JP2019510793A5 - - Google Patents
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- Publication number
- JP2019510793A5 JP2019510793A5 JP2018552707A JP2018552707A JP2019510793A5 JP 2019510793 A5 JP2019510793 A5 JP 2019510793A5 JP 2018552707 A JP2018552707 A JP 2018552707A JP 2018552707 A JP2018552707 A JP 2018552707A JP 2019510793 A5 JP2019510793 A5 JP 2019510793A5
- Authority
- JP
- Japan
- Prior art keywords
- alkylene
- formula
- group
- compound according
- compound
- 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 20
- 125000002947 alkylene group Chemical group 0.000 claims 10
- 108020004707 nucleic acids Proteins 0.000 claims 9
- 102000039446 nucleic acids Human genes 0.000 claims 9
- 150000007523 nucleic acids Chemical class 0.000 claims 9
- NBIIXXVUZAFLBC-UHFFFAOYSA-N Phosphoric acid Chemical compound OP(O)(O)=O NBIIXXVUZAFLBC-UHFFFAOYSA-N 0.000 claims 6
- LYCAIKOWRPUZTN-UHFFFAOYSA-N Ethylene glycol Chemical group OCCO LYCAIKOWRPUZTN-UHFFFAOYSA-N 0.000 claims 5
- -1 alkylene ether Chemical compound 0.000 claims 5
- RTZKZFJDLAIYFH-UHFFFAOYSA-N ether Substances CCOCC RTZKZFJDLAIYFH-UHFFFAOYSA-N 0.000 claims 5
- 125000002467 phosphate group Chemical group [H]OP(=O)(O[H])O[*] 0.000 claims 5
- RYYWUUFWQRZTIU-UHFFFAOYSA-N Thiophosphoric acid Chemical compound OP(O)(S)=O RYYWUUFWQRZTIU-UHFFFAOYSA-N 0.000 claims 4
- 208000008338 non-alcoholic fatty liver disease Diseases 0.000 claims 4
- 229910000147 aluminium phosphate Inorganic materials 0.000 claims 3
- 125000006834 (C4-C20) alkylene group Chemical group 0.000 claims 2
- OVRNDRQMDRJTHS-CBQIKETKSA-N N-Acetyl-D-Galactosamine Chemical compound CC(=O)N[C@H]1[C@@H](O)O[C@H](CO)[C@H](O)[C@@H]1O OVRNDRQMDRJTHS-CBQIKETKSA-N 0.000 claims 2
- MBLBDJOUHNCFQT-UHFFFAOYSA-N N-acetyl-D-galactosamine Natural products CC(=O)NC(C=O)C(O)C(O)C(O)CO MBLBDJOUHNCFQT-UHFFFAOYSA-N 0.000 claims 2
- 229910052799 carbon Inorganic materials 0.000 claims 2
- 206010053219 non-alcoholic steatohepatitis Diseases 0.000 claims 2
- MSWZFWKMSRAUBD-IVMDWMLBSA-N 2-amino-2-deoxy-D-glucopyranose Chemical compound N[C@H]1C(O)O[C@H](CO)[C@@H](O)[C@@H]1O MSWZFWKMSRAUBD-IVMDWMLBSA-N 0.000 claims 1
- 206010000599 Acromegaly Diseases 0.000 claims 1
- 208000022309 Alcoholic Liver disease Diseases 0.000 claims 1
- 208000007848 Alcoholism Diseases 0.000 claims 1
- 208000030760 Anaemia of chronic disease Diseases 0.000 claims 1
- 108091023037 Aptamer Proteins 0.000 claims 1
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 1
- 208000024172 Cardiovascular disease Diseases 0.000 claims 1
- 102000053642 Catalytic RNA Human genes 0.000 claims 1
- 108090000994 Catalytic RNA Proteins 0.000 claims 1
- 208000008964 Chemical and Drug Induced Liver Injury Diseases 0.000 claims 1
- WQZGKKKJIJFFOK-QTVWNMPRSA-N D-mannopyranose Chemical compound OC[C@H]1OC(O)[C@@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-QTVWNMPRSA-N 0.000 claims 1
- 206010072268 Drug-induced liver injury Diseases 0.000 claims 1
- 208000032928 Dyslipidaemia Diseases 0.000 claims 1
- 229930091371 Fructose Natural products 0.000 claims 1
- 239000005715 Fructose Substances 0.000 claims 1
- RFSUNEUAIZKAJO-ARQDHWQXSA-N Fructose Chemical compound OC[C@H]1O[C@](O)(CO)[C@@H](O)[C@@H]1O RFSUNEUAIZKAJO-ARQDHWQXSA-N 0.000 claims 1
- WQZGKKKJIJFFOK-GASJEMHNSA-N Glucose Natural products OC[C@H]1OC(O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-GASJEMHNSA-N 0.000 claims 1
- 208000018565 Hemochromatosis Diseases 0.000 claims 1
- 208000031220 Hemophilia Diseases 0.000 claims 1
- 208000009292 Hemophilia A Diseases 0.000 claims 1
- 206010019799 Hepatitis viral Diseases 0.000 claims 1
- 208000035150 Hypercholesterolemia Diseases 0.000 claims 1
- 208000026350 Inborn Genetic disease Diseases 0.000 claims 1
- 208000017170 Lipid metabolism disease Diseases 0.000 claims 1
- 206010067125 Liver injury Diseases 0.000 claims 1
- 208000008589 Obesity Diseases 0.000 claims 1
- 108091030071 RNAI Proteins 0.000 claims 1
- 208000035977 Rare disease Diseases 0.000 claims 1
- 108020004459 Small interfering RNA Proteins 0.000 claims 1
- 208000002903 Thalassemia Diseases 0.000 claims 1
- 201000007930 alcohol dependence Diseases 0.000 claims 1
- 125000004450 alkenylene group Chemical group 0.000 claims 1
- WQZGKKKJIJFFOK-PHYPRBDBSA-N alpha-D-galactose Chemical compound OC[C@H]1O[C@H](O)[C@H](O)[C@@H](O)[C@H]1O WQZGKKKJIJFFOK-PHYPRBDBSA-N 0.000 claims 1
- 208000007502 anemia Diseases 0.000 claims 1
- 208000022400 anemia due to chronic disease Diseases 0.000 claims 1
- 230000000692 anti-sense effect Effects 0.000 claims 1
- 125000000732 arylene group Chemical group 0.000 claims 1
- MSWZFWKMSRAUBD-UHFFFAOYSA-N beta-D-galactosamine Natural products NC1C(O)OC(CO)C(O)C1O MSWZFWKMSRAUBD-UHFFFAOYSA-N 0.000 claims 1
- WQZGKKKJIJFFOK-VFUOTHLCSA-N beta-D-glucose Chemical compound OC[C@H]1O[C@@H](O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-VFUOTHLCSA-N 0.000 claims 1
- 150000001721 carbon Chemical group 0.000 claims 1
- 238000007385 chemical modification Methods 0.000 claims 1
- 208000019425 cirrhosis of liver Diseases 0.000 claims 1
- 238000004132 cross linking Methods 0.000 claims 1
- 125000002993 cycloalkylene group Chemical group 0.000 claims 1
- 238000002716 delivery method Methods 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 229930182830 galactose Natural products 0.000 claims 1
- 230000009368 gene silencing by RNA Effects 0.000 claims 1
- 208000016361 genetic disease Diseases 0.000 claims 1
- 229960002442 glucosamine Drugs 0.000 claims 1
- 239000008103 glucose Substances 0.000 claims 1
- 208000031169 hemorrhagic disease Diseases 0.000 claims 1
- 231100000753 hepatic injury Toxicity 0.000 claims 1
- 125000005549 heteroarylene group Chemical group 0.000 claims 1
- 208000006575 hypertriglyceridemia Diseases 0.000 claims 1
- 238000000338 in vitro Methods 0.000 claims 1
- 238000003780 insertion Methods 0.000 claims 1
- 230000037431 insertion Effects 0.000 claims 1
- 210000005229 liver cell Anatomy 0.000 claims 1
- 208000019423 liver disease Diseases 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 208000030159 metabolic disease Diseases 0.000 claims 1
- 238000012986 modification Methods 0.000 claims 1
- 230000004048 modification Effects 0.000 claims 1
- 229910052757 nitrogen Inorganic materials 0.000 claims 1
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 1
- 235000020824 obesity Nutrition 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 108091092562 ribozyme Proteins 0.000 claims 1
- 210000000130 stem cell Anatomy 0.000 claims 1
- 238000006467 substitution reaction Methods 0.000 claims 1
- 201000001862 viral hepatitis Diseases 0.000 claims 1
- 0 CCOCCNCC* Chemical compound CCOCCNCC* 0.000 description 2
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP16163939.8 | 2016-04-05 | ||
| EP16163939.8A EP3228326A1 (en) | 2016-04-05 | 2016-04-05 | Nucleic acid linked to a trivalent glycoconjugate |
| PCT/EP2017/058112 WO2017174657A1 (en) | 2016-04-05 | 2017-04-05 | Nucleic acid linked to a trivalent glycoconjugate |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2019510793A JP2019510793A (ja) | 2019-04-18 |
| JP2019510793A5 true JP2019510793A5 (https=) | 2020-05-14 |
| JP7120925B2 JP7120925B2 (ja) | 2022-08-17 |
Family
ID=55697082
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018552707A Active JP7120925B2 (ja) | 2016-04-05 | 2017-04-05 | 新規コンジュゲート |
Country Status (11)
| Country | Link |
|---|---|
| US (2) | US10913945B2 (https=) |
| EP (3) | EP3228326A1 (https=) |
| JP (1) | JP7120925B2 (https=) |
| CN (2) | CN116036117A (https=) |
| AU (1) | AU2017245687B2 (https=) |
| CA (1) | CA3019981A1 (https=) |
| DK (1) | DK3439703T3 (https=) |
| ES (1) | ES2805026T3 (https=) |
| HU (1) | HUE049931T2 (https=) |
| PL (1) | PL3439703T3 (https=) |
| WO (1) | WO2017174657A1 (https=) |
Families Citing this family (47)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| SG10202008301UA (en) * | 2016-04-11 | 2020-10-29 | Arbutus Biopharma Corp | Targeted nucleic acid conjugate compositions |
| WO2018185253A1 (en) * | 2017-04-05 | 2018-10-11 | Silence Therapeutics Gmbh | Ligand modified double-stranded nucleic acids |
| WO2019193144A1 (en) | 2018-04-05 | 2019-10-10 | Silence Therapeutics Gmbh | siRNAs WITH VINYLPHOSPHONATE AT THE 5' END OF THE ANTISENSE STRAND |
| EP3550022A1 (en) | 2018-04-05 | 2019-10-09 | Silence Therapeutics GmbH | Products and compositions |
| WO2018185252A1 (en) | 2017-04-05 | 2018-10-11 | Silence Therapeutics Gmbh | Nucleic acid conjugates |
| JP7155239B2 (ja) * | 2017-04-05 | 2022-10-18 | サイレンス・セラピューティクス・ゲーエムベーハー | 産物及び組成物 |
| WO2018185240A1 (en) | 2017-04-05 | 2018-10-11 | Silence Therapeutics Gmbh | Products and compositions |
| EP3385272A1 (en) * | 2017-04-05 | 2018-10-10 | Silence Therapeutics GmbH | Further novel oligonucleotide-ligand conjugates |
| EP4029942A1 (en) | 2017-04-05 | 2022-07-20 | Silence Therapeutics GmbH | Products and compositions |
| EP3483269A1 (en) | 2017-11-13 | 2019-05-15 | Silence Therapeutics GmbH | Products and compositions |
| IL274611B2 (en) * | 2017-11-13 | 2024-10-01 | Silence Therapeutics Gmbh | Nucleic acids for inhibiting expression of a target gene comprising phosphorodithioate linkages |
| MX2020004897A (es) | 2017-11-13 | 2020-10-05 | Silence Therapeutics Gmbh | Acidos nucleicos para inhibir la expresion de lpa en una celula. |
| CA3118327A1 (en) | 2017-11-13 | 2019-05-16 | Silence Therapeutics Gmbh | Nucleic acids for inhibiting expression of aldh2 in a cell |
| EP3483270A1 (en) | 2017-11-13 | 2019-05-15 | Silence Therapeutics GmbH | Products and compositions |
| EP3549610A1 (en) | 2018-04-05 | 2019-10-09 | Silence Therapeutics GmbH | Nucleic acid conjugates |
| EP3550021A1 (en) | 2018-04-05 | 2019-10-09 | Silence Therapeutics GmbH | Products and compositions for inhibiting expression of a target gene |
| EP3598995A1 (en) | 2018-07-26 | 2020-01-29 | Silence Therapeutics GmbH | Products and compositions |
| BR112021009213A2 (pt) | 2018-11-13 | 2021-08-10 | Silence Therapeutics Gmbh | ácidos nucleicos para inibição da expressão de lpa em uma célula |
| EP3730617A1 (en) | 2019-04-26 | 2020-10-28 | Silence Therapeutics GmbH | Nucleic acids for inhibiting expression of c3 in a cell |
| CA3119234A1 (en) | 2018-11-23 | 2020-05-28 | Silence Therapeutics Gmbh | Nucleic acids for inhibiting expression of c3 in a cell |
| EP3886851A1 (en) | 2018-11-26 | 2021-10-06 | Asociación Centro de Investigación Cooperativa en Biociencias - CIC bioGUNE | Methods for diagnosing and/or treating acute or chronic liver, kidney or lung disease |
| WO2020225301A1 (en) | 2019-05-07 | 2020-11-12 | Universität Bern | Nucleic acids for inhibiting expression of pros1 in a cell |
| EP4022060A1 (en) | 2019-08-27 | 2022-07-06 | Silence Therapeutics GmbH | Nucleic acids for inhibiting expression of c3 in a cell |
| EP4025252A4 (en) | 2019-09-03 | 2023-10-18 | Arcturus Therapeutics, Inc. | ASIALOGLYCOPROTEIN RECEPTOR-MEDIATED ADMINISTRATION OF THERAPEUTICALLY ACTIVE CONJUGATES |
| EP4048801A4 (en) * | 2019-10-24 | 2023-11-22 | Genevant Sciences Gmbh | Conjugates and methods for treating acromegaly |
| US20240229041A2 (en) | 2020-05-27 | 2024-07-11 | Asociación Centro De Investigación Cooperativa En Biociencias-Cic Biogune | Nucleic acids for inhibiting expression of cnnm4 in a cell |
| WO2022096424A1 (en) | 2020-11-04 | 2022-05-12 | Universität Bern | Nucleic acids for inhibiting expression of pros1 in a cell |
| AU2021373262A1 (en) | 2020-11-04 | 2023-06-01 | Silence Therapeutics Gmbh | Nucleic acids for inhibiting expression of pros1 in a cell |
| WO2022184852A1 (en) | 2021-03-03 | 2022-09-09 | Silence Therapeutics Gmbh | Conjugated nucleic acids comprising a phosphorodithioate for inhibiting gene expression in a cell |
| WO2022223557A1 (en) | 2021-04-20 | 2022-10-27 | Silence Therapeutics Gmbh | Nucleic acids for inhibiting expression of xdh in a cell |
| US20240240187A1 (en) | 2021-04-27 | 2024-07-18 | Silence Therapeutics Gmbh | Sirna targeting tmprss6 for the treatment of myeloproliferative disorders |
| KR20240051221A (ko) | 2021-09-02 | 2024-04-19 | 사일런스 테라퓨틱스 게엠베하 | 세포에서 보체 인자 b (cfb)의 발현을 억제하기 위한 핵산 |
| JP2024541559A (ja) * | 2021-11-29 | 2024-11-08 | シャンハイ アルゴ バイオファーマシューティカル カンパニー，リミテッド | Ｂ型肝炎ウイルス（ｈｂｖ）タンパク質の発現を阻害するための組成物および方法 |
| WO2023208106A1 (zh) * | 2022-04-29 | 2023-11-02 | 石药集团中奇制药技术（石家庄）有限公司 | 具有肝靶向递送效应的化合物及其寡聚核苷酸缀合物 |
| WO2024013334A1 (en) * | 2022-07-15 | 2024-01-18 | Silence Therapeutics Gmbh | Nucleic acids for inhibiting expression of agt in a cell |
| WO2024126687A1 (en) | 2022-12-16 | 2024-06-20 | Silence Therapeutics Gmbh | Nucleic acids conjugated to an albumin binding moiety |
| EP4687983A1 (en) | 2023-03-27 | 2026-02-11 | Silence Therapeutics GmbH | Compounds and compositions for use in stem cell transplantation |
| CN116444589B (zh) * | 2023-06-15 | 2023-09-19 | 北京悦康科创医药科技股份有限公司 | 新型GalNAc化合物及其硫代寡核苷酸缀合物和偶联方法 |
| US20250051771A1 (en) | 2023-07-24 | 2025-02-13 | Astrazeneca Ab | Multivalent cargo-carrying complexes and uses thereof |
| GB202311334D0 (en) | 2023-07-24 | 2023-09-06 | Astrazeneca Ab | Multivalent cargo-carrying complexes and uses thereof |
| GB202311324D0 (en) | 2023-07-24 | 2023-09-06 | Astrazeneca Ab | Multivalent cargo-carrying complexes and uses thereof |
| WO2025132845A1 (en) | 2023-12-21 | 2025-06-26 | Silence Therapeutics Gmbh | Galnac phosphoramidites and their uses |
| WO2025162939A1 (en) | 2024-01-29 | 2025-08-07 | Silence Therapeutics Gmbh | Nucleic acids for inhibiting expression of gpr146 in a cell |
| WO2025163186A1 (en) | 2024-02-01 | 2025-08-07 | Silence Therapeutics Gmbh | Conjugated nucleic acids and nucleic acids comprising locked nucleosides and inverted nucleotides for inhibiting gene expression in a cell |
| WO2025169133A1 (en) | 2024-02-09 | 2025-08-14 | Astrazeneca Ab | Double-stranded rnai agents and compositions for reducing expression of angiopoietin-like 3 (angptl3) and methods of use thereof |
| US20260015617A1 (en) | 2024-07-12 | 2026-01-15 | Novartis Ag | DOUBLE STRANDED RNAi AGENTS, COMPOSITIONS AND METHODS OF USE |
| US12454693B1 (en) * | 2024-09-27 | 2025-10-28 | Dexcel Pharma Technologies Ltd. | Nucleic acids for inhibiting expression of transferrin receptor 2 |
Family Cites Families (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5378825A (en) | 1990-07-27 | 1995-01-03 | Isis Pharmaceuticals, Inc. | Backbone modified oligonucleotide analogs |
| KR940703846A (ko) | 1991-12-24 | 1994-12-12 | 비. 린네 파샬 | 갭(gap)이 형성된 2′ 변성된 올리고뉴클레오티드(gapped 2′ modifed oligonucleotides) |
| NL9201440A (nl) | 1992-08-11 | 1994-03-01 | Univ Leiden | Triantennaire clusterglycosiden, hun bereiding en toepassing. |
| US5885613A (en) | 1994-09-30 | 1999-03-23 | The University Of British Columbia | Bilayer stabilizing components and their use in forming programmable fusogenic liposomes |
| US5820873A (en) | 1994-09-30 | 1998-10-13 | The University Of British Columbia | Polyethylene glycol modified ceramide lipids and liposome uses thereof |
| US5753613A (en) | 1994-09-30 | 1998-05-19 | Inex Pharmaceuticals Corporation | Compositions for the introduction of polyanionic materials into cells |
| AU3751299A (en) | 1998-04-20 | 1999-11-08 | Ribozyme Pharmaceuticals, Inc. | Nucleic acid molecules with novel chemical compositions capable of modulating gene expression |
| US10077443B2 (en) * | 2012-11-15 | 2018-09-18 | Roche Innovation Center Copenhagen A/S | Oligonucleotide conjugates |
| DK2991656T3 (da) * | 2013-05-01 | 2020-03-23 | Ionis Pharmaceuticals Inc | Sammensætninger og fremgangsmåder til modulering af apolipoprotein c-iii-ekspression |
| PT3137605T (pt) * | 2014-05-01 | 2020-12-18 | Ionis Pharmaceuticals Inc | Composições e métodos para modulação da expressão de angiopoietina de tipo 3 |
| WO2016055601A1 (en) * | 2014-10-10 | 2016-04-14 | F. Hoffmann-La Roche Ag | Galnac phosphoramidites, nucleic acid conjugates thereof and their use |
-
2016
- 2016-04-05 EP EP16163939.8A patent/EP3228326A1/en not_active Ceased
-
2017
- 2017-04-05 JP JP2018552707A patent/JP7120925B2/ja active Active
- 2017-04-05 US US16/091,503 patent/US10913945B2/en active Active
- 2017-04-05 DK DK17715730.2T patent/DK3439703T3/da active
- 2017-04-05 EP EP17715730.2A patent/EP3439703B1/en active Active
- 2017-04-05 CN CN202211456959.7A patent/CN116036117A/zh active Pending
- 2017-04-05 ES ES17715730T patent/ES2805026T3/es active Active
- 2017-04-05 HU HUE17715730A patent/HUE049931T2/hu unknown
- 2017-04-05 EP EP20171464.9A patent/EP3744350A1/en active Pending
- 2017-04-05 CA CA3019981A patent/CA3019981A1/en active Pending
- 2017-04-05 PL PL17715730T patent/PL3439703T3/pl unknown
- 2017-04-05 WO PCT/EP2017/058112 patent/WO2017174657A1/en not_active Ceased
- 2017-04-05 CN CN201780035060.9A patent/CN109562188B/zh active Active
- 2017-04-05 AU AU2017245687A patent/AU2017245687B2/en active Active
-
2020
- 2020-11-25 US US17/104,502 patent/US11912993B2/en active Active
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