CN101827856B - 作为胞嘧啶核苷脱氨酶抑制剂的2′-氟-2′-脱氧四氢尿苷 - Google Patents
作为胞嘧啶核苷脱氨酶抑制剂的2′-氟-2′-脱氧四氢尿苷 Download PDFInfo
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- CN101827856B CN101827856B CN2008801117195A CN200880111719A CN101827856B CN 101827856 B CN101827856 B CN 101827856B CN 2008801117195 A CN2008801117195 A CN 2008801117195A CN 200880111719 A CN200880111719 A CN 200880111719A CN 101827856 B CN101827856 B CN 101827856B
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- 0 *=C(NC(CC1)O)N1C([C@@]1O)O[C@@](CO)[C@@]1O Chemical compound *=C(NC(CC1)O)N1C([C@@]1O)O[C@@](CO)[C@@]1O 0.000 description 5
- VUDZSIYXZUYWSC-RKEPMNIXSA-N OC[C@H]([C@H](C1(F)F)O)OC1N(CC[C@H](N1)O)C1=O Chemical compound OC[C@H]([C@H](C1(F)F)O)OC1N(CC[C@H](N1)O)C1=O VUDZSIYXZUYWSC-RKEPMNIXSA-N 0.000 description 1
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/04—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- 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
-
- 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
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/04—Antineoplastic agents specific for metastasis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
- C07H1/00—Processes for the preparation of sugar derivatives
-
- 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
-
- 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
- C07H19/073—Pyrimidine radicals with 2-deoxyribosyl as the saccharide radical
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/13—Crystalline forms, e.g. polymorphs
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- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Molecular Biology (AREA)
- Engineering & Computer Science (AREA)
- Biotechnology (AREA)
- Biochemistry (AREA)
- Genetics & Genomics (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Epidemiology (AREA)
- Oncology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Hematology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Saccharide Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US98039707P | 2007-10-16 | 2007-10-16 | |
| US60/980397 | 2007-10-16 | ||
| PCT/US2008/080163 WO2009052287A1 (en) | 2007-10-16 | 2008-10-16 | 2 ' -flu0r0-2 ' -deoxytetrahydrouridines as cytidine deaminase inhibitors |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN101827856A CN101827856A (zh) | 2010-09-08 |
| CN101827856B true CN101827856B (zh) | 2013-02-06 |
Family
ID=40251685
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN2008801117195A Active CN101827856B (zh) | 2007-10-16 | 2008-10-16 | 作为胞嘧啶核苷脱氨酶抑制剂的2′-氟-2′-脱氧四氢尿苷 |
Country Status (39)
Families Citing this family (39)
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| US11116782B2 (en) | 2002-10-15 | 2021-09-14 | Celgene Corporation | Methods of treating myelodysplastic syndromes with a combination therapy using lenalidomide and azacitidine |
| US8404716B2 (en) | 2002-10-15 | 2013-03-26 | Celgene Corporation | Methods of treating myelodysplastic syndromes with a combination therapy using lenalidomide and azacitidine |
| US7964580B2 (en) | 2007-03-30 | 2011-06-21 | Pharmasset, Inc. | Nucleoside phosphoramidate prodrugs |
| JO2778B1 (en) * | 2007-10-16 | 2014-03-15 | ايساي انك | Certain vehicles, installations and methods |
| ES2969144T3 (es) | 2008-05-15 | 2024-05-16 | Celgene Corp | Formulaciones orales de análogos de citidina y métodos de uso de los mismos |
| US8173621B2 (en) | 2008-06-11 | 2012-05-08 | Gilead Pharmasset Llc | Nucleoside cyclicphosphates |
| US20100055047A1 (en) * | 2008-08-26 | 2010-03-04 | Yiyu Zou | Methods for treating bronchial premalignancy and lung cancer |
| CL2009002206A1 (es) * | 2008-12-23 | 2011-08-26 | Gilead Pharmasset Llc | Compuestos derivados de pirrolo -(2-3-d]-pirimidin-7(6h)-tetrahidrofuran-2-il fosfonamidato, composicion farmaceutica; y su uso en el tratamiento de enfermedades virales. |
| US8609631B2 (en) | 2009-04-06 | 2013-12-17 | Eisai Inc. | Compositions and methods for treating cancer |
| WO2010118013A1 (en) * | 2009-04-06 | 2010-10-14 | Eisai Inc. | Combination of cytidine-based antineoplastic drugs with cytidine deaminase inhibitor and use thereof in the treatment of cancer |
| TWI477508B (zh) * | 2009-04-06 | 2015-03-21 | Otsuka Pharma Co Ltd | 用以治療癌症之組成物及方法 |
| UY32546A (es) * | 2009-04-06 | 2010-10-29 | Eisai Inc | Composiciones y metodos para tratar cancer |
| GB0907551D0 (en) | 2009-05-01 | 2009-06-10 | Univ Dundee | Treatment or prophylaxis of proliferative conditions |
| TWI576352B (zh) | 2009-05-20 | 2017-04-01 | 基利法瑪席特有限責任公司 | 核苷磷醯胺 |
| US8618076B2 (en) | 2009-05-20 | 2013-12-31 | Gilead Pharmasset Llc | Nucleoside phosphoramidates |
| BR112012024884A2 (pt) | 2010-03-31 | 2016-10-18 | Gilead Pharmasset Llc | síntese estereosseletiva de ativos contendo fósforo |
| US8563530B2 (en) | 2010-03-31 | 2013-10-22 | Gilead Pharmassel LLC | Purine nucleoside phosphoramidate |
| AR084044A1 (es) | 2010-11-30 | 2013-04-17 | Pharmasset Inc | Compuestos 2’-espiro-nucleosidos |
| CN104244945B (zh) | 2011-09-16 | 2016-08-31 | 吉利德制药有限责任公司 | 用于治疗hcv的方法 |
| US8889159B2 (en) | 2011-11-29 | 2014-11-18 | Gilead Pharmasset Llc | Compositions and methods for treating hepatitis C virus |
| DK2950786T3 (da) | 2013-01-31 | 2020-02-17 | Gilead Pharmasset Llc | Kombinationsformulering af to antivirale forbindelser |
| ES2792503T3 (es) | 2013-08-27 | 2020-11-11 | Gilead Pharmasset Llc | Formulación combinada de dos compuestos antivirales |
| CA2926734C (en) * | 2013-10-29 | 2022-03-15 | Otsuka Pharmaceutical Co., Ltd. | Synthetic route to 2'-deoxy-2',2'-difluorotetrahydrouridines |
| EP3125920B1 (en) | 2014-04-04 | 2020-12-23 | Del Mar Pharmaceuticals | Dianhydrogalactitol, diacetyldianhydrogalactitol or dibromodulcitol to treat non-small-cell carcinoma of the lung and ovarian cancer |
| HUE061382T2 (hu) | 2014-08-22 | 2023-06-28 | Celgene Corp | Eljárás myeloma multiplex kezelésére immunomoduláló vegyületekkel, antestekkel kombinálva |
| WO2017096357A1 (en) | 2015-12-03 | 2017-06-08 | Epidestiny, Inc. | Compositions containing decitabine, 5azacytidine and tetrahydrouridine and uses thereof |
| WO2017158396A1 (en) * | 2016-03-16 | 2017-09-21 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Cytidine deaminase inhibitors for the treatment of pancreatic cancer |
| WO2019152955A1 (en) | 2018-02-02 | 2019-08-08 | Steven Albert Everett | Small molecule drug conjugates of gemcitabine monophosphate |
| US11224610B2 (en) * | 2018-09-19 | 2022-01-18 | Otsuka Pharmaceutical Co., Ltd. | Low dose combination CDA substrate drug/cedazuridine with extended administration |
| US20210388361A1 (en) * | 2018-10-19 | 2021-12-16 | Interoligo Corporation | Modified nucleic acid having improved treatment efficacy, and anticancer pharmaceutical composition containing same |
| CN112888700A (zh) * | 2018-10-19 | 2021-06-01 | 因特欧力多公司 | 具有改善治疗功效的修饰核酸和含有其的抗癌药物组合物 |
| MX2022004271A (es) * | 2019-10-08 | 2022-06-09 | Otsuka Pharma Co Ltd | 2'-desoxi-2',2'-difluoro tetrahidruridina de alta pureza y metodos para su preparacion. |
| EP4069254A4 (en) * | 2020-02-25 | 2023-11-29 | Otsuka Pharmaceutical Co., Ltd. | ORAL SOLID DOSAGE FORMS OF DEITABINE AND CEDURIDINE |
| BR112023019182A2 (pt) * | 2021-03-26 | 2023-11-28 | Cleveland Clinic Found | Uso de um inibidor de citidina desaminase na preparação de um medicamento, sistema, kit ou artigo de manufatura e composição |
| WO2022254457A1 (en) * | 2021-05-29 | 2022-12-08 | Msn Laboratories Private Limited, R&D Center | An improved process for the preparation of (4r)-1-[(2r,4r,5r)-3,3-difluoro-4-hydroxy-5-(hydroxymethyl) oxolan-2-yl]-4-hydroxy-1,3-diazinan-2one and its intermediate compounds |
| US11938143B2 (en) | 2021-10-19 | 2024-03-26 | Akirabio, Inc. | Compositions comprising 2′-deoxycytidine analogs and use thereof for the treatment of sickle cell disease, thalassemia, and cancers |
| WO2023076332A1 (en) * | 2021-11-01 | 2023-05-04 | St. John's University | Injectable liquid pharmaceutical compostion containing gemcitabine and a cytidine deaminase inhibitor |
| US20230271996A1 (en) * | 2021-12-25 | 2023-08-31 | Scinopharm Taiwan, Ltd. | Process for preparing cedazuridine |
| WO2024047394A1 (en) | 2022-08-31 | 2024-03-07 | Otsuka Pharmaceutical Co., Ltd. | Combination therapies for treatment of t-cell lymphomas with tolinapant, cedazuridine and decitabine |
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-
2008
- 2008-10-14 JO JO2008459A patent/JO2778B1/en active
- 2008-10-15 TW TW097139594A patent/TWI445539B/zh active
- 2008-10-16 EA EA201000642A patent/EA018757B1/ru unknown
- 2008-10-16 PT PT08840633T patent/PT2207786E/pt unknown
- 2008-10-16 NZ NZ584229A patent/NZ584229A/en unknown
- 2008-10-16 MX MX2010004109A patent/MX2010004109A/es active IP Right Grant
- 2008-10-16 ES ES08840633T patent/ES2384011T3/es active Active
- 2008-10-16 RS RS20120232A patent/RS52323B/en unknown
- 2008-10-16 CN CN2008801117195A patent/CN101827856B/zh active Active
- 2008-10-16 CA CA2702274A patent/CA2702274C/en active Active
- 2008-10-16 UA UAA201003977A patent/UA99476C2/ru unknown
- 2008-10-16 EP EP12151552.2A patent/EP2447272B1/en active Active
- 2008-10-16 AT AT08840633T patent/ATE548374T1/de active
- 2008-10-16 SI SI200830624T patent/SI2207786T1/sl unknown
- 2008-10-16 PL PL08840633T patent/PL2207786T3/pl unknown
- 2008-10-16 BR BRPI0818672A patent/BRPI0818672B8/pt active IP Right Grant
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Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4017606A (en) * | 1973-10-04 | 1977-04-12 | The Upjohn Company | Organic compounds and process |
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