KR101224828B1 - ｓｉＲＮＡ 접합체 및 그 제조방법 - Google Patents

ｓｉＲＮＡ 접합체 및 그 제조방법 Download PDF

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KR101224828B1
KR101224828B1 KR1020090042297A KR20090042297A KR101224828B1 KR 101224828 B1 KR101224828 B1 KR 101224828B1 KR 1020090042297 A KR1020090042297 A KR 1020090042297A KR 20090042297 A KR20090042297 A KR 20090042297A KR 101224828 B1 KR101224828 B1 KR 101224828B1
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South Korea
Prior art keywords
sirna
conjugate
polymer compound
peg
bond
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KR1020090042297A
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Korean (ko)
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KR20100123214A (ko
Inventor
한보람
박한오
신미식
이삼용
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(주)바이오니아
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Priority to KR1020090042297A priority Critical patent/KR101224828B1/ko
Application filed by (주)바이오니아 filed Critical (주)바이오니아
Priority to AU2010248239A priority patent/AU2010248239B2/en
Priority to EP10775118.2A priority patent/EP2463371B1/en
Priority to PCT/KR2010/003039 priority patent/WO2010131916A2/ko
Priority to EP13159602.5A priority patent/EP2626427A3/en
Priority to CA2871888A priority patent/CA2871888A1/en
Priority to CN201210301551.2A priority patent/CN102888404B/zh
Priority to CN201310147988.XA priority patent/CN103233003B/zh
Priority to RU2011150787/10A priority patent/RU2558258C2/ru
Priority to BRPI1012141A priority patent/BRPI1012141B1/pt
Priority to CN201080021324.3A priority patent/CN102439148B/zh
Priority to CA2761749A priority patent/CA2761749C/en
Priority to EP13185358.2A priority patent/EP2682466B1/en
Priority to US13/319,885 priority patent/US8779114B2/en
Priority to JP2012510752A priority patent/JP5758381B2/ja
Publication of KR20100123214A publication Critical patent/KR20100123214A/ko
Priority to US13/613,071 priority patent/US8772472B2/en
Application granted granted Critical
Publication of KR101224828B1 publication Critical patent/KR101224828B1/ko
Priority to JP2013098798A priority patent/JP5797688B2/ja
Priority to RU2013151977/10A priority patent/RU2571218C2/ru
Priority to US14/291,540 priority patent/US9211343B2/en
Priority to US14/291,656 priority patent/US20140350233A1/en
Priority to JP2014244541A priority patent/JP2015107115A/ja
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    • C—CHEMISTRY; METALLURGY
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    • C07F7/00—Compounds containing elements of Groups 4 or 14 of the Periodic Table
    • C07F7/02—Silicon compounds
    • C07F7/08—Compounds having one or more C—Si linkages
    • C07F7/0834—Compounds having one or more O-Si linkage
    • C07F7/0836—Compounds with one or more Si-OH or Si-O-metal linkage
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    • C12N15/09—Recombinant DNA-technology
    • C12N15/11—DNA or RNA fragments; Modified forms thereof; Non-coding nucleic acids having a biological activity
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    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/56—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule
    • A61K47/59—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes
    • A61K47/60—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes the organic macromolecular compound being a polyoxyalkylene oligomer, polymer or dendrimer, e.g. PEG, PPG, PEO or polyglycerol
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    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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    • A61K9/107—Emulsions ; Emulsion preconcentrates; Micelles
    • A61K9/1075—Microemulsions or submicron emulsions; Preconcentrates or solids thereof; Micelles, e.g. made of phospholipids or block copolymers
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H21/00—Compounds containing two or more mononucleotide units having separate phosphate or polyphosphate groups linked by saccharide radicals of nucleoside groups, e.g. nucleic acids
    • C07H21/02—Compounds containing two or more mononucleotide units having separate phosphate or polyphosphate groups linked by saccharide radicals of nucleoside groups, e.g. nucleic acids with ribosyl as saccharide radical
    • C—CHEMISTRY; METALLURGY
    • C08—ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
    • C08G—MACROMOLECULAR COMPOUNDS OBTAINED OTHERWISE THAN BY REACTIONS ONLY INVOLVING UNSATURATED CARBON-TO-CARBON BONDS
    • C08G65/00—Macromolecular compounds obtained by reactions forming an ether link in the main chain of the macromolecule
    • C08G65/02—Macromolecular compounds obtained by reactions forming an ether link in the main chain of the macromolecule from cyclic ethers by opening of the heterocyclic ring
    • C08G65/32—Polymers modified by chemical after-treatment
    • C08G65/329—Polymers modified by chemical after-treatment with organic compounds
    • C08G65/335—Polymers modified by chemical after-treatment with organic compounds containing phosphorus
    • C08G65/3356—Polymers modified by chemical after-treatment with organic compounds containing phosphorus having nitrogen in addition to phosphorus
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    • C12N15/113—Non-coding nucleic acids modulating the expression of genes, e.g. antisense oligonucleotides; Antisense DNA or RNA; Triplex- forming oligonucleotides; Catalytic nucleic acids, e.g. ribozymes; Nucleic acids used in co-suppression or gene silencing
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    • C12N15/87—Introduction of foreign genetic material using processes not otherwise provided for, e.g. co-transformation
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/34—Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers
    • B—PERFORMING OPERATIONS; TRANSPORTING
    • B82—NANOTECHNOLOGY
    • B82Y—SPECIFIC USES OR APPLICATIONS OF NANOSTRUCTURES; MEASUREMENT OR ANALYSIS OF NANOSTRUCTURES; MANUFACTURE OR TREATMENT OF NANOSTRUCTURES
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    • C12N2320/51—Methods for regulating/modulating their activity modulating the chemical stability, e.g. nuclease-resistance
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    • Y10S—TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y10S977/00—Nanotechnology
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  • Bioinformatics & Cheminformatics (AREA)
  • Biochemistry (AREA)
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  • General Engineering & Computer Science (AREA)
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  • Animal Behavior & Ethology (AREA)
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  • Pharmacology & Pharmacy (AREA)
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  • Physics & Mathematics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Communicable Diseases (AREA)
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  • Polymers & Plastics (AREA)
  • Virology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
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  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Apparatus Associated With Microorganisms And Enzymes (AREA)
  • Other Resins Obtained By Reactions Not Involving Carbon-To-Carbon Unsaturated Bonds (AREA)
  • Polyethers (AREA)
KR1020090042297A 2009-05-14 2009-05-14 ｓｉＲＮＡ 접합체 및 그 제조방법 Active KR101224828B1 (ko)

Priority Applications (21)

Application Number Priority Date Filing Date Title
KR1020090042297A KR101224828B1 (ko) 2009-05-14 2009-05-14 ｓｉＲＮＡ 접합체 및 그 제조방법
US13/319,885 US8779114B2 (en) 2009-05-14 2010-05-13 siRNA conjugate and preparation method thereof
PCT/KR2010/003039 WO2010131916A2 (ko) 2009-05-14 2010-05-13 siRNA 접합체 및 그 제조방법
EP13159602.5A EP2626427A3 (en) 2009-05-14 2010-05-13 Sirna conjugate and preparation method thereof
CA2871888A CA2871888A1 (en) 2009-05-14 2010-05-13 Sirna conjugate and preparation method thereof
CN201210301551.2A CN102888404B (zh) 2009-05-14 2010-05-13 siRNA缀合物及其制备方法
CN201310147988.XA CN103233003B (zh) 2009-05-14 2010-05-13 siRNA缀合物及其制备方法
EP10775118.2A EP2463371B1 (en) 2009-05-14 2010-05-13 Sirna conjugate and preparation method thereof
BRPI1012141A BRPI1012141B1 (pt) 2009-05-14 2010-05-13 conjugado de sirna e método de preparação do mesmo
CN201080021324.3A CN102439148B (zh) 2009-05-14 2010-05-13 siRNA缀合物及其制备方法
AU2010248239A AU2010248239B2 (en) 2009-05-14 2010-05-13 siRNA conjugate and preparation method thereof
EP13185358.2A EP2682466B1 (en) 2009-05-14 2010-05-13 siRNA conjugate and preparation method thereof
RU2011150787/10A RU2558258C2 (ru) 2009-05-14 2010-05-13 Конъюгат мирнк и способ его получения
CA2761749A CA2761749C (en) 2009-05-14 2010-05-13 Sirna conjugate and preparation method thereof
JP2012510752A JP5758381B2 (ja) 2009-05-14 2010-05-13 ｓｉＲＮＡ接合体及びその製造方法
US13/613,071 US8772472B2 (en) 2009-05-14 2012-09-13 SiRNA conjugate and preparation method thereof
JP2013098798A JP5797688B2 (ja) 2009-05-14 2013-05-08 ｓｉＲＮＡ接合体及びその製造方法
RU2013151977/10A RU2571218C2 (ru) 2009-05-14 2013-11-21 Конъюгат мирнк и способ его получения
US14/291,540 US9211343B2 (en) 2009-05-14 2014-05-30 siRNA conjugate and preparation method thereof
US14/291,656 US20140350233A1 (en) 2009-05-14 2014-05-30 Sirna conjugate and preparation method thereof
JP2014244541A JP2015107115A (ja) 2009-05-14 2014-12-02 ｓｉＲＮＡ接合体及びその製造方法

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Application Number Priority Date Filing Date Title
KR1020090042297A KR101224828B1 (ko) 2009-05-14 2009-05-14 ｓｉＲＮＡ 접합체 및 그 제조방법

Related Child Applications (2)

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KR1020120069988A Division KR101241852B1 (ko) 2012-06-28 2012-06-28 ｓｉＲＮＡ 접합체 및 그 제조방법
KR1020120114011A Division KR101392973B1 (ko) 2012-10-15 2012-10-15 ｓｉＲＮＡ 접합체 및 그 제조방법

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KR20100123214A KR20100123214A (ko) 2010-11-24
KR101224828B1 true KR101224828B1 (ko) 2013-01-22

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KR1020090042297A Active KR101224828B1 (ko) 2009-05-14 2009-05-14 ｓｉＲＮＡ 접합체 및 그 제조방법

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Country Link
US (4) US8779114B2 (cg-RX-API-DMAC10.html)
EP (3) EP2682466B1 (cg-RX-API-DMAC10.html)
JP (3) JP5758381B2 (cg-RX-API-DMAC10.html)
KR (1) KR101224828B1 (cg-RX-API-DMAC10.html)
CN (3) CN103233003B (cg-RX-API-DMAC10.html)
AU (1) AU2010248239B2 (cg-RX-API-DMAC10.html)
BR (1) BRPI1012141B1 (cg-RX-API-DMAC10.html)
CA (2) CA2761749C (cg-RX-API-DMAC10.html)
RU (2) RU2558258C2 (cg-RX-API-DMAC10.html)
WO (1) WO2010131916A2 (cg-RX-API-DMAC10.html)

Cited By (17)

* Cited by examiner, † Cited by third party
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WO2014054927A1 (ko) 2012-10-05 2014-04-10 (주)바이오니아 엠피레귤린 특이적 이중 나선 올리고 rna, 그러한 이중나선 올리고 rna를 포함하는 이중나선 올리고 rna 구조체 및 이를 포함하는 호흡기 질환의 예방 또는 치료용 조성물
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JP2015107115A (ja) 2015-06-11
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AU2010248239B2 (en) 2015-01-22
US20130096288A1 (en) 2013-04-18
US20140350233A1 (en) 2014-11-27
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CA2871888A1 (en) 2010-11-18
CN102439148A (zh) 2012-05-02
US20140350232A1 (en) 2014-11-27
US20120108803A1 (en) 2012-05-03
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