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    SYNTHESIS OF OSELTAMIVIR CONTAINING PHOSPHONATE CONGENERS WITH ANTI-INFLUENZA ACTIVITY
    5.
    发明专利
    SYNTHESIS OF OSELTAMIVIR CONTAINING PHOSPHONATE CONGENERS WITH ANTI-INFLUENZA ACTIVITY 未知

    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.

    ALPHA-GALACTOSYL CERAMIDE ANALOGS AND THEIR USE AS IMMUNOTHERAPIES, ADJUVANTS, AND INTIVIRAL, ANTIBACTERIAL, AND ANTICANCER AGENTS
    8.
    发明申请
    ALPHA-GALACTOSYL CERAMIDE ANALOGS AND THEIR USE AS IMMUNOTHERAPIES, ADJUVANTS, AND INTIVIRAL, ANTIBACTERIAL, AND ANTICANCER AGENTS 审中-公开
    ALPHA-GALACTOSYL CERAMIDE ANALOGS及其作为免疫抑制剂，调节剂和杀虫剂，抗真菌剂和抗原剂的用途

    公开(公告)号：WO2010006315A3

    公开(公告)日：2010-03-25

    申请号：PCT/US2009050328

    申请日：2009-07-10

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

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

    IPC: A61K39/39 ,  A61K31/70 ,  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 (a- GalCer) analogs, and their use as immunotherapies, adjuvants, and antiviral, antibacterial, and anticancer agents. 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.

    Abstract translation: 本公开内容涉及合成的α-半乳糖神经酰胺（a-GalCer）类似物，以及它们作为免疫疗法，佐剂和抗病毒，抗菌和抗癌剂的用途。 一方面，在受试者中激活细胞因子应答的方法包括向受试者施用有效量的化合物，其中所述受试者具有包括细胞群的适应性免疫系统，所述群体包括至少一种淋巴细胞和 至少一种抗原呈递细胞，并且其中所述化合物由式1的结构表示： 或其药学上可接受的盐; 在化合物和抗原呈递细胞之间形成复合物，其中复合物的形成导致淋巴细胞上受体的活化; 并激活淋巴细胞以产生细胞因子反应。

    AGENTES ANTI - INFLUENZA CONJUGADOS CON ACTIVIDAD ANTI - INFLAMATORIA MEJORADOS.
    9.
    发明专利
    AGENTES ANTI - INFLUENZA CONJUGADOS CON ACTIVIDAD ANTI - INFLAMATORIA MEJORADOS. 未知

    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

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

    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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