JP2009519345A5 - - Google Patents
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- Publication number
- JP2009519345A5 JP2009519345A5 JP2008545782A JP2008545782A JP2009519345A5 JP 2009519345 A5 JP2009519345 A5 JP 2009519345A5 JP 2008545782 A JP2008545782 A JP 2008545782A JP 2008545782 A JP2008545782 A JP 2008545782A JP 2009519345 A5 JP2009519345 A5 JP 2009519345A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- aryl
- compound
- formula
- substituted
- 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
- 150000001875 compounds Chemical class 0.000 claims description 14
- 125000003118 aryl group Chemical group 0.000 claims 7
- 125000000217 alkyl group Chemical group 0.000 claims 6
- 125000003710 aryl alkyl group Chemical group 0.000 claims 6
- 125000000547 substituted alkyl group Chemical group 0.000 claims 6
- 125000000623 heterocyclic group Chemical group 0.000 claims 5
- 125000000753 cycloalkyl group Chemical group 0.000 claims 4
- 239000003814 drug Substances 0.000 claims 4
- 208000015181 infectious disease Diseases 0.000 claims 4
- 125000003107 substituted aryl group Chemical group 0.000 claims 4
- 229910052739 hydrogen Inorganic materials 0.000 claims 3
- 239000001257 hydrogen Substances 0.000 claims 3
- 125000004435 hydrogen atom Chemical class [H]* 0.000 claims 3
- 238000004519 manufacturing process Methods 0.000 claims 3
- ISAKRJDGNUQOIC-UHFFFAOYSA-N Uracil Chemical compound O=C1C=CNC(=O)N1 ISAKRJDGNUQOIC-UHFFFAOYSA-N 0.000 claims 2
- OPTASPLRGRRNAP-UHFFFAOYSA-N cytosine Chemical compound NC=1C=CNC(=O)N=1 OPTASPLRGRRNAP-UHFFFAOYSA-N 0.000 claims 2
- UYTPUPDQBNUYGX-UHFFFAOYSA-N guanine Chemical compound O=C1NC(N)=NC2=C1N=CN2 UYTPUPDQBNUYGX-UHFFFAOYSA-N 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- 150000003431 steroids Chemical class 0.000 claims 2
- RWQNBRDOKXIBIV-UHFFFAOYSA-N thymine Chemical compound CC1=CNC(=O)NC1=O RWQNBRDOKXIBIV-UHFFFAOYSA-N 0.000 claims 2
- 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
- 229960000643 adenine Drugs 0.000 claims 1
- 239000003795 chemical substances by application Substances 0.000 claims 1
- 229940104302 cytosine Drugs 0.000 claims 1
- 229940079593 drug Drugs 0.000 claims 1
- 239000002773 nucleotide Substances 0.000 claims 1
- 125000003729 nucleotide group Chemical group 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 229940113082 thymine Drugs 0.000 claims 1
- 229940035893 uracil Drugs 0.000 claims 1
- 230000007062 hydrolysis Effects 0.000 description 3
- 238000006460 hydrolysis reaction Methods 0.000 description 3
- 108090000371 Esterases Proteins 0.000 description 2
- 102000001708 Protein Isoforms Human genes 0.000 description 2
- 108010029485 Protein Isoforms Proteins 0.000 description 2
- IQFYYKKMVGJFEH-XLPZGREQSA-N Thymidine Chemical compound O=C1NC(=O)C(C)=CN1[C@@H]1O[C@H](CO)[C@@H](O)C1 IQFYYKKMVGJFEH-XLPZGREQSA-N 0.000 description 2
- 238000006243 chemical reaction Methods 0.000 description 2
- 239000000539 dimer Substances 0.000 description 2
- 239000008363 phosphate buffer Substances 0.000 description 2
- 210000002966 serum Anatomy 0.000 description 2
- SXUXMRMBWZCMEN-UHFFFAOYSA-N 2'-O-methyl uridine Natural products COC1C(O)C(CO)OC1N1C(=O)NC(=O)C=C1 SXUXMRMBWZCMEN-UHFFFAOYSA-N 0.000 description 1
- DWRXFEITVBNRMK-UHFFFAOYSA-N Beta-D-1-Arabinofuranosylthymine Natural products O=C1NC(=O)C(C)=CN1C1C(O)C(O)C(CO)O1 DWRXFEITVBNRMK-UHFFFAOYSA-N 0.000 description 1
- 241000283690 Bos taurus Species 0.000 description 1
- 108090000317 Chymotrypsin Proteins 0.000 description 1
- 241000283973 Oryctolagus cuniculus Species 0.000 description 1
- 238000010521 absorption reaction Methods 0.000 description 1
- IQFYYKKMVGJFEH-UHFFFAOYSA-N beta-L-thymidine Natural products O=C1NC(=O)C(C)=CN1C1OC(CO)C(O)C1 IQFYYKKMVGJFEH-UHFFFAOYSA-N 0.000 description 1
- 230000002925 chemical effect Effects 0.000 description 1
- 229960002376 chymotrypsin Drugs 0.000 description 1
- 231100000433 cytotoxic Toxicity 0.000 description 1
- 230000001472 cytotoxic effect Effects 0.000 description 1
- 238000006477 desulfuration reaction Methods 0.000 description 1
- 230000023556 desulfurization Effects 0.000 description 1
- 125000004185 ester group Chemical group 0.000 description 1
- 230000003301 hydrolyzing effect Effects 0.000 description 1
- 210000004185 liver Anatomy 0.000 description 1
- 239000008176 lyophilized powder Substances 0.000 description 1
- 239000000203 mixture Substances 0.000 description 1
- 230000000269 nucleophilic effect Effects 0.000 description 1
- 238000004007 reversed phase HPLC Methods 0.000 description 1
- -1 thiophosphate triester Chemical group 0.000 description 1
- 229940104230 thymidine Drugs 0.000 description 1
Applications Claiming Priority (7)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US75003605P | 2005-12-13 | 2005-12-13 | |
| US60/750,036 | 2005-12-13 | ||
| US80029406P | 2006-05-15 | 2006-05-15 | |
| US60/800,294 | 2006-05-15 | ||
| US11/637,520 US8076303B2 (en) | 2005-12-13 | 2006-12-12 | Nucleotide and oligonucleotide prodrugs |
| US11/637,520 | 2006-12-12 | ||
| PCT/US2006/047617 WO2007070598A2 (en) | 2005-12-13 | 2006-12-13 | Nucleotide and oligonucleotide prodrugs |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2009519345A JP2009519345A (ja) | 2009-05-14 |
| JP2009519345A5 true JP2009519345A5 (https=) | 2012-06-07 |
| JP5044854B2 JP5044854B2 (ja) | 2012-10-10 |
Family
ID=38194676
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2008545782A Expired - Fee Related JP5044854B2 (ja) | 2005-12-13 | 2006-12-13 | ヌクレオチドプロドラッグおよびオリゴヌクレオチドプロドラッグ |
Country Status (17)
| Country | Link |
|---|---|
| US (6) | US8076303B2 (https=) |
| EP (3) | EP3090748B1 (https=) |
| JP (1) | JP5044854B2 (https=) |
| KR (2) | KR101123534B1 (https=) |
| CN (2) | CN101437397B (https=) |
| CY (2) | CY1117576T1 (https=) |
| DK (2) | DK3090748T3 (https=) |
| ES (2) | ES2573928T3 (https=) |
| HR (1) | HRP20160531T1 (https=) |
| HU (2) | HUE029190T2 (https=) |
| IN (1) | IN2015DN01786A (https=) |
| LT (1) | LT3090748T (https=) |
| PL (2) | PL1968612T3 (https=) |
| PT (1) | PT3090748T (https=) |
| RS (1) | RS54867B1 (https=) |
| SI (2) | SI1968612T1 (https=) |
| WO (1) | WO2007070598A2 (https=) |
Families Citing this family (43)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7589075B2 (en) * | 2001-01-16 | 2009-09-15 | Can-Fite Biopharma Ltd. | Use of an adenosine A3 receptor agonist for inhibition of viral replication |
| US8076303B2 (en) * | 2005-12-13 | 2011-12-13 | Spring Bank Pharmaceuticals, Inc. | Nucleotide and oligonucleotide prodrugs |
| GB2471806B (en) | 2008-04-03 | 2012-12-19 | Spring Bank Pharmaceuticals Inc | Compositions and methods for treating viral infections |
| US8691971B2 (en) * | 2008-09-23 | 2014-04-08 | Scott G. Petersen | Self delivering bio-labile phosphate protected pro-oligos for oligonucleotide based therapeutics and mediating RNA interference |
| CN102282155B (zh) | 2008-12-02 | 2017-06-09 | 日本波涛生命科学公司 | 磷原子修饰的核酸的合成方法 |
| EP2382227A1 (en) * | 2008-12-23 | 2011-11-02 | Girindus America, Inc. | Sulfurizing reagents and their use for oligonucleotides synthesis |
| RU2612521C2 (ru) * | 2009-07-06 | 2017-03-09 | Онтории, Инк. | Новые пролекарства нуклеиновых кислот и способы их применения |
| AU2015255202B2 (en) * | 2009-07-06 | 2017-07-27 | Wave Life Sciences Ltd. | Novel nucleic acid prodrugs and methods of use thereof |
| CN101659612B (zh) * | 2009-09-24 | 2013-01-09 | 华润赛科药业有限责任公司 | 一种选择性酯化的方法 |
| US9040234B2 (en) * | 2010-08-30 | 2015-05-26 | Spring Bank Pharmaceuticals, Inc. | Oligonucleotide analogs as therapeutic agents |
| JP5868324B2 (ja) | 2010-09-24 | 2016-02-24 | 株式会社Wave Life Sciences Japan | 不斉補助基 |
| CN103796657B (zh) | 2011-07-19 | 2017-07-11 | 波涛生命科学有限公司 | 合成官能化核酸的方法 |
| KR101327026B1 (ko) | 2011-11-29 | 2013-11-13 | 현대자동차주식회사 | 운전자 보호장치 |
| PL2872485T3 (pl) | 2012-07-13 | 2021-05-31 | Wave Life Sciences Ltd. | Asymetryczna grupa pomocnicza |
| CA2879066C (en) | 2012-07-13 | 2019-08-13 | Shin Nippon Biomedical Laboratories, Ltd. | Chiral nucleic acid adjuvant |
| KR102213609B1 (ko) * | 2012-07-13 | 2021-02-08 | 웨이브 라이프 사이언시스 리미티드 | 키랄 제어 |
| 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 |
| JPWO2015108048A1 (ja) | 2014-01-15 | 2017-03-23 | 株式会社新日本科学 | 抗腫瘍作用を有するキラル核酸アジュバンド及び抗腫瘍剤 |
| US10322173B2 (en) | 2014-01-15 | 2019-06-18 | Shin Nippon Biomedical Laboratories, Ltd. | Chiral nucleic acid adjuvant having anti-allergic activity, and anti-allergic agent |
| JPWO2015108047A1 (ja) | 2014-01-15 | 2017-03-23 | 株式会社新日本科学 | 免疫誘導活性を有するキラル核酸アジュバンド及び免疫誘導活性剤 |
| BR112016016400A2 (pt) | 2014-01-16 | 2017-10-03 | Wave Life Sciences Ltd | Composições de oligonucleotídeos quiralmente controlados, seu uso, sua composição farmacêutica, e métodos |
| GB201403697D0 (en) * | 2014-03-03 | 2014-04-16 | Link Technologies Ltd | Compounds and methods of use |
| EP3197459B1 (en) * | 2014-09-28 | 2025-02-12 | Huahui Health Ltd. | Polymeric bile acid derivatives inhibit hepatitis b and d virus and ntcp transport |
| TW201642872A (zh) * | 2015-04-07 | 2016-12-16 | 春季銀行製藥公司 | 用於治療ｈｃｖ感染之組成物和方法 |
| EP3317290A4 (en) * | 2015-07-02 | 2019-04-10 | Spring Bank Pharmaceuticals, Inc. | COMPOSITIONS AND METHOD FOR TREATING VIRUS INFECTION |
| EP3426671A4 (en) * | 2016-03-11 | 2019-11-20 | Spring Bank Pharmaceuticals, Inc. | COMPOUNDS AND COMPOSITIONS FOR THE TREATMENT OF INFECTIONS |
| 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 |
| PE20210255A1 (es) * | 2016-12-01 | 2021-02-10 | Takeda Pharmaceuticals Co | Dinucleotido ciclico como agonistas de sting (estimulador de genes de interferon) |
| US20200055883A1 (en) | 2017-02-17 | 2020-02-20 | Eisai R&D Management Co., Ltd. | Cyclic di-nucleotides derivative for the treatment of cancer |
| AR113224A1 (es) | 2017-04-28 | 2020-02-19 | Novartis Ag | Conjugados de anticuerpo que comprenden un agonista de sting |
| US11584774B2 (en) | 2017-09-11 | 2023-02-21 | F-star Therapeutics, Inc. | Compounds, compositions, and methods for the treatment of disease |
| US11707531B2 (en) * | 2017-09-11 | 2023-07-25 | F-star Therapeutics, Inc. | Compounds, compositions, and methods for the treatment of disease |
| CN110467646A (zh) * | 2018-05-09 | 2019-11-19 | 博瑞生物医药（苏州）股份有限公司 | 双核苷酸前体药物 |
| CN110467647B (zh) * | 2018-05-09 | 2022-08-30 | 博瑞生物医药（苏州）股份有限公司 | 双核苷酸前体药物的制备方法 |
| WO2019219070A1 (zh) * | 2018-05-18 | 2019-11-21 | 正大天晴药业集团股份有限公司 | 氘代的低聚核苷酸及前体药物 |
| BR112020024605A2 (pt) | 2018-06-01 | 2021-04-06 | Eisai R&D Management Co., Ltd. | Métodos para o tratamento de câncer de bexiga |
| FR3082434B1 (fr) | 2018-06-14 | 2021-04-30 | Cairdac | Implant cardiaque autonome de type "capsule leadless", comprenant un recuperateur d'energie a lame piezoelectrique |
| US11691990B2 (en) | 2018-08-16 | 2023-07-04 | Eisai R&D Management Co., Ltd | Salts of compounds and crystals thereof |
| WO2020089815A1 (en) | 2018-10-31 | 2020-05-07 | Novartis Ag | Antibody conjugates comprising sting agonist |
| WO2020092617A1 (en) | 2018-10-31 | 2020-05-07 | Novartis Ag | Dc-sign antibody conjugates comprising sting agonists |
| CN113164506B (zh) * | 2018-12-06 | 2023-12-08 | 正大天晴药业集团股份有限公司 | 二核苷酸化合物及其前体药物 |
| 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 |
| CN111484540B (zh) * | 2019-01-25 | 2023-09-08 | 博瑞生物医药（苏州）股份有限公司 | 含双核苷酸结构的化合物 |
Family Cites Families (24)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US688183A (en) | 1900-12-17 | 1901-12-03 | Carl C Lantz | Adjusting-clip for garment-supporters. |
| DE2817041C2 (de) | 1978-04-19 | 1987-02-19 | Reich Spezialmaschinen GmbH, 7440 Nürtingen | Vorrichtung zum Aufteilen von Platten |
| CS264222B1 (en) * | 1986-07-18 | 1989-06-13 | Holy Antonin | N-phosphonylmethoxyalkylderivatives of bases of pytimidine and purine and method of use them |
| US5914331A (en) | 1990-02-01 | 1999-06-22 | Emory University | Antiviral activity and resolution of 2-hydroxymethyl-5-(5-fluorocytosin-1-yl)-1,3-oxathiolane |
| US5204466A (en) | 1990-02-01 | 1993-04-20 | Emory University | Method and compositions for the synthesis of bch-189 and related compounds |
| ES2147721T3 (es) | 1990-04-18 | 2000-10-01 | Procter & Gamble Pharma | Quinolonil lactamas antimicrobianas. |
| US5444063A (en) | 1990-12-05 | 1995-08-22 | Emory University | Enantiomerically pure β-D-dioxolane nucleosides with selective anti-Hepatitis B virus activity |
| US5432165A (en) | 1992-04-06 | 1995-07-11 | Oclassen Pharmaceuticals, Inc. | Methods for the treatment of infection caused by Hepatitis B virus (HBV) |
| US5955591A (en) * | 1993-05-12 | 1999-09-21 | Imbach; Jean-Louis | Phosphotriester oligonucleotides, amidites and method of preparation |
| FR2705099B1 (fr) * | 1993-05-12 | 1995-08-04 | Centre Nat Rech Scient | Oligonucléotides phosphorothioates triesters et procédé de préparation. |
| FR2709754B1 (fr) | 1993-09-10 | 1995-12-01 | Centre Nat Rech Scient | Composés 2' ou 3'-déoxy- et 2', 3'-didéoxy-beta-L-pentofuranonucléosides, procédé de préparation et application thérapeutique, notamment anti-virale. |
| US5587362A (en) | 1994-01-28 | 1996-12-24 | Univ. Of Ga Research Foundation | L-nucleosides |
| US5581639A (en) | 1995-05-04 | 1996-12-03 | National Research Council Of Canada | Raman-nath diffraction grating |
| WO1998007734A1 (en) | 1996-08-21 | 1998-02-26 | Hybridon, Inc. | Oligonucleotide prodrugs |
| AU4988697A (en) | 1996-10-24 | 1998-05-15 | Vion Pharmaceuticals, Inc. | Monophosphate prodrugs of beta-l-fd4c and beta-l-fddc as potent antiviral agents |
| CA2599597A1 (en) | 1998-08-10 | 2000-02-24 | Idenix (Cayman) Limited | .beta.-l-2'-deoxy-nucleosides for the treatment of hepatitis b |
| PT2415776T (pt) | 1998-08-10 | 2016-07-07 | Novartis Ag | Beta-l-2'-desoxi-nucleosidos para o tratamento da hepatite b |
| US6444652B1 (en) | 1998-08-10 | 2002-09-03 | Novirio Pharmaceuticals Limited | β-L-2'-deoxy-nucleosides for the treatment of hepatitis B |
| US6875751B2 (en) | 2000-06-15 | 2005-04-05 | Idenix Pharmaceuticals, Inc. | 3′-prodrugs of 2′-deoxy-β-L-nucleosides |
| US20020119443A1 (en) | 2000-07-21 | 2002-08-29 | Gilead Sciences, Inc. | Prodrugs of phosphonate nucleotide analogues and methods for selecting and making same |
| WO2002092006A2 (en) * | 2001-05-16 | 2002-11-21 | Micrologix Biotech, Inc. | Nucleic acid-based compounds and methods of use thereof |
| US8076303B2 (en) * | 2005-12-13 | 2011-12-13 | Spring Bank Pharmaceuticals, Inc. | Nucleotide and oligonucleotide prodrugs |
| CN101146337B (zh) | 2006-09-15 | 2011-04-20 | 华为技术有限公司 | 新接入节点随机接入的方法及其系统 |
| GB2471806B (en) * | 2008-04-03 | 2012-12-19 | Spring Bank Pharmaceuticals Inc | Compositions and methods for treating viral infections |
-
2006
- 2006-12-12 US US11/637,520 patent/US8076303B2/en not_active Expired - Fee Related
- 2006-12-13 LT LTEP16158945.2T patent/LT3090748T/lt unknown
- 2006-12-13 EP EP16158945.2A patent/EP3090748B1/en not_active Not-in-force
- 2006-12-13 PL PL06848625.7T patent/PL1968612T3/pl unknown
- 2006-12-13 EP EP19157583.6A patent/EP3553072A1/en not_active Withdrawn
- 2006-12-13 DK DK16158945.2T patent/DK3090748T3/da active
- 2006-12-13 HU HUE06848625A patent/HUE029190T2/en unknown
- 2006-12-13 HR HRP20160531TT patent/HRP20160531T1/hr unknown
- 2006-12-13 SI SI200632048A patent/SI1968612T1/sl unknown
- 2006-12-13 JP JP2008545782A patent/JP5044854B2/ja not_active Expired - Fee Related
- 2006-12-13 RS RS20160328A patent/RS54867B1/sr unknown
- 2006-12-13 CN CN2006800509299A patent/CN101437397B/zh not_active Expired - Fee Related
- 2006-12-13 PT PT16158945T patent/PT3090748T/pt unknown
- 2006-12-13 IN IN1786DEN2015 patent/IN2015DN01786A/en unknown
- 2006-12-13 DK DK06848625.7T patent/DK1968612T3/en active
- 2006-12-13 KR KR1020087015713A patent/KR101123534B1/ko not_active Expired - Fee Related
- 2006-12-13 WO PCT/US2006/047617 patent/WO2007070598A2/en not_active Ceased
- 2006-12-13 SI SI200632329T patent/SI3090748T1/sl unknown
- 2006-12-13 ES ES06848625.7T patent/ES2573928T3/es active Active
- 2006-12-13 ES ES16158945T patent/ES2729657T3/es active Active
- 2006-12-13 KR KR1020117025810A patent/KR101248873B1/ko not_active Expired - Fee Related
- 2006-12-13 HU HUE16158945A patent/HUE044034T2/hu unknown
- 2006-12-13 EP EP06848625.7A patent/EP1968612B1/en active Active
- 2006-12-13 PL PL16158945T patent/PL3090748T3/pl unknown
- 2006-12-13 CN CN201210257654.3A patent/CN102796155B/zh not_active Expired - Fee Related
-
2011
- 2011-11-14 US US13/296,221 patent/US8691787B2/en not_active Expired - Fee Related
-
2014
- 2014-02-21 US US14/186,768 patent/US20140323554A1/en not_active Abandoned
-
2015
- 2015-11-12 US US14/939,397 patent/US10047114B2/en not_active Expired - Fee Related
-
2016
- 2016-05-09 CY CY20161100388T patent/CY1117576T1/el unknown
-
2018
- 2018-03-15 US US15/922,581 patent/US10344046B2/en not_active Expired - Fee Related
-
2019
- 2019-05-20 CY CY20191100534T patent/CY1121639T1/el unknown
- 2019-05-23 US US16/420,311 patent/US20200087338A1/en not_active Abandoned
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