HRP20210244T1 - Moduliranje eksprimiranja virusa hepatitisa b (hbv) - Google Patents

Moduliranje eksprimiranja virusa hepatitisa b (hbv) Download PDF

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HRP20210244T1
HRP20210244T1 HRP20210244TT HRP20210244T HRP20210244T1 HR P20210244 T1 HRP20210244 T1 HR P20210244T1 HR P20210244T T HRP20210244T T HR P20210244TT HR P20210244 T HRP20210244 T HR P20210244T HR P20210244 T1 HRP20210244 T1 HR P20210244T1
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compound
liver
segment
disease
modified oligonucleotide
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HRP20210244TT
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Eric E. Swayze
Susan M. Freier
Michael L. Mccaleb
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Glaxo Group Limited
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Application filed by Glaxo Group Limited filed Critical Glaxo Group Limited
Publication of HRP20210244T1 publication Critical patent/HRP20210244T1/hr

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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
    • A61K31/7088—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
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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
    • 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
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • 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
    • A61P31/14—Antivirals for RNA viruses
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • 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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    • C12N2310/00—Structure or type of the nucleic acid
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    • C12N2310/00—Structure or type of the nucleic acid
    • C12N2310/30—Chemical structure
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    • C12N2310/00—Structure or type of the nucleic acid
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    • C—CHEMISTRY; METALLURGY
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    • C12N2310/00—Structure or type of the nucleic acid
    • C12N2310/30—Chemical structure
    • C12N2310/32—Chemical structure of the sugar
    • C12N2310/321—2'-O-R Modification
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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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    • C12N2310/00—Structure or type of the nucleic acid
    • C12N2310/30—Chemical structure
    • C12N2310/33—Chemical structure of the base
    • C12N2310/334—Modified C
    • C12N2310/3341—5-Methylcytosine
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    • C12N2310/00—Structure or type of the nucleic acid
    • C12N2310/30—Chemical structure
    • C12N2310/34—Spatial arrangement of the modifications
    • C12N2310/341—Gapmers, i.e. of the type ===---===
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    • C12N2310/30—Chemical structure
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    • C12N2310/30—Chemical structure
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    • C12N2310/346—Spatial arrangement of the modifications having a combination of backbone and sugar modifications
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    • C12N2320/30—Special therapeutic applications

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Claims (6)

1. Spoj, naznačen time što sadrži jednolančani modificirani oligonukleotid, namijenjen upotrebi u liječenju bolesti, poremećaja ili stanja povezanog s HBV kod subjekta, gdje je bolest, poremećaj ili stanje žutica, upala jetre, fibroza jetre, upala, ciroza jetre, zatajenje jetre, rak jetre, difuzna hepatocelularna upalna bolest, hemofagocitni sindrom, serumski hepatitis, viremija HBV, ili presađivanje povezano s bolešću jetre, gdje se jednolančani modificirani oligonukleotid sastoji od 20 spojenih nukleozida koji imaju slijed nukleobaza sa SEQ ID NO: 226 i sadrži: razmačni segment, koji se sastoji od deset spojenih dezoksinukleozida; 5′ bočni segment, koji se sastoji od 5 spojenih nukleozida; i 3′ bočni segment, koji se sastoji od 5 spojenih nukleozida; gdje je razmačni segment smješten između 5′ bočnog segmenta i 3′ bočnog segmenta, gdje svaki nukleozid svakog bočnog segmenta sadrži 2′-O-metoksietilirani šećer, gdje je svaka internukleozidna veza fosforotioatna veza, te gdje je svaki citozin 5-metilcitozin.
2. Spoj namijenjen upotrebi u skladu s patentnim zahtjevom 1, naznačen time što se spoj sastoji od jednolančanog modificiranog oligonukleotida.
3. Spoj namijenjen upotrebi u skladu s patentnim zahtjevom 1, naznačen time što je spoj konjugirani protusmisleni spoj.
4. Pripravak namijenjen upotrebi u liječenju bolesti, poremećaja ili stanja povezanog s HBV kod subjekta, naznačen time što je bolest, poremećaj ili stanje žutica, upala jetre, fibroza jetre, upala, ciroza jetre, zatajenje jetre, rak jetre, difuzna hepatocelularna upalna bolest, hemofagocitni sindrom, serumski hepatitis, viremija HBV, ili presađivanje povezano s bolešću jetre, gdje pripravak sadrži spoj, ili njegovu sol, i farmaceutski prihvatljivi nosač ili razrjeđivač, gdje spoj sadrži jednolančani modificirani oligonukleotid, gdje se jednolančani modificirani oligonukleotid sastoji od 20 spojenih nukleozida koji imaju slijed nukleobaza sa SEQ ID NO: 226 i sadrži: razmačni segment, koji se sastoji od deset spojenih dezoksinukleozida; 5′ bočni segment, koji se sastoji od 5 spojenih nukleozida; i 3′ bočni segment, koji se sastoji od 5 spojenih nukleozida; gdje je razmačni segment smješten između 5′ bočnog segmenta i 3′ bočnog segmenta, gdje svaki nukleozid svakog bočnog segmenta sadrži 2′-O-metoksietilirani šećer, gdje je svaka internukleozidna veza fosforotioatna veza, te gdje je svaki citozin 5-metilcitozin.
5. Pripravak namijenjen upotrebi u skladu s patentnim zahtjevom 4, naznačen time što se spoj sastoji od jednolančanog modificiranog oligonukleotida.
6. Pripravak namijenjen upotrebi u skladu s patentnim zahtjevom 4, naznačen time što je spoj konjugirani protusmisleni spoj.
HRP20210244TT 2011-04-21 2021-02-11 Moduliranje eksprimiranja virusa hepatitisa b (hbv) HRP20210244T1 (hr)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201161478040P 2011-04-21 2011-04-21
US201161478038P 2011-04-21 2011-04-21
US201261596692P 2012-02-08 2012-02-08
US201261596690P 2012-02-08 2012-02-08
EP19155538.2A EP3505528B1 (en) 2011-04-21 2012-04-20 Modulation of hepatitis b virus (hbv) expression

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HRP20210244T1 true HRP20210244T1 (hr) 2021-04-30

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HRP20210244TT HRP20210244T1 (hr) 2011-04-21 2021-02-11 Moduliranje eksprimiranja virusa hepatitisa b (hbv)

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US (7) US8642752B2 (hr)
EP (4) EP3505528B1 (hr)
JP (3) JP6042871B2 (hr)
KR (3) KR102247463B1 (hr)
CN (3) CN111172162A (hr)
AU (1) AU2012245243B2 (hr)
CA (1) CA2833766C (hr)
CL (1) CL2013003053A1 (hr)
CO (1) CO6862103A2 (hr)
CR (2) CR20190207A (hr)
CY (1) CY1124327T1 (hr)
DK (1) DK3505528T3 (hr)
DO (1) DOP2013000246A (hr)
EA (1) EA029137B1 (hr)
ES (1) ES2856266T3 (hr)
HR (1) HRP20210244T1 (hr)
HU (1) HUE053401T2 (hr)
IL (2) IL228874B (hr)
LT (1) LT3505528T (hr)
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PT (1) PT3505528T (hr)
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SG (2) SG194555A1 (hr)
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