Abstract: The purified Group A polysaccharide antigen isolated from N. meningitidis for vaccination against this type of bacterial meningitidis is prepared from an isotonic ratio of aqueous sodium chloride solution freeze-dried at temperatures of from -20.degree. C. to -30.degree. C. This low temperature lyophilization dries the sodium chloride polysaccharide menstrum without loss of molecular weight, i.e., potency.
Abstract: A novel improved molecular sieve is prepared by a caustic wash process. The sieves so prepared show improved properties in reactions involving e.g., superior acid scavenging ability.
Type:
Grant
Filed:
August 31, 1977
Date of Patent:
January 16, 1979
Assignee:
Merck & Co., Inc.
Inventors:
Alan J. Rein, David D. Saperstein, Seemon H. Pines
Abstract: Freeze-thaw and heat stable icings are obtained by using an icing composition containing a high melting point fat and a gelling system consisting essentially of xanthan gum and locust bean gum.
Abstract: Biological fluid containing hepatitis B surface antigen is subjected to isopycnic banding with collection of fractions rich in Dane particles. The Dane particles are useful as diagnostic and immunologic agents.
Abstract: Disclosed is the antibiotic 5-methyl-2-(1-carboxyl-2-methyl-propen-1-yl)-3-oxo-6-thia-2-azabicyclo [2.2.0] hexane (I): ##STR1## Also disclosed are processes for preparing I and its pharmaceutically acceptable salts and esters; pharmaceutical compositions comprising such compounds; and methods of treatment comprising administering such compounds and compositions when an antibiotic effect is indicated.
Abstract: 1,3,5-s-Hexahydrotrisubstituted triazines exemplified by 1,3,5-tris(furfuryl)-1,3,5-hexahydro-s-triazines are useful as antimicrobial agents particularly when employed as a component of metal-working compositions subject to fungal and bacterial attack.
Abstract: Thienamycin sulfoxide (I, n=1), Thienamycin sulfone (I, n=2), and their pharmaceutically acceptable salts are disclosed to be useful as antibiotics: ##STR1## 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: Disclosed are the antibiotics 6-ethylpenicillanic acid and 6-ethylpenicillanic acid sulfoxide (I): ##STR1## Also disclosed are processes for preparing I and its pharmaceutically acceptable salts and esters; pharmaceutical compositions comprising such compounds; and methods of treatment comprising administering such compounds and compositions when an antibiotic effect is indicated.
Abstract: A vaccine against Group C meningococcal meningitis consisting of a polysaccharide of which at least 80% by weight has a molecular weight in excess of 1,000,000 daltons is prepared. The polysaccharide was isolated from Group C hexadecyl trimethylammonium bromide cell paste with 1.0M CaCl.sub.2 extraction and purified by phenol extraction, ultracentrifugation at 100,000 g. and ethanol fractionation (30%-45% v/v in ethanol).
Type:
Grant
Filed:
August 1, 1977
Date of Patent:
October 31, 1978
Assignee:
Merck & Co., Inc.
Inventors:
Arpi Hagopian, Dennis J. Carlo, Thomas H. Stoudt
Abstract: Disclosed is a class of cephalosporins including the carba, aza and oxa nuclear analogues thereof which bear at the 3-position a substituted thio substituent; such compounds 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: By serially passaging virulent respiratory syncytial virus in human diploid lung fibroblasts, a non-pathogenic but antigenic live respiratory syncytial virus is produced. This virus is useful in preparing a live virus vaccine.
Abstract: New 7-(Amidinothio)acetamido-7-methoxy-3-carbamoyloxymethyl-3-cephem-4-carboxy lic acid compounds are prepared which are useful as antibacterial agents, especially Pseudomonas.
Type:
Grant
Filed:
February 4, 1977
Date of Patent:
October 17, 1978
Assignee:
Merck & Co., Inc.
Inventors:
Robert F. Czaja, Edward J. J. Grabowski
Abstract: 1,3,5-s-Hexahydrotrisubstituted triazines exemplified by 1,3,5-tris(tetrahydrofurfuryl)-1,3,5-hexahydro-s-triazines are useful as antimicrobial agents particularly when employed as a component of metal-working compositions subject to fungal and bacterial attack.
Abstract: New 7-diacylimido cephalosporins are produced by reacting 7-acylamido cephalosporins with an acylating agent in the presence of a silyl reagent. The 7-diacylimido cephalosporins are cleaved to produce cephalosporins containing a different acylamido moiety. Thus, the aminoadipoyl group of cephalosporins produced by fermentation is replaced by a different acyl group by the process of the present invention. The cephalosporins produced are antibiotics having enhanced activity against gram-negative and gram-positive pathogens.
Type:
Grant
Filed:
April 25, 1977
Date of Patent:
August 15, 1978
Assignee:
Merck & Co., Inc.
Inventors:
Burton G. Christensen, Lovji D. Cama, Sandor Karady, Meyer Sletzinger
Abstract: A process is provided which yields derivatives of cephalosporins and penicillins. The process starts with 7-acylaminocephalosporin, or 6-acylaminopenicillin, then the latter compounds are treated with an organolithium compound, followed with t-butyl-hypochlorite. Finally, a defined reagent is added yielding a side chain on the carbon adjacent to the amino-nitrogen. Novel intermediate compounds are also described. The end compounds prepared are active against both gram-positive and gram-negative bacteria.
Type:
Grant
Filed:
February 14, 1977
Date of Patent:
July 25, 1978
Assignee:
Merck & Co., Inc.
Inventors:
Raymond A. Firestone, Lovji D. Cama, Burton G. Christensen
Abstract: Novel dibicyclo [2.2.2] octyl dibicyclo [2.2.2] octenyl polyamines are useful antimicrobial agents, as well as algae inhibitors. They are especially useful as hard surface disinfectants and as additives to oil well drilling muds, injection brines and industrial water where bacterial control is desired.
Type:
Grant
Filed:
June 10, 1976
Date of Patent:
July 11, 1978
Assignee:
Merck & Co., Inc.
Inventors:
Nathaniel Grier, Richard A. Dybas, Robert A. Strelitz
Abstract: A novel total synthesis process is provided, yielding cephalosporin or penicillin compounds. The process uses as starting material a glycine ester, which first is reacted to yield a dihydrothiazine, and subsequently condensed with azidoacetyl chloride to form the cepham nucleus, then dehydrated to yield the desired 3-unsaturation. Subsequent reduction and acylation steps are analogous to known chemistry. The end products are antibacterial agents.
Type:
Grant
Filed:
March 30, 1976
Date of Patent:
July 4, 1978
Assignee:
Merck & Co., Inc.
Inventors:
Burton G. Christensen, Ronald W. Ratcliffe
Abstract: Organic compounds containing one or more alcoholic hydroxyl groups are transformed into fluorine compounds by reacting them with sulfur tetrafluoride in liquid hydrogen fluoride solution, at temperatures between around -80.degree. C. and +20.degree. C. The method can be descriptively termed "fluorodehydroxylation", because it represents the reaction:ROH.fwdarw.RF.
Abstract: A method for the total chemical synthesis of flavipucine employs the condensation of 4-hydroxy-6-methyl-2-pyridone with isobutylglyoxal in alkali alkoxide. The resulting alkali salt is acylated in both the 1' and 4 positions. Treatment of the 1',4-diacyloxy derivative with excess alkaline peroxide yields flavipucine.
Type:
Grant
Filed:
May 19, 1977
Date of Patent:
June 13, 1978
Assignee:
Merck & Co., Inc.
Inventors:
Norman L. Wendler, Narindar N. Girotra, Zbigniew S. Zelawski, deceased
Abstract: 2-R-substituted-1,2,5-thiadiazole-3-ones have broad spectrum antibacterial and antifungal activity. They are especially useful in agriculture to protect plants against diseases such as leaf, stem, and fruit spotting, internal discoloration and decay of fruits and vegetables. These compounds are particularly active against diseases caused by the genera Pseudomonas, Xanthomonas, Erwinia, and Corynebacterium.