JP2012529279A5 - - Google Patents
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- JP2012529279A5 JP2012529279A5 JP2012514491A JP2012514491A JP2012529279A5 JP 2012529279 A5 JP2012529279 A5 JP 2012529279A5 JP 2012514491 A JP2012514491 A JP 2012514491A JP 2012514491 A JP2012514491 A JP 2012514491A JP 2012529279 A5 JP2012529279 A5 JP 2012529279A5
- Authority
- JP
- Japan
- Prior art keywords
- linkage
- nucleotides
- phosphorothioate
- nucleotide analogs
- group
- 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.)
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- 125000003729 nucleotide group Chemical group 0.000 description 5
- 239000002773 nucleotide Substances 0.000 description 3
- RYYWUUFWQRZTIU-UHFFFAOYSA-K thiophosphate Chemical group [O-]P([O-])([O-])=S RYYWUUFWQRZTIU-UHFFFAOYSA-K 0.000 description 3
- 125000002467 phosphate group Chemical group [H]OP(=O)(O[H])O[*] 0.000 description 1
- NINIDFKCEFEMDL-UHFFFAOYSA-N sulfur Chemical compound [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 description 1
- 229910052717 sulfur Inorganic materials 0.000 description 1
- 239000011593 sulfur Substances 0.000 description 1
Description
ヌクレオチド間の連結
用語「連結基」または「ヌクレオチド間連結」は、2つのヌクレオチド、2つのヌクレオチドアナログ、およびヌクレオチドおよびヌクレオチドアナログ等を一緒に共有結合させることができる基を意味すると意図される。特定かつ好ましい例には、リン酸基およびホスホロチオエート基が含まれる。
用語「連結基」または「ヌクレオチド間連結」は、2つのヌクレオチド、2つのヌクレオチドアナログ、およびヌクレオチドおよびヌクレオチドアナログ等を一緒に共有結合させることができる基を意味すると意図される。特定かつ好ましい例には、リン酸基およびホスホロチオエート基が含まれる。
本明細書中で提供されるものとして、好適な硫黄(S)を含むヌクレオチド間連結が好ましい。ホスホロチオエートヌクレオチド間連結もまた、ギャップマーのギャップ領域(B)にとって特に好ましい。また、ホスホロチオエート連結を、フランキング領域(AおよびC、ならびにAまたはCをDに連結するため、および必要に応じて領域D内の)に使用することもできる。
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 | ||
EPPCT/EP2009/067561 | 2009-12-18 | ||
PCT/EP2009/067561 WO2010076248A1 (en) | 2008-12-31 | 2009-12-18 | Use of lna apob antisense oligomers for the treatment of acute coronary syndromes |
PCT/EP2010/058278 WO2010142805A1 (en) | 2009-06-12 | 2010-06-14 | New potent anti apob antisense compounds |
Publications (2)
Publication Number | Publication Date |
---|---|
JP2012529279A JP2012529279A (ja) | 2012-11-22 |
JP2012529279A5 true JP2012529279A5 (ja) | 2013-08-01 |
Family
ID=42541569
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
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 |
Country Status (12)
Country | Link |
---|---|
US (1) | US9290758B2 (ja) |
EP (1) | EP2440215B1 (ja) |
JP (1) | JP2012529279A (ja) |
CN (1) | CN102802637A (ja) |
AU (1) | AU2010258570B2 (ja) |
BR (1) | BR112012000214A2 (ja) |
CA (1) | CA2764822A1 (ja) |
ES (1) | ES2555057T3 (ja) |
IL (1) | IL216519A0 (ja) |
MX (1) | MX2011013078A (ja) |
NZ (1) | NZ596608A (ja) |
WO (1) | WO2010142805A1 (ja) |
Families Citing this family (6)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US10077443B2 (en) | 2012-11-15 | 2018-09-18 | Roche Innovation Center Copenhagen A/S | Oligonucleotide conjugates |
DK2951305T3 (en) | 2013-01-30 | 2018-10-29 | Hoffmann La Roche | LNA oligonucleotide KULHYDRATKONJUGATER |
CN112263682A (zh) | 2013-06-27 | 2021-01-26 | 罗氏创新中心哥本哈根有限公司 | 靶向pcsk9的反义寡聚体和缀合物 |
JP2017501684A (ja) * | 2013-11-14 | 2017-01-19 | ロシュ・イノベーション・センター・コペンハーゲン・アクティーゼルスカブRoche Innovation Center Copenhagen A/S | Apobアンチセンスコンジュゲート化合物 |
SG11202007652UA (en) * | 2018-02-21 | 2020-09-29 | Bristol Myers Squibb Co | Camk2d antisense oligonucleotides and uses thereof |
CA3117981A1 (en) * | 2018-11-13 | 2020-05-22 | Regulus Therapeutics Inc. | Microrna compounds and methods for modulating mir-10b activity |
Family Cites Families (24)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
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 |
EP1523348B1 (en) * | 2002-07-19 | 2011-03-30 | Medela Holding AG | Connector device |
US7087229B2 (en) | 2003-05-30 | 2006-08-08 | Enzon Pharmaceuticals, Inc. | Releasable polymeric conjugates based on aliphatic biodegradable linkers |
US7687617B2 (en) | 2002-11-18 | 2010-03-30 | Santaris Pharma A/S | Oligonucleotides with alternating segments of locked and non-locked nucleotides |
WO2004080406A2 (en) * | 2003-03-07 | 2004-09-23 | Alnylam Pharmaceuticals | Therapeutic compositions |
JP4912873B2 (ja) * | 2003-04-09 | 2012-04-11 | 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 |
AU2004229519B2 (en) * | 2003-04-09 | 2011-07-21 | Alnylam Pharmaceuticals, Inc. | iRNA conjugates |
EP2199298A1 (en) * | 2004-11-17 | 2010-06-23 | 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 |
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 |
AU2007229161B2 (en) | 2006-03-23 | 2012-07-12 | Roche Innovation Center Copenhagen A/S | Small internally segmented interfering RNA |
US7547684B2 (en) | 2006-05-11 | 2009-06-16 | Isis Pharmaceuticals, Inc. | 5′-modified bicyclic nucleic acid analogs |
WO2008034122A2 (en) | 2006-09-15 | 2008-03-20 | Enzon Pharmaceuticals, Inc. | Hindered ester-based biodegradable linkers for oligonucleotide delivery |
AU2007296055A1 (en) | 2006-09-15 | 2008-03-20 | Enzon Pharmaceuticals, Inc. | Polymeric conjugates containing positively-charged moieties |
EP2090127A2 (en) | 2006-10-30 | 2009-08-19 | Nokia Corporation | Method, apparatus and system providing operator controlled mobility for user equipment |
WO2008113830A1 (en) | 2007-03-22 | 2008-09-25 | Santaris Pharma A/S | Rna antagonist compounds for the inhibition of apo-b100 expression |
US8278425B2 (en) | 2007-05-30 | 2012-10-02 | Isis Pharmaceuticals, Inc. | N-substituted-aminomethylene bridged bicyclic nucleic acid analogs |
WO2008154401A2 (en) | 2007-06-08 | 2008-12-18 | Isis Pharmaceuticals, Inc. | Carbocyclic bicyclic nucleic acid analogs |
AU2008272918B2 (en) | 2007-07-05 | 2012-09-13 | Isis Pharmaceuticals, Inc. | 6-disubstituted bicyclic nucleic acid analogs |
US8546556B2 (en) | 2007-11-21 | 2013-10-01 | Isis Pharmaceuticals, Inc | Carbocyclic alpha-L-bicyclic nucleic acid analogs |
-
2010
- 2010-06-14 US US13/140,777 patent/US9290758B2/en not_active Expired - Fee Related
- 2010-06-14 CA CA2764822A patent/CA2764822A1/en not_active Abandoned
- 2010-06-14 EP EP10724511.0A patent/EP2440215B1/en not_active Not-in-force
- 2010-06-14 CN CN2010800257913A patent/CN102802637A/zh active Pending
- 2010-06-14 ES ES10724511.0T patent/ES2555057T3/es active Active
- 2010-06-14 AU AU2010258570A patent/AU2010258570B2/en not_active Ceased
- 2010-06-14 MX MX2011013078A patent/MX2011013078A/es active IP Right Grant
- 2010-06-14 WO PCT/EP2010/058278 patent/WO2010142805A1/en active Application Filing
- 2010-06-14 JP JP2012514491A patent/JP2012529279A/ja active Pending
- 2010-06-14 BR BR112012000214A patent/BR112012000214A2/pt not_active IP Right Cessation
- 2010-06-14 NZ NZ596608A patent/NZ596608A/en not_active IP Right Cessation
-
2011
- 2011-11-22 IL IL216519A patent/IL216519A0/en not_active IP Right Cessation
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