公开(公告)号：US20130040952A1

公开(公告)日：2013-02-14

申请号：US13567355

申请日：2012-08-06

申请人： Chi-Huey Wong ,  Ming-Daw Tsai ,  Ying-Ta Wu ,  Yih-Shyun E. Cheng ,  Yu-Hou Chen ,  Yu-Fang Shen

发明人： Chi-Huey Wong ,  Ming-Daw Tsai ,  Ying-Ta Wu ,  Yih-Shyun E. Cheng ,  Yu-Hou Chen ,  Yu-Fang Shen

IPC分类号： A61K31/5377 ,  C12N5/07 ,  A61P31/16 ,  G01N33/53 ,  A61K31/167 ,  A61K31/517

CPC分类号： A61K31/167 ,  A61K31/517 ,  A61K31/5377 ,  G01N33/56983

摘要： Methods for identifying agents capable of disrupting a salt bridge in an influenza A virus nucleoprotein corresponding to the E339 . . . R416 salt bridge in SEQ ID NO:1, and thus the trimerization of the NP protein; and uses of such agents, e.g., small molecules and peptides, for inhibiting influenza virus replication and treating infection caused by influenza virus.

摘要翻译： 鉴定能够破坏对应于E339的甲型流感病毒核蛋白中的盐桥的试剂的方法。 。 。 R416盐桥，因此NP蛋白的三聚化; 以及这些药剂（例如小分子和肽）用于抑制流感病毒复制和治疗由流感病毒引起的感染的用途。

公开(公告)号：US20090076143A1

公开(公告)日：2009-03-19

申请号：US12212607

申请日：2008-09-17

申请人： Chi-Huey Wong ,  Yih-Shyun E. Cheng ,  Hui-Ming Yu ,  Ting-Jen R. Cheng ,  Chung-Yi Wu ,  Jim-Min Fang

发明人： Chi-Huey Wong ,  Yih-Shyun E. Cheng ,  Hui-Ming Yu ,  Ting-Jen R. Cheng ,  Chung-Yi Wu ,  Jim-Min Fang

IPC分类号： A61K31/235 ,  A61K31/215 ,  C12P21/00 ,  A61P29/00

CPC分类号： A61K36/53 ,  A61K31/215 ,  A61K31/235

摘要： The crude extract of Plectranthus Amboinicus (PA) has anti-inflammatory effects and can inhibit AP-1 binding in vitro. The incubation with PA crude extract resulted in significant inhibition of the LPS-induced expression of IL-6, IL-12, MCP-1, and RANTES in HUVEC cells. After the crude extract was further fractionated using preparative HPLC, fraction 8, 9, 10 and 11 were identified to inhibit the AP-1 binding activity. The active component of fraction 8 is Mena 987; fraction 9 is Mena 998; fraction 10 is Mena 9102; and fraction 11 is rosmarinic acid and the synthestic rosmarinic acid analogues. Other compounds showed inhibitory activities as well. These compounds have inhibitory effects on AP-1 activity and are useful as preventive or therapeutic agent for diseases in which excessive expression or activities of AP-1 are involved.

摘要翻译： 芍药（Plectranthus Amboinicus，PA）的粗提物具有抗炎作用，能体外抑制AP-1结合。 与PA粗提取物的孵育导致LPS诱导的HUVEC细胞中IL-6，IL-12，MCP-1和RANTES的表达的显着抑制。 在使用制备型HPLC进一步分馏粗提取物后，鉴定出8,9,10和11级分抑制AP-1结合活性。 级分8的活性组分是Mena 987; 9级是Mena 998; 级分10是Mena 9102; 并且级分11是迷迭香酸和合成迷迭香酸类似物。 其他化合物也显示抑制活性。 这些化合物对AP-1活性具有抑制作用，可用作涉及AP-1过度表达或活性的疾病的预防或治疗剂。

公开(公告)号：US08105636B2

公开(公告)日：2012-01-31

申请号：US12212607

申请日：2008-09-17

申请人： Chi-Huey Wong ,  Yih-Shyun E. Cheng ,  Hui-Ming Yu ,  Ting-Jen R. Cheng ,  Chung-Yi Wu ,  Jim-Min Fang

发明人： Chi-Huey Wong ,  Yih-Shyun E. Cheng ,  Hui-Ming Yu ,  Ting-Jen R. Cheng ,  Chung-Yi Wu ,  Jim-Min Fang

IPC分类号： A61K36/00 ,  A61K31/045 ,  A61K31/05

CPC分类号： A61K36/53 ,  A61K31/215 ,  A61K31/235

摘要： The crude extract of Plectranthus Amboinicus (PA) has anti-inflammatory effects and can inhibit AP-1 binding in vitro. The incubation with PA crude extract resulted in significant inhibition of the LPS-induced expression of IL-6, IL-12, MCP-1, and RANTES in HUVEC cells. After the crude extract was further fractionated using preparative HPLC, fraction 8, 9, 10 and 11 were identified to inhibit the AP-1 binding activity. The active component of fraction 8 is Mena 987; fraction 9 is Mena 998; fraction 10 is Mena 9102; and fraction 11 is rosmarinic acid and the synthetic rosmarinic acid analogues. Other compounds showed inhibitory activities as well. These compounds have inhibitory effects on AP-1 activity and are useful as preventive or therapeutic agent for diseases in which excessive expression or activities of AP-1 are involved.

摘要翻译： 芍药（Plectranthus Amboinicus，PA）的粗提物具有抗炎作用，能体外抑制AP-1结合。 与PA粗提取物的孵育导致LPS诱导的HUVEC细胞中IL-6，IL-12，MCP-1和RANTES的表达的显着抑制。 在使用制备型HPLC进一步分馏粗提取物后，鉴定出8,9,10和11级分抑制AP-1结合活性。 级分8的活性组分是Mena 987; 9级是Mena 998; 级分10是Mena 9102; 并且级分11是迷迭香酸和合成的迷迭香酸类似物。 其他化合物也显示抑制活性。 这些化合物对AP-1活性具有抑制作用，可用作涉及AP-1过度表达或活性的疾病的预防或治疗剂。

公开(公告)号：US09073941B2

公开(公告)日：2015-07-07

申请号：US13806228

申请日：2011-06-28

申请人： Chi-Huey Wong ,  Ying-Ta Wu

发明人： Chi-Huey Wong ,  Ying-Ta Wu

IPC分类号： A61K31/415 ,  C07D498/04 ,  C07C49/753 ,  C07C49/755 ,  C07D401/12 ,  C07D405/14 ,  C07D413/14 ,  C07D417/14 ,  C07D487/04

CPC分类号： C07D498/04 ,  C07C49/753 ,  C07C49/755 ,  C07D401/12 ,  C07D405/14 ,  C07D413/14 ,  C07D417/14 ,  C07D487/04

摘要： The present invention provides compounds which are potent inhibitors against Lpd activity, PDH activity, and/or the growth of tubercle bacillus, and thus are useful in the treatment of tuberculosis infection and associated conditions. The present invention is further directed to in vitro- and in vzivo-based methods of inhibiting Lpd and/or PDH activity. In certain embodiments, these methods are useful in inhibiting Lpd and/or PDH activity key to a pathogen's survival.

摘要翻译： 本发明提供了对Lpd活性，PDH活性和/或结核杆菌生长有效的抑制剂的化合物，因此可用于治疗结核病感染和相关病症。 本发明还涉及基于体外和基于vzivo的抑制Lpd和/或PDH活性的方法。 在某些实施方案中，这些方法可用于抑制病原体存活的Lpd和/或PDH活性。

公开(公告)号：US20130345223A9

公开(公告)日：2013-12-26

申请号：US13806228

申请日：2011-06-28

申请人： Chi-Huey Wong ,  Ying-Ta Wu

发明人： Chi-Huey Wong ,  Ying-Ta Wu

IPC分类号： C07D498/04 ,  C07D405/14 ,  C07D417/14 ,  C07C49/755 ,  C07D413/14 ,  C07D487/04 ,  C07D401/12

CPC分类号： C07D498/04 ,  C07C49/753 ,  C07C49/755 ,  C07D401/12 ,  C07D405/14 ,  C07D413/14 ,  C07D417/14 ,  C07D487/04

摘要： The present invention provides compounds which are potent inhibitors against Lpd activity, PDH activity, and/or the growth of tubercle bacillus, and thus are useful in the treatment of tuberculosis infection and associated conditions. The present invention is further directed to in vitro- and in vzivo-based methods of inhibiting Lpd and/or PDH activity. In certain embodiments, these methods are useful in inhibiting Lpd and/or PDH activity key to a pathogen's survival.

摘要翻译： 本发明提供了对Lpd活性，PDH活性和/或结核杆菌生长有效的抑制剂的化合物，因此可用于治疗结核病感染和相关病症。 本发明还涉及基于体外和基于vzivo的抑制Lpd和/或PDH活性的方法。 在某些实施方案中，这些方法可用于抑制病原体存活的Lpd和/或PDH活性。

公开(公告)号：US20130158037A1

公开(公告)日：2013-06-20

申请号：US13806228

申请日：2011-06-28

申请人： Chi-Huey Wong ,  Ying-Ta Wu

发明人： Chi-Huey Wong ,  Ying-Ta Wu

IPC分类号： C07D498/04 ,  C07D405/14 ,  C07D417/14 ,  C07C49/755 ,  C07D413/14 ,  C07D487/04 ,  C07D401/12

CPC分类号： C07D498/04 ,  C07C49/753 ,  C07C49/755 ,  C07D401/12 ,  C07D405/14 ,  C07D413/14 ,  C07D417/14 ,  C07D487/04

摘要： The present invention provides compounds which are potent inhibitors against Lpd activity, PDH activity, and/or the growth of tubercle bacillus, and thus are useful in the treatment of tuberculosis infection and associated conditions. The present invention is further directed to in vitro- and in vzivo-based methods of inhibiting Lpd and/or PDH activity. In certain embodiments, these methods are useful in inhibiting Lpd and/or PDH activity key to a pathogen's survival.

公开(公告)号：US09816981B2

公开(公告)日：2017-11-14

申请号：US13159339

申请日：2011-06-13

申请人： Masaaki Sawa ,  Chi-Huey Wong ,  Tsui-Ling Hsu ,  Sarah Hanson

发明人： Masaaki Sawa ,  Chi-Huey Wong ,  Tsui-Ling Hsu ,  Sarah Hanson

IPC分类号： C07H15/04 ,  C07H19/10 ,  G01N33/50 ,  G01N33/533

CPC分类号： G01N33/5005 ,  G01N33/5008 ,  G01N33/533 ,  G01N2400/00

摘要： Methods for metabolic oligosaccharide engineering that incorporates derivatized alkyne-bearing sugar analogs as “tags” into cellular glycoconjugates are disclosed. Alkynyl derivatized Fuc and alkynyl derivatized ManNAc sugars are incorporated into cellular glycoconjugates. Chemical probes comprising an azide group and a visual or fluorogenic probe and used to label alkyne-derivatized sugar-tagged glycoconjugates are disclosed. Chemical probes bind covalently to the alkynyl group by Cu(I)-catalyzed [3+2] azide-alkyne cycloaddition and are visualized at the cell surface, intracellularly, or in a cellular extract. The labeled glycoconjugate is capable of detection by flow cytometry, SDS-PAGE, Western blot, ELISA, confocal microscopy, and mass spectrometry.

公开(公告)号：US08916540B2

公开(公告)日：2014-12-23

申请号：US12354717

申请日：2009-01-15

申请人： Chi-Huey Wong ,  Ting-Jen Cheng ,  Che Alex Ma ,  Wei-Chieh Cheng

发明人： Chi-Huey Wong ,  Ting-Jen Cheng ,  Che Alex Ma ,  Wei-Chieh Cheng

IPC分类号： C07K14/195 ,  C07K14/26 ,  C07K14/315 ,  C07K14/25 ,  C07K14/235 ,  C07K14/32 ,  C07K14/31 ,  C07K14/21 ,  C07K14/33 ,  C07K14/255 ,  C07K14/22 ,  C07K14/265 ,  G01N33/573 ,  A61K31/19 ,  A61K31/715 ,  A61K31/427 ,  A61K31/365

CPC分类号： A61K31/702 ,  A61K31/19 ,  A61K31/365 ,  A61K31/427 ,  A61K31/715 ,  C07K14/195 ,  C07K14/21 ,  C07K14/22 ,  C07K14/235 ,  C07K14/25 ,  C07K14/255 ,  C07K14/26 ,  C07K14/265 ,  C07K14/31 ,  C07K14/315 ,  C07K14/3156 ,  C07K14/32 ,  C07K14/33 ,  G01N33/573 ,  G01N2333/91091 ,  Y02A50/473 ,  Y02A50/475 ,  Y02A50/481

摘要： Moenomycin inhibits bacterial growth by clocking the transglycosylase activity of class A penicillin-binding proteins (PBPs), which are key enzymes in bacterial cell wall synthesis. The binding affinities of moenomycin A with various truncated PBPs were compared showing that the transmembrane domain is important for moenomycin binding. Full-length class-A PBPs from 16 bacterial species were produced, and their binding activities showed a correlation with the antimicrobial activity of moenomycin against Enterococcus faecalis and Staphylococcus aureus. Moreover, a fluorescence anisotropy-based high-throughput assay was developed and used successfully for identification of transglycosylase inhibitors.

摘要翻译： 霉菌素通过计时细菌细胞壁合成中的关键酶A类青霉素结合蛋白（PBP）的转糖苷酶活性抑制细菌生长。 比较了霉酚霉素A与各种截短的PBP的结合亲和力，结果表明跨膜结构域对于霉酚霉素结合是重要的。 产生了16种细菌种类的全长class-A PBPs，其结合活性与霉酚霉素对粪肠球菌和金黄色葡萄球菌的抗菌活性呈显着相关性。 此外，开发了基于荧光各向异性的高通量测定，并成功地用于鉴定转糖基酶抑制剂。

公开(公告)号：US08906832B2

公开(公告)日：2014-12-09

申请号：US12423733

申请日：2009-04-14

申请人： Chi-Huey Wong ,  Pi-Hui Liang

发明人： Chi-Huey Wong ,  Pi-Hui Liang

IPC分类号： C07H3/00 ,  C40B40/12 ,  B01J19/00 ,  C40B30/04 ,  C40B20/02

CPC分类号： G01N33/5308 ,  B01J19/0046 ,  C40B30/04 ,  C40B40/12 ,  G01N2400/00 ,  G01N2400/10

摘要： A method, system and device to identify, study and/or mimic carbohydrate-protein interactions on cell surfaces and in solution measured by a glycan microarray. In some instances the method, system and device uses very small quantities of carbohydrate as low as attomol. In some instances the system, method and device is high-throughput. The small quantity sensitivity may allow for close placement of carbohydrate array members wherein due to close proximity multivalent interactions with proteins may be identified.

摘要翻译： 鉴定，研究和/或模拟细胞表面和聚糖微阵列测量溶液中碳水化合物 - 蛋​​白质相互作用的方法，系统和装置。 在某些情况下，该方法，系统和装置使用非常少量的碳水化合物，与阿托莫尔一样低。 在某些情况下，系统，方法和设备是高吞吐量的。 小量的灵敏度可以允许碳水化合物阵列成员的紧密放置，其中由于与蛋白质的近似多价相互作用可以被鉴定。

公开(公告)号：US08481571B2

公开(公告)日：2013-07-09

申请号：US11121314

申请日：2005-05-03

申请人： Chi-Huey Wong ,  Chung-Yi Wu ,  Jia-Tsrong Jan

发明人： Chi-Huey Wong ,  Chung-Yi Wu ,  Jia-Tsrong Jan

IPC分类号： A61K31/44 ,  A61K31/40 ,  A61K31/165 ,  A61K31/325

CPC分类号： A61K31/165 ,  A61K31/325 ,  A61K31/40 ,  A61K31/44

摘要： A method of treating coronavirus infection. The method includes administering to a subject suffering from or being at risk of suffering from such infection an effective amount of a compound of formula (I). Each variable in this formula is defined in the specification.

摘要翻译： 治疗冠状病毒感染的方法。 该方法包括给患有或有风险患有此类感染的受试者施用有效量的式（I）化合物。 该公式中的每个变量在规范中定义。