Abstract: 7.beta.-Acylamino-3-alkoxycarbonyl-(and 3-keto)-1-carba(1-dethia)-3-cephem-4-carboxylic acids and derivatives and related 3-substituted compounds are provided as antibiotics useful for treating infections in man and animals. Pharmaceutical formulations comprising the antibiotics and intermediates a process for their preparation are provided. Exemplary compounds provided are 7.beta.-[D-(2-phenyl-2-aminoacetyl)amino]-3-methoxycarbonyl-1-carba(1-deth ia)-3-cephem-4-carboxylic acid and 7.beta.-[2-(2-aminothiazol-4-yl)-2-methoxyimino-acetamido]-3-acetyl-1-carb a(1-dethia)-3-cephem-4-carboxylic acid.

Abstract: Crystalline p-nitrobenzyl 7.beta.-phenoxyacetylamino-3-hydroxy-1-carba(dethia)-3-cephem-4-carboxylat e and the crystalline mono-acetic acid solvate thereof are provided by mixing a carboxylic acid or a sulfonic acid with a solution of the 3-hydroxy ester in DMF or DMAC. Acetic acid provides the crystalline acetic acid solvate while other acids provide crystalline non-solvated 3-hydroxy ester. The crystalline forms are useful purified intermediates to antibiotics.

Abstract: 7.beta.-Acylamino-3-trifluoromethylsulfonyloxy-1-carba-3-cephem-4-carboxyli c acid antibiotic compounds, esters and salts thereof, and the corresponding 7-amino and protected 7-amino 1-carbacephalosporins are provided. The 3-trifluoromethylsulfonyloxy-substituted 1-carbacephalosporins also are useful in a process for preparing 3-halo-1-carbacephalosporins which comprises reacting a 3-triflate ester with a lithium halide in an aprotic polar solvent.

Abstract: Carbacephem and cephem compounds represented by the formula: ##STR1## [Wherein X is S or CH.sub.2 ; n is an integer of 1 to 5; R.sub.1 is an unsubstituted or substituted heterocyclic group (where the heterocyclic group is a 5- or 6-membered heterocyclic group having 1 to 4 of O, S and N); R.sub.2 is a group represented by the formula: ##STR2## (where R.sub.4 is an unsubstituted or substituted phenyl or 2-aminothiazolyl) or a group represented by the formula: ##STR3## (where R.sub.5 is an unsubstituted or substituted lower alkyl); R.sub.3 is hydrogen, an alkali metal, an alkaline earth metal, an organic ammonium group or an ester residue, and R.sub.1 may be a quaternary ammonium group, where --CO.sub.2 R.sub.3 represents --CO.sub.2.sup.- ] have strong antibacterial activity against Gram-positive and Gram-negative bacteria, and are useful for treating various infections.

Abstract: Disclosed are optically active acylated cephalosporin analogs which are useful as antibacterial agents and methods for preparing such compounds.

Abstract: The present invention relates to novel 2-piperazinopyrimidine derivatives represented by the following general formula [I] which are useful as, for example, an active ingredient of herbicides ##STR1## wherein R.sup.1 is a hydrogen atom or an aralkyl group and Y is one of the groups represented by the following general formulas [II] to [VII] ##STR2## (wherein a and b are positions to be bound to positions 4 and 5 of the pyrimidine ring of the formula [I], respectively; l.sub.1 and l.sub.2 each are an integer of 2 to 4; l.sub.3 is 2 or 0; l.sub.4 is 0 or 1, provided that l.sub.4 is 0 when l.sub.3 is 2 and l.sub.4 is 1 when l.sub.3 is 0; l.sub.5 is 2 or 3; l.sub.6 is 1 or 2; l.sub.7 is 2 or 3; R.sup.2 is a hydroxyl group or a toluenesulfonyloxy group; and R.sup.3, R.sup.4, R.sup.5, R.sup.6 and R.sup.7 each are a hydrogen atom or a lower alkyl group).

Abstract: Optically active cephalosporin analogs are produced by optically selective deacylation of an optically inactive acylated analog. The compounds are useful as intermediates in the preparation of optically active acylated antimicrobial agents.

Abstract: Tetrahydroazeto[2,1-a]isoquinoline of the formula (I): ##STR1## wherein R, R.sup.1, R.sup.2 and R.sup.3 are substituents and x and y are 0-2. Also pharmaceutical compositions for relieving depression in mammals, e.g. in humans, and methods for synthesis and use of formula (I) compounds as well as novel intermediates in the synthesis.

Abstract: Novel cephalosporin analogs are disclosed which have antibacterial activity. Methods for producing the compounds are also disclosed.

Abstract: .beta.-Lactam compounds represented by the general formula: ##STR1## (wherein X represents CH.sub.2, S or O; Y represents a hydroxyl group, a lower alkanoyloxy group or a lower alkoxycarbonyloxy group; W is a group represented by CH.sub.2, NH, ##STR2## A is a phenyl group, a naphthyl group, or a monocyclic or dicyclic heterocyclic group, respectively substituted by (Y).sub.n ; R.sub.4 and R.sub.5 each are a hydrogen atom, a lower alkyl group, or a cycloalkylidene group with a carbon atom combined therewith; l is 0 or an integer of 1, 2 or 3; m is 0 or 1; n is an integer of 1, 2, 3, 4 or 5; and R.sub.1, R.sub.2 and R.sub.3 are groups often used in the conventional .beta.-lactam compounds) have strong antimicrobial activities against a wide range of Gram positive and negative bacteria; particularly Gram negative bacteria including Pseudomonas aeruginosa, Pseudomonas sepatia and various Enterobacters.

Abstract: The presence of a copper salt during the oximation of a .beta.-lactam containing compound having glyoxylamino substituents of the formula ##STR1## by reaction with an aminooxy compound having the formulaH.sub.2 N--O--R.sub.a,or a salt or ester thereof, results in a product wherein the ratio of syn isomer to anti isomer is increased.

Abstract: 7.beta.-Acylamino-3-trifluoromethylsulfonyloxy-1-carba-3-cephem-4-carboxyli c acid antibiotic compounds, esters and salts thereof, and the corresponding 7-amino and protected 7-amino 1-carbacephalosporins are provided. The 3-trifluoromethylsulfonyloxy-substituted 1-carbacephalosporins also are useful in a process for preparing 3-halo-1-carbacephalosporins which comprises reacting a 3-triflate ester with a lithium halide in an aprotic polar solvent.

Abstract: Optically active cephalosporin analogs of the formula ##STR1## wherein R.sub.2 represents a hydrogen or a group represented by the formula ##STR2## wherein R.sub.3 is a straight or branched lower alkyl group having 1 to 6 carbon atoms, a straight or branched lower alkoxy group having 1 to 6 carbon atoms or a phenyl group and R.sub.4 is a hydrogen or a straight or branched lower alkyl group having 1 to 6 carbon atoms; and A.sub.2 represents a straight or branched lower alkyl group having 1 to 6 carbon atoms or a straight or branched lower alkyl group having 1 to 6 carbon atoms which is substituted with one or two carboxyl groups, are useful as antibacterial agents.

Abstract: .beta.-Lactam antibiotics having an .alpha.-formamido substituent on the carbon atom adjacent to the carbonyl group of the .beta.-lactam ring and in particular bicyclic compounds having the partial structure: ##STR1## Intermediates and processes for the preparation of the compounds are further disclosed.