JP2017536366A5 - - Google Patents
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- Publication number
- JP2017536366A5 JP2017536366A5 JP2017526905A JP2017526905A JP2017536366A5 JP 2017536366 A5 JP2017536366 A5 JP 2017536366A5 JP 2017526905 A JP2017526905 A JP 2017526905A JP 2017526905 A JP2017526905 A JP 2017526905A JP 2017536366 A5 JP2017536366 A5 JP 2017536366A5
- Authority
- JP
- Japan
- Prior art keywords
- lna
- phosphorothioate
- sterically defined
- nucleoside
- oligonucleotide
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Pending
Links
- 108091034117 Oligonucleotide Proteins 0.000 claims 19
- RYYWUUFWQRZTIU-UHFFFAOYSA-K thiophosphate Chemical compound [O-]P([O-])([O-])=S RYYWUUFWQRZTIU-UHFFFAOYSA-K 0.000 claims 19
- 239000002777 nucleoside Substances 0.000 claims 15
- 230000000707 stereoselective effect Effects 0.000 claims 7
- 150000003833 nucleoside derivatives Chemical class 0.000 claims 5
- -1 LNA nucleoside Chemical class 0.000 claims 4
- RYYWUUFWQRZTIU-UHFFFAOYSA-N Thiophosphoric acid Chemical class OP(O)(S)=O RYYWUUFWQRZTIU-UHFFFAOYSA-N 0.000 claims 4
- 125000003835 nucleoside group Chemical group 0.000 claims 4
- 125000003729 nucleotide group Chemical group 0.000 claims 2
- 102100034343 Integrase Human genes 0.000 claims 1
- 101710203526 Integrase Proteins 0.000 claims 1
- FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 claims 1
- JLCPHMBAVCMARE-UHFFFAOYSA-N [3-[[3-[[3-[[3-[[3-[[3-[[3-[[3-[[3-[[3-[[3-[[5-(2-amino-6-oxo-1H-purin-9-yl)-3-[[3-[[3-[[3-[[3-[[3-[[5-(2-amino-6-oxo-1H-purin-9-yl)-3-[[5-(2-amino-6-oxo-1H-purin-9-yl)-3-hydroxyoxolan-2-yl]methoxy-hydroxyphosphoryl]oxyoxolan-2-yl]methoxy-hydroxyphosphoryl]oxy-5-(5-methyl-2,4-dioxopyrimidin-1-yl)oxolan-2-yl]methoxy-hydroxyphosphoryl]oxy-5-(6-aminopurin-9-yl)oxolan-2-yl]methoxy-hydroxyphosphoryl]oxy-5-(6-aminopurin-9-yl)oxolan-2-yl]methoxy-hydroxyphosphoryl]oxy-5-(6-aminopurin-9-yl)oxolan-2-yl]methoxy-hydroxyphosphoryl]oxy-5-(6-aminopurin-9-yl)oxolan-2-yl]methoxy-hydroxyphosphoryl]oxyoxolan-2-yl]methoxy-hydroxyphosphoryl]oxy-5-(5-methyl-2,4-dioxopyrimidin-1-yl)oxolan-2-yl]methoxy-hydroxyphosphoryl]oxy-5-(4-amino-2-oxopyrimidin-1-yl)oxolan-2-yl]methoxy-hydroxyphosphoryl]oxy-5-(5-methyl-2,4-dioxopyrimidin-1-yl)oxolan-2-yl]methoxy-hydroxyphosphoryl]oxy-5-(5-methyl-2,4-dioxopyrimidin-1-yl)oxolan-2-yl]methoxy-hydroxyphosphoryl]oxy-5-(6-aminopurin-9-yl)oxolan-2-yl]methoxy-hydroxyphosphoryl]oxy-5-(6-aminopurin-9-yl)oxolan-2-yl]methoxy-hydroxyphosphoryl]oxy-5-(4-amino-2-oxopyrimidin-1-yl)oxolan-2-yl]methoxy-hydroxyphosphoryl]oxy-5-(4-amino-2-oxopyrimidin-1-yl)oxolan-2-yl]methoxy-hydroxyphosphoryl]oxy-5-(4-amino-2-oxopyrimidin-1-yl)oxolan-2-yl]methoxy-hydroxyphosphoryl]oxy-5-(6-aminopurin-9-yl)oxolan-2-yl]methoxy-hydroxyphosphoryl]oxy-5-(4-amino-2-oxopyrimidin-1-yl)oxolan-2-yl]methyl [5-(6-aminopurin-9-yl)-2-(hydroxymethyl)oxolan-3-yl] hydrogen phosphate Polymers Cc1cn(C2CC(OP(O)(=O)OCC3OC(CC3OP(O)(=O)OCC3OC(CC3O)n3cnc4c3nc(N)[nH]c4=O)n3cnc4c3nc(N)[nH]c4=O)C(COP(O)(=O)OC3CC(OC3COP(O)(=O)OC3CC(OC3COP(O)(=O)OC3CC(OC3COP(O)(=O)OC3CC(OC3COP(O)(=O)OC3CC(OC3COP(O)(=O)OC3CC(OC3COP(O)(=O)OC3CC(OC3COP(O)(=O)OC3CC(OC3COP(O)(=O)OC3CC(OC3COP(O)(=O)OC3CC(OC3COP(O)(=O)OC3CC(OC3COP(O)(=O)OC3CC(OC3COP(O)(=O)OC3CC(OC3COP(O)(=O)OC3CC(OC3COP(O)(=O)OC3CC(OC3COP(O)(=O)OC3CC(OC3COP(O)(=O)OC3CC(OC3CO)n3cnc4c(N)ncnc34)n3ccc(N)nc3=O)n3cnc4c(N)ncnc34)n3ccc(N)nc3=O)n3ccc(N)nc3=O)n3ccc(N)nc3=O)n3cnc4c(N)ncnc34)n3cnc4c(N)ncnc34)n3cc(C)c(=O)[nH]c3=O)n3cc(C)c(=O)[nH]c3=O)n3ccc(N)nc3=O)n3cc(C)c(=O)[nH]c3=O)n3cnc4c3nc(N)[nH]c4=O)n3cnc4c(N)ncnc34)n3cnc4c(N)ncnc34)n3cnc4c(N)ncnc34)n3cnc4c(N)ncnc34)O2)c(=O)[nH]c1=O JLCPHMBAVCMARE-UHFFFAOYSA-N 0.000 claims 1
- 239000002671 adjuvant Substances 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 239000000178 monomer Substances 0.000 claims 1
- 239000002773 nucleotide Substances 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 150000003839 salts Chemical class 0.000 claims 1
- 239000011780 sodium chloride Substances 0.000 claims 1
- 239000002904 solvent Substances 0.000 claims 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims 1
Applications Claiming Priority (13)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP14193887 | 2014-11-19 | ||
| EP14193887.8 | 2014-11-19 | ||
| EP14198167 | 2014-12-16 | ||
| EP14198167.0 | 2014-12-16 | ||
| EP15182401 | 2015-08-25 | ||
| EP15182401.8 | 2015-08-25 | ||
| EP15191076.7 | 2015-10-22 | ||
| EP15191074 | 2015-10-22 | ||
| EP15191075 | 2015-10-22 | ||
| EP15191076 | 2015-10-22 | ||
| EP15191074.2 | 2015-10-22 | ||
| EP15191075.9 | 2015-10-22 | ||
| PCT/EP2015/076971 WO2016079183A1 (en) | 2014-11-19 | 2015-11-18 | Lna chiral phosphorothioates |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2017536366A JP2017536366A (ja) | 2017-12-07 |
| JP2017536366A5 true JP2017536366A5 (enExample) | 2018-11-15 |
Family
ID=54608516
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017526905A Pending JP2017536366A (ja) | 2014-11-19 | 2015-11-18 | Ｌｎａキラルホスホロチオエート |
| JP2017526918A Pending JP2017536119A (ja) | 2014-11-19 | 2015-11-18 | キラルホスホロチオエート連結を含むｌｎａギャップマーオリゴヌクレオチド |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017526918A Pending JP2017536119A (ja) | 2014-11-19 | 2015-11-18 | キラルホスホロチオエート連結を含むｌｎａギャップマーオリゴヌクレオチド |
Country Status (4)
| Country | Link |
|---|---|
| US (2) | US20180016575A1 (enExample) |
| EP (2) | EP3221329A1 (enExample) |
| JP (2) | JP2017536366A (enExample) |
| WO (2) | WO2016079183A1 (enExample) |
Families Citing this family (45)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| SG171914A1 (en) | 2008-12-02 | 2011-07-28 | Chiralgen Ltd | Method for the synthesis of phosphorus atom modified nucleic acids |
| US9744183B2 (en) | 2009-07-06 | 2017-08-29 | Wave Life Sciences Ltd. | Nucleic acid prodrugs and methods of use thereof |
| DK2620428T3 (da) | 2010-09-24 | 2019-07-01 | Wave Life Sciences Ltd | Asymmetrisk hjælpegruppe |
| RU2014105311A (ru) | 2011-07-19 | 2015-08-27 | Уэйв Лайф Сайенсес Пте. Лтд. | Способы синтеза функционализованных нуклеиновых кислот |
| PT2872485T (pt) | 2012-07-13 | 2021-03-05 | Wave Life Sciences Ltd | Grupo auxiliar assimétrico |
| KR102712879B1 (ko) | 2012-07-13 | 2024-10-04 | 웨이브 라이프 사이언시스 리미티드 | 키랄 제어 |
| BR112015000723A2 (pt) | 2012-07-13 | 2017-06-27 | Shin Nippon Biomedical Laboratories Ltd | adjuvante de ácido nucléico quiral |
| US11162096B2 (en) | 2013-10-14 | 2021-11-02 | Ionis Pharmaceuticals, Inc | Methods for modulating expression of C9ORF72 antisense transcript |
| JPWO2015108047A1 (ja) | 2014-01-15 | 2017-03-23 | 株式会社新日本科学 | 免疫誘導活性を有するキラル核酸アジュバンド及び免疫誘導活性剤 |
| JPWO2015108048A1 (ja) | 2014-01-15 | 2017-03-23 | 株式会社新日本科学 | 抗腫瘍作用を有するキラル核酸アジュバンド及び抗腫瘍剤 |
| JPWO2015108046A1 (ja) | 2014-01-15 | 2017-03-23 | 株式会社新日本科学 | 抗アレルギー作用を有するキラル核酸アジュバンド及び抗アレルギー剤 |
| PT3094728T (pt) | 2014-01-16 | 2022-05-19 | Wave Life Sciences Ltd | Desenho quiral |
| EP3712269A1 (en) | 2014-12-17 | 2020-09-23 | ProQR Therapeutics II B.V. | Targeted rna editing |
| WO2016112132A1 (en) * | 2015-01-06 | 2016-07-14 | Ionis Pharmaceuticals, Inc. | Compositions for modulating expression of c9orf72 antisense transcript |
| WO2016167780A1 (en) | 2015-04-16 | 2016-10-20 | Ionis Pharmaceuticals, Inc. | Compositions for modulating expression of c9orf72 antisense transcript |
| MA43072A (fr) | 2015-07-22 | 2018-05-30 | Wave Life Sciences Ltd | Compositions d'oligonucléotides et procédés associés |
| EP3394258B1 (en) * | 2015-10-22 | 2021-09-22 | Roche Innovation Center Copenhagen A/S | In vitro toxicity screening assay |
| US11267843B2 (en) * | 2016-03-18 | 2022-03-08 | Roche Innovation Center Copenhagen A/S | Stereodefining L-monomers |
| MA45270A (fr) | 2016-05-04 | 2017-11-09 | Wave Life Sciences Ltd | Compositions d'oligonucléotides et procédés associés |
| WO2017216325A1 (en) * | 2016-06-17 | 2017-12-21 | F. Hoffmann-La Roche Ag | In vitro nephrotoxicity screening assay |
| JP7049271B2 (ja) * | 2016-06-17 | 2022-04-06 | エフ．ホフマン－ラ ロシュ アーゲー | インビトロ腎毒性スクリーニングアッセイ |
| 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 |
| CN109477103A (zh) | 2016-06-22 | 2019-03-15 | ProQR治疗上市公司Ⅱ | 单链rna-编辑寡核苷酸 |
| KR102501980B1 (ko) | 2016-09-01 | 2023-02-20 | 프로큐알 테라퓨틱스 Ⅱ 비.브이. | 화학적으로 변형된 단일 가닥 rna-편집 올리고뉴클레오타이드 |
| JP7115669B2 (ja) * | 2016-11-14 | 2022-08-09 | 学校法人東京理科大学 | 重合性化合物、化合物、及び、ボラノホスフェートオリゴマーの製造方法 |
| US11873316B2 (en) | 2016-11-23 | 2024-01-16 | Wave Life Sciences Ltd. | Compositions and methods for phosphoramidite and oligonucleotide synthesis |
| WO2018130583A1 (en) * | 2017-01-13 | 2018-07-19 | Roche Innovation Center Copenhagen A/S | Antisense oligonucleotides for modulating nfkb1 expression |
| EP3568481A1 (en) * | 2017-01-13 | 2019-11-20 | Roche Innovation Center Copenhagen A/S | Antisense oligonucleotides for modulating relb expression |
| EP3571300A1 (en) | 2017-01-19 | 2019-11-27 | ProQR Therapeutics II B.V. | Oligonucleotide complexes for use in rna editing |
| EP3694995A1 (en) | 2017-10-13 | 2020-08-19 | Roche Innovation Center Copenhagen A/S | Methods for identifying improved stereodefined phosphorothioate oligonucleotide variants of antisense oligonucleotides utilising sub-libraries of partially stereodefined oligonucleotides |
| TW202424191A (zh) * | 2017-10-16 | 2024-06-16 | 瑞士商赫孚孟拉羅股份公司 | 用於降低PAPD5及PAPD7 mRNA以治療B型肝炎感染之核酸分子 |
| CN118291458A (zh) | 2017-12-01 | 2024-07-05 | 德克萨斯A&M大学体系 | 天使综合征反义治疗 |
| BR112020012427A8 (pt) * | 2017-12-22 | 2024-04-02 | Roche Innovation Ct Copenhagen As | Oligonucleotídeos, sal farmaceuticamente aceitável, conjugado, composição farmacêutica e processo para a fabricação de um oligonucleotídeo |
| JP2021508327A (ja) * | 2017-12-22 | 2021-03-04 | ロシュ イノベーション センター コペンハーゲン エーエス | 新規のチオホスホラミダイト |
| EP4092117A1 (en) * | 2017-12-22 | 2022-11-23 | Roche Innovation Center Copenhagen A/S | Gapmer oligonucleotides comprising a phosphorodithioate internucleoside linkage |
| CA3088112A1 (en) | 2018-01-12 | 2019-07-18 | Bristol-Myers Squibb Company | Antisense oligonucleotides targeting alpha-synuclein and uses thereof |
| BR112020014011A2 (pt) * | 2018-01-12 | 2020-12-08 | Bristol-Myers Squibb Company | Oligonucleotídeos antissenso dirigidos à alfa-sinucleína e usos dos mesmos |
| CN112236438B (zh) | 2018-04-13 | 2024-10-15 | 百时美施贵宝公司 | 基于磷(v)的试剂，其制备方法，以及其在制备立体限定的有机磷(v)化合物中的用途 |
| GB201808146D0 (en) | 2018-05-18 | 2018-07-11 | Proqr Therapeutics Ii Bv | Stereospecific Linkages in RNA Editing Oligonucleotides |
| RU2768285C1 (ru) | 2018-07-03 | 2022-03-23 | Ф. Хоффманн-Ля Рош Аг | Олигонуклеотиды для модуляции экспрессии тау-белка |
| WO2020009151A1 (ja) * | 2018-07-04 | 2020-01-09 | 国立大学法人名古屋大学 | タウのスプライシングを制御するアンチセンスオリゴヌクレオチド及びその用途 |
| JP2022521510A (ja) * | 2019-02-20 | 2022-04-08 | ロシュ イノベーション センター コペンハーゲン エーエス | ホスホノアセテートギャップマー型オリゴヌクレオチド |
| MX2021014206A (es) | 2019-05-31 | 2022-01-06 | Aligos Therapeutics Inc | Oligonucleotidos gapmer modificados y metodos de uso. |
| AU2021209076A1 (en) | 2020-01-16 | 2022-07-07 | Bristol-Myers Squibb Company | Reagents and their use for modular enantiodivergent synthesis of C–P bonds |
| CN120187734A (zh) | 2022-09-19 | 2025-06-20 | 百时美施贵宝公司 | 新的基于磷(v)的试剂、其制备方法以及其在制备立体定义的有机磷(v)化合物中的用途 |
Family Cites Families (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6242589B1 (en) * | 1998-07-14 | 2001-06-05 | Isis Pharmaceuticals, Inc. | Phosphorothioate oligonucleotides having modified internucleoside linkages |
| AU2007310989B2 (en) * | 2006-10-18 | 2014-05-29 | Isis Pharmaceuticals, Inc. | Antisense compounds |
| KR102712879B1 (ko) * | 2012-07-13 | 2024-10-04 | 웨이브 라이프 사이언시스 리미티드 | 키랄 제어 |
| EP2951305B1 (en) * | 2013-01-30 | 2018-08-15 | F.Hoffmann-La Roche Ag | Lna oligonucleotide carbohydrate conjugates |
-
2015
- 2015-11-18 JP JP2017526905A patent/JP2017536366A/ja active Pending
- 2015-11-18 EP EP15797651.5A patent/EP3221329A1/en not_active Withdrawn
- 2015-11-18 JP JP2017526918A patent/JP2017536119A/ja active Pending
- 2015-11-18 WO PCT/EP2015/076971 patent/WO2016079183A1/en not_active Ceased
- 2015-11-18 EP EP15797652.3A patent/EP3220921A1/en not_active Withdrawn
- 2015-11-18 US US15/527,765 patent/US20180016575A1/en not_active Abandoned
- 2015-11-18 US US15/527,832 patent/US20180112217A1/en not_active Abandoned
- 2015-11-18 WO PCT/EP2015/076967 patent/WO2016079181A1/en not_active Ceased