JP2014500230A5 - - Google Patents
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- JP2014500230A5 JP2014500230A5 JP2013527134A JP2013527134A JP2014500230A5 JP 2014500230 A5 JP2014500230 A5 JP 2014500230A5 JP 2013527134 A JP2013527134 A JP 2013527134A JP 2013527134 A JP2013527134 A JP 2013527134A JP 2014500230 A5 JP2014500230 A5 JP 2014500230A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- aryl
- independently
- substituted
- aralkyl
- 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.)
- Pending
Links
- 125000000217 alkyl group Chemical group 0.000 claims 33
- 125000000547 substituted alkyl group Chemical group 0.000 claims 33
- 125000003710 aryl alkyl group Chemical group 0.000 claims 27
- 125000003118 aryl group Chemical group 0.000 claims 27
- ISAKRJDGNUQOIC-UHFFFAOYSA-N Uracil Chemical compound O=C1C=CNC(=O)N1 ISAKRJDGNUQOIC-UHFFFAOYSA-N 0.000 claims 26
- 150000001875 compounds Chemical class 0.000 claims 23
- 125000000753 cycloalkyl group Chemical group 0.000 claims 20
- 125000000623 heterocyclic group Chemical group 0.000 claims 20
- 125000003107 substituted aryl group Chemical group 0.000 claims 20
- 150000003839 salts Chemical class 0.000 claims 15
- 125000001572 5'-adenylyl group Chemical group C=12N=C([H])N=C(N([H])[H])C=1N=C([H])N2[C@@]1([H])[C@@](O[H])([H])[C@@](O[H])([H])[C@](C(OP(=O)(O[H])[*])([H])[H])([H])O1 0.000 claims 13
- 125000001417 5'-guanylyl group Chemical group C=12N=C(N([H])[H])N([H])C(=O)C=1N=C([H])N2[C@@]1([H])[C@@](O[H])([H])[C@@](O[H])([H])[C@](C(OP(=O)(O[H])[*])([H])[H])([H])O1 0.000 claims 13
- 108091034117 Oligonucleotide Proteins 0.000 claims 13
- 239000001177 diphosphate Substances 0.000 claims 13
- XPPKVPWEQAFLFU-UHFFFAOYSA-J diphosphate(4-) Chemical compound [O-]P([O-])(=O)OP([O-])([O-])=O XPPKVPWEQAFLFU-UHFFFAOYSA-J 0.000 claims 13
- 235000011180 diphosphates Nutrition 0.000 claims 13
- 229910052739 hydrogen Inorganic materials 0.000 claims 13
- 239000001257 hydrogen Substances 0.000 claims 13
- 125000004435 hydrogen atom Chemical class [H]* 0.000 claims 13
- 150000004712 monophosphates Chemical class 0.000 claims 13
- 125000003835 nucleoside group Chemical class 0.000 claims 13
- 125000002264 triphosphate group Chemical group [H]OP(=O)(O[H])OP(=O)(O[H])OP(=O)(O[H])O* 0.000 claims 13
- 229940035893 uracil Drugs 0.000 claims 13
- 108091032973 (ribonucleotides)n+m Proteins 0.000 claims 8
- 108020004459 Small interfering RNA Proteins 0.000 claims 8
- 239000012634 fragment Substances 0.000 claims 7
- 238000000034 method Methods 0.000 claims 7
- 239000008194 pharmaceutical composition Substances 0.000 claims 7
- 230000003637 steroidlike Effects 0.000 claims 7
- 230000001404 mediated effect Effects 0.000 claims 6
- 239000002773 nucleotide Substances 0.000 claims 6
- 125000003729 nucleotide group Chemical group 0.000 claims 6
- 230000000845 anti-microbial effect Effects 0.000 claims 4
- 238000007385 chemical modification Methods 0.000 claims 4
- 102000040650 (ribonucleotides)n+m Human genes 0.000 claims 3
- 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 3
- 230000001413 cellular effect Effects 0.000 claims 3
- HBAQYPYDRFILMT-UHFFFAOYSA-N 8-[3-(1-cyclopropylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical class C1(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O HBAQYPYDRFILMT-UHFFFAOYSA-N 0.000 claims 2
- 239000004599 antimicrobial Substances 0.000 claims 2
- 230000002401 inhibitory effect Effects 0.000 claims 2
- 238000004519 manufacturing process Methods 0.000 claims 2
- 230000009437 off-target effect Effects 0.000 claims 2
- -1 racemic Chemical class 0.000 claims 2
- 230000001225 therapeutic effect Effects 0.000 claims 2
- 102000044503 Antimicrobial Peptides Human genes 0.000 claims 1
- 108700042778 Antimicrobial Peptides Proteins 0.000 claims 1
- 241000450599 DNA viruses Species 0.000 claims 1
- 241000710831 Flavivirus Species 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- 206010046865 Vaccinia virus infection Diseases 0.000 claims 1
- 208000036142 Viral infection Diseases 0.000 claims 1
- 241000700605 Viruses Species 0.000 claims 1
- 230000001093 anti-cancer Effects 0.000 claims 1
- 230000000692 anti-sense effect Effects 0.000 claims 1
- 239000002246 antineoplastic agent Substances 0.000 claims 1
- 230000005775 apoptotic pathway Effects 0.000 claims 1
- 239000000090 biomarker Substances 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 229940125898 compound 5 Drugs 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 241001493065 dsRNA viruses Species 0.000 claims 1
- 230000002708 enhancing effect Effects 0.000 claims 1
- 230000003308 immunostimulating effect Effects 0.000 claims 1
- 238000000338 in vitro Methods 0.000 claims 1
- 238000001727 in vivo Methods 0.000 claims 1
- 208000015181 infectious disease Diseases 0.000 claims 1
- 206010022000 influenza Diseases 0.000 claims 1
- 230000000813 microbial effect Effects 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 108090000765 processed proteins & peptides Proteins 0.000 claims 1
- 102000004169 proteins and genes Human genes 0.000 claims 1
- 108090000623 proteins and genes Proteins 0.000 claims 1
- 230000001105 regulatory effect Effects 0.000 claims 1
- 230000004936 stimulating effect Effects 0.000 claims 1
- 239000000126 substance Substances 0.000 claims 1
- 208000007089 vaccinia Diseases 0.000 claims 1
- 230000009385 viral infection Effects 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US40238010P | 2010-08-30 | 2010-08-30 | |
| US61/402,380 | 2010-08-30 | ||
| PCT/US2011/049213 WO2012030626A2 (en) | 2010-08-30 | 2011-08-25 | Design of oligonucleotide analogs as therapeutic agents |
Related Child Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016028052A Division JP6210392B2 (ja) | 2010-08-30 | 2016-02-17 | 治療薬としてオリゴヌクレオチド類縁体の設計 |
| JP2017157747A Division JP2018010001A (ja) | 2010-08-30 | 2017-08-18 | 治療薬としてオリゴヌクレオチド類縁体の設計 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2014500230A JP2014500230A (ja) | 2014-01-09 |
| JP2014500230A5 true JP2014500230A5 (https=) | 2014-10-09 |
Family
ID=45698055
Family Applications (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2013527134A Pending JP2014500230A (ja) | 2010-08-30 | 2011-08-25 | 治療薬としてオリゴヌクレオチド類縁体の設計 |
| JP2016028052A Expired - Fee Related JP6210392B2 (ja) | 2010-08-30 | 2016-02-17 | 治療薬としてオリゴヌクレオチド類縁体の設計 |
| JP2017157747A Pending JP2018010001A (ja) | 2010-08-30 | 2017-08-18 | 治療薬としてオリゴヌクレオチド類縁体の設計 |
Family Applications After (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016028052A Expired - Fee Related JP6210392B2 (ja) | 2010-08-30 | 2016-02-17 | 治療薬としてオリゴヌクレオチド類縁体の設計 |
| JP2017157747A Pending JP2018010001A (ja) | 2010-08-30 | 2017-08-18 | 治療薬としてオリゴヌクレオチド類縁体の設計 |
Country Status (6)
| Country | Link |
|---|---|
| US (2) | US9040234B2 (https=) |
| EP (2) | EP3524252A1 (https=) |
| JP (3) | JP2014500230A (https=) |
| KR (1) | KR101926419B1 (https=) |
| CN (2) | CN107973833A (https=) |
| WO (1) | WO2012030626A2 (https=) |
Families Citing this family (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US9040234B2 (en) * | 2010-08-30 | 2015-05-26 | Spring Bank Pharmaceuticals, Inc. | Oligonucleotide analogs as therapeutic agents |
| WO2013142157A1 (en) * | 2012-03-22 | 2013-09-26 | Alios Biopharma, Inc. | Pharmaceutical combinations comprising a thionucleotide analog |
| JP6502267B2 (ja) * | 2013-02-18 | 2019-04-17 | スプリング バンク ファーマシューティカルズ，インコーポレイテッド | ワクチンアジュバントおよび治療剤としての短鎖オリゴヌクレオチドの設計 |
| ES2891903T3 (es) * | 2015-02-17 | 2022-01-31 | Cipherome Inc | Método para seleccionar agente antineoplásico basado en información de daño proteínico de individuos para evitar los efectos secundarios del agente antineoplásico |
| WO2016164619A2 (en) * | 2015-04-07 | 2016-10-13 | Spring Bank Pharmaceuticals, Inc. | Compositions and methods for the treatment of hbv infection |
| EP3317290A4 (en) * | 2015-07-02 | 2019-04-10 | Spring Bank Pharmaceuticals, Inc. | COMPOSITIONS AND METHOD FOR TREATING VIRUS INFECTION |
| TW201717968A (zh) * | 2015-07-14 | 2017-06-01 | 春季銀行製藥公司 | 誘導ｒｉｇ－ｉ和其他模式辨識受體之化合物及組成物 |
| EP3507367A4 (en) * | 2016-07-05 | 2020-03-25 | Aduro BioTech, Inc. | CYCLIC DINUCLEOTID COMPOUNDS WITH INCLUDED NUCLEIC ACIDS AND USES THEREOF |
| WO2018013887A1 (en) * | 2016-07-15 | 2018-01-18 | Sperovie Biosciences, Inc. | Compounds, compositions, and methods for the treatment of disease |
| CN109715202A (zh) * | 2016-07-15 | 2019-05-03 | 斯必乐维生物科学公司 | 用于治疗疾病的化合物、组合物和方法 |
| CA3033867A1 (en) | 2016-08-17 | 2018-02-22 | Solstice Biologics, Ltd. | Polynucleotide constructs |
| US11597744B2 (en) | 2017-06-30 | 2023-03-07 | Sirius Therapeutics, Inc. | Chiral phosphoramidite auxiliaries and methods of their use |
| CN111484541B (zh) * | 2019-01-25 | 2023-06-02 | 博瑞生物医药（苏州）股份有限公司 | 双核苷酸前体药物及其制备方法 |
| US20230242918A1 (en) * | 2020-05-22 | 2023-08-03 | President And Fellows Of Harvard College | Interferon- inducing oligonucleotide duplexes and methods of use |
Family Cites Families (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2002092006A2 (en) * | 2001-05-16 | 2002-11-21 | Micrologix Biotech, Inc. | Nucleic acid-based compounds and methods of use thereof |
| CA2549173A1 (en) | 2003-12-08 | 2005-07-07 | Hybridon, Inc. | Modulation of immunostimulatory properties by small oligonucleotide-based compounds |
| JP2007526253A (ja) | 2004-02-19 | 2007-09-13 | コーリー ファーマシューティカル グループ，インコーポレイテッド | 免疫刺激性ウイルスｒｎａオリゴヌクレオチド |
| JP2008523785A (ja) | 2004-10-12 | 2008-07-10 | カーランテック，インコーポレーテッド | 神経変性、自己免疫脱髄、および糖尿病のウイルス病原に対する動物モデル系 |
| US8076303B2 (en) * | 2005-12-13 | 2011-12-13 | Spring Bank Pharmaceuticals, Inc. | Nucleotide and oligonucleotide prodrugs |
| ES2911034T3 (es) * | 2006-08-08 | 2022-05-17 | Univ Bonn Rheinische Friedrich Wilhelms | Estructura y uso de oligonucleótidos 5' fosfato |
| US20100040576A1 (en) * | 2007-12-18 | 2010-02-18 | The Texas A&M University System | Modified Oligonucleotides For The Treatment Of Hepatitis C Infection |
| GB2471806B (en) * | 2008-04-03 | 2012-12-19 | Spring Bank Pharmaceuticals Inc | Compositions and methods for treating viral infections |
| WO2009141146A1 (en) * | 2008-05-21 | 2009-11-26 | Gunther Hartmann | 5' triphosphate oligonucleotide with blunt end and uses thereof |
| US9040234B2 (en) * | 2010-08-30 | 2015-05-26 | Spring Bank Pharmaceuticals, Inc. | Oligonucleotide analogs as therapeutic agents |
-
2011
- 2011-08-25 US US13/218,259 patent/US9040234B2/en not_active Expired - Fee Related
- 2011-08-25 CN CN201711195027.0A patent/CN107973833A/zh active Pending
- 2011-08-25 EP EP19151383.7A patent/EP3524252A1/en not_active Withdrawn
- 2011-08-25 EP EP11822383.3A patent/EP2611451A4/en not_active Ceased
- 2011-08-25 CN CN2011800522858A patent/CN103298475A/zh active Pending
- 2011-08-25 JP JP2013527134A patent/JP2014500230A/ja active Pending
- 2011-08-25 WO PCT/US2011/049213 patent/WO2012030626A2/en not_active Ceased
- 2011-08-25 KR KR1020137008383A patent/KR101926419B1/ko not_active Expired - Fee Related
-
2015
- 2015-04-20 US US14/691,019 patent/US20150329864A1/en not_active Abandoned
-
2016
- 2016-02-17 JP JP2016028052A patent/JP6210392B2/ja not_active Expired - Fee Related
-
2017
- 2017-08-18 JP JP2017157747A patent/JP2018010001A/ja active Pending
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