Glaxo Group Limited

Smithkline Beecham Corporation

Glaxo Wellcome Inc.

Michael John Dawson

David Noble

Nigel Stephen Watson

Mahmoud Mahmoudian

Michael V Hayes

Alan Shuttleworth

Allan Baxter

Robert M Tait

Howard G Wildman

Jesus Chicharro Gonzalo

Christopher John Wallis

Jose R Gomez

Silvestre Garcia-Ochoa Dorado

Federico Gomez De Las Heras

Richard M Hall

Jose J Martin

The present invention relates to a process for the preparation of enantiomerically enriched N-derivatized (1R,4S)-2-azabicyclo&lsqb;2.2.1&rsqb;hept-5-en-3-ones by use of an enzyme.

Process for preparing enantiomerically enriched N-derivatized lactams

A method for the preparation of N-acetyl-D-neuraminic acid (NANA) N-acetyl-D-glucosamine (NAG) is described.

Process for the preparation of N-acetylneuraminic acid

Antifungal sordaridin derivatives

Compounds are described of the formula ##STR1## wherein R.sub.1 represents a hydrogen atom, a hydroxyl group or a group selected from --OCOCH.dbd.CHCH(CH.sub.3)(CH.sub.2).sub.3 CH.sub.3, --OCOCH.dbd.CHC(CH.sub.3).dbd.CHCH(CH.sub.3)--CH.sub.2 CH.sub.3, or --OCO--X--CH.sub.2 CH(CH.sub.3)CH.sub.2 CH.sub.3 [where X is --CH.dbd.CHCH(CH.sub.3)--, --CH.sub.2 CH(OH)CH(CH.sub.3)--, --CH.dbd.CHC(OH)(CH.sub.3)--, --CH.sub.2 CH(OH)CH.sub.2 -- or --CH.sub.2 CH.sub.2 CH(CH.sub.3)--)]; R.sub.2 represents a hydrogen atom or a hydroxyl group; R.sub.3 represents a group selected from --C(.dbd.CH.sub.2)CH(OR.sub.7)CH(CH.sub.3)CH.sub.2 Ph (where R.sub.7 is a hydrogen atom or an acetyl group), --C(CH.sub.3).dbd.CHCH(CH.sub.2 R.sub.8)CH.sub.2 Ph (where R.sub.8 is a hydrogen or a hydroxyl group), --C(CH.sub.2 OH).dbd.CHCH(CH.sub.3)CH.sub.2 Ph, --C(.dbd.CH.sub.2)CH(OH)CH(CH.sub.2 OH)CH.sub.2 Ph, --C(.dbd.CH.sub.2)CH(NHCOCH.sub.3)CH(CH.sub.3)CH.sub.2 Ph, --C(CH.sub.2 NHCOCH.sub.3).dbd.CHCH(CH.sub.3)CH.sub.2 Ph or ##STR2## R.sub.4, R.sub.5 and R.sub.6 may each independently represent a hydrogen atom or a methyl group and salts thereof; with the proviso that when either of R.sub.1 and R.sub.2 represents a hydrogen atom R.sub.3 is a group selected from --C(.dbd.CH.sub.2)CH(OR.sub.7)CH(CH.sub.3)CH.sub.2 Ph and --C(CH.sub.3).dbd.CHCH(CH.sub.3)CH.sub.2 Ph and when both of R.sub.1 and R.sub.2 represent hydrogen atoms R.sub.3 represents --C(CH.sub.3).dbd.CHCH(CH.sub.3)CH.sub.2 Ph. These compounds inhibit the enzyme squalene synthase and/or are intermediates for the preparation of compounds which inhibit the enzyme squalene synthase. Compounds of the invention may be formulated for use in a variety of conditions where a lowering of the level of blood plasma cholesterol in animals would be beneficial and for use in combating fungal infections in animals.

Cyclic ketal derivatives

The invention is directed to a biologically pure culture of the microorganism Phoma sp. IMI 332962 or a mutant thereof.

Growing community of inventors

Stevenage, United Kingdom

Michael John Dawson