IP Library Granted Patent US 9,549,917
Granted Patent B2
US 9,549,917 · App. 14/343,448 · Granted Jan 24, 2017

Heterocyclic-substituted benzofuran derivatives and methods of use thereof for the treatment of viral diseases

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Quick Facts
Patent No.
US 9,549,917
App. No.
14/343,448
Granted
Jan 24, 2017
Kind
B2
Abstract

The present invention relates to compounds of formula (I) that are useful as hepatitis C virus (HCV) NS5B polymerase inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5B polymerase activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system.

Claims (22)

1. A compound having the formula:

or a pharmaceutically acceptable salt thereof, wherein:

the group

is selected from:

R 4 is H, —N(R 6 )SO 2 R 7 or

R 6 is C 1 -C 6 alkyl or C 1 -C 6 haloalkyl; and

R 7 is independently C 1 -C 6 alkyl.

2. The compound of claim 1 , wherein R 4 is —N(CH 3 )SO 2 CH 3 .

3. The compound of claim 1 , wherein the group

is selected from:

4. A compound having the structure:

or a pharmaceutically acceptable salt thereof.

5. A pharmaceutical composition comprising a pharmaceutically acceptable carrier and a compound of claim 1 or a pharmaceutically acceptable salt thereof.

6. The pharmaceutical composition of claim 5 , further comprising a second therapeutic agent selected from the group consisting of HCV antiviral agents, immunomodulators, and anti-infective agents.

7. The pharmaceutical composition of claim 6 , wherein the second therapeutic agent is selected from the group consisting of HCV protease inhibitors, HCV NS5A inhibitors and HCV NS5B polymerase inhibitors.

8. A method of treating a patient infected with HCV, the method comprising administering to the patient the compound of claim 1 , or a pharmaceutically acceptable salt thereof, in an amount effective to treat infection by HCV in the patient.

9. The method of claim 8 , further comprising the step of administering pegylated-interferon alpha and ribovirin to the patient.

10. A pharmaceutical composition comprising a pharmaceutically acceptable carrier and a compound of claim 4 or a pharmaceutically acceptable salt thereof.

11. The pharmaceutical composition of claim 10 , further comprising a second therapeutic agent selected from the group consisting of HCV antiviral agents, immunomodulators, and anti-infective agents.

12. The pharmaceutical composition of claim 11 , wherein the second therapeutic agent is selected from the group consisting of HCV protease inhibitors, HCV NS5A inhibitors and HCV NS5B polymerase inhibitors.

13. A method of treating a patient infected with HCV, the method comprising administering to the patient the compound of claim 4 , or a pharmaceutically acceptable salt thereof, in an amount effective to treat infection by HCV in the patient.

14. The method of claim 13 , further comprising the step of administering pegylated-interferon alpha and ribovirin to the patient.

Assignments (5)
MERGER Recorded Aug 8, 2022
From: MERCK SHARP & DOHME CORP.
To: MERCK SHARP & DOHME LLC
Reel/Frame 061102/0145 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Nov 20, 2014
From: HABERMANN, JOERG; KOCH, UWE; NARJES, FRANK
To: MSD ITALIA S.R.L.
Reel/Frame 034219/0507 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Nov 20, 2014
From: LI, PENG; PENG, XUANJIA; SOLL, RICHARD; WU, HAO
To: WUXI APPTEC CO., LTD.
Reel/Frame 034220/0661 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Nov 20, 2014
From: WUXI APPTEC CO., LTD.
To: MERCK SHARP & DOHME CORP.
Reel/Frame 034221/0535 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Nov 17, 2014
From: MCCOMAS, CASEY C.; LIVERTON, NIGEL J.; PALANI, ANANDAN; DAI, XING; LIU, HONG; HE, SHUWEN; LAI, ZHONG; DANG, QUN; ZORN, NICOLAS
To: MERCK SHARP & DOHME CORP.
Reel/Frame 034188/0707 →