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) | CN103298475A (https=) |
| WO (1) | WO2012030626A2 (https=) |
Families Citing this family (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR101926419B1 (ko) * | 2010-08-30 | 2018-12-10 | 스프링 뱅크 파마슈티칼스, 인크. | 치료제로서 올리고뉴클레오타이드 유사체의 설계 |
| US9012427B2 (en) * | 2012-03-22 | 2015-04-21 | Alios Biopharma, Inc. | Pharmaceutical combinations comprising a thionucleotide analog |
| EP2956145A4 (en) * | 2013-02-18 | 2016-08-17 | Spring Bank Pharmaceuticals Inc | DESIGN OF SHORT OLIGONUCLEOTIDES AS VACCINATE ADJUVANTIES AND THERAPEUTICS |
| 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 |
| KR20170132327A (ko) * | 2015-04-07 | 2017-12-01 | 스프링 뱅크 파마슈티칼스, 인크. | Hbv 감염의 치료를 위한 조성물 및 방법 |
| 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 |
| WO2018009466A1 (en) * | 2016-07-05 | 2018-01-11 | Aduro Biotech, Inc. | Locked nucleic acid cyclic dinucleotide compounds and uses thereof |
| MX2019000660A (es) * | 2016-07-15 | 2019-10-02 | Sperovie Biosciences Inc | Compuestos, composiciones y métodos para el tratamiento de enfermedades. |
| WO2018013887A1 (en) * | 2016-07-15 | 2018-01-18 | Sperovie Biosciences, Inc. | Compounds, compositions, and methods for the treatment of disease |
| JP2019532027A (ja) | 2016-08-17 | 2019-11-07 | ソルスティス バイオロジクス，リミティッド | ポリヌクレオチド構築物 |
| WO2019006455A1 (en) | 2017-06-30 | 2019-01-03 | Solstice Biologics, Ltd. | AUXILIARIES OF CHIRAL PHOSPHORAMIDITIS AND METHODS OF USE THEREOF |
| 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 |
| WO2021237067A1 (en) * | 2020-05-22 | 2021-11-25 | 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 |
|---|---|---|---|---|
| CN101113160A (zh) | 2001-05-16 | 2008-01-30 | 米珍尼克斯公司 | 基于核酸的化合物及其使用方法 |
| CN101094594B (zh) * | 2003-12-08 | 2012-08-15 | 海布里顿公司 | 通过基于小寡核苷酸的化合物调节免疫刺激性质 |
| WO2005097993A2 (en) * | 2004-02-19 | 2005-10-20 | Coley Pharmaceutical Group, Inc. | Immunostimulatory viral rna oligonucleotides |
| 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 |
| EP3342415B1 (en) * | 2006-08-08 | 2022-01-26 | Rheinische Friedrich-Wilhelms-Universität Bonn | Structure and use of 5' phosphate oligonucleotides |
| 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 |
| EP2297323A1 (en) * | 2008-05-21 | 2011-03-23 | Hartmann, Gunther | 5' triphosphate oligonucleotide with blunt end and uses thereof |
| KR101926419B1 (ko) * | 2010-08-30 | 2018-12-10 | 스프링 뱅크 파마슈티칼스, 인크. | 치료제로서 올리고뉴클레오타이드 유사체의 설계 |
-
2011
- 2011-08-25 KR KR1020137008383A patent/KR101926419B1/ko not_active Expired - Fee Related
- 2011-08-25 US US13/218,259 patent/US9040234B2/en not_active Expired - Fee Related
- 2011-08-25 JP JP2013527134A patent/JP2014500230A/ja active Pending
- 2011-08-25 CN CN2011800522858A patent/CN103298475A/zh active Pending
- 2011-08-25 CN CN201711195027.0A patent/CN107973833A/zh active Pending
- 2011-08-25 WO PCT/US2011/049213 patent/WO2012030626A2/en not_active Ceased
- 2011-08-25 EP EP19151383.7A patent/EP3524252A1/en not_active Withdrawn
- 2011-08-25 EP EP11822383.3A patent/EP2611451A4/en not_active Ceased
-
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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