Pharmacia Corporation

Thomas P Kasten

Gilles H Goetz

John J Likos

George G Harrigan

Mark G Currie

William M Moore

Kay Broschat

The present invention is directed toward a composition comprising a compound isolated fromspecies sponges that is capable of inhibiting serine proteases of the coagulation cascade. In particular, this composition inhibits the TF/VIIa complex of the coagulation cascade. The invention is also directed toward methods employing this composition as a part of anticoagulant therapy.

Protease inhibitors of the coagulation cascade isolated from Dysidea sponges

The present invention relates to a rapid high-throughput ion-exchange resin assay for determining enzyme activity. This novel assay uses a radiometric technique which separates the radioactive substrate from the product (or the radioactive product from the substrate) by exploiting the differences in the net charges of the molecules using ion-exchange resin. This assay is useful, for example, for studies of enzyme kinetics, the identification of functional sites in the enzyme, and in the automated screening of compound libraries for pharmaceutical drug development.

Ion-exchange resin/enzyme activity assay

The present invention is directed toward a composition comprising a compound isolated from Dysidea species sponges that is capable of inhibiting serine proteases of the coagulation cascade. In particular, this composition inhibits the TF/VIIa complex of the coagulation cascade. The invention is also directed toward methods employing this composition as a part of anticoagulant therapy.

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O'Fallon, IL, United States of America

Thomas P Kasten