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    Esterification/saponification-based method for liposomal encapsulation of hydrophilic glucuronides
    52.
    发明授权
    Esterification/saponification-based method for liposomal encapsulation of hydrophilic glucuronides 有权

    公开(公告)号：US11013690B2

    公开(公告)日：2021-05-25

    申请号：US16067643

    申请日：2017-01-04

    Applicant: Academia Sinica

    Inventor： Steve R. Roffler ,  Pierre-Alain Burnouf

    IPC: A61K9/127 ,  A61K47/54 ,  A61K47/69 ,  A61P35/00

    Abstract: Described herein is a method for loading a hydrophilic compound into liposomes after addition of an alkylester group to form an esterified compound. After loading, the alkylester is hydrolyzed to reform the hydrophilic compound inside the liposomes. Also described is a method for loading drugs under a glucuronide methylester form into liposomes. The glucuronide methylester form of the drug is saponified to a glucuronide form of the drug inside the liposomes for better drug retention. The glucuronide residue conjugated to drugs can be removed inside cells to regenerate the parental drug upon cell uptake, liposomal degradation and enzyme hydrolysis. In case of cancer, this method can be used to safely deliver drugs to tumors.

    Treatment of Fabry disease
    54.
    发明授权
    Treatment of Fabry disease 有权

    公开(公告)号：US10995067B2

    公开(公告)日：2021-05-04

    申请号：US16313057

    申请日：2017-06-14

    Applicant: Academia Sinica

    Inventor： Wei-Chieh Cheng

    IPC: A61K31/7028 ,  C07D207/02 ,  C07D207/12 ,  A61K31/40 ,  A61K45/06 ,  A61P3/00 ,  A61K38/47

    Abstract: Disclosed herein are novel uses of a polyhydroxylated pyrrolidine for the manufacture of a medicament for treating Fabry disease (FD). Accordingly, the present disclosure provides a method of treating a subject having or suspected of having FD. The method includes the step of, administering to the subject a therapeutically effective amount of a compound of formula (I), a salt, an ester or a solvate thereof, wherein: R1 is H, or C1-3 amine optionally substituted with —COR2; R2 is alkyl or alkene optionally substituted with cycloalkyl or phenyl having at least one substituent selected from the group consisting of, halo, alkyl, haloalkyl, and alkoxyl; so as to ameliorate, alleviate mitigate and/or prevent symptoms associated with the FD. According to preferred embodiments of the present disclosure, the compound of formula (I) is a chaperon of a mutated human lysosomal α-galactosidase A (α-Gal A).

    CAPTURE, PURIFICATION, AND RELEASE OF BIOLOGICAL SUBSTANCES USING A SURFACE COATING
    58.
    发明申请
    CAPTURE, PURIFICATION, AND RELEASE OF BIOLOGICAL SUBSTANCES USING A SURFACE COATING 有权

    公开(公告)号：US20210088514A1

    公开(公告)日：2021-03-25

    申请号：US16832396

    申请日：2020-03-27

    Applicant: Academia Sinica

    Inventor： Ying-Chih CHANG ,  Han-Chung WU ,  Po-Yuan TSENG ,  Jen-Chia WU

    IPC: G01N33/543 ,  C07K17/14 ,  C07K16/30 ,  G01N33/574 ,  G01N1/40

    Abstract: This invention relates to a surface coating for capture circulating rare cells, comprising a nonfouling composition to prevent the binding of non-specific cells and adsorption of serum components; a bioactive composition for binding the biological substance, such as circulating tumor cells; with or without a linker composition that binds the nonfouling and bioactive compositions. The invention also provide a surface coating for capture and purification of a biological substance, comprising a releasable composition to release the non-specific cells and other serum components; a bioactive composition for binding the biological substance, such as circulating tumor cells; with or without a linker composition that binds the releasable and bioactive compositions. The present invention also discloses a novel microfluidic chip, with specific patterned microstructures to create a flow disturbance and increase the capture rate of the biological substance.

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