HRP20191232T1 - Inhibicija, posredovana rna interferencijom, ekspresije gena virusa hepatitisa b (hbv) korištenjem kratkih interferirajućih nukleinskih kiselina (sina) - Google Patents
Inhibicija, posredovana rna interferencijom, ekspresije gena virusa hepatitisa b (hbv) korištenjem kratkih interferirajućih nukleinskih kiselina (sina) Download PDFInfo
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- HRP20191232T1 HRP20191232T1 HRP20191232T HRP20191232T1 HR P20191232 T1 HRP20191232 T1 HR P20191232T1 HR P20191232 T HRP20191232 T HR P20191232T HR P20191232 T1 HRP20191232 T1 HR P20191232T1
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- Prior art keywords
- sina
- nucleic acid
- molecule
- short interfering
- interfering nucleic
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- 230000002452 interceptive effect Effects 0.000 title claims 9
- 108020004707 nucleic acids Proteins 0.000 title claims 9
- 150000007523 nucleic acids Chemical class 0.000 title claims 9
- 102000039446 nucleic acids Human genes 0.000 title claims 9
- 241000700721 Hepatitis B virus Species 0.000 title claims 6
- 230000014509 gene expression Effects 0.000 title claims 2
- 230000001404 mediated effect Effects 0.000 title claims 2
- 238000012228 RNA interference-mediated gene silencing Methods 0.000 title 1
- 230000009368 gene silencing by RNA Effects 0.000 title 1
- 230000005764 inhibitory process Effects 0.000 title 1
- HVYWMOMLDIMFJA-DPAQBDIFSA-N cholesterol Chemical compound C1C=C2C[C@@H](O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@H]([C@H](C)CCCC(C)C)[C@@]1(C)CC2 HVYWMOMLDIMFJA-DPAQBDIFSA-N 0.000 claims 6
- 239000002773 nucleotide Substances 0.000 claims 4
- 125000003729 nucleotide group Chemical group 0.000 claims 4
- NRJAVPSFFCBXDT-HUESYALOSA-N 1,2-distearoyl-sn-glycero-3-phosphocholine Chemical compound CCCCCCCCCCCCCCCCCC(=O)OC[C@H](COP([O-])(=O)OCC[N+](C)(C)C)OC(=O)CCCCCCCCCCCCCCCCC NRJAVPSFFCBXDT-HUESYALOSA-N 0.000 claims 3
- 235000012000 cholesterol Nutrition 0.000 claims 3
- 208000015181 infectious disease Diseases 0.000 claims 3
- 239000002246 antineoplastic agent Substances 0.000 claims 2
- 239000003085 diluting agent Substances 0.000 claims 2
- 239000003937 drug carrier Substances 0.000 claims 2
- 206010073071 hepatocellular carcinoma Diseases 0.000 claims 2
- 231100000844 hepatocellular carcinoma Toxicity 0.000 claims 2
- 208000019423 liver disease Diseases 0.000 claims 2
- 238000012986 modification Methods 0.000 claims 2
- 230000004048 modification Effects 0.000 claims 2
- SYPDLJYRMSBNEX-AUGURXLVSA-N (13z,16z)-n,n-dimethyl-3-nonyldocosa-13,16-dien-1-amine Chemical compound CCCCCCCCCC(CCN(C)C)CCCCCCCCC\C=C/C\C=C/CCCCC SYPDLJYRMSBNEX-AUGURXLVSA-N 0.000 claims 1
- MLDQJTXFUGDVEO-UHFFFAOYSA-N BAY-43-9006 Chemical compound C1=NC(C(=O)NC)=CC(OC=2C=CC(NC(=O)NC=3C=C(C(Cl)=CC=3)C(F)(F)F)=CC=2)=C1 MLDQJTXFUGDVEO-UHFFFAOYSA-N 0.000 claims 1
- 206010016654 Fibrosis Diseases 0.000 claims 1
- 239000005511 L01XE05 - Sorafenib Substances 0.000 claims 1
- 108091081021 Sense strand Proteins 0.000 claims 1
- 230000000692 anti-sense effect Effects 0.000 claims 1
- -1 cationic lipid Chemical class 0.000 claims 1
- 230000007882 cirrhosis Effects 0.000 claims 1
- 208000019425 cirrhosis of liver Diseases 0.000 claims 1
- 229960003787 sorafenib Drugs 0.000 claims 1
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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
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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
- A61K31/713—Double-stranded nucleic acids or oligonucleotides
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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
- A61K47/16—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing nitrogen, e.g. nitro-, nitroso-, azo-compounds, nitriles, cyanates
- A61K47/18—Amines; Amides; Ureas; Quaternary ammonium compounds; Amino acids; Oligopeptides having up to five amino 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
- A61K47/06—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
- A61K47/28—Steroids, e.g. cholesterol, bile acids or glycyrrhetinic acid
-
- 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
- A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
- A61K47/34—Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers
-
- 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
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/50—Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals
- A61K9/51—Nanocapsules; Nanoparticles
- A61K9/5107—Excipients; Inactive ingredients
- A61K9/5123—Organic compounds, e.g. fats, sugars
-
- 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
-
- 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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- 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
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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 N.A.
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- C12N2310/00—Structure or type of the nucleic acid
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- C12N2310/31—Chemical structure of the backbone
- C12N2310/315—Phosphorothioates
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- C12N2310/00—Structure or type of the nucleic acid
- C12N2310/30—Chemical structure
- C12N2310/32—Chemical structure of the sugar
- C12N2310/322—2'-R Modification
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- C12N2310/00—Structure or type of the nucleic acid
- C12N2310/30—Chemical structure
- C12N2310/35—Nature of the modification
- C12N2310/353—Nature of the modification linked to the nucleic acid via an atom other than carbon
- C12N2310/3531—Hydrogen
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- C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
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- C12N2320/00—Applications; Uses
- C12N2320/30—Special therapeutic applications
- C12N2320/32—Special delivery means, e.g. tissue-specific
Claims (14)
1. Molekula s dvolančanom kratkom interferirajućom nukleinskom kiselinom (siNA) koja inhibira ekspresiju virusa hepatitisa B (HBV), naznačena time, da sadržava sens lanac koji sadržava nukleotidnu sekvencu 5 '- uuCCgcagUauGGaUCGGCUsU - 3' (SEQ ID NO: 376) i antisense lanac koji sadržava nukleotidnu sekvencu 5'-B GccGAuccAuAcuGcGGAAUsU B-3 '(SEQ ID NO: 224),
pri čemu je B invertirana nebazična skupina; nukleotidi prikazani masnim slovima sadržavaju 2'-O-metil modifikacije, nukleotidi prikazani malim slovima sadržavaju 2'-fluoro modifikacije a s je fosforotioatna veza.
2. Pripravak, naznačen time, da sadržava molekulu s dvolančanom kratkom interferirajućom nukleinskom kiselinom (siNA) u skladu s patentnim zahtjevom 1 i farmaceutski prihvatljiv nosač ili razrjeđivač.
3. Pripravak naznačen time, da sadržava:
(a) molekulu s dvolančanom kratkom interferirajućom nukleinskom kiselinom (siNA) u skladu s patentnim zahtjevom 1;
(b) kationski lipid;
(c) kolesterol;
(d) DSPC; i
(e) PEG-DMG.
4. Pripravak, naznačen time, da sadržava:
(a) molekulu s dvolančanom kratkom interferirajućom nukleinskom kiselinom (siNA) u skladu s patentnim zahtjevom 1;
(b) (13Z, 16Z) -N,N-dimetil-3-nonildocoza-13,16-dien-1-amin;
(c) kolesterol;
(d) DSPC; i (e) PEG-DMG.
5. Pripravak u skladu s patentnim zahtjevom 4, naznačen time, da je molarni omjer (13Z, 16Z)-N,N-dimetil-3-nonildocoza-13,16-dien-1-amin, kolesterol, DSPC i PEG-DMG 50:30:10:2.
6. Pripravak, naznačen time, da sadržava pripravak u skladu s patentnim zahtjevom 5 i farmaceutski prihvatljiv nosač ili razrjeđivač.
7. Molekula s dvolančanom kratkom interferirajućom nukleinskom kiselinom (siNA) u skladu s patentnim zahtjevom 1, naznačena time, da se koristi u liječenju ljudskog subjekta koji pati od stanja koje je posredovano djelovanjem virusa hepatitisa B (HBV).
8. Molekula za upotrebu u skladu s patentnim zahtjevom 7, naznačena time, da je navedeno stanje HBV infekcija.
9. Molekula za upotrebu u skladu s patentnim zahtjevom 7, naznačena time, da je navedeno stanje bolest jetre.
10. Molekula za upotrebu u skladu s patentnim zahtjevom 9, naznačena time, da je bolest jetre ciroza.
11. Molekula s dvolančanom kratkom interferirajućom nukleinskom kiselinom (siNA) u skladu s patentnim zahtjevom 1, naznačena time, da se koristi za liječenje ljudi koji pate od infekcije virusom hepatitisa B (HBV) da bi se smanjila učestalost razvoja HBV infekcije u hepatocelularni karcinom.
12. Kombinacija, naznačen time, da sadržava molekulu s dvolančanom kratkom interferirajućom nukleinskom kiselinom (siNA) u skladu s patentnim zahtjevom 1 i sredstvo protiv raka za upotrebu u postupku liječenja hepatocelularnog karcinoma.
13. Molekula za upotrebu u skladu s patentnim zahtjevom 12, naznačena time, da je navedeno sredstvo protiv raka sorafenib.
14. Komplet, naznačen time, da sadržava molekulu s dvolančanom kratkom interferirajućom nukleinskom kiselinom (siNA) u skladu s patentnim zahtjevom 1.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US37455510P | 2010-08-17 | 2010-08-17 | |
| PCT/US2011/047512 WO2012024170A2 (en) | 2010-08-17 | 2011-08-12 | RNA INTERFERENCE MEDIATED INHIBITION OF HEPATITIS B VIRUS (HBV) GENE EXPRESSION USING SHORT INTERFERING NUCLEIC ACID (siNA) |
| EP11818592.5A EP2606134B1 (en) | 2010-08-17 | 2011-08-12 | RNA INTERFERENCE MEDIATED INHIBITION OF HEPATITIS B VIRUS (HBV) GENE EXPRESSION USING SHORT INTERFERING NUCLEIC ACID (siNA) |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| HRP20191232T1 true HRP20191232T1 (hr) | 2019-11-01 |
Family
ID=45605615
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HRP20191232 HRP20191232T1 (hr) | 2010-08-17 | 2019-07-10 | Inhibicija, posredovana rna interferencijom, ekspresije gena virusa hepatitisa b (hbv) korištenjem kratkih interferirajućih nukleinskih kiselina (sina) |
Country Status (14)
| Country | Link |
|---|---|
| US (5) | US9029341B2 (hr) |
| EP (3) | EP2606134B1 (hr) |
| JP (5) | JP2013537423A (hr) |
| KR (2) | KR102413007B1 (hr) |
| CN (2) | CN103282497B (hr) |
| AU (1) | AU2011292261B2 (hr) |
| CA (1) | CA2807307C (hr) |
| DK (1) | DK2606134T3 (hr) |
| HR (1) | HRP20191232T1 (hr) |
| HU (1) | HUE044815T2 (hr) |
| LT (1) | LT2606134T (hr) |
| RU (2) | RU2624045C2 (hr) |
| SI (1) | SI2606134T1 (hr) |
| WO (1) | WO2012024170A2 (hr) |
Families Citing this family (51)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8575327B2 (en) | 2003-06-12 | 2013-11-05 | Alnylam Pharmaceuticals, Inc. | Conserved HBV and HCV sequences useful for gene silencing |
| US8598334B2 (en) | 2009-10-16 | 2013-12-03 | Glaxo Group Limited | HBV antisense inhibitors |
| RU2624045C2 (ru) | 2010-08-17 | 2017-06-30 | Сирна Терапьютикс,Инк | ОПОСРЕДУЕМОЕ РНК-ИНТЕРФЕРЕНЦИЕЙ ИНГИБИРОВАНИЕ ЭКСПРЕССИИ ГЕНОВ ВИРУСА ГЕПАТИТА B (HBV) С ПРИМЕНЕНИЕМ МАЛОЙ ИНТЕРФЕРИРУЮЩЕЙ НУКЛЕИНОВОЙ КИСЛОТЫ (миНК) |
| MX349088B (es) * | 2010-09-20 | 2017-07-10 | Merck Sharp & Dohme | Lípidos catiónicos novedosos de bajo peso molecular para la entrega de oligonucleótidos. |
| EP2699583A4 (en) | 2011-04-21 | 2015-04-15 | Isis Pharmaceuticals Inc | MODULATION OF EXPRESSION OF HEPATITIS B VIRUS (HBV) |
| TW202244278A (zh) * | 2011-06-30 | 2022-11-16 | 美商艾羅海德製藥公司 | 用於抑制ｂ型肝炎病毒基因表現之組合物及方法 |
| US9993460B2 (en) | 2013-07-26 | 2018-06-12 | Race Oncology Ltd. | Compositions to improve the therapeutic benefit of bisantrene and analogs and derivatives thereof |
| EP3556353A3 (en) | 2014-02-25 | 2020-03-18 | Merck Sharp & Dohme Corp. | Lipid nanoparticle vaccine adjuvants and antigen delivery systems |
| GB201408623D0 (en) | 2014-05-15 | 2014-07-02 | Santaris Pharma As | Oligomers and oligomer conjugates |
| EP3201338B1 (en) * | 2014-10-02 | 2021-11-03 | Arbutus Biopharma Corporation | Compositions and methods for silencing hepatitis b virus gene expression |
| JOP20200092A1 (ar) * | 2014-11-10 | 2017-06-16 | Alnylam Pharmaceuticals Inc | تركيبات iRNA لفيروس الكبد B (HBV) وطرق لاستخدامها |
| EA202191771A1 (ru) * | 2015-03-24 | 2022-01-31 | Элнилэм Фармасьютикалз, Инк. | КОМПОЗИЦИИ НА ОСНОВЕ RNAi ПРОТИВ ВИРУСА ГЕПАТИТА В (HBV) И СПОСОБЫ ИХ ПРИМЕНЕНИЯ |
| JP7191690B2 (ja) * | 2015-05-06 | 2022-12-19 | ベニテック バイオファーマ リミテッド | Ｂ型肝炎ウイルス（ｈｂｖ）感染を治療するための試薬及びその使用 |
| US20170137821A1 (en) | 2015-07-17 | 2017-05-18 | Arcturus Therapeutics, Inc. | Molecules and agents for treating hepatitis b virus |
| US20170016000A1 (en) | 2015-07-17 | 2017-01-19 | Arcturus Therapeutics, Inc. | Compositions and agents against hepatitis b virus and uses thereof |
| KR20180038465A (ko) | 2015-08-07 | 2018-04-16 | 애로우헤드 파마슈티컬스 인코포레이티드 | Ｂ형 간염 바이러스 감염에 대한 ｒｎａｉ 치료법 |
| ES2929928T3 (es) | 2015-11-09 | 2022-12-05 | Purotech Bio Inc | Compuestos para usar en el tratamiento de afecciones relacionadas con el VHB y el VHC |
| SG10201912314QA (en) * | 2016-01-08 | 2020-02-27 | Arbutus Biopharma Corp | Therapeutic compositions and methods for treating hepatitis b |
| HUE053172T2 (hu) | 2016-03-14 | 2021-06-28 | Hoffmann La Roche | Oligonukleotidok a PD-L1 expresszió csökkentésére |
| MA45496A (fr) | 2016-06-17 | 2019-04-24 | Hoffmann La Roche | Molécules d'acide nucléique pour la réduction de l'arnm de padd5 ou pad7 pour le traitement d'une infection par l'hépatite b |
| JOP20170161A1 (ar) * | 2016-08-04 | 2019-01-30 | Arrowhead Pharmaceuticals Inc | عوامل RNAi للعدوى بفيروس التهاب الكبد ب |
| US20210290537A1 (en) * | 2016-12-08 | 2021-09-23 | Mallinckrodt Llc | Liposomal elinafide formulations and uses thereof |
| KR20200015895A (ko) | 2017-04-18 | 2020-02-13 | 알닐람 파마슈티칼스 인코포레이티드 | B형 간염 바이러스 (hbv)에 감염된 대상체의 치료 방법 |
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| WO2018199338A1 (ja) * | 2017-04-27 | 2018-11-01 | 国立大学法人広島大学 | Ｂ型肝炎治療用核酸分子 |
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