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公开(公告)号：CA2870335A1
公开(公告)日：2013-10-17
申请号：CA2870335
申请日：2013-04-12
Applicant: ACADEMIA SINICA , WONG CHI-HUEY , FANG JIM-MIN , LIU KUNG-CHENG , JAN JIA-TSRONG , CHENG YIH-SHYUN E , CHENG TING-JEN R
Inventor： WONG CHI-HUEY , FANG JIM-MIN , LIU KUNG-CHENG , JAN JIA-TSRONG , CHENG YIH-SHYUN E , CHENG TING-JEN R
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.
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公开(公告)号：AU2008292859B2
公开(公告)日：2013-09-19
申请号：AU2008292859
申请日：2008-08-29
Applicant: ACADEMIA SINICA
Inventor： CHENG YIH-SHYUN EDMOND , FANG JIM-MIN , JAN JIA-TSRONG , WONG CHI-HUEY , SHIE JIUN-JIE
IPC: C07F9/00 , A61K9/16 , A61K31/7052 , A61K31/7076 , C07C233/52 , C07C247/14 , C07H19/04
Abstract: Novel phosphonate compounds are described. The compounds have activity as neuraminidase inhibitors against wild-type and H274Y mutant of H1N1 and H5N1 viruses. The present disclosure also provides an enantioselective synthetic route to known neuraminidase inhibitors oseltamivir and the anti-flu drug Tamiflu®, as well as novel phosphonate compounds, via D-xylose. Another efficient and flexible synthesis of Tamiflu and the highly potent neuraminidase inhibitor Tamiphosphor was also achieved in 11 steps and > 20% overall yields from the readily available fermentation product (1
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公开(公告)号：NZ550945A
公开(公告)日：2010-04-30
申请号：NZ55094505
申请日：2005-05-03
Applicant: ACADEMIA SINICA
Inventor： WONG CHI-HUEY , WU CHUNG-YI , JAN JIA-TSRONG
IPC: A01N47/10 , A61K31/27 , C07C261/00 , C07C269/00 , C07C271/00
Abstract: Disclosed is a compound of formula (I), or a salt thereof, wherein R5 and R11 are alkyl substituted with aryl, and wherein the rest of the substituents are as defined in the specification. Also disclosed is the use of the above compound for treating an infection with a coronavirus.
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公开(公告)号：CA2756053A1
公开(公告)日：2010-01-14
申请号：CA2756053
申请日：2009-07-10
Applicant: ACADEMIA SINICA
Inventor： WONG CHI-HUEY , YU ALICE , CHANG YA-JEN , LIN KUN-HSIEN , CHENG Y S EDMOND , JAN JIA-TSRONG , LIN YI-LING , HUNG JUNG-TUNG
Abstract: The present disclosure relates to synthetic alpha-galactosyl ceramide (.alpha.- GalCer) analogs, and their use as immunotherapies, adju-vants, and antiviral, antibacterial, and anticancer agents. In one aspect, a method of activating a cy-tokine response in a subject includes administer-ing an effective amount of a compound to a sub-ject, wherein the subject has an adaptive immune system that includes a population of cells, the population including at least one lymphocyte and at least one antigen-presenting cell, and wherein the compound is represented by the structure of formula 1 :; or a pharmaceutically acceptable salt thereof; forming a complex between the com-pound and the antigen-presenting cell, wherein the formation of the complex results in the activa-tion of a receptor on the lymphocyte; and activat-ing the lymphocyte to produce the cytokine re-sponse.
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公开(公告)号：CA2870335C
公开(公告)日：2022-05-03
申请号：CA2870335
申请日：2013-04-12
Applicant: ACADEMIA SINICA , WONG CHI HUEY , FANG JIM MIN , LIU KUNG CHENG , JAN JIA TSRONG , CHENG YIH SHYUN E , CHENG TING JEN R
Inventor： WONG CHI-HUEY , FANG JIM-MIN , LIU KUNG-CHENG , JAN JIA-TSRONG , CHENG YIH-SHYUN E , CHENG TING-JEN R
IPC: C07D309/28 , A61K31/195 , A61K31/215 , A61K31/351 , A61K31/662 , A61P29/00 , A61P31/16 , C07C229/64 , C07C279/16 , C07D407/12 , C07F9/655
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.
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Patent Agency Ranking
公开(公告)号：AU2009268381B2
公开(公告)日：2016-04-21
申请号：AU2009268381
申请日：2009-07-10
Applicant: ACADEMIA SINICA
Inventor： HUNG JUNG-TUNG , LIN KUN-HSIEN , YU ALICE , JAN JIA-TSRONG , CHANG YA-JEN , LIN YI-LING , WONG CHI-HUEY , CHENG Y S EDMOND
Abstract: The present disclosure relates to synthetic alpha-galactosyl ceramide (α- GalCer) analogs, and their use as immunotherapies, adjuvants, and antiviral, antibacterial, and anticancer agents. In one aspect, a method of activating a cytokine response in a subject includes administering an effective amount of a compound to a subject, wherein the subject has an adaptive immune system that includes a population of cells, the population including at least one lymphocyte and at least one antigen-presenting cell, and wherein the compound is represented by the structure of formula 1 :; or a pharmaceutically acceptable salt thereof; forming a complex between the compound and the antigen-presenting cell, wherein the formation of the complex results in the activation of a receptor on the lymphocyte; and activating the lymphocyte to produce the cytokine response.
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公开(公告)号：AU2009268381A1
公开(公告)日：2010-01-14
申请号：AU2009268381
申请日：2009-07-10
Applicant: ACADEMIA SINICA
Inventor： HUNG JUNG-TUNG , LIN YI-LING , JAN JIA-TSRONG , WONG CHI-HUEY , CHENG Y S EDMOND , YU ALICE , CHANG YA-JEN , LIN KUN-HSIEN
Abstract: The present disclosure relates to synthetic alpha-galactosyl ceramide (α-GalCer) analogs, and their use as immunotherapies. In one aspect. a method of activating a cytokine response in a subject includes administering an effective amount of a compound to a subject, wherein the subject has an adaptive immune system that includes a population of cells, the population including at least one lymphocyte and at least one antigen-presenting cell, and wherein the compound is represented by the structure of formula 1: or a pharmaceutically acceptable salt thereof; forming a complex between the compound and the antigen-presenting cell, wherein the formation of the complex results in the activation of a receptor on the lymphocyte; and activating the lymphocyte to produce the cytokine response.
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公开(公告)号：GB2461656A
公开(公告)日：2010-01-13
申请号：GB0917142
申请日：2009-07-10
Applicant: ACADEMIA SINICA
Inventor： WONG CHI-HUEY , YU ALICE , CHANG YA-JEN , LIN KUN-HSIEN , CHENG Y S EDMOND , JAN JIA-TSRONG , LIN YI-LING , HUNG JUNG-TUNG
IPC: C07H15/18 , A61K31/7034 , A61P31/04 , A61P31/12 , A61P31/14 , A61P31/16 , A61P31/18 , A61P31/20 , A61P35/00 , A61P43/00
Abstract: The present disclosure relates to synthetic alpha-galaclosyl ceramide (alpha-GalCer) analogs, and their use as immunotherapies, adjuwants, and antiviral, antibacterial, and anticancer agents. In one aspect, a method of activating a cytokine response in a subject includes administering an effective amount of a compound to a subject, wherein the subject has an adaptive immune system that includes a population of cells, the population including at least one lymphocyte and at least one antigen-presenting cell, and wherein the compound is represented by the structure of formula 1:: or a pharmaceutically acceptable salt thereof; forming a complex between the compound and the antigen-presenting cell, wherein the formation of the complex results in the activation of a receptor on the lymphocyte; and activating the lymphocyte to produce the cytokine response.
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公开(公告)号：CA2697837A1
公开(公告)日：2009-03-05
申请号：CA2697837
申请日：2008-08-29
Applicant: ACADEMIA SINICA
Inventor： WONG CHI-HUEY , FANG JIM-MIN , SHIE JIUN-JIE , CHENG YIH-SHYUN EDMOND , JAN JIA-TSRONG
IPC: A61K31/7076 , A61K9/16 , A61K31/70 , A61K31/7052 , C07C233/52 , C07C247/14 , C07H19/04
Abstract: Novel phosphonate compounds are described. The compounds have activity as neuraminidase inhibitors against wild-type and H274Y mutant of H1N1 and H5N1 viruses. The present disclosure also provides an enantioselective synthetic route to known neuraminidase inhibitors oseltamivir and the anti-flu drug Tamiflu®, as well as novel phosphonate compounds, via D-xylose. Another efficient and flexible synthesis of Tamiflu and the highly potent neuraminidase inhibitor Tamiphosphor was also achieved in 11 steps and > 20% overall yields from the readily available fermentation product (1S-cis)-3-bromo-3,5- cyclohexadiene-1,2-diol. Most of the reaction intermediates were obtained as crystals without tedious purification procedures. The key transformations include an initial regio- and stereoselective bromoamidation of a bromoarene cis- dihydrodiol, as well as the final palladium-catalyzed carbonylation and phosphonylation.
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公开(公告)号：AU2005323435A1
公开(公告)日：2006-07-13
申请号：AU2005323435
申请日：2005-05-03
Applicant: ACADEMIA SINICA
Inventor： WONG CHI-HUEY , WU CHUNG-YI , JAN JIA-TSRONG
IPC: A61K31/44 , A61K31/165 , A61K31/325 , A61K31/40
Abstract: 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.
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