公开(公告)号：EP2190439A4

公开(公告)日：2013-02-20

申请号：EP08828468

申请日：2008-08-29

Applicant: ACADEMIA SINICA

Inventor： FANG JIM-MIN ,  SHIE JIUN-JIE ,  WONG CHI-HUEY ,  CHENG YIH-SHYUN EDMOND ,  JAN JIA-TSRONG

IPC: A61K31/7076 ,  A61K9/16 ,  A61K31/7052 ,  C07C233/52 ,  C07C247/14 ,  C07H19/04

CPC classification number: A61K31/70 ,  A61K31/7076

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

IPC: A61K31/35 ,  A61K31/36 ,  A61K47/48 ,  A61P29/00 ,  A61P31/16

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.

公开(公告)号：EP2320947A4

公开(公告)日：2012-03-28

申请号：EP09795269

申请日：2009-07-10

Applicant: ACADEMIA SINICA

Inventor： WONG CHI-HUEY ,  YU ALICE ,  CHANG YA-JEN ,  LIN KUN-HSIEN ,  CHENG EDMOND Y S ,  JAN JIA-TSRONG ,  LIN YI-LING ,  HUNG JUNG-TUNG

IPC: C07H15/18 ,  A61K31/70 ,  A61K31/7034 ,  A61K39/00 ,  A61K39/39 ,  A61P31/04 ,  A61P31/16 ,  A61P35/00

CPC classification number: C07H15/18 ,  A61K31/7034 ,  A61K39/0011 ,  A61K2039/57

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.