IP Library › Granted Patent US 11,312,715
Granted Patent B2
US 11,312,715 · App. 16/650,967 · Granted Apr 26, 2022

Fused ring derivative as A

Inventors: Kevin X Chen (Shanghai, CN); Kai Zhou (Shanghai, CN); Boyu Hu (Shanghai, CN); Minliang Xiao (Shanghai, CN); Shuhui Chen (Shanghai, CN)
Assignees: CSTONE PHARMACEUTICALS (SUZHOU) CO., LTD.; CSTONE PHARMACEUTICALS (SHANGHAI) CO., LTD.; CSTONE PHARMACEUTICALS
C07D471/04A61P35/00C07D519/00
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Quick Facts
Patent No.
US 11,312,715
App. No.
16/650,967
Granted
Apr 26, 2022
Kind
B2
Abstract

Disclosed are a compound represented by formula (I) or a pharmaceutically acceptable salt thereof, and an application of the compound or slat in preparation of drugs for treating diseases related to an A 2A receptor.

Claims (43)

1. A compound represented by formula (I) or a pharmaceutically acceptable salt thereof,

wherein,

1 or 2 of T 1 , T 2, T 3 and T 4 is N, the rest are independently CH;

each of R 1 is independently selected from H, halogen, OH, NH 2 or C 1-3 alkyl optionally substituted by 1, 2 or 3 R;

each of R 2 is independently selected from H, halogen, OH, NH 2 or C 1-3 alkyl optionally substituted by 1, 2 or 3 R;

n is selected from 0, 1, 2 and 3;

m is selected from 0, 1, 2 and 3;

ring A is selected from 6-10 membered aryl and 5-10 membered heteroaryl;

ring B is selected from phenyl and 5-6 membered heteroaryl;

R is selected from F, Cl, Br, I, OH, NH 2 and CN;

the “hetero” in the 5-6 membered heteroaryl and 5-10 membered heteroaryl are each independently selected from N, O, S, NH, —C(═O)—, —C(═O)O— and —C(═O)NH—;

the number of the heteroatom or heteroatom group is independently selected from 1, 2, 3 and 4.

2. The compound or the pharmaceutically acceptable salt thereof according to claim 1 , wherein each of R 1 is independently selected from H, F, Cl, Br, I, OH, NH 2 , Me and Et, wherein the Me and Et are optionally substituted by 1, 2 or 3 R.

3. The compound or the pharmaceutically acceptable salt thereof according to claim 2 , wherein each of R 1 is independently selected from H, F, Cl, Br, I, OH, NH 2 , Me, CF 3 and Et.

4. The compound or the pharmaceutically acceptable salt thereof according to claim 1 , wherein each of R 2 is independently selected from H, F, Cl, Br, I, OH, NH 2 and Me optionally substituted by 1, 2 or 3 R.

5. The compound or the pharmaceutically acceptable salt thereof according to claim 4 , wherein each of R 2 is independently selected from F, Cl, Br, I, OH, NH 2 and Me.

6. The compound or the pharmaceutically acceptable salt thereof according to claim 1 , wherein ring A is selected from phenyl, pyridyl, quinoxalyl, 1,2,3,4-tetrahydroquinolyl, 3,4-dihydro-2H-benzo[b][1,4]oxazinyl, benzo[d]isoxazolyl, [1 ,2,4]triazolo[4,3-a]pyridyl, 1H-benzo [d][1,2,3]triazolyl, cinnolinyl, quinazolinyl, quinolyl, isoquinolyl, imidazo[1,2-a]pyridyl, [1,2,4]triazolo[1,5-a]pyridyl, 1H-indazolyl and benzo[d]thiazolyl.

7. The compound or the pharmaceutically acceptable salt thereof according to claim 5 , wherein the structural unit

is selected from

8. The compound or the pharmaceutically acceptable salt thereof according to claim 3 , wherein the structural unit

is selected from

9. The compound or the pharmaceutically acceptable salt thereof according to claim 1 , wherein ring B is selected from phenyl, furanyl, thienyl and pyrazolyl.

10. The compound or the pharmaceutically acceptable salt thereof according to claim 9 , wherein the structural unit

is selected from

11. The compound or the pharmaceutically acceptable salt thereof according to claim 5 , wherein the structural unit

is selected from

12. The compound or the pharmaceutically acceptable salt thereof according to claim 1 , wherein the structural unit

is selected from

13. The compound or the pharmaceutically acceptable salt thereof according to claim 1 , which is selected from the group consisting of:

wherein,

R 1 and R 2 are as defined in claim 1 ;

ring C is selected from 5-6 membered heteroaryl and 5-6 membered heterocycloalkyl;

ring D is 5-6 membered heteroaryl;

the “hetero” in the 5-6 membered heteroaryl is selected from N, S and NH;

the “hetero” in the 5-6 membered heterocycloalkyl is NH;

the number of the heteroatom or heteroatom group is independently selected from 1, 2, 3 and 4.

14. The compound or the pharmaceutically acceptable salt thereof according to claim 13 , wherein the structural unit

is selected from

15. The compound or the pharmaceutically acceptable salt thereof according to claim 13 , wherein the structural unit

is selected from

16. A compound or a pharmaceutically acceptable salt thereof, wherein the compound is selected from the group consisting of:

17. A method for treating a disease related to A 2A receptor in a subject in need thereof, comprising administering a therapeutically effective amount of the compound or the pharmaceutically acceptable salt thereof according to claim 1 to the subject, wherein the disease related to A 2A receptor is a colon cancer.

18. A pharmaceutical composition comprising the compound or the pharmaceutically acceptable salt thereof according to claim 1 and a pharmaceutical excipient.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Mar 30, 2020
From: CHEN, KEVIN X; ZHOU, KAI; HU, BOYU; XIAO, MINLIANG; CHEN, SHUHUI
To: CSTONE PHARMACEUTICALS (SUZHOU) CO., LTD.; CSTONE PHARMACEUTICALS (SHANGHAI) CO., LTD.; CSTONE PHARMACEUTICALS
Reel/Frame 052255/0378 →
Priority Claims (2)
CN 201710900542.8 · Sep 28, 2017 · national
CN 201810239824.2 · Mar 21, 2018 · national
Continuity (1)
Related Publication 20200239465A1 · Jul 30, 2020
Cited By (1)
US 12,583,869