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: 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 (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: 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: 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: .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: This invention relates to novel substituted benzamides having useful pharmacological properties, to pharmaceutical compositions containing them, to a process for their preparation and to intermediates therefor.N-(2-Diethylaminoethyl)-2-methoxy-4-amino-5-chlorobenzamide, 1-ethyl-2(2-methoxy-5-sulphamoylbenzamidomethyl)pyrrolidine and N-[4'-(1"-benzyl)-piperidyl]-2-methoxy-4-amino-5-chlorobenzamide are well known compounds having useful pharmacological activity such as the ability to regulate the gastro-intestinal function anti-emetic activity and CNS activity.It has now been found that certain intermediates for a structurally distinct class of substituted benzamides also has useful pharmacological activity, in particular dopamine antagonist activity.

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.