Abstract: There are provided cephalosporin and penicillin carboxylic acid derivatives which comprise polymers carrying a plurality of molecules of said acid, the carboxyl groups of which are blocked by attachment to the polymer, principally by forming ester linkages to aliphatic carbon atoms in the polymer. There are also provided methods of immobilizing cephalosporin and penicillin acids on polymers and of carrying out chemical reactions to modify said acids.

Abstract: The invention provides novel antibiotic compounds which are 7.beta.-acylamidoceph-3-em-4-carboxylic acids, and non-toxic derivatives thereof characterized in that the acylamido group has the structure ##STR1## where R is a hydrogen atom or an organic group and R.sup.a is an etherifying monovalent organic group linked to the oxygen atom through a carbon atom. The compounds are syn isomers or exist as mixtures containing at least 75% of the syn isomer. These antibiotic compounds possess high antibacterial activity against a range of gram positive and gram negative organisms coupled with particularly high stability to .beta.-lactamases produced by various gram negative organisms. The invention is also concerned with the administration of the compounds.

Abstract: Compounds of the general formula: ##STR1## wherein the groups CHR.sup.1 NR.sup.2 R.sup.3 and CHR.sup.4 NR.sup.5 R.sup.6 may be the same or different and where the group CHR.sup.4 NR.sup.5 R.sup.6 is in either the 1 or the 3 position and R.sup.1 and R.sup.4 independently represent a hydrogen atom or an aryl group;R.sup.2, r.sup.3, r.sup.5 and R.sup.6 which may be the same or different are each a hydrogen atom or an alkyl group or an aryl group both of which may in turn be substituted by one or more hydroxy, alkoxy, acyloxy, dialkylamino or aryl groups or the groups --NR.sup.2 R.sup.3 and/or NR.sup.5 R.sup.6 represent a heterocyclic ring containing one or more hetero atoms and which ring may optionally be substituted by an alkyl, aryl or aralkyl group and in which either aromatic ring of the naphthalene nucleus may be further substituted; with the proviso that when R.sup.1, R.sup.4, R.sup.2 and R.sup.5 are hydrogen, then R.sup.3 and R.sup.

Abstract: N-blocked amino acids, particularly derived from natural sources such as fermentation liquors, are extractively esterified from aqueous media by treatment of the aqueous solution with a diazoalkane, e.g. diphenyldiazomethane, in the presence of a water-immiscible organic solvent. Useful applications of the process include the extractive esterification of N-blocked derivatives of cephalosporin C and desacetyl cephalosporin C from fermentation broths.

Abstract: Novel polymers are provided which carry diazomethylene or hydrazonomethylene groups. Such polymers are of especial use in immobilizing carboxylic acids, such as amino acids, with a view to subsequent chemical transformation of such acids, e.g. peptide synthesis. Alcohols and thiols may also be immobilized using the new polymers. Methods for the preparation of the polymers are provided, starting from a variety of polymer types.

Abstract: The invention provides novel antibiotic compounds which are 7.beta.-acylamidoceph-3-em-4-carboxylic acids, and non-toxic derivatives thereof characterized in that the acylamido group has the structure ##STR1## where R is a hydrogen atom or an organic group and R.sup.a is an etherifying monovalent organic group linked to the oxygen atom through a carbon atom. The compounds are syn isomers or exist as mixtures containing at least 75% of the syn isomer. These antibiotic compounds possess high antibacterial activity against a range of gram positive and gram negative organisms coupled with particularly high stability to .beta.-lactamases produced by various gram negative organisms. The invention is also concerned with the administration of the compounds.

Abstract: The invention provides novel antibiotic compounds which are 7.beta.-acylamidoceph-3-em-4-carboxylic acids, and non-toxic derivatives thereof characterized in that the acylamido group has the structure ##STR1## WHERE R is a hydrogen atom or an organic group and R.sup.a is an etherifying monovalent organic group linked to the oxygen atom through a carbon atom. The compounds are syn isomers or exist as mixtures containing at least 75% of the syn isomer. These antibiotic compounds possess high antibacterial activity against a range of gram positive and gram negative organisms coupled with particularly high stability to .beta.-lactamases produced by various gram negative organisms. The invention is also concerned with the administration of the compounds.

Abstract: The invention provides novel antibiotic compounds which are 7.beta.-acylamidoceph-3-em-4-carboxylic acids, and non-toxic derivatives thereof characterized in that the acylamido group has the structure ##STR1## WHERE R is a hydrogen atom or an organic group and R.sup.a is an etherifying monovalent organic group linked to the oxygen atom through a carbon atom. The compounds are syn isomers or exist as mixtures containing at least 75% of the syn isomer. These antibiotic compounds possess high antibacterial activity against a range of gram positive and gram negative organisms coupled with particularly high stability to .beta.-lactamases produced by various gram negative organisms. The invention is also concerned with the administration of the compounds.

Abstract: The invention provides novel antibiotic compounds which are 7.beta.-acylamidoceph-3-em-4-carboxylic acids, and non-toxic derivatives thereof, and 6.beta.-acylamidopenam-3-carboxylic acids, and non-toxic derivatives thereof, characterized in that the acylamido group has the structure ##STR1## where R is a hydrogen atom or an organic group and R.sup.a is a hydrogen atom or an acyl group. The compounds are syn isomers or exist as mixtures containing at least 75% of the syn isomer. These antibiotic compounds possess high antibacterial activity against a range of gram positive and gram negative organisms coupled with particularly high stability to .beta.-lactamases produced by various gram negative organisms. The invention is also concerned with the administration of the compounds.

Abstract: Cephalosporin antibiotics of formula ##STR1## (where R is thienyl or furyl; R.sup.a and R.sup.b are each selected from hydrogen, C.sub.1-4 alkyl, C.sub.2-4 alkenyl, C.sub.3-7 cycloalkyl, phenyl, naphthyl, thienyl, furyl, carboxy, C.sub.2-5 alkoxycarbonyl and cyano, 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 or cycloalkenylidene group; m and n are each 0 or 1 such that the sum of m and n is 0 or 1; and P is hydrogen or halogen) and their non-toxic derivatives exhibit broad spectrum antibiotic activity characterized by particularly high activity against gram negative microorganisms, including those which produce .beta.-lactamases. The compounds, which are syn isomers or exist as mixtures of syn and anti isomers containing at least 90% of the syn isomer, have particularly high in vitro activity against strains of Escherichia coli, Haemophilus influenzae and Proteus organisms; compounds wherein at least one of R.sup.a and R.sup.

Abstract: Novel 6.beta.-isocyano penicillin and 7.beta.-isocyano cephalosporin esters of value as intermediates in the synthesis of penicillin and cephalosporin antibiotics are provided. The novel compounds may be prepared by reaction of the corresponding 6.beta.-formamido penicillin ester or 7.beta.-formamido cephalosporin ester with an acid halide derived from phosphorus, sulphur or carbon or from an oxygen acid of one of said elements, suitable halides including thionyl chloride or phosgene, or with a trivalent phosphorus compound such as triphenylphosphine and a halogenated hydrocarbon such as carbon tetrachloride. The conversion of the novel products to 6.beta.- and 7.beta.-(.alpha.-hydroxy) arylacetamido penicillins and cephalosporins respectively by reaction under acidic conditions with an aromatic aldehyde followed by treatment with an aqueous medium is also described.

Abstract: .alpha.-(Etherified oximino)carboxylic acids, represented by the formula:- ##STR1## where R is hydrogen or an organic group having 1-20 carbon atoms and R.sup.a is an etherifying monovalent organic group having 1-16 carbon atoms linked to the oxygen atom through a carbon atom, and the corresponding acid chlorides, are useful intermediates in the preparation of highly active, highly .beta.-lactamase-stable 7.beta.-[.alpha.-(etherified oximino)acylamido]-ceph-3-em-4-carboxylic acid antibiotics. The compounds are syn isomers or exist as mixtures of syn and anti isomers containing at least 75% of the syn isomer.

Abstract: The Specification describes a method of systemically treating immunological disorders or inflammatory disorders having a significant immunological component which comprises administering to a subject suffering from such a disorder an initial dosage in the case of a human adult subject of 50 to 500 mg of from more than betamethasone 21-adamantane-1'-carboxylate, dexamethasone 21-adamantane-1'-carboxylate or a corresponding 11-ketone, or in the case of other subjects, an equivalent dosage calculated on the body weight of the subject. The Specification further describes pharmaceutical and veterinary compositions for use in the above method, each dosage unit containing 50 to 500 mg of the 21-adamantane-1'-carboxylate steroid.

Abstract: Novel antibiotic compounds which are 7.beta.-acrylamidoceph-3-em-4-carboxylic acids, and 6.beta.-acrylamidopenam-3-carboxylic acids and non-toxic derivatives thereof wherein the acrylamido group has the structure ##STR1## wherein A is aryl group and B is a substituted or unsubstituted lower alkyl, lower alkenyl or lower alkynyl group; or an aryl, cycloalkyl or cycloalkenyl group. These compounds possess antibacterial activity against gram-positive and gram-negative organisms coupled with stability to .beta.-lactamases. The invention further relates to the administration of the compounds.

Abstract: The invention relates to novel semisynthetic intermediates or relay compounds of use in the production of cephalosporins and related .beta.-lactam antibiotic compounds. The novel compounds are 3-hydroxy- and 3-oxo-7-amino- and blocked amino --(6R,7R)-cephams. Process for the preparation of the novel compounds are described and exemplified.

Abstract: Protection of the amino group of a 7.beta.-aminoceph-4-carboxylic acid or derivative thereof while at least one reaction is being carried out to introduce a desired group at at least one of the positions 1, 2, 3 and 4 by first converting the amino group to a formamido group and then regenerating the amino group after the desired group has been introduced. Novel intermediates may be produced which are compounds of the formula ##STR1## wherein R is C.sub.1 -C.sub.4 alkyl and Z is --O--, --S--, ##STR2## or salts or esters thereof.

Abstract: A process is described for the preparation of aryl .alpha.-keto acids in which the corresponding methyl ketone or aldehyde is oxidized in aqueous solution with an inorganic nitrite salt and hydrochloric or sulfuric acid.

Abstract: There are described new compounds of formula ##STR1## in which E is selected from the group consisting of residues of formula ##STR2## in which R" is selected from the group consisting of amino, vinyl, allyl, ethynyl, C.sub.1 -C.sub.5 alkyl, C.sub.1 -C.sub.5 alkoxy, or C.sub.1 -C.sub.5 alkylthio or a C.sub.1 -C.sub.5 alkyl group susbstituted by at least one halogen atom; and hydrogen; in which R.sup.1 and R.sup.2 are each selected from the group consisting of hydrogen, halogen, methyl and ethyl; and R' is selected from substituted phenyl when R" is other than hydrogen, and phenyl, thienyl and substituted phenyl and thienyl when R" is hydrogen.The compounds are useful in the control of parasites.Certain of the compounds have antimicrobial properties.

Abstract: A bacterial B-amylase from strains of Bacillus circulans producing no .alpha.-amylase can be isolated by simple fractionation techniques and used in the production of maltose, especially high maltose syrups. The enzyme is not inhibited by organomercurials.

Abstract: Cephalosporin antibiotics in which the 7.beta.-acylamido group is syn 2-furyl-2-methoxyiminoacetamido and in which the 3-position substituent is a chloroalkylcarbamoyloxymethyl group exhibit high antibacterial activity against a broad range of gram positive and gram negative organisms, particularly high stability to .beta.-lactamases produced by various organisms, and stability in vivo. The compounds are syn isomers or exist as mixtures of syn and anti isomers containing at least 90% of the syn isomer.