IP Library Granted Patent US 10,414,747
Granted Patent B2
US 10,414,747 · App. 15/722,093 · Granted Sep 17, 2019

Benzo[b]thiophene compounds as sting agonists

Inventors: Michael D. Altman (Needham, MA); Brandon D. Cash (Stoughton, MA); Wonsuk Chang (Princeton, NJ); Jared N. Cumming (Winchester, MA); Andrew M. Haidle (Somerville, MA); Timothy J. Henderson (Natick, MA); James P. Jewell (Newton, MA); Matthew A. Larsen (Dedham, MA); Rui Liang (New Brunswick, NJ); Jongwon Lim (Lexington, MA); Min Lu (Brookline, MA); Ryan D. Otte (Natick, MA); Tony Siu (Brookline, MA); Benjamin Wesley Trotter (Medfield, MA); Sriram Tyagarajan (Edison, NJ)
Assignee: Merck Sharp & Dohme Corp.
C07D333/60C07D333/62C07D409/12C07D498/04
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Quick Facts
Patent No.
US 10,414,747
App. No.
15/722,093
Granted
Sep 17, 2019
Kind
B2
Abstract

Compounds of general formula (Ia), compounds of general formula (Ia′), compounds of general formula (Ib), compounds of general formula (Ib′), compounds of general formula (I), compounds of general formula (I′), and their pharmaceutically acceptable salts, wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 8 , R 9 , X 1 , X 2 , and X 3 are defined herein, that may be useful as inductors of type I interferon production, specifically as STING active agents, are provided. Also provided are processes for the synthesis and use of compounds of the disclosure.

Claims (35)

1. A compound selected from the group consisting of:

or a pharmaceutically acceptable salt thereof.

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

or a pharmaceutically acceptable salt thereof.

3. A pharmaceutical composition comprising a compound, or a pharmaceutically acceptable salt thereof, according to claim 1 , and a pharmaceutically acceptable carrier.

4. A compound selected from the group consisting of

and pharmaceutically acceptable salts thereof.

5. A pharmaceutical composition comprising the compound, or a pharmaceutically acceptable salt thereof, according to claim 4 , and a pharmaceutically acceptable carrier.

6. A compound selected from the group consisting of

7. A pharmaceutical composition comprising the compound, or a pharmaceutically acceptable salt thereof, according to claim 6 , and a pharmaceutically acceptable carrier.

8. A compound selected from the group consisting of

and pharmaceutically acceptable salts thereof.

9. A pharmaceutical composition comprising the compound, or a pharmaceutically acceptable salt thereof, according to claim 8 , and a pharmaceutically acceptable carrier.

10. A compound selected from the group consisting of

11. A pharmaceutical composition comprising the compound, or a pharmaceutically acceptable salt thereof, according to claim 10 , and a pharmaceutically acceptable carrier.

12. A compound selected from the group consisting of

and pharmaceutically acceptable salts thereof.

13. A pharmaceutical composition comprising the compound, or a pharmaceutically acceptable salt thereof, according to claim 12 , and a pharmaceutically acceptable carrier.

14. A compound selected from the group consisting of

15. A pharmaceutical composition comprising the compound, or a pharmaceutically acceptable salt thereof, according to claim 14 , and a pharmaceutically acceptable carrier.

16. A compound selected from the group consisting of

and pharmaceutically acceptable salts thereof.

17. A pharmaceutical composition comprising the compound, or a pharmaceutically acceptable salt thereof, according to claim 16 , and a pharmaceutically acceptable carrier.

18. A compound selected from the group consisting of

19. A pharmaceutical composition comprising the compound, or a pharmaceutically acceptable salt thereof, according to claim 18 , and a pharmaceutically acceptable carrier.

20. A compound selected from the group consisting of

and pharmaceutically acceptable salts thereof.

21. A pharmaceutical composition comprising the compound, or a pharmaceutically acceptable salt thereof, according to claim 20 , and a pharmaceutically acceptable carrier.

22. A compound selected from the group consisting of

23. A pharmaceutical composition comprising the compound, or a pharmaceutically acceptable salt thereof, according to claim 22 , and a pharmaceutically acceptable carrier.

24. A compound selected from the group consisting of

and pharmaceutically acceptable salts thereof.

25. A pharmaceutical composition comprising the compound, or a pharmaceutically acceptable salt thereof, according to claim 24 , and a pharmaceutically acceptable carrier.

26. A compound selected from the group consisting of

27. A pharmaceutical composition comprising the compound, or a pharmaceutically acceptable salt thereof, according to claim 26 , and a pharmaceutically acceptable carrier.

Assignments (2)
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 Apr 11, 2018
From: ALTMAN, MICHAEL D.; CASH, BRANDON D.; CHANG, WONSUK; CUMMING, JARED N.; HAIDLE, ANDREW M.; HENDERSON, TIMOTHY J.; JEWELL, JAMES P.; LARSEN, MATTHEW A.; LIANG, RUI; LIM, JONGWON; LU, MIN; OTTE, RYAN D.; SIU, TONY; TROTTER, BENJAMIN WESLEY; TYAGARAJAN, SRIRAM
To: MERCK SHARP & DOHME CORP.
Reel/Frame 045911/0953 →
Cited By (1)
US 12,269,816