KR20140019820A - 5-아자시티딘의 합성 - Google Patents

5-아자시티딘의 합성 Download PDF

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Publication number
KR20140019820A
KR20140019820A KR1020137028446A KR20137028446A KR20140019820A KR 20140019820 A KR20140019820 A KR 20140019820A KR 1020137028446 A KR1020137028446 A KR 1020137028446A KR 20137028446 A KR20137028446 A KR 20137028446A KR 20140019820 A KR20140019820 A KR 20140019820A
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South Korea
Prior art keywords
azacytidine
salt
acid
less
reaction
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KR1020137028446A
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English (en)
Korean (ko)
Inventor
킨나필라이 라젠디란
페리얀디 나가라잔
자스티 벤카테스왈라우
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셀진 인터내셔널 에스에이알엘
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Publication of KR20140019820A publication Critical patent/KR20140019820A/ko
Withdrawn legal-status Critical Current

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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)
KR1020137028446A 2011-03-31 2012-03-29 5-아자시티딘의 합성 Withdrawn KR20140019820A (ko)

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 (1)

Publication Number Publication Date
KR20140019820A true KR20140019820A (ko) 2014-02-17

Family

ID=46000343

Family Applications (1)

Application Number Title Priority Date Filing Date
KR1020137028446A Withdrawn KR20140019820A (ko) 2011-03-31 2012-03-29 5-아자시티딘의 합성

Country Status (13)

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

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PT2695609T (pt) 2008-05-15 2020-03-02 Celgene Corp Formulações orais de análogos da citidina e métodos de utilização dos mesmos
CA2825152A1 (en) 2011-01-31 2012-08-09 Celgene Corporation Pharmaceutical compositions of cytidine analogs and methods of use thereof
WO2014160698A1 (en) * 2013-03-26 2014-10-02 Celgene Corporation SOLID FORMS COMPRISING 4-AMINO-I-β-D-RIBOFURANOSYL-1,3,5-TRIAZIN-2(1H)-ONE AND A COFORMER, COMPOSITIONS AND METHODS OF USE THEREOF
US10221216B2 (en) 2013-04-11 2019-03-05 Carnegie Mellon University Template-directed γPNA synthesis process 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
CN109923105A (zh) 2016-09-26 2019-06-21 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
CA3211506A1 (en) 2018-02-07 2019-08-15 Lovelace Biomedical Research Institute Inhalable dry powder cytidine analogue composition and method of use as a treatment for cancer
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
KR20230035524A (ko) 2020-05-01 2023-03-14 이슘 리서치 디벨롭먼트 컴퍼니 오브 더 히브루 유니버시티 오브 예루살렘 엘티디. Covid-19 치료제로서 e 단백질 채널 차단제 및 orf3 억제제
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
US20250195653A1 (en) 2023-11-28 2025-06-19 Sanofi Multifunctional natural killer (nk) cell engager combination therapy for treating hematological neoplastic disorders

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GB1050899A (enExample) 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
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US6887855B2 (en) * 2003-03-17 2005-05-03 Pharmion Corporation Forms of 5-azacytidine
US6943249B2 (en) 2003-03-17 2005-09-13 Ash Stevens, Inc. Methods for isolating crystalline Form I of 5-azacytidine
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US20060069060A1 (en) 2004-09-27 2006-03-30 Sanjeev Redkar Salts of decitabine
WO2008028193A2 (en) 2006-09-01 2008-03-06 Pharmion Corporation Colon-targeted oral formulations of cytidine analogs
EP2118117A2 (en) 2007-01-11 2009-11-18 IVAX Pharmaceuticals s.r.o. Solid state forms of 5-azacytidine and processes for preparation thereof
US20110288042A1 (en) 2007-08-02 2011-11-24 Chemagis Ltd. Stable highly pure azacitidine and preparation methods therefor
EP2048151A1 (en) 2007-10-10 2009-04-15 Cilag AG Method for producing nucleosides by direct glycosylation of the nucleoside base
JP2011505336A (ja) 2007-11-01 2011-02-24 セルジーン コーポレイション 骨髄異形成症候群治療のためのシチジンアナログ
PT2695609T (pt) 2008-05-15 2020-03-02 Celgene Corp Formulações orais de análogos da citidina e métodos de utilização dos mesmos
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KR101660549B1 (ko) * 2008-08-08 2016-09-27 시노팜 타이완 리미티드 ５―아자시토신 뉴클레오시드 및 이의 유도체의 제조 방법
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
ZA201307142B (en) 2015-11-25
US20140128593A1 (en) 2014-05-08
IL228604A0 (en) 2013-12-31
MX2013010945A (es) 2014-03-12
CN103619864A (zh) 2014-03-05
RU2013148580A (ru) 2015-05-10
US9951098B2 (en) 2018-04-24
SG193622A1 (en) 2013-11-29
JP6289361B2 (ja) 2018-03-07
WO2012135405A1 (en) 2012-10-04
BR112013025167A2 (pt) 2019-09-24
EP2691408B1 (en) 2017-06-28
AU2012236476A1 (en) 2013-05-02
JP2014510755A (ja) 2014-05-01
EP2691408A1 (en) 2014-02-05

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Date Code Title Description
PA0105 International application

Patent event date: 20131028

Patent event code: PA01051R01D

Comment text: International Patent Application

PG1501 Laying open of application
PC1203 Withdrawal of no request for examination
WITN Application deemed withdrawn, e.g. because no request for examination was filed or no examination fee was paid