AU2003222743B2 - Synthesis of locked nucleic acid derivatives - Google Patents

Synthesis of locked nucleic acid derivatives Download PDF

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Publication number
AU2003222743B2
AU2003222743B2 AU2003222743A AU2003222743A AU2003222743B2 AU 2003222743 B2 AU2003222743 B2 AU 2003222743B2 AU 2003222743 A AU2003222743 A AU 2003222743A AU 2003222743 A AU2003222743 A AU 2003222743A AU 2003222743 B2 AU2003222743 B2 AU 2003222743B2
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AU
Australia
Prior art keywords
lna
formula
compound
etoac
mmol
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
Application number
AU2003222743A
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English (en)
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AU2003222743A1 (en
Inventor
Signe M. Christensen
Troels Koch
Daniel Sejer Pedersen
Christoph Rosenbohm
Mads Detlef Sorensen
Jesper Wengel
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Roche Innovation Center Copenhagen AS
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Roche Innovation Center Copenhagen AS
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Publication date
Application filed by Roche Innovation Center Copenhagen AS filed Critical Roche Innovation Center Copenhagen AS
Publication of AU2003222743A1 publication Critical patent/AU2003222743A1/en
Assigned to SANTARIS PHARMA A/S reassignment SANTARIS PHARMA A/S Request for Assignment Assignors: EXIQON A/S, SANTARIS PHARMA A/S
Application granted granted Critical
Publication of AU2003222743B2 publication Critical patent/AU2003222743B2/en
Assigned to ROCHE INNOVATION CENTER COPENHAGEN A/S reassignment ROCHE INNOVATION CENTER COPENHAGEN A/S Request to Amend Deed and Register Assignors: SANTARIS PHARMA A/S
Anticipated expiration legal-status Critical
Expired legal-status Critical Current

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Classifications

    • 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

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Health & Medical Sciences (AREA)
  • Biochemistry (AREA)
  • Biotechnology (AREA)
  • General Health & Medical Sciences (AREA)
  • Genetics & Genomics (AREA)
  • Molecular Biology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Saccharide Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
AU2003222743A 2002-05-08 2003-05-08 Synthesis of locked nucleic acid derivatives Expired AU2003222743B2 (en)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
DKPA200200712 2002-05-08
DKPA200200712 2002-05-08
DKPA200201214 2002-08-16
DKPA200201214 2002-08-16
PCT/DK2003/000305 WO2003095467A1 (en) 2002-05-08 2003-05-08 Synthesis of locked nucleic acid derivatives

Publications (2)

Publication Number Publication Date
AU2003222743A1 AU2003222743A1 (en) 2003-11-11
AU2003222743B2 true AU2003222743B2 (en) 2008-12-11

Family

ID=29421786

Family Applications (1)

Application Number Title Priority Date Filing Date
AU2003222743A Expired AU2003222743B2 (en) 2002-05-08 2003-05-08 Synthesis of locked nucleic acid derivatives

Country Status (9)

Country Link
EP (1) EP1501848B1 (https=)
JP (1) JP4476802B2 (https=)
AT (1) ATE369375T1 (https=)
AU (1) AU2003222743B2 (https=)
CA (1) CA2484526C (https=)
DE (1) DE60315444T2 (https=)
DK (1) DK1501848T3 (https=)
ES (1) ES2290448T3 (https=)
WO (1) WO2003095467A1 (https=)

Families Citing this family (67)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
USRE44779E1 (en) 1997-03-07 2014-02-25 Santaris Pharma A/S Bicyclonucleoside and oligonucleotide analogues
AU2003225495B2 (en) 2002-04-05 2009-01-15 Roche Innovation Center Copenhagen A/S Oligomeric compounds for the modulation HIF-1alpha expression
WO2004046160A2 (en) 2002-11-18 2004-06-03 Santaris Pharma A/S Amino-lna, thio-lna and alpha-l-oxy-ln
US7713738B2 (en) 2003-02-10 2010-05-11 Enzon Pharmaceuticals, Inc. Oligomeric compounds for the modulation of survivin expression
ATE443765T1 (de) 2003-03-21 2009-10-15 Santaris Pharma As Analoga kurzer interferierender rna (sirna)
WO2005061710A1 (en) 2003-12-23 2005-07-07 Santaris Pharma A/S Oligomeric compounds for the modulation of bcl-2
MX2007005558A (es) 2004-11-09 2008-01-31 Santaris Pharma As Oligonucleotidos de lna potentes para la inhibicion dela expresion de hif-1a.
WO2006050732A2 (en) 2004-11-09 2006-05-18 Santaris Pharma A/S Lna oligonucleotides and the treatment of cancer
US9447138B2 (en) 2004-11-09 2016-09-20 Roche Innovation Center Copenhagen A/S Potent LNA oligonucleotides for the inhibition of HIF-1a expression
US8071306B2 (en) 2005-01-25 2011-12-06 Merck Sharp & Dohme Corp. Methods for quantitating small RNA molecules
WO2007107162A2 (en) 2006-03-23 2007-09-27 Santaris Pharma A/S Small internally segmented interfering rna
SG10201406016SA (en) 2006-04-03 2014-11-27 Stella Aps Pharmaceutical composition comprising anti-mirna antisense oligonucleotides
EP2007888A2 (en) 2006-04-03 2008-12-31 Santaris Pharma A/S Pharmaceutical composition comprising anti-mirna antisense oligonucleotides
EP2054415A1 (en) * 2006-07-14 2009-05-06 Santaris Pharma A/S Adenosine receptor antagonists
US8470791B2 (en) 2007-03-22 2013-06-25 Santaris Pharma A/S RNA antagonist compounds for the inhibition of Apo-B100 expression
DK2149605T3 (da) 2007-03-22 2013-09-30 Santaris Pharma As Korte RNA antagonist forbindelser til modulering af det ønskede mRNA
CA2689602A1 (en) 2007-06-06 2008-12-18 Avi Biopharma, Inc. Soluble her2 and her3 splice variant proteins, splice-switching oligonucleotides, and their use in the treatment of disease
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
EP2195428B1 (en) 2007-09-19 2013-12-11 Applied Biosystems, LLC SiRNA SEQUENCE-INDEPENDENT MODIFICATION FORMATS FOR REDUCING OFF-TARGET PHENOTYPIC EFFECTS IN RNAi, AND STABILIZED FORMS THEREOF
EP2623599B1 (en) 2007-10-04 2019-01-02 Roche Innovation Center Copenhagen A/S Micromirs
CA2717792A1 (en) 2008-03-07 2009-09-11 Santaris Pharma A/S Pharmaceutical compositions for treatment of microrna related diseases
WO2010012667A1 (en) 2008-08-01 2010-02-04 Santaris Pharma A/S Micro-rna mediated modulation of colony stimulating factors
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
EP2456870A1 (en) 2009-07-21 2012-05-30 Santaris Pharma A/S Antisense oligomers targeting pcsk9
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
WO2011105901A2 (en) 2010-02-23 2011-09-01 Academisch Ziekenhuis Bij De Universiteit Van Amsterdam Antagonists of complement component 9 (c9) and uses thereof
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
EP2542678B1 (en) 2010-03-04 2017-04-12 InteRNA Technologies B.V. A MiRNA MOLECULE DEFINED BY ITS SOURCE AND ITS THERAPEUTIC USES IN CANCER ASSOCIATED WITH EMT
EP2591106A1 (en) 2010-07-06 2013-05-15 InteRNA Technologies B.V. Mirna and its diagnostic and therapeutic uses in diseases or conditions associated with melanoma, or in diseases or conditions associated with activated braf pathway
GB201012418D0 (en) 2010-07-23 2010-09-08 Santaris Pharma As Process
EP2474617A1 (en) 2011-01-11 2012-07-11 InteRNA Technologies BV Mir for treating neo-angiogenesis
WO2013011122A1 (en) * 2011-07-21 2013-01-24 Rhodia Operations Guar hydroxypropyltrimethylammonium chloride and uses thereof in hair treatment compositions
EP3369818B1 (en) 2011-12-22 2021-06-09 InteRNA Technologies B.V. Mirna for treating head and neck cancer
SG10201913554YA (en) 2011-12-22 2020-03-30 Alios Biopharma Inc Substituted nucleosides, nucleotides and analogs thereof
USRE48171E1 (en) 2012-03-21 2020-08-25 Janssen Biopharma, Inc. Substituted nucleosides, nucleotides and analogs thereof
US9441007B2 (en) 2012-03-21 2016-09-13 Alios Biopharma, Inc. Substituted nucleosides, nucleotides and analogs thereof
EP2917348A1 (en) 2012-11-06 2015-09-16 InteRNA Technologies B.V. Combination for use in treating diseases or conditions associated with melanoma, or treating diseases or conditions associated with activated b-raf pathway
WO2014108759A1 (en) 2013-01-14 2014-07-17 Pierfrancesco Tassone INHIBITORS OF miRNAs 221 AND 222 FOR ANTI-TUMOR ACTIVITY IN MULTIPLE MYELOMA
US9428537B2 (en) 2013-03-15 2016-08-30 The Board Of Trustees Of The Leland Stanford Junior University tRNA derived small RNAs (tsRNAs) involved in cell viability
HUE048738T2 (hu) 2013-06-27 2020-08-28 Roche Innovation Ct Copenhagen As Antiszensz oligomerek és konjugátumok, amelyek a PCK9-t célozzák meg
GB201410693D0 (en) 2014-06-16 2014-07-30 Univ Southampton Splicing modulation
AU2015327836B2 (en) 2014-10-03 2021-07-01 Cold Spring Harbor Laboratory Targeted augmentation of nuclear gene output
WO2016128583A2 (en) 2015-02-15 2016-08-18 Ribo Task Aps Acyl-amino-lna and/or hydrocarbyl-amino-lna oligonucleotides
TW201718618A (zh) * 2015-09-18 2017-06-01 田邊三菱製藥股份有限公司 架橋型核酸ＧｕＮＡ，其製造方法，及中間體化合物
CN108603230A (zh) 2015-10-09 2018-09-28 南安普敦大学 基因表达的调节与蛋白质表达失调的筛选
WO2017106377A1 (en) 2015-12-14 2017-06-22 Cold Spring Harbor Laboratory Antisense oligomers for treatment of autosomal dominant mental retardation-5 and dravet syndrome
US11096956B2 (en) 2015-12-14 2021-08-24 Stoke Therapeutics, Inc. Antisense oligomers and uses thereof
US11390867B2 (en) 2016-04-29 2022-07-19 Nanyang Technological University G-quadruplex-containing antisense oligonucleotides
EP3494219A1 (en) 2016-08-03 2019-06-12 Aalborg Universitet ANTISENSE OLIGONUCLEOTIDES (ASOs) DESIGNED TO INHIBIT IMMUNE CHECKPOINT PROTEINS
KR102318434B1 (ko) 2017-08-25 2021-11-01 스톡 테라퓨틱스, 인크. 병태 및 질환 치료용 안티센스 올리고머
CN111566212A (zh) 2017-11-03 2020-08-21 因特尔纳技术有限公司 miRNA分子，等同物，安塔够妙或其来源用于治疗和/或诊断与神经元缺陷相关的病症和/或疾病或用于神经元生成和/或再生
JP2021513508A (ja) 2018-02-12 2021-05-27 インテアールエヌエー テクノロジーズ ビー．ヴイ．ＩｎｔｅＲＮＡ Ｔｅｃｈｎｏｌｏｇｉｅｓ Ｂ．Ｖ． 抗がんマイクロｒｎａ及びその脂質製剤
CA3099280A1 (en) 2018-05-04 2019-11-07 Stoke Therapeutics, Inc. Methods and compositions for treatment of cholesteryl ester storage disease
AU2020227825B2 (en) 2019-02-27 2026-03-26 Stoke Therapeutics, Inc. Antisense oligomers for treatment of conditions and diseases
IT201900017234A1 (it) 2019-09-25 2021-03-25 Int Centre For Genetic Engineering And Biotechnology Anti-miRNA per il trattamento del leiomioma
CN115867657A (zh) 2020-05-11 2023-03-28 斯托克制药公司 用于治疗疾患和疾病的opa1反义寡聚物
CN117280030A (zh) 2021-02-12 2023-12-22 梅兰德制药公司 用于治疗缺氧和缺血相关病症的药剂、组合物和方法
WO2022200633A1 (en) 2021-03-26 2022-09-29 Neumirna Therapeutics Aps Microrna-27b inhibitors
AU2022245292A1 (en) 2021-03-26 2023-10-12 Neumirna Therapeutics Aps Microrna-134 inhibitors
WO2022254021A1 (en) 2021-06-04 2022-12-08 Neumirna Therapeutics Aps Antisense oligonucleotides targeting adenosine kinase
CN118202050A (zh) 2021-08-17 2024-06-14 韩国科学技术院 靶向cav3.1基因的反义寡核苷酸及其用途
EP4388096A1 (en) 2021-08-19 2024-06-26 Neumirna Therapeutics ApS Antisense oligonucleotides targeting adenosine kinase
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
EP4450626A1 (en) 2023-04-21 2024-10-23 IFOM - Istituto Fondazione di Oncologia Molecolare ETS Fnip2 inhibitors for treating ataxia telangiectasia
WO2025015676A1 (zh) * 2023-07-21 2025-01-23 瑞孚医药科技（广州）有限公司 碳环核苷、寡核苷酸及其制备方法和医药用途
EP4512899A1 (en) 2023-08-23 2025-02-26 Lipigon Pharmaceuticals AB Angptl4 aso compositions for treatment of atherosclerosis in humans
WO2026068729A1 (en) 2024-09-26 2026-04-02 Neumirna Therapeutics Aps Antimir-27b for treatment of parkinson's disease

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7053207B2 (en) * 1999-05-04 2006-05-30 Exiqon A/S L-ribo-LNA analogues
JP4413493B2 (ja) * 2000-10-04 2010-02-10 サンタリス ファーマ アー／エス プリンｌｎａ類似体の改善された合成方法

Also Published As

Publication number Publication date
JP2005532319A (ja) 2005-10-27
ES2290448T3 (es) 2008-02-16
CA2484526C (en) 2009-10-13
EP1501848B1 (en) 2007-08-08
DE60315444D1 (en) 2007-09-20
AU2003222743A1 (en) 2003-11-11
EP1501848A1 (en) 2005-02-02
DK1501848T3 (da) 2007-10-22
JP4476802B2 (ja) 2010-06-09
DE60315444T2 (de) 2008-04-30
CA2484526A1 (en) 2003-11-20
ATE369375T1 (de) 2007-08-15
WO2003095467A1 (en) 2003-11-20

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Date Code Title Description
PC1 Assignment before grant (sect. 113)

Owner name: SANTARIS PHARMA A/S

Free format text: FORMER APPLICANT(S): SANTARIS PHARMA A/S; EXIQON A/S

FGA Letters patent sealed or granted (standard patent)
TH Corrigenda

Free format text: IN VOL 18, NO 2, PAGE(S) 579 UNDER THE HEADING APPLICATIONS OPI NAME INDEX UNDER THE NAME SANTARIS PHARMA A/S, APPLICATION NO. 2003222743, UNDER INID (43) CORRECT PUBLICATION DATE TO READ 24 NOVEMBER 2003.

MK14 Patent ceased section 143(a) (annual fees not paid) or expired