Abstract: The compounds of the formula (II): ##STR1## or pharmaceutically acceptable salts or esters thereof wherein A is a hydrogen atom or an esterifying radical; X is an alkyl group of 1-12 carbon atoms optionally substituted by a hydroxy, amino, acylamino of C.sub.1-6 alkoxy group, which substituents are not on the carbon atom adjacent to the nitrogen atom; or a C.sub.5-7 cycloalkyl group; or a phenylalkyl group wherein the carbon atom content of the alkyl part is 1-6 and the phenyl part is optionally substituted with a fluorine, bromine, chlorine, C.sub.1-6 alkyl, or C.sub.1-6 alkoxy; with the proviso that when X represents an optionally substituted phenylalkyl group and A represents C.sub.1-3 alkyl, then the --CO.sub.2 A group is attached to the alkyl part of the phenylalkyl group; have been found to be .beta.-lactamase inhibitors and antibacterial agents. Their preparation and use is described.

Abstract: The present invention provides the salts of the formula (II): ##STR1## wherein R.sup.1 is a hydrogen atom or a lower alkyl, aralkyl, phenyl or inertly substituted lower alkyl, aralkyl or phenyl group; R.sup.2 is a hydrogen atom or a lower alkyl, aralkyl, phenyl or inertly substituted lower alkyl, aralkyl or phenyl group; and R.sup.3 is lower alkyl, aralkyl, phenyl or inertly substituted lower alkyl, aralkyl or phenyl group; any of said groups R.sup.1, R.sup.2 and R.sup.3 being optionally interlinked to form a ring of 5-7 ring atoms. The compounds are antibacterials.

Abstract: A monocyclic .beta.-lactam antibiotic having a formamido substituent at the 3S-position, including compounds of the formula (I): ##STR1## and salts thereof wherein R is --SO.sub.3 H; --PO(OH)Y wherein Y is C.sub.1-6 alkoxy, hydroxy, aryloxy, C.sub.1-6 alkyl or aryl; ##STR2## wherein Z represents C.sub.1-6 alkyl or aryl; ##STR3## wherein Z.sup.1 and Z.sup.2 may be the same or different and each represents hydrogen, C.sub.1-6 alkyl, aryl, amino or C.sub.1-6 alkoxy, or Z.sup.1 and Z.sup.2 together form the residue of a heterocyclic ring; --OSO.sub.3 H; or ##STR4## where X is hydrogen or hydroxy; R.sup.1 is an amino, protected amino or carboxylic acylamino group, and R.sup.2 and R.sup.3 are independently selected from hydrogen or a hydrocarbon group of 1 to 18 carbon atoms.

Abstract: This invention provides a novel process for the preparation of clavulanic acid and pharmaceutically acceptable salts and esters thereof which process utilizes the preparation of the tertiary-butylamine salt of clavulanic acid optionally in the form of an acetone solvate and subsequently converting said salt into the desired product.

Abstract: Compounds of formula (I): ##STR1## wherein the various substituents are defined hereinbelow, having anti-hypertensive activity.

Abstract: Process for racemization of amino acids by use of a ketone and an organic acid such as acetic acid. In particular, a process for resolution of free .alpha.-amino acids with in situ racemization. The resolution of 4-hydroxyphenylglycine and 3,4-dihydroxyphenylglycine with 3-bromocamphor-9-sulphonic acid with in situ racemization are specifically mentioned.

Abstract: Tetrazolyl derivatives of clavulanic acid are described, having the formula: ##STR1## wherein X is an optionally substituted tetrazolyl group attached via a nitrogen atom. These compounds are useful as antibiotics and .beta.-lactamase inhibitors.

Abstract: Anti-hypertensive compounds of formula (I): ##STR1## wherein: one of R.sub.1 and R.sub.2 is nitro, cyano or C.sub.1-3 alkylcarbonyl, and the other is methoxy or amino optionally substituted by one or two C.sub.1-6 alkyl or by C.sub.2-7 alkanoyl;one of R.sub.3 and R.sub.4 is hydrogen or C.sub.1-4 alkyl and the other is C.sub.1-4 alkyl, or R.sub.3 and R.sub.4 together with the carbon atom to which they are attached are C.sub.3-6 spiroalkyl;R.sub.5 is hydrogen, C.sub.1-3 alkyl or C.sub.1-8 acyl; andn is 1 or 2; the lactam group being trans to the OR.sub.5 group; or, when the other of R.sub.1 and R.sub.2 is amino, a pharmaceutically acceptable salt thereof.

Abstract: Compounds of formula (I): ##STR1## wherein: either one of R.sub.1 and R.sub.2 is hydrogen and the other is selected from the class of C.sub.1-6 alkylcarbonyl, benzoyl, C.sub.1-6 alkoxycarbonyl, C.sub.1-6 alkylcarbonyloxy, C.sub.1-6 alkylhydroxymethyl, nitro, cyano, chloro, trifluoromethyl, C.sub.1-6 alkylsulphinyl, C.sub.1-6 alkylsulphonyl, C.sub.1-6 alkoxysulphinyl, C.sub.1-6 alkoxysulphonyl, C.sub.1-6 alkylcarbonylamino, C.sub.1-6 alkoxycarbonylamino, C.sub.1-6 alkyl-thiocarbonyl, C.sub.1-6 alkoxy-thiocarbonyl, C.sub.1-6 alkyl-thiocarbonyloxy, C.sub.1-6 alkyl-thiolmethyl, formyl or aminosulphinyl, aminosulphonyl or aminocarbonyl, the amino moiety being optionally substituted by one or two C.sub.1-6 alkyl groups, or C.sub.1-6 alkylsulphinylamino, C.sub.1-6 alkylsulphonylamino C.sub.1-6 alkoxysulphinylamino or C.sub.1-6 alkoxysulphonylamino or ethylenyl terminally substituted by C.sub.1-6 alkylcarbonyl, nitro or cyano, or --C(C.sub.1-6 alkyl)NOH or --C(C.sub.1-6 alkyl)NNH.sub.2, or one of R.sub.1 and R.sub.

Abstract: Procedure for isolating lithium pseudomonate from a crude preparation containing pseudomonic acid by extracting the crude preparation into a suitable organic solvent in which pseudomonic acid is soluble, treating the extract with a lithium alkanoic acid and separating the resulting crystalline non-hygroscopic lithium pseudomonate, the crude preparation containing pseudomonic acid being a culture medium on or in which pseudomonic acid producing strains of bacteria have been grown, such as Pseudomonas fluorescens.

Abstract: Compounds of formula (I), ##STR1## or an N-oxide or pharmaceutically acceptable salt thereof, wherein R.sub.1 is hydrogen, C.sub.1-7 alkyl, C.sub.3-7 cycloalkyl, C.sub.4-7 cycloalkenyl or C.sub.1-4 alkyl substituted by C.sub.2-7 alkenyl, C.sub.2-7 alkynyl, C.sub.3-7 cycloalkyl, hydroxy, thiol, C.sub.1-4 alkoxy, C.sub.1-4 alkylthio, carboxy, C.sub.1-4 alkoxycarbonyl, C.sub.1-4 alkanoyl, amino optionally substituted by one or two C.sub.1-4 alkyl or by C.sub.4-6 polymethylene optionally containing an oxygen or nitrogen atom, aminocarbonyl optionally N-substituted by one or two C.sub.1-4 alkyl, or benzoyl or phenyl either being optionally ring-substituted by C.sub.1-4 alkyl, C.sub.1-4 alkoxy, halogen or trifluoromethyl, R.sub.2 and R.sub.3 are the same or different and are hydrogen, hydroxy, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, C.sub.1-4 alkylthio, halogen or trifluoromethyl, m is 1 to 3 and n is 1 or 2, the hydrogen atom bonded to the C.sub.a carbon atom being trans to the hydrogen atom bonded to the C.sub.

Abstract: A compound of formula (I): ##STR1## or a pharmaceutically acceptable salt, ester or amide thereof, in which: W is an optionally substituted phenyl group of the formula ##STR2## wherein R.sup.1 is hydrogen or fluorine, R.sup.2 is hydrogen, C.sub.1-6 alkyl, halogen or trifluoromethyl; or W is a phenoxymethyl or benzofuran-2-yl group;R.sup.3 is C.sub.1-12 alkyl or phenyl C.sub.1-6 alkyl;A is hydrogen or methyl,X is carboxy, --Z--CO.sub.2 H, --Z--OH, T--Z--CO.sub.2 H,--Z--NR.sup.4 R.sup.5, --T--Y--OM, --T--Y--NR.sup.4 R.sup.5, or --T--R.sup.6, in the para- or meta-position with respect to the --(CH.sub.2).sub.n group,whereinR.sup.4 and R.sup.5 are each hydrogen or C.sub.1-6 alkyl,R.sup.6 is C.sub.1-6 alkyl,T is 0, S, --NH or --N--R.sup.7, in which R.sup.7 is C.sub.1-6 alkylZ is C.sub.1-10 straight or branched alkylene optionally containing a carbon-carbon double bond;Y is C.sub.2-10 straight or branched alkylene, provided that the hetero atoms in --T--Y--OM and --T--Y--NR.sup.4 R.sup.

Abstract: Compounds of formula (I): ##STR1## wherein: R.sub.1 -R.sub.6 are as defined in the specification;X is oxygen or sulphur; and the R.sub.6 NCXR.sub.5 and OCOH moieties are trans and, when one or the other of R.sub.1 and R.sub.2 is an amino group, pharmaceutically acceptable salts thereof, a process and intermediates for preparing them, pharmaceutical compositions containing them, and their use in the treatment of mammals.

Abstract: A compound of formula I ##STR1## or a salt or ester thereof. Processes for the preparation of these compounds and the use of these compounds in the preparation of further bicyclic compounds are also disclosed.

Abstract: Compounds of formula (II): ##STR1## or salt thereof; wherein R.sup.1 is hydrogen or methyl,R.sup.2 is hydrogen or methyl,R.sup.3 is hydrogen, C.sub.1-12 straight or branched alkyl, C.sub.3-10 cycloalkyl, phenyl(C.sub.1-4)-alkyl or benzyl optionally substituted by C.sub.1-4 alkyl, C.sub.1-4 alkoxy or halogen;R.sup.4 is hydrogen, halogen, hydroxy, C.sub.1-4 alkyl or C.sub.1-4 alkoxy,R.sup.5 is hydrogen or fluorine,R.sup.6 is hydrogen or fluorine,R.sup.7 is halogen; andn is 1 or 2,have anti-obesity and/or anti-hyperglycaemic activity.

Abstract: Compounds of formula (I) and pharmaceutically acceptable salts thereof: ##STR1## wherein: X is NR wherein R is hydrogen or C.sub.1-6 alkyl, oxygen, sulphur, SO or SO.sub.2 ;R.sub.1 is COR.sub.5 wherein R.sub.5 is hydroxy, or COR.sub.5 is a pharmaceutically acceptable ester or amide group; or CF.sub.3 ; and R.sub.2 is hydrogen, C.sub.1-6 alkyl or phenyl optionally substituted by halogen, CF.sub.3, C.sub.1-4 alkoxy or C.sub.1-4 alkyl; or R.sub.2 is COR.sub.5 as defined or CF.sub.3 and R.sub.1 is hydrogen;R.sub.3 is C.sub.1-10 alkyl, optionally substituted by hydroxy, C.sub.1-4 alkoxy, thiol, C.sub.1-4 alkylthio or NR.sub.6 R.sub.7 wherein R.sub.6 and R.sub.7 are independently hydrogen or C.sub.1-6 alkyl or together are C.sub.3-6 polymethylene; C.sub.2-10 alkenyl or phenyl optionally substituted by one or two of halogen, CF.sub.3, C.sub.1-4 alkoxy, C.sub.1-4 alkyl, hydroxy, nitro, cyano, C.sub.2-10 acyloxy, NR.sub.8 R.sub.9 wherein R.sub.8 and R.sub.9 are independently selected from hydrogen, C.sub.1-6 alkyl, C.

Abstract: A compound of formula (I): ##STR1## wherein: either one of R.sub.1 and R.sub.2 is hydrogen and the other is selected from the class of C.sub.1-6 alkylcarbonyl, C.sub.1-6 alkoxycarbonyl, C.sub.1-6 alkylcarbonyloxy, C.sub.1-6 alkylhydroxymethyl, nitro, cyano, chloro, trifluoromethyl, C.sub.1-6 alkylsulphinyl, C.sub.1-6 alkylsulphonyl, C.sub.1-6 alkoxysulphinyl, C.sub.1-6 alkoxysulphonyl, C.sub.1-6 alkylcarbonylamino, C.sub.1-6 alkoxycarbonylamino, C.sub.1-6 alkyl-thiocarbonyl, C.sub.1-6 alkoxy-thiocarbonyl, C.sub.1-6 alkyl-thiocarbonyloxy, 1-mercapto C.sub.2-7 alkyl, formyl, or aminosulphinyl, aminosulphonyl or aminocarbonyl, the amino moiety being optionally substituted by one or two C.sub.1-6 alkyl groups, or C.sub.1-6 alkylsulphinylamino, C.sub.1-6 alkylsulphonylamino, C.sub.1-6 alkoxysulphinylamino or C.sub.1-6 alkoxysulphonylamino, or ethylenyl terminally substituted by C.sub.1-6 alkylcarbonyl, nitro or cyano, or --C(C.sub.1-6 alkyl)NOH or --C(C.sub.1-6 alkyl)NNH.sub.2, or one of R.sub.1 and R.sub.

Abstract: A compound of formula (I), or a pharmaceutically acceptable salt, or N-oxide thereof, or a solvate of any of the foregoing: ##STR1## wherein p is 0 to 2; q is 0 to 3; j is 0 to 4;one of R.sub.5 and R.sub.6 is hydrogen, C.sub.1-6 alkyl, phenyl or phenyl-C.sub.1-3 alkyl, which phenyl moieties may be substituted by C.sub.1-6 alkyl, C.sub.1-6 alkoxy, CF.sub.3 or halogen;and the other of R.sub.5 and R.sub.6 is hydrogen or C.sub.1-6 alkyl; andA is of formula (II): ##STR2## wherein R.sub.2, R.sub.3 and R.sub.4 are each independently selected from hydrogen, halogen, CF.sub.3 C.sub.1-6 alkyl, C.sub.1-6 alkoxy, C.sub.1-6 alkylthio, C.sub.1-7 acyl, C.sub.1-7 carboxylic acylamino, C.sub.1-6 alkylsulphonylamino, N-(C.sub.1-6 alkylsulphonyl)-N-C.sub.1-4 alkylamino, C.sub.1-6 alkylsulphonyl, C.sub.1-6 alkylsulphinyl, hydroxy, nitro or amino, aminocarbonyl, aminosulphonyl, aminosulphonylamino or N-(aminosulphonyl)-C.sub.1-4 alkylamino optionally N-substituted by one or two groups selected from C.sub.1-6 alkyl, C.sub.

Abstract: A compound of formula (I): ##STR1## wherein: either one of R.sub.1 and R.sub.2 is hydrogen and the other is selected from the class of C.sub.1-6 alkylcarbonyl, C.sub.1-6 alkoxycarbonyl, C.sub.1-6 alkylcarbonyloxy, C.sub.1-6 alkylhydroxymethyl, nitro, cyano, chloro, trifluoromethyl, C.sub.1-6 alkylsulphinyl, C.sub.1-6 alkylsulphonyl, C.sub.1-6 alkoxysulphinyl, C.sub.1-6 alkoxysulphonyl, C.sub.1-6 alkylcarbonylamino, C.sub.1-6 alkoxycarbonylamino, C.sub.1-6 alkyl-thiocarbonyl, C.sub.1-6 alkoxy-thiocarbonyl, C.sub.1-6 alkyl-thiocarbonyloxy, 1-mercapto-C.sub.2-7 alkyl, formyl or aminosulphinyl, aminosulphonyl or aminocarbonyl, the amino moiety being optionally substituted by one or two C.sub.1-6 alkyl groups, or C.sub.1-6 alkysulphinylamino, C.sub.1-6 alkylsulphonylamino C.sub.1-6 alkoxysulphinylamino or C.sub.1-6 alkoxysulphonylamino or ethylenyl terminally substituted by C.sub.1-6 alkylcarbonyl, nitro or cyano, or --C(C.sub.1-6 alkyl)NOH or --C(C.sub.1-6 alkyl)NNH.sub.2, or one of R.sub.1 and R.sub.

Abstract: The compounds of the formula (II): ##STR1## and salts and esters thereof wherein R is an inert organic group of up to 18 carbon atoms and are able to inhibit the action of various bacterial .beta.-lactamases. Thus when a compound of the formula (II) or its salt or ester is used together with a penicillin or cephalosporin, the effectiveness of that penicillin or cephalosporin can be considerably enhanced. These novel synergysts can be prepared by etherification of an ester of clavulanic acid followed if desired by deesterification. The novel synergysts also possess antibacterial activity.