IP Library Granted Patent US 7,816,326
Granted Patent B2
US 7,816,326 · App. 11/733,479 · Granted Oct 19, 2010

Sulfur compounds as inhibitors of hepatitis C virus NS3 serine protease

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Quick Facts
Patent No.
US 7,816,326
App. No.
11/733,479
Granted
Oct 19, 2010
Kind
B2
Abstract

The present invention discloses novel compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of using them to treat disorders associated with the HCV protease.

Claims (18)

1. A compound exhibiting HCV protease inhibitory activity, or an enantiomer, stereoisomer, rotamer, tautomer, or racemate of said compound, or a pharmaceutically acceptable salt or solvate or ester of said compound or of said enantiomer, stereoisomer, rotamer, tautomer, or racemate, said compound being selected from the group consisting of the compounds of structures listed below:

2. A pharmaceutical composition comprising as an active ingredient therapeutically effective amounts of at least one compound of claim 1 .

3. The pharmaceutical composition of claim 2 for use in treating disorders associated with hepatitis C virus (“HCV”).

4. The pharmaceutical composition of claim 2 additionally comprising at least one pharmaceutically acceptable carrier.

5. The pharmaceutical composition of claim 4 , additionally containing at least one antiviral agent.

6. The pharmaceutical composition of claim 5 , still additionally containing at least one interferon.

7. The pharmaceutical composition of claim 6 , wherein said at least one antiviral agent is ribavirin and said at least one interferon is α-interferon or pegylated interferon.

8. A method of treating disorders associated with the HCV, said method comprising administering to a patient in need of such treatment a pharmaceutical composition which comprises therapeutically effective amounts of at least one compound of claim 1 .

9. The method of claim 8 , wherein said administration is oral or subcutaneous.

10. A compound exhibiting HCV protease inhibitory activity, or an enantiomer, stereoisomer, rotamer, tautomer, or racemate of said compound, or a pharmaceutically acceptable salt or solvate or ester of said compound or of said enantiomer, stereoisomer, rotamer, tautomer, or racemate, said compound having the structure:

11. A compound exhibiting HCV protease inhibitory activity, or an enantiomer, stereoisomer, rotamer, tautomer, or racemate of said compound, or a pharmaceutically acceptable salt or solvate or ester of said compound or of said enantiomer, stereoisomer, rotamer, tautomer, or racemate, said compound having the structure:

12. A compound exhibiting HCV protease inhibitory activity, or an enantiomer, stereoisomer, rotamer, tautomer, or racemate of said compound, or a pharmaceutically acceptable salt or solvate or ester of said compound or of said enantiomer, stereoisomer, rotamer, tautomer, or racemate, said compound having the structure:

13. A compound exhibiting HCV protease inhibitory activity, or an enantiomer, stereoisomer, rotamer, tautomer, or racemate of said compound, or a pharmaceutically acceptable salt or solvate or ester of said compound or of said enantiomer, stereoisomer, rotamer, tautomer, or racemate, said compound having the structure:

14. A compound exhibiting HCV protease inhibitory activity, or an enantiomer, stereoisomer, rotamer, tautomer, or racemate of said compound, or a pharmaceutically acceptable salt or solvate or ester of said compound or of said enantiomer, stereoisomer, rotamer, tautomer, or racemate, said compound having

15. A compound exhibiting HCV protease inhibitory activity, or an enantiomer, stereoisomer, rotamer, tautomer, or racemate of said compound, or a pharmaceutically acceptable salt or solvate or ester of said compound or of said enantiomer, stereoisomer, rotamer, tautomer, or racemate, said compound having the structure:

16. A compound exhibiting HCV protease inhibitory activity, or an enantiomer, stereoisomer, rotamer, tautomer, or racemate of said compound, or a pharmaceutically acceptable salt or solvate or ester of said compound or of said enantiomer, stereoisomer, rotamer, tautomer, or racemate, said compound having the structure:

17. A compound exhibiting HCV protease inhibitory activity, or an enantiomer, stereoisomer, rotamer, tautomer, or racemate of said compound, or a pharmaceutically acceptable salt or solvate or ester of said compound or of said enantiomer, stereoisomer, rotamer, tautomer, or racemate, said compound having the structure:

18. A compound of claim 1 in purified form.

Assignments (3)
MERGER Recorded Aug 8, 2022
From: MERCK SHARP & DOHME CORP.
To: MERCK SHARP & DOHME LLC
Reel/Frame 061102/0145 →
CHANGE OF NAME Recorded Aug 30, 2012
From: SCHERING CORPORATION
To: MERCK SHARP & DOHME CORP.
Reel/Frame 028884/0151 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded May 10, 2007
From: VELAZQUEZ, FRANCISCO; BOGEN, STEPHANE L.; ARASAPPAN, ASHOK; VENKATRAMAN, SRIKANTH; NJOROGE, F. GEORGE; SHIH, NENG-YANG
To: SCHERING CORPORATION
Reel/Frame 019276/0251 →