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 |
|---|---|---|---|
| EP14193887.8 | 2014-11-19 | ||
| EP14193887 | 2014-11-19 | ||
| EP14198167 | 2014-12-16 | ||
| EP14198167.0 | 2014-12-16 | ||
| EP15182401 | 2015-08-25 | ||
| EP15182401.8 | 2015-08-25 | ||
| EP15191076 | 2015-10-22 | ||
| EP15191074 | 2015-10-22 | ||
| EP15191076.7 | 2015-10-22 | ||
| EP15191075 | 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 (2) | 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 (2) |
| EP (2) | EP3220921A1 (2) |
| JP (2) | JP2017536366A (2) |
| WO (2) | WO2016079181A1 (2) |
Families Citing this family (46)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| RU2572826C2 (ru) | 2008-12-02 | 2016-01-20 | Чиралджен, Лтд. | Способ синтеза модифицированных по атому фосфора нуклеиновых кислот |
| CA2767253A1 (en) | 2009-07-06 | 2011-01-13 | Ontorii, Inc. | Novel nucleic acid prodrugs and methods of use thereof |
| JP5868324B2 (ja) | 2010-09-24 | 2016-02-24 | 株式会社Wave Life Sciences Japan | 不斉補助基 |
| AU2012284265B2 (en) | 2011-07-19 | 2017-08-17 | Wave Life Sciences Ltd. | Methods for the synthesis of functionalized nucleic acids |
| JP6453212B2 (ja) | 2012-07-13 | 2019-01-16 | ウェイブ ライフ サイエンシズ リミテッドＷａｖｅ Ｌｉｆｅ Ｓｃｉｅｎｃｅｓ Ｌｔｄ． | キラル制御 |
| SG11201500239VA (en) | 2012-07-13 | 2015-03-30 | Wave Life Sciences Japan | Asymmetric auxiliary group |
| CN104684923B (zh) | 2012-07-13 | 2018-09-28 | 株式会社新日本科学 | 手性核酸佐剂 |
| US11162096B2 (en) | 2013-10-14 | 2021-11-02 | Ionis Pharmaceuticals, Inc | Methods for modulating expression of C9ORF72 antisense transcript |
| WO2015108047A1 (ja) | 2014-01-15 | 2015-07-23 | 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 |
| 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 |
| WO2015108048A1 (ja) | 2014-01-15 | 2015-07-23 | 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 |
| ES2917473T3 (es) | 2014-01-16 | 2022-07-08 | Wave Life Sciences Ltd | Diseño quiral |
| US10676737B2 (en) | 2014-12-17 | 2020-06-09 | 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 |
| CN108135921B (zh) | 2015-07-22 | 2023-10-17 | 波涛生命科学有限公司 | 寡核苷酸组合物及其方法 |
| EP3394258B1 (en) * | 2015-10-22 | 2021-09-22 | Roche Innovation Center Copenhagen A/S | In vitro toxicity screening assay |
| WO2017157672A1 (en) * | 2016-03-18 | 2017-09-21 | Roche Innovation Center Copenhagen A/S | Acyl-protected l-lna-guanosine monomers |
| JP2019516680A (ja) | 2016-05-04 | 2019-06-20 | ウェイブ ライフ サイエンシズ リミテッドＷａｖｅ Ｌｉｆｅ Ｓｃｉｅｎｃｅｓ Ｌｔｄ． | オリゴヌクレオチド組成物およびその方法 |
| CN109414448B (zh) | 2016-06-17 | 2021-10-26 | 豪夫迈·罗氏有限公司 | 用于减少PAPD5或PAPD7 mRNA治疗乙型肝炎感染的核酸分子 |
| US11105794B2 (en) * | 2016-06-17 | 2021-08-31 | Hoffmann-La Roche Inc. | In vitro nephrotoxicity screening assay |
| WO2017216325A1 (en) * | 2016-06-17 | 2017-12-21 | F. Hoffmann-La Roche Ag | In vitro nephrotoxicity screening assay |
| EP3475424A1 (en) | 2016-06-22 | 2019-05-01 | ProQR Therapeutics II B.V. | Single-stranded rna-editing oligonucleotides |
| US10941402B2 (en) | 2016-09-01 | 2021-03-09 | Proqr Therapeutics Ii B.V. | Chemically modified single-stranded RNA-editing oligonucleotides |
| US11542292B2 (en) | 2016-11-14 | 2023-01-03 | Tokyo University Of Science Foundation | Polymerizable compound, compound, and method for producing boranophosphate oligomer |
| MA46905A (fr) * | 2016-11-23 | 2019-10-02 | Wave Life Sciences Ltd | Compositions et procédés de synthèse de phosphoramidites et d'oligonucléotides |
| US20190367920A1 (en) * | 2017-01-13 | 2019-12-05 | Roche Innovation Center Copenhagen A/S | Antisense oligonucleotides for modulating nfkb1 expression |
| WO2018130585A1 (en) * | 2017-01-13 | 2018-07-19 | Roche Innovation Center Copenhagen A/S | Antisense oligonucleotides for modulating relb expression |
| US11274300B2 (en) | 2017-01-19 | 2022-03-15 | Proqr Therapeutics Ii B.V. | Oligonucleotide complexes for use in RNA editing |
| CN111226114A (zh) | 2017-10-13 | 2020-06-02 | 罗氏创新中心哥本哈根有限公司 | 用部分立体限定的寡核苷酸子文库鉴定反义寡核苷酸改进的立体限定硫代磷酸酯寡核苷酸变体的方法 |
| UA126931C2 (uk) * | 2017-10-16 | 2023-02-22 | Ф. Хоффманн-Ля Рош Аг | МОЛЕКУЛИ НУКЛЕЇНОВИХ КИСЛОТ ДЛЯ ЗМЕНШЕННЯ РІВНЯ мРНК PAPD5 І PAPD7 ДЛЯ ЛІКУВАННЯ ІНФЕКЦІЙНОГО ГЕПАТИТУ B |
| PT3717646T (pt) | 2017-12-01 | 2025-07-28 | Texas A & M Univ Sys | Tratamento antisense da síndrome de angelman |
| WO2019122279A1 (en) * | 2017-12-22 | 2019-06-27 | Roche Innovation Center Copenhagen A/S | Oligonucleotides comprising a phosphorodithioate internucleoside linkage |
| WO2019122282A1 (en) * | 2017-12-22 | 2019-06-27 | Roche Innovation Center Copenhagen A/S | Gapmer oligonucleotides comprising a phosphorodithioate internucleoside linkage |
| CN111448316B (zh) * | 2017-12-22 | 2025-02-14 | 罗氏创新中心哥本哈根有限公司 | 新的硫代亚磷酰胺 |
| EA202091693A1 (ru) | 2018-01-12 | 2021-04-14 | Бристол-Маерс Сквибб Компани | Антисмысловые олигонуклеотиды, целенаправленно воздействующие на альфа-синуклеин, и их применения |
| BR112020013994A2 (pt) | 2018-01-12 | 2020-12-08 | Bristol-Myers Squibb Company | Oligonucleotídeos antissenso que direcionam alfa-sinucleína e seus usos |
| US11613554B2 (en) | 2018-04-13 | 2023-03-28 | Bristol-Myers Squibb Company | Phosphorous (V)-based reagents, processes for the preparation thereof, and their use in making stereo-defined organophoshorous (V) compounds |
| GB201808146D0 (en) | 2018-05-18 | 2018-07-11 | Proqr Therapeutics Ii Bv | Stereospecific Linkages in RNA Editing Oligonucleotides |
| SG11202012759XA (en) | 2018-07-03 | 2021-01-28 | Hoffmann La Roche | Oligonucleotides for modulating tau expression |
| EP3819378A4 (en) * | 2018-07-04 | 2022-09-14 | Aichi Medical University | OLIGONUCLEOTIDES FOR CONTROL OF TAU SPLICING AND THEIR USES |
| CA3130431A1 (en) * | 2019-02-20 | 2020-08-27 | Roche Innovation Center Copenhagen A/S | Phosphonoacetate gapmer oligonucleotides |
| CN113905744A (zh) | 2019-05-31 | 2022-01-07 | 阿利戈斯治疗公司 | 经修饰的间隙子寡核苷酸及其使用方法 |
| IL294618A (en) | 2020-01-16 | 2022-09-01 | Bristol Myers Squibb Co | Reagents and their use for the modular synthesis of c-p bonds |
| US20240182889A1 (en) * | 2021-03-26 | 2024-06-06 | Neumirna Therapeutics Aps | Microrna-27b inhibitors |
| US20240166675A1 (en) | 2022-09-19 | 2024-05-23 | Bristol-Myers Squibb Company | Novel phosphorous (v)-based reagents, processes for the preparation thereof, and their use in making stereo-defined organophoshorous (v) compounds |
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 |
| WO2008049085A1 (en) * | 2006-10-18 | 2008-04-24 | Isis Pharmaceuticals, Inc. | Antisense compounds |
| JP6453212B2 (ja) * | 2012-07-13 | 2019-01-16 | ウェイブ ライフ サイエンシズ リミテッドＷａｖｅ Ｌｉｆｅ Ｓｃｉｅｎｃｅｓ Ｌｔｄ． | キラル制御 |
| CN104955952A (zh) * | 2013-01-30 | 2015-09-30 | 弗·哈夫曼-拉罗切有限公司 | Lna寡核苷酸碳水化合物缀合物 |
-
2015
- 2015-11-18 JP JP2017526905A patent/JP2017536366A/ja active Pending
- 2015-11-18 EP EP15797652.3A patent/EP3220921A1/en not_active Withdrawn
- 2015-11-18 JP JP2017526918A patent/JP2017536119A/ja active Pending
- 2015-11-18 US US15/527,765 patent/US20180016575A1/en not_active Abandoned
- 2015-11-18 EP EP15797651.5A patent/EP3221329A1/en not_active Withdrawn
- 2015-11-18 WO PCT/EP2015/076967 patent/WO2016079181A1/en not_active Ceased
- 2015-11-18 US US15/527,832 patent/US20180112217A1/en not_active Abandoned
- 2015-11-18 WO PCT/EP2015/076971 patent/WO2016079183A1/en not_active Ceased
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