JP2017536119A - 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 - Google Patents

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 Download PDF

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JP2017536119A
JP2017536119A JP2017526918A JP2017526918A JP2017536119A JP 2017536119 A JP2017536119 A JP 2017536119A JP 2017526918 A JP2017526918 A JP 2017526918A JP 2017526918 A JP2017526918 A JP 2017526918A JP 2017536119 A JP2017536119 A JP 2017536119A
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lna
phosphorothioate
nucleoside
oligonucleotide
region
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JP2017536119A5 (enExample
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ナンナ アルベク
ナンナ アルベク
ヘンリック フリデンランド ハンセン
ヘンリック フリデンランド ハンセン
コッホ　トロールス
トロールス コッホ
ジェイコブ ラバン
ジェイコブ ラバン
クリストフ ローゼンバーム
クリストフ ローゼンバーム
ピーター ヘッジドーン
ピーター ヘッジドーン
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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
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
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    • C12N2310/00—Structure or type of the nucleic acid
    • C12N2310/30—Chemical structure
    • C12N2310/31—Chemical structure of the backbone
    • C12N2310/315—Phosphorothioates
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    • C12N2310/32—Chemical structure of the sugar
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    • C12N2310/341—Gapmers, i.e. of the type ===---===
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  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Saccharide Compounds (AREA)
  • Enzymes And Modification Thereof (AREA)
  • Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)
JP2017526918A 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 Pending JP2017536119A (ja)

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
EP15191076 2015-10-22
EP15191075 2015-10-22
EP15191075.9 2015-10-22
EP15191074.2 2015-10-22
EP15191074 2015-10-22
PCT/EP2015/076967 WO2016079181A1 (en) 2014-11-19 2015-11-18 Lna gapmer oligonucleotides comprising chiral phosphorothioate linkages

Publications (2)

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JP2017536119A true JP2017536119A (ja) 2017-12-07
JP2017536119A5 JP2017536119A5 (enExample) 2018-11-15

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JP2017526905A Pending JP2017536366A (ja) 2014-11-19 2015-11-18 Ｌｎａキラルホスホロチオエート

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EP (2) EP3220921A1 (enExample)
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Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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

Families Citing this family (44)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RU2015151857A (ru) 2008-12-02 2019-01-15 Уэйв Лайф Сайенсес Джапан, Инк. Способ синтеза модифицированных по атому фосфора нуклеиновых кислот
MX342945B (es) 2009-07-06 2016-10-18 Ontorii Inc * Profármacos de ácido nucleico novedosos y métodos de uso de los mismos.
US10428019B2 (en) 2010-09-24 2019-10-01 Wave Life Sciences Ltd. Chiral auxiliaries
EP3248982A1 (en) 2011-07-19 2017-11-29 Wave Life Sciences Ltd. Thiosulfonate reagents for the synthesis of functionalized nucleic acids
CA2879023C (en) 2012-07-13 2017-03-28 Wave Life Sciences Japan Asymmetric auxiliary group
CA2879066C (en) 2012-07-13 2019-08-13 Shin Nippon Biomedical Laboratories, Ltd. Chiral nucleic acid adjuvant
CN104661664B (zh) 2012-07-13 2020-07-03 波涛生命科学有限公司 手性控制
US11162096B2 (en) 2013-10-14 2021-11-02 Ionis Pharmaceuticals, Inc Methods for modulating expression of C9ORF72 antisense transcript
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
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
US10322173B2 (en) 2014-01-15 2019-06-18 Shin Nippon Biomedical Laboratories, Ltd. Chiral nucleic acid adjuvant having anti-allergic activity, and anti-allergic agent
MX2016009290A (es) 2014-01-16 2017-02-28 Wave Life Sciences Ltd Diseño quiral.
DK3234134T3 (da) 2014-12-17 2020-07-27 Proqr Therapeutics Ii Bv Målrettet rna-redigering
WO2016112132A1 (en) * 2015-01-06 2016-07-14 Ionis Pharmaceuticals, Inc. Compositions for modulating expression of c9orf72 antisense transcript
US10407678B2 (en) 2015-04-16 2019-09-10 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
US10955407B2 (en) 2015-10-22 2021-03-23 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
JP7012033B2 (ja) * 2016-06-17 2022-02-10 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
EP3472348B1 (en) * 2016-06-17 2022-06-29 F. Hoffmann-La Roche AG In vitro nephrotoxicity screening assay
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
WO2017220751A1 (en) 2016-06-22 2017-12-28 Proqr Therapeutics Ii B.V. Single-stranded rna-editing oligonucleotides
ES2837076T3 (es) 2016-09-01 2021-06-29 Proqr Therapeutics Ii Bv Oligonucleótidos para la edición de ARN de cadena sencilla modificados químicamente
WO2018088491A1 (ja) 2016-11-14 2018-05-17 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
WO2018098264A1 (en) * 2016-11-23 2018-05-31 Wave Life Sciences Ltd. Compositions and methods for phosphoramidite and oligonucleotide synthesis
US20190367920A1 (en) * 2017-01-13 2019-12-05 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
US11274300B2 (en) 2017-01-19 2022-03-15 Proqr Therapeutics Ii B.V. Oligonucleotide complexes for use in RNA editing
JP2021502059A (ja) 2017-10-13 2021-01-28 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 部分的に立体定義されたオリゴヌクレオチドのサブライブラリーを使用することによる、アンチセンスオリゴヌクレオチドの、改良された立体定義されたホスホロチオエートオリゴヌクレオチド変異体を同定するための方法
AU2018350693B2 (en) 2017-10-16 2021-03-04 F. Hoffmann-La Roche Ag Nucleic acid molecule for reduction of PAPD5 and PAPD7 mRNA for treating hepatitis B infection
BR112020009431A2 (pt) 2017-12-01 2020-10-13 The Texas A&M University System tratamento antisense da síndrome de angelman
CN111757936B (zh) * 2017-12-22 2025-07-04 罗氏创新中心哥本哈根有限公司 包含二硫代磷酸酯核苷间连接的寡核苷酸
US11597926B2 (en) 2017-12-22 2023-03-07 Roche Innovation Center Copenhagen A/S Thiophosphoramidites
US20200332289A1 (en) * 2017-12-22 2020-10-22 Roche Innovation Center Copenhagen A/S Gapmer oligonucleotides comprising a phosphorodithioate internucleoside linkage
KR102839166B1 (ko) 2018-01-12 2025-07-28 브리스톨-마이어스 스큅 컴퍼니 알파-시누클레인을 표적화하는 안티센스 올리고뉴클레오티드 및 그의 용도
CA3088112A1 (en) 2018-01-12 2019-07-18 Bristol-Myers Squibb Company Antisense oligonucleotides targeting alpha-synuclein and uses thereof
MX2020009416A (es) 2018-04-13 2021-01-08 Bristol Myers Squibb Co Nuevos reactivos a base de fosforo (v), procesos para su preparacion y su uso en la elaboracion de compuestos de organofosforo (v) estereo-definidos.
GB201808146D0 (en) 2018-05-18 2018-07-11 Proqr Therapeutics Ii Bv Stereospecific Linkages in RNA Editing Oligonucleotides
MY206038A (en) 2018-07-03 2024-11-26 Hoffmann La Roche Oligonucleotides for modulating tau expression
JP7340794B2 (ja) * 2018-07-04 2023-09-08 学校法人 愛知医科大学 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
SG11202112741XA (en) 2019-05-31 2021-12-30 Aligos Therapeutics Inc Modified gapmer oligonucleotides and methods of use
BR112022012340A2 (pt) 2020-01-16 2022-09-06 Bristol Myers Squibb Co Reagentes e uso dos mesmos para síntese enantiodivergente modular de ligações c-p
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

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2010507579A (ja) * 2006-10-18 2010-03-11 アイシス ファーマシューティカルズ， インコーポレーテッド アンチセンス化合物
WO2014012081A2 (en) * 2012-07-13 2014-01-16 Ontorii, Inc. Chiral control

Family Cites Families (2)

* Cited by examiner, † Cited by third party
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
RU2649367C2 (ru) * 2013-01-30 2018-04-02 Ф. Хоффманн-Ля Рош Аг Конъюгаты углевода и lna-олигонуклеотида

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2010507579A (ja) * 2006-10-18 2010-03-11 アイシス ファーマシューティカルズ， インコーポレーテッド アンチセンス化合物
WO2014012081A2 (en) * 2012-07-13 2014-01-16 Ontorii, Inc. Chiral control

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
NUCLEIC ACIDS RES., vol. 42, no. 22, JPN6019032985, 14 November 2014 (2014-11-14), pages 13456 - 13468, ISSN: 0004237397 *

Cited By (1)

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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

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EP3220921A1 (en) 2017-09-27
WO2016079181A1 (en) 2016-05-26
JP2017536366A (ja) 2017-12-07
WO2016079183A1 (en) 2016-05-26
US20180016575A1 (en) 2018-01-18
EP3221329A1 (en) 2017-09-27
US20180112217A1 (en) 2018-04-26

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