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1. 发明专利

AU2012353058B2 Novel oligonucleotide conjugates and use thereof 未知
公开(公告)号：AU2012353058B2
公开(公告)日：2015-05-21
申请号：AU2012353058
申请日：2012-12-14
申请人： BIONEER CORP
发明人： CHAE JEIWOOK , HAN BORAM , KIM HAN-NA , PARK HAN OH , YOON PYOUNG OH , KIM SUN GI , JUNG KWANG-JU , KWON TAEWOO , CHOI JONG DEOK , LEE SAM YOUNG , JUNG EUN-JUNG
IPC分类号： A61K47/48 , A61K9/16 , A61K48/00 , C12N15/11
摘要： The present invention provides a double helix oligo-RNA structure in which target-specific ligands are bonded to the double helix oligo-RNA structure in which high molecular compounds for improving the delivery of double helix oligo-RNA that can be valuably used in treating diseases, specifically, cancer, are covalently bonded. The present invention also provides a method for preparing the RNA structure and a target-specific double helix oligo-RNA delivery technology through said structure. Nanoparticles constituted by the double helix oligo-RNA structure to which ligands are bonded may efficiently deliver double helix oligo-RNA to a target, and thus may exhibit an activity of double helix oligo-RNA structure in a target cell even with an administration of double helix oligo-RNA of relatively lower concentration. The nanoparticles may prevent the delivery of non-specific double helix oligo-RNA to other organs and cells, and therefore, can be valuably used not only as a tool for double helix oligo-RNA for treating various diseases, specifically, cancer, but also as a new type of double helix oligo-RNA delivery system. The present invention also relates to hybrid conjugates in which a hydrophilic material and a hydrophobic material are connected to both ends of antisense oligonucleotide(ASO) through covalent bond so as to achieve in vivo stability of the ASO, and to a method for preparing the hybrid conjugates and to nanoparticles constituted by the conjugates. The conjugates between ASO and macromolecules according to the present invention may improve in vivo stability of ASO, and therefore, can efficiently deliver ASO for treatment into cells and may exhibit an activity of ASO even with an administration of a relatively lower concentration.

2. 发明专利

CA2859127A1 NOVEL OLIGONUCLEOTIDE CONJUGATES AND USE THEREOF 未知
公开(公告)号：CA2859127A1
公开(公告)日：2013-06-20
申请号：CA2859127
申请日：2012-12-14
申请人： BIONEER CORP
发明人： CHAE JEIWOOK , HAN BORAM , KIM HAN-NA , PARK HAN OH , YOON PYOUNG OH , KIM SUN GI , JUNG KWANG-JU , KWON TAEWOO , CHOI JONG DEOK , LEE SAM YOUNG , JUNG EUN-JUNG
IPC分类号： A61K47/48 , A61K9/16 , A61K48/00 , C12N15/11
摘要： The present invention provides a double helix oligo-RNA structure in which target-specific ligands are bonded to the double helix oligo-RNA structure in which high molecular compounds for improving the delivery of double helix oligo-RNA that can be valuably used in treating diseases, specifically, cancer, are covalently bonded. The present invention also provides a method for preparing the RNA structure and a target-specific double helix oligo-RNA delivery technology through said structure. Nanoparticles constituted by the double helix oligo-RNA structure to which ligands are bonded may efficiently deliver double helix oligo-RNA to a target, and thus may exhibit an activity of double helix oligo-RNA structure in a target cell even with an administration of double helix oligo-RNA of relatively lower concentration. The nanoparticles may prevent the delivery of non-specific double helix oligo-RNA to other organs and cells, and therefore, can be valuably used not only as a tool for double helix oligo-RNA for treating various diseases, specifically, cancer, but also as a new type of double helix oligo-RNA delivery system. The present invention also relates to hybrid conjugates in which a hydrophilic material and a hydrophobic material are connected to both ends of antisense oligonucleotide(ASO) through covalent bond so as to achieve in vivo stability of the ASO, and to a method for preparing the hybrid conjugates and to nanoparticles constituted by the conjugates. The conjugates between ASO and macromolecules according to the present invention may improve in vivo stability of ASO, and therefore, can efficiently deliver ASO for treatment into cells and may exhibit an activity of ASO even with an administration of a relatively lower concentration.

3. 发明专利

PL2796150T3 NOWE KONIUGATY OLIGONUKLEOTYDOWE I ICH ZASTOSOWANIE 未知
公开(公告)号：PL2796150T3
公开(公告)日：2021-08-30
申请号：PL12857568
申请日：2012-12-14
申请人： BIONEER CORP
发明人： CHAE JEIWOOK , HAN BORAM , KIM HAN-NA , PARK HAN OH , YOON PYOUNG OH , KIM SUN GI , JUNG KWANG-JU , KWON TAEWOO , CHOI JONG DEOK , LEE SAM YOUNG , JUNG EUN-JUNG
IPC分类号： C12N15/113 , A61K9/16 , A61K31/713 , A61K47/54 , A61K47/55 , A61K47/60 , C12N15/11

4. 发明专利

CA2917299C IMPROVED NANOPARTICLE TYPE OLIGONUCLEOTIDE STRUCTURE HAVING HIGH EFFICIENCY AND METHOD FOR PREPARING SAME 未知
公开(公告)号：CA2917299C
公开(公告)日：2020-07-21
申请号：CA2917299
申请日：2014-07-04
申请人： BIONEER CORP
发明人： PARK HAN OH , CHAE JEIWOOK , YOON PYOUNG OH , HAN BORAM , CHOI GI-EUN , KO YOUNGHO , KWON TAEWOO , LEE JAE DON , KIM SUN GI
IPC分类号： C12N15/113 , A61K48/00 , C07H21/00
摘要： The present invention relates to an oligonucleotide structure and a method for preparing the same and, more particularly, to an oligonucleotide structure in which a polymer compound is linked to an oligonucleotide via a covalent bond to improve in vivo stability of the oligonucleotide and cellular delivery efficiency of the oligonucleotide; and to a method for preparing the same. The oligonucleotide structure is improved into a homogenous material, thereby solving the problem in material verification due to polydispersion characteristics occurring when a hydrophilic material linked to the oligonucleotide is a synthetic polymer; the nucleotide structure is easy to synthesize compared with the existing process; and the size of a double helix oilgo-RNA structure can be accurately adjusted through the control of the number of repetitions of a hydrophilic material block, and thus, the gene expression regulation function of the oligonucleotide does not deteriorate through the synthesis of the optimized oligonucleotide structure, and the oligonucleotide can be delivered into cells at even a relatively low-concentration dosage. Therefore, the oligonucleotide structure of the present invention can be useful as a novel type oligonucleotide delivery system as well as a tool for treating cancers, infectious diseases, and the like.

5. 发明专利

AU2014284834A1 Improved nanoparticle type oligonucleotide structure having high efficiency and method for preparing same 未知
公开(公告)号：AU2014284834A1
公开(公告)日：2016-02-18
申请号：AU2014284834
申请日：2014-07-04
申请人： BIONEER CORP
发明人： PARK HAN OH , CHAE JEIWOOK , YOON PYOUNG OH , HAN BORAM , CHOI GI-EUN , KO YOUNGHO , KWON TAEWOO , LEE JAE DON , KIM SUN GI
IPC分类号： C12N15/113 , A61K48/00 , C07H21/00
摘要： The present invention relates to an oligonucleotide structure and a method for preparing the same and, more particularly, to an oligonucleotide structure in which a polymer compound is linked to an oligonucleotide via a covalent bond to improve in vivo stability of the oligonucleotide and cellular delivery efficiency of the oligonucleotide; and to a method for preparing the same. The oligonucleotide structure is improved into a homogenous material, thereby solving the problem in material verification due to polydispersion characteristics occurring when a hydrophilic material linked to the oligonucleotide is a synthetic polymer; the nucleotide structure is easy to synthesize compared with the existing process; and the size of a double helix oilgo-RNA structure can be accurately adjusted through the control of the number of repetitions of a hydrophilic material block, and thus, the gene expression regulation function of the oligonucleotide does not deteriorate through the synthesis of the optimized oligonucleotide structure, and the oligonucleotide can be delivered into cells at even a relatively low-concentration dosage. Therefore, the oligonucleotide structure of the present invention can be useful as a novel type oligonucleotide delivery system as well as a tool for treating cancers, infectious diseases, and the like.

6. 发明专利

CA2917299A1 IMPROVED NANOPARTICLE TYPE OLIGONUCLEOTIDE STRUCTURE HAVING HIGH EFFICIENCY AND METHOD FOR PREPARING SAME 未知
公开(公告)号：CA2917299A1
公开(公告)日：2015-01-08
申请号：CA2917299
申请日：2014-07-04
申请人： BIONEER CORP
发明人： PARK HAN OH , CHAE JEIWOOK , YOON PYOUNG OH , HAN BORAM , CHOI GI-EUN , KO YOUNGHO , KWON TAEWOO , LEE JAE DON , KIM SUN GI
IPC分类号： C12N15/113 , A61K48/00 , C07H21/00
摘要： The present invention relates to an oligonucleotide structure and a method for preparing the same and, more particularly, to an oligonucleotide structure in which a polymer compound is linked to an oligonucleotide via a covalent bond to improve in vivo stability of the oligonucleotide and cellular delivery efficiency of the oligonucleotide; and to a method for preparing the same. The oligonucleotide structure is improved into a homogenous material, thereby solving the problem in material verification due to polydispersion characteristics occurring when a hydrophilic material linked to the oligonucleotide is a synthetic polymer; the nucleotide structure is easy to synthesize compared with the existing process; and the size of a double helix oilgo-RNA structure can be accurately adjusted through the control of the number of repetitions of a hydrophilic material block, and thus, the gene expression regulation function of the oligonucleotide does not deteriorate through the synthesis of the optimized oligonucleotide structure, and the oligonucleotide can be delivered into cells at even a relatively low-concentration dosage. Therefore, the oligonucleotide structure of the present invention can be useful as a novel type oligonucleotide delivery system as well as a tool for treating cancers, infectious diseases, and the like.

7. 发明公开

EP2796150A4 NOVEL OLIGONUCLEOTIDE CONJUGATES AND USE THEREOF 有权
标题翻译：新型它们的用途寡核苷酸缀合物和
公开(公告)号：EP2796150A4
公开(公告)日：2015-07-01
申请号：EP12857568
申请日：2012-12-14
申请人： BIONEER CORP
发明人： CHAE JEIWOOK , HAN BORAM , KIM HAN-NA , PARK HAN OH , YOON PYOUNG OH , KIM SUN GI , JUNG KWANG-JU , KWON TAEWOO , CHOI JONG DEOK , LEE SAM YOUNG , JUNG EUN-JUNG
IPC分类号： A61K47/48 , A61K9/16 , A61K31/713 , A61K48/00 , C12N15/11
CPC分类号： A61K47/42 , A61K31/713 , A61K47/549 , A61K47/551 , A61K47/60 , C12N15/111 , C12N15/113 , C12N2310/11 , C12N2310/14 , C12N2310/3513 , C12N2310/3515 , C12N2320/32
摘要： The present invention provides a double-stranded RNA structure, which comprises a polymer compound covalently bonded to a double-helix oligo RNA useful for the treatment of diseases, particularly cancer, in order to enhance the delivery of the double-helix oligo RNA, and further comprises a target-specific ligand bonded thereto, a preparation method thereof, and a technique of delivering the double-helix oligo RNA in a target-specific manner using the RNA structure. A nanoparticle composed of the ligand-bonded double-helix oligo RNA structures can efficiently deliver the double-helix oligo RNA to a target, and thus can exhibit the activity of the double-helix oligo RNA even when the double-helix oligo RNA is administered at a relatively low concentration. Also, it can prevent the non-specific delivery of the double-helix oligo RNA into other organs and cells. Accordingly, the ligand-bonded double-stranded RNA structure can be used for the treatment for various diseases, particularly cancer, and can also be effectively used as a new type of double-helix oligo RNA delivery system. Particularly, the ligand-bonded double-stranded RNA structure can be effectively used for the treatment of diseases, including cancer and infectious diseases. Moreover, the present invention relates to a hybrid conjugate, which comprises a hydrophilic material and hydrophobic material bonded to both ends of an antisense oligonucleotide (ASO) by a covalent bond in order to enhance the in vivo stability of the ASO, a method for preparing the hybrid conjugate, and a nanoparticle composed of the conjugates. The ASO-polymer conjugate according to the invention can increase the in vivo stability of the ASO, making it possible to efficiently deliver the therapeutic ASO into cells. Also, the ASO-polymer conjugate can exhibit the activity of the ASO even when it is administered at a relatively low concentration.

8. 发明公开

EP3018208A4 IMPROVED NANOPARTICLE TYPE OLIGONUCLEOTIDE STRUCTURE HAVING HIGH EFFICIENCY AND METHOD FOR PREPARING SAME 有权
标题翻译： WITH其制造高效方法，通过改进寡核苷酸纳米微粒结构
公开(公告)号：EP3018208A4
公开(公告)日：2017-03-08
申请号：EP14819529
申请日：2014-07-04
申请人： BIONEER CORP
发明人： PARK HAN OH , CHAE JEIWOOK , YOON PYOUNG OH , HAN BORAM , CHOI GI-EUN , KO YOUNGHO , KWON TAEWOO , LEE JAE DON , KIM SUN GI
IPC分类号： C12N15/11 , C12N15/113
CPC分类号： C12N15/113 , A61K9/127 , A61K9/5123 , A61K31/713 , A61K47/48023 , A61K47/48907 , A61K47/54 , A61K47/6935 , C07H21/00 , C12N15/111 , C12N2310/11 , C12N2310/14 , C12N2310/351 , C12N2310/3515 , C12N2320/32 , C12N2330/30
摘要： The present invention relates to an oligonucleotide structure and a method for preparing the same and, more particularly, to an oligonucleotide structure in which a polymer compound is linked to an oligonucleotide via a covalent bond to improve in vivo stability of the oligonucleotide and cellular delivery efficiency of the oligonucleotide; and to a method for preparing the same. The oligonucleotide structure is improved into a homogenous material, thereby solving the problem in material verification due to polydispersion characteristics occurring when a hydrophilic material linked to the oligonucleotide is a synthetic polymer; the nucleotide structure is easy to synthesize compared with the existing process; and the size of a double helix oilgo-RNA structure can be accurately adjusted through the control of the number of repetitions of a hydrophilic material block, and thus, the gene expression regulation function of the oligonucleotide does not deteriorate through the synthesis of the optimized oligonucleotide structure, and the oligonucleotide can be delivered into cells at even a relatively low-concentration dosage. Therefore, the oligonucleotide structure of the present invention can be useful as a novel type oligonucleotide delivery system as well as a tool for treating cancers, infectious diseases, and the like.

9. 发明公开

EP2881385A4 NOVEL AZO COMPOUND, USE THEREOF AND METHOD FOR PREPARING SAME 审中-公开
标题翻译：新型偶氮化合物，它们的用途和方法及其生产
公开(公告)号：EP2881385A4
公开(公告)日：2016-06-29
申请号：EP13826196
申请日：2013-08-02
申请人： BIONEER CORP
发明人： KIM SUN GI , KWON TAEWOO , CHOI JUNG YUNG
IPC分类号： C07D213/72 , C07D277/82 , C09K3/00 , C09K11/06
CPC分类号： C12Q1/6818 , C07D213/72 , C07D277/82 , C09B31/14 , C09B31/153

10. 发明专利

ES2899043T3 Novedosos conjugados de oligonucleótidos y su uso 未知
公开(公告)号：ES2899043T3
公开(公告)日：2022-03-09
申请号：ES12857568
申请日：2012-12-14
申请人： BIONEER CORP
发明人： CHAE JEIWOOK , HAN BORAM , KIM HAN-NA , PARK HAN OH , YOON PYOUNG OH , KIM SUN GI , JUNG KWANG-JU , KWON TAEWOO , CHOI JONG DEOK , LEE SAM YOUNG , JUNG EUN-JUNG
IPC分类号： C12N15/113 , A61K9/16 , A61K31/713 , A61K47/54 , A61K47/55 , A61K47/60 , C12N15/11
摘要： Una estructura terapéutica de fármaco-polímero que tiene una estructura de la siguiente fórmula (1) y que comprende un ligando unido a ella: Fórmula 1 L-A-X-R-y-B en donde A es un material hidrófilo; B es un material hidrófobo; X e y son cada uno un enlace covalente simple o un enlace covalente mediado por enlazador, independientemente el uno del otro; R es un oligo ARN de doble hélice; y L es un ligando específico del receptor que tiene la propiedad de mejorar la internalización de la célula diana por endocitosis mediada por el receptor (RME), unida covalentemente al extremo del material hidrófilo, estando dicho ligando seleccionado entre folato, N-acetilgalactosamina (NAG) y manosa.

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