US 12,441,727 B2
Tricyclic compounds as inhibitors of KRAS
Pei Gan, Wilmington, DE (US); Jeffrey Yang, Wilmington, DE (US); Yong Li, Wilmington, DE (US); Le Zhao, Wilmington, DE (US); Chunhong He, Wilmington, DE (US); Chunyin Marshall Law, Wilmington, DE (US); Xiaozhao Wang, Mt. Laurel, NJ (US); and Wenqing Yao, Wilmington, DE (US)
Assigned to Incyte Corporation, Wilmington, DE (US)
Filed by Incyte Corporation, Wilmington, DE (US)
Filed on Jul. 6, 2022, as Appl. No. 17/810,915.
Claims priority of provisional application 63/310,811, filed on Feb. 16, 2022.
Claims priority of provisional application 63/292,774, filed on Dec. 22, 2021.
Claims priority of provisional application 63/219,274, filed on Jul. 7, 2021.
Prior Publication US 2023/0056631 A1, Feb. 23, 2023
Int. Cl. C07D 471/04 (2006.01); A61P 35/00 (2006.01)
CPC C07D 471/04 (2013.01) [A61P 35/00 (2018.01)] 31 Claims
 
1. A compound having Formula I:

OG Complex Work Unit Chemistry
or a pharmaceutically acceptable salt thereof, wherein:
Y is N or CH;
R1 is selected from Cl, CH3, CH2F, CHF2, and CF3;
Cy1 is selected from

OG Complex Work Unit Chemistry

OG Complex Work Unit Chemistry

OG Complex Work Unit Chemistry
R2 is selected from F and Cl;
R3 is selected from

OG Complex Work Unit Chemistry
and,
Cy2 is selected from

OG Complex Work Unit Chemistry
provided that the compound of Formula I is other than,
 
2-((2S,4S)-4-(7-(2-chloro-3-methylphenyl)-4-(3-(dimethylamino)-3-
methylazetidin-1-yl)-6-fluoro-8-methyl-1H-[1,2,3]triazolo[4,5-c]quinolin-
1-yl)-1-((E)-4-fluorobut-2-enoyl)piperidin-2-yl)acetonitrile,
2-((2S,4S)-4-(4-(3-(dimethylamino)-3-methylazetidin-1-yl)-7-(2,3-
dimethylphenyl)-6-fluoro-8-methyl-1H-[1,2,3]triazolo[4,5-c]quinolin-1-
yl)-1-((E)-4-fluorobut-2-enoyl)piperidin-2-yl)acetonitrile, and
2-((2S,4S)-4-(4-(3-(dimethylamino)-3-methylazetidin-1-yl)-6-fluoro-7-(6-
fluoro-5-methyl-1H-indazol-4-yl)-8-methyl-1H-[1,2,3]triazolo[4,5-
c]quinolin-1-yl)-1-((E)-4-methoxybut-2-enoyl)piperidin-2-yl)acetonitrile.