Corvas International, Inc.

Other

Corvas Inc.

Terence Kevin Brunck

Joseph Edward Semple

William Charles Ripka

Marguerita S Lim-Wilby

Robert J Ardecky

Susan Yoshiko Tamura

Yu Ge

Ruth F Nutt

Thomas R Webb

Stephen H Carpenter

Edwin L Madison

Howard R Soule

Daniel A Pearson

Matthew M Abelman

Kent Pryor

Michael G Pepe

David C Rowley

Viyyoor Moopil Girijavallabhan

Ashit K Ganguly

F George Njoroge

Anil K Saksena

Frank W Bennett

Ashok Arasappan

Stephane L Bogen

Raymond G Lovey

Yi-Tsung Liu

Odile Esther Levy

Patrick A Pinto

Russell E Pike

Edwin Jao

Haiyan Wang

David Duncan

Jinping L McCormick

Tejal Parekh

Scott Jeffrey Kemp

Ronald D Lewis, Ii

C Maxwell Lawrence

The present invention discloses novel peptide compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such peptides as well as methods of using them to treat disorders associated with the HCV protease.

Peptides as NS3-serine protease inhibitors of hepatitis C virus

Compounds and pharmaceutical compositions useful as plasminogen activator inhibitor (PAI) antagonists are provided. In particular, methods of antagonizing PAI with substituted and unsubstituted aryl and heteroaryl ethers and thioethers, benzils, benzyl ethers, benzoate esters, sulfones and benzophenones are provided.

Plasminogen activator inhibitor antagonists

Compounds and pharmaceutical compositions useful as plasminogen activator inhibitor (PAI) antagonists are provided. In particular, methods of antagonizing PAI with substituted and unsubstituted aryl and heteroaryl ethers and thioethers are provided.

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

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

Coagulation protein antagonists are disclosed, which include monoclonal-type antibodies and related cell lines disclosed for the production of specific, neutralizing antibodies against factors VII and VIIa and the tissue factor/factor VIIa bimolecular complex, which antibodies are useful for the prevention or treatment of thrombotic and related diseases, for immunoaffinity isolation and purification of factors VII and VIIa and the tissue factor/factor VIIa complex, and for determination of factors VII or VIIa and the tissue factor/factors VII or VIIa complex in a biological sample.

Blood coagulation protein antagonists and uses therefor

The present invention provides peptide aldehydes having an 3-amino-2-hydro yenyl acetamide group as part of the peptide backbone d an arginine group or analog at P1. These compounds e potent and specific or inhibitors of thrombin. Ther pharmaceutically acceptable salts, pharmaceutic ly acceptable compositions thereof, and methods of using t as therapeutic agents for disease states in mammals charachterized by abnormal thrombosis are also described. Also described are 3-amino-2-hydroxyphenyl-acetamide derivatives having in history activity towards proteases of the trypsin/chymotrypsin class.

Substituted 3-amino-2-hydroxyphenylacetamide derivatives as enzyme inhibitors (II)

3-amino-2-oxo-1-piperidnercetic derivatives as enzyme inhibitors

The present invention provides peptide aldehydes having a 3-amino-2-hydroxyphyenyl-acetamide 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 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. Also described are 3-amino-2-hydroxyphenyl-acetamide derivatives having inhibitory activity toward proteases of the trypsin/chymotrypsin class.

Substituted 3-amino-2-hydroxyphenylacetamide derivatives as enzyme

Aromatic hetherocyclic derivatives as enzyme inhibitors

Novel compounds, their salts and compositions related thereto having activity against mammalian factor Xa are disclosed. The novel compounds include peptide aldehyde analogues having substantial potency and specificity as inhibitors of mammalian factor Xa are further disclosed. The compounds are thought useful as inhibitors of factor xa in vitro or as a therapeutic agent for the prevention and treatment of conditions characterized by abnormal thrombosis in mammals. Intermediates useful for the preparation of the novel compounds are also disclosed.

Inhibitors of factor Xa

Novel compounds, their salts and compositions related thereto having activity against mammalian factor Xa are disclosed. The novel compounds include peptide aldehyde analogues having substantial potency and specificity as inhibitors of mammalian factor Xa are further disclosed. The compounds are thought useful as inhibitors of factor Xa in vitro or as a therapeutic agent for the prevention and treatment of conditions: characterized by abnormal thrombosis in mammals. Intermediates useful for the preparation of the novel compounds are also disclosed.

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San Diego, CA, United States of America

Terence Kevin Brunck