p is 0, 1 or 2; R.sup.1 is selected from hydrogen, alkyl having 1-6 carbon atoms, and aryl having 6-10 carbon atoms; and Z is imino (.dbd.NH), oxo (.dbd.O), hydrogen, amino, or alkyl having 1-6 carbon atoms. Such compounds and their pharmaceutically acceptable salt and ester derivatives are useful as antibiotics. Also disclosed are processes for the preparation of such compounds pharmaceutical compositions comprising such compounds and methods of treatment comprising administering such compounds and compositions when an antibiotic effect is indicated.
Type:
Grant
Filed:
December 28, 1977
Date of Patent:
February 19, 1980
Assignee:
Merck & Co., Inc.
Inventors:
Burton G. Christensen, John Hannah, David H. Shih
Abstract: A method and apparatus for recovering embryos from embryonated eggs wherein the egg is cracked open the shell discarded and the contents dropped onto a continuously vibrating screen which separates the embryo from the yolk sac and accompanying fluid. This associated material, which is less cohesive than the embryo, passes through the screen. The screen itself is tilted at a compound angle from the horizontal and its vibrating action causes the embryos to move along the upper surface of the screen toward a discharge chute located at the lower corner of the screen.
Abstract: A process for producing a heteropolysaccharide by a bacterial fermentation procedure in which a species of bacteria or a mutant thereof is incubated in a fermentation medium which contains a carbon source, preferably a hydrolyxed starch, a source of magnesium ions, a source of phosphorous, a source of nitrogen and water with the incubation taking place at a temperature of about 28.degree. to about 35.degree. C.
Type:
Grant
Filed:
December 27, 1977
Date of Patent:
January 29, 1980
Assignee:
Merck & Co., Inc.
Inventors:
Kenneth S. Kang, George T. Veeder, III, Danny D. Richey
Abstract: Hepatitis B surface antigen free of gradient-derived added cesium and potassium ions, for example the antigen in an aqueous solution of sodium bromide.
Abstract: High purity HB.sub.s Ag is injected into guinea pigs to stimulate formulation of HB.sub.s Ab-positive serum. Gamma globulins containing HB.sub.s Ab are separated from the serum and the globulin fraction containing HB.sub.s Ab is isolated and coupled to a Sepharose gel. HB.sub.s Ag from HB.sub.s Ag-positive plasma is adsorbed on the gel by formation of an HB.sub.s Ab-HB.sub.s Ag complex. HB.sub.s Ag is eluted from the column and dialysed.