公开(公告)号：US20180050037A1

公开(公告)日：2018-02-22

申请号：US15239288

申请日：2016-08-17

Applicant: Macau University of Science and Technology

Inventor： Xiao-Jun Yao ,  Elaine Lai-Han Leung ,  Lian-Xiang Luo ,  Liang Liu

IPC: A61K31/519

CPC classification number: A61K31/519

Abstract: A compound for treating a disease, in particular cancer like non-small cell lung cancer, exceptionally inhibits activity of oncogenic ALK kinase. Compositions, particularly pharmaceutical compositions, are provided comprising this compound. Methods for targeting cancer cells harboring an abnormality in the ALK gene are also The compound for treating a disease has certain structural elements, namely a tricyclic, more specifically heterocyclic, backbone as the core part of the compound at least one highly electronegative atom in form of a tertiary amine attached to the backbone via an at most 6-membered linking group with a terminal highly electronegative atom in form of a nitrogen as secondary amine, and a further hydrophobic moiety fused to the backbone. The structural components allow for an advantageous interaction with the ALK kinase domain. The compound therefor represents a highly promising treatment option for patients in particular those bearing ALK-dependent non-small cell lung cancer.

公开(公告)号：US09861623B1

公开(公告)日：2018-01-09

申请号：US15337293

申请日：2016-10-28

Applicant: Macau University of Science and Technology

Inventor： Liang Liu ,  David Ward ,  Elaine Lai-Han Leung ,  Xiao Jun Yao ,  Vincent Kam-Wai Wong ,  Lian-Xiang Luo

IPC: A61K31/454 ,  A61K31/52

CPC classification number: A61K31/454 ,  A61K31/52 ,  A61K45/06 ,  A61K2300/00

Abstract: The present invention provides methods for treatment of a RAS-positive disease, in particular KRAS-positive non-small cell lung cancer as well as a method for potentiating the apoptotic activity of a PDEδ inhibitor by combining the PDEδ inhibitor with a direct autophagy inhibitor. The PDEδ inhibitor is preferably, but not exclusively, deltarasin, and the direct autophagy inhibitor is in particular 3-methyladenine. Further provided by the present invention are a kit and a pharmaceutical composition comprising the PDEδ inhibitor and a direct autophagy inhibitor. The methods of the present invention in particular provide a new treatment option for RAS-positive diseases such as KRAS-positive non-small cell lung cancer allowing for an increased apoptotic activity of the PDEδ inhibitor by simultaneously blocking its “tumor protective” autophagy.

公开(公告)号：US10111876B2

公开(公告)日：2018-10-30

申请号：US15239288

申请日：2016-08-17

Applicant: Macau University of Science and Technology

Inventor： Xiao-Jun Yao ,  Elaine Lai-Han Leung ,  Lian-Xiang Luo ,  Liang Liu

IPC: A61K31/519

Abstract: A compound for treating a disease, in particular cancer like non-small cell lung cancer, exceptionally inhibits activity of oncogenic ALK kinase. Compositions, particularly pharmaceutical compositions, are provided comprising this compound. Methods for targeting cancer cells harboring an abnormality in the ALK gene are also The compound for treating a disease has certain structural elements, namely a tricyclic, more specifically heterocyclic, backbone as the core part of the compound at least one highly electronegative atom in form of a tertiary amine attached to the backbone via an at most 6-membered linking group with a terminal highly electronegative atom in form of a nitrogen as secondary amine, and a further hydrophobic moiety fused to the backbone. The structural components allow for an advantageous interaction with the ALK kinase domain. The compound therefor represents a highly promising treatment option for patients in particular those bearing ALK-dependent non-small cell lung cancer.

公开(公告)号：US09522125B1

公开(公告)日：2016-12-20

申请号：US14945436

申请日：2015-11-19

Applicant: Macau University of Science and Technology

Inventor： Xiao-Jun Yao ,  Lai-Han Leung ,  Lian-Xiang Luo ,  Wen-Luan Hsiao ,  Liang Liu

IPC: A61K31/136

CPC classification number: A61K31/136

Abstract: The present invention discloses that a method of treating cancer, preferably non-small cell lung cancer, comprises administrating mitoxantrone. The present invention also discloses a method of inhibiting ROS1 kinase comprising administrating mitoxantrone. A pharmaceutical composition comprising mitoxantrone is also disclosed.

Abstract translation: 本发明公开了一种治疗癌症，优选非小细胞肺癌的方法，包括给予米托蒽醌。 本发明还公开了抑制ROS1激酶的方法，其包括施用米托蒽醌。 还公开了包含米托蒽醌的药物组合物。