公开(公告)号：US11434229B2

公开(公告)日：2022-09-06

申请号：US16081490

申请日：2017-02-28

Applicant: Academia Sinica ,  National Taiwan University

Inventor： Chi-Huey Wong ,  Pan-Chyr Yang ,  Rong-Jie Chein ,  Szu-Hua Pan ,  Ting-Jen R. Cheng

IPC: C07D405/12 ,  C07D307/92 ,  C07D403/12 ,  C07D413/12

Abstract: The present disclosure provides compounds of Formulas (I), (II), and pharmaceutically acceptable salts thereof. The compounds described herein are useful in treating proliferative diseases, for example, cancer (e.g., lung cancer), and infectious diseases (e.g., bacterial infections).

公开(公告)号：US20200095233A1

公开(公告)日：2020-03-26

申请号：US16081490

申请日：2017-02-28

Applicant: Academia Sinica ,  National Taiwan University

Inventor： Chi-Huey Wong ,  Pan-Chyr Yang ,  Rong-Jie Chein ,  Szu-Hua Pan ,  Ting-Jen R. Cheng

IPC: C07D405/12 ,  C07D413/12 ,  C07D307/92 ,  C07D403/12

Abstract: The present disclosure provides compounds of Formulas (I), (II), and pharmaceutically acceptable salts thereof. The compounds described herein are useful in treating proliferative diseases, for example, cancer (e.g., lung cancer), and infectious diseases (e.g., bacterial infections).

公开(公告)号：US20180369249A1

公开(公告)日：2018-12-27

申请号：US16075202

申请日：2017-02-03

Applicant: Academia Sinica ,  National Taiwan University

Inventor： Chi-Huey Wong ,  Pan-Chyr Yang ,  Jim-Min Fang ,  Szu-Hua Pan ,  Ting-Jen R. Cheng ,  Ling-Wei Li

IPC: A61K31/522 ,  A61K35/00

Abstract: The present disclosure provides compounds of Formulas (I′) and (I), and pharmaceutically acceptable salts thereof. The compounds described herein may be useful in treating and/or preventing proliferative diseases (e.g., cancer). Also provided in the present disclosure are pharmaceutical compositions, kits, and uses thereof for treating proliferative diseases.

公开(公告)号：US10130714B2

公开(公告)日：2018-11-20

申请号：US13836356

申请日：2013-03-15

Applicant: Academia Sinica

Inventor： Chi-Huey Wong ,  Jim-Min Fang ,  Kung-Cheng Liu ,  Jia-Tsrong Jan ,  Yih-Shyun E. Cheng ,  Ting-Jen R. Cheng

IPC: A61K31/351 ,  C07D309/28 ,  A61K47/55 ,  A61K47/48

Abstract: Novel dual-targeted, bifunctional anti-influenza drugs formed by conjugation with anti-inflammatory agents are disclosed. Exemplary drugs according to the invention include caffeic acid (CA)-bearing zanamivir (ZA) conjugates ZA-7-CA (1), ZA-7-CA-amide (7) and ZA-7-Nap (43) for simultaneous inhibition of influenza virus neuraminidase and suppression of proinflammatory cytokines. Synthetic methods for preparation of these enhanced anti-influenza conjugate drugs are provided. The synthetic bifunctional ZA conjugates act synergistically towards protection of mice lethally infected by H1N1 or H5N1 influenza viruses. The efficacy of ZA-7-CA, ZA-7-CA-amide and ZA-7-Nap conjugates is much greater than the combination therapy of ZA with anti-inflammatory agents.

公开(公告)号：US10765681B2

公开(公告)日：2020-09-08

申请号：US16075202

申请日：2017-02-03

Applicant: Academia Sinica ,  National Taiwan University

Inventor： Chi-Huey Wong ,  Pan-Chyr Yang ,  Jim-Min Fang ,  Szu-Hua Pan ,  Ting-Jen R. Cheng ,  Ling-Wei Li

IPC: C07D473/00 ,  A61K31/522 ,  A61K45/06 ,  A61K31/337 ,  A61K31/52 ,  A61K31/506 ,  A61K31/502 ,  A61K31/167 ,  A61K31/454 ,  A61K38/05 ,  A61K31/517 ,  A61K31/4025 ,  A61K31/5377 ,  A61K31/69 ,  A61K31/44 ,  A61K35/00

Abstract: The present disclosure provides compounds of Formulas (I′) and (I), and pharmaceutically acceptable salts thereof. The compounds described herein may be useful in treating and/or preventing proliferative diseases (e.g., cancer). Also provided in the present disclosure are pharmaceutical compositions, kits, and uses thereof for treating proliferative diseases.

公开(公告)号：US11919886B2

公开(公告)日：2024-03-05

申请号：US17811880

申请日：2022-07-12

Applicant: Academia Sinica ,  National Taiwan University

Inventor： Chi-Huey Wong ,  Pan-Chyr Yang ,  Rong-Jie Chein ,  Szu-Hua Pan ,  Ting-Jen R. Cheng

IPC: A61K31/4025 ,  A61K31/4178 ,  C07D307/92 ,  C07D403/12 ,  C07D405/12 ,  C07D413/12

CPC classification number: C07D405/12 ,  A61K31/4025 ,  A61K31/4178 ,  C07D307/92 ,  C07D403/12 ,  C07D413/12

Abstract: The present disclosure provides compounds of Formulas (I), (II), and pharmaceutically acceptable salts thereof. The compounds described herein are useful in treating proliferative diseases, for example, cancer (e.g., lung cancer), and infectious diseases (e.g., bacterial infections).

公开(公告)号：US20230010562A1

公开(公告)日：2023-01-12

申请号：US17811880

申请日：2022-07-12

Applicant: Academia Sinica ,  National Taiwan University

Inventor： Chi-Huey Wong ,  Pan-Chyr Yang ,  Rong-Jie Chein ,  Szu-Hua Pan ,  Ting-Jen R. Cheng

IPC: C07D405/12 ,  C07D307/92 ,  C07D403/12 ,  C07D413/12

Abstract: The present disclosure provides compounds of Formulas (I), (II), and pharmaceutically acceptable salts thereof. The compounds described herein are useful in treating proliferative diseases, for example, cancer (e.g., lung cancer), and infectious diseases (e.g., bacterial infections).

公开(公告)号：US20130274229A1

公开(公告)日：2013-10-17

申请号：US13836356

申请日：2013-03-15

Applicant: ACADEMIA SINICA

Inventor： Chi-Huey Wong ,  Jim-Min Fang ,  Kung-Cheng Liu ,  Jia-Tsrong Jan ,  Yih-Shyun E. Cheng ,  Ting-Jen R. Cheng

IPC: A61K47/48

CPC classification number: C07D309/28 ,  A61K31/351 ,  A61K47/55

Abstract: Novel dual-targeted, bifunctional anti-influenza drugs formed by conjugation with anti-inflammatory agents are disclosed. Exemplary drugs according to the invention include caffeic acid (CA)-bearing zanamivir (ZA) conjugates ZA-7-CA (1), ZA-7-CA-amide (7) and ZA-7-Nap (43) for simultaneous inhibition of influenza virus neuraminidase and suppression of proinflammatory cytokines. Synthetic methods for preparation of these enhanced anti-influenza conjugate drugs are provided. The synthetic bifunctional ZA conjugates act synergistically towards protection of mice lethally infected by H1N1 or H5N1 influenza viruses. The efficacy of ZA-7-CA, ZA-7-CA-amide and ZA-7-Nap conjugates is much greater than the combination therapy of ZA with anti-inflammatory agents.

Abstract translation: 公开了通过与抗炎剂缀合形成的新型双靶向双功能抗流感药物。 根据本发明的示例性药物包括用于同时抑制的咖啡酸（CA） - 扎尼米韦（ZA）缀合物ZA-7-CA（1），ZA-7-CA-酰胺（7）和ZA-7-Nap（43） 的流感病毒神经氨酸酶和抑制促炎细胞因子。 提供了制备这些增强型抗流感病毒缀合物药物的合成方法。 合成双功能ZA缀合物协同作用以保护由H1N1或H5N1流感病毒致死的小鼠。 ZA-7-CA，ZA-7-CA-酰胺和ZA-7-Nap缀合物的功效远远大于ZA与抗炎剂的组合疗法。