CN111194217B - 作为hcv rna复制抑制剂的4’-氟-2’-甲基取代的核苷衍生物 - Google Patents
作为hcv rna复制抑制剂的4’-氟-2’-甲基取代的核苷衍生物 Download PDFInfo
- Publication number
- CN111194217B CN111194217B CN201880061322.3A CN201880061322A CN111194217B CN 111194217 B CN111194217 B CN 111194217B CN 201880061322 A CN201880061322 A CN 201880061322A CN 111194217 B CN111194217 B CN 111194217B
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- CN
- China
- Prior art keywords
- formula
- amino
- compound
- difluoro
- methyltetrahydrofuran
- Prior art date
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Classifications
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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
- C07H19/10—Pyrimidine radicals with the saccharide radical esterified by phosphoric or polyphosphoric acids
-
- 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
- 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
- A61K31/7072—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 having two oxo groups directly attached to the pyrimidine ring, e.g. uridine, uridylic acid, thymidine, zidovudine
-
- 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
- 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
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
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- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical & Material Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Molecular Biology (AREA)
- Epidemiology (AREA)
- Organic Chemistry (AREA)
- Virology (AREA)
- Communicable Diseases (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Oncology (AREA)
- Engineering & Computer Science (AREA)
- Biochemistry (AREA)
- Biotechnology (AREA)
- Genetics & Genomics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Saccharide Compounds (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201762561237P | 2017-09-21 | 2017-09-21 | |
| US62/561,237 | 2017-09-21 | ||
| PCT/US2018/052239 WO2019060740A1 (en) | 2017-09-21 | 2018-09-21 | 4'-FLUORO-2'-METHYL SUBSTITUTED NUCLEOSIDE DERIVATIVES AS INHIBITORS OF HCV RNA REPLICATION |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN111194217A CN111194217A (zh) | 2020-05-22 |
| CN111194217B true CN111194217B (zh) | 2024-01-12 |
Family
ID=65810030
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201880061322.3A Active CN111194217B (zh) | 2017-09-21 | 2018-09-21 | 作为hcv rna复制抑制剂的4’-氟-2’-甲基取代的核苷衍生物 |
Country Status (12)
| Country | Link |
|---|---|
| US (2) | US10682369B2 (https=) |
| EP (1) | EP3684374B1 (https=) |
| JP (1) | JP7299897B2 (https=) |
| KR (1) | KR102735678B1 (https=) |
| CN (1) | CN111194217B (https=) |
| AR (1) | AR112702A1 (https=) |
| AU (1) | AU2018335411B2 (https=) |
| CA (1) | CA3075645A1 (https=) |
| IL (1) | IL273398B2 (https=) |
| SG (1) | SG11202002431SA (https=) |
| TW (1) | TWI860279B (https=) |
| WO (1) | WO2019060740A1 (https=) |
Families Citing this family (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20180200280A1 (en) * | 2013-05-16 | 2018-07-19 | Riboscience Llc | 4'-Fluoro-2'-Methyl Substituted Nucleoside Derivatives as Inhibitors of HCV RNA Replication |
| EP3684374B1 (en) * | 2017-09-21 | 2025-07-30 | Riboscience LLC | 4'-fluoro-2'-methyl substituted nucleoside derivatives as inhibitors of hcv rna replication |
| TW202144465A (zh) | 2020-02-11 | 2021-12-01 | 瑞士商諾和席卓股份有限公司 | 合成聚葡萄胺糖衍生物之新方法及其用途 |
| EP3865535A1 (en) | 2020-02-11 | 2021-08-18 | Bosti Trading Ltd. | New method of synthesis of chitosan derivatives and uses thereof |
| WO2022174179A1 (en) * | 2021-02-15 | 2022-08-18 | Emory University | 4'-halogen containing nucleotide and nucleoside therapeutic compositions and uses related thereto |
| AR126678A1 (es) | 2021-08-06 | 2023-11-01 | Novochizol Sa | Composiciones para el cuidado de las plantas y usos de las mismas |
| US12403221B2 (en) | 2021-08-06 | 2025-09-02 | Novochizol Sa | Preparation of composite gels, polymer scaffolds, aggregates and films comprising soluble cross-linked chitosan and uses thereof |
Citations (13)
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| CN1777432A (zh) * | 2003-02-19 | 2006-05-24 | 耶鲁大学 | 用于治疗病毒感染尤其是hiv感染的抗病毒核苷类似物和方法 |
| CN101172992A (zh) * | 2002-06-28 | 2008-05-07 | 埃迪尼克斯(开曼)有限公司 | 用于治疗黄病毒感染的修饰的2′和3′-核苷前药 |
| CN101287472A (zh) * | 2005-08-15 | 2008-10-15 | 弗·哈夫曼-拉罗切有限公司 | 抗病毒的4'-取代前核苷酸的氨基磷酸酯类化合物 |
| CN101384609A (zh) * | 2006-02-14 | 2009-03-11 | 默克公司 | 用于治疗rna依赖性rna病毒感染的氨基磷酸(核苷)(芳基)酯 |
| WO2013092481A1 (en) * | 2011-12-20 | 2013-06-27 | F. Hoffmann-La Roche Ag | 2',4'-difluoro-2'-methyl substituted nucleoside derivatives as inhibitors of hcv rna replication |
| WO2014100505A1 (en) * | 2012-12-21 | 2014-06-26 | Alios Biopharma, Inc. | Substituted nucleosides, nucleotides and analogs thereof |
| WO2014186637A1 (en) * | 2013-05-16 | 2014-11-20 | Riboscience Llc | 4'-fluor0-2'-methyl substituted nucleoside derivatives |
| CN104244945A (zh) * | 2011-09-16 | 2014-12-24 | 吉利德法莫赛特有限责任公司 | 用于治疗hcv的方法 |
| CN105307661A (zh) * | 2013-05-16 | 2016-02-03 | 里博科学有限责任公司 | 4’-叠氮基,3’-脱氧基-3’-氟取代的核苷衍生物 |
| WO2016035006A1 (en) * | 2014-09-01 | 2016-03-10 | Dr. Reddy’S Laboratories Limited | Novel nucleotide analogs, process for the preparation of sofosbuvir and its analogs, novel forms of sofosbuvir and solid dispersion of sofosbuvir |
| 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 |
| CN107011350A (zh) * | 2012-12-21 | 2017-08-04 | 吉利德科学公司 | 抗病毒化合物 |
| CN109414508A (zh) * | 2016-05-27 | 2019-03-01 | 吉利德科学公司 | 使用ns5a、ns5b或ns3抑制剂治疗乙型肝炎病毒感染的方法 |
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2018
- 2018-09-21 EP EP18859097.0A patent/EP3684374B1/en active Active
- 2018-09-21 CN CN201880061322.3A patent/CN111194217B/zh active Active
- 2018-09-21 TW TW107133372A patent/TWI860279B/zh active
- 2018-09-21 IL IL273398A patent/IL273398B2/en unknown
- 2018-09-21 US US16/138,698 patent/US10682369B2/en active Active
- 2018-09-21 CA CA3075645A patent/CA3075645A1/en active Pending
- 2018-09-21 AU AU2018335411A patent/AU2018335411B2/en active Active
- 2018-09-21 AR ARP180102714 patent/AR112702A1/es unknown
- 2018-09-21 JP JP2020538752A patent/JP7299897B2/ja active Active
- 2018-09-21 SG SG11202002431SA patent/SG11202002431SA/en unknown
- 2018-09-21 WO PCT/US2018/052239 patent/WO2019060740A1/en not_active Ceased
- 2018-09-21 KR KR1020207011082A patent/KR102735678B1/ko active Active
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2020
- 2020-05-04 US US16/865,525 patent/US11351186B2/en active Active
Patent Citations (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101172992A (zh) * | 2002-06-28 | 2008-05-07 | 埃迪尼克斯(开曼)有限公司 | 用于治疗黄病毒感染的修饰的2′和3′-核苷前药 |
| CN1777432A (zh) * | 2003-02-19 | 2006-05-24 | 耶鲁大学 | 用于治疗病毒感染尤其是hiv感染的抗病毒核苷类似物和方法 |
| CN101287472A (zh) * | 2005-08-15 | 2008-10-15 | 弗·哈夫曼-拉罗切有限公司 | 抗病毒的4'-取代前核苷酸的氨基磷酸酯类化合物 |
| CN101384609A (zh) * | 2006-02-14 | 2009-03-11 | 默克公司 | 用于治疗rna依赖性rna病毒感染的氨基磷酸(核苷)(芳基)酯 |
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| US20210046100A1 (en) | 2021-02-18 |
| SG11202002431SA (en) | 2020-04-29 |
| AU2018335411A1 (en) | 2020-03-26 |
| AR112702A1 (es) | 2019-11-27 |
| US10682369B2 (en) | 2020-06-16 |
| EP3684374A4 (en) | 2021-06-16 |
| IL273398B2 (en) | 2025-02-01 |
| WO2019060740A1 (en) | 2019-03-28 |
| EP3684374A1 (en) | 2020-07-29 |
| JP2020534374A (ja) | 2020-11-26 |
| EP3684374B1 (en) | 2025-07-30 |
| IL273398B1 (en) | 2024-10-01 |
| TW201919649A (zh) | 2019-06-01 |
| US11351186B2 (en) | 2022-06-07 |
| CA3075645A1 (en) | 2019-03-28 |
| JP7299897B2 (ja) | 2023-06-28 |
| US20190231804A1 (en) | 2019-08-01 |
| IL273398A (en) | 2020-05-31 |
| TWI860279B (zh) | 2024-11-01 |
| KR102735678B1 (ko) | 2024-11-27 |
| KR20200056420A (ko) | 2020-05-22 |
| CN111194217A (zh) | 2020-05-22 |
| AU2018335411B2 (en) | 2024-06-27 |
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