Hepatitis C Helicase Inhibitors

Multiple effects – Inhibits both the helicase and protease activities of HCV NS3 Broad Acting – Inhibit all HCV genotypes with similar potency Fewer potential side effects – No detectable toxicity in cell culture Compatible with other DAAs– Enhance the effects of telaprevir Combination Potential – Shows synergy in combination with other drugs on market

Hepatitis C in combination with hepatitis B, accounts for about 75% of all liver disease around the world.170-200 million people are infected with HCV worldwide with 3-5 million in the USA. Chronic HCVinfection develops in 70%–85% of HCV-infected persons. 60%–70% of chronically infected persons haveevidence of active liver disease. The global Hepatitis C virus market is attractive due to high levels of unmet need. The unmet need in themarket is approximately 70%, which equals about $3 billion. Some of this market availability is due to thelack of effective options for treatment as well as the lack of treatments with good efficacy and moderate safety profiles. Serious side effects still exist with a majority of the single and combination treatmentsused today. The global Hepatitis C market was worth approximately $4.4 billion in in 2009. It is expectedto reach $9.8 billion by 2016.

The invention consists of new direct acting antivirals (DAAs) that act against the Hepatitis C virus (HCV)replicon and inhibit the NS3 helicase activity. These DAAs are additionally unique compared to otherHCV helicase inhibitors because they are also capable of inhibiting HCV NS3 protease activity.

Non-Confidential Summary

USA