Abstract: An aminothiazolyl- or aminothiadiazolyl-cephalosporin derivative represented by the following general formula (I) which has a condensed-ring thio group as a 3-positioned substituent group that contains a thiazolylthio group, an oxazolylthio group or a heterocyclic ring thereof as one of the ring components. The compound according to the present invention has excellent activities to inhibit growth of various bacteria, especially Gram-positive bacteria including methicillin-resistant Staphylococcus aureus (MRSA), and therefore, the antibacterial agent comprising, as an active ingredient, the inventive compound can be used as a therapeutic drug for the treatment of various bacterial infections.

Abstract: A cephalosporin derivative having a quaternary salt type substituent group at the 3-position, represented by formula (I): ##STR1## wherein X is a carbon atom or a nitrogen atom; Y is a sulfur atom, an oxygen atom or a nitrogen atom substituted with a substituted or unsubstituted lower alkyl group; R.sup.1 is a hydrogen atom, a lower alkyl group or a substituted lower alkyl group; R.sup.2 is a lower alkyl group, a substituted lower alkyl group, a lower alkylene group or a substituted lower alkylene group; and A is an unsaturated six-membered heterocyclic ring containing at least one nitrogen atom, or a pharmaceutically acceptable salt thereof is disclosed. The derivatives have excellent antibacterial activities and can be used as a drug for the treatment of various bacterial infections.

Abstract: As new antibacterial agent are provided cephalosporin derivatives having a general formula (I): ##STR1## wherein R.sup.1 is a hydrogen atom, a lower alkyl group or a substituted lower alkyl group, R.sup.2 is a hydrogen atom or an ester-forming group easily cleavable by an esterase present in the digestive tracts, R.sup.3 and R.sup.4 may be the same and each is independently a hydrogen atom, a halogen atom, a lower alkyl group, a lower alkenyl group, hydroxyl group, amino group or a lower alkoxy group, and a pharmaceutically acceptable salt thereof.The cephalosporin derivative of formula (I) is useful as an orally or injectably administrable cephalosporin derivative which exhibits in combination a high antibacterial activity and a favorable characteristic capable of giving a high concentration of this compound in blood when administered.

Abstract: Novel cephalosporin compounds represented by formula (I): ##STR1## wherein R.sup.1 represents a lower alkyl group which may optionally have a substituent; each of R.sup.2 and R.sup.3 independently represents a hydrogen atom or hydroxy group; and A represents a hydrogen atom or a residue of nucleophilic compound, and pharmacologically acceptable salts or esters thereof exhibit a potent antibacterial activity against gram positive and gram negative bacteria.

Abstract: A novel cephem compound which has antimicrobial activity is disclosed. The cephem compound is represented by the formula: ##STR1## wherein R.sup.1 represents a hydrogen atom or a carboxyl group; R.sup.2 and R.sup.3, which may be the same or different, each represent a hydrogen atom or a lower alkyl group of 1-3 carbon atoms; and R.sup.4 and R.sup.5, which may be the same or different, each represent a hydrogen atom or an acyl group; and pharmaceutically acceptable salts thereof.

Abstract: Cephalosporin compounds of the formula (I): ##STR1## wherein R.sup.1 and R.sup.2 may be the same or different and are a hydrogen atom or a lower alkyl group of 1-5 carbon atoms and A is a hydrogen atom or a nucleophilic compound residue or pharmacologically acceptable salts thereof have excellent antibacterial activity against Gram positive and Gram negative microorganisms.

Abstract: Disclosed is a novel cephem compound which is either one of a cis- or trans-isomer or a mixture of the cis-and trans-isomers, represented by the following general formula (I) and a pharmacologically acceptable salt thereof: ##STR1## wherein all of the substituents are as defined hereinbefore. Also disclosed are a process for producing the above compound and its use as an anti-bacterial agent comprising the same.

Abstract: This is a class of antibacterial compounds of the formula: ##STR1## wherein Y is straight or branched alkyl or alkenyl chain, cycloalkanomethyl of 3-6 carbon atoms, each group being optionally substituted by halogen, or a group ##STR2## wherein n is 0 or an integer of 1-3, A is a group --COR.sup.3 wherein R.sup.3 is hydroxy, a group ##STR3## wherein R.sup.4 and R.sup.5, which may be the same or different, are hydrogen or alkyl of 1-5 carbon atoms, a group ##STR4## or a 5- or 6-membered heterocyclic group containing nitrogen and/or sulfur, and R.sup.1 and R.sup.2, which may be the same or different, are hydrogen, alkyl of 1-5 carbon atoms, or R.sup.1 and R.sup.2 may be combined together to form cycloalkylidene of 3-5 carbon atoms, and Z is a group of the formula: ##STR5## wherein m is 0 or an integer of 3-5, R.sup.6 is hydrogen or alkyl of 1-3 carbon atoms, and R.sup.7, when m is an integer of 3-5, is alkyl of 1-5 carbon atoms, alkenyl, cyclopropyl, a group --(CH.sub.2).sub.

Abstract: Cephalosporin compounds represented by the following formula (I) and pharmaceutically acceptable salts thereof have a broad bactericidal spectrum against various pathogenic bacteria including Psuedomonas aeruginosa and are useful as bactericidal remedies for pathogenic diseases of human and animals: ##STR1## wherein A represents an unsubstituted or substituted pyridylthio group of a formula (I-1); ##STR2## or an unsubstituted or substituted pyridiniumthio group of a formula (I-2): ##STR3## or an unsubstituted or substituted pyridinium group of a formula (I-3); ##STR4## or a 5- or 6-membered heterocyclicthio or bicycloheterocyclicthio group of a formula (I-4):--S--Het (I-4).

Abstract: A 7.alpha.-methoxycephalosporin derivative represented by the formula (I): ##STR1## wherein R.sub.1 represents a heterocyclic ring or an --S-- heterocyclic ring; R.sub.2 represents a hydrogen atom, a carboxy group or a --COOR.sub.5 group wherein R.sub.5 represents a lower alkyl group, a dialkylamino-lower alkyl group or a ##STR2## group wherein R.sub.6 represents a lower alkyl group, a lower acyl group or a lower alkoxycarbonyl group and Y represents a hydrogen atom or a lower alkyl group; R.sub.3 represents a hydrogen atom, a carbamoyl group or a lower acyl group; R.sub.4 represents a hydrogen atom, a lower alkyl group, a dialkylamino-lower alkyl group or a ##STR3## group wherein R.sub.6 and Y are defined as above; A and B, which may be the same or different, each represents a straight chain or branched chain alkylene group having 1 to 5 carbon atoms; and x represents 0 or 1; or a pharmaceutically acceptable salt thereof and a process for producing the same.

Abstract: New antibacterial 1-oxadethiacephalosporin derivatives of the general formula ##STR1## wherein R is a heterocyclic group or a group --S--Het where Het denotes a heterocyclic group, Y is a hydrogen atom or a methoxy group; x and y are each an integer of 1 to 3 is produced by a process comprising condensing a 1-oxacephem compound of the formula ##STR2## wherein R, Y, y are as defined above; R' is a hydrogen atom or a carboxyl-protecting group; and Z is a halo group, with a sulfur-containing amino acid of the formula ##STR3## wherein x is as defined above, in a solvent and removing, if necessary, the residual protective group from the resultant condensation product. The new 1-oxadethiacephalosporin derivatives and the pharmaceutically acceptable salts and esters thereof exhibit high and broad "in vitro" and "in vivo" antibacterial activity, particularly against .beta.-lactamase-producing strains of gram-negative bacteria.

Abstract: A new, efficient process is provided for the production of 7.beta.-[(2D-2-amino-2-carboxy)-ethylthio-acetamido]-7.alpha.-methoxy-3-[( 1-methyl-1H-tetrazole-5-yl) thiomethyl]-3-cephem-4-carboxylic acid useful as new antibacterial agent. This process is economic in using as the starting material the inexpensive, corresponding cephem compound containing no 7.alpha.-methoxy group on the cephem nucleus and comprises 7.alpha.-methoxylation of a protected derivative of the starting cephem compound with t-butyl hypochlorite and lithium methoxide, followed by inactivation of the excessive methoxylation reagents with a trialkyl phosphite and acetic acid to prevent undesired side-reactions such as oxidation of the alkylthioacetyl group of the product, and further by conventional removal of the protecting groups.

Abstract: A chemotherapeutic, antibacterial agent, 7.beta.-[(2D-2-amino-2-carboxy)ethylthioacetamido]-7.alpha.-methoxy-3-[(1- methyl-1H-tetrazole-5-yl)thiomethyl]-3-cephem-4-carboxylic acid is produced economically and efficiently starting from cephamycin A and/or B by a "new route" process comprising the consecutive steps of reaction of cephamycin with 5-mercapto-1-methyl-1H-tetrazole; protection of the terminal amino group thereof by acylation; protection of the two carboxyl groups thereof by esterification; replacement of the acyl group initially having attached to the 7-amino group by a halogenoacetyl group; deprotection of the blocked 4-carboxyl group; and condensation of D-cysteine with the halogenoacetyl group attaching to the 7-amino group.

Abstract: New antibiotics SF-1130-x.sub.1 substance and SF-1130-x.sub.2 substance are produced by cultivating a microorganism Streptomyces myxogenes SF-1130 now deposited under FERM-P. 676 and ATCC. 31305 in a liquid culture medium under aerobic conditions, and these antibiotics may be isolated from the fermentation broth and are useful as an activator for enhancing the host defense system in living animals. The activity of these antibiotics may be improved when used in combination with one or more of maltose, maltotriose, maltotetraose, maltopentaose, maltohexaose and maltoheptaose.

Abstract: Maltopentaose and maltohexaose are produced with commercial advantage by cultivation of Streptomyces myxogenes SF-1130 strain under aerobic conditions in an appropriate culture medium and recovery from the resultant culture.

Abstract: As new compounds are provided 9,3",4"-trialkanoyl SF-837 M.sub.1 substances which have therapeutically useful antibacterial activity and do not show any objectionable long-lasting bitter taste upon its oral administration. These 9,3",4"-trialkanoyl SF-837 M.sub.1 substances may be prepared from SF-837 substance, 9,2',3"-tri-acetyl SF-837 M.sub.1 substance, 9,2'-di-acetyl SF-837 substance, 9-propionyl SF-837 substance or 9,2'-dipropionyl SF-837 substance by acylating the latter with an alkanoic acid anhydride at 50.degree.-120.degree. C to produce the corresponding 9,2',3",4"-tetra-alkanoyl SF-837 M.sub.1 substance and occasionally the 9,18,2',3",4"-penta-alkanoyl SF-837 M.sub.1 substance, with involving the shift of the 4"-alkanoyl group to the 3"-hydroxyl group. Partial and selective hydrolysis of the 9,2',3",4"-tetra-alkanoyl SF-837 M.sub.1 substance and/or the 9,18,2',3",4"-penta-alkanoyl SF-837 M.sub.1 substance so produced gives the desired 9,3",4"-tri-alkanoyl SF-837 M.sub.1 substance.

Abstract: A 9-O-alkanoyl-3"-O-alkanoyloxymethyl-SF-837 substance is now synthetized, which is a new compound useful in that this new 9-O-alkanoyl-3"-O-alkanoyloxymethyl derivative of the SF-837 substance exhibits an antibacterial activity comparable to that of the parent SF-837 substance but is advantageously free from the unpleasant bitter taste inherent to the SF-837 substance and is hence adapted for oral administration. A process of producing the 9-O-alkanoyl-3"-O-alkanoyloxymethyl-SF-837 substance is also provided, which comprises hydrolysing partially and selectively a 9,2'-di-O-alkanoyl-3"-O-alkanoyloxymethyl-SF-837 substance in an aqueous alkanol or aqueous acetone. The 9,2'-di-O-alkanoyl-3"-O-alkanopyloxymethyl-SF-837 substance may be prepared by reacting a 9,2'-di-alkanoyl- or O-mono-O-alkanoyl-3"-O-thiomethoxymethyl-SF-837 substance with an alkanoic anhydride which is exemplified by acetic anhydride or propionic anhydride in the specification.