Trypsin-like serine protease inhibitors, and their preparation and use

US8513461B2 · kind B2 · utility

Assignee

• THE MEDICINES COMPANY (LEIPZIG) GMBH · DE

Inventors

• Torsten Steinmetzer · Jena, DE
• Andrea Schweinitz · Jena, DE
• Joerg Stuerzebecher · Erfurt, DE
• Peter Steinmetzer · Jena, DE
• Anett Soeffing · Weimar, DE
• Andreas Van De Locht · Munich, DE
• Silke Nicklisch · Leipzig, DE
• Claudia Reichelt · Leipzig, DE
• Friedrich-Alexander Ludwig · Leipzig, DE
• Alexander Schulze · Bad Liebenwerda, DE
• Mohammed Daghish · Leipzig, DE
• Jochen Heinicke · Leipzig, DE

Key dates

• Filing date: Feb 19, 2013
• Grant date: Aug 20, 2013
• Expiry date: Feb 19, 2033

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07K5/06086
• WIPO field: Organic fine chemistry
• WIPO sector: Chemistry

Abstract

The invention relates to inhibitors of trypsin-like serine proteases, including those of the general formula (IV) which, as well as plasmin, also inhibit plasma kallikrien, and to their use as medicaments, preferably for treatment of blood loss, especially in the case of hyperfibrinolytic states, in organ transplants or heart surgery interventions, in particular with a cardiopulmonary bypass, or as a constituent of a fibrin adhesive.