Hcv ns-3 serine protease inhibitors

C - Chemistry – Metallurgy – 07 – K

Patent

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Details

C07K 5/02 (2006.01) A61K 31/47 (2006.01) A61P 31/12 (2006.01) C07D 245/04 (2006.01) C07D 401/12 (2006.01) C07D 417/14 (2006.01) C07D 487/04 (2006.01)

Patent

CA 2552319

Peptidomimetic compounds are described which inhibit the NS3 protease of the hepatitis C virus (HCV). The compounds have the formula where the variable definitions are as provided in the specification. The compounds comprise a carbocyclic P2 unit in conjunction with a novel linkage to those portions of the inhibitor more distal to the nominal cleavage site of the native substrate, which linkage reverses the orientation of peptidic bonds on the distal side relative to those proximal to the cleavage site.

L'invention concerne des composés peptidomimétiques qui inhibent la NS3 protéase du virus de l'hépatite C (VHC). Lesdits composés sont représentés par la formule (VI) dans laquelle les définitions de variable sont telles que prévues dans la spécification. Ces composés comprennent une unité carbocyclique P2 associée à une nouvelle liaison avec les parties de l'inhibiteur les plus distales du site de clivage natif du substrat natif, ladite liaison inversant le sens des liaisons peptidiques sur le côté distal par rapport aux parties qui sont proximales au site de clivage.

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