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    GLOBO H AND STAGE SPECIFIC EMBRYONIC ANTIGENS AND Bb4 AND RELATED ANTI-CANCER VACCINES WITH NOVEL GLYCOLIPID ADJUVANTS
    161.
    发明专利
    GLOBO H AND STAGE SPECIFIC EMBRYONIC ANTIGENS AND Bb4 AND RELATED ANTI-CANCER VACCINES WITH NOVEL GLYCOLIPID ADJUVANTS 未知

    公开(公告)号：NZ590140A

    公开(公告)日：2012-07-27

    申请号：NZ59014009

    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: Disclosed is an immunogenic composition comprising: (a) a glycan conjugate including a carrier protein, and a glycan including Globo H, an immunogenic fragment thereof, or stage-specific embryonic antigen-4 (SSEA-4), wherein the glycan is conjugated with the carrier protein through a linker; and (b) an adjuvant including C34, wherein C34 is defined in the specification. Also disclosed is the use of the immunogenic composition in the manufacture of a medicament for the treatment or inhibition of tumor growth, wherein administration of medicament induces au immune response that produces a higher relative level of IgG isotype antibodies as compared to IgM isotype antibodies.

    GLOBO H AND RELATED ANTI-CANCER VACCINES WITH NOVEL GLYCOLIPID ADJUVANTS
    163.
    发明专利
    GLOBO H AND RELATED ANTI-CANCER VACCINES WITH NOVEL GLYCOLIPID ADJUVANTS 未知

    公开(公告)号：CA2728341A1

    公开(公告)日：2010-01-14

    申请号：CA2728341

    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: Immunogenic compositions, cancer vaccines and methods for treating cancer are provided. Compositions comprising: (a) a glycan such as Globo H or an immunogenic fragment thereof, wherein the glycan is conjugated with a carrier protein by a linker such as para-nitrophenyl; and (b) an adjuvant comprising glycolipid capable of binding CDId on a dendritic cell, such as an a-galactosyl-ceramide derivative, wherein the immunogenic composition induces an immune response that induces a higher relative level of IgG isotype antibodies as compared to IgM isotype antibodies, are provided. Immunogenic compositions comprising the carrier protein diphtheria toxin cross-reacting material 197 (DT-CRM 197) and the adjuvant C34 are provided. Antibodies generated by immunogenic compositions disclosed herein further neutralize at least one of the antigens Globo H, stage-specific embryonic antigen-3 (SSEA-3) and stage-specific embryonic antigen-4 (SSEA-4). Therapeutics against breast cancer stem cells comprising immunogenic compositions comprising Globo H, SSEA-3 or SSEA-4 conjugated with DT-CRM 197.

    SYNTHESIS OF OSELTAMIVIR CONTAINING PHOSPHONATE CONGENERS WITH ANTI-INFLUENZA ACTIVITY
    166.
    发明专利
    SYNTHESIS OF OSELTAMIVIR CONTAINING PHOSPHONATE CONGENERS WITH ANTI-INFLUENZA ACTIVITY 未知

    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.

    ALPHA-GALACTOSYL CERAMIDE ANALOGS AND THEIR USE AS IMMUNOTHERAPIES
    167.
    发明专利
    ALPHA-GALACTOSYL CERAMIDE ANALOGS AND THEIR USE AS IMMUNOTHERAPIES 未知

    公开(公告)号：CA2683681A1

    公开(公告)日：2008-10-23

    申请号：CA2683681

    申请日：2008-04-14

    Applicant: ACADEMIA SINICA

    Inventor： WONG CHI-HUEY ,  YU ALICE ,  CHANG YA-JEN

    IPC: A61K8/42 ,  A61K8/00 ,  C07C235/80 ,  C07C237/10

    Abstract: The present disclosure relates to synthetic alpha-galactosyl ceramide (.a lpha.-GalCer) analogs, and their use as immunotherapies. In one aspect, a me thod of activating a cytokine response in a subject includes administering a n effective amount of a compound to a subject, wherein the subject has an ad aptive immune system that includes a population of cells, the population inc luding at least one lymphocyte and at least one antigen-presenting cell, and wherein the compound is represented by the structure of formula (1) wherein , n is 0 to 25; X is selected from O and S; R1is selected from H, CH3, and p henyl, where phenyl is optionally substituted with H, OH, OCH3, F, CF3, phen yl, phenyl-F, C1-C6 alkyl, or C2-C6 branched alkyl; R2 is selected from OH a nd H; R3 is selected from C1-C15 alkyl, and phenyl, where phenyl is optional ly substituted with H, OH, OCH3, F, CF3, phenyl, C1-C6 alkyl, or C2-C6 branc hed alkyl; R4 is selected from OH, OSO3H, OSO3Na, and OSO3K; and R5 is selec ted from CH2OH and CO2H; or a pharmaceutically acceptable salt thereof; form ing 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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