Tri-peptide hepatitis C serine protease inhibitors

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Peptide containing doai

Reexamination Certificate

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Reexamination Certificate

active

10849107

ABSTRACT:
The present invention relates to compounds of Formula I, or a pharmaceutically acceptable salt, ester, or prodrug, thereof:which inhibit serine protease activity, particularly the activity of hepatitis c virus (HCV) NS3-NS4A protease. Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis c virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.

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Ingallinella et al, Potent peptide inhibitors of humas hepatitis C virus NS3 protease are obtained by optimizing the cleavage products, Biochemistry (1998) vol. 37, 8906-8914.
March, “Advanced Organinc Chemistry,” 3rdEdition, p. 312.
Llinas-Brunet et al., Peptide-Based Inhibitors of the Hepatitis C Virus Serine Protease, Biorg. Med. Chem., Letters 8 (1998), 1713-1718.
A. Spatola, “Peptide Backbone Modifications: A Structure-Activity Analysis of Peptides Containing Amide Bond Surrogates, Conformational Constraints, and Rela,” Department of Chemistry, University of Louisville, Louisville Kentucky, pp. 267-357, XP 002032461.

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