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公开(公告)号：US20120058139A1
公开(公告)日：2012-03-08
申请号：US13062339
申请日：2009-09-02
IPC分类号： A61K39/385 , A61P43/00 , A61P37/04 , C12N15/63 , A61K48/00
CPC分类号： A61K48/0041 , A61K9/1272 , A61K9/1273 , A61K47/6911
摘要： A stabilized multimodular assembly for intracellular delivery comprising a complex of at least one cationic transfection agent and of at least one negatively charged macromolecule, wherein the complex has a theoretical charge ratio ranging from about 0 to about 4, and an efficient amount of at least one amphiphilic block co-polymer acting as a steric colloidal stabilizer with respect to the complex, the block co-polymer having hydrophilic and hydrophobic blocks wherein at least one hydrophilic block is conjugated with at least one targeting ligand.
摘要翻译： 一种用于细胞内递送的稳定的多模式组合物，其包含至少一种阳离子转染剂和至少一个带负电荷的大分子的复合物，其中所述络合物具有约0至约4的理论电荷比，以及有效量的至少一种 作为相对于配合物的空间胶体稳定剂的两亲嵌段共聚物，嵌段共聚物具有亲水和疏水嵌段，其中至少一个亲水嵌段与至少一个靶向配体缀合。
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公开(公告)号：US08790664B2
公开(公告)日：2014-07-29
申请号：US13062339
申请日：2009-09-02
IPC分类号： A61K48/00
CPC分类号： A61K48/0041 , A61K9/1272 , A61K9/1273 , A61K47/6911
摘要： A stabilized multimodular assembly for intracellular delivery comprising a complex of at least one cationic transfection agent and of at least one negatively charged macromolecule, wherein the complex has a theoretical charge ratio ranging from about 0 to about 4, and an efficient amount of at least one amphiphilic block co-polymer acting as a steric colloidal stabilizer with respect to the complex, the block co-polymer having hydrophilic and hydrophobic blocks wherein at least one hydrophilic block is conjugated with at least one targeting ligand.
摘要翻译： 一种用于细胞内递送的稳定的多模式组合物，其包含至少一种阳离子转染剂和至少一个带负电荷的大分子的复合物，其中所述络合物具有约0至约4的理论电荷比，以及有效量的至少一种 作为相对于配合物的空间胶体稳定剂的两亲嵌段共聚物，嵌段共聚物具有亲水和疏水嵌段，其中至少一个亲水嵌段与至少一个靶向配体缀合。
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3.发明申请Formulation of stabilized cationic transfection agent (s) /nucleic acid particles 失效稳定的阳离子转染剂/核酸颗粒的制剂公开(公告)号：US20050026287A1
公开(公告)日：2005-02-03
申请号：US10944872
申请日：2004-09-21
申请人： Joel Crouzet , Bruno Pitard
发明人： Joel Crouzet , Bruno Pitard
CPC分类号： B82Y5/00 , A61K9/0019 , A61K9/1075 , A61K9/1272 , A61K47/10 , A61K47/60 , A61K47/69 , A61K47/6949 , A61K48/0008 , A61K48/0025 , A61K48/0041
摘要： The invention concerns a composition containing stabilised particles of cationic transfection agent(s)/nucleic acid complexes characterised in that it includes besides said transfection agent and nucleic acid at least a non-ionic surfactant in sufficient amount for preventing the aggregation of the particles in course of time. In a preferred embodiment, the surfactant is a polyoxyalkylene or a derivative thereof.
摘要翻译： 本发明涉及包含阳离子转染剂/核酸复合物稳定化颗粒的组合物，其特征在于，其包括除了所述转染剂和核酸之外，至少一种足够量的非离子表面活性剂防止颗粒聚集 的时间。 在优选的实施方案中，表面活性剂是聚氧化烯或其衍生物。
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4.发明授权公开(公告)号：US06521252B1
公开(公告)日：2003-02-18
申请号：US09610727
申请日：2000-07-06
IPC分类号： A61K9127
CPC分类号： C12N15/87 , A61K47/6901 , A61K48/00 , C07C323/60 , C07K5/06026
摘要： The invention concerns a novel agent for transferring nucleic acids into cells. Said agent is particularly characterised in that it comprises one or several disulphide bonds sensitive to reducing conditions. The invention also concerns compositions comprising such an agent for transferring in vivo, ex vivo or in vitro nucleic acids of interest into different cell types.
摘要翻译： 本发明涉及用于将核酸转移到细胞中的新型药剂。 所述试剂的特征在于其包含对还原条件敏感的一个或几个二硫键。 本发明还涉及包含用于将体内，离体或体外感兴趣的核酸转移到不同细胞类型中的这种试剂的组合物。
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公开(公告)号：US07709452B2
公开(公告)日：2010-05-04
申请号：US10502973
申请日：2003-02-07
申请人： Bruno Pitard
发明人： Bruno Pitard
CPC分类号： A61K48/0041 , A61K31/77 , A61K31/785
摘要： The invention relates to a pharmaceutical composition which combines a tetrafunctional copolymer with a nucleic acid, said copolymer having formula I (namely a poloxamine), and preferably taking the form of one of the cationic mineral or organic salts thereof. The inventive composition can be used to improve in vivo gene transfer.
摘要翻译： 本发明涉及将四官能共聚物与核酸组合的药物组合物，所述共聚物具有式I（即泊洛沙胺），优选以阳离子矿物质或其有机盐之一的形式。 本发明的组合物可用于改善体内基因转移。
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公开(公告)号：US08367631B2
公开(公告)日：2013-02-05
申请号：US12659618
申请日：2010-03-15
申请人： Bruno Pitard
发明人： Bruno Pitard
CPC分类号： A61K48/0041 , A61K31/77 , A61K31/785
摘要： A pharmaceutical composition, including at least one nucleic acid, a Tyrode's medium having 140 mM NaC1, 6 mM KC1, 3 mM CaC12, 2 mM MgC12, 10 mM Hepes, pH 7.4, and 10 mM glucose; and a tetrafunctional copolymer of formula (I): where x and y represent, independently of one another, an integer of between 1 and 500, the tetrafunctional copolymer is in a form of a mineral salt wherein said tetrafunctional copolymer is in a cationic form. The compound of formula (I) has a molecular weight of between 1,000 and 25,000 g/mol and an EO/PO ratio of 0.8 to 1.2.
摘要翻译： 包含至少一种核酸的药物组合物，具有140mM NaCl，6mM KCl，3mM CaCl 2，2mM MgCl 2，10mM Hepes，pH 7.4和10mM葡萄糖的Tyrode's培养基; 和式（I）的四官能共聚物：其中x和y彼此独立地表示1至500的整数，所述四官能共聚物是矿物盐的形式，其中所述四官能共聚物是阳离子形式。 式（I）化合物的分子量为1,000〜25,000g / mol，EO / PO比为0.8〜1.2。
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7.发明授权Formulation of stabilized cationic transfection agent(s) /nucleic acid particles 失效稳定的阳离子转染剂/核酸颗粒的制剂公开(公告)号：US06884430B1
公开(公告)日：2005-04-26
申请号：US09369883
申请日：1999-08-09
申请人： Joël Crouzet , Bruno Pitard
发明人： Joël Crouzet , Bruno Pitard
CPC分类号： B82Y5/00 , A61K9/0019 , A61K9/1075 , A61K9/1272 , A61K47/10 , A61K47/60 , A61K47/69 , A61K47/6949 , A61K48/0008 , A61K48/0025 , A61K48/0041
摘要： The invention concerns a composition containing stabilized particles of cationic transfection agents/nucleic acid complexes characterized in that it includes besides said transfection agent and nucleic acid at least a non-ionic surfactant in sufficient amount for preventing the aggregation of the particles in course of time. In a preferred embodiment, the surfactant is a polyoxyalkylene or a derivative thereof.
摘要翻译： 本发明涉及含有阳离子转染剂/核酸复合物稳定化颗粒的组合物，其特征在于，除了所述转染剂和核酸之外，还包含至少一种足够量的非离子表面活性剂以防止颗粒在时间上的聚集。 在优选的实施方案中，表面活性剂是聚氧化烯或其衍生物。
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公开(公告)号：US20100179212A1
公开(公告)日：2010-07-15
申请号：US12659618
申请日：2010-03-15
申请人： Bruno Pitard
发明人： Bruno Pitard
IPC分类号： A61K31/713 , A61K31/7088 , A61P21/00 , A61P9/00
CPC分类号： A61K48/0041 , A61K31/77 , A61K31/785
摘要： A pharmaceutical composition which combines a tetrafunctional copolymer with a nucleic acid, said copolymer having formula I (namely a poloxamine), and preferably taking the form of one of the cationic mineral or organic salts thereof. The composition can be used to improve in vivo gene transfer.
摘要翻译： 将四官能共聚物与核酸组合的药物组合物，所述具有式I的共聚物（即泊洛沙胺），优选以阳离子矿物质或其有机盐之一的形式。 该组合物可用于改善体内基因转移。
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公开(公告)号：US20050152870A1
公开(公告)日：2005-07-14
申请号：US10502973
申请日：2003-02-07
申请人： Bruno Pitard
发明人： Bruno Pitard
IPC分类号： A61K47/04 , A61K31/7088 , A61K31/77 , A61K31/785 , A61K38/16 , A61K38/46 , A61K47/34 , A61K48/00 , A61P21/00 , A61P43/00
CPC分类号： A61K48/0041 , A61K31/77 , A61K31/785
摘要： The invention relates to a pharmaceutical composition which combines a tetrafunctional copolymer with a nucleic acid, said copolymer having formula I (namely a poloxamine), and preferably taking the form of one of the cationic mineral or organic salts thereof. The inventive composition can be used to improve in vivo gene transfer.
摘要翻译： 本发明涉及将四官能共聚物与核酸组合的药物组合物，所述共聚物具有式I（即泊洛沙胺），优选以阳离子矿物质或其有机盐之一的形式。 本发明的组合物可用于改善体内基因转移。
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10.发明申请COMPOSITIONS COMPRISING A SIRNA AND LIPIDIC 4,5-DISUBSTITUTED 2-DEOXYSTREPTAMINE RING AMINOGLYCOSIDE DERIVATIVES AND USES THEREOF 审中-公开包含SIRNA和脂质的4-dis取代的2-脱氧蛋白环环氨基酰胺衍生物的组合物及其用途公开(公告)号：US20100035974A1
公开(公告)日：2010-02-11
申请号：US12444390
申请日：2007-10-04
IPC分类号： A61K31/7008 , A61K38/02 , C12N5/08
CPC分类号： C12N15/111 , A61K31/713 , A61K48/0025 , C12N2310/14 , C12N2320/32
摘要： The present invention relates to a composition comprising a siRNA and a transfecting compound consisting of an aminoglycoside of the class of 4,5-disubstituted 2-deoxystreptamine ring linked via a spacer molecule to a lipid moiety of formula —(R1)R2 wherein R1 and R2 represent, independently of one another, a hydrogen atom or a fatty aliphatic chain or R1 or R2 is absent, with the proviso that at least one of R1 and R2 represents a fatty aliphatic chain; or —OR3 or —NR3 wherein R3 represents a steroidal derivative. The invention also concerns in vitro and in vivo applications of these compositions.
摘要翻译： 本发明涉及一种组合物，其包含siRNA和由间隔分子连接到式 - （R1）R2的脂质部分的4,5-二取代的2-脱氧链霉胺环类的氨基糖苷组成的转染化合物，其中R 1和 R2彼此独立地表示氢原子或脂肪族脂肪链，或者R1或R2不存在，条件是R1和R2中的至少一个表示脂肪族脂肪链; 或-OR 3或-NR 3，其中R 3表示甾体衍生物。 本发明还涉及这些组合物的体外和体内应用。
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