US 12,466,828 B2
Bicyclic amines as CDK2 inhibitors
Yingda Ye, Wilmington, DE (US); Zhenwu Li, Wilmington, DE (US); Ding-Quan Qian, Newark, DE (US); Sarah Winterton, Wilmington, DE (US); Kaijiong Xiao, Clark, NJ (US); Liangxing Wu, Wilmington, DE (US); Wenqing Yao, Chadds Ford, PA (US); Joshua Hummel, Hockessin, DE (US); Meizhong Xu, Hockessin, DE (US); Min Ye, Garnet Valley, PA (US); Yingnan Chen, Wilmington, DE (US); Margaret Favata, North East, MD (US); and Yvonne Lo, Hockessin, DE (US)
Assigned to Incyte Corporation, Wilmington, DE (US)
Filed by Incyte Corporation, Wilmington, DE (US)
Filed on Nov. 1, 2023, as Appl. No. 18/386,224.
Application 18/386,224 is a division of application No. 17/067,203, filed on Oct. 9, 2020, granted, now 11,851,426.
Claims priority of provisional application 62/914,114, filed on Oct. 11, 2019.
Prior Publication US 2024/0174664 A1, May 30, 2024
Int. Cl. C07D 471/04 (2006.01); A61P 35/00 (2006.01); C07D 487/04 (2006.01); C07D 519/00 (2006.01)
CPC C07D 471/04 (2013.01) [A61P 35/00 (2018.01); C07D 487/04 (2013.01); C07D 519/00 (2013.01)] 47 Claims
 
1. A method of treating a cancer in a human subject, comprising administering to the patient a therapeutically effective amount of a compound selected from:
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;
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;
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;
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; and
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 pharmaceutically acceptable salt thereof, wherein the cancer is selected from breast cancer, ovarian cancer, lung cancer, fallopian tube cancer, endometrial cancer, gastrointestinal cancer, uterine cancer, urothelial cancer, anal cancer, bile duct cancer, cancer of the small bowel, cancer of the large bowel, colon cancer, colorectal cancer, rectal cancer, cancer of the small intestine, esophageal cancer, islet cell cancer, liver cancer, pancreatic cancer, and gastric cancer.