Abstract: The invention relates to novel cephem compounds of high antimicrobial activity of the formula: ##STR1## wherein R.sup.1 is amino or protected amino,R.sup.2 is halogen,R.sup.3 is hydrogen or lower alkyl,R.sup.4 is hydrogen, lower alkyl or lower alkoxy,R.sup.5 is hydrogen, halogen, lower alkyl, lower alkoxy, hydroxymethyl or unsaturated heterocyclicthiomethyl in which the heterocyclic moiety may be substituted with lower alkyl or lower alkenyl, andR.sup.6 is carboxy or functionally modified carboxy, and its pharmaceutically acceptable salt thereof.

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 compound of the formula: ##STR1## wherein R.sub.1 stands for n-propyl or isopropyl; and R.sub.2 stands for n-butyl, isobutyl, n-pentyl, n-hexyl or 2-ethylbutyl, or a pharmaceutically acceptable salt thereof, processes for preparing the same and a pharmaceutical composition thereof are provided. The compound can orally be applied as antibiotics having improved bioavailability.

Abstract: The use of cephem compounds of the general formula I ##STR1## to increase the immunological responsiveness of mammals and formulations which contain an effective content of cephem compounds of the general formula I.

Abstract: Cephalosporin derivatives represented by the general formula ##STR1## Wherein X represents a hydrogen atom, a lower alkyl group having 1 to 4 carbon atoms, an allyl group, a cycloalkyl group having 5 or 6 carbon atoms or a benzyl group, and the non-toxic salts thereof are disclosed. These compounds are useful as antibacterial agents.

Abstract: O-Substituted oximinocephalosporins represented by the formula ##STR1## wherein R is a 5-membered or 6-membered heterocycle, preferably amino-substituted, e.g., 2-aminothiazol-4-yl, R.sub.1 is an arylalkyl, aryloxyalkyl, or arylthioalkyl group, especially substituted benzyl; R.sub.2 is a 1,2,4-triazin-3-yl thio group; and M is a salt or a biologically labile ester group; are potent antibacterial agents. Also provided are antibiotic formulations of said compounds and a method for treating infectious diseases in man or animals comprising the administration of said compounds.

Abstract: The invention relates to novel cephem compounds, of high antimicrobial activity, of the formula ##STR1## wherein R.sup.1 is amino or protected amino,R.sup.2 is lower alkyl substituted with 1 to 3 halogen atoms,R.sup.3 is thiadiazolylthiomethyl which may be substituted with lower alkyl, or tetrazolylthiomethyl which may be substituted with lower alkyl or lower alkenyl, andR.sup.4 is carboxy or protected carboxy, and a pharmaceutically acceptable salt thereof.

Abstract: This application discloses antibacterial cephems of the formula: ##STR1## wherein R.sub.1 represents hydrogen, alkyl, alkenyl, heterocyclylalkyl, or aralkyl; R.sub.3 is a 5- or 6-membered heterocyclic ring selected from: ##STR2## and X is sulfur or oxygen. Included also are pharmaceutically acceptable salts and esters of such compounds; pharmaceutical compositions thereof, and methods of treatment comprising such compositions when an antibiotic effect is needed.

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: Novel cephalosporin compounds of the formula ##STR1## wherein the wavy line means syn-form and anti-form bonds, R.sup.1 represents a cyanomethyl group, a thiocarbamoylmethyl group or an aminothiazolylmethyl group, and A represents a unsubstituted or substituted pyridinio group; and salts thereof. These compounds have excellent antibacterial activities.

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: Disclosed herein are 7-beta-[2-(2-amino-4-thiazolyl)-2-methoxyiminoacetamido]-3-(2-amino-1,3,4- thiadiazolyl-5-thiomethyl)-3-cepheme-4-carboxylic acid, salts thereof and pivaloyloxymethyl ester thereof, and a pharmaceutical composition containing the same as an active ingredient.

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: 7.beta.-[2-(2-Aminothiazol(oxazol)-4-yl)-2-oximinoacetamido]-3-(thiazolium or substituted thiazolium-3-yl)methyl-3-cephem-4-carboxylates and the correspondingly substituted 1-oxadethia and 1-carbadethia 3-cephem compounds are potent antibacterials useful in a therapeutic method for treating bacterial diseases. Also provided are pharmaceutical formulations of these thiazolium-substituted compounds and intermediates useful in the preparation thereof.

Abstract: The compounds according to the invention correspond to the formula: ##STR1## in which: The COOA group at the 4 position is an acid radical, or an alkaline or alkaline-earth salt, or an amino acid or amine salt, for example triethylamine or ethanolamines, or an easily hydrolyzable or metabolically labile and pharmaceutically acceptable ester radical.X denotes an oxygen atom or a sulfur atomn is zero or 1R.sub.1 and R.sub.2 each denote independently hydrogen or a lower alkyl group, preferably a methyl group, orR.sub.1 and R.sub.2 taken together with the carbon atom to which they are linked form a cyclobutyl or cyclopentyl nucleus.B is the residue of a primary or secondary amine.

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: This invention relates to novel compounds of high antimicrobial activity of the formula: ##STR1## wherein R.sup.1 is carboxy(lower)alkyl or protected carboxy(lower)alkyl,R.sup.2 is carboxy or protected carboxy,R.sup.3 is hydrogen or lower alkyl, andR.sup.4 is lower alkyl, lower alkoxy, acyloxymethyl, lower alkylthiomethyl, lower alkoxymethyl, halogen, lower alkenyl or hydrogen,and pharmaceutically acceptable salts thereof,and processes for making the same.

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: 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: Substituted cephalosporin sulfoxides are found to be potent elastase inhibitors and thereby useful anti-inflammatory/antidegenerative agents.

Abstract: Cephalosporin antibiotics of general formula: ##STR1## (wherein R.sup.a and R.sup.b, which may be the same or different, each represent a C.sub.1-4 alkyl group or R.sup.a and R.sup.b together with the carbon atom to which they are attached form a C.sub.3-7 cycloalkylidene group, and Y.sup..sym. represents a C-linked 5- or 6-membered heterocyclic ring containing at least one C.sub.1-4 alkyl-substituted quaternary nitrogen atom, which ring may also contain one or more sulphur atoms) exhibit broad spectrum antibiotic activity, the activity being unusually high against gram-negative organisms such as strains of Pseudomonas organisms.A particular antibiotic compound of formula (I) possessing excellent antibacterial activity against strains of Pseudomonas organisms, as well as other valuable therapeutic properties, is (6R,7R)-7-[(Z)-2-(2-aminothiazol-4-yl)-2-(1-carboxycyclobut-1-oxyimino)ace tamido]-3-[(1-methylpyridinium-4-yl)-thiomethyl]ceph-3-em-4-carboxylate.

Abstract: An antibacterial cephalosporin hydroxamic acid derivative represented by the following formula (I), processes for its preparation, compositions containing the same as an active ingredient, and a method for killing bacteria by contacting with said compound. ##STR1## (wherein, R is acyl; R.sup.1 is hydrogen or methoxy; R.sup.2 is alkylene; R.sup.3 is hydrogen, aliphatic group or a hydroxy-protecting group; R.sup.4 is hydrogen or amino-protecting group; R.sup.5 is hydrogen, light metal atom or carboxy-protecting group; and X is oxygen, sulfur, or sulfinyl).

Abstract: The present invention relates to new cephalosporins of general formula ##STR1## in which R.sub.1 =R.sub.2 =CH.sub.3 or R.sub.1 and R.sub.2 together form a 1,3-propylene group, A is H, a cation, an ester or a hemiacetal, and R.sub.3 is a heterocycle comprising five or six atoms including at least one atom in the ring of nitrogen. It also relates to a process for preparing these cephalosporins and to the drugs containing them.

Abstract: Novel cephem compounds are provided having the formula: ##STR1## wherein R represents lower alkyl, which may be substituted with lower acyloxy, lower alkylthio or certain 5 or 6-membered heterocyclic ring-containing groups. The cephem compounds and salts thereof exhibit antibacterial activity to many pathogens. A process for producing the cephem compounds is also provided.

Abstract: 3-(alkynylalkyloxy)cephalosporin antibiotics and the intermediates therefor are disclosed. Pharmaceutical compositions for the antibiotics are also disclosed.

Abstract: Cephalosporin derivatives effective against gram-negative bacteria and virtually inactive against staphylococci are disclosed. The derivatives have the following general formula: ##STR1## in which R is ##STR2## R" and R"' are hydrogen, lower alkyl or together are 1,3-propylene or 1,4-butylene, andX and X' are hydrogen, cation or easily metabolically labile and pharmaceutically acceptable ester or hemiacetal.

Abstract: What are disclosed are cephalosporin compounds of the formula ##STR1## pharmaceutical preparations which are active against bacterial infections and in which these cephem compounds are present, process for the preparation of the cephem compounds and of the pharmaceutical preparations, use of the cephem compounds for combating bacterial infections, and compounds used as starting materials in the synthesis of said cephem compounds.

Abstract: The present invention relates to cephalosporins of general formula: ##STR1## in which: R.sub.1 is H or CH.sub.3, R.sub.2 is CH.sub.3, or R.sub.1 and R.sub.2 taken together form a 1,3-propylene group,R.sub.3 is lower alkyl, alkenyl, alkynyl or CH.sub.2 COO alkyl,R.sub.4 is H or OH, the S being bonded to the pyridine ring in 2 or 4 position,A is H or cation or ester or hemiacetal which is easily hydrolyzable,and X is a derivative of a mineral or organic acid.The invention also relates to a process for preparing these new cephalosporins and to the drugs containing said cephalosporins.

Abstract: The invention relates to novel compounds of high antimicrobial activity of the formula: ##STR1## wherein R.sup.1 is amino or acylamino; andR.sup.9 is a group of the formula: ##STR2## wherein R.sup.2 is organic group,X is CH or N,Z is acid residueY is CH or N and n is O; orY is N.sup..sym. --R.sup.2 wherein R.sup.2 is as defined above and n is 1,or a group of the formula:--A--N.sup..sym. (R.sup.10).sub.3whereinR.sup.10 is lower alkyl andA is lower alkylene.

Abstract: A cephalosporin derivative of the formula ##STR1## wherein R is a hydrogen atom, a lower alkyl group which may have been substituted or a carbamoyl group which may have been substituted; R.sub.1 is hydrogen atom or a methoxy group; R.sub.2 is a hydrogen atom, an acyloxy group, or a nitrogen-containing 5-membered heterocyclic thio group which may have been substituted; R.sub.3 is a free amino group or an amino group having a protective group; and R.sub.4 is a free carboxy group or a carboxy group having a protective group or the salts thereof.The compound of this invention has an excellent antibacterial activity against gram negative bacteria and gram positive bacteria.

Abstract: The present invention relates to cephalosporins having the formula: ##STR1## in which COOA is an acidic radical, salt or ester, and R.sub.1 represents a group: ##STR2## in which R.sub.A and R.sub.B are H or alkyl or together form a cycloalkyl with the carbon to which they are bonded, R.sub.2 and R.sub.3 are H, alkyl or alkenyl, R.sub.4 and R.sub.5 are H, alkyl or alkenyl or together form a ring to the nitrogen atom with which they are bonded. This invention also relates to a process for the preparation of these compounds and to drugs containing them.

Abstract: A cephalosporin compound of the formula: ##STR1## wherein R.sup.1 is a hydrogen atom, a lower alkyl group, a carboxy(lower)alkyl group, a hydroxy(lower)alkyl group, a carbamoyl(lower)alkyl group, an N-(lower)alkyl-carbamoyl(lower)alkyl group, a cycloalkyl group, a carboxycycloalkyl group, or a tetrazolylmethyl group, R.sup.2 is a hydrogen atom, a lower alkyl group, a formyl group or a lower alkanol group, R.sup.3 is a hydrogen atom, or R.sup.2 and R.sup.3 are combined together to form an aralkylidene group, or a pharmaceutically acceptable salt thereof which is useful as an antimicrobial agent, and process for their preparation.

Abstract: This invention relates to a new cephem compound of the formula: ##STR1## wherein R.sup.1 is amino or a substituted amino group;R.sup.2 is carboxy or a protected carboxy group;R.sup.3 is a tetrazolyl group having a lower alkynyl group; andX is --S-- or ##STR2## and pharmaceutically acceptable salts thereof, of high antimicrobial activity.

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: The invention relates to novel cephem compounds of high antimicrobial activity of the formula: ##STR1## wherein R.sup.1 is amino or lower alkanoylamino,R.sup.2 is lower alkyl, lower alkynyl, carboxy (lower) alkyl or esterified carboxy (lower) alkyl,R.sup.3 is amino or lower alkanoylamino, andX is hydrogen or halogen; 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: 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: An antibacterial composition is provided consisting of a 7-[2-(2-aminothiazol)-4-yl)-2-(syn)-methoxyiminoacetamido]cephalosporin compound of the formula ##STR1## wherein R.sub.2 NH is amino or a protected amino group, n is an integer of 1 to 3 and R is a di-C.sub.1-3 alkylamino, carboxyl or sulfo group, or a pharmaceutically acceptable salt or ester thereof.

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: This invention relates to novel cephem compounds, of antimicrobial activity, of the formula: ##STR1## wherein R.sup.1 is carboxy (C.sub.1 -C.sub.6) alkyl or esterified carboxy (C.sub.1 -C.sub.6) alkyl,R.sup.2 is carboxy or an esterified carboxy group, andR.sup.3 is (C.sub.1 -C.sub.6) alkanoylamino, (C.sub.1 -C.sub.6) alkanesulfonyl, triazolylthio, tetrazolylthio having (C.sub.1 -C.sub.6) alkyl, pyridazinylthio having (C.sub.1 -C.sub.6) alkyl, thiadiazolylthio having (C.sub.1 -C.sub.6) alkyl, triazolopyridazinylthio or tetrazolopyridazinylthio, and pharmaceutically acceptable salts thereof.

Abstract: Cephalosporin derivatives of the formula: ##STR1## wherein R.sub.1 is methyl or ethyl and R.sub.2 is a straight-chain or branched alkyl group of 5 to 7 carbon atoms, and their pharmaceutically acceptable salts, which are effective as orally administrable antibiotic agents against both gram-positive- and negative-bacteria, and the production and compositions thereof, are proposed.

Abstract: New cephalosporin derivatives, of the formula: ##STR1## in which R.sub.1 is a heterocyclic, phenyl, p-hydroxyphenyl, phenoxy or dichlorophenylthio radical and R.sub.2 is a hydrogen atom, or R.sub.1 is phenyl or p-hydroxyphenyl and R.sub.2 is an amino radical, R.sub.3 is hydrogen, phenyl, substituted phenyl, alkylthio or substituted amino or a radical of the structure --A--R'.sub.3, which A is --CH.sub.2 --, --NH-- or --NHCO-- and R'.sub.3 is a substituted pyridinio radical, R is a carboxyl radical or a carboxylato radical if R.sub.3 is a --AR'.sub.3 radical and X is a sulphur or oxygen atom, the said alkyl moieties or radicals containing 1 to 4 carbon atoms each in their D, L and D,L forms, where these exist, and their salts are narrow-spectrum anti-bacterial agents which are active against gram-positive bacteria.