Benzo[b]thiophene compounds as sting agonists

Patent metadata

Field	Value
Publication number	US-10414747-B2
Application number	US-201715722093-A
Country	US
Kind code	B2
Filing date	Oct 2, 2017
Priority date	Oct 4, 2016
Publication date	Sep 17, 2019
Grant date	Sep 17, 2019

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 R1, R2, R3, R4, R5, R6, R8, R9, X1, X2, and X3 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.

First claim

What is claimed is:

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.

Assignees

• Merck Sharp & Dohme

Inventors

• 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

Classifications

• A61P37/04

  Immunostimulants · CPC title

• A61P37/00

  Drugs for immunological or allergic disorders · CPC title

• A61P35/00

  Antineoplastic agents · CPC title

• C07D409/12

  linked by a chain containing hetero atoms as chain links · CPC title

• C07D498/04

  Ortho-condensed systems · CPC title