Smith Kline & French Laboratories Limited

Smithkline Beecham Corporation

The Johns Hopkins University

Sk&f Laboratories Ltd.

Deirdre M Hickey

Albert A Jaxa-Chamiec

Robert John Ife

Dashyant Dhanak

David G Cooper

Colin Andrew Leach

James David Winkler

Floyd Harold Chilton, Iii

David Graham Tew

Virendra P Shah

David Alston

Azetidinone derivatives for the treatment of atherosclerosis

Substituted azetidin-2-ones for treatment of atherosclerosis

Inhibition of inflammatory lipid mediators

Coenzyme A-independent transacylase is required for the release of free arachidonic acid, and the production of arachidonic acid metabolites and platelet activation factor. Blocking of this enzyme inhibits the production of these inflammatory mediators and will be of therapeutic utility in a broad range of allergic and inflammatory diseases and disorders. Compounds are described herein which inhibit the action of CoA-IT and are therefore useful in the treatment of disease states caused thereby.

CoA-IT and PAF inhibitors

Polymethacrylate polymers, pharmaceutical compositions containing them and their use in medicine as cholesterol lowering agents. A particular polymer of the invention is 11-N,N,N-trimethylammonioundecyl methacrylate chloride copolymer.

Compounds

##STR1## Substituted 4,5-diaryl-2-imidazolones of structure (I), in which each group AR is the same or different and is optionally substituted phenyl or optionally substituted heteroaryl; R.sup.1 is hydrogen, alkyl, optionally substituted phenyl or optionally substituted heteroaryl; n is 4 to 12; and X is 5-tetrazolyl, SO.sub.3 H, P(O)(OR).sub.2, P(O)(OH).sub.2 or P(O)(R)(OR) in which R is hydrogen acceptable salt thereof, processes for preparing them, pharmaceutical compositions containing them and their use in therapy, inter alia, in the treatment of cardiovascular disorders.

Substituted 2-imidazolone derivatives, their preparation and

Polystyrene polymers bearing a quaternary ammonium group are disclosed. They are useful in the treatment of hypercholesterolaemia and the prevention of atherosclerosis. A compound of the invention is 6-(N,N-dimethyl-N-octylammonio)hexanoylated polystyrene chloride.

Polystyrene anion exchange polymers

Polystyrene polymers having a quaternised ammonium group and their use in a method of treatment of hypercholesterolaemia. A particular compound of the invention is (N,N-dimethyl-N-dodecyl-ammoniomethylstyrene-ethyl methacrylate-divinylbenzene co-polymer, chloride salt.

Polystyrene anion exchange polymer pharmaceutical composition

Polymers bearing a quaternary ammonium group are disclosed as being useful in lowering serum cholesterol levels in man. A compound of the invention is N,N-dimethyl-N-(2-(N,N-dimethylcarbamoyl)ethyl)-ammoniomethyl-substitut ed polystyrene, chloride salt.

Polymers bearing a quaternary ammonium group are disclosed as being useful in lowering serum cholesterol levels in man. A compound of the invention is N-(2-N,N-dimethylamino)ethyl)-N,N-dimethylammoniomethyl-substituted polystyrene, chloride salt.

Pyridiniomethacrylate polymers are described which are of use in the treatment of elevated serum cholesterol levels. A compound of the invention is cross-linked 3-(N-methyl-3-pyridinio)propyl methacrylate chloride.

Crosslinked pyridinomethacrylate polymers

Polystyrene polymers having a quaternized ammonium group and their use in a method of treatment of hypercholesterolaemia. A particular compound of the invention is N,N-dimethyl-N-dodecylammoniomethyl-substituted polystyrene.

Growing community of inventors

Welwyn, United Kingdom

Deirdre M Hickey