JP2014503192A5 - - Google Patents
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- Publication number
- JP2014503192A5 JP2014503192A5 JP2013537906A JP2013537906A JP2014503192A5 JP 2014503192 A5 JP2014503192 A5 JP 2014503192A5 JP 2013537906 A JP2013537906 A JP 2013537906A JP 2013537906 A JP2013537906 A JP 2013537906A JP 2014503192 A5 JP2014503192 A5 JP 2014503192A5
- Authority
- JP
- Japan
- Prior art keywords
- oligonucleotide
- base
- modification
- nucleotides
- aminocarbonyl
- 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.)
- Granted
Links
- 108091034117 Oligonucleotide Proteins 0.000 claims 47
- 238000012986 modification Methods 0.000 claims 15
- 230000004048 modification Effects 0.000 claims 15
- 125000003729 nucleotide group Chemical group 0.000 claims 15
- 239000002773 nucleotide Substances 0.000 claims 14
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims 10
- 239000008194 pharmaceutical composition Substances 0.000 claims 9
- 210000004027 cell Anatomy 0.000 claims 5
- 238000000034 method Methods 0.000 claims 4
- 239000002679 microRNA Substances 0.000 claims 4
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 3
- 125000001424 substituent group Chemical group 0.000 claims 3
- 108700011259 MicroRNAs Proteins 0.000 claims 2
- CZPWVGJYEJSRLH-UHFFFAOYSA-N Pyrimidine Chemical group C1=CN=CN=C1 CZPWVGJYEJSRLH-UHFFFAOYSA-N 0.000 claims 2
- DRTQHJPVMGBUCF-XVFCMESISA-N Uridine Chemical compound O[C@@H]1[C@H](O)[C@@H](CO)O[C@H]1N1C(=O)NC(=O)C=C1 DRTQHJPVMGBUCF-XVFCMESISA-N 0.000 claims 2
- 125000003342 alkenyl group Chemical group 0.000 claims 2
- 125000000217 alkyl group Chemical group 0.000 claims 2
- 230000000295 complement effect Effects 0.000 claims 2
- 239000003937 drug carrier Substances 0.000 claims 2
- RAXXELZNTBOGNW-UHFFFAOYSA-N imidazole Natural products C1=CNC=N1 RAXXELZNTBOGNW-UHFFFAOYSA-N 0.000 claims 2
- 108091071651 miR-208 stem-loop Proteins 0.000 claims 2
- 108091084446 miR-208a stem-loop Proteins 0.000 claims 2
- 108091062547 miR-208a-1 stem-loop Proteins 0.000 claims 2
- 108091055375 miR-208a-2 stem-loop Proteins 0.000 claims 2
- 108091070501 miRNA Proteins 0.000 claims 2
- 239000000693 micelle Substances 0.000 claims 2
- 238000007911 parenteral administration Methods 0.000 claims 2
- 235000000346 sugar Nutrition 0.000 claims 2
- RYYWUUFWQRZTIU-UHFFFAOYSA-K thiophosphate Chemical compound [O-]P([O-])([O-])=S RYYWUUFWQRZTIU-UHFFFAOYSA-K 0.000 claims 2
- RWQNBRDOKXIBIV-UHFFFAOYSA-N thymine Chemical compound CC1=CNC(=O)NC1=O RWQNBRDOKXIBIV-UHFFFAOYSA-N 0.000 claims 2
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical group [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 1
- 206010007572 Cardiac hypertrophy Diseases 0.000 claims 1
- 208000006029 Cardiomegaly Diseases 0.000 claims 1
- 206010019280 Heart failures Diseases 0.000 claims 1
- 229910019142 PO4 Inorganic materials 0.000 claims 1
- KDCGOANMDULRCW-UHFFFAOYSA-N Purine Natural products N1=CNC2=NC=NC2=C1 KDCGOANMDULRCW-UHFFFAOYSA-N 0.000 claims 1
- FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 claims 1
- JLCPHMBAVCMARE-UHFFFAOYSA-N [3-[[3-[[3-[[3-[[3-[[3-[[3-[[3-[[3-[[3-[[3-[[5-(2-amino-6-oxo-1H-purin-9-yl)-3-[[3-[[3-[[3-[[3-[[3-[[5-(2-amino-6-oxo-1H-purin-9-yl)-3-[[5-(2-amino-6-oxo-1H-purin-9-yl)-3-hydroxyoxolan-2-yl]methoxy-hydroxyphosphoryl]oxyoxolan-2-yl]methoxy-hydroxyphosphoryl]oxy-5-(5-methyl-2,4-dioxopyrimidin-1-yl)oxolan-2-yl]methoxy-hydroxyphosphoryl]oxy-5-(6-aminopurin-9-yl)oxolan-2-yl]methoxy-hydroxyphosphoryl]oxy-5-(6-aminopurin-9-yl)oxolan-2-yl]methoxy-hydroxyphosphoryl]oxy-5-(6-aminopurin-9-yl)oxolan-2-yl]methoxy-hydroxyphosphoryl]oxy-5-(6-aminopurin-9-yl)oxolan-2-yl]methoxy-hydroxyphosphoryl]oxyoxolan-2-yl]methoxy-hydroxyphosphoryl]oxy-5-(5-methyl-2,4-dioxopyrimidin-1-yl)oxolan-2-yl]methoxy-hydroxyphosphoryl]oxy-5-(4-amino-2-oxopyrimidin-1-yl)oxolan-2-yl]methoxy-hydroxyphosphoryl]oxy-5-(5-methyl-2,4-dioxopyrimidin-1-yl)oxolan-2-yl]methoxy-hydroxyphosphoryl]oxy-5-(5-methyl-2,4-dioxopyrimidin-1-yl)oxolan-2-yl]methoxy-hydroxyphosphoryl]oxy-5-(6-aminopurin-9-yl)oxolan-2-yl]methoxy-hydroxyphosphoryl]oxy-5-(6-aminopurin-9-yl)oxolan-2-yl]methoxy-hydroxyphosphoryl]oxy-5-(4-amino-2-oxopyrimidin-1-yl)oxolan-2-yl]methoxy-hydroxyphosphoryl]oxy-5-(4-amino-2-oxopyrimidin-1-yl)oxolan-2-yl]methoxy-hydroxyphosphoryl]oxy-5-(4-amino-2-oxopyrimidin-1-yl)oxolan-2-yl]methoxy-hydroxyphosphoryl]oxy-5-(6-aminopurin-9-yl)oxolan-2-yl]methoxy-hydroxyphosphoryl]oxy-5-(4-amino-2-oxopyrimidin-1-yl)oxolan-2-yl]methyl [5-(6-aminopurin-9-yl)-2-(hydroxymethyl)oxolan-3-yl] hydrogen phosphate Polymers Cc1cn(C2CC(OP(O)(=O)OCC3OC(CC3OP(O)(=O)OCC3OC(CC3O)n3cnc4c3nc(N)[nH]c4=O)n3cnc4c3nc(N)[nH]c4=O)C(COP(O)(=O)OC3CC(OC3COP(O)(=O)OC3CC(OC3COP(O)(=O)OC3CC(OC3COP(O)(=O)OC3CC(OC3COP(O)(=O)OC3CC(OC3COP(O)(=O)OC3CC(OC3COP(O)(=O)OC3CC(OC3COP(O)(=O)OC3CC(OC3COP(O)(=O)OC3CC(OC3COP(O)(=O)OC3CC(OC3COP(O)(=O)OC3CC(OC3COP(O)(=O)OC3CC(OC3COP(O)(=O)OC3CC(OC3COP(O)(=O)OC3CC(OC3COP(O)(=O)OC3CC(OC3COP(O)(=O)OC3CC(OC3COP(O)(=O)OC3CC(OC3CO)n3cnc4c(N)ncnc34)n3ccc(N)nc3=O)n3cnc4c(N)ncnc34)n3ccc(N)nc3=O)n3ccc(N)nc3=O)n3ccc(N)nc3=O)n3cnc4c(N)ncnc34)n3cnc4c(N)ncnc34)n3cc(C)c(=O)[nH]c3=O)n3cc(C)c(=O)[nH]c3=O)n3ccc(N)nc3=O)n3cc(C)c(=O)[nH]c3=O)n3cnc4c3nc(N)[nH]c4=O)n3cnc4c(N)ncnc34)n3cnc4c(N)ncnc34)n3cnc4c(N)ncnc34)n3cnc4c(N)ncnc34)O2)c(=O)[nH]c1=O JLCPHMBAVCMARE-UHFFFAOYSA-N 0.000 claims 1
- 230000003187 abdominal effect Effects 0.000 claims 1
- 125000003118 aryl group Chemical group 0.000 claims 1
- 239000011324 bead Substances 0.000 claims 1
- DRTQHJPVMGBUCF-PSQAKQOGSA-N beta-L-uridine Natural products O[C@H]1[C@@H](O)[C@H](CO)O[C@@H]1N1C(=O)NC(=O)C=C1 DRTQHJPVMGBUCF-PSQAKQOGSA-N 0.000 claims 1
- 229910052799 carbon Inorganic materials 0.000 claims 1
- 230000000747 cardiac effect Effects 0.000 claims 1
- 125000002091 cationic group Chemical group 0.000 claims 1
- 238000001246 colloidal dispersion Methods 0.000 claims 1
- 239000002131 composite material Substances 0.000 claims 1
- 238000013270 controlled release Methods 0.000 claims 1
- 125000000753 cycloalkyl group Chemical group 0.000 claims 1
- 230000003111 delayed effect Effects 0.000 claims 1
- GLUUGHFHXGJENI-UHFFFAOYSA-N diethylenediamine Natural products C1CNCCN1 GLUUGHFHXGJENI-UHFFFAOYSA-N 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 230000002526 effect on cardiovascular system Effects 0.000 claims 1
- 230000000694 effects Effects 0.000 claims 1
- 210000002064 heart cell Anatomy 0.000 claims 1
- 210000005003 heart tissue Anatomy 0.000 claims 1
- 125000001072 heteroaryl group Chemical group 0.000 claims 1
- 125000000623 heterocyclic group Chemical group 0.000 claims 1
- 150000002460 imidazoles Chemical class 0.000 claims 1
- 238000001727 in vivo Methods 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 claims 1
- 238000002347 injection Methods 0.000 claims 1
- 239000007924 injection Substances 0.000 claims 1
- 238000007918 intramuscular administration Methods 0.000 claims 1
- 238000001990 intravenous administration Methods 0.000 claims 1
- 125000005647 linker group Chemical group 0.000 claims 1
- 239000002502 liposome Substances 0.000 claims 1
- 210000004962 mammalian cell Anatomy 0.000 claims 1
- 230000001404 mediated effect Effects 0.000 claims 1
- 108091031326 miR-15b stem-loop Proteins 0.000 claims 1
- 108091047268 miR-208b stem-loop Proteins 0.000 claims 1
- 108091062762 miR-21 stem-loop Proteins 0.000 claims 1
- 108091041631 miR-21-1 stem-loop Proteins 0.000 claims 1
- 108091044442 miR-21-2 stem-loop Proteins 0.000 claims 1
- 239000004005 microsphere Substances 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 125000004573 morpholin-4-yl group Chemical group N1(CCOCC1)* 0.000 claims 1
- 208000010125 myocardial infarction Diseases 0.000 claims 1
- 239000002088 nanocapsule Substances 0.000 claims 1
- 239000007764 o/w emulsion Substances 0.000 claims 1
- 230000001575 pathological effect Effects 0.000 claims 1
- 230000007170 pathology Effects 0.000 claims 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 1
- NBIIXXVUZAFLBC-UHFFFAOYSA-K phosphate Chemical compound [O-]P([O-])([O-])=O NBIIXXVUZAFLBC-UHFFFAOYSA-K 0.000 claims 1
- 239000010452 phosphate Substances 0.000 claims 1
- 150000004885 piperazines Chemical class 0.000 claims 1
- 150000003053 piperidines Chemical class 0.000 claims 1
- 229920000642 polymer Polymers 0.000 claims 1
- 125000000561 purinyl group Chemical group N1=C(N=C2N=CNC2=C1)* 0.000 claims 1
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 1
- 150000003839 salts Chemical class 0.000 claims 1
- 239000011780 sodium chloride Substances 0.000 claims 1
- 238000007920 subcutaneous administration Methods 0.000 claims 1
- 150000008163 sugars Chemical class 0.000 claims 1
- 239000000829 suppository Substances 0.000 claims 1
- 238000013268 sustained release Methods 0.000 claims 1
- 239000012730 sustained-release form Substances 0.000 claims 1
- 150000003512 tertiary amines Chemical class 0.000 claims 1
- NQRYJNQNLNOLGT-UHFFFAOYSA-N tetrahydropyridine hydrochloride Natural products C1CCNCC1 NQRYJNQNLNOLGT-UHFFFAOYSA-N 0.000 claims 1
- 229940113082 thymine Drugs 0.000 claims 1
- DRTQHJPVMGBUCF-UHFFFAOYSA-N uracil arabinoside Natural products OC1C(O)C(CO)OC1N1C(=O)NC(=O)C=C1 DRTQHJPVMGBUCF-UHFFFAOYSA-N 0.000 claims 1
- 150000003672 ureas Chemical group 0.000 claims 1
- 229940045145 uridine Drugs 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US41067210P | 2010-11-05 | 2010-11-05 | |
| US61/410,672 | 2010-11-05 | ||
| PCT/US2011/059588 WO2012061810A1 (en) | 2010-11-05 | 2011-11-07 | Base modified oligonucleotides |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2014503192A JP2014503192A (ja) | 2014-02-13 |
| JP2014503192A5 true JP2014503192A5 (https=) | 2014-12-25 |
| JP5995855B2 JP5995855B2 (ja) | 2016-09-21 |
Family
ID=46024863
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2013537906A Expired - Fee Related JP5995855B2 (ja) | 2010-11-05 | 2011-11-07 | 塩基修飾オリゴヌクレオチド |
Country Status (7)
| Country | Link |
|---|---|
| US (1) | US9416360B2 (https=) |
| EP (1) | EP2635681B8 (https=) |
| JP (1) | JP5995855B2 (https=) |
| CN (1) | CN103492569B (https=) |
| AU (1) | AU2011323085B2 (https=) |
| CA (1) | CA2817002C (https=) |
| WO (1) | WO2012061810A1 (https=) |
Families Citing this family (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2013202528B2 (en) * | 2010-04-12 | 2015-07-30 | Somalogic Operating Co., Inc. | 5-position modified pyrimidines and their use |
| JP5901610B2 (ja) | 2010-04-12 | 2016-04-13 | ソマロジック・インコーポレーテッド | ５位修飾ピリミジンとその使用 |
| ITRM20110685A1 (it) | 2011-12-23 | 2013-06-24 | Internat Ct For Genetic En Gineering And | Microrna per la rigenerazione cardiaca attraverso l induzione della proliferazione dei miociti cardiaci |
| CN107236735B (zh) * | 2012-06-21 | 2019-11-08 | 米拉根医疗股份有限公司 | 包含锁核酸基序的基于寡核苷酸的抑制剂 |
| DK2970968T3 (en) | 2013-03-15 | 2018-03-05 | Miragen Therapeutics Inc | CONNECTED BICYCLIC Nucleosides |
| KR102290214B1 (ko) | 2013-11-21 | 2021-08-18 | 소마로직, 인크. | 시티딘-5-카르복스아미드 변형된 뉴클레오티드 조성물 및 그와 관련된 방법들 |
| GB201400598D0 (en) | 2014-01-14 | 2014-03-05 | Univ Glasgow | Materials and methods for modulation of tendon healing |
| US20160361340A1 (en) * | 2014-02-11 | 2016-12-15 | Inetitut Pasteur | Treatment of cardiac diseases with modulators of the hippo pathway |
| EP3247716A4 (en) | 2015-01-20 | 2018-10-17 | Miragen Therapeutics, Inc. | Mir-92 inhibitors and uses thereof |
| EP3833762A4 (en) | 2018-08-09 | 2022-09-28 | Verseau Therapeutics, Inc. | Oligonucleotide compositions for targeting ccr2 and csf1r and uses thereof |
| CN110346493B (zh) * | 2019-05-23 | 2021-01-05 | 中国人民解放军军事科学院军事医学研究院 | 检测猕猴血浆中中期因子反义寡核苷酸含量的方法 |
| CN119032177A (zh) * | 2022-06-23 | 2024-11-26 | 安沛治疗有限公司 | 包含喹啉修饰的靶特异性核酸分子 |
| KR20240139119A (ko) * | 2023-03-09 | 2024-09-23 | 주식회사 압타머사이언스 | 티미딘으로부터 개질된 뉴클레오시드의 제조방법 |
| AU2024325721A1 (en) * | 2023-08-17 | 2026-02-26 | Adarx Pharmaceuticals, Inc. | Oligonucleotides containing a ligand at a nucleobase, 2' position, or 3' position |
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| JP5901610B2 (ja) | 2010-04-12 | 2016-04-13 | ソマロジック・インコーポレーテッド | ５位修飾ピリミジンとその使用 |
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-
2011
- 2011-11-07 WO PCT/US2011/059588 patent/WO2012061810A1/en not_active Ceased
- 2011-11-07 CA CA2817002A patent/CA2817002C/en not_active Expired - Fee Related
- 2011-11-07 AU AU2011323085A patent/AU2011323085B2/en not_active Ceased
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- 2011-11-07 EP EP11838938.6A patent/EP2635681B8/en not_active Not-in-force
- 2011-11-07 JP JP2013537906A patent/JP5995855B2/ja not_active Expired - Fee Related
- 2011-11-07 CN CN201180064239.XA patent/CN103492569B/zh not_active Expired - Fee Related
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