JP6289361B2 - ５−アザシチジンの合成 - Google Patents

５−アザシチジンの合成 Download PDF

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Publication number
JP6289361B2
JP6289361B2 JP2014502770A JP2014502770A JP6289361B2 JP 6289361 B2 JP6289361 B2 JP 6289361B2 JP 2014502770 A JP2014502770 A JP 2014502770A JP 2014502770 A JP2014502770 A JP 2014502770A JP 6289361 B2 JP6289361 B2 JP 6289361B2
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azacytidine
less
reaction
acid
hours
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JP2014510755A5 (https=
JP2014510755A (ja
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ラジェンドイラン チンナピルルアイ
ラジェンドイラン チンナピルルアイ
ナガラジャン ペリヤンドイ
ナガラジャン ペリヤンドイ
ベンカテスワルルアウ ジャストイ
ベンカテスワルルアウ ジャストイ
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セルジーン インターナショナル サルル
セルジーン インターナショナル サルル
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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
    • 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
    • C07H19/12—Triazine radicals
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • 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
    • C07H1/00—Processes for the preparation of sugar derivatives
    • C07H1/06—Separation; Purification
    • 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
    • Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00—Technologies relating to chemical industry
    • Y02P20/50—Improvements relating to the production of bulk chemicals
    • Y02P20/582—Recycling of unreacted starting or intermediate materials

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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)
  • Engineering & Computer Science (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Biotechnology (AREA)
  • Genetics & Genomics (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Hematology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Oncology (AREA)
  • Diabetes (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Saccharide Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Plural Heterocyclic Compounds (AREA)
JP2014502770A 2011-03-31 2012-03-29 ５−アザシチジンの合成 Active JP6289361B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201161470392P 2011-03-31 2011-03-31
US61/470,392 2011-03-31
PCT/US2012/031059 WO2012135405A1 (en) 2011-03-31 2012-03-29 Systhesis of 5-azacytidine

Publications (3)

Publication Number Publication Date
JP2014510755A JP2014510755A (ja) 2014-05-01
JP2014510755A5 JP2014510755A5 (https=) 2015-05-07
JP6289361B2 true JP6289361B2 (ja) 2018-03-07

Family

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Family Applications (1)

Application Number Title Priority Date Filing Date
JP2014502770A Active JP6289361B2 (ja) 2011-03-31 2012-03-29 ５−アザシチジンの合成

Country Status (13)

Country Link
US (1) US9951098B2 (https=)
EP (1) EP2691408B1 (https=)
JP (1) JP6289361B2 (https=)
KR (1) KR20140019820A (https=)
CN (1) CN103619864A (https=)
AU (1) AU2012236476A1 (https=)
BR (1) BR112013025167A2 (https=)
IL (1) IL228604A0 (https=)
MX (1) MX2013010945A (https=)
RU (1) RU2013148580A (https=)
SG (1) SG193622A1 (https=)
WO (1) WO2012135405A1 (https=)
ZA (1) ZA201307142B (https=)

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EP3782612B1 (en) 2008-05-15 2023-11-08 Celgene Corporation Oral formulations of cytidine analogs and methods of use thereof
WO2012106299A1 (en) 2011-01-31 2012-08-09 Celgene Corporation Pharmaceutical compositions of cytidine analogs and methods of use thereof
US9968627B2 (en) 2013-03-26 2018-05-15 Celgene Corporation Solid forms comprising 4-amino-1-β-D-ribofuranosyl-1,3,5-triazin-2(1H)-one and a coformer, compositions and methods of use thereof
WO2014169216A2 (en) 2013-04-11 2014-10-16 Carnegie Mellon University TEMPLATE-DIRECTED γPNA SYNTHESIS AND γPNA TARGETING COMPOUNDS
WO2014169206A2 (en) 2013-04-11 2014-10-16 Carnegie Mellon University Divalent nucleobase compounds and uses therefor
CN103450303A (zh) * 2013-09-04 2013-12-18 重庆泰濠制药有限公司 阿扎胞苷晶型a、阿扎胞苷晶型b及其制备方法
CN104672289A (zh) * 2013-11-29 2015-06-03 南京圣和药业股份有限公司 一种阿扎胞苷杂质的制备方法
WO2017183215A1 (ja) * 2016-04-21 2017-10-26 大原薬品工業株式会社 ５－アザシチジン類の糖部シリルエーテル誘導体
CN114907272A (zh) 2016-09-26 2022-08-16 卡耐基梅隆大学 二价核碱基化合物及其用途
CN109305992A (zh) * 2017-07-28 2019-02-05 江苏先声药业有限公司 一种阿扎胞苷的制备方法
CN109988207B (zh) * 2017-12-29 2022-01-04 江苏豪森药业集团有限公司 阿扎胞苷晶型的制备方法
CN110092807A (zh) * 2018-01-30 2019-08-06 中国医学科学院药物研究所 一种高纯、低灼烧残渣的制备阿扎胞苷的方法
JP7017638B2 (ja) 2018-02-07 2022-02-08 ラブレス バイオメディカル リサーチ インスティテュート 吸入可能な乾燥粉末シチジン類似体組成物及び癌への治療として使用する方法
KR20190136284A (ko) * 2018-05-30 2019-12-10 주식회사 삼양바이오팜 안정한 아자시티딘-함유 약제학적 조성물의 제조방법
WO2022113069A1 (en) 2020-11-24 2022-06-02 Yissum Research Development Company Of The Hebrew University Of Jerusalem Ltd. E protein channel blockers and orf3 inhibitors as anti-covid-19 agents
BR112022022243A2 (pt) 2020-05-01 2022-12-20 Yissum Res Dev Co Of Hebrew Univ Jerusalem Ltd Bloqueadores do canal de proteína e e inibidores de orf3 como agentes anti-covid-19.
CN113201039B (zh) * 2021-05-19 2022-04-29 南京德克瑞医药化工有限公司 一种医药中间体2’,3’,5’-三乙酰阿扎胞苷的制备方法
AR134497A1 (es) 2023-11-28 2026-01-21 Sanofi Sa Combiterapia multifuncional con activador de los linfocitos citolíticos naturales (nk) para tratar trastornos neoplásicos hemáticos

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GB1050899A (https=) 1963-12-22
CH527207A (de) 1968-05-08 1972-08-31 Ceskoslovenska Akademie Ved Verfahren zur Herstellung von 1-Glycosyl-5-azacytosinen
CH507969A (de) 1968-11-12 1971-05-31 Ceskoslovenska Akademie Ved Verfahren zur Herstellung von 1-Glycosyl-5-azacytosinen
DE2012888C3 (de) 1970-03-14 1981-04-02 Schering Ag, 1000 Berlin Und 4619 Bergkamen Verfahren zur Herstellung von 5-Azapyrimidinnucleosiden
FR2123632A6 (en) 1971-01-26 1972-09-15 Ceskoslovenska Akademie Ved Prepn of 5-azacytosines and 5-azacytidines - from bis trimethylsilyl-5-azacytosine
DE2122991C2 (de) 1971-05-04 1982-06-09 Schering Ag, 1000 Berlin Und 4619 Bergkamen Verfahren zur Herstellung von Cytosin- und 6-Azacytosinnucleosiden
DE2508312A1 (de) 1975-02-24 1976-09-02 Schering Ag Neues verfahren zur herstellung von nucleosiden
DE2757365A1 (de) 1977-12-20 1979-06-21 Schering Ag Neues verfahren zur herstellung von nucleosiden
IL129126A0 (en) * 1996-10-16 2000-02-17 Icn Pharmaceuticals Monocyclic l-nucleosides analogs and uses thereof
AU2003278904A1 (en) 2002-09-24 2004-04-19 Kornis Pharmaceuticals, Incorporated 1, 3, 5-triazines for treatment of viral diseases
US7189740B2 (en) 2002-10-15 2007-03-13 Celgene Corporation Methods of using 3-(4-amino-oxo-1,3-dihydro-isoindol-2-yl)-piperidine-2,6-dione for the treatment and management of myelodysplastic syndromes
US6943249B2 (en) 2003-03-17 2005-09-13 Ash Stevens, Inc. Methods for isolating crystalline Form I of 5-azacytidine
US7038038B2 (en) 2003-03-17 2006-05-02 Pharmion Corporation Synthesis of 5-azacytidine
US6887855B2 (en) 2003-03-17 2005-05-03 Pharmion Corporation Forms of 5-azacytidine
CA2535889A1 (en) 2003-08-29 2005-03-17 Aton Pharma, Inc. Combination methods of treating cancer
US7192781B2 (en) 2004-04-13 2007-03-20 Pharmion Corporation Methods for stabilizing 5-azacytidine in plasma
US20060069060A1 (en) 2004-09-27 2006-03-30 Sanjeev Redkar Salts of decitabine
US20060063735A1 (en) 2004-09-17 2006-03-23 Supergen, Inc. Salts of 5-azacytidine
US20080057086A1 (en) 2006-09-01 2008-03-06 Pharmion Corporation Colon-targeted oral formulations of cytidine analogs
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US20110288042A1 (en) 2007-08-02 2011-11-24 Chemagis Ltd. Stable highly pure azacitidine and preparation methods therefor
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AR073003A1 (es) 2008-08-08 2010-10-06 Scinopharm Taiwan Ltd Proceso para preparar 5-azacitosina nucleosidos y sus derivados
US20110042247A1 (en) 2009-06-25 2011-02-24 Chandrasekhar Kocherlakota Formulations of azacitidine and its derivatives
IT1399195B1 (it) 2010-03-30 2013-04-11 Chemi Spa Processo per la sintesi di azacitidina e decitabina

Also Published As

Publication number Publication date
CN103619864A (zh) 2014-03-05
SG193622A1 (en) 2013-11-29
IL228604A0 (en) 2013-12-31
WO2012135405A1 (en) 2012-10-04
ZA201307142B (en) 2015-11-25
EP2691408B1 (en) 2017-06-28
EP2691408A1 (en) 2014-02-05
KR20140019820A (ko) 2014-02-17
BR112013025167A2 (pt) 2019-09-24
JP2014510755A (ja) 2014-05-01
RU2013148580A (ru) 2015-05-10
US20140128593A1 (en) 2014-05-08
US9951098B2 (en) 2018-04-24
MX2013010945A (es) 2014-03-12
AU2012236476A1 (en) 2013-05-02

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