Biphenylderivatives of benzamidine as Factor Xa inhibitors

Abstract

The protease Factor Xa has a critical function in the coagulation cascade, since it activates the clot forming protease, thrombin. Consequently, Factor Xa has emerged as an attractive target for the development of antithrombotic drugs. Amidino-biphenyl compounds were identified as highly potent inhibitors of Factor Xa with favourable pharmacological properties. The discussed patent claims the synthesis of biphenyl derivatives as building blocks for the synthesis of Factor Xa inhibitors. Procedures for the synthesis of biphenyl derivatives with amidino groups as substituents in meta and para positions of the aromatic ring are outlined in the application. However, the scope of substituents listed in the application is large, resulting in a highly diverse group of compounds covered. No data were included to demonstrate the potency of the claimed compounds.

• anticoagulant
• biphenyl derivative
• Factor Xa
• inhibitors