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    Method for preparing natural bioactive peptide Tubulysin U
    6.
    发明授权
    Method for preparing natural bioactive peptide Tubulysin U 有权

    公开(公告)号：US11702444B2

    公开(公告)日：2023-07-18

    申请号：US17984642

    申请日：2022-11-10

    申请人： Shenzhen Institute of Geriatrics ,  Zhengzhi Wu

    发明人： Zhengzhi Wu ,  Bohua Long ,  Limin Li ,  Zhiyue Li ,  Zhanyan Liu

    IPC分类号： C07K1/00 ,  C07K1/02 ,  C07K1/22

    CPC分类号： C07K1/026 ,  C07K1/22

    摘要： A preparation method of a novel natural bioactive peptide Tubulysin U includes: dissolving a compound 2 in trifluoroacetic acid, heating under reflux to prepare an intermediate, reacting with a compound 3 and N,N-diisopropylethylamine to obtain a product, reacting the product with 2, 6-dimethylpyridine and tert-butyldimethylsilyl trifluoromethanesulfonate, adding sodium hydroxide after the reaction to prepare an intermediate acid, reacting the intermediate acid with a compound 6, HATU and N,N-diisopropylethylamine to obtain a product, adding triphenylphosphine to prepare an intermediate amine, adding a compound 8 and HATU to react, adding ammonium fluoride to prepare a first intermediate, adding sodium hydroxide to the first intermediate to prepare a second intermediate, adding acetic anhydride to the second intermediate to prepare a third intermediate, adding trifluoroacetic acid to the third intermediate to prepare a fourth intermediate, and adding formaldehyde and sodium cyanoborohydride to the fourth intermediate to react, thereby obtaining a target product.

    METHOD FOR PREPARING LIRAGLUTIDE USING ENVIRONMENT-FRIENDLY SOLVENT
    7.
    发明申请
    METHOD FOR PREPARING LIRAGLUTIDE USING ENVIRONMENT-FRIENDLY SOLVENT 有权

    公开(公告)号：US20230047729A1

    公开(公告)日：2023-02-16

    申请号：US17963739

    申请日：2022-10-11

    申请人： DAEBONG LS CO., LTD.

    发明人： Eun Ju PARK ,  Eun Teak KIM ,  Jin Oh PARK

    IPC分类号： C07K1/10 ,  C07K1/02

    摘要： Proposed is a novel method for preparing liraglutide by means of an ionic liquid and a eutectic solvent, which are environment-friendly solvents. More specifically, the method is characterized in that fractionated peptide 1 represented by the following formula (1) and fractionated peptide 2 represented by the following formula (2) are subjected to a coupling reaction in the presence of an ionic liquid or a eutectic solvent. In preparing GLP-1 analogues such as liraglutide, the present method increases reactivity when producing liraglutide, which is an unprocessed reactant, by using an ionic liquid and a eutectic solvent as environment-friendly solvents instead of using organic solvents. Accordingly, through a relatively short and simple purification process, the present method has advantages of reducing the formation of related substances, improving purity, improving yields, shortening reaction times, reducing production cost, and lowering the manufacturing cost.

    RNA OLIGONUCLEOTIDES FOR PREVENTING AGGREGATION OF PROTEINS
    8.
    发明申请
    RNA OLIGONUCLEOTIDES FOR PREVENTING AGGREGATION OF PROTEINS 有权

    公开(公告)号：US20220411794A1

    公开(公告)日：2022-12-29

    申请号：US17771790

    申请日：2020-10-23

    申请人： Universitaet Wien

    发明人： Bojan ZAGROVIC ,  Anton POLYANSKY

    IPC分类号： C12N15/113 ,  C07K1/02 ,  C07K16/32

    摘要： A composition comprising a protein and at least one single-stranded linear RNA oligonucleotide with an unfolded tertiary structure, which is characterized by: a) a relative content of each of the nucleotides A, C, U, and G, which is the number of each of the nucleotides per total nucleotide number in the oligonucleotide, which relative content is the same ±10% (number of nucleotides per total nucleotide number) as compared to the relative content of the respective nucleotide in a reference; and/or b) a relative content of at least 50% (number of nucleotides per total nucleotide number) of one type of nucleotide selected from the group consisting of nucleotides A, C, U, and G, which exhibits the highest relative content (number of each of the nucleotides per total nucleotide number) in a reference; wherein the reference consists of a native mRNA or a set of different RNA sequences that covers all RNA sequences allowed by the universal genetic code, each encoding an amino acid sequence of at least three amino acids within a p re-determined aggregation-prone target region of said protein, wherein the oligonucleotide has a length which is the same length as the reference, or longer.

    Method for producing amide compound
    9.
    发明授权
    Method for producing amide compound 有权

    公开(公告)号：US11512108B2

    公开(公告)日：2022-11-29

    申请号：US17047464

    申请日：2019-04-25

    申请人： CHUBU UNIVERSITY EDUCATIONAL FOUNDATION

    发明人： Hisashi Yamamoto ,  Wataru Muramatsu ,  Tomohiro Hattori

    IPC分类号： C07K1/08 ,  C07K1/00 ,  C07C231/02 ,  C07K1/02

    摘要： Provided is a novel method whereby an amide compound can be produced by highly stereoselectively and efficiently performing amidation between a plurality of amino acids and/or peptides. A compound of general formula (3) is synthesized by forming an amide bond between the carboxyl group on the right side of general formula (1) in a compound represented thereby and the amino group on the left side of general formula (2) in a compound represented thereby, in the presence of a Lewis acid catalyst and a silylating agent [in formulae (1), (2) and (3), each symbol has the same meaning as defined in claims].

    PEPTIDE SYNTHESIS
    10.
    发明申请
    PEPTIDE SYNTHESIS 有权

    公开(公告)号：US20220332754A1

    公开(公告)日：2022-10-20

    申请号：US17309150

    申请日：2019-11-04

    申请人： ORIGIN PEPTIDES LIMITED

    发明人： Sara TEN HAVE

    IPC分类号： C07K1/02 ,  C07K14/62

    摘要： There is provided a method to synthesise peptides, a peptide being synthesised based on the amino acid sequence of a template peptide, peptides provided by the method and use of the peptides.