JP2010505432A5 - - Google Patents
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- JP2010505432A5 JP2010505432A5 JP2009531824A JP2009531824A JP2010505432A5 JP 2010505432 A5 JP2010505432 A5 JP 2010505432A5 JP 2009531824 A JP2009531824 A JP 2009531824A JP 2009531824 A JP2009531824 A JP 2009531824A JP 2010505432 A5 JP2010505432 A5 JP 2010505432A5
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- Prior art keywords
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- oligomer according
- lna
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- Prior art date
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- 125000003729 nucleotide group Chemical group 0.000 claims 29
- 101001098868 Homo sapiens Proprotein convertase subtilisin/kexin type 9 Proteins 0.000 claims 15
- 239000002773 nucleotide Substances 0.000 claims 14
- 102100038955 Proprotein convertase subtilisin/kexin type 9 Human genes 0.000 claims 13
- 150000007523 nucleic acids Chemical class 0.000 claims 12
- 108020004414 DNA Proteins 0.000 claims 9
- 108020004707 nucleic acids Proteins 0.000 claims 8
- 102000039446 nucleic acids Human genes 0.000 claims 8
- 230000000295 complement effect Effects 0.000 claims 6
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 6
- 108091032973 (ribonucleotides)n+m Proteins 0.000 claims 5
- 108091028043 Nucleic acid sequence Proteins 0.000 claims 4
- 150000001875 compounds Chemical class 0.000 claims 4
- 208000035475 disorder Diseases 0.000 claims 4
- 208000027866 inflammatory disease Diseases 0.000 claims 4
- 208000030159 metabolic disease Diseases 0.000 claims 4
- 239000008194 pharmaceutical composition Substances 0.000 claims 4
- 102100034343 Integrase Human genes 0.000 claims 3
- 101710203526 Integrase Proteins 0.000 claims 3
- 229910019142 PO4 Inorganic materials 0.000 claims 3
- 239000010452 phosphate Substances 0.000 claims 3
- 150000003839 salts Chemical group 0.000 claims 3
- RYYWUUFWQRZTIU-UHFFFAOYSA-K thiophosphate Chemical compound [O-]P([O-])([O-])=S RYYWUUFWQRZTIU-UHFFFAOYSA-K 0.000 claims 3
- 208000024827 Alzheimer disease Diseases 0.000 claims 2
- 201000001320 Atherosclerosis Diseases 0.000 claims 2
- 208000035150 Hypercholesterolemia Diseases 0.000 claims 2
- 208000001145 Metabolic Syndrome Diseases 0.000 claims 2
- 201000000690 abdominal obesity-metabolic syndrome Diseases 0.000 claims 2
- 230000000692 anti-sense effect Effects 0.000 claims 2
- 206010003246 arthritis Diseases 0.000 claims 2
- 208000006673 asthma Diseases 0.000 claims 2
- 206010012601 diabetes mellitus Diseases 0.000 claims 2
- 201000010099 disease Diseases 0.000 claims 2
- 239000003814 drug Substances 0.000 claims 2
- 230000002708 enhancing effect Effects 0.000 claims 2
- 102000053786 human PCSK9 Human genes 0.000 claims 2
- 108020004999 messenger RNA Proteins 0.000 claims 2
- PCTMTFRHKVHKIS-BMFZQQSSSA-N (1s,3r,4e,6e,8e,10e,12e,14e,16e,18s,19r,20r,21s,25r,27r,30r,31r,33s,35r,37s,38r)-3-[(2r,3s,4s,5s,6r)-4-amino-3,5-dihydroxy-6-methyloxan-2-yl]oxy-19,25,27,30,31,33,35,37-octahydroxy-18,20,21-trimethyl-23-oxo-22,39-dioxabicyclo[33.3.1]nonatriaconta-4,6,8,10 Chemical compound C1C=C2C[C@@H](OS(O)(=O)=O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@H]([C@H](C)CCCC(C)C)[C@@]1(C)CC2.O[C@H]1[C@@H](N)[C@H](O)[C@@H](C)O[C@H]1O[C@H]1/C=C/C=C/C=C/C=C/C=C/C=C/C=C/[C@H](C)[C@@H](O)[C@@H](C)[C@H](C)OC(=O)C[C@H](O)C[C@H](O)CC[C@@H](O)[C@H](O)C[C@H](O)C[C@](O)(C[C@H](O)[C@H]2C(O)=O)O[C@H]2C1 PCTMTFRHKVHKIS-BMFZQQSSSA-N 0.000 claims 1
- ZOBPZXTWZATXDG-UHFFFAOYSA-N 1,3-thiazolidine-2,4-dione Chemical compound O=C1CSC(=O)N1 ZOBPZXTWZATXDG-UHFFFAOYSA-N 0.000 claims 1
- RHCSKNNOAZULRK-APZFVMQVSA-N 2,2-dideuterio-2-(3,4,5-trimethoxyphenyl)ethanamine Chemical compound NCC([2H])([2H])C1=CC(OC)=C(OC)C(OC)=C1 RHCSKNNOAZULRK-APZFVMQVSA-N 0.000 claims 1
- XQCZBXHVTFVIFE-UHFFFAOYSA-N 2-amino-4-hydroxypyrimidine Chemical compound NC1=NC=CC(O)=N1 XQCZBXHVTFVIFE-UHFFFAOYSA-N 0.000 claims 1
- MWBWWFOAEOYUST-UHFFFAOYSA-N 2-aminopurine Chemical compound NC1=NC=C2N=CNC2=N1 MWBWWFOAEOYUST-UHFFFAOYSA-N 0.000 claims 1
- HBJGQJWNMZDFKL-UHFFFAOYSA-N 2-chloro-7h-purin-6-amine Chemical compound NC1=NC(Cl)=NC2=C1NC=N2 HBJGQJWNMZDFKL-UHFFFAOYSA-N 0.000 claims 1
- FWMNVWWHGCHHJJ-SKKKGAJSSA-N 4-amino-1-[(2r)-6-amino-2-[[(2r)-2-[[(2r)-2-[[(2r)-2-amino-3-phenylpropanoyl]amino]-3-phenylpropanoyl]amino]-4-methylpentanoyl]amino]hexanoyl]piperidine-4-carboxylic acid Chemical compound C([C@H](C(=O)N[C@H](CC(C)C)C(=O)N[C@H](CCCCN)C(=O)N1CCC(N)(CC1)C(O)=O)NC(=O)[C@H](N)CC=1C=CC=CC=1)C1=CC=CC=C1 FWMNVWWHGCHHJJ-SKKKGAJSSA-N 0.000 claims 1
- LQLQRFGHAALLLE-UHFFFAOYSA-N 5-bromouracil Chemical compound BrC1=CNC(=O)NC1=O LQLQRFGHAALLLE-UHFFFAOYSA-N 0.000 claims 1
- LRSASMSXMSNRBT-UHFFFAOYSA-N 5-methylcytosine Chemical group CC1=CNC(=O)N=C1N LRSASMSXMSNRBT-UHFFFAOYSA-N 0.000 claims 1
- UJBCLAXPPIDQEE-UHFFFAOYSA-N 5-prop-1-ynyl-1h-pyrimidine-2,4-dione Chemical compound CC#CC1=CNC(=O)NC1=O UJBCLAXPPIDQEE-UHFFFAOYSA-N 0.000 claims 1
- VKKXEIQIGGPMHT-UHFFFAOYSA-N 7h-purine-2,8-diamine Chemical compound NC1=NC=C2NC(N)=NC2=N1 VKKXEIQIGGPMHT-UHFFFAOYSA-N 0.000 claims 1
- GFFGJBXGBJISGV-UHFFFAOYSA-N Adenine Chemical compound NC1=NC=NC2=C1N=CN2 GFFGJBXGBJISGV-UHFFFAOYSA-N 0.000 claims 1
- 229930024421 Adenine Natural products 0.000 claims 1
- 102100030431 Fatty acid-binding protein, adipocyte Human genes 0.000 claims 1
- 229940121710 HMGCoA reductase inhibitor Drugs 0.000 claims 1
- 101001062864 Homo sapiens Fatty acid-binding protein, adipocyte Proteins 0.000 claims 1
- UGQMRVRMYYASKQ-KQYNXXCUSA-N Inosine Chemical compound O[C@@H]1[C@H](O)[C@@H](CO)O[C@H]1N1C2=NC=NC(O)=C2N=C1 UGQMRVRMYYASKQ-KQYNXXCUSA-N 0.000 claims 1
- 229930010555 Inosine Natural products 0.000 claims 1
- 241000283984 Rodentia Species 0.000 claims 1
- 229940123464 Thiazolidinedione Drugs 0.000 claims 1
- 239000002671 adjuvant Substances 0.000 claims 1
- 230000003110 anti-inflammatory effect Effects 0.000 claims 1
- 230000000840 anti-viral effect Effects 0.000 claims 1
- 239000000969 carrier Substances 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 208000016097 disease of metabolism Diseases 0.000 claims 1
- 229940125753 fibrate Drugs 0.000 claims 1
- 229960003786 inosine Drugs 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- -1 nucleic acid salts Chemical class 0.000 claims 1
- 108091033319 polynucleotide Proteins 0.000 claims 1
- 102000040430 polynucleotide Human genes 0.000 claims 1
- 239000002157 polynucleotide Substances 0.000 claims 1
- 239000000651 prodrug Substances 0.000 claims 1
- 229940002612 prodrug Drugs 0.000 claims 1
- 229940124597 therapeutic agent Drugs 0.000 claims 1
Applications Claiming Priority (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US82873506P | 2006-10-09 | 2006-10-09 | |
| US97293207P | 2007-09-17 | 2007-09-17 | |
| US97740907P | 2007-10-04 | 2007-10-04 | |
| PCT/EP2007/060703 WO2008043753A2 (en) | 2006-10-09 | 2007-10-09 | Rna antagonist compounds for the modulation of pcsk9 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2010505432A JP2010505432A (ja) | 2010-02-25 |
| JP2010505432A5 true JP2010505432A5 (enExample) | 2010-12-02 |
Family
ID=39125211
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2009531824A Withdrawn JP2010505432A (ja) | 2006-10-09 | 2007-10-09 | Ｐｃｓｋ９を調節するためのｒｎａアンタゴニスト化合物 |
Country Status (9)
| Country | Link |
|---|---|
| US (1) | US20100216864A1 (enExample) |
| EP (2) | EP2076597A2 (enExample) |
| JP (1) | JP2010505432A (enExample) |
| AU (1) | AU2007306361A1 (enExample) |
| CA (1) | CA2666191C (enExample) |
| ES (1) | ES2603379T3 (enExample) |
| IL (1) | IL197668A0 (enExample) |
| MX (1) | MX2009003729A (enExample) |
| WO (1) | WO2008043753A2 (enExample) |
Families Citing this family (78)
| Publication number | Priority date | Publication date | Assignee | Title |
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| EP2505646A1 (en) | 2006-05-05 | 2012-10-03 | Isis Pharmaceuticals, Inc. | Compounds and methods for modulating expression of CRP |
| US8093222B2 (en) | 2006-11-27 | 2012-01-10 | Isis Pharmaceuticals, Inc. | Methods for treating hypercholesterolemia |
| EA200900741A1 (ru) | 2006-11-27 | 2010-04-30 | Айзис Фармасьютикалз, Инк. | Способы лечения гиперхолестеринемии |
| US8470791B2 (en) | 2007-03-22 | 2013-06-25 | Santaris Pharma A/S | RNA antagonist compounds for the inhibition of Apo-B100 expression |
| US20110054011A1 (en) * | 2007-08-30 | 2011-03-03 | Mccullagh Keith | RNA Antagonist Compounds for the Modulation of FABP4/AP2 |
| US20110224280A1 (en) * | 2008-04-16 | 2011-09-15 | Niels Fisker Nielsen | Pharmaceutical Composition Comprising Anti PCSK9 Oligomers |
| US9089522B2 (en) | 2008-05-22 | 2015-07-28 | Merck Sharp & Dohme Corp. | Method of reducing total cholesterol level by administering matrilin-2 polypeptide |
| WO2009148605A2 (en) * | 2008-06-04 | 2009-12-10 | Isis Pharmaceuticals, Inc. | Methods for treating hypercholesterolemia |
| US8563528B2 (en) | 2009-07-21 | 2013-10-22 | Santaris Pharma A/S | Antisense oligomers targeting PCSK9 |
| US9364495B2 (en) | 2009-10-20 | 2016-06-14 | Roche Innovation Center Copenhagen A/S | Oral delivery of therapeutically effective LNA oligonucleotides |
| GB2481373A (en) * | 2010-06-21 | 2011-12-28 | Weiming Xu | Treatment of hypercholesterolaemia by ubiquitination of PCSK9 |
| US9127280B2 (en) | 2010-08-31 | 2015-09-08 | Osaka University | Oligonucleotide, and therapeutic agent for dyslipidemia containing oligonucleotide as active ingredient |
| EP3702460A1 (en) | 2010-11-12 | 2020-09-02 | The General Hospital Corporation | Polycomb-associated non-coding rnas |
| EP3521451A1 (en) | 2010-11-17 | 2019-08-07 | Ionis Pharmaceuticals, Inc. | Modulation of alpha synuclein expression |
| KR20200023495A (ko) | 2011-01-10 | 2020-03-04 | 더 리젠츠 오브 더 유니버시티 오브 미시간 | 줄기 세포 인자 억제제 |
| WO2013001372A2 (en) | 2011-06-30 | 2013-01-03 | University Of Oslo | Methods and compositions for inhibition of activation of regulatory t cells |
| RS55088B1 (sr) | 2011-07-06 | 2016-12-30 | Sykehuset Sorlandet Hf | Egfr ciljana terapija |
| HK1200484A1 (zh) | 2011-09-14 | 2015-08-07 | Translate Bio Ma, Inc. | 多聚寡核苷酸化合物 |
| CN104126010B (zh) | 2011-12-16 | 2021-04-06 | 国立大学法人东京医科齿科大学 | 嵌合的双链核酸 |
| US9255154B2 (en) | 2012-05-08 | 2016-02-09 | Alderbio Holdings, Llc | Anti-PCSK9 antibodies and use thereof |
| CN104583398A (zh) | 2012-05-16 | 2015-04-29 | Rana医疗有限公司 | 用于调节基因表达的组合物和方法 |
| WO2013184209A1 (en) | 2012-06-04 | 2013-12-12 | Ludwig Institute For Cancer Research Ltd. | Mif for use in methods of treating subjects with a neurodegenerative disorder |
| JP2015165772A (ja) * | 2012-07-04 | 2015-09-24 | 国立大学法人大阪大学 | オリゴヌクレオチド、およびオリゴヌクレオチドを有効成分として含有する脂質異常症治療剤 |
| EP2906697A4 (en) | 2012-10-15 | 2016-06-22 | Ionis Pharmaceuticals Inc | METHOD FOR MONITORING THE C9ORF72 EXPRESSION |
| US10443052B2 (en) | 2012-10-15 | 2019-10-15 | Ionis Pharmaceuticals, Inc. | Compositions for modulating C9ORF72 expression |
| FI2906696T4 (fi) | 2012-10-15 | 2023-03-18 | Menetelmiä c9orf72:n ilmentymisen moduloimiseksi | |
| US10058630B2 (en) | 2012-10-22 | 2018-08-28 | Concievalve, Llc | Methods for inhibiting stenosis, obstruction, or calcification of a stented heart valve or bioprosthesis |
| CA2889044A1 (en) | 2012-11-15 | 2014-05-22 | Roche Innovation Center Copenhagen A/S | Anti apob antisense conjugate compounds |
| KR102228358B1 (ko) | 2012-12-21 | 2021-03-16 | 쉬케후세트 솔란데트 에이치에프 | 신경 장애 및 통증의 ｅｇｆｒ 표적 치료 |
| CA2893801A1 (en) | 2013-01-30 | 2014-08-07 | F. Hoffmann-La Roche Ag | Lna oligonucleotide carbohydrate conjugates |
| WO2014132671A1 (en) | 2013-03-01 | 2014-09-04 | National University Corporation Tokyo Medical And Dental University | Chimeric single-stranded antisense polynucleotides and double-stranded antisense agent |
| JP6472087B2 (ja) | 2013-05-30 | 2019-02-27 | 国立大学法人 東京医科歯科大学 | 治療用オリゴヌクレオチドを送達するための二本鎖剤 |
| CN105324119A (zh) | 2013-06-16 | 2016-02-10 | 国立大学法人东京医科齿科大学 | 具有外显子跳跃效应的双链反义核酸 |
| MX367083B (es) * | 2013-06-27 | 2019-08-05 | Roche Innovation Ct Copenhagen As | Oligomeros antisentido y conjugados con diana en la proteina-convertasa subtilisina/kexina tipo 9(pcsk9). |
| WO2015006554A1 (en) | 2013-07-10 | 2015-01-15 | The Regents Of The University Of Michigan | Therapeutic antibodies and uses thereof |
| MY192689A (en) | 2013-10-11 | 2022-09-01 | Ionis Pharmaceuticals Inc | Compositions for modulating c9orf72 expression |
| EP3161159B1 (en) | 2014-06-25 | 2020-08-05 | The General Hospital Corporation | Targeting human satellite ii (hsatii) |
| EP3271405A1 (en) * | 2015-03-20 | 2018-01-24 | Aarhus Universitet | Inhibitors of pcsk9 for treatment of lipoprotein metabolism disorders |
| AU2016248997B2 (en) * | 2015-04-15 | 2019-03-07 | ConcieValve LLC | Devices and methods for inhibiting stenosis, obstruction, or calcification of a native heart valve, stented heart valve or bioprosthesis |
| WO2016168592A2 (en) | 2015-04-16 | 2016-10-20 | Ionis Pharmaceuticals, Inc. | Compositions for modulating c9orf72 expression |
| WO2017079291A1 (en) | 2015-11-02 | 2017-05-11 | Ionis Pharmaceuticals, Inc. | Compounds and methods for modulating c90rf72 |
| US11384112B2 (en) | 2016-02-17 | 2022-07-12 | Tokyo Institute Of Technology | Artificial nucleoside and artificial nucleotide, and artificial oligonucleotide |
| US11433089B2 (en) | 2016-09-23 | 2022-09-06 | National University Corporation Tokyo Medical And Dental University | Blood-brain barrier permeable heteroduplex nucleic acid |
| US11260134B2 (en) | 2016-09-29 | 2022-03-01 | National University Corporation Tokyo Medical And Dental University | Double-stranded nucleic acid complex having overhang |
| JP7188087B2 (ja) | 2017-02-06 | 2022-12-13 | 日産化学株式会社 | 一本鎖オリゴヌクレオチド |
| US11273222B2 (en) | 2017-05-26 | 2022-03-15 | National Cerebral And Cardiovascular Center | Antisense nucleic acid targeting PCSK9 |
| JP6974872B2 (ja) | 2017-06-30 | 2021-12-01 | 国立大学法人 東京医科歯科大学 | ヘテロ二本鎖型ａｎｔｉｍｉＲ |
| US11555188B2 (en) | 2017-07-26 | 2023-01-17 | Nissan Chemical Corporation | Single-stranded oligonucleotide |
| US11674141B2 (en) | 2018-02-28 | 2023-06-13 | National University Corporation Tokyo Medical And Dental University | Ischemic-lesion-site-specific gene therapy |
| EP3766972B1 (en) | 2018-03-14 | 2025-04-23 | Institute of Science Tokyo | Nucleic acid complex |
| US11851654B2 (en) | 2018-03-19 | 2023-12-26 | National University Corporation Tokyo Medical And Dental University | Nucleic acid with reduced toxicity |
| EP3770256A4 (en) | 2018-03-20 | 2021-12-22 | Tokyo Institute of Technology | ANTISENSE OLIGONUCLEOTIDE WITH REDUCED TOXICITY |
| JP7262816B2 (ja) | 2018-03-22 | 2023-04-24 | 国立大学法人 東京医科歯科大学 | ヘテロ核酸のｂｂｂ通過脂質リガンド |
| CN112512584A (zh) | 2018-07-27 | 2021-03-16 | 国立大学法人大阪大学 | 用于抑制衰老、预防、改善或治疗衰老相关疾病或症状、或者延长寿命的组合物 |
| EP3830259A4 (en) | 2018-08-02 | 2022-05-04 | Dyne Therapeutics, Inc. | MUSCLE TARGETED COMPLEXES AND THEIR USES IN THE TREATMENT OF FACIOSCAPULOHUMERAL MUSCULAR DYSTROPHY |
| EP3981431A4 (en) | 2019-03-14 | 2023-06-28 | Rena Therapeutics Inc. | Nucleic acid complex for modulating ihh expression |
| CN113677374A (zh) | 2019-04-08 | 2021-11-19 | 国立大学法人东京医科齿科大学 | 肌疾病治疗用药物组合物 |
| WO2021054370A1 (ja) | 2019-09-18 | 2021-03-25 | 国立大学法人東京医科歯科大学 | 核酸複合体 |
| EP4043565A4 (en) | 2019-10-11 | 2024-01-24 | National University Corporation Tokyo Medical and Dental University | MODIFIED HETERONUCLEIC ACID |
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| EP4353266A4 (en) | 2021-05-31 | 2026-04-29 | Rena Therapeutics Inc | LIGAND-BOND NUCLEIC ACID COMPLEX |
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| WO2023026994A1 (ja) | 2021-08-21 | 2023-03-02 | 武田薬品工業株式会社 | ヒトトランスフェリンレセプター結合ペプチド－薬物コンジュゲート |
| US20250179486A1 (en) | 2021-09-15 | 2025-06-05 | National University Corporation Tokyo Medical And Dental University | Heteronucleic acid including 2'-modified nucleoside |
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| WO2024071099A1 (ja) | 2022-09-29 | 2024-04-04 | 国立大学法人東京医科歯科大学 | ５'－シクロプロピレン修飾を含む核酸分子 |
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| WO2025047953A1 (ja) | 2023-08-30 | 2025-03-06 | 株式会社Stratoimmune | ＲａｓＧＲＰ４のアンチセンスオリゴヌクレオチド |
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-
2007
- 2007-10-09 EP EP07821072A patent/EP2076597A2/en not_active Withdrawn
- 2007-10-09 AU AU2007306361A patent/AU2007306361A1/en not_active Abandoned
- 2007-10-09 US US12/444,806 patent/US20100216864A1/en not_active Abandoned
- 2007-10-09 MX MX2009003729A patent/MX2009003729A/es not_active Application Discontinuation
- 2007-10-09 ES ES11181596.5T patent/ES2603379T3/es active Active
- 2007-10-09 WO PCT/EP2007/060703 patent/WO2008043753A2/en not_active Ceased
- 2007-10-09 EP EP11181596.5A patent/EP2444494B1/en active Active
- 2007-10-09 CA CA2666191A patent/CA2666191C/en active Active
- 2007-10-09 JP JP2009531824A patent/JP2010505432A/ja not_active Withdrawn
-
2009
- 2009-03-18 IL IL197668A patent/IL197668A0/en active IP Right Grant
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