HEPATITIS C VIRUS INHIBITOR AND USES THEREOF

• US 20190135828A1
• Filed: 12/21/2018
• Published: 05/09/2019
• Est. Priority Date: 06/21/2016
• Status: Active Grant

• Current Assignee: Zhejiang Palo Alto Pharmaceuticals, Inc.
• Original Assignee: Zhejiang Palo Alto Pharmaceuticals, Inc.
• Inventors: XI, Zhijian, XU, Huaqiang, LU, Chunping
• Granted Patent: US 10,640,515 B2
• Time in Patent Office: Days
• CPC Class Codes: A61K 38/05 Dipeptides
• CPC Class Codes: A61P 31/14 for RNA viruses
• CPC Class Codes: C07D 498/04 Ortho-condensed systems

Abstract

Disclosed is a compound of formula (I) as an inhibitor of hepatitis C virus (HCV), or an optical isomer, a pharmaceutically acceptable salt, a hydrate or a solvate thereof, usable to treat HCV infections or hepatitis C diseases, and is also useful as an inhibitor of HCV non-structural protein 5A (NS5A).

Claims

1. A compound of formula (I-a)

2. The compound of claim 1, wherein the compound is selected from the group consisting of

3. The compound of claim 2, wherein the compound comprises a stereoisomer thereof.

4. A pharmaceutical composition comprising a therapeutically effective amount of the compound of claim 1 or an optical isomer, a pharmaceutically acceptable salt, a hydrate or a solvate thereof, and a pharmaceutically acceptable auxiliary, diluent or carrier.

5. The pharmaceutical composition of claim 4, further comprising at least one HCV inhibitor for inhibiting HCV replication process and/or function of HCV protein.

6. The pharmaceutical composition of claim 4, wherein the HCV replication process comprises HCV entry, HCV uncoating, HCV transcription, HCV replication, HCV assembly and/or HCV release.

7. The pharmaceutical composition of claim 4, wherein the HCV protein is selected from the group consisting of NS2, NS3, NS4A, NS4B, NS5A and NS5B.

8. A method of preparing the compound of claim 1, comprising:

(a) reacting compound 1 with diphenylmethanimine in an inert solvent to form compound 2