US 12,435,045 B2
Tyrosine kinase inhibitors and pharmaceutical application thereof
Huabiao Chen, Zhenjiang (CN); Zhengyu Long, Zhenjiang (CN); and Tao Li, Zhenjiang (CN)
Assigned to JIANGSU CONCORD BIOTECHNOLOGY CO., LTD, Zhenjiang (CN)
Filed by JIANGSU CONCORD BIOTECHNOLOGY CO., LTD, Zhenjiang (CN)
Filed on Sep. 14, 2022, as Appl. No. 17/944,395.
Application 17/944,395 is a continuation of application No. PCT/CN2022/078934, filed on Mar. 3, 2022.
Claims priority of application No. 202110237399.5 (CN), filed on Mar. 4, 2021; and application No. 202210197875.X (CN), filed on Mar. 2, 2022.
Prior Publication US 2023/0043449 A1, Feb. 9, 2023
Int. Cl. C07D 239/86 (2006.01)
CPC C07D 239/86 (2013.01) 4 Claims
 
1. A tyrosine kinase inhibitor (TKI), having the following formula (I):

OG Complex Work Unit Chemistry
wherein:
R1 is alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, phenyl, mono-substituted phenyl, poly-substituted phenyl, trifluoromethyl, 2,2,2-trifluoroethyl, CH3O(CH2)K—,

OG Complex Work Unit Chemistry
R being methyl, ethyl, isopropyl, trifluoromethyl, 2,2,2-trifluoroethyl, cyclopropyl, acetyl or acryloyl;
R2 is halogen, hydrogen, amino, substituted amino, cyano, hydroxyl, sulfonic acid group, sulfonamide, trifluoromethyl, 2,2,2-trifluoroethyl, methyl, methoxy or ethynyl;
R3 is halogen, hydrogen, amino, substituted amino, cyano, hydroxyl, sulfonic acid group, sulfonamide, trifluoromethyl, 2,2,2-trifluoroethyl, methyl, methoxy or ethynyl;
R2 and R3 are in an ortho, para or meta position;
Y is NH, O, S or Z—N, wherein Z is methyl, ethyl, isopropyl, trifluoromethyl, 2,2,2-trifluoroethyl or cyclopropyl; and
X is Cl, Br or F, n and k each being an integer from 0 to 6.