Corvas International, Inc.

St. Jude Children's Research Hospital

Chembridge Corporation

Corvas Inc.

Thomas R Webb

George Phillip Vlasuk

Matthew M Abelman

Daniel A Pearson

William Charles Ripka

Terence Kevin Brunck

Todd Anthony Miller

Sergey Zozulya

Tong Zhu

Alexander Chucholowski

Vlad Edward Gregor

Jason Conrad Pickens

Susan Yoshiko Tamura

Yahua Liu

Raymond Dagnino, Jr

John Eugene Reiner

Vidyasagar Gantla

Luyong Jiang

Zheng Yan

Douglas Eric McGrath

Alexey Vyacheslavovich Anikin

Charles Chamchoumis Mikel

Michael G Pepe

Danny Peter Claude McGee

Chandraiah Lagisetti

Ruth F Nutt

Rajendran Vairagoundar

Sergey Sviridov

Vincent A Boyd

Mohan Santhanam Thiruvazhi

Goverdhan Reddy Vavilala

Aleksander Kadushkin

Alexander Kadushkin

Vidyasagar Reddy Gantla

Jason C Pickens

Alexey Anikin

Danny Peter Mcgee

Charles Mikel

Douglas Eric Mcgrath

Danny Peter Claude Mcgee

In one aspect, the invention relates to compounds having anticancer activity; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating disorders associated with uncontrolled cellular proliferation using the compounds and compositions. This abstract is intended to be used as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

Anticancer compounds

In one aspect, the invention relates to novel, broad-spectrum anti-viral, pyrimidinone compounds, methods of use, compositions and kits useful in treating and/or preventing influenza. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

Pyrimidinone compounds and methods for treating influenza

Anticancer compounds and methods of making and using same

The present invention provides compounds capable of modulating tyrosine kinases, compositions comprising the compounds and methods of their use.

Heterocyclic compounds useful in the treatment of neoplastic diseases, inflammatory disorders and immunomodulatory disorders

Provided are compounds of the formula (I): or a stereoisomer, tautomer, salt, hydrate or prodrug thereof that modulate tyrosine kinase activity, compositions comprising the compounds and methods of their use.

Tricyclic compound derivatives useful in the treatment of neoplastic diseases, inflammatory disorders and immunomodulatory disorders

This invention relates to peptide aldehyde analogs that inhibit the thrombin or Factor Xa. The compounds are thought useful for preventing or treating conditions in mammal characterized by abnormal thrombosis.

Inhibitors of thrombosis

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

The present invention is directed to novel arginine alpha-keto-amide derivatives, their pharmaceutically acceptable salts and compositions thereof which are useful as antithrombotic agents in mammals and also the use of these compounds as antithrombotic agents. Also, described are methods of using these inhibitors as inhibitors of coagulation proteases and as therapeutic agents for disease states characterized by abnormal thrombus formation and/or disorders of the blood coagulation process. Further described herein are compounds useful as intermediates in the preparation of these compounds.

Arginine keto-amide 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.

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

Novel compounds having activity against trypsin are disclosed. Specifically, novel peptide aldehyde analogues that have substantial potency and specificity as inhibitors of mammalian pancreatic trypsin are presented. The compounds are useful in the prevention and treatment of the tissue damage or destruction associated with pancreatitis.

Trypsin Inhibitors

a-Ketoamide derivatives, their pharmaceutically acceptable salts, compositions, diagnostic compositions and pharmaceutical compositions, which are useful for preventing or treating in a mammal a pathological condition characterized by thrombosis are described. a-Ketoamide derivatives, their pharmaceutically acceptable salts, compositions and diagnostic compositions, which are useful for in vivo imaging of thrombi in a mammal are also described. Methods of preventing or treating in a mammal a pathological condition characterized by thrombosis and methods of in vivo imaging of thrombi in a mammal are also disclosed.

.alpha.-ketoamide derivatives as inhibitors of thrombosis

.alpha.-Ketoamide derivatives, their pharmaceutically acceptable salts, compositions, diagnostic compositions and pharmaceutical compositions, which are useful for preventing or treating in a mammal a pathological condition characterized by thrombosis are described. .alpha.-Ketoamide derivatives, their pharmaceutically acceptable salts, compositions and diagnostic compositions, which are useful for in vivo imaging of thrombi in a mammal are also described. Methods of preventing or treating in a mammal a pathological condition characterized by thrombosis and methods of in vivo imaging of thrombi in a mammal are also disclosed.

The present invention is directed to N-sulfonyl arginine alpha-keto-amide derivatives, their pharmaceutically acceptable salts and compositions thereof which are useful as antithrombotic agents in mammals and also the use of these compounds as antithrombotic agents. Also, disclosed are methods of using these inhibitors in their various embodiments as therapeutic agents for disease states characterized by disorders of the blood coagulation process. Further disclosed are compounds useful as intermediates in the preparation of these compounds.

N-sulfonylarginine keto-amide compounds

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Encinitas, CA, United States of America

Thomas R Webb