Antiviral Compounds for the Treatment of HCV

Title:	Antiviral Compounds
Patent Application Number:	WO2013124335	Publication date:	August 29, 2013
Priority Application:	US61/602,687	Priority date:	February 21, 2012
Inventors:	Cheung, Adrian Wai-Hing; Schoenfeld, Ryan Craig; Yun, Weiya; Zhao, Shu-Hai.
Assignee Company:	F. Hoffmann-La Roche, AG
Disease Area:	Viral Infection	Biological Target:	Hepatitis C
Summary:	Hepatitis C viral (HCV) infection remains a major global health issue despite decades of research devoted to identifying novel treatments for patients in need. The current standard of care, pegylated interferon-α in combination with ribazirin, is associated with a variety of side effects. The identification of novel therapeutics capable of treating HCV infection in the absence of interferon-α could be accomplished with therapies that disrupt viral replication. Direct acting antivirals (DAAs) therapies capable of inhibiting NS3 protease and NS5A protease have been identified, but viral resistance has been an issue. Additional therapeutically useful compounds are necessary. The compounds described in the present application are capable of inhibiting viral replication and are claimed as useful for the treatment of HCV infection, either alone or in combination with other antiviral agents.
Important Compound Classes:
Definitions:	Q is phenyl or naphthalene substituted with one or more Q′;
	Q′ is hydroxyl, lower alkyl, or halo;
	Rl is lower alkyl, cycloalkyl, phenyl, or heterocycloalkyl;
	R2 is −C(=O)OR2′, −C(=O)R2′, −C(=O)ON(R2)2′ monocyclic or bicyclic heteroaryl, optionally substituted with one or more R2′;
	Each R2′ is independently H, lower alkyl, or heterocycloalkyl;
	R3 is H or lower alkyl; and
	X is CH2 or C(=O);
	n is 1 or 2;
Key Structures:
Recent Review Articles:	1. Kiser J. J.; Flexner C.. Direct-acting antiviral agents for hepatitis C virus infection. Annu. Rev. Pharmacol. Toxicol. 2013, 53, 427–449.
	2. Casey L. C.; Lee W. M.. Hepatitis C virus therapy update 2013. Curr. Opin. Gastroenterol. 2013, 29 (3), 243–249.
Biological Assay:	HCV GtaT1b inhibitory replicon activity assay, luciferase reporter system.
Biological Data:
Claims:	18 Total claims.
	11 Composition of matter claims.
	7 Method of use claims.

The authors declare no competing financial interest.