Astrazeneca Ab

Ingemar Nilsson

David Gustafsson

Kenneth Lars Granberg

Magnus Polla

Jonas Brånalt

Emma Bratt

Yantao Chen

This invention relates to novel pharmaceutically useful compounds of formula (I), in particular compounds that are competitive inhibitors of trypsin-like serine proteases, especially thrombin, their use as medicaments, pharmaceutical compositions containing them and synthetic routes to their production. 

Compounds 148

The invention relates to heterocyclic derivatives of formula (I), wherein Ris amino, a group ORor a group &#x2014;Y&#x2014;Rwhere Ris hydrogen or Calkyl, Y is Calkylene, Ris hydrogen, halo, hydroxy, Calkoxy, CalkoxyCalkoxyC, or a group NRRwhere Rand Rare independently selected from hydrogen, Calkyl, hydroxyCalkyl or alkoxyCalkyl, or Rand Rtogether with the nitrogen atom to which they are attached form a saturated 5-6-membered heterocyclic ring which optionally contains an additional heteroatom; n is one or two and each Ris independently selected from halo, haloCalkyl, hydroxy, oxo, amino, Calkylamino or di-Cdialkylamino; or a pharmaceutically acceptable salt thereof. These compounds 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. 

Derivatives of 6-{4-[4-(1H-indole-2-sulphonyl)-piperazin-1-carbonyl-phenyl]}pyradizin-3-one

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Mölndal, Sweden

Ingemar Nilsson