EA018757B1 - 2'-фтор-2'-дезокситетрагидроуридины в качестве ингибиторов цитидиндеаминазы - Google Patents
2'-фтор-2'-дезокситетрагидроуридины в качестве ингибиторов цитидиндеаминазы Download PDFInfo
- Publication number
- EA018757B1 EA018757B1 EA201000642A EA201000642A EA018757B1 EA 018757 B1 EA018757 B1 EA 018757B1 EA 201000642 A EA201000642 A EA 201000642A EA 201000642 A EA201000642 A EA 201000642A EA 018757 B1 EA018757 B1 EA 018757B1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- compound
- substrate
- drug
- pharmaceutically acceptable
- cancer
- Prior art date
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Classifications
-
- 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
Landscapes
- 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)
- Genetics & Genomics (AREA)
- Biotechnology (AREA)
- Biochemistry (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Epidemiology (AREA)
- Oncology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Hematology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Saccharide Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US98039707P | 2007-10-16 | 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 |
|---|---|
| EA201000642A1 EA201000642A1 (ru) | 2010-10-29 |
| EA018757B1 true EA018757B1 (ru) | 2013-10-30 |
Family
ID=40251685
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| EA201000642A EA018757B1 (ru) | 2007-10-16 | 2008-10-16 | 2'-фтор-2'-дезокситетрагидроуридины в качестве ингибиторов цитидиндеаминазы |
Country Status (39)
Families Citing this family (40)
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| US8404716B2 (en) | 2002-10-15 | 2013-03-26 | Celgene Corporation | Methods of treating myelodysplastic syndromes with a combination therapy using lenalidomide and azacitidine |
| US11116782B2 (en) | 2002-10-15 | 2021-09-14 | 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 Compounds, Compositions and Methods |
| PT3782611T (pt) | 2008-05-15 | 2022-11-18 | Celgene Corp | Formulações orais de análogos da citidina e métodos de utilização dos mesmos |
| 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 |
| EA019295B1 (ru) | 2008-12-23 | 2014-02-28 | Джилид Фармассет, Ллс. | Соединения пуриновых нуклеозидов и способ их получения |
| US8329666B2 (en) | 2009-04-06 | 2012-12-11 | Eisai Inc. | Compositions and methods for treating cancer |
| US8324180B2 (en) * | 2009-04-06 | 2012-12-04 | Eisai Inc. | Compositions and methods for treating cancer |
| US8329665B2 (en) | 2009-04-06 | 2012-12-11 | Eisai Inc. | Compositions and methods for treating cancer |
| US8609631B2 (en) * | 2009-04-06 | 2013-12-17 | Eisai Inc. | Compositions and methods for treating cancer |
| GB0907551D0 (en) | 2009-05-01 | 2009-06-10 | Univ Dundee | Treatment or prophylaxis of proliferative conditions |
| TWI583692B (zh) | 2009-05-20 | 2017-05-21 | 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 |
| TWI498117B (zh) | 2010-03-31 | 2015-09-01 | Gilead Pharmasset Llc | 核苷氨基磷酸酯 |
| US8563530B2 (en) | 2010-03-31 | 2013-10-22 | Gilead Pharmassel LLC | Purine nucleoside phosphoramidate |
| US8841275B2 (en) | 2010-11-30 | 2014-09-23 | Gilead Pharmasset Llc | 2′-spiro-nucleosides and derivatives thereof useful for treating hepatitis C virus and dengue virus infections |
| DE202012013074U1 (de) | 2011-09-16 | 2014-10-29 | Gilead Pharmasset Lcc | Zusammensetzungen zur Behandlung von HCV |
| US8889159B2 (en) | 2011-11-29 | 2014-11-18 | Gilead Pharmasset Llc | Compositions and methods for treating hepatitis C virus |
| EP2950786B1 (en) | 2013-01-31 | 2019-11-27 | Gilead Pharmasset LLC | Combination formulation of two antiviral compounds |
| JP2016529293A (ja) | 2013-08-27 | 2016-09-23 | ギリアド ファーマセット エルエルシー | 2つの抗ウイルス化合物の組合せ製剤 |
| MY176465A (en) * | 2013-10-29 | 2020-08-11 | Otsuka Pharma Co Ltd | Synthetic route to 2?-deoxy-2?,2?-difluorotetrahydrouridines |
| JP6783224B2 (ja) | 2014-04-04 | 2020-11-11 | デル マー ファーマシューティカルズ | 肺の非小細胞癌腫及び卵巣癌を処置するためのジアンヒドロガラクチトール及びその類縁体又は誘導体の使用 |
| HRP20230265T1 (hr) | 2014-08-22 | 2023-04-14 | Celgene Corporation | Postupci liječenja multiplog mijeloma imunomodulatornim spojevima u kombinaciji s protutijelima |
| EP3960182B1 (en) | 2015-12-03 | 2025-03-19 | EpiDestiny, Inc. | Compositions containing decitabine, 5-azacytidine 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 |
| CA3091027A1 (en) | 2018-02-02 | 2019-08-08 | Maverix Oncology, Inc. | Small molecule drug conjugates of gemcitabine monophosphate |
| CN121324657A (zh) * | 2018-08-28 | 2026-01-13 | 上海宜晟生物科技有限公司 | 测定准确度改善 |
| US11224610B2 (en) * | 2018-09-19 | 2022-01-18 | Otsuka Pharmaceutical Co., Ltd. | Low dose combination CDA substrate drug/cedazuridine with extended administration |
| KR102280330B1 (ko) * | 2018-10-19 | 2021-07-21 | 인터올리고 주식회사 | 치료 효능을 개선한 핵산 변형체 및 이를 포함하는 항암용 약학 조성물 |
| US12448624B2 (en) | 2018-10-19 | 2025-10-21 | Interoligo Corporation | Modified nucleic acid having improved treatment efficacy, and anticancer pharmaceutical composition containing same |
| CN120040527A (zh) | 2019-10-08 | 2025-05-27 | 大塚制药株式会社 | 包括2’-脱氧-2’,2’-二氟四氢尿苷的组合物 |
| ES2992301T3 (es) * | 2020-02-25 | 2024-12-11 | Otsuka Pharma Co Ltd | Formas de dosificación oral sólidas que comprenden decitabina y cedazuridina |
| WO2022204126A1 (en) * | 2021-03-26 | 2022-09-29 | The Cleveland Clinic Foundation | Treatment of rna virus infection with a cytidine deaminase inhibitor |
| US20240279266A1 (en) * | 2021-05-29 | 2024-08-22 | 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 |
| JP2024539267A (ja) | 2021-10-19 | 2024-10-28 | アキラバイオ, インコーポレイテッド | 2’-デオキシシチジンアナログを含む組成物、ならびに鎌状赤血球症、サラセミアおよびがんを処置するためのその使用 |
| US20250127806A1 (en) * | 2021-11-01 | 2025-04-24 | St. John's University | Injectable liquid pharmaceutical composition containing gemcitabine and a cytidine deaminase inhibitor |
| US20230271996A1 (en) * | 2021-12-25 | 2023-08-31 | Scinopharm Taiwan, Ltd. | Process for preparing cedazuridine |
| AU2022476674A1 (en) | 2022-08-31 | 2025-04-17 | Taiho Pharmaceutical Co., Ltd. | Combination therapies for treatment of t-cell lymphomas with tolinapant, cedazuridine and decitabine |
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| WO2008085611A2 (en) * | 2006-11-27 | 2008-07-17 | University Of Miami | Designer theraphy of pancreatic tumors |
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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 BR BRPI0818672A patent/BRPI0818672B8/pt active IP Right Grant
- 2008-10-16 EP EP12151552.2A patent/EP2447272B1/en active Active
- 2008-10-16 EA EA201000642A patent/EA018757B1/ru unknown
- 2008-10-16 PL PL08840633T patent/PL2207786T3/pl unknown
- 2008-10-16 NZ NZ584229A patent/NZ584229A/en unknown
- 2008-10-16 ME MEP-2010-68A patent/ME00997B/me unknown
- 2008-10-16 US US12/252,961 patent/US8268800B2/en active Active
- 2008-10-16 KR KR1020107010621A patent/KR101543049B1/ko active Active
- 2008-10-16 DK DK08840633.5T patent/DK2207786T3/da active
- 2008-10-16 ES ES08840633T patent/ES2384011T3/es active Active
- 2008-10-16 JP JP2010530110A patent/JP5496899B2/ja active Active
- 2008-10-16 WO PCT/US2008/080163 patent/WO2009052287A1/en not_active Ceased
- 2008-10-16 CA CA2702274A patent/CA2702274C/en active Active
- 2008-10-16 UA UAA201003977A patent/UA99476C2/ru unknown
- 2008-10-16 MY MYPI2010001528A patent/MY147970A/en unknown
- 2008-10-16 ES ES12151552.2T patent/ES2616566T3/es active Active
- 2008-10-16 SI SI200830624T patent/SI2207786T1/sl unknown
- 2008-10-16 PT PT08840633T patent/PT2207786E/pt unknown
- 2008-10-16 MX MX2010004109A patent/MX2010004109A/es active IP Right Grant
- 2008-10-16 EP EP08840633A patent/EP2207786B1/en active Active
- 2008-10-16 HR HRP20120419AT patent/HRP20120419T1/hr unknown
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Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4017606A (en) * | 1973-10-04 | 1977-04-12 | The Upjohn Company | Organic compounds and process |
| WO2008085611A2 (en) * | 2006-11-27 | 2008-07-17 | University Of Miami | Designer theraphy of pancreatic tumors |
Non-Patent Citations (1)
| Title |
|---|
| WATANABE K.A. ET AL.: "Nucleosides. 110. Synthesis and Antiherpes Virus Activity of Some 2'-Fluoro-2'-deoxyarabinofuranosylpyrimidine Nucleosides" J. MED. CHEM., vol. 22, no. 1, 1979, pages 21-24, XP002511651 * Compound of formula 9a * table I * |
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