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公开(公告)号：AU2013245756B2
公开(公告)日：2017-09-28
申请号：AU2013245756
申请日：2013-04-12
Applicant: ACADEMIA SINICA , CHENG TING JEN R , CHENG YIH SHYUN E , FANG JIM MIN , JAN JIA TSRONG , LIU KUNG CHENG , WONG CHI HUEY
Inventor： WONG CHI-HUEY , FANG JIM-MIN , LIU KUNG-CHENG , JAN JIA-TSRONG , CHENG YIH-SHYUN E , CHENG TING-JEN R
IPC: C07D309/28 , A61K31/35 , A61K31/36 , A61P29/00 , A61P31/16
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：AU2013306098A1
公开(公告)日：2015-02-12
申请号：AU2013306098
申请日：2013-08-16
Applicant: WONG CHI-HUEY , FANG JIM-MIN , CHENG YIH SHYUN , ACADEMIA SINICA , TSAI CHARNG-SHENG
Inventor： WONG CHI-HUEY , FANG JIM-MIN , CHENG YIH-SHYUN E , TSAI CHARNG-SHENG
Abstract: Provided herein are novel irreversible sialidase inhibitors. These compounds can be conjugated with a detectable tagging moiety such as azide-annexed biotin via CuAAC for isolation and identification of sialidases. The provided compounds and the corresponding detectable conjugates are useful for detecting sialidase-containing pathogens and imaging
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公开(公告)号：CA2880701A1
公开(公告)日：2014-02-27
申请号：CA2880701
申请日：2013-08-16
Applicant: ACADEMIA SINICA , WONG CHI-HUEY , FANG JIM-MIN , CHENG YIH-SHYUN E , TSAI CHARNG-SHENG
Inventor： WONG CHI-HUEY , FANG JIM-MIN , CHENG YIH-SHYUN E , TSAI CHARNG-SHENG
Abstract: Provided herein are novel irreversible sialidase inhibitors. These compounds can be conjugated with a detectable tagging moiety such as azide-annexed biotin via CuAAC for isolation and identification of sialidases. The provided compounds and the corresponding detectable conjugates are useful for detecting sialidase-containing pathogens and imaging in situ sialidase activities under physiological conditions.
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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：MX2014012413A
公开(公告)日：2015-08-07
申请号：MX2014012413
申请日：2013-04-12
Applicant: ACADEMIA SINICA
Inventor： WONG CHI-HUEY , FANG JIM-MIN , LIU KUNG-CHENG , JAN JIA-TSRONG , CHENG YIH-SHYUN E , CHENG TING-JEN R
Abstract: Se describen novedosos fármacos anti-influenza bi-funcionales, de doble enfoque, formados mediante conjugación con agentes anti-inflamatorios. Fármacos ejemplares de acuerdo con la invención incluyen conjugados de zanamivir (ZA) que porta ácido cafeico (CA) ZA-7-CA (1), ZA-7-CA-amida (7) y ZA-7-Nap (43) para inhibición simultánea de neuraminidasa de virus de influenza y supresión de citosinas proinflamatorias. Se proporcionan métodos sintéticos para la preparación de estos fármacos conjugados anti-influenza mejorados. Los conjugados de ZA bifuncionales sintéticos actúan sinérgicamente hacia la protección de ratones infectados letalmente por virus de influenza H1N1 o H5N1. La eficacia de conjugados ZA-7-CA, ZA-7-CA-amida y ZA-7-Nap es mucho mayor que la terapia de combinación de ZA con agentes anti-inflamatorios.
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公开(公告)号：AU2013245756A1
公开(公告)日：2014-11-06
申请号：AU2013245756
申请日：2013-04-12
Applicant: WONG CHI-HUEY , LIU KUNG-CHENG , FANG JIM-MIN , CHENG YIH SHYUN , JAN JIA-TSRONG , ACADEMIA SINICA , CHENG TING JEN
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：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：EP2885311A4
公开(公告)日：2016-04-13
申请号：EP13831440
申请日：2013-08-16
Applicant: ACADEMIA SINICA
Inventor： WONG CHI-HUEY , FANG JIM-MIN , CHENG YIH-SHYUN E , TSAI CHARNG-SHENG
CPC classification number: C12Q1/40 , C07H5/00 , C07H13/04 , C07H13/12 , C12N9/2402 , C12Q1/04 , C12Q1/34 , C12Q1/70 , C12Y302/01018 , G01N2333/11
Abstract: Provided herein are novel irreversible sialidase inhibitors. These compounds can be conjugated with a detectable tagging moiety such as azide-annexed biotin via CuAAC for isolation and identification of sialidases. The provided compounds and the corresponding detectable conjugates are useful for detecting sialidase-containing pathogens and imaging in situ sialidase activities under physiological conditions.
Abstract translation: 本文提供了新的不可逆唾液酸酶抑制剂。 这些化合物可以通过CuAAC与可检测的标记部分如叠氮化物附着的生物素缀合，用于分离和鉴定唾液酸酶。 提供的化合物和相应的可检测的缀合物可用于检测含唾液酸酶的病原体并在生理条件下成像原位唾液酸酶活性。
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9.发明公开
公开(公告)号：EP2841066A4
公开(公告)日：2015-11-25
申请号：EP13775664
申请日：2013-04-12
Applicant: ACADEMIA SINICA , WONG CHI HEUY , 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
CPC classification number: A61K47/481 , 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.
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