HRP20230023T1 - Postupci liječenja infekcije hepatitisom b - Google Patents
Postupci liječenja infekcije hepatitisom b Download PDFInfo
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- HRP20230023T1 HRP20230023T1 HRP20230023TT HRP20230023T HRP20230023T1 HR P20230023 T1 HRP20230023 T1 HR P20230023T1 HR P20230023T T HRP20230023T T HR P20230023TT HR P20230023 T HRP20230023 T HR P20230023T HR P20230023 T1 HRP20230023 T1 HR P20230023T1
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- 238000000034 method Methods 0.000 title claims 4
- 208000002672 hepatitis B Diseases 0.000 title 1
- 108091034117 Oligonucleotide Proteins 0.000 claims 10
- 239000002773 nucleotide Substances 0.000 claims 8
- 125000003729 nucleotide group Chemical group 0.000 claims 7
- 241000700721 Hepatitis B virus Species 0.000 claims 4
- 239000003937 drug carrier Substances 0.000 claims 4
- 230000000692 anti-sense effect Effects 0.000 claims 3
- 210000004027 cell Anatomy 0.000 claims 3
- 239000000427 antigen Substances 0.000 claims 2
- 102000036639 antigens Human genes 0.000 claims 2
- 108091007433 antigens Proteins 0.000 claims 2
- 239000002612 dispersion medium Substances 0.000 claims 2
- 239000002904 solvent Substances 0.000 claims 2
- RYYWUUFWQRZTIU-UHFFFAOYSA-K thiophosphate Chemical compound [O-]P([O-])([O-])=S RYYWUUFWQRZTIU-UHFFFAOYSA-K 0.000 claims 2
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims 2
- 108091081021 Sense strand Proteins 0.000 claims 1
- 229960000980 entecavir Drugs 0.000 claims 1
- YXPVEXCTPGULBZ-WQYNNSOESA-N entecavir hydrate Chemical compound O.C1=NC=2C(=O)NC(N)=NC=2N1[C@H]1C[C@H](O)[C@@H](CO)C1=C YXPVEXCTPGULBZ-WQYNNSOESA-N 0.000 claims 1
- 210000003494 hepatocyte Anatomy 0.000 claims 1
- 238000000338 in vitro Methods 0.000 claims 1
- 208000015181 infectious disease Diseases 0.000 claims 1
- 108020004999 messenger RNA Proteins 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 239000008363 phosphate buffer Substances 0.000 claims 1
- 239000012266 salt solution Substances 0.000 claims 1
- 239000000126 substance Substances 0.000 claims 1
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- 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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- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
- A61K31/52—Purines, e.g. adenine
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- A61K31/7105—Natural ribonucleic acids, i.e. containing only riboses attached to adenine, guanine, cytosine or uracil and having 3'-5' phosphodiester links
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- 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
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- A01K—ANIMAL HUSBANDRY; CARE OF BIRDS, FISHES, INSECTS; FISHING; REARING OR BREEDING ANIMALS, NOT OTHERWISE PROVIDED FOR; NEW BREEDS OF ANIMALS
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Claims (15)
1. Oligonukleotid za smanjenje ekspresije površinskog antigena virusa hepatitisa B (HBsAg) mRNA, te oligonukleotid sadrži smisleni lanac koji tvori dupleks regiju s protusmislenim lancem, naznačen time što:
se smisleni lanac sastoji od sekvence kako je navedeno u GACAAAAAUCCUCACAAUAAGCAGCCGAAAGGCUGC (SEQ ID NO:9) i sadrži 2'-fluoro modificirane nukleotide na položajima 3, 8-10, 12, 13, i 17,
2'-O-metil modificirane nukleotide na položajima 1, 2, 4-7, 11, 14-16, 18-26, i 31-36, i jednu fosforotioatnu internukleotidnu vezu između nukleotida na položajima 1 i 2, pri čemu je svaki od nukleotida iz -GAAA- sekvence na smislenom lancu konjugiran na jednovalentni GalNac dio, pri čemu -GAAA- sekvenca sadrži strukturu:
[image]
i
protusmisleni lanac se sastoji od sekvence kako je navedeno u
UUAUUGUGAGGAUUUUUGUCGG (SEQ ID NO: 6) i sadrži
2'-fluoro modificirane nukleotide na položajima 2, 3, 5, 7, 8, 10, 12, 14, 16, i 19,
2'-O-metil modificirane nukleotide na položajima 1, 4, 6, 9, 11, 13, 15, 17, 18, i 20-22, i pet fosforotioatnih internukleotidnih veza između nukleotida na položajima 1 i 2, između nukleotida na položajima 2 i 3, između nukleotida na položajima 3 i 4,
između nukleotida na položajima 20 i 21, i između nukleotida na položajima 21 i 22,
pri čemu 5'-nukleotid protusmislenog lanca ima sljedeću strukturu:
[image]
2. Pripravak koji sadrži oligonukleotid prema zahtjevu 1 .
3. Pripravak prema zahtjevu 2, naznačen time što sadrži protuion.
4. Pripravak prema zahtjevu 2, naznačen time što sadrži Na+ protuione.
5. Pripravak prema bilo kojem od zahtjeva 2 do 4, naznačen time što sadrži farmaceutski prihvatljiv nosač.
6. Pripravak prema zahtjevu 5, naznačen time što je farmaceutski prihvatljiv nosač otapalo ili disperzijski medij koji sadrži vodu.
7. Pripravak prema bilo kojem od zahtjeva 2 do 6, naznačen time što sadrži pomoćnu tvar.
8. Pripravak prema bilo kojem od zahtjeva 2 do 7, naznačen time što sadrži otopinu soli s fosfatnim puferom.
9. In vitro postupak smanjenja ekspresije površinskog antigena (HBV) virusa hepatitisa B (HBV) u stanici, naznačen time što postupak uključuje isporuku u stanicu oligonukleotida prema zahtjevu 1, ili pripravka prema bilo kojem od zahtjeva 2 do 8.
10. Postupak prema zahtjevu 9, naznačen time što je stanica hepatocit.
11. Oligonukleotid prema zahtjevu 1 ili pripravak prema bilo kojem od zahtjeva 2 do 8, naznačen time što se koristi u postupku liječenja HBV infekcije kod subjekta.
12. Oligonukleotid ili pripravak za upotrebu prema zahtjevu 11, naznačen time što se oligonukleotid ili pripravak daje subjektu potkožno.
13. Oligonukleotid ili pripravak za upotrebu prema zahtjevu 11, naznačen time što se oligonukleotid ili pripravak daje subjektu intravenski.
14. Pripravak za upotrebu prema zahtjevu 13, naznačen time što sadrži farmaceutski prihvatljiv nosač, pri čemu je farmaceutski prihvatljiv nosač otapalo ili disperzijski medij koji sadrži vodu.
15. Oligonukleotid ili pripravak za upotrebu u skladu s bilo kojim od patentnih zahtjeva 11-14, naznačen time što se subjektu također daje učinkovita količina Entekavira.
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US201762575358P | 2017-10-20 | 2017-10-20 | |
PCT/US2018/056801 WO2019079781A2 (en) | 2017-10-20 | 2018-10-19 | METHODS OF TREATING HEPATITIS B TYPE INFECTIONS |
EP18868404.7A EP3684377B1 (en) | 2017-10-20 | 2018-10-19 | Methods for treating hepatitis b infection |
Publications (1)
Publication Number | Publication Date |
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HRP20230023T1 true HRP20230023T1 (hr) | 2023-03-17 |
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CN114940991B (zh) * | 2021-04-13 | 2023-02-03 | 厦门甘宝利生物医药有限公司 | 一种抑制乙型肝炎病毒基因表达的rna抑制剂及其应用 |
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