Abstract: Compounds of the formula (I): ##STR1## and salts and pro-drugs thereof, wherein: R.sub.1 is a hydrogen atom or a lower alkyl group;R.sub.2 is a hydrogen atom or a lower alkyl group;R.sub.3 is a hydrogen atom or a lower alkyl group;R.sub.4 is a hydrogen atom or an alkyl group;R.sub.5 is a lower alkyl or a substituted alkyl group;or R.sub.4 and R.sub.5 are joined so that together with the nitrogen atom to which they are attached they form a 5-, 6- or 7-membered ring optionally containing an oxygen or sulphur atom;R.sub.6 is an electron donating group;R.sub.7 is an electron withdrawing group; andthe NR.sub.4 R.sub.5 and OR.sub.3 moieties are trans having antihypertensive activity, pharmaceutical compositions containing them and processes for their preparation.

Abstract: An improved process for the preparation of 3-substituted thiophenes. The thiophenes are useful for the preparation of penicillins and cephalosporins.The process is for the preparation of a thiophene of formula (I): ##STR1## where R.sup.1 represents a carboxylic acid group, or an ester or amide thereof or a nitrile group; R.sup.2 represents a group suitable for use as an .alpha.-substituent in the side-chain of a penicillin or cephalosporin; which comprises treating under basic conditions a compound of formula (II): ##STR2## wherein X represents halogen or optionally functionalized hydroxyl, Y represents halogen, hydroxyl, or alkoxy; with a source of nucleophilic sulphur ionically bound to a polymeric support.

Abstract: Certain substituted aralkylanilines in which the aromatic aniline ring carries, at the para position to the amino function, a substituent which comprises a carboxylic acid, salt or ester, an alkyl, hydroxyalkyl, cyano or acyl group, have hypolipidaemic activity.

Abstract: Compounds of formula (II): ##STR1## in which Y represents ##STR2## and R.sub.0 represents a C.sub.2-20 alkyl, C.sub.3-8 cycloalkyl, C.sub.4-20 alkenyl, arakyl, cycloalkylalkyl, heterocyclyl or heterocyclylalkyl group, which is substituted by a hydroxyiminohydrazono- or semicarbazono group, have activity against human and veterinary bacteria and mycoplasma. They may be produced by conventional methods and are used in conventional formulations.

Abstract: The compounds of the formula (XVII) ##STR1## and their esters wherein R.sub.2 is a hydrogen, fluorine, chlorine or bromine atom or an alkyl group of 1-3 carbon atoms, an alkoxyl group of 1-3 carbon atoms, an acyloxyl group of 1-3 atoms, a hydroxyl group, an alkoxycarbonyl group containing 1-3 carbon atoms in the alkoxy part, or a group --N(R.sub.5)CO.R.sub.6, --N(R.sub.5)SO.sub.2 R.sub.6 or --CO-NR.sub.5 R.sub.6 where R.sub.5 is a hydrogen atom or an alkyl group of 1-3 carbon atoms or a phenyl or benzyl group and R.sub.6 is an alkyl group of 1-3 carbon atoms or a phenyl or benzyl group; R.sub.3 is a hydrogen, fluorine or chlorine atom or an alkyl group of 1-3 carbon atoms, an alkoxyl group of 1-3 carbon atoms; or an acyloxyl group of 1-3 carbon atoms R.sub.4 is a hydrogen fluorine or chlorine atom or an alkyl group of 1-3 atoms or an alkoxyl group of 1-3 carbon atoms; and X is a bond or alkylene group of 1-4 carbon atoms; have been found to be .beta.-lactamase inhibitors and antibacterial agents.

Abstract: A compound of formula (II): ##STR1## wherein R is a C.sub.1-4 alkyl group;R.sub.1 is a hydrogen atom or a C.sub.1-4 alkyl group;R.sub.2 is a hydrogen or halogen atom, or a C.sub.1-4 alkyl, C.sub.1-4 alkoxy or C.sub.1-4 alkylthio group;and pro-drugs thereof; and the pharmaceutically acceptable salts of the compounds of formula (II) and of their pro-drugs; has useful anti-inflammatory and analgesic activity.

Abstract: A toothpaste contains 2% by weight of calcium metasilicate, 0.80% of sodium monofluorophosphate and 44.77% calcium carbonate. The presence of calcium metasilicate in combination with the monofluorophosphate and carbonate increases the fluoride uptake over and above that which is expected from the level of free fluoride present.

Abstract: A compound with hypoglycaemic activity having formula (II) or a pharmaceutically acceptable ammonium or acid addition salt thereof: ##STR1## wherein R.sup.1 and R.sup.2 are the same or different and represent hydrogen, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, hydroxy or halogen;R.sup.3 and R.sup.4 are the same or different and represent hydrogen or C.sub.1-6 alkyl;R.sup.5 represents hydrogen or C.sub.1-6 alkyl;R.sup.6 represents C.sub.1-6 alkyl, phenyl optionally substituted with up to 3 groups selected from halogen, C.sub.1-6 alkyl, and C.sub.1-6 alkoxy; or benzyl optionally substituted with up to 3 groups selected from halogen, C.sub.1-6 alkyl and C.sub.1-6 alkoxy; or R.sup.5 and R.sup.6 together represent the remaining members of a 5- or 6-membered ring optionally containing an oxygen, sulphur or additional nitrogen atom and being optionally substituted with C.sub.1-6 alkyl, carboxy or C.sub.1-6 alkoxycarbonyl; andR.sup.7 represents phenyl, optionally substituted with up to 3 groups selected from halogen, C.sub.

Abstract: Esters of the compound of the formula: ##STR1## are useful for their antibacterial and .beta.-lactamase inhibitory activity.

Abstract: Compounds of the formula (I): ##STR1## wherein: R.sub.1 and R.sub.2 are independently selected from a hydrogen atom and a C.sub.1-3 alkyl group;R.sub.3 is a hydrogen atom, a C.sub.1-3 alkyl or C.sub.2-4 acyl group;R.sub.4 is a hydrogen atom or C.sub.1-5 alkyl group;R.sub.5 is a C.sub.1-5 alkyl group, a straight chain C.sub.1-3 alkyl group terminally substituted by a chlorine atom; orR.sub.4 and R.sub.5 are joined so that together with the nitrogen atom to which they are attached they form a 5-, 6- or 7-membered ring optionally containing an oxygen or sulphur atom;R.sub.6 is a C.sub.1-5 alkyl group;the NR.sub.4 R.sub.5 and OR.sub.3 moieties are trans; and pharmaceutically acceptable salts thereof having antihypertensive activity, processes for their preparation and their use in compositions.

Abstract: Compounds of the formula (I) and pharmaceutically acceptable salts thereof: ##STR1## wherein: X is oxygen or sulphur;R.sub.1 is a C.sub.1-6 alkoxy or C.sub.1-6 alkylthio group;R.sub.2 and R.sub.3 are the same or different and are hydrogen, halogen, CF.sub.3, C.sub.1-7 acyl, C.sub.1-7 acylamino or amino, aminocarbonyl or aminosulphonyl optionally substituted by one or two C.sub.1-6 alkyl groups, C.sub.1-6 alkylsulphonyl, C.sub.1-6 alkylsulphinyl, C.sub.1-6 alkoxy, C.sub.1-6 alkylthio, hydroxy or nitro or R.sub.1 and R.sub.2 taken together are methylenedioxy or ethylenedioxy in which case R.sub.3 is any one of the groups given for R.sub.2 and R.sub.3 above;R.sub.4 is C.sub.1-7 alkyl or a group --(CH.sub.2).sub.s R.sub.5 where s is 0 to 2 and R.sub.5 is a C.sub.3-8 cycloalkyl group, or a group --(CH.sub.2).sub.t R.sub.6 where t is 1 or 2 and R.sub.6 is a phenyl group optionally substituted by one or two substituents selected from C.sub.1-6 alkyl, C.sub.

Abstract: Compounds are described of the formula (II): ##STR1## wherein R.sub.1 is a group such that CO.sub.2 R.sub.1 is an ester group; A.sub.1 is a hydrogen atom; and A.sub.2 is a group CR.sub.2 R.sub.3 R.sub.4 wherein R.sub.2 is a hydrogen atom or a hydroxyl group; R.sub.3 is a hydrogen atom or a lower alkyl group; and R.sub.4 is a hydrogen atom or a lower alkyl group, a benzyl group, a phenyl group or is joined to R.sub.3 to form part of a C.sub.5-7 carboxylic ring or is a group of the formula CH(OH)R.sub.5 or CHX wherein R.sub.5 is a hydrogen atom or lower alkyl group and X is an oxygen atom or a CR.sub.6 R.sub.7 group where R.sub.6 is a hydrogen atom or a lower alkyl, phenyl, CN, CO.sub.2 R.sub.8 where R.sub.8 is a lower alkyl, phenyl or benzyl group and R.sub.7 is a hydrogen atom or a lower alkyl group or is joined to R.sub.6 to form part of a C.sub.5-7 carbocyclic ring. These compounds have been found to possess antibacterial properties. The preparation of these compounds is described.

Abstract: A class of 2-substituted benzisothiazolones carrying a nitrogen-containing heterocyclic ring are effective in inhibiting platelet aggregation and are therefore of value in the prophylactic and therapeutic treatment of thrombotic diseases.

Abstract: Compounds of the formula (III) and pharmaceutically acceptable salts thereof: ##STR1## wherein: R.sub.1 is a C.sub.1-6 alkoxy or C.sub.1-6 alkylthio group;R.sub.2 and R.sub.3 are the same or different and are hydrogen, halogen, CF.sub.3, C.sub.1-7 acyl, C.sub.1-7 acylamino or amino, aminocarbonyl or aminosulphonyl optionally substituted by one or two C.sub.1-6 alkyl groups, C.sub.1-6 alkylsulphonyl, C.sub.1-6 alkylsulphinyl, C.sub.1-6 alkoxy, C.sub.1-6 alkylthio, hydroxy or nitro or R.sub.1 and R.sub.2 taken together are methylenedioxy or ethylenedioxy in which case R.sub.3 is any one of the groups given for R.sub.2 and R.sub.3 above;R.sub.4 is C.sub.1-7 alkyl or a group --(CH.sub.2).sub.s R.sub.6 where s is 0 to 2 and R.sub.6 is a C.sub.3-8 cycloalkyl group, or a group --(CH.sub.2).sub.t R.sub.7 where t is 1 or 2 and R.sub.7 is a phenyl group optionally substituted by one or two substituents selected from C.sub.1-6 alkyl, C.sub.

Abstract: A compound of formula (I) or a pharmaceutically acceptable salt or in vivo hydrolyzable ester thereof: ##STR1## wherein R is phenyl 4-hydroxy phenyl, or a 5- 6- membered heterocyclic ring containing up to three heteroatoms selected from oxygen, sulphur or nitrogen, optionally substituted with hydroxy, amino, halogen or C.sub.1-6 alkoxy;R.sup.1 represents hydrogen or C.sub.1-6 alkyl;R.sup.2 and R.sup.3 are the same or different and represent hydrogen, C.sub.1-6 alkyl, halogen, amino, hydroxy, or C.sub.1-6 alkoxy.Their preparation and use is described.

Abstract: A process for the preparation of .alpha.-carboxy, 6, .alpha.-methoxy penicillin derivatives by the enzymatic hydrolysis of an esterified derivative.The process is for the preparation of a compound of formula (I): ##STR1## wherein R represents phenyl or 2- or 3-thienyl, which process comprises subjecting a compound of formula (IV): ##STR2## where R.sup.1 is an aryl radical, to the action of an enzyme selected from bromelain, papain, gelatase, trypsin, pancreatin or an esterase-producing strain of Escherichia coli, Pseudomonas aeruginosa, Aspergillus niger or Saccharomyces sp.

Abstract: The compound 6-.beta.-chloropenicillanic acid can be prepared in substantially pure form and is a .beta.-lactamase inhibitor which may be used to enhance the effectiveness of penicillins acid cephalosporins against .beta.-lactamase producing lacteria.The process comprises the reaction of a compound of the formula: ##STR1## wherein R.sup.X is hydrogen or a carboxyl-blocking group and R is an aryl group, with a trialkyl tin hydride or a triaryl tin hydride or a dialkyl tin dihydride and optionally removing any carboxyl-blocking group R.sup.X, and/or oxidizing the atoms to an SO or SO.sub.2 ; and/or esterifying a salt of the acid to yield an in-vivo hydrolysable ester.

Abstract: Compounds of the formula ##STR1## which are intermediates for producing antibacterial and .beta.-lactamase inhibiting compounds of the formula ##STR2## wherein R.sub.1 is alkyl of 1 to 6 carbon atoms, unsubstituted or substituted with hydroxy, amino, nitro, alkanoylamido of 1 to 6 carbon atoms, benzyloxycarbonylamido or p-nitrobenzyloxycarbonylamido; trityl; phenyl; or phenyl substituted by one or more members selected from the group consisting of halo, alkyl of 1 to 6 carbon atoms, alkoxy of 1 to 6 carbon atoms, amino, alkanoylamido of 1 to 6 carbon atoms, benzyloxycarbonylamido or p-nitrobenzyloxycarbonylamido;R is alkyl of 1 to 6 carbon atoms, benzyl, p-nitrobenzyl, p-methoxybenzyl, phenacyl, p-bromophenacyl, 2,2,2-trichloroethyl, phthalidyl, phthalimidomethyl, .alpha.

Abstract: A process for the preparation of .alpha.-carboxy, 6, .alpha.-methoxy penicillin derivatives by the enzymatic hydrolysis of an esterified derivative.The process is for the preparation of a compound of formula (I): ##STR1## wherein R represents phenyl or 2- or 3-thienyl, which process comprises subjecting a compound of formula (IV): ##STR2## wherein R.sup.1 is an ester-forming radical, to the action of the enzyme .alpha.-chymotrypsin or an esterase-producing strain of Streptomyces sp.

Abstract: Compounds of the formula (I): ##STR1## and pharmaceutically acceptable salts and N-oxides thereof, wherein: R.sub.1 is a C.sub.1-6 alkoxy group;R.sub.2 and R.sub.3 are the same or different and are hydrogen, halogen, CF.sub.3, C.sub.1-7 acyl, C.sub.1-7 acylamino, C.sub.1-6 alkyl-S(O).sub.n wherein n is 0, 1 or 2, nitro, C.sub.1-6 alkoxy, hydroxy, or amino, aminocarbonyl or aminosulphonyl optionally substituted by one or two C.sub.1-6 alkyl groups;or R.sub.1 and R.sub.2 taken together are methylenedioxy or ethylenedioxy in which case R.sub.3 is any one of the groups given for R.sub.1 and R.sub.2 above;R.sub.4 is hydrogen, C.sub.1-4 alkyl, phenyl or phenyl C.sub.1-4 alkyl;R.sub.5 is hydrogen or C.sub.1-4 alkyl;X is an oxygen or sulphur atom; or a sulphoxide group >S.about.O;p is 1 or 2; andr is 1 or 2; are useful in the treatment of disorders related to imparied gastrointestinal motility.