AU2018350693B2 - Nucleic acid molecule for reduction of PAPD5 and PAPD7 mRNA for treating hepatitis B infection - Google Patents

Nucleic acid molecule for reduction of PAPD5 and PAPD7 mRNA for treating hepatitis B infection Download PDF

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AU2018350693B2
AU2018350693B2 AU2018350693A AU2018350693A AU2018350693B2 AU 2018350693 B2 AU2018350693 B2 AU 2018350693B2 AU 2018350693 A AU2018350693 A AU 2018350693A AU 2018350693 A AU2018350693 A AU 2018350693A AU 2018350693 B2 AU2018350693 B2 AU 2018350693B2
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oligonucleotide
nucleosides
antisense oligonucleotide
conjugate
nucleic acid
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AU2018350693A1 (en
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Susanne KAMMLER
Anaïs LOPEZ
Henrik Mueller
Søren OTTOSEN
Lykke PEDERSEN
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F Hoffmann La Roche AG
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F Hoffmann La Roche AG
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    • 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
    • C12N15/1131—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 against viruses
    • 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
    • A61K31/7088—Compounds having three or more nucleosides or nucleotides
    • A61K31/7115—Nucleic acids or oligonucleotides having modified bases, i.e. other than adenine, guanine, cytosine, uracil or thymine
    • 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
    • A61K31/7088—Compounds having three or more nucleosides or nucleotides
    • 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
    • A61K31/7088—Compounds having three or more nucleosides or nucleotides
    • A61K31/7105—Natural ribonucleic acids, i.e. containing only riboses attached to adenine, guanine, cytosine or uracil and having 3'-5' phosphodiester links
    • 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
    • A61K31/7088—Compounds having three or more nucleosides or nucleotides
    • A61K31/712—Nucleic acids or oligonucleotides having modified sugars, i.e. other than ribose or 2'-deoxyribose
    • 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
    • A61K31/7088—Compounds having three or more nucleosides or nucleotides
    • A61K31/7125—Nucleic acids or oligonucleotides having modified internucleoside linkage, i.e. other than 3'-5' phosphodiesters
    • 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
    • A61K31/7088—Compounds having three or more nucleosides or nucleotides
    • A61K31/713—Double-stranded nucleic acids or oligonucleotides
    • 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
    • A61K47/50—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
    • A61K47/54—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 compound
    • A61K47/549—Sugars, nucleosides, nucleotides or nucleic acids
    • 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
    • A61K47/50—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
    • A61K47/62—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 a protein, peptide or polyamino acid
    • A61K47/64—Drug-peptide, drug-protein or drug-polyamino acid conjugates, i.e. the modifying agent being a peptide, protein or polyamino acid which is covalently bonded or complexed to a therapeutically active agent
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • 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
    • A61P31/12—Antivirals
    • A61P31/20—Antivirals for DNA viruses
    • 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
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    • 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
    • C—CHEMISTRY; METALLURGY
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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
    • 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
    • C12N15/1137—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 against enzymes
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    • C12N2310/00—Structure or type of the nucleic acid
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    • C12N2310/11—Antisense
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    • 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
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    • C12N2310/00—Structure or type of the nucleic acid
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    • C12N2310/31—Chemical structure of the backbone
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    • C12N2310/00—Structure or type of the nucleic acid
    • C12N2310/30—Chemical structure
    • C12N2310/32—Chemical structure of the sugar
    • C12N2310/323—Chemical structure of the sugar modified ring structure
    • C12N2310/3231—Chemical structure of the sugar modified ring structure having an additional ring, e.g. LNA, ENA
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    • C12N2310/30—Chemical structure
    • C12N2310/34—Spatial arrangement of the modifications
    • C12N2310/341—Gapmers, i.e. of the type ===---===
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AU2018350693A 2017-10-16 2018-10-16 Nucleic acid molecule for reduction of PAPD5 and PAPD7 mRNA for treating hepatitis B infection Active AU2018350693B2 (en)

Priority Applications (2)

Application Number Priority Date Filing Date Title
AU2021203300A AU2021203300B2 (en) 2017-10-16 2021-05-21 Nucleic acid molecule for reduction of PAPD5 and PAPD7 mRNA for treating hepatitis B infection
AU2024201873A AU2024201873A1 (en) 2017-10-16 2024-03-22 Nucleic acid molecule for reduction of PAPD5 and PAPD7 mRNA for treating hepatitis B infection

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
EP17196554 2017-10-16
EP17196554.4 2017-10-16
EP17208056.6 2017-12-18
EP17208056 2017-12-18
PCT/EP2018/078136 WO2019076842A1 (en) 2017-10-16 2018-10-16 NUCLEIC ACID MOLECULE FOR THE REDUCTION OF PAPD5 AND PAPD7 MRNA FOR THE TREATMENT OF HEPATITIS B INFECTION

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AU2021203300A Division AU2021203300B2 (en) 2017-10-16 2021-05-21 Nucleic acid molecule for reduction of PAPD5 and PAPD7 mRNA for treating hepatitis B infection

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AU2018350693A1 AU2018350693A1 (en) 2020-03-12
AU2018350693B2 true AU2018350693B2 (en) 2021-03-04

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AU2018350693A Active AU2018350693B2 (en) 2017-10-16 2018-10-16 Nucleic acid molecule for reduction of PAPD5 and PAPD7 mRNA for treating hepatitis B infection
AU2021203300A Active AU2021203300B2 (en) 2017-10-16 2021-05-21 Nucleic acid molecule for reduction of PAPD5 and PAPD7 mRNA for treating hepatitis B infection
AU2024201873A Pending AU2024201873A1 (en) 2017-10-16 2024-03-22 Nucleic acid molecule for reduction of PAPD5 and PAPD7 mRNA for treating hepatitis B infection

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AU2024201873A Pending AU2024201873A1 (en) 2017-10-16 2024-03-22 Nucleic acid molecule for reduction of PAPD5 and PAPD7 mRNA for treating hepatitis B infection

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US (4) US10953034B2 (https=)
EP (1) EP3645723A1 (https=)
JP (4) JP2021500013A (https=)
KR (5) KR102769100B1 (https=)
CN (2) CN111511914B (https=)
AU (3) AU2018350693B2 (https=)
BR (2) BR122020018622A2 (https=)
CA (1) CA3072314A1 (https=)
CL (1) CL2020000945A1 (https=)
CR (2) CR20200205A (https=)
IL (2) IL272566B2 (https=)
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MX (1) MX2020003464A (https=)
PE (1) PE20200868A1 (https=)
PH (1) PH12020550436A1 (https=)
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SG (1) SG11202003461TA (https=)
TW (3) TWI762732B (https=)
UA (1) UA126931C2 (https=)
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EP4219767A1 (en) 2016-06-17 2023-08-02 F. Hoffmann-La Roche AG Papd5 and papd7 inhibitors for treating a hepatitis b infection
CN111511914B (zh) 2017-10-16 2023-11-17 豪夫迈·罗氏有限公司 减少PAPD5和PAPD7 mRNA的核酸分子用于治疗乙型肝炎感染
WO2019157531A1 (en) * 2018-02-12 2019-08-15 Ionis Pharmaceuticals, Inc. Modified compounds and uses thereof
PE20210346A1 (es) 2018-07-03 2021-02-25 Hoffmann La Roche Oligonucleotidos para modular la expresion de tau
CN112534055A (zh) 2018-07-13 2021-03-19 豪夫迈·罗氏有限公司 用于调节rtel1表达的寡核苷酸
US20220220483A1 (en) * 2019-05-30 2022-07-14 Seoul National University R&Db Foundation Method for inhibiting infection and activation of virus
SG11202112741XA (en) * 2019-05-31 2021-12-30 Aligos Therapeutics Inc Modified gapmer oligonucleotides and methods of use
EP4081217A1 (en) * 2019-12-24 2022-11-02 F. Hoffmann-La Roche AG Pharmaceutical combination of antiviral agents targeting hbv and/or an immune modulator for treatment of hbv
WO2022109129A1 (en) * 2020-11-20 2022-05-27 Aligos Therapeutics, Inc. Conjugates of s-antigen transport inhibiting oligonucleotide polymers having enhanced liver targeting
WO2025199466A1 (en) 2024-03-22 2025-09-25 Purdue Research Foundation Liver-specific asialoglycoprotein receptor targeting ligands, conjugates comprising same, and related compositions and methods of use

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WO2015173208A2 (en) * 2014-05-15 2015-11-19 F. Hoffmann-La Roche Ag Oligomers and oligomer conjugates
WO2016079181A1 (en) * 2014-11-19 2016-05-26 Roche Innovation Center Copenhagen A/S Lna gapmer oligonucleotides comprising chiral phosphorothioate linkages
WO2016127002A1 (en) * 2015-02-04 2016-08-11 Bristol-Myers Squibb Company Lna oligonucleotides with alternating flanks
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