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公开(公告)号:US20170135979A1
公开(公告)日:2017-05-18
申请号:US14940406
申请日:2015-11-13
Applicant: Macau University of Science and Technology
Inventor: Xiao Jun Yao , Lai Han Leung , Lian Xiang Luo , Liang Liu
IPC: A61K31/343
CPC classification number: A61K31/343
Abstract: The present invention relates to the administration of a novel compound advantageously efficacious as PDEδ inhibitor and its effects on subjects with cancer. More specifically, the present invention is directed to a method for administering a compound having favorable geometric properties for interacting with the PDEδ prenyl-binding pocket, namely has certain structural components such as a three-cyclic backbone and at least one benzoyl-moiety in a side chain having at least two substituents containing highly electronegative atoms and being linked to the backbone via an aliphatic chain, for treating a subject suffering from a disease such as cancer, in particular non-small-cell lung cancer. The presence of said structural components particularly contributes to an advantageous interaction with PDEδ, in particular with amino acids deep in the binding pocket. The present invention further provides a method to target tumor cells harboring an RAS gene mutation as well as pharmaceutical compositions comprising said compound.
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公开(公告)号:US10208028B1
公开(公告)日:2019-02-19
申请号:US15839873
申请日:2017-12-13
Applicant: Macau University of Science and Technology
Inventor: Lai Han Elaine Leung , Xiao Jun Yao , Liang Liu , Jia Hui Xu , Ying Li , Qian Qian Wang
IPC: A61K31/42 , C07D413/12 , A61K31/423 , A61P35/00 , A61K45/06 , G01N33/574
Abstract: One embodiment is a method of treating cancer. The method includes administering a therapeutically effective amount of a compound to a patient. The compound is represented by Formula I:
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3.
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.
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公开(公告)号:US10702500B2
公开(公告)日:2020-07-07
申请号:US16257018
申请日:2019-01-24
Applicant: Macau University of Science and Technology
Inventor: Xiao Jun Yao , Lai Han Elaine Leung , Liang Liu , Qian Qian Wang , Jia Hui Xu , Ying Li
IPC: A61K31/4045 , A61K45/06 , G01N33/574 , A61P35/00 , C12Q1/48
Abstract: One embodiment is a method of treating cancer. The method includes administering a therapeutically effective amount of a compound to a patient. The compound is represented by Formula I:
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公开(公告)号:US09884047B1
公开(公告)日:2018-02-06
申请号:US15632407
申请日:2017-06-26
Applicant: Macau University of Science and Technology
Inventor: Xiao Jun Yao , Lai Han Elaine Leung , Liang Liu , Xing Xing Fan , Chun Xie
IPC: A61K31/428 , G01N33/574 , C07D277/72 , C07K14/47 , C12Q1/68 , G01N33/68 , A61K38/00
CPC classification number: A61K31/428 , A61K38/00 , C07D277/72 , C07K14/47 , C07K2319/00 , C12Q1/6886 , C12Q2600/106 , C12Q2600/112 , G01N33/574 , G01N33/57423 , G01N33/57484 , G01N33/68
Abstract: One example embodiment relates to a method of treating non-small cell lung cancer by administering a compound of formula (I) to a patient. Another example embodiment relates to a method of inhibiting progress of tumor growth in a patient with cancer, wherein tumor cells of the cancer have a mutant V-Ki-ras2 Kirsten rat sarcoma viral oncogene homolog (KRAS) gene, and the method includes administering to the patient the compound with the following formula I:
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公开(公告)号:US10278955B1
公开(公告)日:2019-05-07
申请号:US15839875
申请日:2017-12-13
Applicant: Macau University of Science and Technology
Inventor: Xiao Jun Yao , Lai Han Elaine Leung , Liang Liu , Qian Qian Wang , Jia Hui Xu , Ying Li
IPC: A61K31/4045 , A61P35/00 , G01N33/574 , A61K45/06
Abstract: One embodiment is a method of treating cancer. The method includes administering a therapeutically effective amount of a compound to a patient. The compound is represented by Formula I:
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7.
公开(公告)号:US20190017116A1
公开(公告)日:2019-01-17
申请号:US15647414
申请日:2017-07-12
Applicant: Macau University of Science and Technology
Inventor: Liang Liu , Lai Han Leung , Ying Li , Xiao Jun Yao , Hu Dan Pan
Abstract: A method of identifying a gene associated with a disease or pathological condition of the disease includes: a) obtaining a first group of exome sequences from a first population suffering from the disease or pathological condition and a second group of exome sequences from a second population not having the disease or pathological condition; b) identifying one or more variants in the first group by comparing it with the second group, and optionally with a public database, to generate a first set of variant data; c) applying a variant quality score calibration tool with a truth sensitivity threshold to remove false-positive variants having a sensitivity lower than the threshold and background variants from the first set of variant data so as to obtain a second set of variant data; d) removing synonymous variants from the second set of variant data to obtain a third set of variant data; and e) identifying one or more deleterious variants from the third set of variant data using a gene burden analysis, optionally generating a fourth set of variant data.
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公开(公告)号:US09884046B1
公开(公告)日:2018-02-06
申请号:US15632406
申请日:2017-06-26
Applicant: Macau University of Science and Technology
Inventor: Xiao Jun Yao , Lai Han Elaine Leung , Liang Liu , Xing Xing Fan , Chun Xie
IPC: A61K31/428 , C07D277/72 , G01N33/574 , C07K14/47 , C12Q1/68 , G01N33/68 , A61K38/00
CPC classification number: A61K31/428 , A61K38/00 , C07D277/72 , C07K14/47 , C07K2319/00 , C12Q1/6886 , C12Q2600/112 , G01N33/574 , G01N33/57423 , G01N33/57484 , G01N33/68
Abstract: One embodiment relates to a method of treating lung cancer by administering a compound of formula I to a patient. Another embodiment relates to a method of treating cancer with a KRAS mutation that includes administering to a patient the compound with the following formula I:
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公开(公告)号:US09526722B1
公开(公告)日:2016-12-27
申请号:US14744042
申请日:2015-06-19
Applicant: Macau University of Science and Technology
Inventor: Xiao Jun Yao , Lai Han Leung , Lian Xiang Luo , Yan Ling Zhou , Liang Liu
IPC: A01N43/42 , A61K31/444 , A61K31/4745
CPC classification number: A61K31/4745
Abstract: The present invention provides a compound that inhibits activity of oncogenic ROS1, a composition comprising said compound. The present invention also provides the use of said composition for treating cancer.
Abstract translation: 本发明提供抑制致癌ROS1活性的化合物,其是包含所述化合物的组合物。 本发明还提供了所述组合物用于治疗癌症的用途。
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10.
公开(公告)号:US10787708B2
公开(公告)日:2020-09-29
申请号:US15647414
申请日:2017-07-12
Applicant: Macau University of Science and Technology
Inventor: Liang Liu , Lai Han Leung , Ying Li , Xiao Jun Yao , Hu Dan Pan
IPC: C12Q1/6883 , G16B30/00 , G16B50/00 , G16B20/20 , G16B5/00 , G16B15/00 , G16B40/20 , C12Q1/6869
Abstract: A method of identifying a gene associated with a disease or pathological condition of the disease includes: a) obtaining a first group of exome sequences from a first population suffering from the disease or pathological condition and a second group of exome sequences from a second population not having the disease or pathological condition; b) identifying one or more variants in the first group by comparing it with the second group, and optionally with a public database, to generate a first set of variant data; c) applying a variant quality score calibration tool with a truth sensitivity threshold to remove false-positive variants having a sensitivity lower than the threshold and background variants from the first set of variant data so as to obtain a second set of variant data; d) removing synonymous variants from the second set of variant data to obtain a third set of variant data; and e) identifying one or more deleterious variants from the third set of variant data using a gene burden analysis, optionally generating a fourth set of variant data.
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