公开(公告)号：US09913811B2

公开(公告)日：2018-03-13

申请号：US15186795

申请日：2016-06-20

Applicant: Macau University of Science and Technology

Inventor： Liang Liu ,  Lai Han Leung ,  Xia Li ,  Xing-Xing Fan

IPC: A61K31/122

CPC classification number: A61K31/122

Abstract: A compound suitable for treating EGFR-dependent non-small cell lung cancer exceptionally inhibits activity of the EGFR kinase, in particular in EGFR-dependent non-small cell lung cancer with intrinsic or acquired resistance against at least one EGFR inhibitor. Methods for inhibiting EGFR kinase activity in non-small cell lung cancer cells which harbor an abnormality in the EGFR gene and for targeting cancer cells harboring an abnormality in EGFR gene by contacting EGFR-dependent non-small cell lung cancer cells with said compound are also provided. The compounds allow for an advantageous inhibition of the EGFR kinase activity and induction of apoptosis of the non-small cell lung cancer cells with abnormality in the EGFR gene. Hence, said compounds represent a highly promising treatment option for patients harboring EGFR-dependent cancer.

公开(公告)号：US20170360721A1

公开(公告)日：2017-12-21

申请号：US15186795

申请日：2016-06-20

Applicant: Macau University of Science and Technology

Inventor： Liang Liu ,  Lai Han Leung ,  Xia Li ,  Xing-Xing Fan

IPC: A61K31/122

CPC classification number: A61K31/122

Abstract: A compound suitable for treating EGFR-dependent non-small cell lung cancer exceptionally inhibits activity of the EGFR kinase, in particular in EGFR-dependent non-small cell lung cancer with intrinsic or acquired resistance against at least one EGFR inhibitor. Methods for inhibiting EGFR kinase activity in non-small cell lung cancer cells which harbor an abnormality in the EGFR gene and for targeting cancer cells harboring an abnormality in EGFR gene by contacting EGFR-dependent non-small cell lung cancer cells with said compound are also provided. The compounds allow for an advantageous inhibition of the EGFR kinase activity and induction of apoptosis of the non-small cell lung cancer cells with abnormality in the EGFR gene. Hence, said compounds represent a highly promising treatment option for patients harboring EGFR-dependent cancer.