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1. 发明申请

WO2015005669A1 LIVER CANCER RELATED GENES-SPECIFIC siRNA, DOUBLE-STRANDED OLIGO RNA MOLECULES COMPRISING THE siRNA, AND COMPOSITION FOR PREVENTING OR TREATING CANCER COMPRISING THE SAME 审中-公开
标题翻译：肝癌相关基因特异性siRNA，包含siRNA的双链寡聚RNA分子，以及用于预防或治疗包含其的癌症的组合物
公开(公告)号：WO2015005669A1
公开(公告)日：2015-01-15
申请号：PCT/KR2014/006145
申请日：2014-07-09
申请人： BIONEER CORPORATION , SANOFI-AVENTIS KOREA CO., LTD.
发明人： CHAE, Jeiwook , PARK, Han Oh , YOON, Pyoung Oh , HAN, Boram , KIM, Han-Na , YUN, Sung-Il , PARK, Jun Hong , KO, Youngho , CHOI, Gi-Eun , JUNG, Junsoo , KIM, Jae Eun
IPC分类号： C12N15/113 , A61K31/7088 , A61K48/00 , A61P35/00
CPC分类号： C12N15/1135 , A61K9/0019 , A61K9/51 , A61K31/713 , A61K47/60 , C12N2310/14
摘要： There is provided a liver cancer related specific siRNA and high efficiency double-stranded oligo RNA molecules containing the same. The double-stranded oligo RNA molecules have a structure in which hydrophilic and hydrophobic compounds are conjugated to both ends of the double-stranded oligo RNA molecules by a simple covalent bond or a linker-mediated covalent bond in order to be efficiently delivered into cells and may be converted into nanoparticles in an aqueous solution by hydrophobic interactions of the double-stranded oligo RNA molecules. The siRNA contained in the double-stranded oligo RNA molecules may be liver cancer related genes, particularly Gankyrin or BMI-1 specific siRNA. In addition, the present invention relates to a method of preparing the double-stranded oligo RNA molecules, and a pharmaceutical composition for preventing or treating cancer, particularly, liver cancer, containing the double-stranded oligo RNA molecules.
摘要翻译：提供了与相关肝癌相关的特异性siRNA和高效双链寡聚RNA分子。双链寡RNA分子具有通过简单的共价键或连接体介导的共价键将亲水和疏水化合物与双链寡RNA分子的两端缀合以便有效地递送到细胞中的结构，可以通过双链寡聚RNA分子的疏水相互作用在水溶液中转化成纳米颗粒。双链寡核苷酸分子中含有的siRNA可能是肝癌相关基因，特别是Gankyrin或BMI-1特异性siRNA。此外，本发明涉及制备双链寡聚RNA分子的方法和用于预防或治疗包含双链寡RNA分子的癌症，特别是肝癌的药物组合物。

2. 发明申请

WO2015005670A1 LIVER CANCER RELATED GENES-SPECIFIC siRNA, DOUBLE-STRANDED OLIGO RNA MOLECULES COMPRISING THE siRNA, AND COMPOSITION FOR PREVENTING OR TREATING CANCER COMPRISING THE SAME 审中-公开
标题翻译：肝癌相关基因特异性siRNA，包含siRNA的双链寡聚RNA分子，以及用于预防或治疗包含其的癌症的组合物
公开(公告)号：WO2015005670A1
公开(公告)日：2015-01-15
申请号：PCT/KR2014/006146
申请日：2014-07-09
申请人： BIONEER CORPORATION , SANOFI-AVENTIS KOREA CO., LTD.
发明人： CHAE, Jeiwook , YOON, Pyoung Oh , KIM, Han-Na , PARK, Han Oh , HAN, Boram , KO, Youngho , CHOI, Gi-Eun , KIM, Jae Eun
IPC分类号： C12N15/113 , A61K48/00 , A61K31/7088 , A61P35/00
CPC分类号： C12N15/1137 , A61K9/1075 , A61K31/713 , A61K47/6907 , C12N15/113 , C12N15/1135 , C12N2310/14 , C12N2310/31 , C12N2310/351 , C12N2320/30
摘要： There is provided a liver cancer related specific siRNA and high efficiency double-stranded oligo RNA molecules containing the same. The double-stranded oligo RNA molecules have a structure in which hydrophilic and hydrophobic compounds are conjugated to both ends of the double-stranded oligo RNA molecules by a simple covalent bond or a linker-mediated covalent bond in order to be efficiently delivered into cells and may be converted into nanoparticles in an aqueous solution by hydrophobic interactions of the double-stranded oligo RNA molecules. The siRNA contained in the double-stranded oligo RNA molecules may be liver cancer related genes, particularly ZBTB7A, YAP1 or CHD1L specific siRNA. In addition, the present invention relates to a method of preparing the double-stranded oligo RNA molecules, and a pharmaceutical composition for preventing or treating cancer, particularly, liver cancer, containing the double-stranded oligo RNA molecules.
摘要翻译：提供了与相关肝癌相关的特异性siRNA和高效双链寡聚RNA分子。双链寡RNA分子具有通过简单的共价键或连接体介导的共价键将亲水和疏水化合物与双链寡RNA分子的两端缀合以便有效地递送到细胞中的结构，可以通过双链寡聚RNA分子的疏水相互作用在水溶液中转化成纳米颗粒。双链寡核苷酸分子中包含的siRNA可能是肝癌相关基因，特别是ZBTB7A，YAP1或CHD1L特异性siRNA。此外，本发明涉及制备双链寡聚RNA分子的方法和用于预防或治疗包含双链寡RNA分子的癌症，特别是肝癌的药物组合物。

3. 发明公开

EP3019612A1 LIVER CANCER RELATED GENES-SPECIFIC siRNA, DOUBLE-STRANDED OLIGO RNA MOLECULES COMPRISING THE siRNA, AND COMPOSITION FOR PREVENTING OR TREATING CANCER COMPRISING THE SAME 审中-公开
标题翻译：肝癌相关基因特异性的siRNA，双OLIGO RNA分子的siRNA及组成预防和治疗癌症的任何保证，
公开(公告)号：EP3019612A1
公开(公告)日：2016-05-18
申请号：EP14823194.7
申请日：2014-07-09
申请人： Bioneer Corporation , Sanofi-Aventis Korea Co. Ltd.
发明人： CHAE, Jeiwook , YOON, Pyoung Oh , KIM, Han-Na , PARK, Han Oh , HAN, Boram , KO, Youngho , CHOI, Gi-Eun , KIM, Jae Eun
IPC分类号： C12N15/113 , A61K48/00 , A61K31/7088 , A61P35/00
CPC分类号： C12N15/1137 , A61K9/1075 , A61K31/713 , A61K47/6907 , C12N15/113 , C12N15/1135 , C12N2310/14 , C12N2310/31 , C12N2310/351 , C12N2320/30
摘要： There is provided a liver cancer related specific siRNA and high efficiency double-stranded oligo RNA molecules containing the same. The double-stranded oligo RNA molecules have a structure in which hydrophilic and hydrophobic compounds are conjugated to both ends of the double-stranded oligo RNA molecules by a simple covalent bond or a linker-mediated covalent bond in order to be efficiently delivered into cells and may be converted into nanoparticles in an aqueous solution by hydrophobic interactions of the double-stranded oligo RNA molecules. The siRNA contained in the double-stranded oligo RNA molecules may be liver cancer related genes, particularly ZBTB7A, YAP1 or CHD1L specific siRNA. In addition, the present invention relates to a method of preparing the double-stranded oligo RNA molecules, and a pharmaceutical composition for preventing or treating cancer, particularly, liver cancer, containing the double-stranded oligo RNA molecules.
摘要翻译：提供了相关的特异性siRNA和高效率双链寡RNA分子含有其的肝癌。该双链寡RNA分子具有其中亲水性和疏水性化合物通过简单的共价键或在顺序的接头 - 介导的共价键结合到双链寡RNA分子的两端的结构被有效地递送到细胞和可以在由双链寡RNA分子的疏水性相互作用wässrige溶液被转化成纳米颗粒英寸中含有的双链寡RNA分子的siRNA可以是肝癌相关基因，尤其是ZBTB7A，YAP1或CHD1L特异siRNA。此外，本发明涉及制备该双链寡RNA分子的方法，以及用于预防或治疗癌症，特别是肝癌，通过含有双链寡RNA分子的药物组合物。

4. 发明公开

EP3019611A1 LIVER CANCER RELATED GENES-SPECIFIC siRNA, DOUBLE-STRANDED OLIGO RNA MOLECULES COMPRISING THE siRNA, AND COMPOSITION FOR PREVENTING OR TREATING CANCER COMPRISING THE SAME 审中-公开
标题翻译：肝癌相关基因特异性siRNA，包含该siRNA的双链寡核苷酸分子，以及用于预防或治疗包含该癌症的癌症的组合物
公开(公告)号：EP3019611A1
公开(公告)日：2016-05-18
申请号：EP14822311.8
申请日：2014-07-09
申请人： Bioneer Corporation , Sanofi-Aventis Korea Co. Ltd.
发明人： CHAE, Jeiwook , PARK, Han Oh , YOON, Pyoung Oh , HAN, Boram , KIM, Han-Na , YUN, Sung-Il , PARK, Jun Hong , KO, Youngho , CHOI, Gi-Eun , JUNG, Junsoo , KIM, Jae Eun
IPC分类号： C12N15/113 , A61K31/7088 , A61K48/00 , A61P35/00
CPC分类号： C12N15/1135 , A61K9/0019 , A61K9/51 , A61K31/713 , A61K47/60 , C12N2310/14
摘要： There is provided a liver cancer related specific siRNA and high efficiency double-stranded oligo RNA molecules containing the same. The double-stranded oligo RNA molecules have a structure in which hydrophilic and hydrophobic compounds are conjugated to both ends of the double-stranded oligo RNA molecules by a simple covalent bond or a linker-mediated covalent bond in order to be efficiently delivered into cells and may be converted into nanoparticles in an aqueous solution by hydrophobic interactions of the double-stranded oligo RNA molecules. The siRNA contained in the double-stranded oligo RNA molecules may be liver cancer related genes, particularly Gankyrin or BMI-1 specific siRNA. In addition, the present invention relates to a method of preparing the double-stranded oligo RNA molecules, and a pharmaceutical composition for preventing or treating cancer, particularly, liver cancer, containing the double-stranded oligo RNA molecules.
摘要翻译：提供了肝癌相关特异性siRNA和包含其的高效双链寡RNA分子。双链寡RNA分子具有这样的结构，其中亲水性和疏水性化合物通过简单的共价键或接头介导的共价键与双链寡RNA分子的两个末端缀合，以便有效递送到细胞中，并且可以通过双链寡RNA分子的疏水相互作用转化成水溶液中的纳米颗粒。包含在双链寡RNA分子中的siRNA可以是肝癌相关基因，特别是Gankyrin或BMI-1特异性siRNA。此外，本发明涉及制备双链寡RNA分子的方法，以及用于预防或治疗癌症，特别是包含双链寡RNA分子的肝癌的药物组合物。

5. 发明公开

EP2796150A1 NOVEL OLIGONUCLEOTIDE CONJUGATES AND USE THEREOF 有权
标题翻译：维也纳戴维顿的神经元寡妇
公开(公告)号：EP2796150A1
公开(公告)日：2014-10-29
申请号：EP12857568.5
申请日：2012-12-14
申请人： Bioneer Corporation
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 , C12N15/11 , A61K9/16 , A61K48/00
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.
摘要翻译：本发明提供双链RNA结构，其包含与用于治疗疾病，特别是癌症的双螺旋寡聚RNA共价键合的高分子化合物，以增强双螺旋寡聚RNA的递送，以及还包括与其键合的靶特异性配体，其制备方法，以及使用RNA结构以目标特异性方式递送双螺旋寡聚RNA的技术。由配体键合的双螺旋寡聚RNA结构组成的纳米粒子可以有效地将双螺旋寡聚RNA递送到靶，因此即使施用双螺旋寡核苷酸RNA也能显示双螺旋寡聚RNA的活性浓度相对较低。此外，它可以防止双螺旋寡聚RNA非特异性递送到其他器官和细胞中。因此，配体键合的双链RNA结构可以用于各种疾病，特别是癌症的治疗，也可以有效地用作新型双螺旋寡聚RNA递送系统。特别地，配体键合的双链RNA结构可以有效地用于治疗包括癌症和感染性疾病在内的疾病。此外，本发明涉及一种杂合缀合物，其包含通过共价键与反义寡核苷酸（ASO）的两端键合的亲水性材料和疏水性材料，以增强ASO的体内稳定性，制备方法杂交缀合物和由缀合物组成的纳米颗粒。根据本发明的ASO-聚合物缀合物可以增加ASO的体内稳定性，使得可以有效地将治疗性ASO递送到细胞中。此外，即使以相对低的浓度施用，ASO-聚合物缀合物也可以表现出ASO的活性。

6. 发明公开

EP3913055A1 DOUBLE-STRANDED OLIGONUCLEOTIDE TARGETING DKK1 GENE, CONSTRUCT INCLUDING SAME, AND HAIR LOSS PREVENTION OR HAIR GROWTH COMPOSITION CONTAINING SAME 审中-实审
公开(公告)号：EP3913055A1
公开(公告)日：2021-11-24
申请号：EP20742087.8
申请日：2020-01-15
申请人： Bioneer Corporation
发明人： PARK, Han-Oh , YUN, Sung Il , BYUN, Sang-Jin , YOON, Pyoung Oh , LEE, Sang-Kyu , KIM, Tae-Rim , KO, Young-Ho , SON, Seung-Seob , GOH, Eun-Ah , KIM, Hyung-Jin
IPC分类号： C12N15/113 , A61K31/713 , A61K9/14 , A61P17/14
摘要： The present invention pertains to: a double-stranded oligonucleotide construct having a structure in which a hydrophilic substance and a hydrophobic substance are conjugated by a simple covalent bond or a linker-mediated covalent bond at both ends of a DKK1-specific double-stranded oligonucleotide to efficiently deliver the double-stranded oligonucleotide into cells; a nanoparticle capable of being produced through self-assembly of the double-stranded oligonucleotide construct through a hydrophobic interaction in an aqueous solution; and a hair-loss-preventing and hair-growth-promoting composition containing the double-stranded oligonucleotide construct or the nanoparticle. A double-stranded oligonucleotide construct including a DKK1-specific double-stranded oligonucleotide, a nanoparticle, and a hair loss prevention or hair growth composition containing the double-stranded oligonucleotide construct or the nanoparticle as an active ingredient according to the present invention very efficiently suppress the expression of DKK1 without side effects and are remarkably effective for preventing hair loss and promoting hair growth, and can thus be very usefully used for a composition for preventing hair loss and promoting hair growth.

7. 发明授权

EP3018208B1 IMPROVED NANOPARTICLE TYPE OLIGONUCLEOTIDE STRUCTURE HAVING HIGH EFFICIENCY AND METHOD FOR PREPARING SAME 有权
公开(公告)号：EP3018208B1
公开(公告)日：2020-05-27
申请号：EP14819529.0
申请日：2014-07-04
申请人： Bioneer Corporation
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 , A61K9/127 , A61K47/54 , A61K47/69

8. 发明公开

EP3591053A1 RESPIRATORY DISEASE-RELATED GENE SPECIFIC SIRNA, DOUBLE-HELICAL OLIGO RNA STRUCTURE CONTAINING SIRNA, COMPOSITON CONTAINING SAME FOR PREVENTING OR TREATING RESPIRATORY DISEASE 审中-公开
公开(公告)号：EP3591053A1
公开(公告)日：2020-01-08
申请号：EP19180054.9
申请日：2014-07-04
申请人： Bioneer Corporation , Yuhan Corporation
发明人： CHAE, Jeiwook , PARK, Han Oh , YOON, Pyoung Oh , HAN, Boram , KIM, Mi Na
IPC分类号： C12N15/113 , C07H21/02 , A61K48/00 , A61P11/00
摘要： The present invention relates to respiratory diseases, especially to gene specific siRNA related to idiopathic pulmonary fibrosis and chronic obstructive pulmonary disease (COPD), and a highly efficient double-helical oligo RNA structure containing the same, wherein the double-helical oligo RNA structure has a structure in which hydrophilic and hydrophobic materials are bonded at the both ends of the double-helical RNA (siRNA) using a simple covalent bond or a linker-mediated covalent bond to be effectively transferred into a cell, and is converted into nanoparticles by the hydrophobic interaction of the double-helical oligo RNA structure in a solution. It is desirable that the siRNA contained in the double-helical oligo RNA structure is a siRNA specific to a CTGF, Cyr61, or Plekhol, which are genes related to respiratory diseases, particularly idiopathic pulmonary fibrosis and COPD. In addition, the present invention relates to a method for producing the double-helical oligo RNA structure and a pharmaceutical composition containing the double-helical oligo RNA structure for preventing or treating respiratory diseases, particularly idiopathic pulmonary fibrosis and COPD.

9. 发明公开

EP3816285A1 AMPHIREGULIN GENE-SPECIFIC DOUBLE-STRANDED OLIGONUCLEOTIDE AND COMPOSITION, FOR PREVENTING AND TREATING FIBROSIS-RELATED DISEASES AND RESPIRATORY DISEASES, COMPRISING SAME 审中-实审
公开(公告)号：EP3816285A1
公开(公告)日：2021-05-05
申请号：EP19806488.3
申请日：2019-05-22
申请人： Bioneer Corporation
发明人： KIM, Tae-Rim , YOON, Pyoung Oh , KO, Youngho , BAE, Seon Joo , PARK, Han-Oh , SON, Seung Seob , PARK, Jun Hong , YUN, Sung Il
IPC分类号： C12N15/113 , A61K31/713 , A61P11/00 , A61P11/06 , A61P29/00
摘要： The present invention relates to a double-stranded oligonucleotide which can highly specifically and efficiently inhibit an amphiregulin expression and, preferably, a double-stranded oligonucleotide comprising a sequence in the form of RNA/RNA, DNA/DNA or DNA/RNA hybrid, a double-stranded oligonucleotide structure comprising the double-stranded oligonucleotide, nanoparticles comprising the double-stranded oligonucleotide structure, and a fibrosis or respiratory disease preventive or therapeutic use thereof.

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