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8 条记录 (耗时 0.021 秒)

    CONJUGATION REACTIONS
    1.
    发明申请
    CONJUGATION REACTIONS 有权
    联合反应

    公开(公告)号：US20120016082A1

    公开(公告)日：2012-01-19

    申请号：US13243923

    申请日：2011-09-23

    申请人： Andrew Lennard LEWIS ,  Simon William LEPPARD

    发明人： Andrew Lennard LEWIS ,  Simon William LEPPARD

    IPC分类号： C08F8/32 ,  C08F2/38 ,  C07D207/46

    CPC分类号： C08F246/00 ,  C07D207/46 ,  C07F9/091 ,  C07F9/5537 ,  C08F4/00

    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-propionate)phenyl)-propionic 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。 引发剂优选为4-（3-（2-溴，2-甲基 - 丙酸酯）苯基） - 丙酸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。

    DRUG DELIVERY FROM EMBOLIC AGENTS
    2.
    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：US20110182952A1

    公开(公告)日：2011-07-28

    申请号：US13084228

    申请日：2011-04-11

    申请人： Andrew Lennard LEWIS ,  Peter W. STRATFORD ,  Simon William LEPPARD

    发明人： Andrew Lennard LEWIS ,  Peter W. STRATFORD ,  Simon William LEPPARD

    IPC分类号： A61K9/14 ,  A61P23/02 ,  A61K31/167 ,  A61K31/245

    CPC分类号： A61L24/0015 ,  A61L24/0031 ,  A61L2300/402 ,  A61L2430/36

    摘要： A pharmaceutical composition for embolization 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 copolymerization of PVA macromer with other ethylenically unsaturated monomers. The composition provides a synergistic treatment for the symptoms of tumours such as uterine fibrioids, leading to size regression as well as pain relief.

    摘要翻译： 用于栓塞血管，特别是良性肿瘤的药物组合物包含聚合物栓塞剂，并且以可释放形式的聚合物与局部麻醉剂相关联。 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纤维样肿瘤的症状提供协同治疗，导致大小消退以及疼痛缓解。

    DRUG CARRIERS COMPRISING AMPHILPHILIC BLOCK COPOLYMERS
    3.
    发明申请
    DRUG CARRIERS COMPRISING AMPHILPHILIC BLOCK COPOLYMERS 审中-公开
    包含AMPHILPHILIC嵌段共聚物的药物载体

    公开(公告)号：US20120157550A1

    公开(公告)日：2012-06-21

    申请号：US13355910

    申请日：2012-01-23

    申请人： Andrew Lennard LEWIS ,  Steven Peter ARMES ,  Andrew W. LLOYD ,  Jonathan P. SALVAGE

    发明人： Andrew Lennard LEWIS ,  Steven Peter ARMES ,  Andrew W. LLOYD ,  Jonathan P. SALVAGE

    IPC分类号： A61K47/30 ,  A61P35/00

    CPC分类号： C08L53/00 ,  A61K9/1075 ,  C08F293/005 ,  C08L2666/02

    摘要： An aqueous composition comprises an amphiphilic block copolymer, having a hydrophilic block comprising pendant zwitterionic groups and a hydrophobic block, and a biologically active compound associated with the polymer. The polymer is preferably in the form of micelles, and preferably the biological active is a hydrophobic drug. The hydrophilic block is preferably formed from acrylic monomer including phosphorylcholine groups. The hydrophobic group is suitably formed from monomer which has groups which can be ionised at useful pH's, especially tertiary amine groups. Micelles may be formed by dissolving the block copolymer in aqueous solvent at a pH at which the amine groups are protonated then raising the pH to a value at which the amine groups are substantially deprotonated, whereupon micelles spontaneously form. The preformed micelles are then contacted with active, under conditions such that solubilisation of the active occurs. The active may be for tumour treatment.

    摘要翻译： 水性组合物包含具有包含侧基两性离子基团和疏水嵌段的亲水嵌段的两亲性嵌段共聚物和与聚合物缔合的生物活性化合物。 聚合物优选为胶束形式，优选生物活性物质为疏水性药物。 亲水性嵌段优选由包含磷酸胆碱基团的丙烯酸单体形成。 疏水基团适当地由具有可以在有用pH，特别是叔胺基团离子化的基团的单体形成。 胶束可以通过将嵌段共聚物溶解在水性溶剂中，在胺基质子化的pH下将pH升高至胺基基本上去质子化的值，由此胶束自发形成。 然后在预先形成的胶束与活性物质接触的条件下，使活性物发生溶解。 活性物质可用于肿瘤治疗。

    POLYMER CONJUGATES
    4.
    发明申请
    POLYMER CONJUGATES 有权
    聚合物混合物

    公开(公告)号：US20120016085A1

    公开(公告)日：2012-01-19

    申请号：US13243887

    申请日：2011-09-23

    申请人： Andrew Lennard LEWIS

    发明人： Andrew Lennard LEWIS

    IPC分类号： C08F8/00 ,  C08F8/18

    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。