Vertex Pharmaceuticals, Inc.

Michael Stephen Brieger

Roger D Tung

Stephen Colin Price

Michael Robin Hale

Eric Steven Furfine

Istvan Kaldor

Andrew Spaltenstein

Vicente Samano

John Franklin Miller

Wayne Carl Schairer

Robin David Wilkes

Ashley Nicholas Jarvis

Ronald George Sherrill

The present invention relates to a novel class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of HIV aspartyl protease inhibitors characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting HIV-1 and HIV-2 protease activity and consequently, may be advantageously used as anti-viral agents against the HIV-1 and HIV-2 viruses. This invention also relates to methods for inhibiting the activity of HIV aspartyl protease using the compounds of this invention and methods for screening compounds for anti-HIV activity.

Inhibitors of aspartyl protease

The invention provides novel compounds of formula (I)wherein all variables are as defined in the specification, that are useful as inhibitors of aspartyl proteases.

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Greenwood, IN, United States of America

Michael Stephen Brieger