JP2012529279A - 新規の強力な抗ａｐｏｂアンチセンス化合物 - Google Patents

新規の強力な抗ａｐｏｂアンチセンス化合物 Download PDF

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JP2012529279A
JP2012529279A JP2012514491A JP2012514491A JP2012529279A JP 2012529279 A JP2012529279 A JP 2012529279A JP 2012514491 A JP2012514491 A JP 2012514491A JP 2012514491 A JP2012514491 A JP 2012514491A JP 2012529279 A JP2012529279 A JP 2012529279A
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oligomer
nucleotide
lna
substituted
certain embodiments
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JP2012529279A5 (https=
Inventor
ニルス・フィスケル・ニルセン
エレン・マリー・ストラールップ
マリエ・リンドホルム
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Roche Innovation Center Copenhagen AS
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Santaris Pharma AS
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Priority claimed from PCT/EP2009/067561 external-priority patent/WO2010076248A1/en
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Publication of JP2012529279A publication Critical patent/JP2012529279A/ja
Publication of JP2012529279A5 publication Critical patent/JP2012529279A5/ja
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    • C—CHEMISTRY; METALLURGY
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    • C12N15/00—Mutation or genetic engineering; DNA or RNA concerning genetic engineering, vectors, e.g. plasmids, or their isolation, preparation or purification; Use of hosts therefor
    • C12N15/09—Recombinant DNA-technology
    • C12N15/11—DNA or RNA fragments; Modified forms thereof; Non-coding nucleic acids having a biological activity
    • C12N15/113—Non-coding nucleic acids modulating the expression of genes, e.g. antisense oligonucleotides; Antisense DNA or RNA; Triplex- forming oligonucleotides; Catalytic nucleic acids, e.g. ribozymes; Nucleic acids used in co-suppression or gene silencing
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7088—Compounds having three or more nucleosides or nucleotides
    • A61K31/712—Nucleic acids or oligonucleotides having modified sugars, i.e. other than ribose or 2'-deoxyribose
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7088—Compounds having three or more nucleosides or nucleotides
    • A61K31/713—Double-stranded nucleic acids or oligonucleotides
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/06—Antihyperlipidemics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12N—MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
    • C12N2310/00—Structure or type of the nucleic acid
    • C12N2310/10—Type of nucleic acid
    • C12N2310/11—Antisense
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12N—MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
    • C12N2310/00—Structure or type of the nucleic acid
    • C12N2310/30—Chemical structure
    • C12N2310/31—Chemical structure of the backbone
    • C12N2310/315—Phosphorothioates
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12N—MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
    • C12N2310/00—Structure or type of the nucleic acid
    • C12N2310/30—Chemical structure
    • C12N2310/32—Chemical structure of the sugar
    • C12N2310/321—2'-O-R Modification
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
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    • C12N2310/00—Structure or type of the nucleic acid
    • C12N2310/30—Chemical structure
    • C12N2310/32—Chemical structure of the sugar
    • C12N2310/322—2'-R Modification
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12N—MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
    • C12N2310/00—Structure or type of the nucleic acid
    • C12N2310/30—Chemical structure
    • C12N2310/32—Chemical structure of the sugar
    • C12N2310/323—Chemical structure of the sugar modified ring structure
    • C12N2310/3231—Chemical structure of the sugar modified ring structure having an additional ring, e.g. LNA, ENA

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  • Health & Medical Sciences (AREA)
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  • Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • General Health & Medical Sciences (AREA)
  • Genetics & Genomics (AREA)
  • Molecular Biology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Organic Chemistry (AREA)
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  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Biochemistry (AREA)
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  • Epidemiology (AREA)
  • General Engineering & Computer Science (AREA)
  • Zoology (AREA)
  • Wood Science & Technology (AREA)
  • Biotechnology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Plant Pathology (AREA)
  • Biophysics (AREA)
  • Physics & Mathematics (AREA)
  • Microbiology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Saccharide Compounds (AREA)
  • Micro-Organisms Or Cultivation Processes Thereof (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
JP2012514491A 2009-06-12 2010-06-14 新規の強力な抗ａｐｏｂアンチセンス化合物 Pending JP2012529279A (ja)

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
US18638809P 2009-06-12 2009-06-12
US61/186,388 2009-06-12
US25309009P 2009-10-20 2009-10-20
US61/253,090 2009-10-20
PCT/EP2009/067561 WO2010076248A1 (en) 2008-12-31 2009-12-18 Use of lna apob antisense oligomers for the treatment of acute coronary syndromes
EPPCT/EP2009/067561 2009-12-18
PCT/EP2010/058278 WO2010142805A1 (en) 2009-06-12 2010-06-14 New potent anti apob antisense compounds

Publications (2)

Publication Number Publication Date
JP2012529279A true JP2012529279A (ja) 2012-11-22
JP2012529279A5 JP2012529279A5 (https=) 2013-08-01

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JP2012514491A Pending JP2012529279A (ja) 2009-06-12 2010-06-14 新規の強力な抗ａｐｏｂアンチセンス化合物

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Country Link
US (1) US9290758B2 (https=)
EP (1) EP2440215B1 (https=)
JP (1) JP2012529279A (https=)
CN (1) CN102802637A (https=)
AU (1) AU2010258570B2 (https=)
BR (1) BR112012000214A2 (https=)
CA (1) CA2764822A1 (https=)
ES (1) ES2555057T3 (https=)
IL (1) IL216519A0 (https=)
MX (1) MX2011013078A (https=)
NZ (1) NZ596608A (https=)
WO (1) WO2010142805A1 (https=)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2021513861A (ja) * 2018-02-21 2021-06-03 ブリストル−マイヤーズ スクイブ カンパニーＢｒｉｓｔｏｌ−Ｍｙｅｒｓ Ｓｑｕｉｂｂ Ｃｏｍｐａｎｙ Ｃａｍｋ２ｄアンチセンスオリゴヌクレオチドおよびその使用

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US10077443B2 (en) 2012-11-15 2018-09-18 Roche Innovation Center Copenhagen A/S Oligonucleotide conjugates
CN104955952A (zh) 2013-01-30 2015-09-30 弗·哈夫曼-拉罗切有限公司 Lna寡核苷酸碳水化合物缀合物
ES2770667T3 (es) 2013-06-27 2020-07-02 Roche Innovation Ct Copenhagen As Oligómeros antisentido y conjugados que se dirigen a PCSK9
KR20160083876A (ko) * 2013-11-14 2016-07-12 로슈 이노베이션 센터 코펜하겐 에이/에스 ApoB 안티센스 접합체 화합물
KR20210091732A (ko) * 2018-11-13 2021-07-22 레굴루스 테라퓨틱스 인크 Mir-10b 활성을 조정하는 마이크로rna 및 방법
CR20230308A (es) 2020-12-11 2023-09-08 Civi Biopharma Inc Entrega oral de conjugados antisentido que tienen por blanco a pcsk9

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WO2006053430A1 (en) * 2004-11-17 2006-05-26 Protiva Biotherapeutics, Inc. Sirna silencing of apolipoprotein b
JP2006522831A (ja) * 2003-04-09 2006-10-05 アルナイラム ファーマシューティカルズ インコーポレイテッド ｉＲＮＡ複合体
JP2009507499A (ja) * 2005-09-15 2009-02-26 サンタリス ファーマ アー／エス Ａｐｏ−ｂ１００発現の抑制のためのｒｎａアンタゴニスト化合物

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US4962029A (en) 1987-10-02 1990-10-09 Cetus Corporation Covalent oligonucleotide-horseradish peroxidase conjugate
US4914210A (en) 1987-10-02 1990-04-03 Cetus Corporation Oligonucleotide functionalizing reagents
US6617442B1 (en) 1999-09-30 2003-09-09 Isis Pharmaceuticals, Inc. Human Rnase H1 and oligonucleotide compositions thereof
US7407943B2 (en) 2001-08-01 2008-08-05 Isis Pharmaceuticals, Inc. Antisense modulation of apolipoprotein B expression
AU2003256602C1 (en) * 2002-07-19 2009-05-21 Medela Holding Ag Breast pump connector device
US7087229B2 (en) 2003-05-30 2006-08-08 Enzon Pharmaceuticals, Inc. Releasable polymeric conjugates based on aliphatic biodegradable linkers
US9045518B2 (en) 2002-11-18 2015-06-02 Santaris Pharma A/S Amino-LNA, thio-LNA and alpha-L-oxy-LN
WO2004080406A2 (en) * 2003-03-07 2004-09-23 Alnylam Pharmaceuticals Therapeutic compositions
CA2521464C (en) 2003-04-09 2013-02-05 Alnylam Pharmaceuticals, Inc. Irna conjugates
WO2007031091A2 (en) 2005-09-15 2007-03-22 Santaris Pharma A/S Rna antagonist compounds for the modulation of p21 ras expression
JP5342881B2 (ja) 2006-01-27 2013-11-13 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 ６−修飾された二環式核酸類似体
WO2007107162A2 (en) 2006-03-23 2007-09-27 Santaris Pharma A/S Small internally segmented interfering rna
AU2007249349B2 (en) 2006-05-11 2012-03-08 Isis Pharmaceuticals, Inc. 5'-Modified bicyclic nucleic acid analogs
JP2010503707A (ja) 2006-09-15 2010-02-04 エンゾン ファーマスーティカルズ インコーポレイテッド オリゴヌクレオチドの送達を目的としたヒンダードエステル系生体分解性リンカー
EP2076257A4 (en) 2006-09-15 2014-04-16 Belrose Pharma Inc POLYMER CONJUGATES WITH POSITIVELY LOADED PARTS
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CA2681406A1 (en) 2007-03-22 2008-09-25 Santaris Pharma A/S Rna antagonist compounds for the inhibition of apo-b100 expression
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EP2173760B2 (en) 2007-06-08 2015-11-04 Isis Pharmaceuticals, Inc. Carbocyclic bicyclic nucleic acid analogs
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JP2006522831A (ja) * 2003-04-09 2006-10-05 アルナイラム ファーマシューティカルズ インコーポレイテッド ｉＲＮＡ複合体
WO2006053430A1 (en) * 2004-11-17 2006-05-26 Protiva Biotherapeutics, Inc. Sirna silencing of apolipoprotein b
JP2009507499A (ja) * 2005-09-15 2009-02-26 サンタリス ファーマ アー／エス Ａｐｏ−ｂ１００発現の抑制のためのｒｎａアンタゴニスト化合物

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2021513861A (ja) * 2018-02-21 2021-06-03 ブリストル−マイヤーズ スクイブ カンパニーＢｒｉｓｔｏｌ−Ｍｙｅｒｓ Ｓｑｕｉｂｂ Ｃｏｍｐａｎｙ Ｃａｍｋ２ｄアンチセンスオリゴヌクレオチドおよびその使用
JP7500426B2 (ja) 2018-02-21 2024-06-17 ブリストル－マイヤーズ スクイブ カンパニー Ｃａｍｋ２ｄアンチセンスオリゴヌクレオチドおよびその使用

Also Published As

Publication number Publication date
ES2555057T3 (es) 2015-12-28
BR112012000214A2 (pt) 2018-06-19
WO2010142805A4 (en) 2011-03-03
US9290758B2 (en) 2016-03-22
CN102802637A (zh) 2012-11-28
EP2440215A1 (en) 2012-04-18
IL216519A0 (en) 2012-02-29
AU2010258570B2 (en) 2016-09-01
US20120115936A1 (en) 2012-05-10
AU2010258570A1 (en) 2011-12-15
MX2011013078A (es) 2012-02-01
CA2764822A1 (en) 2010-12-16
NZ596608A (en) 2014-01-31
EP2440215B1 (en) 2015-10-21
WO2010142805A1 (en) 2010-12-16

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