JP6804790B1 - N4−ヒドロキシシチジンおよび誘導体ならびにそれらに関連する抗ウイルス用途 - Google Patents
N4−ヒドロキシシチジンおよび誘導体ならびにそれらに関連する抗ウイルス用途 Download PDFInfo
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- JP6804790B1 JP6804790B1 JP2020524817A JP2020524817A JP6804790B1 JP 6804790 B1 JP6804790 B1 JP 6804790B1 JP 2020524817 A JP2020524817 A JP 2020524817A JP 2020524817 A JP2020524817 A JP 2020524817A JP 6804790 B1 JP6804790 B1 JP 6804790B1
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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
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- 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)
- Chemical Kinetics & Catalysis (AREA)
- Oncology (AREA)
- Communicable Diseases (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (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)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Saccharide Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
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 |
|---|---|---|---|
| JP2020195927A Division JP7179372B2 (ja) | 2017-12-07 | 2020-11-26 | N4-ヒドロキシシチジンおよび誘導体ならびにそれらに関連する抗ウイルス用途 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP6804790B1 true JP6804790B1 (ja) | 2020-12-23 |
| JP2021505530A JP2021505530A (ja) | 2021-02-18 |
Family
ID=66751806
Family Applications (4)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2020524817A Active JP6804790B1 (ja) | 2017-12-07 | 2018-12-07 | N4−ヒドロキシシチジンおよび誘導体ならびにそれらに関連する抗ウイルス用途 |
| JP2020195927A Active JP7179372B2 (ja) | 2017-12-07 | 2020-11-26 | N4-ヒドロキシシチジンおよび誘導体ならびにそれらに関連する抗ウイルス用途 |
| JP2021106296A Active JP7305205B2 (ja) | 2017-12-07 | 2021-06-28 | N4-ヒドロキシシチジンおよび誘導体ならびにそれらに関連する抗ウイルス用途 |
| JP2023062657A Pending JP2023082213A (ja) | 2017-12-07 | 2023-04-07 | N4-ヒドロキシシチジンおよび誘導体ならびにそれらに関連する抗ウイルス用途 |
Family Applications After (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2020195927A Active JP7179372B2 (ja) | 2017-12-07 | 2020-11-26 | N4-ヒドロキシシチジンおよび誘導体ならびにそれらに関連する抗ウイルス用途 |
| JP2021106296A Active JP7305205B2 (ja) | 2017-12-07 | 2021-06-28 | N4-ヒドロキシシチジンおよび誘導体ならびにそれらに関連する抗ウイルス用途 |
| JP2023062657A Pending JP2023082213A (ja) | 2017-12-07 | 2023-04-07 | N4-ヒドロキシシチジンおよび誘導体ならびにそれらに関連する抗ウイルス用途 |
Country Status (27)
| Country | Link |
|---|---|
| US (3) | US11331331B2 (enExample) |
| EP (2) | EP3706762B1 (enExample) |
| JP (4) | JP6804790B1 (enExample) |
| KR (3) | KR20240011880A (enExample) |
| CN (2) | CN111372592A (enExample) |
| AU (2) | AU2018378832B9 (enExample) |
| BR (1) | BR122022008466B1 (enExample) |
| CA (1) | CA3082191C (enExample) |
| DK (1) | DK3706762T3 (enExample) |
| ES (1) | ES2995458T3 (enExample) |
| FI (1) | FI3706762T3 (enExample) |
| GB (2) | GB2581936B (enExample) |
| HR (1) | HRP20241620T1 (enExample) |
| HU (1) | HUE069306T2 (enExample) |
| IL (2) | IL274155B (enExample) |
| LT (1) | LT3706762T (enExample) |
| MX (2) | MX2020005392A (enExample) |
| PH (2) | PH12022550371A1 (enExample) |
| PL (1) | PL3706762T3 (enExample) |
| PT (1) | PT3706762T (enExample) |
| RS (1) | RS66222B1 (enExample) |
| RU (1) | RU2020116571A (enExample) |
| SA (1) | SA520412305B1 (enExample) |
| SG (1) | SG11202004403QA (enExample) |
| SI (1) | SI3706762T1 (enExample) |
| WO (1) | WO2019113462A1 (enExample) |
| ZA (1) | ZA202002849B (enExample) |
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| CN107427529A (zh) * | 2014-12-26 | 2017-12-01 | 埃莫里大学 | N4‑羟基胞苷和衍生物及与其相关的抗病毒用途 |
| 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 |
| ES2995458T3 (en) * | 2017-12-07 | 2025-02-10 | Univ Emory | N4-hydroxycytidine derivative and anti-viral uses related thereto |
| 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 |
| WO2021050956A1 (en) * | 2019-09-11 | 2021-03-18 | The Scripps Research Institute | Antiviral prodrugs and pharmaceutical compositions thereof |
| 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 |
| WO2021203055A1 (en) * | 2020-04-03 | 2021-10-07 | Selva Therapeutics, Inc. | 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 |
| US20240025938A1 (en) * | 2020-08-27 | 2024-01-25 | Emory University | Novel forms of antiviral nucleosides |
| US20230270669A1 (en) * | 2020-09-04 | 2023-08-31 | 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 |
| EP4262816A4 (en) * | 2020-12-18 | 2024-05-15 | Merck Sharp & Dohme LLC | PRODUCTION 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 |
| US11312743B1 (en) * | 2021-03-20 | 2022-04-26 | Optimus Drugs Private Limited | Process for molnupiravir |
| WO2022208156A1 (en) * | 2021-03-29 | 2022-10-06 | Optimus Pharma Private Limited | Pharmaceutical composition of molnupiravir |
| EP4320100A1 (en) | 2021-04-09 | 2024-02-14 | Immunic AG | Deuterated dhodh inhibitors |
| CN115215914B (zh) * | 2021-04-15 | 2024-05-28 | 中国科学院上海药物研究所 | 核苷类似物及其用途 |
| 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 |
| WO2022265964A1 (en) * | 2021-06-14 | 2022-12-22 | VenatoRx Pharmaceuticals, Inc. | Orally-bioavailable nucleoside analogs |
| 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 |
| WO2022262845A1 (en) * | 2021-06-18 | 2022-12-22 | Suzhou Spring-Sea Bio-Pharmaceuticals Co., Ltd. | Ester derivatives of n4-hydroxycytidine and use thereof |
| 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 |
| CN113735929A (zh) * | 2021-07-21 | 2021-12-03 | 海化生命(厦门)科技有限公司 | 一种抗冠状病毒的化合物及其制备方法与应用 |
| MX2024001645A (es) | 2021-08-06 | 2024-02-27 | Intervet Int Bv | Metodo para el tratamiento de las enfermedades virales veterinarias. |
| CN115960148B (zh) * | 2021-08-27 | 2023-12-12 | 南京知和医药科技有限公司 | 一种新型的胞苷衍生物及其药物组合物和用途 |
| JP2024170686A (ja) * | 2021-10-19 | 2024-12-11 | 興和株式会社 | 新規医薬 |
| 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 |
| CN113880902A (zh) * | 2021-10-26 | 2022-01-04 | 江苏睿实生物科技有限公司 | 一种Molnupiravir药物中间体及其制备方法 |
| EP4426315A1 (en) | 2021-11-01 | 2024-09-11 | Immunic AG | Medical use of n4-hydroxy citicoline compounds |
| CN113929724B (zh) * | 2021-11-02 | 2024-05-31 | 周雨恬 | 一种核苷类化合物及其药物组合物和用途 |
| CN114306254B (zh) * | 2021-11-30 | 2023-11-03 | 南京正济医药研究有限公司 | 一种Molnupiravir口服固体制剂及其制备方法 |
| CN116217632A (zh) * | 2021-12-06 | 2023-06-06 | 广州谷森制药有限公司 | 一种氘代胞苷衍生物的制备方法 |
| WO2023111683A1 (en) * | 2021-12-16 | 2023-06-22 | Ascletis Bioscience Co., Ltd. | N4-hydroxycytidine derivatives and use thereof as antiviral agent |
| US11541071B1 (en) * | 2021-12-16 | 2023-01-03 | Ascletis BioScience Co., Ltd | Nucleoside derivatives and methods of use thereof |
| CN118488831A (zh) | 2021-12-23 | 2024-08-13 | 苏宾特罗有限公司 | 包含油酸的新抗病毒组合物 |
| UY40087A (es) | 2021-12-23 | 2023-06-30 | Immunic Ag | Inhibidores de DHODH que contienen un bioisóstero de ácido carboxílico. |
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| CN114560894B (zh) * | 2022-03-11 | 2023-06-20 | 浙江乐普药业股份有限公司 | 一种抗新冠药物Molnupiravir的制备方法 |
| CN114773405B (zh) * | 2022-06-21 | 2022-09-23 | 和鼎(南京)医药技术有限公司 | 一种莫那比拉韦的制备方法 |
| EP4633644A1 (en) * | 2022-12-16 | 2025-10-22 | Merck Sharp & Dohme LLC | Solid dosage form of a small molecule antiviral and uses thereof |
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| TW202440076A (zh) | 2022-12-23 | 2024-10-16 | 日商明治製菓藥業股份有限公司 | 阿維菌素衍生物 |
| WO2024144420A1 (ru) * | 2022-12-28 | 2024-07-04 | 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 |
| WO2025003402A1 (en) | 2023-06-28 | 2025-01-02 | Immunic Ag | Heteroaromatic dhodh inhibitors |
| TW202523336A (zh) * | 2023-12-07 | 2025-06-16 | 中國化學製藥股份有限公司 | 醫藥溶液組合物及包含其之口腔霧化吸入劑型 |
| US12357577B1 (en) | 2024-02-02 | 2025-07-15 | Gilead Sciences, Inc. | Pharmaceutical formulations and uses thereof |
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| GB1325798A (en) | 1970-09-24 | 1973-08-08 | Upjohn Co | Derivatives of 2,2-anhydro-ara-cytidine |
| GB1386334A (en) | 1972-09-22 | 1975-03-05 | Kohjin Co | 2,2-cyclocytidine derivatives |
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