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 | ||
| EP14198167.0 | 2014-12-16 | ||
| EP14198167 | 2014-12-16 | ||
| EP15182401.8 | 2015-08-25 | ||
| EP15182401 | 2015-08-25 | ||
| EP15191076.7 | 2015-10-22 | ||
| EP15191074 | 2015-10-22 | ||
| EP15191075.9 | 2015-10-22 | ||
| EP15191076 | 2015-10-22 | ||
| EP15191075 | 2015-10-22 | ||
| EP15191074.2 | 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 |
|---|---|---|---|
| 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 |
| JP2017526905A Pending JP2017536366A (ja) | 2014-11-19 | 2015-11-18 | Ｌｎａキラルホスホロチオエート |
Family Applications Before (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) | US20180112217A1 (enExample) |
| EP (2) | EP3221329A1 (enExample) |
| JP (2) | JP2017536119A (enExample) |
| WO (2) | WO2016079183A1 (enExample) |
Families Citing this family (46)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US9394333B2 (en) | 2008-12-02 | 2016-07-19 | Wave Life Sciences Japan | Method for the synthesis of phosphorus atom modified nucleic acids |
| MX342945B (es) | 2009-07-06 | 2016-10-18 | Ontorii Inc * | Profármacos de ácido nucleico novedosos y métodos de uso de los mismos. |
| DK2620428T3 (da) | 2010-09-24 | 2019-07-01 | Wave Life Sciences Ltd | Asymmetrisk hjælpegruppe |
| US9605019B2 (en) | 2011-07-19 | 2017-03-28 | Wave Life Sciences Ltd. | Methods for the synthesis of functionalized nucleic acids |
| KR20240148947A (ko) | 2012-07-13 | 2024-10-11 | 웨이브 라이프 사이언시스 리미티드 | 키랄 제어 |
| SG11201500243WA (en) | 2012-07-13 | 2015-04-29 | Shin Nippon Biomedical Lab Ltd | Chiral nucleic acid adjuvant |
| SG11201500239VA (en) | 2012-07-13 | 2015-03-30 | Wave Life Sciences Japan | Asymmetric auxiliary group |
| US11162096B2 (en) | 2013-10-14 | 2021-11-02 | Ionis Pharmaceuticals, Inc | Methods for modulating expression of C9ORF72 antisense transcript |
| EP3095460A4 (en) | 2014-01-15 | 2017-08-23 | Shin Nippon Biomedical Laboratories, Ltd. | Chiral nucleic acid adjuvant having anti-allergic activity, and anti-allergic agent |
| 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 |
| 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 |
| CA2968336C (en) | 2014-12-17 | 2021-11-23 | Proqr Therapeutics Ii B.V. | Construct for site directed editing of an adenosine nucleotide in target rna |
| US10793855B2 (en) * | 2015-01-06 | 2020-10-06 | 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 |
| CN108025089A (zh) | 2015-07-22 | 2018-05-11 | 波涛生命科学有限公司 | 寡核苷酸组合物及其方法 |
| WO2017067970A1 (en) | 2015-10-22 | 2017-04-27 | 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 |
| CN109477108A (zh) | 2016-05-04 | 2019-03-15 | 波涛生命科学有限公司 | 寡核苷酸组合物和其方法 |
| US11479818B2 (en) * | 2016-06-17 | 2022-10-25 | Hoffmann-La Roche Inc. | In vitro nephrotoxicity screening assay |
| EP3472346B1 (en) | 2016-06-17 | 2023-01-18 | F. Hoffmann-La Roche AG | Papd5 and papd7 inhibitors for treating a hepatitis b infection |
| WO2017216340A1 (en) * | 2016-06-17 | 2017-12-21 | F. Hoffmann-La Roche Ag | In vitro nephrotoxicity screening assay |
| 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 |
| EP3507366B1 (en) | 2016-09-01 | 2020-10-07 | ProQR Therapeutics II B.V. | Chemically modified single-stranded rna-editing oligonucleotides |
| CN114621302A (zh) * | 2016-11-14 | 2022-06-14 | 学校法人东京理科大学 | 聚合性化合物、化合物、及硼烷磷酸酯低聚物的制造方法 |
| JP7296882B2 (ja) | 2016-11-23 | 2023-06-23 | ウェイブ ライフ サイエンシズ リミテッド | ホスホラミダイト及びオリゴヌクレオチド合成のための組成物及び方法 |
| WO2018130583A1 (en) * | 2017-01-13 | 2018-07-19 | 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 |
| 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 |
| HRP20250804T1 (hr) | 2017-12-01 | 2025-09-12 | The Texas A&M University System | Antisense liječenje angelmanovog sindroma |
| US20200339982A1 (en) * | 2017-12-22 | 2020-10-29 | Roche Innovation Center Copenhagen A/S | Oligonucleotides comprising a phosphorodithioate internucleoside linkage |
| KR20200104302A (ko) * | 2017-12-22 | 2020-09-03 | 로슈 이노베이션 센터 코펜하겐 에이/에스 | 신규 티오포스포르아미다이트 |
| KR20200104347A (ko) * | 2017-12-22 | 2020-09-03 | 로슈 이노베이션 센터 코펜하겐 에이/에스 | 포스포로디티오에이트 인터뉴클레오시드 연결을 포함하는 갭머 올리고뉴클레오티드 |
| MX2020007433A (es) | 2018-01-12 | 2020-09-14 | Bristol Myers Squibb Co | Oligonucleotidos antisentido que actuan sobre alfa-sinucleina, y usos de estos. |
| EA202091693A1 (ru) | 2018-01-12 | 2021-04-14 | Бристол-Маерс Сквибб Компани | Антисмысловые олигонуклеотиды, целенаправленно воздействующие на альфа-синуклеин, и их применения |
| EP3774824A1 (en) | 2018-04-13 | 2021-02-17 | Bristol-Myers Squibb Company | Novel 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 |
| PE20220013A1 (es) | 2018-07-03 | 2022-01-11 | Hoffmann La Roche | Oligonucleotidos para modular la expresion de tau |
| CN112469827B (zh) * | 2018-07-04 | 2024-05-24 | 学校法人爱知医科大学 | 控制Tau的剪接的反义寡核苷酸及其用途 |
| CN113490742A (zh) * | 2019-02-20 | 2021-10-08 | 罗氏创新中心哥本哈根有限公司 | 膦酰基乙酸酯缺口聚物寡核苷酸 |
| US11466274B2 (en) | 2019-05-31 | 2022-10-11 | Aligos Therapeutics, Inc. | Modified gapmer oligonucleotides and methods of use |
| WO2021146391A1 (en) | 2020-01-16 | 2021-07-22 | Bristol-Myers Squibb Company | Reagents and their use for modular enantiodivergent synthesis of c–p bonds |
| AU2022242781A1 (en) * | 2021-03-26 | 2023-10-26 | Neumirna Therapeutics Aps | Microrna-27b inhibitors |
| 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 |
| DK2092065T4 (da) * | 2006-10-18 | 2019-10-21 | Ionis Pharmaceuticals Inc | Antisense-forbindelser |
| KR20240148947A (ko) * | 2012-07-13 | 2024-10-11 | 웨이브 라이프 사이언시스 리미티드 | 키랄 제어 |
| DK2951305T3 (en) * | 2013-01-30 | 2018-10-29 | Hoffmann La Roche | LNA oligonucleotide KULHYDRATKONJUGATER |
-
2015
- 2015-11-18 JP JP2017526918A patent/JP2017536119A/ja active Pending
- 2015-11-18 US US15/527,832 patent/US20180112217A1/en not_active Abandoned
- 2015-11-18 EP EP15797651.5A patent/EP3221329A1/en not_active Withdrawn
- 2015-11-18 US US15/527,765 patent/US20180016575A1/en not_active Abandoned
- 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 WO PCT/EP2015/076971 patent/WO2016079183A1/en not_active Ceased
- 2015-11-18 WO PCT/EP2015/076967 patent/WO2016079181A1/en not_active Ceased
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