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1. 发明授权

US08324365B2 Conjugate for gene transfer comprising oligonucleotide and hydrophilic polymer, polyelectrolyte complex micelles formed from the conjugate, and methods for preparation thereof 有权
标题翻译：用于包含寡核苷酸和亲水性聚合物的基因转移的缀合物，由缀合物形成的聚电解质复合物胶束及其制备方法
公开(公告)号：US08324365B2
公开(公告)日：2012-12-04
申请号：US10551466
申请日：2003-04-03
申请人： Ji Hoon Jeong , Tae Gwan Park
发明人： Ji Hoon Jeong , Tae Gwan Park
IPC分类号： C07H21/04
CPC分类号： C12N15/113 , A61K47/60 , A61K47/6907 , A61K48/0041 , C12N15/111 , C12N2310/11 , C12N2310/351 , C12N2320/32
摘要： Disclosed is a conjugate for gene transfer, which is capable of being used for treatment of incurable diseases, comprising an oligonucleotide intended to be transferred into target cells and a hydrophilic polymer, wherein an end of the oligonucleotide is covalently conjugated to the hydrophilic polymer. Also, the present invention discloses polyelectrolyte complex micelles formed from such a conjugate and a cationic polymer or cationic peptide. Such polyelectrolyte complex micelles can effectively transfer oligonucleotides as therapeutic agents into target cells, making it possible to obtain desired activities of the delivered oligonucleotides in target cells even when the micelles are clinically applied at a relatively low concentration. Therefore, the conjugate and the polyelectrolyte complex micelle are very useful in basic life science research and the medical field.
摘要翻译：公开了用于基因转移的缀合物，其能够用于治疗不可治愈的疾病，包括旨在转移到靶细胞中的寡核苷酸和亲水性聚合物，其中寡核苷酸的末端与亲水性聚合物共价缀合。此外，本发明公开了由这种缀合物和阳离子聚合物或阳离子肽形成的聚电解质复合胶束。这样的聚电解质复合物胶束可以有效地将作为治疗剂的寡核苷酸转移到靶细胞中，使得即使当胶束以相对低的浓度临床施用时，也可以在靶细胞中获得递送的寡核苷酸的所需活性。因此，缀合物和聚电解质复合物胶束在基础生命科学研究和医学领域非常有用。

2. 发明授权

US08969543B2 SiRNA-hydrophilic polymer conjugates for intracellular delivery of siRNA and method thereof 有权
标题翻译：用于胞内递送siRNA的siRNA-亲水性聚合物缀合物及其方法
公开(公告)号：US08969543B2
公开(公告)日：2015-03-03
申请号：US11651011
申请日：2007-01-09
申请人： Ji Hoon Jeong , Tae Gwan Park , Sun-Hwa Kim
发明人： Ji Hoon Jeong , Tae Gwan Park , Sun-Hwa Kim
IPC分类号： C07H21/04 , C07H21/02 , A61K48/00
CPC分类号： C12N15/111 , A61K47/551 , A61K47/59 , A61K47/60 , C12N15/113 , C12N2310/14 , C12N2310/351 , C12N2320/32
摘要： The present invention is related to hybrid conjugates formed by covalently bonding siRNA (small interfering RNA) molecules to hydrophilic polymers for improving stability of the siRNA molecules effective for delivering the siRNA in vivo, and polyelectrolyte complex micelles formed by ionic interactions between the conjugates and multifunctional cationic compounds. The siRNA-hydrophilic polymer conjugates and polyelectrolyte complex micelles derived therefrom can be used for improving stability of the siRNA molecules in vivo. Consequently, the delivery of siRNA molecules for therapeutic applications into cells can be facilitated, and the siRNA is still active even though a small dose of the siRNA is used.
摘要翻译：本发明涉及通过将siRNA（小干扰RNA）分子与亲水性聚合物共价键合而形成的杂交缀合物，用于改善有效用于体内递送siRNA的siRNA分子的稳定性，以及通过缀合物与多功能化之间的离子相互作用形成的聚电解质复合胶束阳离子化合物。从其衍生的siRNA-亲水性聚合物缀合物和聚电解质复合物胶束可用于提高siRNA分子在体内的稳定性。因此，可以促进用于治疗应用的siRNA分子递送到细胞中，并且即使使用小剂量的siRNA，siRNA仍然是活性的。

3. 发明授权

US06623729B2 Process for preparing sustained release micelle employing conjugate of anticancer drug and biodegradable polymer 失效
标题翻译：使用抗癌药物和可生物降解聚合物的缀合物制备持续释放胶束的方法
公开(公告)号：US06623729B2
公开(公告)日：2003-09-23
申请号：US09902549
申请日：2001-07-09
申请人： Tae Gwan Park , Hyuk Sang Yoo
发明人： Tae Gwan Park , Hyuk Sang Yoo
IPC分类号： A61K4748
CPC分类号： A61K31/513 , A61K31/282 , A61K31/337 , A61K31/704
摘要： The present invention relates to a process of preparing a sustained release micelle by copolymerizing a biodegradable polyester hydrophobic polymer and a hydrophilic polyethylene glycol (PEG) to obtain a block copolymer, reacting the block copolymer with a linker to the hydroxyl group of the block copolymer and conjugating the linker-bound block copolymer to a drug to obtain a micelle monomer, and dispersing the micelle monomer an aqueous solution. The drug-micelle conjugate of the present invention has practical application in anticancer therapy.
摘要翻译：本发明涉及通过共聚可生物降解的聚酯疏水性聚合物和亲水性聚乙二醇（PEG）来制备持续释放胶束的方法，以获得嵌段共聚物，使嵌段共聚物与连接体与嵌段共聚物的羟基反应，以及将接头结合的嵌段共聚物与药物共轭以获得胶束单体，并将胶束单体分散在水溶液中。本发明的药物 - 胶束缀合物在抗癌治疗中具有实际应用。

4. 发明授权

US08580946B2 Multi-conjugate of siRNA and preparing method thereof 有权
标题翻译： siRNA的多重缀合物及其制备方法
公开(公告)号：US08580946B2
公开(公告)日：2013-11-12
申请号：US12514306
申请日：2009-04-29
申请人： Tae Gwan Park , Hye Jung Mok , Soo Hyeon Lee
发明人： Tae Gwan Park , Hye Jung Mok , Soo Hyeon Lee
IPC分类号： C07H21/04 , C12N15/113
CPC分类号： C12N15/1136 , C12N15/111 , C12N15/113 , C12N2310/14 , C12N2310/51
摘要： The present invention relates to a multi-conjugate of small interfering RNA (siRNA) and a preparing method of the same, more precisely a multi-conjugate of siRNA prepared by direct binding of double stranded sense/antisense siRNA monomers or indirect covalent bonding mediated by a cross-linking agent or a polymer, and a preparing method of the same. The preparing method of a siRNA multi-conjugate of the present invention is characterized by simple and efficient reaction and thereby the prepared siRNA multi-conjugate of the present invention has high molecular weight multiple times the conventional siRNA, so that it has high negative charge density, suggesting that it has excellent ionic interaction with a cationic gene carrier and high gene delivery efficiency.
摘要翻译：本发明涉及小干扰RNA（siRNA）的多重缀合物及其制备方法，更准确地说是通过双链有义/反义siRNA单体的直接结合制备的siRNA的多重缀合物或间接共价结合交联剂或聚合物及其制备方法。本发明的siRNA多偶联物的制备方法的特征在于简单且有效的反应，由此制备的本发明的siRNA多偶联物具有高分子量多次的常规siRNA，因此具有高的负电荷密度表明它与阳离子基因载体具有优异的离子相互作用和高基因传递效率。

5. 发明授权

US07163698B2 Controlled drug delivery system using the conjugation of drug to biodegradable polyester 失效
标题翻译：使用药物与生物可降解聚酯共轭的控制药物递送系统
公开(公告)号：US07163698B2
公开(公告)日：2007-01-16
申请号：US10423536
申请日：2003-04-25
申请人： Jong Eun Oh , Keon Hyoung Lee , Tae Gwan Park , Yoon Sung Nam
发明人： Jong Eun Oh , Keon Hyoung Lee , Tae Gwan Park , Yoon Sung Nam
IPC分类号： A61K9/14 , A61K9/16 , A61K9/50
CPC分类号： B82Y5/00 , A61K47/6927 , A61K47/6937
摘要： The present invention relates to the molecular sustained controlled release system constructed by the conjugation of molecules to be released with biodegradable polyester polymer via covalent bond and method for preparation thereof. In accordance with the present invention, the system may be formulated into microspheres, nanoparticles, or films. The molecular release rate from the above system can be regulated to be proportional to the chemical degradation rate of the biodegradable polyester polymers, resulting in near zero order kinetics profile of release without showing a burst effect. Moreover, the high loading efficiency of hydrophilic drugs can be achieved.
摘要翻译：本发明涉及通过共价键与待分解的分子与可生物降解的聚酯聚合物共轭构成的分子持续控制释放体系及其制备方法。根据本发明，该系统可以配制成微球，纳米颗粒或薄膜。可以调节上述体系的分子释放速率与可生物降解的聚酯聚合物的化学降解速率成比例，导致释放的接近零级动力学特征，而不发生爆裂效应。此外，可以实现亲水药物的高负载效率。

6. 发明申请

US20110044931A1 MULTI-CONJUGATE OF SIRNA AND PREPARING METHOD THEREOF 有权
标题翻译： SIRNA的多重结合及其制备方法
公开(公告)号：US20110044931A1
公开(公告)日：2011-02-24
申请号：US12514306
申请日：2009-04-29
申请人： Tae Gwan Park
发明人： Tae Gwan Park
IPC分类号： A61K31/787 , C07H21/02 , C08G73/04 , C08G73/20 , C08G81/02 , C08G63/08 , C07K16/00 , C07K1/113 , A61K31/713 , A61P35/00
CPC分类号： C12N15/1136 , C12N15/111 , C12N15/113 , C12N2310/14 , C12N2310/51
摘要： The present invention relates to a multi-conjugate of small interfering RNA (siRNA) and a preparing method of the same, more precisely a multi-conjugate of siRNA prepared by direct binding of double stranded sense/antisense siRNA monomers or indirect covalent bonding mediated by a cross-linking agent or a polymer, and a preparing method of the same. The preparing method of a siRNA multi-conjugate of the present invention is characterized by simple and efficient reaction and thereby the prepared siRNA multi-conjugate of the present invention has high molecular weight multiple times the conventional siRNA, so that it has high negative charge density, suggesting that it has excellent ionic interaction with a cationic gene carrier and high gene delivery efficiency.
摘要翻译：本发明涉及小干扰RNA（siRNA）的多重缀合物及其制备方法，更准确地说是通过双链有义/反义siRNA单体的直接结合制备的siRNA的多重缀合物或间接共价结合交联剂或聚合物及其制备方法。本发明的siRNA多偶联物的制备方法的特征在于简单且有效的反应，由此制备的本发明的siRNA多偶联物具有高分子量多次的常规siRNA，因此具有高的负电荷密度表明它与阳离子基因载体具有优异的离子相互作用和高基因传递效率。

7. 发明授权

US06589548B1 Controlled drug delivery system using the conjugation of drug to biodegradable polyester 失效
标题翻译：使用药物与生物可降解聚酯共轭的控制药物递送系统
公开(公告)号：US06589548B1
公开(公告)日：2003-07-08
申请号：US09700380
申请日：2000-11-14
申请人： Jong Eun Oh , Keon Hyoung Lee , Tae Gwan Park , Yoon Sung Nam
发明人： Jong Eun Oh , Keon Hyoung Lee , Tae Gwan Park , Yoon Sung Nam
IPC分类号： A61F200
CPC分类号： B82Y5/00 , A61K47/6927 , A61K47/6937
摘要： The present invention relates to a molecular sustained controlled release system constructed by the conjugation of molecules to be released with biodegradable polyester polymer via covalent bond and method for preparation thereof. In accordance with the present invention, the system may be formulated into microspheres, nanoparticles, or films. The molecular release rate from the above system can be regulated to be proportional to the chemical degradation rate of the biodegradable polyester polymers, resulting in near zero order kinetics profile of release without showing a burst effect, Moreover, a high loading efficiency of hydrophilic drugs can be achieved.
摘要翻译：本发明涉及通过共价键将待释放的分子与可生物降解的聚酯聚合物共轭而构成的分子持续控制释放系统及其制备方法。根据本发明，该系统可以配制成微球，纳米颗粒或薄膜。可以调节上述体系的分子释放速率与生物可降解聚酯聚合物的化学降解速率成比例，导致释放的接近零级动力学特征，而不发生爆裂效应。此外，亲水性药物的高负载效率可以实现。

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