Abstract: .beta.-Lactam antibiotics having an .alpha.-formamido substituent on the carbon atom adjacent to the carbonyl group of the .beta.-lactam ring and in particular bicyclic compounds having the partial structure: ##STR1## Intermediates and processes for the preparation of the compounds are further disclosed.

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.

Abstract: Compounds of formula (I): ##STR1## or a salt thereof, in which W is phenyl optionally substituted by halogen or trifluoromethyl, or a benzofuran-2-yl group,R.sup.1 is hydrogen or methyl,R.sup.2 is carboxyl or a group O--Z--CO.sub.2 H or an ester or amide thereof; a groupO--E--NR.sup.3 R.sup.4 or a group O--E--OR.sup.5,wherein R.sup.3, R.sup.4 and R.sup.5 each represents hydrogen or C.sub.1-6 alkyl, Z is a C.sub.1-6 straight or branched alkylene chain, n is 1 or 2, a is 2 or 3, and E is a C.sub.2-7 straight or branched alkylene chain with at least two carbon atoms separating the two heteroatoms in the group R.sup.2 ; a process for the production of such compounds and their use in treating hyperglycaemia and/or obesity.

Abstract: Known disadvantages of protein Ca are overcome or reduced by acylating the protein to form a derivative which will gradually hydrolyse in vivo to regenerate the active enzyme. The enzyme derivative comprises protein Ca in which the active site essential for anti-coagulant activity is blocked by an acyl group removable in vivo by enzymatic hydrolysis to provide a sustained and controlled release of protein Ca, preferred acyl groups being optionally substituted benzoyl or acryloyl groups.

Abstract: Compounds of formula (I): ##STR1## or a salt or acyl derivative thereof; whereinY is either --CH.dbd.N or ##STR2## R.sup.1 is hydroxy, halogen, (C.sub.1-4) alkyl, or (C.sub.1-4)alkoxy, R.sup.2 is a nitrogen-containing, basic substituent,R.sup.3 is hydrogen, hydroxy, halogen, (C.sub.1-4) alkyl, (C.sub.1-4) alkoxy or a nitrogen-containing, basic substituent, andR.sup.4 is hydrogen or hydroxy,are useful in treating diarrhoea and scours.

Abstract: A derivative of a fibrinolytic enzyme in which the catalytic site on the enzyme which is responsible for fibrinolytic activity is blocked by a human protein attached thereto by way of a reversible linking group.

Abstract: Alpha-carboxy-3-thienylmethyl penicillin having either the R- or the S- configuration at C-10 is obtained in cyrstalline form. The isomers show improved stability and higher biological activity as compared to the amorphous RS material.

Abstract: A compound of formula (I): ##STR1## or a salt thereof wherein R.sup.1 is halogen, C.sub.1-4 alkyl or C.sub.1-4 alkoxyR.sup.2 is hydrogen, halogen, C.sub.1-4 alkyl or C.sub.1-4 alkoxyR.sup.3 and R.sup.4 are the same or different and each is hydrogen, C.sub.1-4 alkyl or acyl andR.sup.5 is either (i) ##STR2## wherein R.sup.6, R.sup.7 and R.sup.8 are the same or different and each is selected from hydrogen, halogen, alkyl, alkoxy, hydroxy, hydroxyalkyl, alkoxyalkyl, mercapto, mercaptoalkyl, amino, aminoalkyl, nitro, cyano, carboxy or a salt, ester or amide of carboxy provided that at least one of R.sup.6, R.sup.7 and R.sup.8 is other than hydrogen or (ii) ##STR3## wherein R.sup.9, R.sup.10 and R.sup.11 are the same or different and each is selected from hydrogen, halogen, alkyl, alkoxy, hydroxy, hydroxyalkyl, alkoxyalkyl, mercapto, mercaptoalkyl, amino, aminoalkyl, nitro, cyano, carboxy or a salt, ester or amide of carboxyand X is --CH.sub.2 -- or --CH.dbd.CH-- or (iii) ##STR4## wherein R.sup.12 and R.sup.

Abstract: A compound of formula (I) ##STR1## or a pharmaceutically acceptable salt thereof, in which R.sup.1 is hydrogen, halogen, or trifluoromethyl;R.sup.2 is hydrogen or halogen;R.sup.3 is hydrogen or methyl;R.sup.4 is --O(CH.sub.2).sub.a CO.sub.2 H or an ester or amide derivative thereof, O(CH.sub.2).sub.b M or --CO.sub.2 H or an ester or amide derivative thereofwhereina is an integer from 1 to 6,b is an integer from 2 to 7, andM is hydroxy, C.sub.1-6 alkoxy or ##STR2## wherein R.sup.6 and R.sup.7 are each hydrogen or C.sub.1-6 alkyl or ##STR3## together form a five or six membered ring; R.sup.5 is C.sub.1-6 alkyl; C.sub.1-6 alkyl substituted by carboxy or esters and amides thereof; or phenyl optionally substituted by C.sub.1-6 alkyl, halogen, alkoxy or trifluoromethyl;R.sup.8 is hydrogen or C.sub.1-6 alkyl or R.sup.8 together withR.sup.5 form a carbocyclic ring; andn is 1 or 2.Processes for preparing these compounds and their use in therapy is also described.

Abstract: Compounds of formula (I) ##STR1## and acid addition salts thereof, wherein R.sup.1 is hydrogen, hydroxy, alkoxy, aryloxy, aralkoxy, heteroaryloxy or heteroaralkoxy; andone of R.sup.2, R.sup.3 and R.sup.4 is hydrogen and the others are the same or different and each is hydrogen, alkyl, aryl, aralkyl, heteroaryl or heteroaralkyl; orR.sup.2 is hydrogen and ##STR2## is mono- or bi-cyclic amino, inhibit enterotoxin-induced secretion into the small intestine and are, therefore, useful in treating enterotoxin induced diarrhoea in humans and scours in animals.

Abstract: A compound of formula (I): ##STR1## or a pharmaceutically acceptable salt, thereof, in which R.sup.1 is hydrogen, halogen, or trifluoromethyl,R.sup.2 is hydrogen or halogen,R.sup.3 is hydrogen or methyl.R.sup.4 is --O(CH.sub.2).sub.a CO.sub.2 H, --O(CH.sub.2).sub.b M, --CO.sub.2 H or an esteror amide derivative thereof in whicha is an integer from 1 to 6,b is an integer from 2 to 7, andM is hydroxy, C.sub.1-6 alkoxy or ##STR2## in which R.sup.5 and R.sup.6 are each hydrogen or C.sub.1-6 alkyl or ##STR3## together form a five or six membered ring, and n is 1 or 2; a process for preparing such a compound and its use in medicine and agriculture.

Abstract: Compounds of formula (I), or a pharmaceutically acceptable salt, quaternized derivative, N-oxide or solvate thereof:R.sub.1 --Ar--(CH.sub.2).sub.a --X--(CH.sub.2).sub.b --NH--Het (I)wherein: the substituents are defined in the specification.The compounds are useful in treating excess gastric acid secretions such as peptic ulcers.

Abstract: Compounds of formula (II): ##STR1## or a pharmaceutically acceptable salt thereof, in which X is an oxygen atom or a bond, R.sup.1 is a hydrogen, fluorine, chlorine or bromine atom or a trifluoromethyl or C.sub.1-4 alkyl group, each of R.sup.2 and R.sup.3 is a hydrogen atom or a C.sub.1-4 alkyl group, R.sup.4 is a C.sub.1-4 alkyl group, R.sup.5 is a hydrogen atom or a C.sub.1-4 alkyl group, and n is an integer of from 1 to 3; are useful as anti-obesity and/or anti-hyperglycaemic agents.

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: 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: A compound of formula (I) or a pharmaceutically acceptable salt thereof: ##STR1## wherein: R.sub.1 and R.sub.2 are independently hydrogen, C.sub.1-6 alkyl or together are a group X which is C.sub.3-6 polymethylene optionally interrupted by O, S or NR.sub.6 wherein R.sub.6 is hydrogen or C.sub.1-6 alkyl;R.sub.3 is phenyl, optionally substituted by one or more substituents selected from halogen, CF.sub.3, nitro, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, C.sub.1-6 alkylthio, C.sub.2-7 alkanoyl, carboxyl, C.sub.1-6 alkoxycarbonyl, cyano, CONR.sub.7 R.sub.8 wherein R.sub.7 and R.sub.8 are selected from hydrogen or C.sub.1-6 alkyl or together are a group X; NR.sub.9 R.sub.10 wherein R.sub.9 and R.sub.10 are selected from hydrogen, C.sub.1-6 alkyl, C.sub.2-7 alkanoyl or C.sub.1-6 alkylsulphonyl or together are a group X; SO.sub.2 NR.sub.11 R.sub.12 wherein R.sub.11 and R.sub.12 are selected from hydrogen or C.sub.1-6 alkyl or together are a group X or S(O).sub.m R.sub.13 wherein m is 1 or 2 and R.sub.13 is C.sub.

Abstract: Compounds of formula (I) and pharmaceutically acceptable salts thereof: ##STR1## wherein: R.sub.1 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;R.sub.2 is hydrogen or C.sub.1-6 alkyl;R.sub.3 is hydroxy, nitro, cyano, C.sub.2-10 acyloxy, NR.sub.6 R.sub.7 wherein R.sub.6 and R.sub.7 are independently selected from hydrogen, C.sub.1-6 alkyl, C.sub.2-7 alkanoyl or C.sub.1-6 alkylsulphonyl; or COR.sub.8 wherein R.sub.8 is hydroxy, C.sub.1-6 alkoxy or NR.sub.9 R.sub.10 wherein R.sub.9 and R.sub.10 are independently selected from hydrogen or C.sub.1-6 alkyl;R.sub.4 is hydrogen, halogen, CF.sub.3, C.sub.1-4 alkoxy, C.sub.1-4 alkyl or any of the groups listed for R.sub.3 ; andR.sub.5 is hydrogen, C.sub.1-4 alkyl or benzyl optionally substituted in the phenyl ring by halogen, CF.sub.3, C.sub.1-4 alkoxy or C.sub.

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, 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 alkoxysulphinylamino, C.sub.1-6 alkoxysulphonylamino 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 one of R.sub.1 and R.sub.2 is nitro, cyano or C.sub.

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, 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 circumference measuring device comprising a flexible tape arranged to form a loop of adjustable size; indicating means comprising a scale and a reference mark movable with respect to one another, one end of the said tape being attached to the indicating means such that the indicating means measures the size of the loop; and zeroing means to preset the reference mark at a predetermined position with respect to the scale.