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 | ||
| EP15191075 | 2015-10-22 | ||
| EP15191074 | 2015-10-22 | ||
| EP15191074.2 | 2015-10-22 | ||
| EP15191075.9 | 2015-10-22 | ||
| EP15191076.7 | 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 (OSRAM) | 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) | US20180112217A1 (OSRAM) |
| EP (2) | EP3221329A1 (OSRAM) |
| JP (2) | JP2017536366A (OSRAM) |
| WO (2) | WO2016079183A1 (OSRAM) |
Families Citing this family (45)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2744987C (en) | 2008-12-02 | 2018-01-16 | Chiralgen, Ltd. | Method for the synthesis of phosphorus atom modified nucleic acids |
| CA2767253A1 (en) | 2009-07-06 | 2011-01-13 | Ontorii, Inc. | Novel nucleic acid prodrugs and methods of use thereof |
| WO2012039448A1 (ja) | 2010-09-24 | 2012-03-29 | 株式会社キラルジェン | 不斉補助基 |
| WO2013012758A1 (en) | 2011-07-19 | 2013-01-24 | Ontorii, Inc. | Methods for the synthesis of functionalized nucleic acids |
| KR102712879B1 (ko) | 2012-07-13 | 2024-10-04 | 웨이브 라이프 사이언시스 리미티드 | 키랄 제어 |
| JP6268157B2 (ja) | 2012-07-13 | 2018-01-24 | 株式会社Ｗａｖｅ Ｌｉｆｅ Ｓｃｉｅｎｃｅｓ Ｊａｐａｎ | 不斉補助基 |
| 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 |
| 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 |
| US10144933B2 (en) | 2014-01-15 | 2018-12-04 | Shin Nippon Biomedical Laboratories, Ltd. | Chiral nucleic acid adjuvant having immunity induction activity, and immunity induction activator |
| EP4137572A1 (en) | 2014-01-16 | 2023-02-22 | Wave Life Sciences Ltd. | Chiral design |
| 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 |
| KR102372122B1 (ko) * | 2016-03-18 | 2022-03-07 | 로슈 이노베이션 센터 코펜하겐 에이/에스 | 아실-보호된 l-lna-구아노신 단량체 |
| MA45270A (fr) | 2016-05-04 | 2017-11-09 | Wave Life Sciences Ltd | Compositions d'oligonucléotides et procédés associés |
| 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 |
| CN109312403B (zh) * | 2016-06-17 | 2023-06-27 | 豪夫迈·罗氏有限公司 | 体外肾毒性筛选测定法 |
| WO2017216340A1 (en) * | 2016-06-17 | 2017-12-21 | F. Hoffmann-La Roche Ag | In vitro nephrotoxicity screening assay |
| US10988763B2 (en) | 2016-06-22 | 2021-04-27 | Proqr Therapeutics Ii B.V. | Single-stranded RNA-editing oligonucleotides |
| PL3507366T3 (pl) | 2016-09-01 | 2021-05-04 | Proqr Therapeutics Ii B.V. | Chemicznie modyfikowane jednoniciowe oligonukleotydy edytujące rna |
| CN109937206B (zh) * | 2016-11-14 | 2022-04-01 | 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 |
| US11873316B2 (en) | 2016-11-23 | 2024-01-16 | Wave Life Sciences Ltd. | Compositions and methods for phosphoramidite and oligonucleotide synthesis |
| EP3568479A1 (en) * | 2017-01-13 | 2019-11-20 | Roche Innovation Center Copenhagen A/S | Antisense oligonucleotides for modulating nfkb1 expression |
| US20190345496A1 (en) * | 2017-01-13 | 2019-11-14 | Roche Innovation Center Copenhagen A/S | Antisense oligonucleotides for modulating relb expression |
| WO2018134301A1 (en) | 2017-01-19 | 2018-07-26 | Proqr Therapeutics Ii B.V. | Oligonucleotide complexes for use in rna editing |
| WO2019073018A1 (en) | 2017-10-13 | 2019-04-18 | Roche Innovation Center Copenhagen A/S | METHODS OF IDENTIFYING ANTISENSE OLIGONUCLEOTIDE IMPROVED OLIGONUCLEOTIDE PHOSPHOROTHIOATE STEREODEFINIS VARIANTS USING PARTIALLY STEREODEFINIS OLIGONUCLEOTIDE SUB LIBRARIES |
| CN118048356A (zh) | 2017-10-16 | 2024-05-17 | 豪夫迈·罗氏有限公司 | 减少PAPD5和PAPD7 mRNA的核酸分子用于治疗乙型肝炎感染 |
| PT3717646T (pt) | 2017-12-01 | 2025-07-28 | Texas A & M Univ Sys | Tratamento antisense da síndrome de angelman |
| MX2020005754A (es) * | 2017-12-22 | 2020-08-20 | Roche Innovation Ct Copenhagen As | Oligonucleotidos gapmeros que comprenden un enlace internucleosido fosforoditioato. |
| EP4092118A1 (en) * | 2017-12-22 | 2022-11-23 | Roche Innovation Center Copenhagen A/S | Novel thiophosphoramidites |
| 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 |
| KR102839166B1 (ko) | 2018-01-12 | 2025-07-28 | 브리스톨-마이어스 스큅 컴퍼니 | 알파-시누클레인을 표적화하는 안티센스 올리고뉴클레오티드 및 그의 용도 |
| BR112020013994A2 (pt) | 2018-01-12 | 2020-12-08 | Bristol-Myers Squibb Company | Oligonucleotídeos antissenso que direcionam alfa-sinucleína e seus usos |
| 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 |
| PE20210346A1 (es) | 2018-07-03 | 2021-02-25 | Hoffmann La Roche | Oligonucleotidos para modular la expresion de tau |
| US20210230598A1 (en) * | 2018-07-04 | 2021-07-29 | National University Corporation Tokai National Higher Education And Research System | Oligonucleotides for controlling tau splicing, and uses thereof |
| AU2020225687A1 (en) * | 2019-02-20 | 2021-08-19 | Roche Innovation Center Copenhagen A/S | Phosphonoacetate gapmer oligonucleotides |
| CA3141874A1 (en) | 2019-05-31 | 2020-12-03 | Aligos Therapeutics, Inc. | Modified gapmer oligonucleotides and methods of use |
| CN115244061A (zh) | 2020-01-16 | 2022-10-25 | 百时美施贵宝公司 | 试剂及其用于模块化对映发散性合成c-p键的用途 |
| JP2025533488A (ja) | 2022-09-19 | 2025-10-07 | ブリストル－マイヤーズ スクイブ カンパニー | 新規なリン（ｖ）系試薬、その調製方法、及び立体的に規定された有機リン（ｖ）化合物の作製におけるそれらの使用 |
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 |
| CA2667055C (en) * | 2006-10-18 | 2017-05-09 | Isis Pharmaceuticals, Inc. | Antisense compounds |
| KR102712879B1 (ko) * | 2012-07-13 | 2024-10-04 | 웨이브 라이프 사이언시스 리미티드 | 키랄 제어 |
| US20150368642A1 (en) * | 2013-01-30 | 2015-12-24 | Hoffmann-La Roche Inc. | Lna oligonucleotide carbohydrate conjugates |
-
2015
- 2015-11-18 JP JP2017526905A patent/JP2017536366A/ja active Pending
- 2015-11-18 US US15/527,832 patent/US20180112217A1/en not_active Abandoned
- 2015-11-18 US US15/527,765 patent/US20180016575A1/en not_active Abandoned
- 2015-11-18 WO PCT/EP2015/076971 patent/WO2016079183A1/en not_active Ceased
- 2015-11-18 EP EP15797651.5A patent/EP3221329A1/en not_active Withdrawn
- 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 WO PCT/EP2015/076967 patent/WO2016079181A1/en not_active Ceased
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