Astrazeneca Ab

John Pavey

David Cladingboel

Colin Thomson

Magnus Munck Af Rosenschöld

Gert Strandlund

Peder Svensson

Michael Lundkvist

Hans Lönn

Antonios Nikitidis

Annika Björe

Kurt-Jürgen Hoffmann

Fritiof Pontén

Magnus Björsne

Michael Wilsterman

Martin Lindsjö

Debra Ainge

David Chapman

Emma Anderson

The invention provides certain novel compounds as listed in the specification and pharmaceutically acceptable salts thereof and particular Forms thereof; together with processes for their preparation, pharmaceutical compositions containing them and their use in therapy. The compounds are inhibitors of human neutrophil elastase. The present neutrophil elastase inhibitors include 6-[1-(4-Cyanophenyl)-1H-pyrazol-5-yl]-5-methyl-3-oxo-4-[3-(trifluoromethyl)phenyl]-3,4-dihydropyrazine-2-carboxamide: 

Some 2-pyrazinone derivatives and their use as inhibitors of neutrophile elastase

The present invention concerns a process for the preparation of an N-(4-piperidinyl)-N-ethyl-phenylacetamide of formula (I); wherein Rand Rare independently selected from the group comprising: hydrogen, halogen, Calkyl, Calkoxy, cyano and S(O)(Calkyl).

[object Object]

There is provided a process for the preparation of a compound of formula I, (I), or a pharmaceutically acceptable derivative thereof, wherein A, B, G, R, R, R, Rand Rto Rhave meanings given in the description, which process comprises the dehydrative cyclisaton of a compound of formula II. (II).

Process for the production of oxabispidines

There is provided compounds of formula I, wherein R, R, R, R, Rto R, A, B and G have meanings given in the description, which are useful in the prophylaxis and in the treatment of arrhythmias, in particular atrial and ventricular arrhythmias.

Oxabispidine compounds useful in the treatment of cardiac arrhythmias

There is provided a process for the preparation of a compound of formula I, (I), or a pharmaceutically acceptable derivative thereof, wherein A, B, G, R, R, R, Rand Rto Rhave meanings given in the description, which process comprises the dehydrative cyclisaton of a compound of formula II, (II).

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Leicestershire, United Kingdom

John Pavey