Abstract: Pharmaceutical compositions are described for anti-allergy therapy comprising an allergen or allergen extract, polysarcosine having an average molecular weight in the range of 2,000 to 12,000 and a chemical linking group connecting a reactive site on the polysarcosine to an amino group on the allergen or allergen extract, the reactive site on the polysarcosine being a H(CH.sub.3)N--, the allergen extract being an extract from an allergen selected from pollens, weeds, house dust mites and venoms, and the chemical linking group having the formula --CO--B--CO where B is a hydrocarbon chain of 1-4 carbon atoms. The disclosure also describes the analogous conjugates.

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: 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: Compounds of formula (I): ##STR1## wherein: one of X and Y is CO and the other is NH;R.sub.1 is C.sub.1-6 alkoxy or C.sub.1-6 alkylthio;R.sub.2 is hydrogen, trifluoromethyl, C.sub.1-6 alkylthio, C.sub.1-7 acyl, C.sub.1-7 acylamino, C.sub.1-6 alkylsulphonyl, C.sub.1-6 alkylsulphinyl, halogen, nitro or amino, aminocarbonyl or aminosulphonyl optionally N-substituted by one or two groups selected from C.sub.1-6 alkyl, C.sub.3-8 cycloalkyl, C.sub.3-8 cycloalkyl C.sub.1-4 alkyl, phenyl or phenyl C.sub.1-4 alkyl groups any of which phenyl moieties may be substituted by one or more halogen, trifluoromethyl, C.sub.1-6 alkoxy or nitro groups, or N-disubstituted by C.sub.2-5 polymethylene;R.sub.3 is amino, aminocarbonyl or aminosulphonyl N-substituted by one or two C.sub.3-8 cycloalkyl, C.sub.3-8 cycloalkyl C.sub.1-4 alkyl, phenyl or phenyl C.sub.1-4 alkyl groups any of which phenyl moieties may be substituted by one or more halogen, trifluoromethyl, C.sub.1-6 alkoxy or nitro groups, or N-disubstituted by C.sub.