Abstract: A process for preparing 7.alpha.-methoxycephalosporin compounds which comprises reacting a salt of a 7.beta.-benzylideneamino-7.alpha.-methoxy-3-cephem-4-carboxylic acid with a hydrazine compound to give a salt of a 7.beta.-amino-7.alpha.-methoxy-3-cephem-4-carboxylic acid and reacting the latter compound with a carboxylic acid or its reactive derivative. The products are useful as antibacterial agents.

Abstract: The invention relates to magnesium halide derivatives of tetrahydroquinolines and related compounds. These are intermediates useful in the preparation of anti-ulcer agents.

Abstract: Certain substituted 6,7-dihydro-7-hydroxy-1-oxo-1H,5H-benzo[ij]quinolizine-2-carboxylic acids and salt and ester derivatives thereof are described. These compounds are useful antibacterial agents. SPThis is a division of application Ser. No. 567,510, filed Apr. 14, 1975, now U.S. Pat. No. 3,985,753.

Abstract: Alkoxy and alkylthioalkylureido 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 lower alkyl; Y is O or S; R.sub.3 is hydrogen or lower alkyl; R.sub.4 is hydrogen, lower alkyl, cycloalkyl, cycloalkenyl, cycloalkadienyl, phenyl, phenyl-lower alkyl, substituted phenyl, substituted phenyl-lower alkyl, or certain heterocyclic groups; R.sub.5 is hydrogen or lower alkyl; R.sub.6 is lower alkyl; and X is hydrogen, lower alkanoyloxy, ##STR3## or certain heterothio groups; are disclosed. These compounds are useful as antibacterial agents.

Abstract: 2,6-Diamino-1,4-dihydropyridines bearing carbonyl functions in the 3- and 5-positions and being substituted in the 4-position by lower alkyl, phenyl, substituted phenyl or a heterocyclic group are antihypertensive agents and coronary vessel dilators. The compounds, of which 2,6-diamino-4-(3-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylic acid 3,5-diethyl ester is a representative embodiment, are prepared through condensation of an amidine with either an aldehyde or an ylidenecyanoacetoacetic acid ester.

Abstract: Cycloalkano-quinolone derivatives having anti-microbial activity characterized by the formula: ##STR1## wherein one of R.sub.1 and R.sub.2 designates hydrogen, halogen, nitro, amino, hydroxyl, acylamino, acyloxy, alkoxy or aryloxy and the other taken together with R.sub.3 forms an alkylene bridge containing 2 to 6 carbon atoms, X is hydrogen, lower alkyl, which may be substituted by a member of the group consisting of halogen, hydroxyl, acyloxy, alkoxy, aryloxy, aralkyloxy, mercapto, alkylmercapto, arylmercapto, arylsulfonyl, and alkylsulfonyl, or X is unsubstituted alkenyl including alkadienyl, or alkynyl and Y is hydroxyl, amino or lower alkoxy, and the pharmaceutically acceptable salts thereof.

Abstract: A process for introducing an alkoxy group into the 7.alpha.-position of a 7-amino-3-cephem-4-carboxylic acid derivative which comprises oxidizing a salt of 7-benzylideneamino-3-cephem-4-carboxylic acid derivative and reacting the product with an alkanol.The 7.alpha.-alkoxy-3-cephem-4-carboxylic acid derivatives obtained by the present invention are useful as intermediates for the synthesis of antibacterial agents.

Abstract: The invention provides a compound of formula I ##STR1## wherein R.sup.1 and R.sup.2 are the same or different and represent hydrogen or alkyl of 1-6 carbon atoms, R.sup.3 represents hydrogen, alkyl of 1-6 carbon atoms, or phenyl, X is Na, K, Li, or CSNHR.sup.4 wherein R.sup.4 is hydrogen or alkyl of 1-6 carbon atoms and n is 3, 4 or 5 or a pharmaceutically acceptacle acid addition salt of a compound where X is CSNHR.sup.4.The compounds of formula I wherein X is CSNHR.sup.4 are anti-ulcer agents. Those in which X is Na, K or Li are intermediates.

Abstract: 4,5-Dihalopyrrole-2-carboxamide derivatives, prepared by reaction of a corresponding 4,5-dihalopyrrole-2-carboxylic acid halide or a corresponding 4,5-dihalopyrrol-2-yl trihalomethyl ketone with an appropriate amine, useful as antibacterial and herbicidal agents.

Abstract: Novel pyrrolobenzoxazalkanes, physiologically tolerable acid addition salts thereof and a method of preparing same are described. Compounds of the present invention are useful as analgesic, tranquilizing and anticonvulsant agents.

Abstract: Novel cephalosporin antibiotic derivatives.

Abstract: The compounds of this invention are cephalosporins having various acyl substituents at the 7-position and a sulfoalkyl substituted oxadiazolylthiomethyl group at the 3-position of the cephem nucleus and intermediates for the preparation thereof. The 7-acylated compounds have antibacterial activity.

Abstract: Pyranoindole and thiopyranoindole derivatives characterized by having an amino(lower)alkyl radical attached to either or both the 1 and 9 position of a pyrano[3,4-b]indole or thiopyrano[3,4-b]indole nucleus or having said radical attached to the 1 position of a pyrano[4,3-b]indole or thiopyrano[4,3-b]indole nucleus are disclosed. The amino portion of the amino(lower)alkyl radical may be further substituted with one or two lower alkyl groups or incorporated into a heterocyclic amine radical. The derivatives having the amino(lower)alkyl radical only at position 1 are further substituted at position 1 and may be optionally substituted at positions 3,4,5,6,7,8, and 9.

Abstract: Compounds of the formula ##STR1## wherein R.sub.1 denotes optionally substituted phenyl, thienyl, furyl or 1,4-cyclohexadienyl, R.sub.2 represents a free carboxyl group or an esterified carboxyl group which can be split physiologically, R.sub.3 represents hydrogen, lower akoxy or an optionally substituted methyl group and B represents an optionally substituted six-membered ring with 1 to 3 ring nitrogen atoms, which is bonded to the carbonyl group --C(.dbd.O)-- by one of its carbon atoms, the nitorgen atoms of a monocyclic six-membered ring having 2 nitrogen atoms being either adjacent or separated by two ring carbon atoms, and the salts of such compounds which have a salt-forming group, including the inner salts, for example the 7.beta.-[D(-)-.alpha.-(3,5-Dioxo-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbo xamido)-phenylacetamido]-cephalosporanic acid, have antibiotic activity.

Abstract: This invention is concerned with 7-(.alpha.-substituted glycinamido)-3-substituted methyl-3-cephem-4-carboxylic acids, derivatives and non-toxic pharmaceutical salts thereof, which possess antibacterial activity, process for preparation thereof, having the following general formula ##STR1## wherein R.sub.1, R.sub.2, R.sub.3 and M are as defined hereinafter.

Abstract: 7-[.alpha.-(guanyl-1-ureido)phenylacetamido]-3-(1-methyl-1H-tetrazol-5-ylth iomethyl)-3-cephem-4-carboxylic acid, 7-[.alpha.-(3-guanyl-1-ureido)phenylacetamido]-3-(5-methyl-1,3,4-thiadiazo l-2-ylthiomethyl)-3-cephem-4-carboxylic acid and related compounds, the pharmaceutically acceptable non-toxic salts and certain esters thereof are valuable broad spectrum antibiotics demonstrating high levels of activity against Pseudomonas species.

Abstract: Reduction of 24-methylene-14a-aza-D-homo-cholesta-8(9), 14(14a)-dienes provides new antifungal agents.

Abstract: Derivatives of quinoline-8-carboxylic acid having pesticidal action are disclosed, as are compositions comprising such derivatives.The quinoline-8-carboxylic acid derivatives which we have found to be effective pesticides include such derivatives having the general formula: ##STR1## in which R represents H, halogen, C.sub.1 -C.sub.3 alkyl, C.sub.2 -C.sub.6 alkenyl, CF.sub.3, C.sub.1 -C.sub.3 - alkoxyl or C.sub.1 -C.sub.3 - alkythio;X represents the group OY, in which Y is H, C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.6 alkenyl, C.sub.2 -C.sub.6 alkinyl optionally substituted, an alkali metal, an alkaline earth metal, a transition metal, Mn, NR.sub.2 in which both R equal or different have the same significance as above or are pyridines, aryl or alkyl or aralkylamines; and the quarternarized nitrogen salts of said compounds.The compounds having formula: I. are distinguished by having good activity as pesticides and, in particular, as insecticides.

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

Abstract: Certain novel 6,7-methylenedioxy-1-(2,2,2-trifluoroethyl)-4(1H)-quinolone-3-carboxylic acid esters are useful in the treatment of bacterial infections in warm-blooded animals. The novel 6,7-methylenedioxy-1-(2,2,2-trifluoroethyl)-4(1H)-quinolone-3-carboxylic acid and its salts and alkyl esters of 1 to 3 carbon atoms are useful as chemical intermediates.