公开(公告)号：US10155721B2

公开(公告)日：2018-12-18

申请号：US15495949

申请日：2017-04-24

Applicant: Macau University of Science and Technology

Inventor： Guo-Yuan Zhu ,  Zhi-Hong Jiang ,  Ji Yang ,  Xiao-Jun Yao ,  Xin Liu ,  Jing Fu ,  Li-Ping Bai ,  Liang Liu

IPC: C07C237/26 ,  C07C231/24

Abstract: One example embodiment is a lignanamide that includes a benzo-angular triquinane skeleton. The lignanamide is represented by formula (I) and any derivative of the formula (I), in which R is represented by —OH or —OCH3. Another example embodiment relates to a method of treating neurodegenerative disease by administering the lignanamide of the formula (I) to a person in need thereof.

公开(公告)号：US09744145B1

公开(公告)日：2017-08-29

申请号：US15406798

申请日：2017-01-16

Applicant: Macau University of Science and Technology

Inventor： Liang Liu ,  Lai-Han Elaine Leung ,  Xiao-Jun Yao ,  Run-Ze Li

IPC: A61K31/18

CPC classification number: A61K31/18

Abstract: This invention provides a method of treating lung cancer including administering a therapeutically effective amount of a compound of 0089-0022 formula I to a subject in need thereof. The compound activates pyruvate kinase M2 isoform (PKM2) to treat the lung cancer. In one example, the lung cancer is Non-Small Cell Lung Cancer (NSCLC).

公开(公告)号：US09364469B1

公开(公告)日：2016-06-14

申请号：US14925996

申请日：2015-10-29

Applicant: Macau University of Science and Technology

Inventor： Lai-Han Leung ,  Xiao-Jun Yao ,  Kam Wai Wong ,  Liang Liu ,  Xi Chen

IPC: A61K31/4439

CPC classification number: A61K31/4439

Abstract: The present invention discloses a method of treating gefitinib-resistant non-small-cell lung cancer, comprising administering an effective amount of D561-0775. A pharmaceutical composition comprising D561-0775 admixed with a pharmaceutical carrier for treating Gefitinib-resistant non-small-cell lung cancer is also disclosed therein.

Abstract translation: 本发明公开了一种治疗耐吉非替尼的非小细胞肺癌的方法，包括给予有效量的D561-0775。 还公开了包含D561-0775的药物组合物，其与药物载体混合以治疗吉非替尼耐药性非小细胞肺癌。

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：US09855250B1

公开(公告)日：2018-01-02

申请号：US15351419

申请日：2016-11-14

Applicant: Macau University of Science and Technology

Inventor： Liang Liu ,  Elaine Lai-Han Leung ,  Xiao-Jun Yao ,  Vincent Kam-Wai Wong ,  Xi Chen

IPC: A61K31/4245

CPC classification number: A61K31/4245

Abstract: One example embodiment relates to a method of treating lung cancer by administering a compound of formula I to a subject in need thereof. Another embodiment relates to a method to treat Non-Small Cell Lung Cancer (NSCLC) by administering the compound of formula I to a patient.

公开(公告)号：US20180348222A1

公开(公告)日：2018-12-06

申请号：US15610709

申请日：2017-06-01

Applicant: Macau University of Science and Technology

Inventor： Liang Liu ,  Lai-Han Elaine Leung ,  Xiao-Jun Yao ,  Run-Ze Li ,  Xing-Xing Fan

IPC: G01N33/574 ,  A61K31/56 ,  A61K31/585

Abstract: A method of treating a subject, in particular a human, suffering from non-small cell lung cancer includes administering a bufadienolide to the subject. A method of inhibiting the proliferation and inducing the cell death of non-small cell lung cancer cells, a method of inhibiting the Epidermal growth factor receptor (EGFR) kinase activity in non-small cell lung cancer cells harboring an abnormality in the EGFR gene, and a method of inhibiting Na+/K+-ATPase in non-small cell lung cancer cells includes contacting those cells with a bufadienolide. Proscillaridin A as bufadienolide, with the structure of Formula (III) has advantageously high cytotoxicity against EGFR-dependent non-small cell lung cancer at nano-molar levels while having low toxicity to normal lung cells.

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。