Beecham Group Plc

Smithkline Beecham Corporation

Keith H Baggaley

Richard M Hindley

Brian Morgan

David Edward Thorne

Frederick Cassidy

Stefan Roland Woroniecki

Arthur W Tyrrell

Stephen W Elson

Barbara Nunn

Christopher Joseph Schofield

Jack Edward Baldwin

Alison Jane Earl

William Henry Holms

David Michael Mousdale

Stephen William Elson

Neville Hubert Nicholson

Jeffrey Edwards

Process for producing clavulanic acid

A compound having the formula (I): ##STR1## is described, together with salts thereof and an enzymatic process for converting such compounds into clavulanic acid. A process for the preparation of the compound of formula (I) and its salts is disclosed, together with intermediates for use therein. This process involves the use of a novel enzyme system to effect the desired cyclisation, which enzyme system is preferably derived from a micro-organism, in particular a species of Streptomyces.

Clavam derivatives and its enzymatic preparation

A compound having the formula (I): ##STR1## is described, together with salts thereof and an enzymatic process for converting such compounds into clavulanic acid. A process for the preparation of the compound of formula (I) and its salts is disclosed, together with intermediates for use therein. This process involves the use of a novel enzyme system to effect the desired cyclization, which enzyme system is preferably derived from a micro-organism, in particular a species of Streptomyces.

Novel clavam derivatives and methods of making same

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.

Hypolipidaemic compounds

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.

Method of inhibiting platelet aggregation

An intermediate compound which is a perhydrofuro [3,2-6] pyrrole of the formula: ##STR1## wherein: R.sub.2 is hydrogen or C.sub.1-4 alkyl; and

Prostacyclin aza analogue intermediates

A compound of formula (I): ##STR1## wherein: A is &gt;CH-- and n is 1 to 6; or

2,4-Disubstituted 5-oxo-5H-hexahydrofuro[3,2b]pyrroles

2-Substituted benzisothiazolones

2-Substituted benzisothiazolones and use thereof

Hypolipidaemic compounds and compositions

The compound 2-[gamma-(1-piperidinyl)propyl]-1,2-benzisothiazole-3-one or a pharmaceutically acceptable acid addition salt thereof and pharmaceutical compositions containing an effective amount of such compound or salt and a carrier, preferably compositions in orally administrable form. The compound or salt is characterized by antithrombotic activity, especially for inhibiting platelet aggregation. Procedures for preparation of the compound are described.

2-[Gamma-(1-piperidinyl)propyl]-1,2-benzisothiazole-3-one, its salts,

A method for the prophylaxis or treatment of thromboses in humans which comprises administering to a human in need thereof a therapeutically effective amount of a compound of the formula (II) ##STR1## or a pharmaceutically acceptable acid addition salt thereof, wherein R is 1-piperidyl or 1-pyrrolidyl. Compounds of the formula (II) are also useful for the inhibition of platelet aggregation in vitro or in vivo.

Prophylaxis or treatment of thromboses and inhibition of platelet

A class of di-(substituted phenoxy) alkanes having from 7 to 25 carbon atoms in the alkane moiety have hypolipidaemic activity.

Growing community of inventors

Redhill, United Kingdom

Keith H Baggaley