Astrazeneca Ab

Astra Aktiebolag

Astra Ab

David Gustafsson

Jan-Erik Nystr&ouml;m

Jan-Erik Nyström

Jan-Erik Nystrom

Thomas Antonsson

Magnus Polla

Kurt-Jürgen Hoffmann

Kurt-J&uuml;rgen Hoffmann

Ingemar Nilsson

Jonas Brånalt

Mikael Sellen

Henrik Sorensen

Mikael Sellén

Mikael Sell&eacute;n

Henrik S&ouml;rensen

Henrik Sörensen

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

There is provided compounds of formula I,RO(O)C&#x2014;CH&#x2014;(R)Cgl-Aze-Pab-RIwherein Rand Rhave meanings given in the description, which are useful as prodrugs of inhibitors of trypsin-like proteases, such as thrombin, and in particular in the treatment of conditions where inhibition of thrombin is required (eg thrombosis) or as anticoagulants.

Prodrugs of thrombin inhibitors

A kit of parts containing (a) a pharmaceutical formulation including a low molecular weight thrombin inhibitor, or a pharmaceutically acceptable derivative thereof, in admixture with a pharmaceutically acceptable adjuvant, diluent or carrier, and (b) a pharmaceutical formulation including a prodrug of a low molecular weight thrombin inhibitor, or a pharmaceutically acceptable derivative of that prodrug, in admixture with a pharmaceutically acceptable adjuvant, diluent or carrier. Components (a) and (b) are each provided in a form that is suitable for administration in conjunction with the other. The kit is useful in the treatment of conditions in which inhibition of thrombin is required or desired.

Pharmaceutical formulation comprising a low molecular weight thrombin inhibitor and its prodrug

There is provided amino acid derivatives of formula I,wherein p, q, R, R, R, R, Y, n and B have meanings given in the description which are useful as competitive inhibitors of trypsin-like proteases, such as thrombin, and in particular in the treatment of conditions where inhibition of thrombin is required (e.g. thrombosis) or as anticoagulants.

Amino acid derivatives

There is provided compounds of formula I,wherein R, R, R, R, Y, n and B have meanings given in the description which are useful as competitive inhibitors of trypsin-like proteases, such as thrombin, and in particular in the treatment of conditions where inhibition of thrombin is required (e.g. thrombosis) or as anticoagulants.

Amino acid derivatives and their use as thrombin inhibitors

According to the invention there is provided the use of melagatran, or a pharmaceutically-acceptable derivative thereof, for the manufacture of a medicament for the treatment of ischemic disorders in patients having, or at risk of, non-valvular atrial fibrillation.

Use of low molecular weight thrombin inhibitor

There is provided compounds of formula I,

Growing community of inventors

Kullavik, Sweden

David Gustafsson