JP7675716B2 - 3’-rnaオリゴヌクレオチドの合成 - Google Patents
3’-rnaオリゴヌクレオチドの合成 Download PDFInfo
- Publication number
- JP7675716B2 JP7675716B2 JP2022530757A JP2022530757A JP7675716B2 JP 7675716 B2 JP7675716 B2 JP 7675716B2 JP 2022530757 A JP2022530757 A JP 2022530757A JP 2022530757 A JP2022530757 A JP 2022530757A JP 7675716 B2 JP7675716 B2 JP 7675716B2
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- base
- uracil
- nucleoside
- alkyl
- group
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/7028—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages
- A61K31/7034—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin
- A61K31/704—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin attached to a condensed carbocyclic ring system, e.g. sennosides, thiocolchicosides, escin, daunorubicin
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- 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
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/24—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing atoms other than carbon, hydrogen, oxygen, halogen, nitrogen or sulfur, e.g. cyclomethicone or phospholipids
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- 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
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/26—Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/10—Dispersions; Emulsions
- A61K9/127—Synthetic bilayered vehicles, e.g. liposomes or liposomes with cholesterol as the only non-phosphatidyl surfactant
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
- C07H1/00—Processes for the preparation of sugar derivatives
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
- C07H19/00—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
- C07H19/02—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
- C07H19/04—Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
- C07H19/06—Pyrimidine radicals
- C07H19/067—Pyrimidine radicals with ribosyl as the saccharide radical
-
- 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
-
- 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
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
- C07H23/00—Compounds containing boron, silicon or a metal, e.g. chelates or vitamin B12
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- C—CHEMISTRY; METALLURGY
- C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
- C12N—MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
- C12N15/00—Mutation or genetic engineering; DNA or RNA concerning genetic engineering, vectors, e.g. plasmids, or their isolation, preparation or purification; Use of hosts therefor
- C12N15/09—Recombinant DNA-technology
- C12N15/11—DNA or RNA fragments; Modified forms thereof; Non-coding nucleic acids having a biological activity
- C12N15/111—General methods applicable to biologically active non-coding nucleic acids
-
- C—CHEMISTRY; METALLURGY
- C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
- C12N—MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
- C12N15/00—Mutation or genetic engineering; DNA or RNA concerning genetic engineering, vectors, e.g. plasmids, or their isolation, preparation or purification; Use of hosts therefor
- C12N15/09—Recombinant DNA-technology
- 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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- C—CHEMISTRY; METALLURGY
- C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
- C12N—MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
- C12N2310/00—Structure or type of the nucleic acid
- C12N2310/10—Type of nucleic acid
- C12N2310/14—Type of nucleic acid interfering nucleic acids [NA]
-
- C—CHEMISTRY; METALLURGY
- C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
- C12N—MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
- C12N2310/00—Structure or type of the nucleic acid
- C12N2310/30—Chemical structure
- C12N2310/31—Chemical structure of the backbone
- C12N2310/319—Chemical structure of the backbone linked by 2'-5' linkages, i.e. having a free 3'-position
-
- C—CHEMISTRY; METALLURGY
- C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
- C12N—MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
- C12N2330/00—Production
- C12N2330/30—Production chemically synthesised
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- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
- Y02P20/00—Technologies relating to chemical industry
- Y02P20/50—Improvements relating to the production of bulk chemicals
- Y02P20/55—Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Engineering & Computer Science (AREA)
- Organic Chemistry (AREA)
- Molecular Biology (AREA)
- General Health & Medical Sciences (AREA)
- Genetics & Genomics (AREA)
- Biochemistry (AREA)
- Biotechnology (AREA)
- Biomedical Technology (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Epidemiology (AREA)
- Wood Science & Technology (AREA)
- General Engineering & Computer Science (AREA)
- Zoology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Biophysics (AREA)
- Oil, Petroleum & Natural Gas (AREA)
- Microbiology (AREA)
- Plant Pathology (AREA)
- Physics & Mathematics (AREA)
- Dispersion Chemistry (AREA)
- Dermatology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Saccharide Compounds (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2025074104A JP2025105841A (ja) | 2019-11-27 | 2025-04-28 | 3’-rnaオリゴヌクレオチドの合成 |
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201962941153P | 2019-11-27 | 2019-11-27 | |
| US62/941,153 | 2019-11-27 | ||
| PCT/US2020/061755 WO2021108291A1 (en) | 2019-11-27 | 2020-11-23 | Synthesis of 3'-rna oligonucleotides |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2025074104A Division JP2025105841A (ja) | 2019-11-27 | 2025-04-28 | 3’-rnaオリゴヌクレオチドの合成 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2023503985A JP2023503985A (ja) | 2023-02-01 |
| JP2023503985A5 JP2023503985A5 (https=) | 2023-10-03 |
| JP7675716B2 true JP7675716B2 (ja) | 2025-05-13 |
Family
ID=76129612
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2022530757A Active JP7675716B2 (ja) | 2019-11-27 | 2020-11-23 | 3’-rnaオリゴヌクレオチドの合成 |
| JP2025074104A Pending JP2025105841A (ja) | 2019-11-27 | 2025-04-28 | 3’-rnaオリゴヌクレオチドの合成 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2025074104A Pending JP2025105841A (ja) | 2019-11-27 | 2025-04-28 | 3’-rnaオリゴヌクレオチドの合成 |
Country Status (10)
| Country | Link |
|---|---|
| US (1) | US20250325575A2 (https=) |
| EP (1) | EP4065715A4 (https=) |
| JP (2) | JP7675716B2 (https=) |
| KR (1) | KR20220107246A (https=) |
| CN (2) | CN118791543A (https=) |
| AU (1) | AU2020391116A1 (https=) |
| CA (1) | CA3162717A1 (https=) |
| IL (2) | IL293327B2 (https=) |
| MX (1) | MX2022006221A (https=) |
| WO (1) | WO2021108291A1 (https=) |
Families Citing this family (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2026085164A2 (en) | 2024-10-16 | 2026-04-23 | Alnylam Pharmaceuticals, Inc. | Snca irna formulations and methods of use thereof |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2012024776A1 (en) | 2010-08-23 | 2012-03-01 | The Royal Institution For The Advancement Of Learning/Mcgill University | Block synthesis of oligoribonucleotides |
| US20130261026A1 (en) | 2001-03-14 | 2013-10-03 | The Regents Of The University Of Michigan | Linkers and co-coupling agents for optimization of oligonucleotide synthesis and purification on solid supports |
Family Cites Families (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4924624A (en) * | 1987-10-22 | 1990-05-15 | Temple University-Of The Commonwealth System Of Higher Education | 2,',5'-phosphorothioate oligoadenylates and plant antiviral uses thereof |
| ATE299509T1 (de) * | 1992-07-23 | 2005-07-15 | Isis Pharmaceuticals Inc | Neue 2'-o-alkyl-nukleoside und -phosphoramidite, verfahren zu ihrer herstellung und ihre verwendungen |
| US6649750B1 (en) * | 2000-01-05 | 2003-11-18 | Isis Pharmaceuticals, Inc. | Process for the preparation of oligonucleotide compounds |
| WO2002018405A2 (en) * | 2000-09-01 | 2002-03-07 | Ribozyme Pharmaceuticals, Incorporated | Methods for synthesizing nucleosides, nucleoside derivatives and non-nucleoside derivatives |
| WO2003039523A2 (en) * | 2001-11-05 | 2003-05-15 | Exiqon A/S | OLIGONUCLEOTIDES MODIFIED WITH NOVEL α-L-RNA ANALOGUES |
| CN100484949C (zh) * | 2005-07-18 | 2009-05-06 | 张必良 | 用于rna寡核苷酸合成中的核苷亚磷酰胺及其合成方法 |
| US8911948B2 (en) * | 2008-04-30 | 2014-12-16 | Integrated Dna Technologies, Inc. | RNase H-based assays utilizing modified RNA monomers |
| US8309707B2 (en) * | 2008-09-06 | 2012-11-13 | Chemgenes Corporation | RNA synthesis-phosphoramidites for synthetic RNA in the reverse direction, and application in convenient introduction of ligands, chromophores and modifications of synthetic RNA at the 3′-end |
| US8541569B2 (en) * | 2008-09-06 | 2013-09-24 | Chemgenes Corporation | Phosphoramidites for synthetic RNA in the reverse direction, efficient RNA synthesis and convenient introduction of 3'-end ligands, chromophores and modifications of synthetic RNA |
| CA2900238A1 (en) * | 2013-02-22 | 2014-08-28 | Sirna Therapeutics, Inc. | Short interfering nucleic acid (sina) molecules containing a 2' internucleoside linkage |
| EP3154996B1 (en) * | 2014-06-10 | 2020-03-11 | Agilent Technologies, Inc. | Protecting groups for "z nucleotide" and methods thereof |
| EP3455232B1 (en) * | 2016-05-12 | 2020-05-06 | Roche Innovation Center Copenhagen A/S | Enhanced coupling of stereodefined oxazaphospholidine phosphoramidite monomers to nucleoside or oligonucleotide |
| WO2018019748A1 (en) * | 2016-07-27 | 2018-02-01 | F. Hoffmann-La Roche Ag | 5's-lna nucleotides and oligonucleotides |
-
2020
- 2020-11-22 IL IL293327A patent/IL293327B2/en unknown
- 2020-11-23 MX MX2022006221A patent/MX2022006221A/es unknown
- 2020-11-23 CN CN202410795160.3A patent/CN118791543A/zh active Pending
- 2020-11-23 AU AU2020391116A patent/AU2020391116A1/en active Pending
- 2020-11-23 WO PCT/US2020/061755 patent/WO2021108291A1/en not_active Ceased
- 2020-11-23 CA CA3162717A patent/CA3162717A1/en active Pending
- 2020-11-23 CN CN202080094679.9A patent/CN115038790B/zh active Active
- 2020-11-23 KR KR1020227021711A patent/KR20220107246A/ko active Pending
- 2020-11-23 JP JP2022530757A patent/JP7675716B2/ja active Active
- 2020-11-23 EP EP20892935.6A patent/EP4065715A4/en active Pending
- 2020-11-23 US US17/779,706 patent/US20250325575A2/en active Pending
-
2025
- 2025-04-28 JP JP2025074104A patent/JP2025105841A/ja active Pending
- 2025-10-23 IL IL324170A patent/IL324170A/en unknown
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20130261026A1 (en) | 2001-03-14 | 2013-10-03 | The Regents Of The University Of Michigan | Linkers and co-coupling agents for optimization of oligonucleotide synthesis and purification on solid supports |
| WO2012024776A1 (en) | 2010-08-23 | 2012-03-01 | The Royal Institution For The Advancement Of Learning/Mcgill University | Block synthesis of oligoribonucleotides |
Non-Patent Citations (6)
| Title |
|---|
| Bioconjugate Chemistry,2003年,Vol. 14,pp. 690-696 |
| GREENE, Theodora W. et al.,Protective Groups in Organic Synthesis, Third Edition,1999年04月09日,pp. 123-125 |
| Helvetica Chimica Acta,2003年,Vol. 86,pp. 2726-2740 |
| Journal of Sciences, Islamic Republic of Iran,1990年,Vol. 1,pp. 355-360 |
| The Journal of Organic Chemistry,1990年,Vol. 55,pp. 4717-4724 |
| Triisopropylsilyl Chloride,Encyclopedia of Reagents for Organic Synthesis,2001年,pp. 1-5,10.1002/047084289X.rt262 |
Also Published As
| Publication number | Publication date |
|---|---|
| WO2021108291A1 (en) | 2021-06-03 |
| IL293327B2 (en) | 2026-04-01 |
| EP4065715A1 (en) | 2022-10-05 |
| CA3162717A1 (en) | 2021-06-03 |
| IL324170A (en) | 2025-12-01 |
| US20230021879A1 (en) | 2023-01-26 |
| EP4065715A4 (en) | 2024-04-10 |
| CN115038790B (zh) | 2024-06-21 |
| IL293327B1 (en) | 2025-12-01 |
| MX2022006221A (es) | 2022-08-10 |
| CN118791543A (zh) | 2024-10-18 |
| IL293327A (en) | 2022-07-01 |
| JP2023503985A (ja) | 2023-02-01 |
| AU2020391116A1 (en) | 2022-07-14 |
| JP2025105841A (ja) | 2025-07-10 |
| US20250325575A2 (en) | 2025-10-23 |
| KR20220107246A (ko) | 2022-08-02 |
| CN115038790A (zh) | 2022-09-09 |
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