Abstract: Novel syn-7.beta.-(2-aryl-2-hydroxyiminoacetamido)ceph-3-em-4- carboxylic acids carrying a 7.alpha.-lower alkoxy substituent, particularly a 7.alpha.-methoxy group, which are broad spectrum antibiotics exhibiting low serum binding are described.

Abstract: The invention is concerned with the preparation of .DELTA..sup.3 -4-carboxy cephalosporin antibiotics possessing a 3-ethyl or substituted 3-ethyl group by means of phosphorous intermediates.

Abstract: Steroid anaesthetics of the pregnane and 19-norpregnane series are described, the compounds possessing a 3.alpha.-hydroxy group, a 5.alpha.-hydrogen atom or a 4,5-double bond, a 17.alpha.-hydrogen atom, a 20-oxo group and at the 21-position a hydrocarbon group which may be substituted by an oxo, ether, hydroxy, acyloxy, esterified carboxy, thioether, thioester, heterocyclic, amino or aromatic group, or a fluorine or chlorine atom. The acetals and 20-enol ethers of compounds having a 21-formyl group are also described.

Abstract: The invention is concerned with .DELTA..sup.3 -4-carboxy cephalosporin antibiotics possessing a 3-vinyl group and having 2,2-disubstituted acetamido group at the 7-position.

Abstract: Novel semisynthetic .beta.-lactam intermediates of use in the production of cephalosporins, penicillins and related .beta.-lactam antibiotic compounds are provided. The novel compounds are prepared from .beta.-lactams obtained by cleavage of the 1,2-sulphur-carbon bond of a penicillin 1-oxide (with subsequent internal or external trapping of the sulphur atom to leave a residual substituent as the .beta.-lactam nitrogen) by removal of the said residual substituent by an oxidative cleavage reaction.

Abstract: The invention provides novel antibiotic compounds which are 6.beta.-acylamidopenam-3-carboxylic acids and non-toxic derivatives thereof, characterized in that the acylamido group has the structure ##EQU1## 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: 1,2,4-Oxadiazoles having as 3- and 5-substituents a hydrogen atom, an aliphatic, cycloaliphatic, araliphatic, aryl or heterocyclic group, or a carbamoyl group of the formula -- CONR.sup.1 R.sup.2 where R.sup.1 & R.sup.2 which can be the same or different, are hydrogen atoms or aliphatic, cycloaliphatic, araliphatic or aryl groups or, taken with the N atom, a heterocvolic ring; provided that at least one of the 3- or 5-substituents is an N-substituted carbamoyl group. Antimicrobial activity, and particularly antiviral, antiparasitic and antibacterial activity is shown in this group. The corresponding oxadiazolins are also described and are useful intermediates in the preparation of the oxadiazoles.

Abstract: Anaesthetic steroids of the androstane and 19-norandrostane series are described, the steroids possessing a 3.alpha.-hydroxy group, a 17.alpha.-hydrogen atom and at the 17.beta.-position a --COSH or esterified --COSH group.

Abstract: Steroid anaesthetics of the pregnane and 19-norpregnane series are described, the steroids having a 3.alpha.-hydroxy group, a 17.alpha.-hydrogen atom, a 20-oxo group and at the 21-position a cyano, azido or basic amino group.

Abstract: The specification describes new anti-inflammatory steroids having the formula ##SPC1##Wherein R.sup.1 represents a C.sub.1-4 alkyl or halo- C.sub.1-4 alkyl group, R.sup.2 represents a methyl, ethyl, n-propyl or iso-propyl group (an ethyl group being especially preferred), X represents a hydrogen, chlorine or fluorine atom and -- represents a single or double bond.The specification describes processes for the preparation of such compounds as well as pharmaceutical compositions containing these compounds.

Abstract: A process for the production of an ester of one enantiomer of an .alpha.-amino acid in the form of a salt with an optically active acid, which comprises reacting an ester of the opposite enantiomer of said .alpha.-amino acid (which may be in admixture with an ester of the desired enantiomer) with said optically active acid and an aldehyde or ketone, whereby an ester of the desired enantiomer separates out in the form of the said salt. The free .alpha.-amino acid and/or its salts may be obtained by hydrolysis of the ester thus formed.Optically active .alpha.-amino acids and their esters are of use in the synthesis of physiologically active compounds e.g. antibiotics of the penicillin and cephalosporin types. The present invention provides a relatively cheap, high yield process for the production of esters of optically active .alpha.-amino acids and for the production of optically active .alpha.-amino acids thereform. Certain novel compounds are disclosed.

Abstract: 3-Acyloxymethylceph-3-em-4-carboxylic acids, for example cephalosporin C, are enzymically deacylated to their 3-hydroxymethyl analogues by means of esterases produced by culturing microorganisms or mutants thereof of the class Basidiomycetes, particularly of the genus Rhodosporidium, for example a microorganism of the species Rhodosporidium toruloides.

Abstract: The invention provides novel antibiotic compounds which are 6.beta.-acylamidopenam-3-carboxylic acids, and nontoxic derivatives thereof, characterized in that the acylamido group has the structure ##EQU1## 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 may be either syn or anti isomers or may exist as mixtures e.g. containing at least 75% of one isomer. These antibiotic compounds possess high antibacterial activity against a range of gram positive organisms including penicillinase - producing staphylococci coupled with high activity against strains of the gram-negative organism Haemophilus influenzae. The invention is also concerned with the administration of the compounds.

Abstract: Cephalosporin antibiotics in which the 7.beta.-acylamido group has the structure ##EQU1## where R.sup.1 is a furyl, thienyl or phenyl group and R.sup.2 is a C.sub.1 -C.sub.4 alkyl, C.sub.3 C.sub.7 cycloalkyl or phenyl group and in which the 3-position substituent is a carbamoyloxymethyl group possess a particularly valuable combination of properties, exhibiting 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. Particularly important compounds of this type are (6R,7R)-3-carbamoyloxymethyl -7-[2-(fur-2-yl)-2-methoxyiminoacetamido]ceph-3-em-4-carboxylic acid (syn isomer) and its non-toxic derivatives, e.g. the sodium salt.

Abstract: New cephalosporin compounds are described characterized by possessing an ethyl group or a 2-cyanoethyl group as 3-position substituent.

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.-Aminoacylpenicillin antibiotics such as ampicillin and amoxycillin may be prepared in particularly simple manner by a process which comprises preparing a solution of 6-aminopenicillanic acid (6-APA) in a water-immiscible organic solvent by treating 6-APA with an excess of a strong tertiary amine base in the presence of said solvent; neutralising the residual strong tertiary amine base in said solution; reacting the neutralised solution with a solution in a water-immiscible organic solvent of an acylating agent which is a mixed anhydride of a lower alkoxyformic acid and an N-protected derivative of an .alpha.-aminoacid wherein the N-protecting group is acid-labile, to yield a solution of an N-protected .alpha.-aminoacylpenicillin derivative; contacting the resulting solution with water and a strong acid to cleave the acid-labile N-protecting group; and isolating the thus-obtained .alpha.-aminoacylpenicillin from the resulting water-containing system.

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 ##EQU1## 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 or 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 3.alpha.-oxygenated pregnane 21-ethers possessing a hydroxy group in the 3.alpha.-position; a hydrogen atom or a methyl group at the 10-position; a hydrogen atom in the 17.alpha.-position; a keto group in the 20-position; and an etherified hydroxyl group in the 21-position.

Abstract: The invention provides novel antibiotic compounds comprising 7.beta.-acylamido-3-carbamoyloxymethylceph-3-em-4-carboxylic acids and non-toxic derivatives thereof wherein the acylamido group has the structure ##EQU1## IN WHICH R is a carbocyclic or heterocyclic aryl group and R.sup.a is a lower alkyl, cycloalkyl or phenyl 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 organisms and stability in the presence of human serum. The invention is also concerned with the administration of the compounds.