Zeneca Limited

Astrazeneca Ab

Anthony Michael Slater

David Huw Davies

Peter R Marsham

David Charles Blakey

John Frederick Hennam

Laurent Francois Andre Hennequin

Francis Thomas Boyle

Robert I Dowell

Roger James

Stuart Eric Pearson

David William Heaton

Laurent Francois Hennequin

Rolf Peter Walker

Hendrikus Johannes Eggelte

Peter Wr Caulkett

Christopher John Taylorson

Brian Robert Rabin

Antonio Tarragona-Fiol

The invention relates to heterocyclic derivatives of formula (I), or pharmaceutically-acceptable salts thereof, which possess antithrombotic and anticoagulant properties and are accordingly useful in methods of treatment of humans or animals. The invention also relates to processes for the preparation of the heterocyclic derivatives, to pharmaceutical compositions containing them and to their use in the manufacture of medicaments for use in the production of an antithrombotic or anticoagulant effect.

Heterocyclic derivatives which inhibit factor Xa

Antibody Directed Enzyme Prodrug Therapy (ADEPT) systems for use in cancer based on mutated carboxypeptidase B (CPB) enzymes. Enzyme conjugates for ADEPT are substantially non-immunogenic in humans comprising a targeting moiety (for example an antibody) capable of binding with a tumor associated antigen, the targeting moiety being linked to a mutated form of a CPB enzyme capable of converting a prodrug into an antineoplastic drug wherein the prodrug is not significantly convertible into antineoplastic drug in humans by natural unmutated enzyme. A preferred enzyme mutant is human pancreatic CPB comprising a Lys or Arg residue at position 253. Suitable mustard prodrugs are disclosed in the specification.

Chemical compounds

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Macclesfield, United Kingdom

Anthony Michael Slater