JP4402454B2 - Lnaホスホラミダイトの製造法 - Google Patents
Lnaホスホラミダイトの製造法 Download PDFInfo
- Publication number
- JP4402454B2 JP4402454B2 JP2003512245A JP2003512245A JP4402454B2 JP 4402454 B2 JP4402454 B2 JP 4402454B2 JP 2003512245 A JP2003512245 A JP 2003512245A JP 2003512245 A JP2003512245 A JP 2003512245A JP 4402454 B2 JP4402454 B2 JP 4402454B2
- Authority
- JP
- Japan
- Prior art keywords
- lna
- phosphoramidite
- cyanoethyl
- ribo
- dci
- 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.)
- Expired - Lifetime
Links
- 0 B[C@@](C1OC2)OC2(C*)C1OP(N(C(C)C)C(C)C)OCCC#N Chemical compound B[C@@](C1OC2)OC2(C*)C1OP(N(C(C)C)C(C)C)OCCC#N 0.000 description 1
Images
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
- C07H1/00—Processes for the preparation of sugar derivatives
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
- C07H1/00—Processes for the preparation of sugar derivatives
- C07H1/02—Phosphorylation
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
- C07H19/00—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
- C07H19/02—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
- C07H19/04—Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
- C07H19/06—Pyrimidine radicals
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
- C07H19/00—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
- C07H19/02—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
- C07H19/04—Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
- C07H19/16—Purine radicals
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Engineering & Computer Science (AREA)
- Biochemistry (AREA)
- Biotechnology (AREA)
- General Health & Medical Sciences (AREA)
- Genetics & Genomics (AREA)
- Molecular Biology (AREA)
- Luminescent Compositions (AREA)
- Saccharide Compounds (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DKPA200101095 | 2001-07-12 | ||
| PCT/DK2002/000488 WO2003006475A2 (en) | 2001-07-12 | 2002-07-12 | Method for preparation of lna phosphoramidites |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2004536125A JP2004536125A (ja) | 2004-12-02 |
| JP2004536125A5 JP2004536125A5 (https=) | 2006-01-05 |
| JP4402454B2 true JP4402454B2 (ja) | 2010-01-20 |
Family
ID=8160624
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2003512245A Expired - Lifetime JP4402454B2 (ja) | 2001-07-12 | 2002-07-12 | Lnaホスホラミダイトの製造法 |
Country Status (7)
| Country | Link |
|---|---|
| EP (1) | EP1409497B1 (https=) |
| JP (1) | JP4402454B2 (https=) |
| AT (1) | ATE287413T1 (https=) |
| AU (1) | AU2002328792A1 (https=) |
| DE (1) | DE60202681T2 (https=) |
| DK (1) | DK1409497T3 (https=) |
| WO (1) | WO2003006475A2 (https=) |
Families Citing this family (71)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2003085110A2 (en) | 2002-04-05 | 2003-10-16 | Santaris Pharma A/S | Oligomeric compounds for the modulation hif-1alpha expression |
| US7713738B2 (en) | 2003-02-10 | 2010-05-11 | Enzon Pharmaceuticals, Inc. | Oligomeric compounds for the modulation of survivin expression |
| PT1592793E (pt) | 2003-02-10 | 2009-09-30 | Santaris Pharma As | Compostos oligoméricos para a modulação da expressão de survivina |
| CA2519860C (en) | 2003-03-21 | 2018-01-16 | Santaris Pharma A/S | Short interfering rna (sirna) analogues |
| RU2377301C2 (ru) | 2003-12-23 | 2009-12-27 | Сантарис Фарма А/С | ОЛИГОМЕРНОЕ СОЕДИНЕНИЕ, ПОНИЖАЮЩЕЕ ЭКСПРЕССИЮ ЧЕЛОВЕЧЕСКОГО ГЕНА Bcl-2, КОНЪЮГАТ, ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ И ПРИМЕНЕНИЕ ОЛИГОМЕРНОГО СОЕДИНЕНИЯ ДЛЯ ЛЕЧЕНИЯ РАКА |
| US9447138B2 (en) | 2004-11-09 | 2016-09-20 | Roche Innovation Center Copenhagen A/S | Potent LNA oligonucleotides for the inhibition of HIF-1a expression |
| KR20070095882A (ko) | 2004-11-09 | 2007-10-01 | 산타리스 팔마 에이/에스 | Lna 올리고뉴클레오티드 및 암의 치료 |
| AU2005304112B2 (en) | 2004-11-09 | 2009-06-04 | Roche Innovation Center Copenhagen A/S | Potent LNA oligonucleotides for the inhibition of HIF-1a expression |
| EP1971371B1 (en) | 2005-12-01 | 2015-08-05 | Pronai Therapeutics, Inc. | Cancer therapies and pharmaceutical compositions used therein |
| WO2007107162A2 (en) | 2006-03-23 | 2007-09-27 | Santaris Pharma A/S | Small internally segmented interfering rna |
| EP2666859B1 (en) | 2006-04-03 | 2019-01-02 | Roche Innovation Center Copenhagen A/S | Pharmaceutical composition comprising anti-mirna antisense oligonucleotides |
| CA2648132C (en) | 2006-04-03 | 2019-05-28 | Santaris Pharma A/S | Pharmaceutical composition comprising anti-mirna antisense oligonucleotides |
| CA2681406A1 (en) | 2007-03-22 | 2008-09-25 | Santaris Pharma A/S | Rna antagonist compounds for the inhibition of apo-b100 expression |
| WO2008113832A2 (en) | 2007-03-22 | 2008-09-25 | Santaris Pharma A/S | SHORT RNA ANTAGONIST COMPOUNDS FOR THE MODULATION OF TARGET mRNA |
| ES2798758T3 (es) | 2007-06-06 | 2020-12-14 | Sarepta Therapeutics Inc | Proteínas variantes de empalme her2 y her3 solubles, oligonucleótidos de cambio de empalme y su uso en el tratamiento de enfermedades |
| WO2009027978A1 (en) | 2007-08-30 | 2009-03-05 | Hadasit Medical Research Services & Development Ltd. | NUCLEIC ACID SEQUENCES COMPRISING NF-ϰB BINDING SITE WITHIN O(6)-METHYLGUANINE-DNA-METHYLTRANSFERASE (MGMT) PROMOTER REGION AND USES THEREOF FOR THE TREATMENT OF CANCER AND IMMUNE-RELATED DISORDERS |
| EP2623599B1 (en) | 2007-10-04 | 2019-01-02 | Roche Innovation Center Copenhagen A/S | Micromirs |
| EP2212437A4 (en) | 2007-11-07 | 2011-09-28 | Univ British Columbia | MICROFLUIDIC DEVICE AND METHOD OF USING THE DEVICE |
| EP2268811A1 (en) | 2008-03-07 | 2011-01-05 | Santaris Pharma A/S | Pharmaceutical compositions for treatment of microrna related diseases |
| ES2541442T3 (es) | 2008-08-01 | 2015-07-20 | Roche Innovation Center Copenhagen A/S | Modulación mediada por microARN de factores estimulantes de colonias |
| ES2599979T3 (es) | 2009-04-24 | 2017-02-06 | Roche Innovation Center Copenhagen A/S | Composiciones farmacéuticas para el tratamiento de pacientes de VHC que no responden al interferón |
| US8563528B2 (en) | 2009-07-21 | 2013-10-22 | Santaris Pharma A/S | Antisense oligomers targeting PCSK9 |
| WO2011105900A2 (en) | 2010-02-23 | 2011-09-01 | Academisch Ziekenhuis Bij De Universiteit Van Amsterdam | Antagonists of complement component 8-alpha (c8-alpha) and uses thereof |
| WO2011105901A2 (en) | 2010-02-23 | 2011-09-01 | Academisch Ziekenhuis Bij De Universiteit Van Amsterdam | Antagonists of complement component 9 (c9) and uses thereof |
| WO2011105902A2 (en) | 2010-02-23 | 2011-09-01 | Academisch Ziekenhuis Bij De Universiteit Van Amsterdam | Antagonists of complement component 8-beta (c8-beta) and uses thereof |
| GB201012418D0 (en) | 2010-07-23 | 2010-09-08 | Santaris Pharma As | Process |
| WO2012027206A1 (en) | 2010-08-24 | 2012-03-01 | Merck Sharp & Dohme Corp. | SINGLE-STRANDED RNAi AGENTS CONTAINING AN INTERNAL, NON-NUCLEIC ACID SPACER |
| BR112015010220A2 (pt) | 2012-11-05 | 2017-12-05 | Pronai Therapeutics Inc | métodos de utilização de biomarcadores para tratamento de câncer |
| WO2014108759A1 (en) | 2013-01-14 | 2014-07-17 | Pierfrancesco Tassone | INHIBITORS OF miRNAs 221 AND 222 FOR ANTI-TUMOR ACTIVITY IN MULTIPLE MYELOMA |
| ES2770667T3 (es) | 2013-06-27 | 2020-07-02 | Roche Innovation Ct Copenhagen As | Oligómeros antisentido y conjugados que se dirigen a PCSK9 |
| WO2015075166A1 (en) | 2013-11-22 | 2015-05-28 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Methods and pharmaceutical compositions for treatment of a bacterial infection |
| US9765332B2 (en) | 2014-01-29 | 2017-09-19 | Inserm (Institut National De La Sante Et De La Recherche Medicale) | Oligonucleotides and methods for inhibiting or reducing bacterial biofilms |
| GB201410693D0 (en) | 2014-06-16 | 2014-07-30 | Univ Southampton | Splicing modulation |
| WO2016041058A1 (en) | 2014-09-18 | 2016-03-24 | The University Of British Columbia | Allele-specific therapy for huntington disease haplotypes |
| CN107109411B (zh) | 2014-10-03 | 2022-07-01 | 冷泉港实验室 | 核基因输出的定向增加 |
| JP6835826B2 (ja) * | 2015-08-24 | 2021-02-24 | 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 | Lna−gプロセス |
| EP3359685B1 (en) | 2015-10-09 | 2026-01-28 | University Of Southampton | Modulation of gene expression for deregulated protein expression |
| EP3933041B1 (en) | 2015-12-14 | 2024-01-31 | Cold Spring Harbor Laboratory | Antisense oligomers for treatment of autosomal dominant retardation |
| US11096956B2 (en) | 2015-12-14 | 2021-08-24 | Stoke Therapeutics, Inc. | Antisense oligomers and uses thereof |
| WO2018024849A1 (en) | 2016-08-03 | 2018-02-08 | Aalborg Universitet | ANTISENSE OLIGONUCLEOTIDES (ASOs) DESIGNED TO INHIBIT IMMUNE CHECKPOINT PROTEINS |
| SG11202001590RA (en) | 2017-08-25 | 2020-03-30 | Stoke Therapeutics Inc | Antisense oligomers for treatment of conditions and diseases |
| WO2019076919A1 (en) | 2017-10-17 | 2019-04-25 | INSERM (Institut National de la Santé et de la Recherche Médicale) | COMBINED TREATMENT OF CYSTIC FIBROSIS |
| US12060558B2 (en) | 2018-05-04 | 2024-08-13 | Stoke Therapeutics, Inc. | Methods and compositions for treatment of cholesteryl ester storage disease |
| KR20210134003A (ko) | 2019-02-27 | 2021-11-08 | 스톡 테라퓨틱스, 인크. | 병태 및 질환의 치료를 위한 안티센스 올리고머 |
| US20220251567A1 (en) | 2019-07-10 | 2022-08-11 | Inserm (Institut National De La Santè Et De La Recherche Médicale) | Methods for the treatment of epilepsy |
| IT201900017234A1 (it) | 2019-09-25 | 2021-03-25 | Int Centre For Genetic Engineering And Biotechnology | Anti-miRNA per il trattamento del leiomioma |
| WO2021074657A1 (en) | 2019-10-17 | 2021-04-22 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Combination treatment for cystic fibrosis |
| IL292286A (en) * | 2019-10-18 | 2022-06-01 | Daiichi Sankyo Co Ltd | Production method for bicyclic phosphoramidite |
| CA3161586A1 (en) * | 2019-11-13 | 2021-05-20 | Nippon Shinyaku Co., Ltd. | Method for producing oligonucleic acid compound |
| US20230016983A1 (en) | 2019-11-19 | 2023-01-19 | lNSERM (INSTITUT NATIONAL DE LA SANTÉ ET DE LA RECHERCHE MÉDICALE) | Antisense oligonucleotides and thier use for the treatment of cancer |
| BR112022022889A2 (pt) | 2020-05-11 | 2023-04-04 | Stoke Therapeutics Inc | Oligômeros antissentido de opa1 para tratamento de condições e doenças |
| KR20230050336A (ko) | 2020-07-10 | 2023-04-14 | 인스티튜트 내셔널 드 라 싼테 에 드 라 리셰르셰 메디칼르 (인 썸) | 뇌전증을 치료하기 위한 방법과 조성물 |
| WO2022124410A1 (ja) * | 2020-12-11 | 2022-06-16 | ヤマサ醤油株式会社 | シトシン型架橋型ヌクレオシドアミダイト結晶及びその製造方法 |
| IL304956A (en) | 2021-02-12 | 2023-10-01 | Merand Pharmaceuticals Inc | Agents, compositions, and methods for the treatment of hypoxia and ischemia-related disorders |
| US20240182889A1 (en) | 2021-03-26 | 2024-06-06 | Neumirna Therapeutics Aps | Microrna-27b inhibitors |
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| EP4389892A4 (en) | 2021-08-17 | 2025-12-10 | Korea Advanced Inst Sci & Tech | Antisense oligonucleotide targeting the CAV3.1 gene and its uses |
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| JP7772362B2 (ja) * | 2021-12-21 | 2025-11-18 | シンクレスト株式会社 | 人工核酸モノマーの製造方法 |
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| EP4332239A1 (en) | 2022-08-30 | 2024-03-06 | Istituto Romagnolo per lo Studio dei Tumori "Dino Amadori" - IRST S.r.l. | Mir-based assay for gastro-entero-pancreatic neuroendocrine tumor diagnosis and prognosis |
| EP4646478A1 (en) | 2023-01-06 | 2025-11-12 | Institut National de la Santé et de la Recherche Médicale | Intravenous administration of antisense oligonucleotides for the treatment of pain |
| EP4450626A1 (en) | 2023-04-21 | 2024-10-23 | IFOM - Istituto Fondazione di Oncologia Molecolare ETS | Fnip2 inhibitors for treating ataxia telangiectasia |
| WO2025008406A1 (en) | 2023-07-04 | 2025-01-09 | Institut National de la Santé et de la Recherche Médicale | Antisense oligonucleotides and their use for the treatment of cancer |
| EP4512899A1 (en) | 2023-08-23 | 2025-02-26 | Lipigon Pharmaceuticals AB | Angptl4 aso compositions for treatment of atherosclerosis in humans |
| CN117233282B (zh) * | 2023-09-14 | 2024-12-20 | 上海奥锐特生物科技有限公司 | 2-氰乙基-n,n,n’,n’-四异丙基亚磷酰二胺的检测方法 |
| WO2025237990A1 (en) | 2024-05-14 | 2025-11-20 | Institut National de la Santé et de la Recherche Médicale | Antisense oligonucleotides and their use for the treatment of pulmonary fibrosis |
| WO2026061986A1 (en) | 2024-09-17 | 2026-03-26 | Institut National de la Santé et de la Recherche Médicale | Antisense oligonucleotide (aso)-mediated down-regulation of cd33 to safely enrich for genetically modified cells |
| WO2026068729A1 (en) | 2024-09-26 | 2026-04-02 | Neumirna Therapeutics Aps | Antimir-27b for treatment of parkinson's disease |
Family Cites Families (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU4800197A (en) * | 1996-10-15 | 1998-05-11 | Nexstar Pharmaceuticals, Inc. | Improved coupling activators for oligonucleotide synthesis |
-
2002
- 2002-07-12 AU AU2002328792A patent/AU2002328792A1/en not_active Abandoned
- 2002-07-12 EP EP02764561A patent/EP1409497B1/en not_active Expired - Lifetime
- 2002-07-12 DK DK02764561T patent/DK1409497T3/da active
- 2002-07-12 WO PCT/DK2002/000488 patent/WO2003006475A2/en not_active Ceased
- 2002-07-12 AT AT02764561T patent/ATE287413T1/de not_active IP Right Cessation
- 2002-07-12 JP JP2003512245A patent/JP4402454B2/ja not_active Expired - Lifetime
- 2002-07-12 DE DE60202681T patent/DE60202681T2/de not_active Expired - Lifetime
Also Published As
| Publication number | Publication date |
|---|---|
| EP1409497A2 (en) | 2004-04-21 |
| EP1409497B1 (en) | 2005-01-19 |
| DE60202681D1 (de) | 2005-02-24 |
| WO2003006475A3 (en) | 2004-02-26 |
| WO2003006475A2 (en) | 2003-01-23 |
| ATE287413T1 (de) | 2005-02-15 |
| DK1409497T3 (da) | 2005-05-30 |
| AU2002328792A1 (en) | 2003-01-29 |
| JP2004536125A (ja) | 2004-12-02 |
| DE60202681T2 (de) | 2006-01-12 |
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Free format text: JAPANESE INTERMEDIATE CODE: R250 |
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