Indole derivatives as inhibitors or factor Xa

US6337344B1 · 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
• Fahad Al-Obeidi · Tucson, US
• Armin Walser · Tucson, US
• Peter Wildgoose · Oberursel, DE
• Hans Matter · Langenselbold, DE

Key dates

• Filing date: Aug 14, 2000
• Grant date: Jan 8, 2002
• Expiry date: Aug 14, 2020

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D471/04
• WIPO field: Organic fine chemistry
• WIPO sector: Chemistry

Abstract

The present invention relates to the inhibition of blood clotting proteins, and more particularly, to indole derivatives of formula (I), in which R1a, R1b, R1c R1d, R2, R3, R4 and A are defined as indicated in the claims. The compounds of formula (I) are inhibitors of the blood clotting enzyme factor Xa. The invention also relates to processes for the preparation of the compounds of formula (I), to methods of inhibiting factor Xa activity and of inhibiting blood clotting, to use of the compounds of formula (I) in the treatment and prophylaxis of diseases which can be cured or prevented by the inhibition of factor Xa activity such as thromboembolic diseases, and to the use of the compounds of formula (I) in the preparation of medicaments to be applied in such diseases. The invention further relates to 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/or auxiliary substances.