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41. 发明申请

US20140220141A1 COMPOSITIONS OF LOPINAVIR AND RITONAVIR 有权
标题翻译： LOPINAVIR和RITONAVIR的组合物
公开(公告)号：US20140220141A1
公开(公告)日：2014-08-07
申请号：US14343453
申请日：2012-09-07
申请人： Marco Norman Giardiello , Thomas Oliver McDonald , Andrew Owen , Steven Paul Rannard , Philip John Martin , Darren Lee Smith
发明人： Marco Norman Giardiello , Thomas Oliver McDonald , Andrew Owen , Steven Paul Rannard , Philip John Martin , Darren Lee Smith
IPC分类号： A61K31/513 , A61K31/427
CPC分类号： A61K31/427 , A61K9/19 , A61K9/5138 , A61K9/5192 , A61K31/513 , A61K38/55 , Y02A50/411 , A61K2300/00
摘要： The present inventions relates to a solid composition and an aqueous dispersion comprising nanoparticles of the anti-retroviral drugs lopinavir and ritonavir. The solid composition and aqueous dispersion additionally comprise a mixture of a hydrophilic polymer and a surfactant. The surfactant is selected from vitamin-E-polyethylene glycol-succinate (Vit-E-PEG-succinate), a polyoxyethylene sorbitan fatty acid ester, N-alkyldimethylbenzylammonium chloride, sodium deoxycholate, dioctyl sodium sulfosuccinate, polyethyleneglycol-12-hydroxystearate, polyvinyl alcohol (PVA), and a block copolymer of polyoxyethylene and polyoxypropylene, or a combination thereof. The hydrophilic polymer is suitably selected from polyvinyl alcohol (PVA), a polyvinyl alcohol-polyethylene glycol graft copolymer, a block copolymer of polyoxyethylene and polyoxypropylene, polyethylene glycol, hydroxypropyl methyl cellulose (HPMC), and polyvinylpyrrolidone, or a combination thereof. The present invention also relates to processes for preparing both the solid composition and the aqueous dispersion, as well as to their use in therapy for the treatment and/or prevention of retroviral infections such as human immunodeficiency virus (HIV).
摘要翻译：本发明涉及包含抗逆转录病毒药物洛匹那韦和利托那韦的纳米颗粒的固体组合物和水分散体。固体组合物和水性分散体还包含亲水性聚合物和表面活性剂的混合物。表面活性剂选自维生素E-聚乙二醇 - 琥珀酸酯（Vit-E-PEG-琥珀酸酯），聚氧乙烯脱水山梨糖醇脂肪酸酯，N-烷基二甲基苄基氯化铵，脱氧胆酸钠，二辛基磺基琥珀酸钠，聚乙二醇-12-羟基硬脂酸酯，聚乙烯醇（PVA）和聚氧乙烯和聚氧丙烯的嵌段共聚物，或其组合。亲水性聚合物适当地选自聚乙烯醇（PVA），聚乙烯醇 - 聚乙二醇接枝共聚物，聚氧乙烯和聚氧丙烯的嵌段共聚物，聚乙二醇，羟丙基甲基纤维素（HPMC）和聚乙烯吡咯烷酮，或其组合。本发明还涉及制备固体组合物和水分散体的方法，以及它们在治疗和/或预防逆转录病毒感染如人类免疫缺陷病毒（HIV）中的用途。

42. 发明申请

US20140220140A1 COMPOSITIONS OF EFAVIRENZ 有权
标题翻译： EFAVIRENZ的组合物
公开(公告)号：US20140220140A1
公开(公告)日：2014-08-07
申请号：US14343203
申请日：2012-09-07
申请人： Marco Norman Giardiello , Thomas Oliver McDonald , Andrew Owen , Steven Paul Rannard , Philip John Martin , Darren Lee Smith
发明人： Marco Norman Giardiello , Thomas Oliver McDonald , Andrew Owen , Steven Paul Rannard , Philip John Martin , Darren Lee Smith
IPC分类号： A61K31/536 , A61K9/16 , A61K9/14
CPC分类号： A61K9/14 , A61K9/10 , A61K9/1682 , A61K9/19 , A61K9/5138 , A61K9/5192 , A61K31/536
摘要： The present inventions relates to a solid composition and an aqueous dispersion comprising nanoparticles of the anti-retroviral drug efavirenz. The solid composition and aqueous dispersion additionally comprise a mixture of a hydrophilic polymer and a surfactant. The surfactant is selected from vitamin-E-polyethylene glycol-succinate (Vit-E-PEG-succinate), a polyoxyethylene sorbitan fatty acid ester, N-alkyldimethylbenzylammonium chloride, sodium deoxycholate, dioctyl sodium sulfosuccinate, polyethyleneglycol-12-hydroxystearate, polyvinyl alcohol (PVA), and a block copolymer of polyoxyethylene and polyoxypropylene, or a combination thereof. The hydrophilic polymer is suitably selected from polyvinyl alcohol (PVA), a polyvinyl alcohol-polyethylene glycol graft copolymer, a block copolymer of polyoxyethylene and polyoxypropylene, polyethylene glycol, hydroxypropyl methyl cellulose (HPMC), and polyvinylpyrrolidone, or a combination thereof. The present invention also relates to processes for preparing both the solid composition and the aqueous dispersion, as well as to their use in therapy for the treatment and/or prevention of retroviral infections such as human immunodeficiency virus (HIV).
摘要翻译：本发明涉及包含抗逆转录病毒药物依法韦仑的纳米颗粒的固体组合物和水性分散体。固体组合物和水性分散体还包含亲水性聚合物和表面活性剂的混合物。表面活性剂选自维生素E-聚乙二醇 - 琥珀酸酯（Vit-E-PEG-琥珀酸酯），聚氧乙烯脱水山梨糖醇脂肪酸酯，N-烷基二甲基苄基氯化铵，脱氧胆酸钠，二辛基磺基琥珀酸钠，聚乙二醇-12-羟基硬脂酸酯，聚乙烯醇（PVA）和聚氧乙烯和聚氧丙烯的嵌段共聚物，或其组合。亲水性聚合物适当地选自聚乙烯醇（PVA），聚乙烯醇 - 聚乙二醇接枝共聚物，聚氧乙烯和聚氧丙烯的嵌段共聚物，聚乙二醇，羟丙基甲基纤维素（HPMC）和聚乙烯吡咯烷酮，或其组合。本发明还涉及制备固体组合物和水分散体的方法，以及它们在治疗和/或预防逆转录病毒感染如人类免疫缺陷病毒（HIV）中的用途。

43. 发明申请

US20100145001A1 BRANCHED ORGANIC-INORGANIC POLYMERS 审中-公开
标题翻译：分支有机无机聚合物
公开(公告)号：US20100145001A1
公开(公告)日：2010-06-10
申请号：US12518744
申请日：2007-12-10
申请人： Paul Hugh Findlay , Steven Paul Rannard , Brodyck James Lachlan Royles , Jonathan Victor Mark Weaver
发明人： Paul Hugh Findlay , Steven Paul Rannard , Brodyck James Lachlan Royles , Jonathan Victor Mark Weaver
IPC分类号： C08G77/04
CPC分类号： C08F290/06 , C08F2/38 , C08F20/14 , C08F220/14 , C08F222/1006 , C08F230/08
摘要： A branched, hybrid polymer obtainable by an addition polymerisation process, preferably a free-radical polymerisation process, comprising organic chains and inorganic chains wherein: (a) said polymer comprises at least two organic chains which are covalently linked by a bridge other than at their ends, (b) at least one inorganic chain is present, either as a covalently-bonded pendant group on an organic chain or within the bridge, and (c) the polymer comprises a residue of optionally but preferably a chain transfer agent and a residue of an initiator, optionally but preferably a free-radical initiator. The invention further provides a method for the synthesis of these polymers.
摘要翻译：可通过加成聚合方法获得的支链杂化聚合物，优选自由基聚合方法，其包含有机链和无机链，其中：（a）所述聚合物包含至少两个有机链，其通过除了它们之外的桥共价连接（b）存在至少一个无机链，作为有机链或桥内的共价键合的侧基，和（c）聚合物包含任选但优选链转移剂的残基和残基的引发剂，任选但优选自由基引发剂。本发明还提供了一种合成这些聚合物的方法。

44. 发明申请

US20130345358A1 USE OF BRANCHED ADDITION COPOLYMERS IN CURING SYSTEMS 审中-公开
标题翻译：分支添加共聚物在固化体系中的应用
公开(公告)号：US20130345358A1
公开(公告)日：2013-12-26
申请号：US13496844
申请日：2010-09-16
申请人： Paul Hugh Findlay , Sharon Todd , Steven Paul Rannard , Brodyck James Lachlan Royles , Neil John Simpson , Roselyne Marie Andree Baudry
发明人： Paul Hugh Findlay , Sharon Todd , Steven Paul Rannard , Brodyck James Lachlan Royles , Neil John Simpson , Roselyne Marie Andree Baudry
IPC分类号： C08F220/14 , C09D133/12
CPC分类号： C08F220/14 , C08F2/38 , C08F212/36 , C08G18/6229 , C08G18/6254 , C09D133/066 , C09D133/12 , C09J133/12 , C08F2220/1825 , C08F222/1006 , C08F222/26 , C08F2220/281
摘要： The present invention relates to the use of branched addition copolymers in systems which can be cured post synthesis to form for example polymer coatings, sealants, inks, adhesives or composites and also relates to methods of preparing the cured systems, compositions comprising such copolymers and the use of the compositions in for example but not limited to coatings, inks, sealants, adhesives or composites.
摘要翻译：本发明涉及分支加成共聚物在可以在后合成固化以形成例如聚合物涂料，密封剂，油墨，粘合剂或复合材料的体系中的用途，还涉及制备固化体系的方法，包含这种共聚物的组合物和组合物在例如但不限于涂料，油墨，密封剂，粘合剂或复合材料中的使用。

45. 发明申请

US20120108679A1 BRANCHED COPOLYMERS, COMPOSITION AND USES 审中-公开
标题翻译：分支共聚物，组合物和用途
公开(公告)号：US20120108679A1
公开(公告)日：2012-05-03
申请号：US13148472
申请日：2010-02-09
申请人： Paul Hugh Findlay , Brodyck James Lachlan Royles , Neil John Simpson , Sharon Todd , Steven Paul Rannard , Jonathan Victor Mark Weaver , Roselyne Marie Andree Baudry
发明人： Paul Hugh Findlay , Brodyck James Lachlan Royles , Neil John Simpson , Sharon Todd , Steven Paul Rannard , Jonathan Victor Mark Weaver , Roselyne Marie Andree Baudry
IPC分类号： A61K47/32 , C08L47/00 , C09D147/00 , C09D11/00 , C10M145/14 , C02F5/00 , C09K5/00 , C09K15/12 , C09K15/06 , C08F236/20 , C09J147/00
CPC分类号： C08F2/38 , C08F212/08 , C08F212/36 , C08F220/18 , C08F222/1006 , C08F2220/1825 , C08F220/20 , C08F220/06 , C08F2222/1013 , C08F226/10
摘要： The present invention relates to a branched copolymer comprising a hydrophilic component obtainable by an addition polymerisation process and compositions and uses thereof said copolymer comprising: i) a residue of at least one monofunctional monomer comprising one polymerisable double bond per molecule and a molecular weight of less than 1000 Daltons; ii) a residue of at least one multifunctional monomer comprising at least two polymerisable double bonds per molecule and a molecular weight of less than 1000 Daltons; and wherein the end termini of the copolymer chains comprise one or more of a residue of a chain transfer agent; an initiator or a terminal group derived from a termination reaction; wherein; the molar ratio of the monofunctional monomer to multifunctional monomer is between 50:1 to 2.5:1 respectively; and wherein the hydrophilic component is comprised of at least 1 mole % of one or more residue of a multifunctional monomer and/or one or more residue of a chain transfer agent comprised of a hydrophilic monomer each with a solubility of 0.18 w/w % in water; and wherein the residue of the at least one monofunctional monomer with a molecular weight of less than 1000 Daltons is selected from the group comprising: vinyl acids, vinyl acid esters, vinyl aryl compounds, vinyl acid anhydrides, vinyl amides, vinyl ethers, vinyl amines, vinyl aryl amines, vinyl nitriles, vinyl ketones, and derivatives thereof; hydroxyl-containing monomers and monomers which can be post-reacted to form hydroxyl groups; acid-containing or acid functional monomers; zwitterionic monomers; quaternised amino monomers, oligomeric monomers; and corresponding allyl monomers of the aforesaid vinyl monomers.
摘要翻译：本发明涉及包含通过加成聚合方法获得的亲水性组分的支链共聚物及其组合物和用途，所述共聚物包含：i）至少一种单分子的功能单体的残基，其每分子包含一个可聚合双键，分子量较小超过1000道尔顿; ii）至少一种多官能单体的残基，每个分子包含至少两个可聚合双键，分子量小于1000道尔顿; 并且其中共聚物链的末端包含一个或多个链转移剂的残基; 来自终止反应的引发剂或末端基团; 其中; 单官能单体与多官能单体的摩尔比分别为50:1至2.5:1; 并且其中所述亲水组分由至少1摩尔％的多官能单体的一个或多个残基和/或链转移剂的一个或多个残基组成，所述链转移剂由亲水性单体组成，每个亲水性单体的溶解度为0.18w / w％水; 并且其中分子量小于1000道尔顿的至少一种单官能单体的残基选自：乙烯基酸，乙烯基酸酯，乙烯基芳基化合物，乙烯基酸酐，乙烯基酰胺，乙烯基醚，乙烯基胺乙烯基芳基胺，乙烯基腈，乙烯基酮及其衍生物; 含羟基的单体和可以后反应形成羟基的单体; 含酸或酸官能单体; 两性离子单体; 季铵化氨基单体，低聚单体; 和上述乙烯基单体的相应的烯丙基单体。

46. 发明申请

US20120108678A1 BRANCHED COPOLYMERS, COMPOSITIONS AND USES 审中-公开
标题翻译：分支共聚物，组合物和用途
公开(公告)号：US20120108678A1
公开(公告)日：2012-05-03
申请号：US13148471
申请日：2010-02-09
申请人： Paul Hugh Findlay , Brodyck James Lachlan Royles , Neil John Simpson , Sharon Todd , Steven Paul Rannard , Jonathan Victor Mark Weaver , Roselyne Marie Andree Baudry
发明人： Paul Hugh Findlay , Brodyck James Lachlan Royles , Neil John Simpson , Sharon Todd , Steven Paul Rannard , Jonathan Victor Mark Weaver , Roselyne Marie Andree Baudry
IPC分类号： A61K47/32 , C08L47/00 , C09D147/00 , C09J147/00 , C09K15/12 , C02F5/00 , C10M107/42 , C10M107/28 , C09K5/00 , C09K15/28 , C08F236/20 , C09D11/00
CPC分类号： C08F2/38 , C08F212/08 , C08F212/36 , C08F220/18 , C08F222/1006 , C08F2220/1825 , C08F220/20 , C08F220/06 , C08F2222/1013 , C08F226/10
摘要： The present invention relates to a branched copolymer obtainable by an addition polymerisation process and uses and compositions thereof comprising: i) a residue of at least one monofunctional monomer comprising one polymerisable double bond per molecule and a molecular weight of less than 1000 Daltons; ii) a residue of at least one multifunctional monomer comprising at least two polymerisable double bonds per molecule and a molecular weight of less than 1000 Daltons; and wherein the end termini of the copolymer chains comprise one or more of a residue of a chain transfer agent; an initiator or a terminal group derived from a termination reaction; wherein; the molar ratio of the monofunctional monomer to multifunctional monomer is between 50:1 to 2.5:1 respectively; and wherein the hydrophilic component is comprised of at least 1 mole % of a combination of a monofunctional monomer, and a multifunctional monomer and/or a chain transfer agent when compared to the total content of monofunctional monomer which is/are comprised of hydrophilic component each with a solubility of 0.18 w/w % in water at 20° C.; and wherein the residue of the at least one monofunctional monomer with a molecular weight of less than 1000 daltons is selected from the group comprising: vinyl acids, vinyl acid ester, vinyl aryl compounds, vinyl acid anhydrides, vinyl amides, vinyl ethers, vinyl amines, vinyl aryl amines, vinyl nitriles, vinyl ketones, and derivatives thereof; hydroxyl-containing monomers and monomers which can be post-reacted to form hydroxyl groups; acid-containing or acid functional monomers; zwitterionic monomers; quaternised amino monomers, oligomeric monomers; and corresponding allyl monomers of the aforesaid vinyl monomers.
摘要翻译：本发明涉及可通过加成聚合方法获得的支链共聚物及其用途及其组合物，其包含：i）至少一种单分子的残基，其每分子包含一个可聚合的双键，分子量小于1000道尔顿; ii）至少一种多官能单体的残基，每个分子包含至少两个可聚合双键，分子量小于1000道尔顿; 并且其中共聚物链的末端包含一个或多个链转移剂的残基; 来自终止反应的引发剂或末端基团; 其中; 单官能单体与多官能单体的摩尔比分别为50:1至2.5:1; 并且其中亲水性组分由至少1摩尔％的单官能单体和多官能单体和/或链转移剂的组合组成，当与由各亲水组分组成的单官能单体的总含量相比时溶解度为0.18W / W％，在20℃的水中。并且其中所述至少一种分子量小于1000道尔顿的单官能单体的残基选自：乙烯基酸，乙烯基酸酯，乙烯基芳基化合物，乙烯基酸酐，乙烯基酰胺，乙烯基醚，乙烯基胺乙烯基芳基胺，乙烯基腈，乙烯基酮及其衍生物; 含羟基的单体和可以后反应形成羟基的单体; 含酸或酸官能单体; 两性离子单体; 季铵化氨基单体，低聚单体; 和上述乙烯基单体的相应的烯丙基单体。

47. 发明申请

US20120059069A1 AMPHIPHILIC BRANCHED COPOLYMER, METHODS OF PREPARATION, EMULSIONS, AND USES 审中-公开
标题翻译：分散共聚物，制备方法，乳液和用途
公开(公告)号：US20120059069A1
公开(公告)日：2012-03-08
申请号：US13266745
申请日：2010-04-28
申请人： Paul Hugh Findlay , Brodyck James Lachlan , Neil John Simpson , Sharon Todd , Roselyne Marie Andree Baudry , Steven Paul Rannard , Jonathan Victor Mark Weaver
发明人： Paul Hugh Findlay , Brodyck James Lachlan , Neil John Simpson , Sharon Todd , Roselyne Marie Andree Baudry , Steven Paul Rannard , Jonathan Victor Mark Weaver
IPC分类号： A61K47/32 , A23D7/005 , C08L39/00 , C08F236/20 , A61K8/81
CPC分类号： C08F220/26
摘要： The present invention relates to an amphiphilic branched copolymer obtainable by an addition polymerisation process, the method of production of same and uses thereof as emulsions wherein said polymer comprises: at least two chains which are covalently linked by a bridge other than at their ends; and wherein the at least two chains comprise at least one ethylenically monounsaturated monomer, and wherein the bridge comprises at least one ethylenically polyunsaturated monomer; and wherein the polymer comprises a residue of a chain transfer agent and optionally a residue of an initiator, and wherein at least one of the monounsaturated monomer(s) and polyunsaturated monomer(s) and chain transfer agent(s) is a hydrophilic residue; and at least one of one of the monounsaturated monomer(s) and polyunsaturated monomer(s) and chain transfer agent(s) is a hydrophobic residue, and wherein the mole ratio of polyunsaturated monomer(s) to monounsaturated monomer(s) is in a range of from 1:100 to 1:4, and wherein at least one of the monounsaturated monomer(s) and polyunsaturated monomer(s) and chain transfer agent(s) comprises a moiety that is capable of responding to an external stimuli thereby creating a physical or chemical change in the solubility of the said moiety; and wherein the air-water surface tension of the polymer changes from between 35 mN/m to 60 mN/m upon application of the external stimulus.
摘要翻译：本发明涉及通过加成聚合方法获得的两亲性支链共聚物，其制备方法及其用途作为乳液，其中所述聚合物包含：至少两个通过桥以外的桥共价连接的链; 并且其中所述至少两条链包含至少一种烯属单不饱和单体，并且其中所述桥包含至少一种烯键式多不饱和单体; 并且其中所述聚合物包含链转移剂的残基和任选的引发剂的残基，并且其中所述单不饱和单体和多不饱和单体和链转移剂中的至少一种是亲水性残基; 并且单不饱和单体和多不饱和单体和链转移剂中的至少一种是疏水性残基，并且其中多不饱和单体与单不饱和单体的摩尔比在 1：100至1：4的范围，并且其中至少一种单不饱和单体和多不饱和单体和链转移剂包含能够响应于外部刺激的部分，造成所述部分的溶解度的物理或化学变化; 并且其中当施加外部刺激时聚合物的空气 - 水表面张力从35mN / m至60mN / m变化。

48. 发明申请

US20110313054A1 BRANCHED COPOLYMERS, COMPOSITION AND USES 审中-公开
标题翻译：分支共聚物，组合物和用途
公开(公告)号：US20110313054A1
公开(公告)日：2011-12-22
申请号：US13148470
申请日：2010-02-09
申请人： Paul Hugh Findlay , Brodyck James Lachlan Royles , Neil John Simpson , Sharon Todd , Steven Paul Rannard , Jonathan Victor Mark Weaver , Roselyne Marie Andree Baudry
发明人： Paul Hugh Findlay , Brodyck James Lachlan Royles , Neil John Simpson , Sharon Todd , Steven Paul Rannard , Jonathan Victor Mark Weaver , Roselyne Marie Andree Baudry
IPC分类号： A61K47/32 , C08L47/00 , C09D147/00 , C10L1/19 , C10M145/14 , C02F5/10 , C09K5/00 , C09K3/00 , C08F236/20 , C09J147/00
CPC分类号： C08F2/38 , C08F212/08 , C08F212/36 , C08F220/18 , C08F222/1006 , C08F2220/1825 , C08F220/20 , C08F220/06 , C08F2222/1013 , C08F226/10
摘要： The present invention relates to a branched copolymer obtainable by an addition polymerisation process and uses and compositions thereof comprising a hydrophilic component, said polymer comprising: i) a residue of at least one monofunctional monomer comprising one polymerisable double bond per molecule and a molecular weight of less than 1000 Daltons; ii) a residue of at least one multifunctional monomer comprising at least two polymerisable double bonds per molecule and a molecular weight of less than 1000 Daltons; and wherein the end termini of the copolymer chains comprise one or more of a residue of a chain transfer agent; an initiator or a terminal group derived from a termination reaction; wherein; the molar ratio of the monofunctional monomer to multifunctional monomer is between 50:1 to 2.5:1 respectively; and wherein the hydrophilic component is comprised solely of at least 1 mole % of one or more monofunctional monomer which is/are comprised of hydrophilic monomer each with a solubility of 0.18 w/w % in water at 20° C.; and wherein the residue of the at least one monofunctional monomer with a molecular weight of less than 1000 daltons is selected from the group comprising: vinyl acids, vinyl acid ester, vinyl aryl compounds, vinyl acid anhydrides, vinyl amides, vinyl ethers, vinyl amines, vinyl aryl amines, vinyl nitriles, vinyl ketones, and derivatives thereof; hydroxyl-containing monomers and monomers which can be post-reacted to form hydroxyl groups; acid-containing or acid functional monomers; zwitterionic monomers; quaternised amino monomers, oligomeric monomers; and corresponding allyl monomers of the aforesaid vinyl monomers.
摘要翻译：本发明涉及通过加成聚合方法获得的支链共聚物及其用途及其组合物，其包含亲水性组分，所述聚合物包含：i）至少一种单官能单体的残基，每单分子含有一个可聚合双键，分子量为小于1000道尔顿; ii）至少一种多官能单体的残基，每个分子包含至少两个可聚合双键，分子量小于1000道尔顿; 并且其中共聚物链的末端包含一个或多个链转移剂的残基; 来自终止反应的引发剂或末端基团; 其中; 单官能单体与多官能单体的摩尔比分别为50:1至2.5:1; 并且其中所述亲水性组分仅由至少1摩尔％的一种或多种单官能单体组成，所述单官能单体由在20℃的水中的溶解度为0.18W / W％的亲水性单体组成。并且其中所述至少一种分子量小于1000道尔顿的单官能单体的残基选自：乙烯基酸，乙烯基酸酯，乙烯基芳基化合物，乙烯基酸酐，乙烯基酰胺，乙烯基醚，乙烯基胺乙烯基芳基胺，乙烯基腈，乙烯基酮及其衍生物; 含羟基的单体和可以后反应形成羟基的单体; 含酸或酸官能单体; 两性离子单体; 季铵化氨基单体，低聚单体; 和上述乙烯基单体的相应的烯丙基单体。

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