Malonamid and malonamic ester derivatives with antithrombotic activity, their preparation, and their use

US6645992B2 · kind B2 · utility

Assignee

• Aventis Pharma Deutschland GmbH · DE

Inventors

• Manfred Schudok · Eppstein, DE
• Otmar Klingler · Rodgau, DE
• Hans-Peter Nestler · Kelkheim, DE
• Hans Matter · Langenselbold, DE
• Herman Schreuder · Frankfurt am Main, DE

Key dates

• Filing date: Oct 1, 2001
• Grant date: Nov 11, 2003
• Expiry date: Oct 1, 2021

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07C257/20
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

Compounds of formula I, in which R1, R2, A, and B having the definitions set forth in the claims, are valuable pharmacologically active compounds, which exhibit a strong antithrombotic effect and are suitable, for example, for treating thromboembolic diseases and restenoses. They are reversible inhibitors of the blood clotting enzyme factor VIIa and can in general be applied in conditions in which an undesired activity of factor VIIa is present or for the cure or prevention of which an inhibition of factor VIIa is intended. Also disclosed are processes for the preparation of compounds of formula I, their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.