POLYOL-BASED OSMOTIC POLYDIXYLITOL POLYMER BASED GENE TRANSPORTER AND USE THEREOF

    公开(公告)号:EP3214178A4

    公开(公告)日:2018-07-11

    申请号:EP15854007

    申请日:2015-10-29

    摘要: The present invention relates to polydixylitol polymer based gene transporter (PdXYP) and a preparation method thereof. Further, the present invention relates to a nucleic acid delivery complex where the nucleic acids for treatment are conjugated to the gene transporter and a pharmaceutical composition for gene therapy including the complex as an active ingredient. In addition, the present invention relates to the gene transporter, gene delivery complex, and gene therapy using the gene transporter and gene delivery complex. It was confirmed that the PdXYP of the present invention has a considerably higher nucleic acid delivery rate than existing gene transporters, has almost no cytotoxicity in the conjugate when conjugated with DNA, also has very high in vivo transfection efficiency, and above all, especially has considerably high transfection efficiency for brain tissues, which has involved difficulty in gene therapy due to the blood brain barrier for a while. Accordingly, the gene transporter of the present invention can not only be used as experimental gene transporters, but can also be broadly used for various tissues in the body based on the nucleic acids for treatment to be conjugated in the field of gene therapy regarding various diseases.

    POLYOXAZOLINE ANTIBODY DRUG CONJUGATES
    8.
    发明公开

    公开(公告)号:EP3180388A4

    公开(公告)日:2018-04-04

    申请号:EP15826412

    申请日:2015-07-31

    IPC分类号: A61K47/60 A61P35/00

    摘要: In the present disclosure, polymer conjugates, including polymer-antibody-drug conjugates (polymer ADCs) are described, as well as the use of such conjugates to treat human disease. The polymer conjugates can contain a large number of polymer-bound agents, thus effectively increasing the drug antibody ration (DAR) of the antibody significantly beyond the currently available technology. This may be of particular importance when antibodies to low density antigens are used as target antibodies. The described polymer-ADCs have improved pharmacokinetics and solubility relative to traditional ADCs. The linker between agent and the polymer can be tailored to provide release of toxin at the desired site and under the desired conditions within the tumor. An additional feature of the polymer-ADCs of the current disclosure is that a purification moiety can be attached to the polymer backbone to provide ease of purification of the polymer-ADCs.

    METHOD FOR THE PREPARATION OF UNIFORM, HIGH MOLAR MASS CYCLIC IMINO ETHER POLYMERS
    10.
    发明公开
    METHOD FOR THE PREPARATION OF UNIFORM, HIGH MOLAR MASS CYCLIC IMINO ETHER POLYMERS 有权
    制备均匀高摩尔质量环状亚胺醚聚合物的方法

    公开(公告)号:EP3204442A1

    公开(公告)日:2017-08-16

    申请号:EP15736496.9

    申请日:2015-07-10

    申请人: Universiteit Gent

    IPC分类号: C08G73/02 C08L79/02

    摘要: A method for production of a uniform polymer of high molar mass is provides, the method comprising: (a) polymerizing cyclic imino ether monomer in a first reaction mixture by cationic ring opening polymerization to produce a polymerized first reaction mixture containing (i) polymerized material and (ii) solvent and/or unreacted cyclic imino ether monomer; (b) separating solvent and/or unreacted cyclic imino ether monomer from polymerized material contained in the polymerized first reaction mixture; (c) copolyerizing by cationic ring opening polymerization a second liquid reaction mixture containing cyclic imino ether monomer and solvent by combining the separated unreacted cyclic imino ether monomer and/or the separated solvent with other components. Also disclosed are polyoxazoline polymers comprising at least 50 wt. % of repeating units derived from a 2-substituted 2-oxazoline monomer selected from 2-methyl-2-oxazoline, 2-ethyl-2-oxazoline, 2-n-propyl-2-oxazoline, 2-i-propyl-2-oxazoline and combinations thereof, said polymer having a DP of at least 250 and a very low dispersity.

    摘要翻译: 提供一种制备高摩尔质量均匀聚合物的方法,所述方法包括:(a)通过阳离子开环聚合在第一反应混合物中聚合环状亚氨醚单体以产生聚合的第一反应混合物,所述第一反应混合物含有(i)聚合材料 和(ii)溶剂和/或未反应的环亚氨基醚单体; (b)从聚合的第一反应混合物中所含的聚合材料中分离溶剂和/或未反应的环亚氨基醚单体; (c)通过阳离子开环聚合共聚合含有环状亚氨醚单体和溶剂的第二液体反应混合物,方法是将分离的未反应的环亚氨基醚单体和/或分离的溶剂与其它组分混合。 还公开了聚恶唑啉聚合物,其包含至少50wt。 由选自2-甲基-2-恶唑啉,2-乙基-2-恶唑啉,2-正丙基-2-恶唑啉,2-异丙基-2-恶唑啉的2-取代2-唑啉单体衍生的重复单元的% 唑啉及其组合,所述聚合物具有至少250的DP和非常低的分散性。