Abstract: The present invention provides antitumor fluoro-substituted 4'-demethylepipodophyllotoxin glucosides.

Abstract: This invention provides novel cephalosporanic acids and esters thereof having the general formula ##STR1## wherein R.sup.2 is hydrogen, or lower acyl, R.sup.3 is hydrogen, or lower alkanoyloxy, andR.sup.4 is hydrogen, 5-methyl-2-oxo-1,3-dioxolen-4-ylmethyl, 1-(ethoxycarbonyloxy)ethyl,1-(pivaloyloxy)ethyl, 1-(cyclohexylacetoxy)ethyl, or 1-(cyclohexyloxycarbonyloxy) ethyl. These compounds, especially esters, are useful as broad spectrum antibiotics in the treatment and prevention of infectious diseases of mammals, and for other purposes known in the art. The acids (R.sup.4 is hydrogen) are useful as intermediates for making the esters.

Abstract: 7-[2-(5-Amino-1,2,4-thiadiazol-3-yl)-2-(substituted)-iminoacetamido]-3-[3-( quaternaryammonio)-1-propen-1-yl]-3-cephem-4-carboxylates of the formula ##STR1## in which R.sup.1 and R.sup.2 are defined herein and --.sup..sym. N.tbd.Q is a quaternary ammonio group as defined herein, and salts, solvates, hydrates and esters thereof, are potent antibacterial agents. Processes for their preparation and intermediates in such processes are described.

Abstract: This invention provides novel cephalosporanic acids and esters thereof having the general formula ##STR1## wherein R.sup.2 is hydrogen, lower alkyl, lower alkenyl, lower alkynyl, cyclo(lower)alkyl or acyl, R.sup.3 is hydrogen, lower alkyl, lower alkoxy, lower alkanoyloxy, andR.sup.4 is hydrogen, pivaloyloxymethyl, acetoxymethyl, 1-acetoxyethyl, 5-methyl-2-oxo-1, 3-dioxolen-4-ylmethyl or 4-glycyloxybenzoyloxymethyl. These compounds, especially esters, are useful as broad spectrum antibiotics in the treatment and prevention of infectious diseases of mammals, and for other purposes known in the art.

Abstract: This invention provides novel cephalosporin intermediates, 7.beta.-amino-3-[(Z)-1-propen-1-y1]-3-cephem-4-carboxylic acid and esters thereof having the general formula ##STR1## wherein the configuration of the 3-propenyl group is Z sometimes referred to as cis- and R is hydrogen or a conventional carboxy-protected group, or a physiologically hydrolyzable esterifying group, and acid addition salts thereof and the metal salts of the foregoing substance wherein R is hydrogen. These compounds are useful as intermediates for preparation of orally active cephalosporins.

Abstract: 3-[(Z)-1-Propen-1-yl]-7-acylamido cephalosporins in which the 7-acyl group is phenylglycyl or substituted phenylglycyl are orally active antibiotics against Gram+ and Gram- bacteria.

Abstract: Temperature stable crystalline mono-hydrochloric and sulfuric acid addition salts of 7-amino-3-(1-methylpyrrolidinio)methyl-3-cephem-4-carboxylate substantially free of .DELTA..sup.2 isomer are intermediates for the preparation of broad spectrum 7-[.alpha.-(2-aminothiazol-4-yl)-.alpha.-(Z)-methoxyiminoacetamido]-3-[(1- methyl-1-pyrrolidinio)methyl]-3-cephem-4-carboxylates.

Abstract: The present invention relates to 7-[(D)-2-amino-2-(3-hydroxyphenyl)acetamido]-3-[(Z)-1-propenyl]-3-cephem-4 -carboxylic acid, which is an orally active antibiotic against Gram-positive and Gram-negative bacteria.

Abstract: 3-[(Z)-1-Propen-1-yl]-7-acylamido cephalosporins in which the 7-acyl group is phenylglycyl or substituted phenylglycyl are orally active antibiotics against Gram+ and Gram- bacteria.

Abstract: Compounds of the formula ##STR1## wherein R.sup.1 is hydrogen or a conventional amino-protecting group, R.sup.2 is a straight or branched chain alkyl, alkenyl or alkynyl containing from 1 to 4 carbon atoms, and ##STR2## is a quaternary ammonio group as described herein, and nontoxic pharmaceutically acceptable salts, physiologically hydrolyzable esters and solvates thereof, as well as processes for their preparation, are disclosed. The compounds in which R.sup.1 is hydrogen are potent antibacterial agents.

Abstract: 3-[(Z)-1-Propen-1-yl]-7-acylamido cephalosporins in which the 7-acyl group is phenylglycyl or substituted phenylglycyl are orally active antibiotics against Gram+ and Gram- bacteria.

Abstract: Compounds of the formula ##STR1## wherein R.sup.1 is hydrogen or a conventional amino-protecting group, R.sup.2 is a straight or branched chain alkyl group containing from 1 to 4 carbon atoms, allyl, 2-butenyl, 3-butenyl, propargyl, 2-butynyl, 3-butynyl, cycloalkyl containing from 3 to 6 carbon atoms or a group of the formula ##STR2## in which R.sup.3 and R.sup.4 each are independently hydrogen, methyl or ethyl, or R.sup.3 and R.sup.4, taken together with the carbon atom to which they are attached, may be a cycloalkylidene ring containing from 3 to 6 carbon atoms or a substituted cyclobutylidene ring of the formula ##STR3## wherein X is halogen, hydroxy or (lower)alkoxy, and R.sup.5 and R.sup.

Abstract: Compounds of the formula ##STR1## wherein R.sup.1 is hydrogen or a conventional amino-protecting group, R.sup.2 is one of various alkyl, alkenyl, alkynyl, cycloalkyl, carboxyalkyl or carboxycycloalkyl moieties described herein, and R.sup.5 is hydrogen, amino, carboxy, formyl, carbamoyl, guanidino, amidino or one of various alkyl, alkoxy, alkylthio or substituted amino moieties described herein, and nontoxic pharmaceutically acceptable acid addition salts, physiologically hydrolyzable esters and solvates thereof, as well as processes for their preparation, are disclosed. The compounds in which R.sup.1 is hydrogen are potent antibacterial agents.

Abstract: 7-{(Z)-2-(2-Aminothiazol-4-yl)-2-[(substituted)oxyimino]acetamido}-3-[3-(qu aternary ammonio)-1-propen-1-yl]-3-cephem-4-carboxylates and salts, esters and solvates thereof, having potent antibacterial activity, are provided. Processes for their preparation and intermediates in their preparation also are disclosed.

Abstract: Potent antibacterial agents of the formula ##STR1## wherein R is methyl, ethyl or isopropyl, and their pharmaceutically acceptable salts, physiologically hydrolyzable esters and solvates, and processes for their preparation, are described.

Abstract: Compounds of the formula ##STR1## wherein R.sup.1 is hydrogen or a conventional amino-protecting group, R.sup.2 and R.sup.3 each are independently methyl or ethyl, and R.sup.4 is methyl, ethyl, n-propyl, isopropyl, n-butyl, isobutyl, allyl, 2-butenyl, 3-butenyl, 2-hydoxyethyl, 3-hydroxypropyl, 2-(dimethylamino)ethyl, pyridylmethyl, pyridylethyl, benzyl or phenethyl, and nontoxic pharmaceutically acceptable acid addition salts and solvates thereof, as well as processes for their preparation, are disclosed. The compounds in which R.sup.1 is hydrogen are potent antibacterial agents.

Abstract: Compounds of the formula ##STR1## wherein R.sup.1 is hydrogen or a conventional amino-protecting group, and R.sup.2 is a straight or branched chain alkyl group containing from 1 to 4 carbon atoms, allyl, 2-butenyl or 3-butenyl, and nontoxic pharmaceutically acceptable salts and solvates thereof, as well as processes for their preparation, are disclosed. The compounds in which R.sup.1 is hydrogen are potent antibacterial agents.

Abstract: Potent antibacterial agents of the formula ##STR1## wherein R is methyl, ethyl or isopropyl, and their pharmaceutically acceptable salts, physiologically hydrolyzable esters and solvates, and processes for their preparation, are described.

Abstract: Certain cephalosporins having a heterocyclicthiomethyl group at the 3-position such as cefoperazone are prepared by reacting a solution of a 7-acylamidocephalosporanic acid having a free amino group as part of said acyl substituent with about an equi-molar amount of the thiolester ##STR1## wherein --S-Het is the desired conventional heterocyclicthio group which displaces the 3-acetoxy group of the starting acid and ##STR2## is the conventional acyl group which displaces a hydrogen on the free amino group which is part of the acyl substituent of the starting 7-acylamidocephalosporanic acid.

Abstract: 7-[D-.alpha.-(4-Hydroxy-1,5-naphthyridine-3-carboxamido)-.alpha.-phenyl (and thienyl and substituted phenyl) acetamido]-3-(2-, 3- or 4-N,N-dimethylaminomethyl-pyridinium)methyl-3-cephem-4-carboxylates were synthesized and found to have potent antibacterial activity in vitro especially against many strains of Pseudomonas aeruginosa.