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公开(公告)号:WO2018197885A1
公开(公告)日:2018-11-01
申请号:PCT/GB2018/051106
申请日:2018-04-26
Applicant: THE UNIVERSITY OF LIVERPOOL
Inventor: RANNARD, Steve , CHAMBON, Pierre , CASSIN, Savannah
IPC: C08F2/38
Abstract: A method of preparing a branched polymer comprises the free radical polymerisation of a multivinyl monomer in the presence of a chain transfer agent, using a source of radicals, wherein the extent of propagation is controlled relative to the extent of chain transfer to prevent gelation of the polymer. The average length of each vinyl polymer chain within the product is short.
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公开(公告)号:WO2020128525A1
公开(公告)日:2020-06-25
申请号:PCT/GB2019/053678
申请日:2019-12-20
Applicant: THE UNIVERSITY OF LIVERPOOL , THE JOHNS HOPKINS UNIVERSITY
Inventor: OWEN, Andrew , RANNARD, Steve , HERN, Faye , LIU, Chung , SHAKIL, Anika , NEARY, Megan , MEYERS, Caren Freel , TEMBURNIKAR, Kartik , BAMBARGER, Lauren , HENRIQUEZ, Stephanie
Abstract: Polymer-of-prodrug (POP) materials enable new nucleoside reverse transcriptase inhibitor (NRTI) therapy strategies. The materials are prodrugs of NRTIs in the form of polymers. Suitable materials include products which are polymeric NRTI delivery systems comprising polymeric materials which are capable of degradation after administration to release NRTIs or NRTI prodrugs which themselves are capable of metabolism to the parent NRTIs. The NRTIs may optionally be selected from tenofovir (TFV), emtricitabine (FTC), lamivudine (3TC) and MK-8591 (EFdA). The invention facilitates long-acting (LA) regimens. Constructs of the materials may be in the form of injectable compositions or implants.
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公开(公告)号:WO2020089647A1
公开(公告)日:2020-05-07
申请号:PCT/GB2019/053104
申请日:2019-10-31
Applicant: THE UNIVERSITY OF LIVERPOOL
Inventor: RANNARD, Steve , CHAMBON, Pierre
IPC: C08F2/06 , C08F12/36 , C08F220/20 , C08F222/10 , C08F297/02
Abstract: A method of preparing a branched polymer comprises the non free radical polymerisation of a multifunctional monomer in the presence of an initiator, wherein a reactor is charged with initiator or wherein initiator is generated in situ in said reactor, and wherein multifunctional monomer is added to said initiator so that the extent of polymerization of multifunctional monomer is controlled relative to the extent of reaction of multifunctional monomer with initiator, to prevent gelation of the polymer. Said non free radical polymerisation may for example be anionic vinyl polymerisation, oxy- anionic vinyl polymerisation, or ring opening polymerisation.
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公开(公告)号:WO2018029476A1
公开(公告)日:2018-02-15
申请号:PCT/GB2017/052355
申请日:2017-08-09
Applicant: THE UNIVERSITY OF LIVERPOOL
Inventor: KEARNS, Victoria , CAULDBECK, Helen , RANNARD, Steve , WILLIAMS, Rachel , LE HELLAYE, Maude
CPC classification number: A61K9/0048 , A61K31/192 , A61K31/203 , A61K47/10 , A61K47/32 , A61K47/34 , A61K47/44 , C08F2/38 , C08F293/005 , C08F2438/03
Abstract: A composition comprises: a base oil; an additive comprising a copolymer comprising hydrophobic and hydrophilic units; and a drug. The copolymer may for example have a comb structure in which the hydrophobic units and hydrophilic units are pendant chains on a backbone of the copolymer. The hydrophobic units and hydrophilic units may for example comprise polydimethylsiloxane moieties and ethylene glycol residues respectively. The composition may for example be used as a tamponade or as a component for a tamponade administered to the eye. The invention is useful for solubilising and/or releasing drugs.
Abstract translation: 组合物包含:基础油; 包含含疏水和亲水单元的共聚物的添加剂; 和一种药物。 共聚物可以例如具有梳状结构,其中疏水单元和亲水单元是共聚物主链上的侧链。 疏水单元和亲水单元可以例如分别包含聚二甲基硅氧烷部分和乙二醇残基。 该组合物可以例如用作填塞物或用作施用于眼睛的填塞物的组分。 本发明可用于增溶和/或释放药物。 p>
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公开(公告)号:WO2018029462A1
公开(公告)日:2018-02-15
申请号:PCT/GB2017/052334
申请日:2017-08-08
Applicant: THE UNIVERSITY OF LIVERPOOL
Inventor: EDWARDS, Stephanie , RANNARD, Steve , OWEN, Andrew
IPC: C08F220/28 , C08F2/38 , A61K9/10
Abstract: The present invention relates to a branched amphiphilic polymer, suitable for stabilizing an emulsion, comprising a plurality of polymer chains comprising hydrophobic chain ends; a plurality of polymer chains comprising functional chain ends capable of associating to a biological substrate; and a plurality of branching units. The present invention also relates to pharmaceutical compositions containing said branched amphiphilic polymers, their methods of use, and methods for their preparation.
Abstract translation: 本发明涉及适用于稳定乳液的支化两亲聚合物,其包含多个包含疏水链端的聚合物链; 多个聚合物链,其包含能够与生物基质缔合的功能链末端; 和多个分支单元。 本发明还涉及含有所述支化两亲聚合物的药物组合物,它们的使用方法及其制备方法。 p>
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公开(公告)号:WO2016124925A1
公开(公告)日:2016-08-11
申请号:PCT/GB2016/050252
申请日:2016-02-03
Applicant: THE UNIVERSITY OF LIVERPOOL
Inventor: RANNARD, Steve , OWEN, Andrew , HOBSON, James , LIPTROTT, Neill , CHAMBON, Pierre
IPC: A61K9/107 , A61K47/10 , A61K47/34 , C08F220/20
CPC classification number: A61K9/1641 , A61K9/0053 , A61K9/107 , A61K9/1075 , A61K31/513 , A61K31/536 , A61K47/10 , A61K47/34 , B01F17/0028 , C08F220/28 , C08F2220/286 , C08F2438/01 , C08F2222/1013
Abstract: An oil-in-water emulsion comprises an emulsifier which is a non-gelled branched polymer (e.g. a branched vinyl polymer), wherein the ends of at least some of the chains of said polymer terminate in an alkyl chain of 5 carbon atoms or more, and wherein the oil-in-water emulsion takes the form of particles having a z-average diameter of no greater than about 1000 nm. This is useful in, for example, facilitating the carrying of hydrophobic materials within aqueous systems, to enhance oral drug delivery. The oil-in-water emulsion may be prepared by mixing an oil phase with an aqueous phase in the presence of an emulsifier, wherein said emulsifier is a non-gelled branched polymer, wherein the ends of at least some of the chains of said polymer terminate in an alkyl chain of 5 carbon atoms or more, and wherein the oil-in-water emulsion takes the form of particles having a z-average diameter of no greater than about 1000 nm. The oil phase may comprise a further solvent which is miscible with the oil, said solvent being allowed to evaporate to produce the final emulsion.
Abstract translation: 水包油乳液包括乳化剂,其是非胶凝的支化聚合物(例如支链乙烯基聚合物),其中所述聚合物的至少一些链的末端终止于5个或更多个碳原子的烷基链 ,并且其中所述水包油乳液采用z平均直径不大于约1000nm的颗粒的形式。 这在例如促进含水系统中的疏水性材料的携带以增强口服药物递送方面是有用的。 水包油乳液可以通过在乳化剂存在下将油相与水相混合来制备,其中所述乳化剂是非胶凝的支化聚合物,其中所述聚合物的至少一些链的末端 终止于5个或更多个碳原子的烷基链,并且其中水包油乳液采用z平均直径不大于约1000nm的颗粒的形式。 油相可以包含与油混溶的另外的溶剂,允许所述溶剂蒸发以产生最终乳液。
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公开(公告)号:WO2020089649A1
公开(公告)日:2020-05-07
申请号:PCT/GB2019/053106
申请日:2019-10-31
Applicant: THE UNIVERSITY OF LIVERPOOL
Inventor: RANNARD, Steve , CHAMBON, Pierre , CASSIN, Savannah
IPC: C08F2/38 , C08F12/36 , C08F220/20 , C08F222/10
Abstract: Responsive or degradable branched polymers may be prepared by the free radical polymerisation of a multivinyl monomer in the presence of a chain transfer agent, using a source of radicals, wherein the extent of propagation is controlled relative to the extent of chain transfer to prevent gelation of the polymer. The multivinyl monomer may comprise a cleavable group, for example an ester, or a multiplicity of such groups, between two vinyl groups. Said monomer may be a macromonomer containing multiple cleavage sites.
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公开(公告)号:WO2018197884A1
公开(公告)日:2018-11-01
申请号:PCT/GB2018/051105
申请日:2018-04-26
Applicant: THE UNIVERSITY OF LIVERPOOL
Inventor: RANNARD, Steve , CHAMBON, Pierre , CASSIN, Savannah
IPC: C08F122/10 , C08F122/38 , C08F112/36
Abstract: A method of preparing a polymer comprises the use of free radical vinyl polymerisation to form carbon-carbon backbone segments of the polymer, wherein the longest chains in the polymer comprise vinyl polymer chains interspersed with other chemical groups and/or chains. The product has the characteristics of astep- growth polymer comprising a mixture of polyfunctional step-growth monomer residues formed by vinyl polymerization.
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公开(公告)号:WO2018029477A1
公开(公告)日:2018-02-15
申请号:PCT/GB2017/052356
申请日:2017-08-09
Applicant: THE UNIVERSITY OF LIVERPOOL
Inventor: KEARNS, Victoria , CAULDBECK, Helen , RANNARD, Steve , WILLIAMS, Rachel , LE HELLAYE, Maude
IPC: A61K47/59 , A61K47/34 , A61K31/07 , A61K31/192
CPC classification number: A61K47/59 , A61K9/0048 , A61K31/192 , A61K31/203 , A61K45/06 , A61K47/34 , A61P27/02
Abstract: A composition comprises: a base oil; an additive; and a drug. The additive has segments which are conjugated, e.g. covalently linked, together. A first segment facilitates solubility in the base oil, whereas a second segment facilitates drug solubility and/or modifies drug release or other behaviour. The first segment may for example comprise a poly(dimethylsiloxane) - containing moiety. The second segment may for example resemble a drug molecule. The composition may for example be used as a tamponade or as a component for a tamponade administered to the eye.
Abstract translation: 组合物包含:基础油; 添加剂; 和一种药物。 该添加剂具有共轭的链段,例如, 共价连接在一起。 第一部分促进基础油中的溶解性,而第二部分促进药物溶解性和/或改变药物释放或其他行为。 第一片段可以例如包含含聚(二甲基硅氧烷)的部分。 第二部分可以例如类似于药物分子。 该组合物可以例如用作填塞物或用作施用于眼睛的填塞物的组分。 p>
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公开(公告)号:WO2016009227A1
公开(公告)日:2016-01-21
申请号:PCT/GB2015/052089
申请日:2015-07-17
Applicant: THE UNIVERSITY OF LIVERPOOL
Inventor: RANNARD, Steve , FORD, Jane , ROGERS, Hannah , CHAMBON, Pierre , GIARDIELLO, Marco , OWEN, Andrew , KITTERINGHAM, Neil
IPC: A61K9/51 , A61K47/48 , A61K31/427 , A61K31/4745 , A61K31/513 , A61K31/536 , C08F2/38 , C08F220/10 , C08G63/08 , C08G83/00 , C08L33/10 , A61P35/00 , A61P31/18
CPC classification number: A61K9/5146 , A61K9/5138 , A61K9/5153 , A61K9/5192 , A61K31/192 , A61K31/427 , A61K31/4745 , A61K31/513 , A61K31/536 , C08F2/38 , C08F220/20 , C08F220/34 , C08F2220/1825 , C08F2222/1013 , C08F2438/01 , C08G63/08 , C08G81/025 , C08G83/003 , C08L33/10 , C08L71/02
Abstract: Particles comprising a branched polymer and either a block copolymer or a linear dendritic hybrid represent a category of useful materials. They may be used in for example drug delivery applications. They may be prepared by a method comprising the steps of: dissolving the branched polymer and block copolymer or linear dendritic hybrid, and optionally other component(s),in a solvent to form a solution; adding said solution to a different liquid; and removing said solvent to form a dispersion of co-precipitated particles.
Abstract translation: 包含支链聚合物和嵌段共聚物或线性树枝状杂化物的颗粒代表一类有用的材料。 它们可以用于例如药物递送应用。 它们可以通过包括以下步骤的方法制备:将支化聚合物和嵌段共聚物或线性树枝状杂化物和任选的其它组分溶解在溶剂中以形成溶液; 将所述溶液加入到不同的液体中; 并除去所述溶剂以形成共沉淀颗粒的分散体。
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