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 CN201210301551.2A priority patent/CN102888404B/zh
Priority to PCT/KR2010/003039 priority patent/WO2010131916A2/ko
Priority to CA2871888A priority patent/CA2871888A1/en
Priority to CA2761749A priority patent/CA2761749C/en
Priority to US13/319,885 priority patent/US8779114B2/en
Priority to AU2010248239A priority patent/AU2010248239B2/en
Priority to JP2012510752A priority patent/JP5758381B2/ja
Priority to RU2011150787/10A priority patent/RU2558258C2/ru
Priority to EP10775118.2A priority patent/EP2463371B1/en
Priority to BRPI1012141A priority patent/BRPI1012141B1/pt
Priority to CN201310147988.XA priority patent/CN103233003B/zh
Priority to EP13185358.2A priority patent/EP2682466B1/en
Priority to CN201080021324.3A priority patent/CN102439148B/zh
Priority to EP13159602.5A priority patent/EP2626427A3/en
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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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
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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
    • A—HUMAN NECESSITIES
    • 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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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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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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    • C12N15/11—DNA or RNA fragments; Modified forms thereof; Non-coding nucleic acids having a biological activity
    • 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
    • B82Y5/00—Nanobiotechnology or nanomedicine, e.g. protein engineering or drug delivery
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    • C12N2310/00—Structure or type of the nucleic acid
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    • C12N2320/51—Methods for regulating/modulating their activity modulating the chemical stability, e.g. nuclease-resistance
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    • Y10—TECHNICAL SUBJECTS COVERED BY FORMER USPC
    • Y10S—TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y10S977/00—Nanotechnology
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  • General Health & Medical Sciences (AREA)
  • Biotechnology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biochemistry (AREA)
  • General Engineering & Computer Science (AREA)
  • Wood Science & Technology (AREA)
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  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Biophysics (AREA)
  • Physics & Mathematics (AREA)
  • Microbiology (AREA)
  • Plant Pathology (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)
  • Medicinal Preparation (AREA)
  • 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
CN201080021324.3A CN102439148B (zh) 2009-05-14 2010-05-13 siRNA缀合物及其制备方法
CA2871888A CA2871888A1 (en) 2009-05-14 2010-05-13 Sirna conjugate and preparation method thereof
CA2761749A CA2761749C (en) 2009-05-14 2010-05-13 Sirna conjugate and preparation method thereof
US13/319,885 US8779114B2 (en) 2009-05-14 2010-05-13 siRNA conjugate and preparation method thereof
AU2010248239A AU2010248239B2 (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
PCT/KR2010/003039 WO2010131916A2 (ko) 2009-05-14 2010-05-13 siRNA 접합체 및 그 제조방법
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
CN201210301551.2A CN102888404B (zh) 2009-05-14 2010-05-13 siRNA缀合物及其制备方法
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
CN201310147988.XA CN103233003B (zh) 2009-05-14 2010-05-13 siRNA缀合物及其制备方法
EP13159602.5A EP2626427A3 (en) 2009-05-14 2010-05-13 Sirna conjugate and preparation method thereof
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

Country Status (10)

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US (4) US8779114B2 (enExample)
EP (3) EP2682466B1 (enExample)
JP (3) JP5758381B2 (enExample)
KR (1) KR101224828B1 (enExample)
CN (3) CN102888404B (enExample)
AU (1) AU2010248239B2 (enExample)
BR (1) BRPI1012141B1 (enExample)
CA (2) CA2761749C (enExample)
RU (2) RU2558258C2 (enExample)
WO (1) WO2010131916A2 (enExample)

Cited By (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
WO2015002511A1 (ko) 2013-07-05 2015-01-08 (주)바이오니아 개선된 고효율 나노입자형 올리고뉴클레오타이드 구조체 및 그의 제조방법
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US20120108803A1 (en) 2012-05-03
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KR20100123214A (ko) 2010-11-24
US8772472B2 (en) 2014-07-08
JP2013230148A (ja) 2013-11-14
US20140350232A1 (en) 2014-11-27
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