Abstract: 7-Acylamido-2-halomethylidene-3-methyl and 3-acetoxymethyl-3-cephem-4-carboxylic acids and esters are prepared via reaction of the corresponding 2-exomethylene-3-cephem ester sulfoxides with chloro (or bromo) dimethyliminium chlorides (or bromides). The 2-halomethylidene derivatives are useful as antimicrobial agents and intermediates to novel 2-acyloxy-methylidene cephalosporins and to the known 2-aryl (or alkyl) mercaptomethylidene cephalosporins.

Abstract: 7.alpha.-(Dimethylamidino)-3-cephem ester 1.alpha.-oxides represented by the formula ##STR1## wherein R is hydrogen or acetoxy and R.sub.1 is a carboxy protecting group, are prepared via DBU epimerization of the corresponding 7.beta.-isomer. When R is hydrogen the intermediates are useful in the preparation of the 7.beta.-acylamino-7.alpha.-methoxy-1-oxa-.beta.-lactam antibiotics, and when R is acetoxy the compounds are intermediates to 7.beta.-acylamino-7.alpha.-methoxy-3-exomethylenecepham compounds.

Abstract: 7-Acylamido-2-halomethylidene-3-methyl and 3-acetoxymethyl-3-cephem-4-carboxylic acids and esters are prepared via reaction of the corresponding 2-exomethylene-3-cephem ester sulfoxides with chloro (or bromo) dimethyliminium chlorides (or bromides). The 2-halomethylidene derivatives are useful as antimicrobial agents and intermediates to novel 2-acyloxymethylidene cephalosporins and to the known 2-aryl (or alkyl) mercaptomethylidene cephalosporins.

Abstract: Compounds of the formula ##STR1## in which R is hydrogen or an acyl group, R.sub.1 is hydrogen or lower alkyl, and R.sub.2 is hydrogen, an alkali metal cation, or a readily removable ester forming group, are active antibiotics or intermediates thereto.

Abstract: 6.beta.-acylaminopenicillin-1.beta.-sulfoxides are epimerized to 6.alpha.-acylaminopenicillin-1.beta.-sulfoxides using triethylamine and chlorotrimethylsilane. The 6.alpha.-acylaminopenicillin-1.beta.-sulfoxides produced in this process are useful intermediates in the synthesis of 7.beta.-acylamino-7.alpha.-alkoxy-3-methyl 1-oxa .beta.-lactam acids, a class of 1-oxa .beta.-lactam antibiotics.

Abstract: Cephalosporin antibiotics of the formula ##STR1## wherein R is cyclohexadienyl, phenyl or substituted phenyl, 2-thienyl, 3-thienyl, 2-furyl or 3-furyl; R.sub.1 is a substituted phenyl having 1 to 4 hydroxy substituents or 1 to 3 amino substituents; and wherein Q is halo, methoxy, methyl or a group of the formula --CH.sub.2 R.sub.2 wherein R.sub.2 is alkanoyloxy, carbamoyloxy, alkoxy, halo, pyridinium or substituted pyridinium or a group of the formula --SR.sub.3 wherein R.sub.3 is alkyl, phenyl, substituted phenyl or a 5 or 6 membered-heteroaryl group having from 1 to 4 heteroatoms selected from the group consisting of O, S, and N;are highly active broad spectrum antibiotics especially useful in the treatment of infections attributable to the gram-negative microorganisms.

Abstract: 6-Epi penicillin .alpha.-sulfoxides represented by the formula ##STR1## wherein R is a carboxy protecting group, are useful for preparing antibiotic compounds and are prepared via epimerization with an alkali metal acetate of corresponding 6.beta.-epimer.

Abstract: The present invention provides novel 5-hydroxyfurochromones, which are useful as antiatherosclerotic agents.

Abstract: The present invention provides novel 7-methyl-6-methylthiomethylsulfinyl-, and methylsulfonylmethylfurochromones, which are useful as antiatherosclerotic agents.

Abstract: The present invention provides novel halofurochromones, which are useful as antiatherosclerotic agents.

Abstract: 7-(2,5-Dichloro or 3,4-dichlorophenyl) cephalosporanic acids or derivatives thereof in which the acetoxy group is replaced by hydroxyl or certain heterocyclic thio groups are useful in the treatment of infections caused by Streptococcus faecalis.

Abstract: The administration of 25-hydroxycholecalciferol, 24,25-dihydroxycholecalciferol, 25,26-dihydroxycholecalciferol, 1,25-dihydroxycholecalciferol, 25-hydroxydihydrotachysterol.sub.3, 25-hydroxyergocalciferol, 1-.alpha.-hydroxycholecalciferol, and their acylates to hens increases the thickness of the egg shells. Compositions and methods are provided.

Abstract: The present specification describes a medicated device adapted for a single and rate-controlled rectal or vaginal administration to a mammal of a systemically active pharmaceutical (SAP). The device accomplishes drug administration at an essentially time-independent rate of dosage. Further, the device advantageously results in the substantial exhaustion of the SAP from the device at the conclusion of the single, acute use. The device comprises three elements:(A) an inert resilient support means contoured for easy vaginal or rectal insertion;(B) a first flexible polymer film layer affixed to the support means and containing the SAP dispersed therethrough, this first polymer film not being rate limiting as to the release of drug from the device; and(C) a second polymer film, laminated onto the first polymer film and providing a release rate therefrom of prostaglandin, which is rate limiting both as to the release of prostaglandin from the device and absorption rate by the rectal or vaginal tissues.

Abstract: Broad spectrum .beta.-lactam antibiotics represented by the formula ##STR1## wherein R is the residue of a carboxylic acid, R.sub.2 is H or OCH.sub.3, and R.sub.4 is hydrogen or C.sub.1 -C.sub.3 alkyl; are obtained by reacting a 7-acylamino-3-halomethyl-1-oxa-.beta.-lactam ester with the desired 1- or 2-tetrazolemethyl substituted 1H or 2H tetrazole-5-thiol. Alternatively, a 7-amino-3-halo-methyl-1-oxa-.beta.-lactam ester is first reacted with the bis-tetrazole thiol and then the product is N-acylated with the desired carboxylic acid.

Abstract: The present invention provides novel benzo[1,2-b:5,4-b']difuran-3(2H)-ones, which are useful as antiatherosclerotic agents.

Abstract: Aryl 4R[1-(2-N-3-methyl-4-al-Z-but-2-ene-oate)-2-oxo-3S-acylamino azetidinone]disulfides are prepared by reacting the corresponding 7.alpha.-acylamino-2.alpha.-alkoxy-3-methyl-3-cephem-4-carboxylates first with either phenylsulfenyl chloride or a monosubstituted-phenylsulfenyl chloride where the substituent is either chloro, methoxy, methyl or acetoxy. The disulfide compounds produced in this invention are intermediates in the synthesis of the 7.beta.-acylamino-7.alpha.-alkoxy-3-methyl 1-oxa .beta.-lactam acids, a class of antibiotic compounds.

Abstract: There is described a process for preparing an enamine of formula (IX): ##STR1## where R.sup.2 is a carboxylic acid protecting group and R.sup.3 is the residue of a carboxylic acid derived acyl group and where R.sup.5 and R.sup.6 are the same or different C.sub.1-4 alkyl or C.sub.7-10 aralkyl groups; or taken together with the adjacent nitrogen atom form a heterocyclic ring containing from 4 to 8 carbon atoms and optionally a further heteroatom selected from oxygen and nitrogen; by reacting a compound of formula (XII): ##STR2## with an amine of formula HNR.sup.5 R.sup.6, the reactant of formula (XII) being prepared by reaction of an appropriate enol derivative with a phosphorus reagent. The enamines of formula (IX) are useful in the preparation of 3-hydroxycephalosporins.

Abstract: Bicyclic 1-oxa-.beta.-lactam diacid antibiotics represented by the formula ##STR1## wherein R is phenyl, hydroxyphenyl, acetoxyphenyl, alkylphenyl, or halophenyl, thienyl or furyl; R.degree. is H or OCH.sub.3 ; and the pharmaceutically acceptable non-toxic salts thereof are broad spectrum antibiotics useful for controlling infections in man and animals. The compounds are prepared by reacting the corresponding 3-halomethyl diester with 1-cyanomethyl-1H-tetrazole -5-thiol followed by deesterification.

Abstract: 7-Acylamino-2-halomethylidene-3-methyl and 3-acetoxymethyl-3-cephem-4-carboxylic acids and esters are prepared via reaction of the corresponding 2-exomethylene-3-cephem ester sulfoxides with chloro (or bromo) dimethyliminium chlorides (or bromides). The 2-halomethylidene derivatives are useful as antimicrobial agents and intermediates to novel 2-acyloxymethylidene cephalosporins and to the known 2-aryl (or alkyl) mercaptomethylidene cephalosporins.

Abstract: Azetidinone alcohol disulfides are synthesized by reduction of the corresponding aldehydes. The azetidinone alcohol disulfides are the substrates for a process which cyclizes these compounds to 1-oxa .beta.-lactam compounds, employing a cyclizing reagent chosen from the class consisting of divalent mercury salts or trivalent phosphine compounds. The 1-oxa .beta.-lactam compounds produced by this process are intermediates in the synthesis of 1-oxa .beta.-lactam antibiotics.