公开(公告)号：US10265298B2

公开(公告)日：2019-04-23

申请号：US15682564

申请日：2017-08-22

Applicant: Macau University of Science and Technology

Inventor： Ying Xie ,  Liang Liu ,  Hua Zhou

IPC: A61K31/357 ,  A61K31/352 ,  A61K9/20 ,  A61P1/16 ,  A61K9/00

Abstract: One example embodiment relates to a method of increasing bioavailability of silybin in a person. The method includes providing silybin and a flavonoid to the person, wherein the flavonoid is tangeretin or baicalein. Another example embodiment relates to a method of treating chronic liver disease in a person by administering silybin and a flavonoid to the person to treat the chronic liver disease.

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：US09962378B2

公开(公告)日：2018-05-08

申请号：US14927825

申请日：2015-10-30

Applicant: Macau University of Science and Technology

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

IPC: A61K31/4743

CPC classification number: A61K31/4743

Abstract: The administration of a compound advantageously efficacious as ROS1 inhibitor and its effect on subjects with cancer includes administering a compound having certain structural components such as a quinoline moiety in the backbone and at least one tertiary amine containing moiety in a side chain as well as heteroatoms, in particular oxygen atoms, present in the backbone and the side chain for treating a subject suffering from a disease such as cancer. The presence of such structural components allows for an advantageous interaction with the ROS1 kinase domain, in particular with the hinge region. The administered compounds represent a highly promising opportunity in particular for patients bearing ROS1-dependent cancer. A method for targeting tumor cells harboring an abnormality in ROS1 gene includes contacting a cell with compounds of the present invention as well as pharmaceutical compositions comprising such compounds.

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.

公开(公告)号：US09782400B2

公开(公告)日：2017-10-10

申请号：US14956620

申请日：2015-12-02

Applicant: Macau University of Science and Technology

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

IPC: A01N43/42 ,  A61K31/444 ,  A61K31/4745

CPC classification number: A61K31/4745

Abstract: A compound suitable for treating cancer, in particular NSCLC, inhibits activity of oncogenic ROS1 kinase and ALK kinase. The compound has certain structural components such as a quinoline moiety in the backbone and at least one phenyl-containing moiety in a side chain with a hydrophobic substituent attached to the backbone via an up to 6-membered linking group as well as a further hydrophobic moiety. The presence of the structural components allows for an advantageous interaction with the ROS1 kinase domain and, further, with the ALK kinase domain. Hence, said compound represents a highly promising opportunity for patients bearing ROS1- or ALK-dependent cancer. A composition, in particular a pharmaceutical composition, includes the compound. A method for targeting cancer cells harboring an abnormality in ROS1 gene or ALK gene includes contacting a cell with the compound.

公开(公告)号：US20170079972A1

公开(公告)日：2017-03-23

申请号：US14927825

申请日：2015-10-30

Applicant: Macau University of Science and Technology

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

IPC: A61K31/4743

CPC classification number: A61K31/4743

Abstract: The administration of a compound advantageously efficacious as ROS1 inhibitor and its effect on subjects with cancer includes administering a compound having certain structural components such as a quinoline moiety in the backbone and at least one tertiary amine containing moiety in a side chain as well as heteroatoms, in particular oxygen atoms, present in the backbone and the side chain for treating a subject suffering from a disease such as cancer. The presence of such structural components allows for an advantageous interaction with the ROS1 kinase domain, in particular with the hinge region. The administered compounds represent a highly promising opportunity in particular for patients bearing ROS1-dependent cancer. A method for targeting tumor cells harboring an abnormality in ROS1 gene includes contacting a cell with compounds of the present invention as well as pharmaceutical compositions comprising such compounds.

公开(公告)号：US09561223B2

公开(公告)日：2017-02-07

申请号：US14985420

申请日：2015-12-31

Applicant: Macau University of Science and Technology

Inventor： Kam Wai Wong ,  Yuen Kwan Law ,  Liang Liu ,  Jingrong Wang

IPC: A61K31/4725 ,  A61K31/4745 ,  A61K31/4748

CPC classification number: A61K31/4745 ,  A61K31/4725 ,  A61K31/4748

Abstract: The present invention discloses a method of treating cancer comprising administering an effective amount of an alkaloid, in which the alkaloid is liensinine, isoliensinine, dauricine, cepharanthine, hernandezine or thalidezine and isolated from the traditional Chinese medicinal herbs. The use of the alkaloid in treating neurodegenerative disorder is also disclosed.

公开(公告)号：US20160367547A1

公开(公告)日：2016-12-22

申请号：US14956620

申请日：2015-12-02

Applicant: Macau University of Science and Technology

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

IPC: A61K31/4745

CPC classification number: A61K31/4745

Abstract: A compound suitable for treating cancer, in particular NSCLC, inhibits activity of oncogenic ROS1 kinase and ALK kinase. The compound has certain structural components such as a quinoline moiety in the backbone and at least one phenyl-containing moiety in a side chain with a hydrophobic substituent attached to the backbone via an up to 6-membered linking group as well as a further hydrophobic moiety. The presence of the structural components allows for an advantageous interaction with the ROS1 kinase domain and, further, with the ALK kinase domain. Hence, said compound represents a highly promising opportunity for patients bearing ROS1- or ALK-dependent cancer. A composition, in particular a pharmaceutical composition, includes the compound. A method for targeting cancer cells harboring an abnormality in ROS1 gene or ALK gene includes contacting a cell with the compound.

Abstract translation: 适用于治疗癌症，特别是NSCLC的化合物抑制致癌ROS1激酶和ALK激酶的活性。 该化合物具有某些结构组分，例如骨架中的喹啉部分，以及至少一个侧链中具有疏水性取代基的至少一个含苯基的部分通过至多6元连接基团连接至骨架，以及另外的疏水部分 。 结构组分的存在允许与ROS1激酶结构域以及进一步与ALK激酶结构域的有利相互作用。 因此，所述化合物对于患有ROS1-或ALK依赖性癌症的患者是非常有希望的机会。 组合物，特别是药物组合物，包括该化合物。 用于靶向在ROS1基因或ALK基因中具有异常的癌细胞的方法包括使细胞与化合物接触。