Eli Lilly and Company

Agouron Pharmaceuticals, Inc.

Marlys Hammond

Stephen W Kaldor

James E Fritz

Siegfried Heinz Reich

John E Munroe

Bruce Anthony Dressman

Timothy Alan Shepherd

William Joseph Hornback

John Howard Tatlock

Vincent J Kalish

Michael J Rodriguez

Krzysztof Appelt

Michael J Rodriquez

Method of making HIV protease inhibitors

Compounds useful as intermediates in the preparation of HIV protease inhibitors. These compounds have the following general formula:

HIV protease inhibitors

HIV protease inhibitors, obtainable by chemical synthesis, inhibit or block the biological activity of the HIV protease enzyme, causing the replication of the HIV virus to terminate. These compounds, as well as pharmaceutical compositions that contain these compounds and optically other anti-viral agents as active ingredients, are suitable for treating patients or hosts infected with the HIV virus, which is known to cause AIDS.

Pharmaceutical compositions containing HIV protease inhibitors and

HIV protease inhibitors, obtainable by chemical synthesis, inhibit or block the biological activity of the HIV protease enzyme, causing the replication of the HIV virus to terminate. These compounds, as well as pharmaceutical compositions that contain these compounds and optionally other anti-viral agents as active ingredients, are suitable for treating patients or hosts infected with the HIV virus, which is known to cause AIDS.

HIV protease inhibtors

The present invention provides a group of novel compounds that inhibit the proteolytic activity of 3C proteases which are found in picornaviruses, particularly rhinoviruses. In picornaviruses the RNA genome is translated into a single large viral polyprotein precursor. The precursor demonstrates auto-proteolytic activity, cleaving itself into mature viral gene products. Therefore, compounds of the current invention are particularly useful in treating picornaviral infections by interrupting the processing of the viral gene products into mature and infectious viral particles. The current invention also provides a novel process the preparation of compounds of the current invention. The process entails the selective reduction of an imide intermediate representing a marked improvement over processes known in the art for making peptidyl-aldehydes.

Anti-picornaviral agents

The present invention provides novel HIV protease inhibitors, pharmaceutical formulations containing those compounds and methods of their use.

Intermediates for inhibitors of HIV protease and method of preparation

The present invention provides novel HIV protease inhibitors, pharmaceutical formulations containing those compounds and methods of treating and/or preventing HIV infection and/or AIDS.

Intermediates for preparing HIV protease inhibitors

Retroviral protease inhibitors

Inhibitors of HIV protease useful for the treatment of AIDS

The present invention provides novel HIV protease inhibitors, pharmaceutical formulations containing those compounds and methods of treating HIV infection.

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Pasadena, CA, United States of America

Marlys Hammond