Corvas International, Inc.

Susan Yoshiko Tamura

William Charles Ripka

Terence Kevin Brunck

Ruth F Nutt

Robert J Ardecky

Joseph Edward Semple

Yu Ge

Stephen H Carpenter

Odile Esther Levy

Thomas R Webb

Matthew M Abelman

Marguerita S Lim-Wilby

Raymond Dagnino, Jr

John Eugene Reiner

Edwin L Madison

The present invention discloses peptide aldehydes which are potent and specific inhibitors of thrombin, their pharmaceutically acceptable salts, pharmaceutically acceptable compositions thereof, and methods of using them as therapeutic agents for disease states in mammals characterized by abnormal thrombosis.

Aromatic heterocyclic derivatives as enzyme inhibitors

Novel inhibitors of urokinase are provided which have an arginine or arginine mimic aldehyde or an arginine ketoamide group at P1. These compounds are useful in vitro for monitoring plasminogen activator levels and in vivo in treatment of conditions which are ameliorated by inhibition of or decreased activity of urokinase.

Title inhibitors of urokinase

Novel compounds having activity inhibitors of urokinase and in reducing or inhibiting blood vessel formation are provided. These compounds have an arginine or arginine mimic aldehyde or an arginine ketoamide group at P1. These compounds are useful in vitro for monitoring plasminogen activator levels and in vivo in treatment of conditions which are ameliorated by inhibition of or decreased activity of urokinase and in treating pathologic conditions wherein blood vessel formation is related to a pathologic condition.

Inhibitors of urokinase and blood vessel formation

Aromatic hetherocyclic derivatives as enzyme inhibitors

The present invention provides peptide aldehydes having an azetidinyl, prolyl or pipecolyl group as part of the peptide backbone and an arginine mimic group such as an amidinopiperidine or amidinophenyl tail. These compounds are potent and specific inhibitors of thrombin. Their pharmaceutically acceptable salts, pharmaceutically acceptable compositions thereof, and methods of using them as therapeutic agents for disease states in mammals characterized by abnormal thrombosis are also described.

Arginine mimic derivatives as enzyme inhibitors

This invention provides solution-phase and solid-phase methods for the synthesis of peptidyl argininals and to �novel! reagents useful therein.

Method of synthesis of peptidyl aldehydes

The present invention discloses heterocyclic aromatic peptide aldehydes which have an oxopyrimidine or oxopyridine group and an argininal tail which are potent and specific inhibitors of thrombin, their pharmaceutically acceptable salts, pharmaceutically acceptable compositions thereof, and methods of using them as therapeutic agents for disease states in mammals characterized by abnormal thrombosis.

The present invention discloses peptide aldehydes which are potent and specific inhibitors of thrombin, their pharmaceutically acceptable salts, pharmaceutically acceptable compositions thereof, and methods of using them as therapeutic agents for disease slates in mammals characterized by abnormal thrombosis.

This invention provides solution-phase methods for the synthesis of peptidyl argininals and to novel reagents useful therein.

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San Diego, CA, United States of America

Susan Yoshiko Tamura