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    • 9. 发明申请
    • POLYOXAZOLINE POLYMERS AND METHODS FOR THEIR PREPARATION, CONJUGATES OF THESE POLYMERS AND MEDICAL USES THEREOF
    • 聚氧乙烯聚合物及其制备方法,这些聚合物的结合及其医疗用途
    • US20150025196A1
    • 2015-01-22
    • US14370181
    • 2012-12-28
    • Universiteit Gent
    • Richard Hoogenboom
    • A61K47/48A61K51/06A61K31/704
    • A61K47/48192A61K47/34A61K47/50A61K47/51A61K47/56A61K47/59A61K47/64A61K51/06A61K51/065C08G73/0233C08L79/02
    • The present invention relates to functionalized ploy(2-oxazoline) polymers, which are very suitable as a carrier and/or delivery vehicle (conjugate) of drugs, such as small therapeutic molecules and bio-pharmaceuticals. These polymers are characterized in that they comprise repeating units that are represented by the following formula —[N(R1)—(CHR2)m]- wherein R1 is R3—(CHR4)n-CONH—R5; R2 is selected from H and optionally substituted C1-5alkyl; R3 is CH2CO, C(O)O, C(O)NH OR C(S)NH; R4 is selected from H and optionally substituted C1-5alkyl; R5 is H; an C1-5alkyl; aryl; or a moiety comprising a functional group that can be used for conjugation; m is 2 or 3 and n is 1-5; or n is 0 and R3 is CH2. The invention relates further to a conjugate of these polyoxazoline polymers with at least one active moiety, such as a therapeutic moiety, a targeting moiety and/or diagnostic moiety, and to the use of these conjugates in the therapeutic treatment or prophylactic treatment or diagnosis of a disease or disorder.
    • 本发明涉及非常适合作为药物如小的治疗分子和生物药物的载体和/或递送载体(缀合物)的官能化的(2-恶唑啉)聚合物。 这些聚合物的特征在于它们包含由下式表示的重复单元 - [N(R1) - (CHR2)m] - ,其中R1是R3-(CHR4)n-CONH-R5; R2选自H和任选取代的C 1-5烷基; R 3是CH 2 CO,C(O)O,C(O)NH OR C(S)NH; R4选自H和任选取代的C 1-5烷基; R5是H; C 1-5烷基; 芳基; 或包含可用于缀合的官能团的部分; m为2或3,n为1-5; 或n为0且R 3为CH 2。 本发明还涉及这些聚恶唑啉聚合物与至少一个活性部分(例如治疗部分,靶向部分和/或诊断部分)的缀合物,以及这些缀合物在治疗性或预防性治疗或诊断中的用途 疾病或病症