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.

公开(公告)号：AU2015267045A1

公开(公告)日：2017-01-05

申请号：AU2015267045

申请日：2015-05-27

Applicant: ACADEMIA SINICA

Inventor： WONG CHI-HUEY ,  WU CHUNG-YI

IPC: C07K16/00

Abstract: The present disclosure relates to a novel class of anti-HER2 monoclonal antibodies comprising a homogeneous population of anti-HER2 IgG molecules having the same N-glycan on each of Fc. The antibodies of the invention can be produced from anti-HER2 monoclonal antibodies by Fc glycoengineering. Importantly, the antibodies of the invention have improved therapeutic values with increased ADCC activity and increased Fc receptor binding affinity compared to the corresponding monoclonal antibodies that have not been glycoengineered.

公开(公告)号：AU2015267052A1

公开(公告)日：2016-12-15

申请号：AU2015267052

申请日：2015-05-27

Applicant: ACADEMIA SINICA

Inventor： WU CHUNG-YI ,  MA CHE ,  WONG CHI-HUEY

IPC: C07K16/28

Abstract: The present disclosure relates to glycoproteins, particularly monoclonal antibodies, comprising a glycoengineered Fc region, wherein said Fc region comprises an optimized N-glycan having the structure of Sia

公开(公告)号：CA2697837C

公开(公告)日：2016-08-16

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: A61K31/662 ,  A61P31/16

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.

公开(公告)号：AU2016206315A1

公开(公告)日：2016-08-11

申请号：AU2016206315

申请日：2016-07-21

Applicant: ACADEMIA SINICA

Inventor： WONG CHI-HUEY ,  WU CHUNG-YI ,  TSAI TSUNG-I

IPC: C12P19/04 ,  C12N9/10

Abstract: Abstract A novel UDP-Gal regeneration process and its combined use with a galactosyltransferease to add galactose to a suitable acceptor substrate. Also described herein are synthetic methods for generating Globo-series oligosaccharides in large scale, wherein the methods may involve the combination of a glycosyltransferase reaction and a nucleotide sugar regeneration process.

公开(公告)号：ES2570630T3

公开(公告)日：2016-05-19

申请号：ES09789075

申请日：2009-08-06

Applicant: ACADEMIA SINICA

Inventor： WONG CHI-HUEY ,  WU CHUNG-YI ,  YU ALICE ,  YU JOHN

IPC: A61K39/00 ,  A61K39/385

Abstract: Una composición inmunogénica que comprende: (a) un glicano que consiste esencialmente en Globo H, el antígeno-3 específico de la etapa embrionaria (SSEA-3. Gb5) y el antígeno-4 específico de la etapa embrionaria (SSEA-4, sialil-Gb5), Bb4, o un fragmento inmunogénico del mismo, en el que el glicano que se conjuga con una proteína portadora es el material 197 que presenta reacción cruzada con la toxina de la difteria (DT-CRM197) o el toxoide de la difteria, a través de un enlazante; y (b) un adyuvante de α-galactosil-ceramida (α-GalCer).

公开(公告)号：AU2014317889A1

公开(公告)日：2016-03-17

申请号：AU2014317889

申请日：2014-09-08

Applicant: ACADEMIA SINICA

Inventor： WONG CHI-HUEY ,  YU ALICE L ,  LIN KUN-HSIEN ,  WU TAI-NA

IPC: A61K35/14 ,  A61K31/7012 ,  A61K31/739

Abstract: Glycosphingolipids (GSLs) bearing α-glucose (α-Glc) that preferentially stimulate human invariant NKT (iNKT) cells are provided. GSLs with α-glucose (α-Glc) that exhibit stronger induction in humans (but weaker in mice) of cytokines and chemokines and expansion and/or activation of immune cells than those with α-galactose (α-Gal) are disclosed. GSLs bearing α-glucose (α-Glc) and derivatives of α-Glc with F at the 4 and/or 6 positions are provided. Methods for iNKT-independent induction of chemokines by the GSL with α-Glc and derivatives thereof are disclosed. Methods for immune stimulation in humans using GSLs with α-Glc and derivatives thereof are provided.

公开(公告)号：ES2555220T3

公开(公告)日：2015-12-29

申请号：ES10756991

申请日：2010-03-29

Applicant: ACADEMIA SINICA

Inventor： WONG CHI-HUEY ,  WU CHUNG-YI ,  CHENG TING-JEN R ,  HSU CHE-HSIUNG

IPC: C07H13/04 ,  C07H1/00

Abstract: Un compuesto donante de sialil-fosfato para la síntesis de sialósidos, en donde el compuesto tiene la estructura:**Fórmula**

公开(公告)号：CA2950423A1

公开(公告)日：2015-12-03

申请号：CA2950423

申请日：2015-05-27

Applicant: ACADEMIA SINICA

Inventor： WONG CHI-HUEY ,  WU CHUNG-YI ,  MA CHE

IPC: C07K16/28

Abstract: The present disclosure relates to glycoproteins, particularly monoclonal antibodies, comprising a glycoengineered Fc region, wherein said Fc region comprises an optimized N-glycan having the structure of Sia2(a2-6)Gal2GlcNAc2Man3GlcNAc2. The glycoengineered Fc region binds Fc?RIIA or Fc?RIIIA with a greater affinity, relative to comparable monoclonal antibodies comprising the wild-type Fc region. The monoclonal antibodies of the invention are particularly useful in preventing, treating, or ameliorating one or more symptoms associated with a disease, disorder, or infection where an enhanced efficacy of effector cell function (e.g., ADCC) mediated by Fc?R is desired, e.g., cancer, autoimmune, infectious disease, and in enhancing the therapeutic efficacy of therapeutic antibodies the effect of which is mediated by ADCC.

公开(公告)号：CA2937123A1

公开(公告)日：2015-07-23

申请号：CA2937123

申请日：2015-01-16

Applicant: ACADEMIA SINICA

Inventor： WONG CHI-HUEY ,  LOU YI-WEI ,  LIN CHIH-WEI ,  YEH SHIH-CHI ,  HSU TSUI-LING ,  WU CHUNG-YI ,  WU HAN-CHUNG

IPC: A61K39/395 ,  G01N33/574

Abstract: Pharmaceutical composition comprising antibodies or antigen binding fragments thereof that bind to SSEA-4 are disclosed herein, as well as methods of use thereof. Methods of use include, without limitation, cancer therapies and diagnostics. The antibodies of the disclosure can bind to certain cancer cell surfaces. Exemplary targets of the antibodies disclosed herein can include carcinomas, such as those in brain, lung, breast, mouse, esophagus, stomach, liver, bile duct, pancreas, colon, kidney, cervix, ovary, and/or prostate cancer.