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)
- Biotechnology (AREA)
- Genetics & Genomics (AREA)
- Biochemistry (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (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)
- 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 |
| US8846628B2 (en) | 2008-05-15 | 2014-09-30 | Celgene Corporation | Oral formulations of cytidine analogs and methods of use thereof |
| 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 |
| NZ593647A (en) | 2008-12-23 | 2013-08-30 | Gilead Pharmasset Llc | Synthesis of purine nucleosides |
| JP5684787B2 (ja) * | 2009-04-06 | 2015-03-18 | 大塚製薬株式会社 | シチジンベースの抗新生物薬とシチジンデアミナーゼ阻害薬との組合せ、および癌の治療におけるその使用 |
| US8609631B2 (en) | 2009-04-06 | 2013-12-17 | Eisai Inc. | Compositions and methods for treating cancer |
| JO3262B1 (ar) * | 2009-04-06 | 2018-09-16 | Otsuka Pharma Co Ltd | توليفة من ديسيتابين مع مثبط سيتيدين دي أميناز واستخدامها في علاج السرطان |
| AR076262A1 (es) * | 2009-04-06 | 2011-06-01 | Eisai Inc | Derivados heterociclicos de diazepin-2-ona, composiciones farmaceuticas y sus usos en el tratamiento del cancer |
| GB0907551D0 (en) | 2009-05-01 | 2009-06-10 | Univ Dundee | Treatment or prophylaxis of proliferative conditions |
| TWI598358B (zh) | 2009-05-20 | 2017-09-11 | 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 |
| JP2013527145A (ja) | 2010-03-31 | 2013-06-27 | ギリード・ファーマセット・エルエルシー | リン含有活性化剤の立体選択的合成 |
| PL3290428T3 (pl) | 2010-03-31 | 2022-02-07 | Gilead Pharmasset Llc | Tabletka zawierająca krystaliczny (S)-2-(((S)-(((2R,3R,4R,5R)-5-(2,4-diokso-3,4-dihydropirymidyn-1(2H)-ylo)-4-fluoro-3-hydroksy-4-metylotetrahydrofuran-2-ylo)metoksy)(fenoksy)fosforylo)amino)propanian izopropylu |
| PT3042910T (pt) | 2010-11-30 | 2019-04-16 | Gilead Pharmasset Llc | 2'-espiro-nucleósidos para utilização na terapia da hepatite c |
| CA2840242C (en) | 2011-09-16 | 2019-03-26 | Gilead Sciences, Inc. | Methods for treating hcv |
| US8889159B2 (en) | 2011-11-29 | 2014-11-18 | Gilead Pharmasset Llc | Compositions and methods for treating hepatitis C virus |
| KR20200060782A (ko) | 2013-01-31 | 2020-06-01 | 길리애드 파마셋 엘엘씨 | 두 항바이러스 화합물의 병용 제형물 |
| EP3650014B1 (en) | 2013-08-27 | 2021-10-06 | Gilead Pharmasset LLC | Combination formulation of two antiviral compounds |
| ES2712877T3 (es) | 2013-10-29 | 2019-05-16 | Otsuka Pharma Co Ltd | Ruta sintética de 2-desoxi-2,2-difluorotetrahidrouridinas |
| WO2015154064A2 (en) | 2014-04-04 | 2015-10-08 | Del Mar Pharmaceuticals | Use of dianhydrogalactitol and analogs or derivatives thereof to treat non-small-cell carcinoma of the lung and ovarian cancer |
| LT3182996T (lt) | 2014-08-22 | 2023-03-10 | Celgene Corporation | Daugybinės mielomos gydymo būdai imunomoduliuojančiais junginiais derinyje su antikūnais |
| CA3007357C (en) * | 2015-12-03 | 2023-12-05 | 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 |
| AU2019216531A1 (en) | 2018-02-02 | 2020-09-24 | Maverix Oncology, Inc. | Small molecule drug conjugates of gemcitabine monophosphate |
| JP2021535395A (ja) * | 2018-08-28 | 2021-12-16 | エッセンリックス コーポレーション | アッセイ精度向上 |
| US11224610B2 (en) * | 2018-09-19 | 2022-01-18 | Otsuka Pharmaceutical Co., Ltd. | Low dose combination CDA substrate drug/cedazuridine with extended administration |
| CN112888700B (zh) * | 2018-10-19 | 2025-03-04 | 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 |
| JP7433662B2 (ja) | 2018-10-19 | 2024-02-20 | インターオリゴ・コーポレイション | 治療効能を改善した核酸変形体及びそれを含む抗癌用薬学組成物 |
| US12187757B2 (en) * | 2019-10-08 | 2025-01-07 | Otsuka Pharmaceutical Co., Ltd. | 2′-deoxy-2′,2′-difluorotetrahydrouridines with high purity and methods of making the same |
| IL294288A (en) * | 2020-02-25 | 2022-08-01 | Otsuka Pharma Co Ltd | Solid oral dosage forms in combination with decitabine and cadazuridine |
| AU2022244240A1 (en) * | 2021-03-26 | 2023-10-05 | 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 |
| AU2022370354A1 (en) | 2021-10-19 | 2024-05-30 | 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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| WO2008085611A2 (en) * | 2006-11-27 | 2008-07-17 | University Of Miami | Designer theraphy of pancreatic tumors |
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| JO3262B1 (ar) | 2009-04-06 | 2018-09-16 | Otsuka Pharma Co Ltd | توليفة من ديسيتابين مع مثبط سيتيدين دي أميناز واستخدامها في علاج السرطان |
| JP5684787B2 (ja) | 2009-04-06 | 2015-03-18 | 大塚製薬株式会社 | シチジンベースの抗新生物薬とシチジンデアミナーゼ阻害薬との組合せ、および癌の治療におけるその使用 |
| US8609631B2 (en) | 2009-04-06 | 2013-12-17 | Eisai Inc. | Compositions and methods for treating cancer |
-
2008
- 2008-10-14 JO JO2008459A patent/JO2778B1/en active
- 2008-10-15 TW TW097139594A patent/TWI445539B/zh active
- 2008-10-16 WO PCT/US2008/080163 patent/WO2009052287A1/en not_active Ceased
- 2008-10-16 AT AT08840633T patent/ATE548374T1/de active
- 2008-10-16 ES ES12151552.2T patent/ES2616566T3/es active Active
- 2008-10-16 ME MEP-2010-68A patent/ME00997B/me unknown
- 2008-10-16 KR KR1020107010621A patent/KR101543049B1/ko active Active
- 2008-10-16 MX MX2010004109A patent/MX2010004109A/es active IP Right Grant
- 2008-10-16 EP EP12151552.2A patent/EP2447272B1/en active Active
- 2008-10-16 PT PT08840633T patent/PT2207786E/pt unknown
- 2008-10-16 JP JP2010530110A patent/JP5496899B2/ja active Active
- 2008-10-16 ES ES08840633T patent/ES2384011T3/es active Active
- 2008-10-16 BR BRPI0818672A patent/BRPI0818672B8/pt active IP Right Grant
- 2008-10-16 PL PL08840633T patent/PL2207786T3/pl 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 |
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| 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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