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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Publication of JP2017536119A publication Critical patent/JP2017536119A/ja
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    • C12N2310/00—Structure or type of the nucleic acid
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    • C12N2310/31—Chemical structure of the backbone
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  • Enzymes And Modification Thereof (AREA)
  • Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)
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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
EP14193887.8 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
EP15191074.2 2015-10-22
EP15191075 2015-10-22
EP15191074 2015-10-22
EP15191076 2015-10-22
EP15191076.7 2015-10-22
EP15191075.9 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
ES2616051T3 (es) 2008-12-02 2017-06-09 Wave Life Sciences Japan, Inc. Método para la síntesis de ácidos nucleicos modificados en el átomo de fósforo
CA2767253A1 (en) 2009-07-06 2011-01-13 Ontorii, Inc. Novel nucleic acid prodrugs and methods of use thereof
EP2620428B1 (en) 2010-09-24 2019-05-22 Wave Life Sciences Ltd. Asymmetric auxiliary group
JP6128529B2 (ja) 2011-07-19 2017-05-17 ウェイブ ライフ サイエンシズ リミテッドＷａｖｅ Ｌｉｆｅ Ｓｃｉｅｎｃｅｓ Ｌｔｄ． 官能化核酸の合成のための方法
US9982257B2 (en) 2012-07-13 2018-05-29 Wave Life Sciences Ltd. Chiral control
MX356830B (es) 2012-07-13 2018-06-15 Shin Nippon Biomedical Laboratories Ltd Adyuvante de acido nucleico quiral.
US9598458B2 (en) 2012-07-13 2017-03-21 Wave Life Sciences Japan, Inc. Asymmetric auxiliary group
US11162096B2 (en) 2013-10-14 2021-11-02 Ionis Pharmaceuticals, Inc Methods for modulating expression of C9ORF72 antisense transcript
EP3095459A4 (en) 2014-01-15 2017-08-23 Shin Nippon Biomedical Laboratories, Ltd. Chiral nucleic acid adjuvant having antitumor effect and antitumor agent
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
WO2015108046A1 (ja) 2014-01-15 2015-07-23 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
DK3094728T3 (da) 2014-01-16 2022-05-16 Wave Life Sciences Ltd Kiralt design
JP6718872B2 (ja) 2014-12-17 2020-07-08 プロキューアール・セラピューティクス・セカンド・ベスローテン・フェンノートシャップＰｒｏＱＲ Ｔｈｅｒａｐｅｕｔｉｃｓ ＩＩ Ｂ．Ｖ． 標的化ｒｎａ編集
US10793855B2 (en) * 2015-01-06 2020-10-06 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
EP3430021A1 (en) * 2016-03-18 2019-01-23 Roche Innovation Center Copenhagen A/S Acyl-protected l-lna-guanosine monomers
MA45270A (fr) 2016-05-04 2017-11-09 Wave Life Sciences Ltd Compositions d'oligonucléotides et procédés associés
US11479818B2 (en) * 2016-06-17 2022-10-25 Hoffmann-La Roche Inc. In vitro nephrotoxicity screening assay
US11105794B2 (en) * 2016-06-17 2021-08-31 Hoffmann-La Roche Inc. 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
JP7074345B2 (ja) 2016-06-22 2022-05-24 プロキューアール セラピューティクス ツー ベスローテン フェンノートシャップ 一本鎖ｒｎａ編集オリゴヌクレオチド
IL264923B2 (en) 2016-09-01 2025-07-01 Proqr Therapeutics Ii Bv Single-stranded RNA-editing oligonucleotides with chemical modifications
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
CN110088113A (zh) * 2016-11-23 2019-08-02 波涛生命科学有限公司 用于亚磷酰胺和寡核苷酸合成的组合物和方法
US20190345496A1 (en) * 2017-01-13 2019-11-14 Roche Innovation Center Copenhagen A/S Antisense oligonucleotides for modulating relb expression
US20190367920A1 (en) * 2017-01-13 2019-12-05 Roche Innovation Center Copenhagen A/S Antisense oligonucleotides for modulating nfkb1 expression
US11274300B2 (en) 2017-01-19 2022-03-15 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
CN111511914B (zh) * 2017-10-16 2023-11-17 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
SMT202500334T1 (it) 2017-12-01 2025-11-10 Texas A & M Univ Sys Trattamento antisenso della sindrome di angelman
BR112020010090A2 (pt) * 2017-12-22 2020-11-03 Roche Innovation Center Copenhagen A/S oligonucleotídeo gapmer, sal farmaceuticamente aceitável do mesmo, conjugado, composição farmacêutica e uso dos mesmos
TW201929870A (zh) * 2017-12-22 2019-08-01 丹麥商羅氏創新中心哥本哈根有限公司 包含二硫代磷酸酯核苷間連結之寡核苷酸
EP3728590B1 (en) * 2017-12-22 2025-07-02 Roche Innovation Center Copenhagen A/S Novel thiophosphoramidites
MX2020007439A (es) * 2018-01-12 2020-09-14 Bristol Myers Squibb Co Oligonucleotidos antisentido que actuan sobre alfa-sinucleina y usos de estos.
CA3088112A1 (en) 2018-01-12 2019-07-18 Bristol-Myers Squibb Company Antisense oligonucleotides targeting alpha-synuclein and uses thereof
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
CA3247235A1 (en) 2018-07-03 2025-11-29 F. Hoffmann-La Roche Ag 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
US11466274B2 (en) 2019-05-31 2022-10-11 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
KR20250069923A (ko) 2022-09-19 2025-05-20 브리스톨-마이어스 스큅 컴퍼니 신규한 인(v)-기반 시약, 이의 제조 방법, 및 입체-규정 유기인(v) 화합물의 제조에 있어서의 그의 용도

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
MX2015009056A (es) * 2013-01-30 2015-10-05 Hoffmann La Roche Conjugados de oligonucleotidos de acido nucleico bloqueado y carbohidratos.

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

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