Abbott Gmbh & Co Kg

Basf Aktiengesellschaft

Abbott Laboratories Corporation

Dorit Baucke

Wilfried Hornberger

Helmut Mack

Werner Seitz

Udo Lange

Thomas Zierke

Hans Wolfgang H&ouml;ffken

Thomas Pfeiffer

Gisela Backfisch

Juergen Delzer

The present invention relates to prodrugs of pharmacologically active five-membered heterocyclic amidines from which are produced in vivo compounds which are competitive inhibitors of trypsin-like serine proteases, in particular thrombin and kininogenases such as kallikrein, to the preparation thereof and to the use thereof as medicines. The invention also relates to pharmaceutical compositions which comprise the prodrugs of the active compounds as ingredients, and to the use of the compounds as thrombin inhibitors, anticoagulants and as antiinflammatory agents.

Prodrugs of thrombin inhibitors

Novel five-membered heterocyclic amidines, their preparation and use as competitive inhibitors of trypsin-like serine proteases, especially thrombin and kininogenases such as kallikrein. Pharmaceutical compositions which contain the compounds as active ingredients, and use of the compounds as thrombin inhibitors, anticoagulants and antiinflammatory agents.

Thrombin inhibitors

Dipeptide benzamidine as a kininogenase inhibitor

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Mannheim, Germany

Dorit Baucke