公开(公告)号：US20190091226A1

公开(公告)日：2019-03-28

申请号：US16081558

申请日：2017-03-01

Applicant: SHANGHAI PHARMACEUTICALS HOLDING CO., LTD.

Inventor： Guangxin XIA ,  Di LI ,  Hongjian ZUO ,  Guangsheng WU ,  Lingjun DUAN ,  Jing ZHANG ,  Yu MAO ,  Yanjun LIU

IPC: A61K31/519 ,  A61K31/541 ,  A61K31/5355 ,  A61K31/5377 ,  A61P35/00

Abstract: Disclosed are a nitrogenous heterocyclic compound, intermediates, a preparation method, a composition and use thereof. The nitrogenous heterocyclic compound in the present invention is as shown in formula I. The compound has a high inhibitory activity towards ErbB2 tyrosine kinase and a relatively good inhibitory activity towards human breast cancer BT-474 and human gastric cancer cell NCI-N87 which express ErbB2 at a high level, and at the same time has a relatively weak inhibitory activity towards EGFR kinase. Namely, the compound is a highly selective small-molecule inhibitor targeted at ErbB2, and hence it has a high degree of safety, and can effectively enlarge the safety window in the process of taking the drug.