SG11201806372UA - Nucleic acid conjugate - Google Patents

Nucleic acid conjugate

Info

Publication number
SG11201806372UA
SG11201806372UA SG11201806372UA SG11201806372UA SG11201806372UA SG 11201806372U A SG11201806372U A SG 11201806372UA SG 11201806372U A SG11201806372U A SG 11201806372UA SG 11201806372U A SG11201806372U A SG 11201806372UA SG 11201806372U A SG11201806372U A SG 11201806372UA
Authority
SG
Singapore
Prior art keywords
nucleic acid
acid conjugate
independently
formula
oligonucleotide
Prior art date
Application number
SG11201806372UA
Inventor
Keiji Uehara
Yasuhiro Suzuki
Hiroto Iwai
Masakazu Homma
Yuichi Fukuda
Tatsuto Kiuchi
Original Assignee
Kyowa Hakko Kirin Co Ltd
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Kyowa Hakko Kirin Co Ltd filed Critical Kyowa Hakko Kirin Co Ltd
Publication of SG11201806372UA publication Critical patent/SG11201806372UA/en

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H21/00Compounds containing two or more mononucleotide units having separate phosphate or polyphosphate groups linked by saccharide radicals of nucleoside groups, e.g. nucleic acids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/70Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7088Compounds having three or more nucleosides or nucleotides
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/70Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7088Compounds having three or more nucleosides or nucleotides
    • A61K31/713Double-stranded nucleic acids or oligonucleotides
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C237/00Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups
    • C07C237/02Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton
    • C07C237/04Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton being acyclic and saturated
    • C07C237/10Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton being acyclic and saturated having the nitrogen atom of at least one of the carboxamide groups bound to an acyclic carbon atom of a hydrocarbon radical substituted by nitrogen atoms not being part of nitro or nitroso groups
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C247/00Compounds containing azido groups
    • C07C247/02Compounds containing azido groups with azido groups bound to acyclic carbon atoms of a carbon skeleton
    • C07C247/04Compounds containing azido groups with azido groups bound to acyclic carbon atoms of a carbon skeleton being saturated
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C271/00Derivatives of carbamic acids, i.e. compounds containing any of the groups, the nitrogen atom not being part of nitro or nitroso groups
    • C07C271/06Esters of carbamic acids
    • C07C271/08Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms
    • C07C271/10Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms
    • C07C271/16Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms to carbon atoms of hydrocarbon radicals substituted by singly-bound oxygen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H15/00Compounds containing hydrocarbon or substituted hydrocarbon radicals directly attached to hetero atoms of saccharide radicals
    • C07H15/02Acyclic radicals, not substituted by cyclic structures
    • C07H15/04Acyclic radicals, not substituted by cyclic structures attached to an oxygen atom of the saccharide radical
    • CCHEMISTRY; METALLURGY
    • C12BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12NMICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
    • C12N15/00Mutation or genetic engineering; DNA or RNA concerning genetic engineering, vectors, e.g. plasmids, or their isolation, preparation or purification; Use of hosts therefor
    • C12N15/09Recombinant DNA-technology
    • C12N15/11DNA or RNA fragments; Modified forms thereof; Non-coding nucleic acids having a biological activity
    • C12N15/113Non-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
    • CCHEMISTRY; METALLURGY
    • C12BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12NMICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
    • C12N2310/00Structure or type of the nucleic acid
    • C12N2310/10Type of nucleic acid
    • C12N2310/14Type of nucleic acid interfering N.A.
    • CCHEMISTRY; METALLURGY
    • C12BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12NMICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
    • C12N2310/00Structure or type of the nucleic acid
    • C12N2310/30Chemical structure
    • C12N2310/35Nature of the modification
    • C12N2310/351Conjugate
    • CCHEMISTRY; METALLURGY
    • C12BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12NMICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
    • C12N2320/00Applications; Uses
    • C12N2320/30Special therapeutic applications
    • C12N2320/32Special delivery means, e.g. tissue-specific

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Molecular Biology (AREA)
  • Genetics & Genomics (AREA)
  • General Health & Medical Sciences (AREA)
  • Biochemistry (AREA)
  • Biotechnology (AREA)
  • Biomedical Technology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Zoology (AREA)
  • Wood Science & Technology (AREA)
  • General Engineering & Computer Science (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Physics & Mathematics (AREA)
  • Biophysics (AREA)
  • Plant Pathology (AREA)
  • Microbiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Crystallography & Structural Chemistry (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Saccharide Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicinal Preparation (AREA)

Abstract

NUCLEIC ACID CONJUGATE The present invention relates to a nucleic acid conjugate represented by the following formula 1: Formula 1: L1-S1 S3-X /- L2-S2 wherein X is an oligonucleotide, Ll and L2 are each independently sugar ligand, and Sl, S2 and S3 are each independently a linker. [No suitable figure]
SG11201806372UA 2016-01-29 2017-01-30 Nucleic acid conjugate SG11201806372UA (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
JP2016016707 2016-01-29
PCT/JP2017/003249 WO2017131236A1 (en) 2016-01-29 2017-01-30 Nucleic acid complex

Publications (1)

Publication Number Publication Date
SG11201806372UA true SG11201806372UA (en) 2018-08-30

Family

ID=59398306

Family Applications (1)

Application Number Title Priority Date Filing Date
SG11201806372UA SG11201806372UA (en) 2016-01-29 2017-01-30 Nucleic acid conjugate

Country Status (11)

Country Link
US (1) US10745700B2 (en)
EP (1) EP3409780B1 (en)
JP (1) JP6853193B2 (en)
KR (1) KR20180103166A (en)
CN (1) CN108699558B (en)
AU (1) AU2017213404A1 (en)
CA (1) CA3012967A1 (en)
ES (1) ES2858090T3 (en)
SG (1) SG11201806372UA (en)
TW (1) TWI733751B (en)
WO (1) WO2017131236A1 (en)

Families Citing this family (21)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR102520362B1 (en) * 2016-06-30 2023-04-10 쿄와 기린 가부시키가이샤 A nucleic acid complex in which a sugar chain ligand is coupled to an oligonucleotide through a linker
US11963974B2 (en) 2017-03-10 2024-04-23 National Center For Child Health And Development Antisense oligonucleotide and composition for prevention or treatment of glycogen storage disease type Ia
US20210108207A1 (en) 2017-04-28 2021-04-15 Kyowa Kirin Co., Ltd. Oligonucleotide derivative or salt thereof
TW201909925A (en) * 2017-08-02 2019-03-16 日商協和醱酵麒麟有限公司 Nucleic acid complex
TW201920668A (en) * 2017-08-02 2019-06-01 日商協和醱酵麒麟有限公司 Nucleic acid complex
CN110997917B (en) * 2017-12-01 2024-04-09 苏州瑞博生物技术股份有限公司 Nucleic acid, composition containing nucleic acid, conjugate, preparation method and application
EP3718572B1 (en) 2017-12-01 2024-07-31 Suzhou Ribo Life Science Co., Ltd. Nucleic acid, composition and conjugate containing nucleic acid, preparation method and use
AU2018377716B2 (en) 2017-12-01 2024-12-19 Suzhou Ribo Life Science Co., Ltd Nucleic acid, composition and conjugate comprising the same, and preparation method and use thereof
KR102398295B1 (en) 2018-03-09 2022-05-17 다이이찌 산쿄 가부시키가이샤 Glycogen disease type Ia treatment
BR112020026073A2 (en) * 2018-06-21 2021-03-23 F. Hoffmann-La Roche Ag method to provide a binding pair, liquid composition, use of a composition and kit to perform a heterogeneous immunoassay
EP3842534A4 (en) 2018-08-21 2022-07-06 Suzhou Ribo Life Science Co., Ltd. Nucleic acid, pharmaceutical composition and conjugate containing nucleic acid, and use thereof
EP3862024A4 (en) * 2018-09-30 2022-08-17 Suzhou Ribo Life Science Co., Ltd. Sirna conjugate, preparation method therefor and use thereof
EP3873486A4 (en) * 2018-11-02 2022-10-19 Arbutus Biopharma Corporation Bivalent targeted conjugates
EP3888663A1 (en) * 2018-11-30 2021-10-06 Kyowa Kirin Co., Ltd. Nucleic acid complex
CN114616332B (en) * 2019-09-10 2024-09-20 第一三共株式会社 GalNAc-oligonucleotide conjugate for delivery to liver and preparation method thereof
WO2021055641A1 (en) * 2019-09-17 2021-03-25 Purdue Research Foundation Fibroblast activation protein (fap)-targeted imaging and therapy of cancers and other fibrotic and inflammatory diseases
CN118591552A (en) * 2022-01-30 2024-09-03 成都凌泰氪生物技术有限公司 Ligand, preparation method and application thereof
WO2023176863A1 (en) 2022-03-16 2023-09-21 第一三共株式会社 Chemically-modified oligonucleotide having rnai activity
WO2023176862A1 (en) 2022-03-16 2023-09-21 第一三共株式会社 siRNA FOR SUPPRESSING EXPRESSION OF TRANSFERRIN RECEPTOR-2
WO2023187760A1 (en) * 2022-04-01 2023-10-05 Genevant Sciences Gmbh Mannose-targeted compositions
CN116444589B (en) * 2023-06-15 2023-09-19 北京悦康科创医药科技股份有限公司 GalNAc compounds, their thio-oligonucleotide conjugates and coupling methods

Family Cites Families (24)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6469158B1 (en) 1992-05-14 2002-10-22 Ribozyme Pharmaceuticals, Incorporated Synthesis, deprotection, analysis and purification of RNA and ribozymes
US5804683A (en) 1992-05-14 1998-09-08 Ribozyme Pharmaceuticals, Inc. Deprotection of RNA with alkylamine
US5977343A (en) 1992-05-14 1999-11-02 Ribozyme Pharmaceuticals, Inc. Synthesis, deprotection, analysis and purification of RNA and ribozymes
DK0748382T3 (en) 1993-09-02 2003-02-17 Ribozyme Pharm Inc Enzymatic nucleic acid containing non-nucleotide
US5889136A (en) 1995-06-09 1999-03-30 The Regents Of The University Of Colorado Orthoester protecting groups in RNA synthesis
JP2000501414A (en) * 1995-11-22 2000-02-08 ザ・ジョンズ・ホプキンス・ユニバーシティー Ligand enhances cellular uptake of biomolecules
US5998203A (en) 1996-04-16 1999-12-07 Ribozyme Pharmaceuticals, Inc. Enzymatic nucleic acids containing 5'-and/or 3'-cap structures
US6111086A (en) 1998-02-27 2000-08-29 Scaringe; Stephen A. Orthoester protecting groups
WO2005113571A2 (en) 2004-05-13 2005-12-01 The University Of North Carolina At Chapel Hill Methods for the delivery of oligomeric compounds
CA3043911A1 (en) 2007-12-04 2009-07-02 Arbutus Biopharma Corporation Targeting lipids
ES2370638B1 (en) 2010-03-05 2012-11-16 Universidad De Castilla La Mancha DENDRIMEROS AS NON-VIRAL VEHICLES FOR GENE THERAPY
CN103492568B (en) * 2010-12-17 2017-04-12 箭头研究公司 Galactose cluster-pharmacokinetic modulator targeting moiety for siRNA
CN103649311A (en) * 2011-06-03 2014-03-19 国立大学法人北海道大学 Oligonucleotide derivative, oligonucleotide derivative-containing pharmaceutical composition for treatment and pharmaceutical composition for diagnosis, and oligonucleotide derivative for regulation of miRNA function
CN108186667B (en) 2011-11-18 2021-07-20 阿尔尼拉姆医药品有限公司 RNAi agents, compositions and methods of use thereof for Treating Transthyretin (TTR) -related diseases
TW201808342A (en) 2012-05-02 2018-03-16 喜納製藥公司 Novel tetraGALNAC containing conjugates and methods for delivery of oligonucleotides
EP3919620A1 (en) 2012-05-02 2021-12-08 Sirna Therapeutics, Inc. Short interfering nucleic acid (sina) compositions
EA201492117A1 (en) 2012-05-16 2015-04-30 Рана Терапьютикс, Инк. COMPOSITIONS AND METHODS FOR MODULATING THE EXPRESSION OF BDNF
EP2850184A4 (en) 2012-05-16 2016-01-27 Rana Therapeutics Inc Compositions and methods for modulating gene expression
JP6452614B2 (en) * 2012-11-15 2019-01-16 ロシュ イノベーション センター コペンハーゲン エーエス Oligonucleotide conjugate
CN105392488B (en) 2013-05-01 2021-04-30 Ionis制药公司 Compositions and methods for modulating apolipoprotein C-III expression
CA2917161C (en) 2013-07-11 2023-12-12 Alnylam Pharmaceuticals, Inc. Oligonucleotide-ligand conjugates and process for their preparation
US9943604B2 (en) 2013-09-20 2018-04-17 Ionis Pharmaceuticals, Inc. Targeted therapeutic nucleosides and their use
JP6482475B2 (en) 2014-01-07 2019-03-13 レナセラピューティクス株式会社 Double stranded oligonucleotides comprising antisense oligonucleotides and sugar derivatives
KR102520362B1 (en) * 2016-06-30 2023-04-10 쿄와 기린 가부시키가이샤 A nucleic acid complex in which a sugar chain ligand is coupled to an oligonucleotide through a linker

Also Published As

Publication number Publication date
US20190055558A1 (en) 2019-02-21
EP3409780A1 (en) 2018-12-05
JP6853193B2 (en) 2021-03-31
KR20180103166A (en) 2018-09-18
CA3012967A1 (en) 2017-08-03
CN108699558A (en) 2018-10-23
AU2017213404A1 (en) 2018-09-20
TW201730200A (en) 2017-09-01
ES2858090T3 (en) 2021-09-29
US10745700B2 (en) 2020-08-18
EP3409780B1 (en) 2021-01-20
CN108699558B (en) 2021-12-07
JPWO2017131236A1 (en) 2018-11-22
WO2017131236A1 (en) 2017-08-03
TWI733751B (en) 2021-07-21
EP3409780A4 (en) 2019-09-25

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