Glaxo Group Limited

Hoechst (uk) Limited

Hoechst Aktiengesellschaft

Barry C Ross

David Middlemiss

Graham Johnson

Michael D Dowle

David I Scopes

Kevin S Cardwell

Michael D Cooke

Torquil I Jack

Duncan B Judd

Nigel Stephen Watson

John G Montana

Michael A Yeomans

Colin David Eldred

Chuen Chan

Pritom Shah

Stephen Paul Watson

Jeffrey D Michael

Panayiotis Alexandrou Procopiou

Michael G Lester

Andrew J Barker

Barrie E Kirk

Martin Pass

Nicholas I Carruthers

The invention provides compounds of formula (I): ##STR1## or a physiologically acceptable salt, solvate or metabolically labile ester thereof wherein the R groups are defined in the specification. The compounds may be used in the treatment or prophylaxis of hypertension and diseases associated with cognitive disorders.

Benzofuran derivatives

The invention provides compounds of the general formula (I): ##STR1## or a physiologically acceptable salt, solvate (e.g. hydrate) or a metabolically labile ester thereof. The compounds may be used in the treatment or prophylaxis of hypertension and diseases associated with cognitive disorders.

C-linked pyrazole derivatives

The invention provides compounds of the general formula (I) ##STR1## and physiologically acceptable salts, solvates or non-toxic metabolically labile esters thereof where R.sup.1 represents a halogen atom; Ar represents the group ##STR2## R.sup.3 represents a C-linked tetrazolyl group; R.sup.4 and R.sup.5, which may be the same or different, each independently represent a hydrogen atom or a halogen atom or a C.sub.1-6 alkyl group; and

The invention provides compounds of formula (I): ##STR1## or a physiologically acceptable salt, solvate or metabolically labile ester thereof wherein

The invention provides compounds of formula (I): ##STR1## or a physiologically acceptable salt, solvate or metabolically labile ester thereof. The compounds may be used in the treatment or prophylaxis of hypertension and diseases associated with cognitive disorders.

Pyrazole containing benzofuran derivatives and pharmaceutical

This invention relates to imidazole derivatives having hypocholesterolemic and hypolipidemic activity, to processes for their preparation, to pharmaceutical compositions containing them and to their use in medicine, particularly in the treatment and/or prevention of atherosclerosis and coronary heart disease.

Imidazole derivatives

Certain novel imidazole derivatives N-substituted by a vinyl group itself carrying a mevalonic acid derivative or corresponding lactone are inhibitors of HMG-CoA reductase and are useful for lowering blood plasma cholesterol levels. The compounds are of general formula (I): ##STR1## in which one of the groups R.sup.1 and R.sup.2 represents a C.sub.1-6 alkyl group optionally substituted by one to three halogen atoms and the other represents a phenyl ring optionally substituted by one to five substituents selected from halogen atoms and hydroxyl, C.sub.1-3 alkyl, C.sub.1-3 alkoxy, S(O).sub.n C.sub.1-3 alkyl, (CH.sub.2).sub.m NR.sup.a R.sup.b, (CH.sub.2).sub.m NR.sup.c COR.sup.d and trifluoromethyl groups;

Imidazole derivatives, pharmaceutical compositions and use

Compounds of formula ##STR1## wherein R.sup.1 or R.sup.2 represents a C.sub.1-6 alkyl group optionally substituted by one to three halogen atoms and the other represents a phenyl or pyridyl ring or N-oxide thereof optionally substituted by one or more substituents selected from halogen atoms and hydroxyl, C.sub.1-3 alkyl, C.sub.1-3 alkoxy and trifluoromethyl groups; wherein R.sup.3 represents a phenyl or pyridyl ring or N-oxide thereof optionally substituted by one or more substituents selected from halogen atoms and hydroxyl, C.sub.1-3 alkyl, C.sub.1-3 alkoxy and trifluoromethyl groups with the proviso that only one of the groups R.sup.1, R.sup.2 or R.sup.3 represents an optionally substituted pyridyl ring; X represents --CH.dbd.CH--; and Z represents ##STR2## wherein R.sup.4 represents a hydrogen atom, a carboxyl protecting group or a cation; and R.sup.5 represents a hydrogen atom or a C.sub.1-3 alkyl group; a solvate thereof, or acid addition salts of compounds wherein R.sup.4 represents a hydrogen atom or a carboxyl protecting group; for use in the treatment and/or prevention of diseases associated with hypercholesteroloma and hyperlipoproteinemia.

Imidazole derivatives and their use as hypercholesterolemia and

A compound of the formula I ##STR1## in which R.sup.1 represents a hydrogen atom or an alkyl group having from 1 to 4 carbon atoms, the --CONHR.sup.1 group being present at the 3- or 4-position on the phenyl ring, and esters thereof at the 2-carboxyl group and/or at the 8-hydroxy group, have antibacterial and/or .beta.-lactamase inhibiting activity.

Antibacterial 7-oxo-4-thia-1-azabicyclo[3,2,0]hept-2-ene derivatives

Intermediate compounds of the formula ##STR1## for the preparation of antibacterially active penem compounds and salts wherein R is hydrogen or an esterifying group, R.sup.1 is an unsubstituted or a mono-, di-, or tri-substituted phenyl, naphthyl, thienyl, pyridyl, quinolyl or isoquinolyl, R.sup.2 is hydrogen or a hydroxyl group which may be protected, R.sup.4 is chlorine or bromine and R.sup.5 is an alkyl or phenyl group; methods for making such compounds or salts.

Intermediate compounds for the preparation of antibacterial penem

The present invention relates to certain penem derivatives of the general formula I ##STR1## in which R represents a hydrogen atom or a carboxyl esterifying group, R.sup.1 represents certain unsubstituted and substituted aromatic and heterocyclic groups, and R.sup.2 represents a hydrogen atom, an unsubstituted or substituted alkyl or aryl group. The compound of formula I and salts thereof may be used in the treatment of bacterial infections in man and other animals.

Antibacterial penem derivatives

Penem-derivatives of the formula I ##STR1## in which R is hydrogen or a carboxyl esterifying group

Compounds of the formula Ia and their tautomers Ib ##STR1## in which formulae R represents a carboxyl esterifying group are described, as well as processes for their manufacture. Ia and Ib are valuable starting materials for the preparation of various derivatives substituted at position 3 that possess antibacterial properties.

7-Oxo-4-thia-1-azabicyclo(3,2,0)heptane derivatives

BIS-Imido carbonate sulphones of the formula: ##STR1## in which R represents phenyl which is unsubstituted or substituted by one or two substituents, which is the same or different, selected from methyl, trifluoromethyl, nitro and cyano groups, and chlorine, flourine and bromine atoms, and p represents the integer 1, are produced by reacting a compound of formula VI ##STR2## in which R is as defined above, with thionyl chloride in the presence of an organic base. The compounds of formula II are useful in the production of 1, 2, 4, 6-thiatriazines.

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Luton, United Kingdom

Barry C Ross