Abstract: [[[(2,4-Dioxo-1-imidazolidinyl)amino]carbonyl]amino]-acetylcephalosporin derivatives having the formula ##STR1## wherein R is hydrogen, lower alkyl, phenyl-lower alkyl, diphenyl-lower alkyl, tri(lower alkyl)silyl, trihaloethyl, a salt forming ion, or the group ##STR2## R.sub.1 is hydrogen or methoxy; R.sub.2, R.sub.3 and R.sub.5 each is hydrogen or lower alkyl; R.sub.4 is hydrogen, lower alkyl, cyclo-lower alkyl, cyclo-lower alkenyl, cyclo-lower alkadienyl, phenyl, phenyl-lower alkyl, substitutted phenyl, substituted phenyl-lower alkyl, or certain heterocyclic groups; R.sub.6 is lower alkyl; and X is hydrogen, lower alkanoyloxy, ##STR3## or certain heterothio groups; are useful as antibacterial agents.

Abstract: The invention provides novel antibiotic compounds which are 7.beta.-acylamidoceph-3-em-4-carboxylic acids, and non-toxic derivatives thereof characterized in that the acylamido group has the structure ##STR1## where R is a hydrogen atom or an organic group and R.sup.a is an etherifying monovalent organic group linked to the oxygen atom through a carbon atom. The compounds are syn isomers or exist as mixtures containing at least 75% of the syn isomer. These antibiotic compounds possess high antibacterial activity against a range of gram positive and gram negative organisms coupled with particularly high stability to .beta.-lactamases produced by various gram negative organisms. The invention is also concerned with the administration of the compounds.

Abstract: The invention provides novel antibiotic compounds which are 7.beta.-acylamidoceph-3-em-4-carboxylic acids, and non-toxic derivatives thereof characterized in that the acylamido group has the structure ##STR1## where R is a hydrogen atom or an organic group and R.sup.a is an etherifying monovalent organic group linked to the oxygen atom through a carbon atom. The compounds are syn isomers or exist as mixtures containing at least 75% of the syn isomer. These antibiotic compounds possess high antibacterial activity against a range of gram positive and gram negative organisms coupled with particularly high stability to .beta.-lactamases produced by various gram negative organisms. The invention is also concerned with the administration of the compounds.

Abstract: Phthalidyl and substituted phthalidyl esters of certain cephalosporins are absorbed by the oral route into the serum, where they are hydrolyzed to the parent antibacterially active cephalosporin.

Abstract: Trifluoroalkylureido cephalosporins of the formula ##STR1## wherein R is hydrogen, lower alkyl, phenyl-lower alkyl, diphenyl-lower alkyl, tri(lower alkyl)silyl, trihaloethyl, a salt forming ion, or the group ##STR2## R.sub.1 is hydrogen or methoxy; A is straight or branched chain alkylene of 1 to 6 carbons; R.sub.2 is hydrogen or lower alkyl; R.sub.3 is hydrogen, lower alkyl, cycloalkyl, cycloalkenyl, cycloalkadienyl, phenyl, phenyl-lower alkyl, substituted phenyl, substituted phenyl-lower alkyl, or certain heterocyclic groups; R.sub.4 is hydrogen or lower alkyl; R.sub.5 is lower alkyl; and X is hydrogen, lower alkanoyloxy, ##STR3## or certain heterothio groups are disclosed. These compounds are useful as antibacterial agents.

Abstract: 7-D-.alpha.-Amino-.alpha.-(p-acetoxyphenyl)acetamido-3-methyl-3-cephem-4-ca rboxylic acid is prepared in a form substantially free of the L-isomer and hydrolyzed enzymatically, preferably using wheat bran, to produce p-hydroxycephalexin (cefadroxil).

Abstract: New .alpha.-hydrazinocarbonylamino cephalosporins which have the formula ##STR1## are useful as antimicrobial agents.

Abstract: An improved process for preparing 4-thia-2,6-diazabicyclo[3,2,0]hept-2-ene-7-ones such as methyl 3-phenoxy-4-thia-2,6-diazabicyclo[3,2,0]hept-2-ene-7-one-6-isopropenylacet ate which comprises extruding sulfur from dithiazeneazetidinones such as methyl 3-phenoxymethyl-4,5-dithia-2,7-diazabicyclo[4,2,0]-oct-2-ene-8-one-7-isopr openylacetate. The compounds obtained are useful intermediates in the preparation of certain 3-cephems.

Abstract: New N-substituted thio (or sulfinyl) aliphatic acylcephalosporin C and derivatives thereof in the 3-position have been prepared. The compounds are useful as intermediates for recovering cephalosporin C and deacetoxycephalosporin C from fermentation broths thereof and also for preparing 7-aminocephalosporanic acid and derivatives thereof in the 3-position.

Abstract: A composition of matter having the structural formula ##STR1## wherein R is a radical selected from the group consisting of carboxylic acid radicals, --OH or --NH.sub.2.

Abstract: Compounds of the formula ##STR1## wherein R.sub.1 is hydrogen, lower alkyl, cycloalkyl, cycloalkenyl, cycloalkadienyl, phenyl, phenyl-lower alkyl and substituted phenyl and phenyl-lower alkyl; R.sub.2 is hydrogen or lower alkyl; R.sub.3 is hydrogen, lower alkyl, phenyl-lower alkyl, substituted phenyl-lower alkyl, diphenyl-lower alkyl, tri(lower alkyl)stannyl, tri(lower alkyl)silyl, a salt forming ion, or the group ##STR2## wherein R is lower alkyl, phenyl, phenyl-lower alkyl, or substituted phenyl and phenyl-lower alkyl; and R.sub.4 represents certain heterocyclic groups are disclosed. These compounds are useful as antibacterial agents.

Abstract: Acylamino quinophthalone compounds which are free from sulfonic acid groups and correspond to the formula ##STR1## in which R.sub.1 and R.sub.2 are hydrogen, halogen, acylamino or lower alkoxy with the proviso that one of the residues R.sub.1 and R.sub.2 denotes acylamino while the other residue stands for hydrogen, halogen or a lower alkoxy; R.sub.3 is hydrogen, halogen or a lower alkoxy; X is a substituent; and n is a number from 0 to 3; are disclosed. The compounds useful as dyestuffs for hydrophobic fiber materials, e.g. polyester, are prepared by reacting an acylamino phthalic acid, the anhydride thereof, or mixtures of acylamino phthalic acids or the anhydrides thereof with a 3-hydroxy-quinalide.

Abstract: Vincaleukoblastine (VLB, vinblastine) is reacted with thionyl chloride to form a bis-sulfite ester which is converted to various 5'-oxygenated derivatives.

Abstract: Novel N-(1-substituted-3-pyrrolidinyl)-1-naphthalene- and 4-quinolinecarboxamides of the formula: ##STR1## wherein R is lower cycloalkyl, R.sup.1 is hydrogen, lower alkyl or aryl, R.sup.2 is hydrogen, lower-alkyl, halogen, lower-alkoxy, amino or nitro, R.sup.3 is hydrogen, lower-alkyl, halogen, lower-alkoxy, amino or nitro, Y is carbon or nitrogen and pharmaceutically acceptable acid addition salts thereof having anti-emetic properties are disclosed.

Abstract: Berberine and protoberberine analogs thereof are oxidatively dimerized in the presence of a base. Treatment of the dimer with alkanolic anhydrous acid yields the corresponding 8-alkoxyberberine (or protoberberine) phenol betaine which, in turn, may be converted to alpha and beta hydrastine.

Abstract: Quinolopyran-4-one-2-carboxylic acid derivatives and salts thereof are provided as novel compounds and as medicines for treatment of allergic asthma, each of the derivatives being represented by the general formula ##STR1## wherein X designates a member selected from the group consisting of alkyl groups having 1 to 5 carbon atoms, alkoxy groups having 1 to 5 carbon atoms, halogen atoms, aryl-substituted alkoxy groups having 7 to 10 total carbon atoms, alkoxycarbonyl groups having 2 to 6 total carbon atoms, and aryl groups having 6 to 10 carbon atoms, and n is any one of the integers 1 through 4, X being the same group or different groups in the case where n is at least 2.

Abstract: Certain esters of 6,7-methylenedioxy-1-(2,2,2-trifluoroethyl)-4(1H)-quinolone-3-carboxylic acid, such as the trimethylacetoxymethyl ester, useful as antibacterials.

Abstract: Carbamoyalkylureido cephalosporins of the formula ##STR1## wherein R is hydrogen, lower alkyl, phenyl-lower alkyl, diphenyl-lower alkyl, tri(lower alkyl)silyl, trihaloethyl, a salt forming ion, or the group ##STR2## R.sub.1 is hydrogen or methoxy; A is straight or branched chain alkylene of 1 to 6 carbons; R.sub.2 and R.sub.3 are independently selected from hydrogen and straight chain alkyl of 1 to 4 carbons, or R.sub.2 is hydrogen and R.sub.3 is branched chain alkyl of 3 or 4 carbons, phenyl, benzyl or phenethyl, or R.sub.2 and R.sub.3 taken together with N atom to which they are attached form ##STR3## R.sub.4 is hydrogen or lower alkyl; R.sub.5 is hydrogen, lower alkyl, cycloalkyl, cycloalkenyl, cycloalkadienyl, phenyl, phenyl-lower alkyl, substituted phenyl, substituted phenyl-lower alkyl, or certain heterocyclic groups; R.sub.6 is hydrogen or lower alkyl; R.sub.7 is lower alkyl; and X is hydrogen, lower alkanoyloxy, ##STR4## or certain heterothio groups; are disclosed.

Abstract: A process for the preparation of azetidinone-thiazoline precursors for cephalosporin synthesis.

Abstract: This invention relates to cephalosporanic acid derivatives of the formula: ##STR1## where R.sub.1 is phenyl or thienyl,R.sub.2 is pyridyl andR.sub.3 is hydrogen or alkylthio, and pharmaceutically aceptable salts thereof, which possess antibacterial activity, pharmactical compositions of the same and processes for the preparation thereof.