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公开(公告)号：CA2927699C
公开(公告)日：2022-07-05
申请号：CA2927699
申请日：2014-10-22
Applicant: ACADEMIA SINICA
Inventor： FANG JIM-MIN , LIN YUN-LIAN , LIN JUNG-HSIN , LIN CHUN-JUNG , CHERN YIJUANG , HUANG NAI-KUEI , WANG HUNG-LI , TU BENJAMIN PANG-HSIEN , CHEN CHIH-CHENG
IPC: C07H19/167 , A61K31/7076 , A61P25/28 , A61P29/00 , C07D498/02
Abstract: Compounds for use in prevention and treatment of neurodegenerative disease and pain are disclosed. In one embodiment of the invention, the compound is selected from the group consisting of N 6 -[(3-halothien-2-yl)methyl]adenosine, N 6 -[(4-halothien-2-yl)methyl]adenosine, and N 6 -[(5-halothien-2-yl)methyl]adenosine. In another embodiment of the invention, the compound is selected from the group consisting of N 6 -[(2-bromothien-3-yl)methyl]adenosine, N 6 -[(4-bromothien-3-yl)methyl]adenosine, N 6 -[(5-bromothien-3-yl)methyl]adenosine N 6 -[(2-chlorothien-3-yl)methyl]adenosine, N 6 -[(4-chlorothien-3-yl)methyl]adenosine, and N 6 -[(5-chlorothien-3-yl)methyl]adenosine. Also disclosed are methods of making and using the same.
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公开(公告)号：AU2014340114B2
公开(公告)日：2018-10-18
申请号：AU2014340114
申请日：2014-10-22
Applicant: ACADEMIA SINICA
Inventor： FANG JIM-MIN , LIN YUN-LIAN , LIN JUNG-HSIN , LIN CHUN-JUNG , CHERN YIJUANG , HUANG NAI-KUEI , WANG HUNG-LI , TU BENJAMIN PANG-HSIEN , CHEN CHIH-CHENG
IPC: C07D498/02 , C07D515/02
Abstract: Compounds for use in prevention and treatment of neurodegenerative disease and pain are disclosed. In one embodiment of the invention, the compound is selected from the group consisting of
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公开(公告)号：SG11201603063WA
公开(公告)日：2016-05-30
申请号：SG11201603063W
申请日：2014-10-22
Applicant: ACADEMIA SINICA
Inventor： FANG JIM-MIN , LIN YUN-LIAN , LIN JUNG-HSIN , LIN CHUN-JUNG , CHERN YIJUANG , HUANG NAI-KUEI , WANG HUNG-LI , TU BENJAMIN PANG-HSIEN , CHEN CHIH-CHENG
IPC: C07D498/02 , C07D515/02
Abstract: Compounds for use in prevention and treatment of neurodegenerative disease and pain are disclosed. In one embodiment of the invention, the compound is selected from the group consisting of N6-[(3-halothien-2-yl)methyl]adenosine, N6-[(4-halothien-2-yl)methyl]adenosine, and N6-[(5-halothien-2-yl)methyl]adenosine. In another embodiment of the invention, the compound is selected from the group consisting of N6-[(2-bromothien-3-yl)methyl]adenosine, N6-[(4-bromothien-3-yl)methyl]adenosine, N6-[(5-bromothien-3-yl)methyl]adenosine N6-[(2-chlorothien-3-yl)methyl]adenosine, N6-[(4-chlorothien-3-yl)methyl]adenosine, and N6-[(5-chlorothien-3-yl)methyl]adenosine. Also disclosed are methods of making and using the same.
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公开(公告)号：CA2927699A1
公开(公告)日：2015-04-30
申请号：CA2927699
申请日：2014-10-22
Applicant: ACADEMIA SINICA
Inventor： FANG JIM-MIN , LIN YUN-LIAN , LIN JUNG-HSIN , LIN CHUN-JUNG , CHERN YIJUANG , HUANG NAI-KUEI , WANG HUNG-LI , TU BENJAMIN PANG-HSIEN , CHEN CHIH-CHENG
IPC: C07D498/02 , A61K31/7076 , A61P25/28 , A61P29/00
Abstract: Compounds for use in prevention and treatment of neurodegenerative disease and pain are disclosed. In one embodiment of the invention, the compound is selected from the group consisting of N 6 -[(3-halothien-2-yl)methyl]adenosine, N 6 -[(4-halothien-2-yl)methyl]adenosine, and N 6 -[(5-halothien-2-yl)methyl]adenosine. In another embodiment of the invention, the compound is selected from the group consisting of N 6 -[(2-bromothien-3-yl)methyl]adenosine, N 6 -[(4-bromothien-3-yl)methyl]adenosine, N 6 -[(5-bromothien-3-yl)methyl]adenosine N 6 -[(2-chlorothien-3-yl)methyl]adenosine, N 6 -[(4-chlorothien-3-yl)methyl]adenosine, and N 6 -[(5-chlorothien-3-yl)methyl]adenosine. Also disclosed are methods of making and using the same.
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5.发明专利
公开(公告)号：HUE050104T2
公开(公告)日：2020-11-30
申请号：HUE13819542
申请日：2013-07-19
Applicant: ACADEMIA SINICA , UNIV NAT TAIWAN
Inventor： CHEN CHING-CHOW , CHEN JHIH-BIN , WEI TZU-TANG , LIN JUNG-HSIN , FANG JIM-MIN , CHERN TING-RONG
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Patent Agency Ranking
公开(公告)号：ZA201603118B
公开(公告)日：2019-04-24
申请号：ZA201603118
申请日：2016-05-10
Applicant: ACADEMIA SINICA
Inventor： FANG JIM-MIN , LIN YUN-LIAN , LIN JUNG-HSIN , LIN CHUN-JUNG , CHERN YIJUANG , HUANG NAI-KUEI , WANG HUNG-LI , TU BENJAMIN PANG-HSIEN , CHEN CHIH-CHENG
Abstract: Compounds for use in prevention and treatment of neurodegenerative disease and pain are disclosed. In one embodiment of the invention, the compound is selected from the group consisting of N6-[(3-halothien-2-yl)methyl]adenosine, N6-[(4-halothien-2-yl)methyl]adenosine, and N6-[(5-halothien-2-yl)methyl]adenosine. In another embodiment of the invention, the compound is selected from the group consisting of N6-[(2-bromothien-3-yl)methyl]adenosine, N6-[(4-bromothien-3-yl)methyl]adenosine, N6-[(5-bromothien-3-yl)methyl]adenosine N6-[(2-chlorothien-3-yl)methyl]adenosine, N6-[(4-chlorothien-3-yl)methyl]adenosine, and N6-[(5-chlorothien-3-yl)methyl]adenosine. Also disclosed are methods of making and using the same.
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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：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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