POLYMER CONJUGATES
    2.
    发明申请
    POLYMER CONJUGATES 审中-公开
    聚合物混合物

    公开(公告)号:WO2003062290A1

    公开(公告)日:2003-07-31

    申请号:PCT/GB2003/000131

    申请日:2003-01-16

    IPC分类号: C08F246/00

    CPC分类号: C08F246/00

    摘要: The present invention relates to conjugates of biologically active compounds, preferably therapeutically active compounds, with polymeric moieties having low polydispersity, as well as controlled polymerisation processes for producing the conjugates. An initiation for a controlled radical polymerisation process comprises a biologically active, usually therapeutically active, moiety and the monomer includes zwitterionic monomer for instance 2-methacryloyloxyethyl-2'-trimethylammonium ethyl phosphate inner salt. The process allows close control of the molecular weight and polydispersity of the polymeric moiety and the possibility of optimising the delivery characteristics of the active agent.

    摘要翻译: 本发明涉及生物活性化合物,优选治疗活性化合物与具有低多分散性的聚合物部分的缀合物,以及用于产生缀合物的受控聚合方法。 受控自由基聚合方法的引发包括生物活性的,通常为治疗活性的部分,并且单体包括两性离子单体,例如2-甲基丙烯酰氧基乙基-2'-三甲基铵乙基磷酸内酯盐。 该方法允许密切控制聚合物部分的分子量和多分散性以及优化活性剂的递送特性的可能性。

    DRUG DELIVERY FROM EMBOLIC AGENTS
    4.
    发明申请
    DRUG DELIVERY FROM EMBOLIC AGENTS 审中-公开
    药物从药剂代用药

    公开(公告)号:WO2006013309A1

    公开(公告)日:2006-02-09

    申请号:PCT/GB2004/003347

    申请日:2004-08-03

    IPC分类号: A61L24/00

    摘要: A pharmaceutical composition for embolisation of blood vessels, especially for benign tumours, comprises a polymeric embolic agent and, associated with the polymer in a releasable form, a local anaesthetic agent. The polymer is preferably in particulate form, such as in the form of microspheres. A suitable polymer is a crosslinked polyvinyl alcohol polymer formed by the copolymerisation of PVA macromer with other ethylenically unsaturated monomers. The composition provides a synergistic treatment for the symptoms of turnours such as uterine fibroids, leading to size regression as well as pain relief.

    摘要翻译: 用于血管栓塞的药物组合物,特别是用于良性肿瘤的药物组合物包含聚合物栓塞剂,并且与可释放形式的聚合物相关联的局部麻醉剂。 聚合物优选为颗粒形式,例如以微球的形式。 合适的聚合物是通过PVA大分子单体与其它烯属不饱和单体的共聚形成的交联聚乙烯醇聚合物。 该组合物对诸如子宫肌瘤等症状的症状进行协同治疗,导致大小消退以及疼痛缓解。

    CONJUGATION REACTIONS
    8.
    发明申请
    CONJUGATION REACTIONS 审中-公开
    联合反应

    公开(公告)号:WO2004063237A1

    公开(公告)日:2004-07-29

    申请号:PCT/GB2004/000140

    申请日:2004-01-16

    IPC分类号: C08F246/00

    摘要: An initiator for the terminal group of the polymer product of an atom or group radical transfer polymerisation has an activated carboxyl or an amine group which is reacted with an amine or carboxyl (respectively) group containing biologically active compound. The initiator is preferably 4-(3-(2­ bromo, 2-methyl-prop ionate)phenyl)-prop ionic acid N-hydroxysuccinimide ester or 2-bromo, 2-methyl-propionic acid N-hydroxysuccinimide ester. The monomers preferably comprise a zwitterionic monomer such as 2­- methacryloxyethyl-2'-trimethyl ammoniumethyl phosphate inner salt

    摘要翻译: 原子或基团自由基转移聚合的聚合物产物的末端基团的引发剂具有活化的羧基或与含有胺或羧基(分别)含有生物活性化合物的基团)反应的胺基。 引发剂优选是4-(3-(2-溴,2-甲基 - 丙酰基)苯基) - 离子酸N-羟基琥珀酰亚胺酯或2-溴-2-甲基 - 丙酸N-羟基琥珀酰亚胺酯。 单体优选包含两性离子单体,例如2-甲基丙烯酰氧基乙基-2'-三甲基磷酸铵乙酯内盐