RU2020116571A - N4-гидроксицитидин и производные и связанные с этим противовирусные применения - Google Patents
N4-гидроксицитидин и производные и связанные с этим противовирусные применения Download PDFInfo
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- RU2020116571A RU2020116571A RU2020116571A RU2020116571A RU2020116571A RU 2020116571 A RU2020116571 A RU 2020116571A RU 2020116571 A RU2020116571 A RU 2020116571A RU 2020116571 A RU2020116571 A RU 2020116571A RU 2020116571 A RU2020116571 A RU 2020116571A
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- RU
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- Prior art keywords
- virus
- pharmaceutically acceptable
- equine encephalitis
- compound
- coronavirus
- Prior art date
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- XCUAIINAJCDIPM-XVFCMESISA-N N(4)-hydroxycytidine Chemical compound O[C@@H]1[C@H](O)[C@@H](CO)O[C@H]1N1C(=O)NC(=NO)C=C1 XCUAIINAJCDIPM-XVFCMESISA-N 0.000 title 1
- 230000000840 anti-viral effect Effects 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims 6
- 239000008194 pharmaceutical composition Substances 0.000 claims 4
- 239000000546 pharmaceutical excipient Substances 0.000 claims 4
- 150000003839 salts Chemical class 0.000 claims 4
- 241000700605 Viruses Species 0.000 claims 3
- 241001502567 Chikungunya virus Species 0.000 claims 2
- 241000710945 Eastern equine encephalitis virus Species 0.000 claims 2
- 201000011001 Ebola Hemorrhagic Fever Diseases 0.000 claims 2
- 241000711950 Filoviridae Species 0.000 claims 2
- 244000309467 Human Coronavirus Species 0.000 claims 2
- 241000712431 Influenza A virus Species 0.000 claims 2
- 241000713196 Influenza B virus Species 0.000 claims 2
- 241000127282 Middle East respiratory syndrome-related coronavirus Species 0.000 claims 2
- 241000712464 Orthomyxoviridae Species 0.000 claims 2
- 241000315672 SARS coronavirus Species 0.000 claims 2
- 241000710959 Venezuelan equine encephalitis virus Species 0.000 claims 2
- 241000710951 Western equine encephalitis virus Species 0.000 claims 2
- 208000015181 infectious disease Diseases 0.000 claims 2
Classifications
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
- A61K31/7052—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
- A61K31/706—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
- A61K31/7052—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
- A61K31/706—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
- A61K31/7064—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines
- A61K31/7068—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/10—Dispersions; Emulsions
- A61K9/12—Aerosols; Foams
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/14—Antivirals for RNA viruses
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/14—Antivirals for RNA viruses
- A61P31/16—Antivirals for RNA viruses for influenza or rhinoviruses
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/20—Antivirals for DNA viruses
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
- C07H19/00—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
- C07H19/02—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
- C07H19/04—Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
- C07H19/06—Pyrimidine radicals
- C07H19/067—Pyrimidine radicals with ribosyl as the saccharide radical
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
- C07H19/00—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
- C07H19/02—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
- C07H19/04—Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
- C07H19/06—Pyrimidine radicals
- C07H19/10—Pyrimidine radicals with the saccharide radical esterified by phosphoric or polyphosphoric acids
-
- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
- Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
- Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change
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- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical & Material Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Virology (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Molecular Biology (AREA)
- Communicable Diseases (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Oncology (AREA)
- Epidemiology (AREA)
- Biotechnology (AREA)
- Engineering & Computer Science (AREA)
- Biochemistry (AREA)
- Genetics & Genomics (AREA)
- Dispersion Chemistry (AREA)
- Pulmonology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicinal Preparation (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Saccharide Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Claims (16)
1. Фармацевтическая композиция, содержащая фармацевтически приемлемое вспомогательное вещество и соединение, выбранное из следующих:
2. Фармацевтическая композиция, содержащая фармацевтически приемлемое вспомогательное вещество и соединение, выбранное из следующих:
3. Фармацевтическая композиция, содержащая фармацевтически приемлемое вспомогательное вещество и соединение следующей структуры:
или его фармацевтически приемлемые или физиологические соли.
4. Фармацевтическая композиция, содержащая фармацевтически приемлемое вспомогательное вещество и соединение следующей структуры:
или его фармацевтически приемлемые или физиологические соли.
5. Способ лечения или предупреждения коронавируса человека, коронавируса SARS, коронавируса MERS, вируса восточного лошадиного энцефалита, вируса западного лошадиного энцефалита, вируса венесуэльского энцефалита лошадей, вируса чикунгунья и инфекции Росс-ривер, вируса Orthomyxoviridae или вируса Paramyxoviridae, или вируса RSV, или вируса гриппа A и вируса гриппа B, или вируса Filoviridae, или инфекции вируса Эбола у пациента, включающий введение пациенту, нуждающемуся в этом, эффективного количества соединения структуры
или его фармацевтически приемлемых или физиологических солей.
6. Способ лечения или предупреждения коронавируса человека, коронавируса SARS, коронавируса MERS, вируса восточного лошадиного энцефалита, вируса западного лошадиного энцефалита, вируса венесуэльского энцефалита лошадей, вируса чикунгунья и инфекции Росс-ривер, вируса Orthomyxoviridae или вируса Paramyxoviridae, или вируса RSV, или вируса гриппа A и вируса гриппа B, или вируса Filoviridae, или инфекции вируса Эбола у пациента, включающий введение пациенту, нуждающемуся в этом, эффективного количества соединения структуры
или его фармацевтически приемлемых или физиологических солей.
Applications Claiming Priority (7)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201762595907P | 2017-12-07 | 2017-12-07 | |
| US62/595,907 | 2017-12-07 | ||
| US201862626998P | 2018-02-06 | 2018-02-06 | |
| US62/626,998 | 2018-02-06 | ||
| US201862760434P | 2018-11-13 | 2018-11-13 | |
| US62/760,434 | 2018-11-13 | ||
| PCT/US2018/064503 WO2019113462A1 (en) | 2017-12-07 | 2018-12-07 | N4-hydroxycytidine and derivatives and anti-viral uses related thereto |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2023133687A Division RU2023133687A (ru) | 2017-12-07 | 2018-12-07 | N4-гидроксицитидин и производные и связанные с этим противовирусные применения |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| RU2020116571A true RU2020116571A (ru) | 2021-11-22 |
| RU2020116571A3 RU2020116571A3 (ru) | 2021-11-22 |
Family
ID=66751806
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2020116571A RU2020116571A (ru) | 2017-12-07 | 2018-12-07 | N4-гидроксицитидин и производные и связанные с этим противовирусные применения |
Country Status (27)
| Country | Link |
|---|---|
| US (3) | US11331331B2 (ru) |
| EP (2) | EP3706762B1 (ru) |
| JP (4) | JP6804790B1 (ru) |
| KR (3) | KR102626210B1 (ru) |
| CN (2) | CN111372592A (ru) |
| AU (2) | AU2018378832B9 (ru) |
| BR (1) | BR122022008466B1 (ru) |
| CA (1) | CA3082191C (ru) |
| DK (1) | DK3706762T3 (ru) |
| ES (1) | ES2995458T3 (ru) |
| FI (1) | FI3706762T3 (ru) |
| GB (2) | GB2590198B (ru) |
| HR (1) | HRP20241620T1 (ru) |
| HU (1) | HUE069306T2 (ru) |
| IL (2) | IL274155B (ru) |
| LT (1) | LT3706762T (ru) |
| MX (2) | MX2020005392A (ru) |
| PH (2) | PH12022550371A1 (ru) |
| PL (1) | PL3706762T3 (ru) |
| PT (1) | PT3706762T (ru) |
| RS (1) | RS66222B1 (ru) |
| RU (1) | RU2020116571A (ru) |
| SA (1) | SA520412305B1 (ru) |
| SG (1) | SG11202004403QA (ru) |
| SI (1) | SI3706762T1 (ru) |
| WO (1) | WO2019113462A1 (ru) |
| ZA (1) | ZA202002849B (ru) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| RU2791806C1 (ru) * | 2022-12-28 | 2023-03-13 | федеральное государственное бюджетное учреждение "Национальный исследовательский центр эпидемиологии и микробиологии имени почетного академика Н.Ф. Гамалеи" Министерства здравоохранения Российской Федерации | Применение 5'-О-(3-фенилпропионил)-N4-гидроксицитидина для ингибирования репликации вируса гриппа in vitro и in vivo |
Families Citing this family (59)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| SG11201705069YA (en) * | 2014-12-26 | 2017-07-28 | Univ Emory | N4-hydroxycytidine and derivatives and anti-viral uses related thereto |
| JP2020518578A (ja) | 2017-05-01 | 2020-06-25 | ギリアード サイエンシーズ， インコーポレイテッド | （Ｓ）−２−エチルブチル２−（（（Ｓ）−（（（２Ｒ，３Ｓ，４Ｒ，５Ｒ）−５−（４−アミノピロロ［２，１−ｆ］［１，２，４］トリアジン−７−イル）−５−シアノ−３，４−ジヒドロキシテトラヒドロフラン−２−イル）メトキシ）（フェノキシ）ホスホリル）アミノ）プロパノエートの結晶形態 |
| PL3706762T3 (pl) | 2017-12-07 | 2025-02-10 | Emory University | N4-hydroksycytydyna i pochodne oraz związane z nimi zastosowania przeciwwirusowe |
| CN112390838A (zh) * | 2019-08-14 | 2021-02-23 | 斯微(上海)生物科技有限公司 | 一种改性核苷及其合成方法 |
| JP7703518B2 (ja) * | 2019-09-11 | 2025-07-07 | ザ スクリプス リサーチ インスティテュート | 抗ウイルスプロドラッグ及びその製剤 |
| PE20230466A1 (es) * | 2020-02-07 | 2023-03-14 | Univ Emory | N4-hidroxicitidina y derivados y usos antivirales relacionados con los mismos |
| CN111285911B (zh) * | 2020-02-26 | 2021-04-02 | 山东大学 | Gem-1mt两亲小分子化合物及其制剂、制备方法和应用 |
| TWI890963B (zh) | 2020-03-12 | 2025-07-21 | 美商基利科學股份有限公司 | 1'-氰基核苷之製備方法 |
| CA3173931A1 (en) * | 2020-04-03 | 2021-10-07 | Felix Frueh | Viral entry inhibitors and rna polymerase inhibitors |
| US11376232B2 (en) | 2020-04-21 | 2022-07-05 | Immunic Ag | Vidofludimus for use in the treatment or prevention of viral diseases |
| US12097212B2 (en) * | 2020-06-08 | 2024-09-24 | Brigham Young University | Use of cationic steroidal antimicrobial compounds to deactivate coronavirus |
| CA3191082A1 (en) * | 2020-08-27 | 2022-03-03 | Jameson R. BOTHE | Novel forms of antiviral nucleosides |
| WO2022049382A1 (en) * | 2020-09-04 | 2022-03-10 | Mexichem Fluor S.A. De C.V. | Pharmaceutical composition |
| US11702440B2 (en) * | 2020-12-10 | 2023-07-18 | Optimus Drugs Private Limited | Pharmaceutical polymorphs of Molnupiravir |
| WO2022133323A1 (en) * | 2020-12-18 | 2022-06-23 | Southern Research Institute | 6-aza-nucleoside prodrugs as antiviral agents for treating virus infections |
| US20240092818A1 (en) * | 2020-12-18 | 2024-03-21 | Merck Sharp & Dohme Llc | Synthesis of antiviral nucleosides |
| CN112608357B (zh) * | 2020-12-21 | 2022-12-09 | 杭州科巢生物科技有限公司 | 一种抗病毒药物Molnupiravir的制备方法 |
| CN112778387A (zh) * | 2021-01-15 | 2021-05-11 | 杭州科巢生物科技有限公司 | 一种Molnupiravir晶型A及其制备方法 |
| WO2022168106A1 (en) * | 2021-02-06 | 2022-08-11 | Fermenta Biotech Limited | Chemo-enzymatic process for synthesis of molnupiravir |
| WO2022168107A1 (en) * | 2021-02-06 | 2022-08-11 | Fermenta Biotech Limited | Enzymatic synthesis of molnupiravir intermediate |
| CN112552288A (zh) * | 2021-02-19 | 2021-03-26 | 南京桦冠生物技术有限公司 | 一种4-肟-5`-（2-甲基丙酰基）尿苷的制备方法 |
| CN113072606A (zh) * | 2021-03-18 | 2021-07-06 | 南京正济医药研究有限公司 | 一种n4-羟基胞苷类化合物的晶型及其制备方法与用途 |
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| US20240199535A1 (en) | 2021-04-09 | 2024-06-20 | Immunic Ag | Deuterated dhodh inhibitors |
| US20240166680A1 (en) * | 2021-04-15 | 2024-05-23 | Shanghai Institute Of Materia Medica, Chinese Academy Of Sciences | Nucleoside analog and use thereof |
| US11407779B1 (en) | 2021-04-23 | 2022-08-09 | Divi's Laboratories Ltd. | Process for the preparation of molnupiravir |
| CN113307834A (zh) * | 2021-04-23 | 2021-08-27 | 安徽贝克联合制药有限公司 | 一种核糖核苷类似物的多晶型物、其制备方法及应用 |
| EP4355755A4 (en) * | 2021-06-14 | 2025-05-07 | Venatorx Pharmaceuticals, Inc. | ORALLY BIOAVAILABLE NUCLEOSIDE ANALOGUES |
| CN113278040B (zh) * | 2021-06-16 | 2022-07-05 | 苏州立新制药有限公司 | 5’-异丁酰基-n4-羟基胞苷的制备方法 |
| CN117642410A (zh) * | 2021-06-18 | 2024-03-01 | 苏州春海生物医药有限公司 | N4-羟基胞苷的酯衍生物及其用途 |
| CN113321694A (zh) * | 2021-06-22 | 2021-08-31 | 药康众拓(江苏)医药科技有限公司 | N4-羟基胞苷衍生物及其制备方法和用途 |
| CN113433242B (zh) * | 2021-06-28 | 2022-12-27 | 成都大学 | Molnupiravir含量及有关物质的检测方法 |
| CN113278041B (zh) * | 2021-07-16 | 2021-10-19 | 南京颐媛生物医学研究院有限公司 | 一种核苷磷酸酯及其合成方法与抗肝炎病毒的制药应用 |
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| WO2023067623A1 (en) * | 2021-10-20 | 2023-04-27 | Council Of Scientific And Industrial Research An Indian Registered Body Incorporated Under The Regn. Of Soc. Act (Act Xxi Of 1860) | A short and cost effective synthetic route towards anti viral eidd-1931 and its hydrate polymorphs |
| CN114085259A (zh) * | 2021-10-21 | 2022-02-25 | 苏州立新制药有限公司 | N4-羟基胞苷一水合物及其晶型b与制备方法和用途 |
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| KR20200140274A (ko) | 2018-03-07 | 2020-12-15 | 에모리 유니버시티 | 4'-할로겐 함유 뉴클레오티드 및 뉴클레오시드 치료 조성물 및 이와 관련된 용도 |
| PE20230466A1 (es) | 2020-02-07 | 2023-03-14 | Univ Emory | N4-hidroxicitidina y derivados y usos antivirales relacionados con los mismos |
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| RU2791806C1 (ru) * | 2022-12-28 | 2023-03-13 | федеральное государственное бюджетное учреждение "Национальный исследовательский центр эпидемиологии и микробиологии имени почетного академика Н.Ф. Гамалеи" Министерства здравоохранения Российской Федерации | Применение 5'-О-(3-фенилпропионил)-N4-гидроксицитидина для ингибирования репликации вируса гриппа in vitro и in vivo |
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