IP Library Granted Patent US 11,851,426
Granted Patent B2
US 11,851,426 · App. 17/067,203 · Granted Dec 26, 2023

Bicyclic amines as CDK2 inhibitors

Inventors: Yingda Ye (Wilmington, DE); Zhenwu Li (Wilmington, DE); Ding-Quan Qian (Newark, DE); Sarah Winterton (Wilmington, DE); Liangxing Wu (Wilmington, DE); Wenqing Yao (Chadds Ford, PA)
Assignee: Incyte Corporation
C07D471/04A61P35/00C07D487/04C07D519/00
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Quick Facts
Patent No.
US 11,851,426
App. No.
17/067,203
Granted
Dec 26, 2023
Kind
B2
Abstract

The present application provides bicyclic amines that are inhibitors of cyclin-dependent kinase 2 (CDK2), as well as pharmaceutical compositions thereof, and methods of treating cancer using the same.

Claims (20)

1. A compound, which is 8-ethoxy-N-((3R,4S)-3-methyl-1-(methylsulfonyl)piperidin-4-yl)-7-(1H-pyrazol-4-yl)-[1,2,4]triazolo[1,5-a]pyridin-2-amine, or a pharmaceutically acceptable salt thereof.

2. The compound of claim 1 , which is 8-ethoxy-N-((3R,4S)-3-methyl-1-(methylsulfonyl)piperidin-4-yl)-7-(1H-pyrazol-4-yl)-[1,2,4]triazolo[1,5-a]pyridin-2-amine.

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

4. A pharmaceutical composition comprising the compound of claim 2 and a pharmaceutically acceptable carrier.

5. A compound, which is N-((3R,4S)-1-(cyclopropylsulfonyl)-3-methylpiperidin-4-yl)-8-ethoxy-7-(1H-pyrazol-4-yl)-[1,2,4]triazolo[1,5-a]pyridin-2-amine, or a pharmaceutically acceptable salt thereof.

6. The compound of claim 5 , which is N-((3R,4S)-1-(cyclopropylsulfonyl)-3-methylpiperidin-4-yl)-8-ethoxy-7-(1H-pyrazol-4-yl)-[1,2,4]triazolo[1,5-a]pyridin-2-amine.

7. A pharmaceutical composition comprising the compound of claim 5 , or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier.

8. A pharmaceutical composition comprising the compound of claim 6 and a pharmaceutically acceptable carrier.

9. A compound, which is 8-isopropoxy-N-((3R,4S)-3-methyl-1-(methylsulfonyl)piperidin-4-yl)-7-(1H-pyrazol-4-yl)-[1,2,4]triazolo[1,5-c]pyrimidin-2-amine, or a pharmaceutically acceptable salt thereof.

10. The compound of claim 9 , which is 8-isopropoxy-N-((3R,4S)-3-methyl-1-(methylsulfonyl)piperidin-4-yl)-7-(1H-pyrazol-4-yl)-[1,2,4]triazolo[1,5-c]pyrimidin-2-amine.

11. A pharmaceutical composition comprising the compound of claim 9 , or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier.

12. A pharmaceutical composition comprising the compound of claim 10 and a pharmaceutically acceptable carrier.

13. A compound, which 8-(ethoxy-d5)-N-((3R,4S)-3-methyl-1-(methylsulfonyl)piperidin-4-yl)-7-(1H-pyrazol-4-yl)-[1,2,4]triazolo[1,5-a]pyridin-2-amine, or a pharmaceutically acceptable salt thereof.

14. The compound of claim 13 , which 8-(ethoxy-d5)-N-((3R,4S)-3-methyl-1-(methylsulfonyl)piperidin-4-yl)-7-(1H-pyrazol-4-yl)-[1,2,4]triazolo[1,5-a]pyridin-2-amine.

15. A pharmaceutical composition comprising the compound of claim 13 , or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier.

16. A pharmaceutical composition comprising the compound of claim 14 and a pharmaceutically acceptable carrier.

17. A compound, which is 8-isopropoxy-N-((3R,4S)-3-methyl-1-(methylsulfonyl)piperidin-4-yl)-7-(1H-pyrazol-4-yl)-[1,2,4]triazolo[1,5-a]pyridin-2-amine, or a pharmaceutically acceptable salt thereof.

18. The compound of claim 17 , which is 8-isopropoxy-N-((3R,4S)-3-methyl-1-(methylsulfonyl)piperidin-4-yl)-7-(1H-pyrazol-4-yl)-[1,2,4]triazolo[1,5-a]pyridin-2-amine.

19. A pharmaceutical composition comprising the compound of claim 17 , or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier.

20. A pharmaceutical composition comprising the compound of claim 18 and a pharmaceutically acceptable carrier.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Mar 30, 2021
From: YE, YINGDA; LI, ZHENWU; QIAN, DING-QUAN; WINTERTON, SARAH; XIAO, KAIJIONG; WU, LIANGXING; YAO, WENQING; HUMMEL, JOSHUA; XU, MEIZHONG; YE, MIN; CHEN, YINGNAN; FAVATA, MARGARET; LO, YVONNE
To: INCYTE CORPORATION
Reel/Frame 055761/0712 →
Continuity (2)
Provisional Application 62914114 · Oct 11, 2019
Related Publication 20210107901A1 · Apr 15, 2021
Cited By (2)
US 12,312,331 US 12,466,828