IP Library › Granted Patent US 10,980,825
Granted Patent B2
US 10,980,825 · App. 16/185,258 · Granted Apr 20, 2021

Cyclic dinucleotide

Inventors: Masato Yoshikawa (Fujisawa Kanagawa, JP); Morihisa Saitoh (Fujisawa Kanagawa, JP); Taisuke Kato (Fujisawa Kanagawa, JP); Yayoi Nakayama (Fujisawa Kanagawa, JP); Tomohiro Seki (Fujisawa Kanagawa, JP); Yasuo Nakagawa (Fujisawa Kanagawa, JP); Yusuke Tominari (Fujisawa Kanagawa, JP); Masaki Seto (Fujisawa Kanagawa, JP); Akito Shibuya (Fujisawa Kanagawa, JP); Kosuke Hidaka (Fujisawa Kanagawa, JP); Zenyu Shiokawa (Fujisawa Kanagawa, JP); Yoshihisa Nakada (Fujisawa Kanagawa, JP); Michiyo Mochizuki (Fujisawa Kanagawa, JP)
Assignee: Takeda Pharmaceutical Company Limited
A61K31/7084A61K31/7076A61K47/6807A61P35/00C07H21/00C07H21/02
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Quick Facts
Patent No.
US 10,980,825
App. No.
16/185,258
Granted
Apr 20, 2021
Kind
B2
Abstract

The present disclosure provides a compound having a STING agonistic activity, which may be expected to be useful as an agent for the prophylaxis or treatment of STING-related diseases. The present disclosure relates to a compound represented by the formula (I): wherein each symbol is as defined in the description, or a salt thereof.

Claims (36)

1. A compound having Formula (X):

R and R 2 are each independently a hydroxy group or a halogen atom;

B 1 consists of:

R 18 is hydrogen or C 1-6 alkyl;

R 19 is a halogen atom;

B 2 is:

and

Q 2 and Q 4 are each independently an oxygen atom or a sulfur atom,

or a pharmaceutically acceptable salt thereof.

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

or a pharmaceutically acceptable salt thereof.

3. The compound of claim 2 , wherein the compound is:

or a pharmaceutically acceptable salt thereof.

4. The compound of claim 2 , wherein the compound is:

or a pharmaceutically acceptable salt thereof.

5. The compound of claim 2 , wherein the compound is:

or a pharmaceutically acceptable salt thereof.

6. The compound of claim 2 , wherein the compound is:

or a pharmaceutically acceptable salt thereof.

7. The compound of claim 2 , wherein the compound is:

or a pharmaceutically acceptable salt thereof.

8. The compound of claim 2 , wherein the compound is:

or a pharmaceutically acceptable salt thereof.

9. The compound of claim 2 , wherein the pharmaceutically acceptable salt is the triethylamine salt.

10. The compound of claim 2 , wherein the pharmaceutically acceptable salt is the sodium salt.

11. A pharmaceutical composition comprising the compound of claim 1 , or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable excipient.

12. A method of treating a patient comprising administering to the patient a therapeutically effective amount of the compound of claim 1 , or a pharmaceutically acceptable salt thereof, wherein the patient has cancer, wherein the activation of STING (stimulator of interferon genes) by said compound suppresses cancer cell growth in said cancer.

13. The compound of claim 1 , wherein R 19 is fluoro, or the compound is a pharmaceutically acceptable salt thereof.

14. The compound of claim 1 , wherein R 1 is a hydroxy group or a fluoro atom, or the compound is a pharmaceutically acceptable salt thereof.

15. The compound of claim 1 , wherein R 2 is a hydroxyl group or a fluoro atom, or the compound is a pharmaceutically acceptable salt thereof.

16. The compound of claim 1 , wherein Q 4 is a sulfur atom, or the compound is a pharmaceutically acceptable salt thereof.

17. The compound of claim 1 , wherein Q 2 is an oxygen atom, or the compound is a pharmaceutically acceptable salt thereof.

18. The compound of claim 1 , wherein Q 2 is a sulfur atom, or the compound is a pharmaceutically acceptable salt thereof.

19. The compound of claim 1 , wherein the compound has the formula (XII):

or a pharmaceutically acceptable salt thereof.

20. The compound of claim 1 , wherein R 18 is hydrogen or methyl, or the compound is a pharmaceutically acceptable salt thereof.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded May 19, 2023
From: YOSHIKAWA, MASATO; SAITOH, MORIHISA; KATO, TAISUKE; YOSHITOMI, YAYOI; SEKI, TOMOHIRO; NAKAGAWA, YASUO; TOMINARI, YUSUKE; SETO, MASAKI; SHIBUYA, AKITO; HIDAKA, KOSUKE; SHIOKAWA, ZENYU; NAKADA, YOSHIHISA; MOCHIZUKI, MICHIYO
To: TAKEDA PHARMACEUTICAL COMPANY LIMITED
Reel/Frame 063709/0830 →
Priority Claims (2)
JP 2016-234553 · Dec 1, 2016 · national
JP 2017-107216 · May 30, 2017 · national
Continuity (3)
Continuation PCTIB2017057588 · Dec 1, 2017
Provisional Application 62589300 · Nov 21, 2017
Related Publication 20190192549A1 · Jun 27, 2019
Cited By (2)
US 12,221,460 US 12,678,512