Malonic acid derivatives, processes for their preparation, for their use and pharmaceutical compositions containing them

US6395737B1 · kind B1 · utility

Assignee

• Aventis Pharma Deutschland GmbH · DE

Inventors

• Elisabeth Defossa · Idstein, DE
• Uwe Heinelt · Wiesbaden, DE
• Otmar Klingler · Rodgau, DE
• Gerhard Zoller · Blankenloch, DE
• Hans Matter · Langenselbold, DE
• Fahad Al-Obeidi · Tucson, US
• Armin Walser · Tucson, US
• Peter Wildgoose · Oberursel, DE

Key dates

• Filing date: Dec 28, 1999
• Grant date: May 28, 2002
• Expiry date: Dec 28, 2019

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07C279/14
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

New compounds for the inhibition of blood clotting proteins, and more particularly, to malonic acid derivatives of the formula I, wherein R(1), R(2), R(3), R(4), R(5), and R(6) have the meanings indicated in the claims. The compounds of formula I are inhibitors of the blood clotting enzyme factor Xa. Processes for the preparation of the compounds of formula I, methods of inhibiting factor Xa activity and of inhibiting blood clotting, use of the compounds of formula I in the treatment and prophylaxis of diseases, which can be treated or prevented by the inhibition of factor Xa activity such as thromboembolic diseases, and use of the compounds of formula I in the preparation of medicaments to be applied in such diseases. Compositions containing a compound of formula I in admixture or otherwise in association with an inert carrier, in particular pharmaceutical compositions containing a compound of formula I together with pharmaceutically acceptable carrier substances and auxiliary substances.