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: Antibacterially effective cephalosporins of the formula ##STR1## in which R.sup.1 denotes C.sub.1 -C.sub.6 -alkyl, phenyl or halogen-substituted phenyl andA represents a nitrogen-containing, positively charged heterocyclic 5-membered to 7-membered ring which is bonded via N and can contain a total of up to 4 hetero-atoms from the group comprising N, O and S, and onto which up to two further rings can be fused, and which can optionally be substituted, with the proviso that, if the ring is a 6-membered ring, A does not represent an unsubstituted pyridine ring or a pyridine ring which is mono- or di-substituted by identical or different substituents from the group comprising C.sub.1 -C.sub.4 -alkyl, chlorine, bromine, carbamoyl or N--C.sub.1 -C.sub.4 -alkylcarbamoyl,or pharmaceutically acceptable salts thereof or esters thereof which can be split under physiological conditions.

Abstract: Novel lysine esters used as absorption enhancing agents for gastrointestinally and rectally administered drugs. Also provided are processes for preparation of said lysine ester compounds as well as pharmaceutical formulations and methods for their use as absorption enhancing agents.

Abstract: Cephalosporin compounds substituted in the 7-position by a 2-(5- or 6-membered heterocyclic)-2-oximinoacetylamino group and in the 3-position with an imidazolo, oxazolo or thiazolopyridinium-methyl group are broad spectrum antibiotics highly effective in combating bacterial infections of gram-negative and gram-positive microorganisms. The cephalosporins are best prepared by reacting a silylated 7-[2-(heterocyclic)-2-oximinoacetylamino-3-iodomethyl-3-cephem-4-carboxyli c acid with an imidazolopyridine, an oxazolopyridine or a thiazolopyridine. Pharmaceutical formulations comprising a compound of the invention and a method for treating bacterial infections comprising their use are also provided.

Abstract: An antibacterial 7beta-(carboxyalkenoyl)amino-3-cephem-4-carboxylic acid represented by the following formula: ##STR1## (wherein R is aryl or a heterocyclic group; R.sup.1 is hydrogen or halogen;R.sup.2 is a single bond, alkylene, or thiaalkylene;R.sup.3 is a hydrogen atom or carboxy modifying group;R.sup.4 is hydrogen or methoxy;R.sup.5 is hydrogen or a 3-substituent of cephalosporins;R.sup.6 is a hydrogen atom or carboxy modifying group; andX is oxygen, sulfur, or sulfinyl)a pharmaceutical composition containing the same, and a method for treating a bacterial infection with the same.

Abstract: Antibacterially active and animal growth-promoting novel .beta.-lactam compounds of the formula ##STR1## in which R.sup.1 represents the radical ##STR2## Y representing N or CR.sup.9, or Y--R.sup.7 representing >C.dbd.O or >C.dbd.N--R.sup.7,Z representing O, S, or NR.sup.10, andR.sup.2 represents hydrogen or a protective group.

Abstract: Antibiotically active penicillins and cephalosporins of the formula ##STR1## in which Z is hydrogen or lower alkoxy,n is 1 or 2,Y, in the form of the free acid, is ##STR2## X is --S--, --n--, --SO-- or --SO.sub.2 --, T is an organic radical, hydrogen or halogen,A is hydroxyl, optionally substituted alkyl, a substituted or unsubstituted phenyl ring, an optionally substituted polycyclic aromatic ring, an optionally substituted 5-membered or 6-membered heterocyclic ring with nitrogen, oxygen and/or sulphur as hetero atoms in the ring, or an optionally substituted polycyclic heterocyclic ring,or non-toxic pharmaceutically tolerated salts thereof.

Abstract: Antibacterially active and animal growth-regulating novel .beta.-lactam compounds of the formula ##STR1## in which R.sup.1 represents an optionally substituted radical of the formula ##STR2## Z represents oxygen, sulphur or --N--R.sup.

Abstract: Acylcarnitine used as a nasal, buccal, sublingual and vaginal drug absorption enhancing vehicle for poorly absorbed drugs.

Abstract: Choline ester salts are used as drug absorption enhancing agents for orally and rectally administered drugs.

Abstract: 7-Amino-3-(3-formamidopyridinium)methyl-3-cephem-4-carboxylate of the formula ##STR1## is produced by (a) reacting a compound of the formula ##STR2## in which R.sup.3 is a phenacetyl or a thienylacetyl group,with 3-formamidopyridine to give the compound of the formula ##STR3## and (b) splitting off the R.sup.3 radical. The product can then be coupled to a suitable acid to produce a cephalosporin and the formyl radical may be split off.

Abstract: Choline esters are used as drug absorption enhancing agents for drugs which are poorly absorbed from the nasal, oral, and vaginal cavities.

Abstract: Cephalosporin compounds substituted in the 7-position by a 2-(5- or 6-membered heterocyclic)-2-oximinoacetylamino group and in the 3-position with an imidazolo, oxazolo or thiazolopyridinium-methyl group are broad spectrum antibiotics highly effective in combating bacterial infections of gram-negative and gram-positive microorganisms. The cephalosporins are best prepared by reacting a silylated 7-[2-(heterocyclic)-2-oximinoacetylamino]-3-iodomethyl-3-cephem-4-carboxyl ic acid with an imidazolopyridine, and oxazolopyridine or a thiazolopyridine. Pharmaceutical formulations comprising a compound of the invention and a method for treating bacterial infections comprising their use are also provided.

Abstract: 7.alpha.-Hydroxyamino-7.beta.-[2-substituted-2-(acylamino)acetamido]cephalo sporin antibiotics, pharmaceutically-acceptable salts and in vivo hydrolyzable esters thereof, a method of treating susceptible infections therewith, and intermediates therefor.

Abstract: A cephalosporin derivative of the formula I: ##STR1## in which X is S, O, CH.sub.2 or SO, R1 is (optionally-substituted)imidazol-2-yl or one of the C-7 acyl groups known in the cephalosporin art, R2 is hydrogen or methoxy, R3 is carboxy or a biodegradable ester thereof and --R4 is of the formula XII, XIII or XIV: ##STR2## in which R32-R40 inclusive are as defined in the specification; and the salts thereof. Pharmaceutical compositions, methods of manufacture and intermediates are also described.

Abstract: The (5-R-2-oxo-1,3-dioxolen-4-yl)methyl moiety: ##STR1## wherein R is loweralkyl of 1-6 carbon atoms, especially methyl or t-butyl; when utilized as an ester on a pharmaceutical having a carboxylic acid functionality, enhances oral absorption of the pharmaceutical. This effect is applicable to a broad range of pharmaceutically active substances, including antibiotics, and antihypertensives as well as other classes of therapeutic agents.

Abstract: The invention relates to cephem derivatives of the general formula I ##STR1## and their physiologically acceptable acid addition salts, to pharmaceutical formulations active against bacterial infections, to processes for preparing the compounds and formulations, and to the use of the compounds for combating bacterial infections.

Abstract: An antibacterial 7beta-(carboxyalkenoyl)amino-3-cephem-4-carboxylic acid represented by the following formula: ##STR1## (wherein R is aryl or a heterocyclic group;R.sup.1 is hydrogen or halogen;R.sup.2 is a single bond, alkylene, or thiaalkylene;R.sup.3 is a hydrogen atom or carboxy modifying group;R.sup.4 is hydrogen or methoxy;R.sup.5 is hydrogen or a 3-substituent of cephalosporins;R.sup.6 is a hydrogen atom or carboxy modifying group; andX is oxygen, sulfur, or sulfinyl)a pharmaceutical composition containing the same, and a method for treating a bacterial infection with the same.

Abstract: Novel antibacterially active cephalosporins of the formula ##STR1## in which R.sup.1 denotes hydrogen, optionally substituted alkyl, a substituted or unsubstituted phenyl ring, a polycyclic aromatic ring or an optionally substituted heterocyclic 5- or 6-member ring having 1-4 heteroatoms,R.sup.2 represents hydrogen, C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -alkenyl, halogen, C.sub.1 -C.sub.4 -alkoxy, C.sub.1 -C.sub.4 -alkylthio, hydroxymethyl, formyloxymethyl, C.sub.1 -C.sub.4 -alkylcarbonyloxymethyl, aminocarbonyloxymethyl, pyridiniummethyl, 4-carbamoylpyridiniummethyl, 4-sulphonylethylpyridiniummethyl, 4-carboxylmethylpyridiniummethyl or heterocyclylthiomethyl, heterocyclyl representing a radical of the formula ##STR2## wherein R.sup.8 denotes hydrogen, methyl, 2-dimethylaminoethyl, carboxymethyl, sulphomethyl, carboxyethyl or sulphoethyl andR.sup.9 denotes hydrogen or methyl,or pharmaceutically tolerated salts or esters thereof.

Abstract: Ceftazidime pentahydrate is formulated with a pharmaceutically acceptable base and amorphous lactose to provide stabilized pharmaceutically acceptable formulations.

Abstract: Anhydrous crystalline (6R,7R)-7-[(Z)-2-(2-aminothiazol-4-yl)-2-(2-carboxyprop-2-oximino)acetamid o]-3-(1-pyridiniummethyl)-3-cephem-4-carboxylate and a process for its preparation, a pharmaceutical formulation which is active against bacterial infections and contains this compound and a process for the preparation of the formulation and the use of this compound for controlling bacterial infections.

Abstract: A cephalosporin compound of the formula: ##STR1## wherein R.sup.1 is hydrogen or lower alkyl;R.sup.2 is acetoxy or (1-methyl-1H-tetrazol-5-yl)thio, andR.sup.3 is carboxy; orR.sup.2 is a group of the formula: ##STR2## R.sup.3 is --COO.sup.- and Y is hydrogen, hydroxymethyl or carbamoyl; andn is an integer of 2 or 3,or a pharmaceutically acceptable salt thereof and processes for their preparation are disclosed. Said cephalosporin compound is useful as an antimicrobial agent.

Abstract: A solid pharmaceutical composition comprising one or more .beta.-lactam antibiotics in acid or amphoteric form in association with at least one physiologically acceptable base in the presence of a gaseous atmosphere containing a stabilizing amount of carbon dioxide at a concentration greater than that of atmospheric air. The compositions exhibit enhanced stability. A preferred antibiotic for the compositions is ceftazidime or a hydrate thereof, and a preferred base is sodium carbonate or a mixture thereof with one or more other bases.

Abstract: The invention relates to the novel compound (6R,7R)-7-(D-5-benzamido-5-carboxypentanamido)-3-(1-pyridiniummethyl)-ceph -3-em-4-carboxylate and salts thereof, which may be prepared in substantially pure form. The novel compounds are useful for the preparation of (6R,7R)-7-amino-3-(1-pyridiniummethyl)ceph-3-em-4-carboxylate or salts thereof, which are themselves useful for the preparation of 7-substituted 3-pyridiniummethyl cephalosporin antibiotics such as ceftazidime and cephaloridine.

Abstract: The invention relates to novel cephem compounds of high antimicrobial activity of the formula: ##STR1## wherein R.sup.1 is phosphono, dihalophosphoryl, di(lower) alkoxyphosphoryl, O-lower alkylphosphono, diaminophosphoryl, (anino) (hydroxy) phosphoryl or (lower alkoxy) (morpholino) phosphoryl,R.sup.2 is lower alkyl or lower alkenyl,R.sup.3 is a group of the formula: ##STR2## wherein X is hydrogen, halogen or lower alkoxy, or a group of the formula: ##STR3## wherein R.sup.4 is lower alkyl, and Y is N or CH; and pharmaceutically acceptable salts thereof.

Abstract: A compound of formula (1) or a pharmaceutically acceptable salt or in vivo hydrolysable ester thereof: ##STR1## wherein R.sup.1 is phenyl, substituted phenyl or a 5- or 6-membered heterocyclic ring containing up to three heteroatoms selected from oxygen, sulphur or nitrogen, optionally substituted with hydroxy, amino, halogen or C.sub.1-6 alkoxy;X represents; ##STR2## wherein R.sup.Y is methyl or acetyl; R.sup.2 and R.sup.3 may be the same or different and each is hydrogen, an aryl group, a heterocyclyl group or a C.sub.1-6 alkyl group optionally substituted by an aryl group or a heterocyclyl group; and R.sup.4 is hydrogen, a C.sub.1-6 alkylcarbonyl group, an aryl group, a heterocyclyl group, a C.sub.1-6 alkyl group optionally substituted by an aryl group or a heterocyclyl group;R.sup.5 represents, hydrogen, methoxy or --NHCHO; and Y is: ##STR3## wherein Y.sup.1 is oxygen, sulphur or --CH.sub.2 -- and Z represents hydrogen, halogen or an organic group such as C.sub.1-4 alkoxy, --CH.sub.2 Q or --CH.dbd.

Abstract: The invention relates to cephem compounds of high antimicrobial activity, of the formula: ##STR1## wherein R.sup.1 is amino or a protected amino group;R.sup.2 is lower alkyl which may be substituted with one carboxy, lower alkenyl, lower alkynyl, cyclo (lower) alkyl or cyclo (lower) alkenyl;R.sup.3 is lower alkylamino, N-(lower) alkanoyl (lower) alkylamino, di (lower) alkylamino, sulfo (lower) alkylamino, hydroxy (lower) alkylamino, N-(lower) alkanoylhydroxy (lower) alkylamino, alkanoyloxy (lower) alkyl, alkenoyloxy (lower) alkyl, lower alkoxy (lower) alkoxy (lower) alkyl, di (lower) alkylamino (lower) alkyl, lower alkylthio (lower) alkyl, lower alkylthio, lower alkoxy, lower alkoxy (lower) alkoxy, hydroxy (lower) alkoxy, lower alkanesulfonyl (lower) alkyl, hydroxy (lower) alkylthio, di (lower) alkylamino (lower) alkylthio, tetrazolyl, tetrazolylthio, tetrazolylthio (lower) alkyl or dihydrotriazinylthio (lower) alkyl substituted with oxo, hydroxy and lower alkyl; andR.sup.

Abstract: A 3-.beta.-(vic-dihydroxyphenylmethyleneamino-2-oxo-imidazolidine)- or 3-.beta.-(vic-dihydroxyphenyl-methyleneamino-2,3-dioxo-piperazine)-1-carbo nylamino-acetamidoazetidin-2-one having an acidic grouping on .sub.1 N, e.g. of the formula ##STR1## The compounds are antibiotically active, especially against Pseudomonas bacteria and can be used in combating bacterial infection, as a preservative and as a growth promoting agent in animal feeds.

Abstract: Cephalosporin derivatives of the formula: ##STR1## in which A is a single bond or a radical --CH.sub.2 --, --NH-- or --NHCO--, attached to the 3-position or 4-position of the pyridinio radical, R is a methyl, carboxymethyl, carbamoylmethyl, benzyl or allyl radical, R.sub.a, R.sub.b and R.sub.c are hydrogen atoms, or alternatively R.sub.a is carboxyl and R.sub.b and R.sub.c, which are identical or different, are hydrogen atoms or alkyl radicals, or together form an alkylene radical, and n equals 0 or 1, in their syn form, and also their addition salts with acids, metal salts and addition salts with nitrogen-containing bases are antibacterial agents having a broad spectrum of activity.

Abstract: An antibacterial cephalosporin derivative of the formula I: ##STR1## in which X.sup.1 is sulphinyl; R.sup.1 is any one of the C-3 substituents from antibacterially-active cephalosporins known in the art; R.sup.2 is any one of the C-4 substituents from antibacterially-active cephalosporins known in the art; R.sup.3 is hydrogen, 1-6C alkoxy or 1-6C alkylthio; X.sup.2 is nitrogen or a radical N.sup..sym. R.sup.5 ; R.sup.4 and R.sup.5 are a variety of radicals described in the specification; --A-- is of the formula II or III: ##STR2## in which R.sup.6, R.sup.7, R.sup.8, R.sup.9, R.sup.10 and R.sup.11 are a variety of substituents described in the specification; and the pharmaceutically-acceptable acid- and base-addition salts thereof. Pharmaceutical compositions and manufacturing processes are also described.

Abstract: Cephalosporin antibiotics of general formula ##STR1## (wherein Y.sup..sym. represents a C-attached 1-C.sub.1-4 alkylpyridinium group) exhibit broad spectrum antibiotic activity with unusually high activity against strains of Pseudomonas organisms as well as high activity against various members of the Enterobacteriaceae. The invention also includes the non-toxic salts, non-toxic metabolically labile esters and 1-oxides of compounds of formula (I). Also described are compositions containing the antibiotics of the invention and processes for the preparation of the antibiotics.

Abstract: Cephalosporin compounds substituted in the 7-position by a 2-(5- or 6-membered heterocyclic)-2-oximinoacetylamino group and in the 3-position with a thienopyridinium methyl group or a furopyridinium methyl group are broad spectrum antibiotics highly effective in combating bacterial infections of gram-negative and gram-positive microorganisms. The cephalosporins are best prepared by reacting a silylated 7-[2-(heterocyclic)-2-oximinoacetylamino-3-iodomethyl-3-cephem-4-carboxyli c acid with the thienopyridine or the furopyridine. Pharmaceutical formulations comprising a compound of the invention and a method for treating bacterial infections comprising their use are also provided.