CN107922456A - 磷酸氟达拉滨的晶型及其制备方法和用途 - Google Patents

磷酸氟达拉滨的晶型及其制备方法和用途 Download PDF

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Publication number
CN107922456A
CN107922456A CN201680048187.XA CN201680048187A CN107922456A CN 107922456 A CN107922456 A CN 107922456A CN 201680048187 A CN201680048187 A CN 201680048187A CN 107922456 A CN107922456 A CN 107922456A
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CN
China
Prior art keywords
crystal form
fluoroadenine
furanose
phosphate
fludarabine phosphate
Prior art date
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Pending
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CN201680048187.XA
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English (en)
Inventor
杨志清
张亮
张相洋
施珍娟
苏迪
骆红英
傅德进
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Zhejiang Hisun Pharmaceutical Co Ltd
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Zhejiang Hisun Pharmaceutical Co Ltd
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Publication date
Application filed by Zhejiang Hisun Pharmaceutical Co Ltd filed Critical Zhejiang Hisun Pharmaceutical Co Ltd
Publication of CN107922456A publication Critical patent/CN107922456A/zh
Pending legal-status Critical Current

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    • 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
    • C07H19/16—Purine radicals
    • C07H19/20—Purine radicals with the saccharide radical esterified by phosphoric or polyphosphoric acids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • 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
    • 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)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Biochemistry (AREA)
  • Biotechnology (AREA)
  • Genetics & Genomics (AREA)
  • Molecular Biology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Saccharide Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

提供一种磷酸氟达拉滨的新晶型及其制备方法、含有其的药物组合物及其制药用途。所述磷酸氟达拉滨的晶型I和II在溶解性、溶解速度、化学稳定性和加工适应性方面具有优异的性质。

Description

PCT国内申请，说明书已公开。

Claims (14)

  1. PCT国内申请，权利要求书已公开。
CN201680048187.XA 2015-08-28 2016-08-26 磷酸氟达拉滨的晶型及其制备方法和用途 Pending CN107922456A (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
CN201510540739 2015-08-28
CN2015105407396 2015-08-28
PCT/CN2016/096878 WO2017036356A1 (zh) 2015-08-28 2016-08-26 磷酸氟达拉滨的晶型及其制备方法和用途

Publications (1)

Publication Number Publication Date
CN107922456A true CN107922456A (zh) 2018-04-17

Family

ID=58186667

Family Applications (1)

Application Number Title Priority Date Filing Date
CN201680048187.XA Pending CN107922456A (zh) 2015-08-28 2016-08-26 磷酸氟达拉滨的晶型及其制备方法和用途

Country Status (4)

Country Link
US (1) US10669302B2 (zh)
EP (1) EP3342778B1 (zh)
CN (1) CN107922456A (zh)
WO (1) WO2017036356A1 (zh)

Citations (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5296589A (en) * 1989-12-04 1994-03-22 Ash Stevens, Inc. Hydrogenation of 2-fluoro-9-(2,3,5-tri-o-benzyl-beta-D-arabinofuranosyl)adenine
US6046322A (en) * 1997-12-11 2000-04-04 Schering Aktiengesellschaft Process for the production of fludarabine-phosphate lithium, sodium, potassium, calcium and magnesium salts and purification process for the production of fludarabine-phosphate and fludarabine-phosphate with a purity of at least 99.5%
WO2004087939A1 (en) * 2003-04-03 2004-10-14 Pro.Bio.Sint. S.P.A. A process for the preparation of fludarabine phosphate from 2-fluoroadenine and fludarabine phosphate salts with amines or ammonia
CN1867575A (zh) * 2003-10-15 2006-11-22 阿多凯姆技术有限公司 氟达拉滨磷酸酯的制备方法
WO2007144168A1 (en) * 2006-06-15 2007-12-21 Adorkem Technology Spa Enzymatic process for preparation of 5'-monophosphate-nucleotides
CN103040855A (zh) * 2012-12-28 2013-04-17 海南锦瑞制药股份有限公司 一种磷酸氟达拉滨的药物组合物及其制备方法
CN104592337A (zh) * 2013-10-31 2015-05-06 山东新时代药业有限公司 一种9-β-D-阿拉伯呋喃糖基-2-氟代腺嘌呤-5’-磷酸酯的制备方法

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE10164510A1 (de) * 2001-12-20 2003-07-10 Schering Ag Orale Fludara reinst Formulierung mit schneller Freisetzung des Wirkstoffes
US8962614B2 (en) * 2008-04-17 2015-02-24 The Johns Hopkins University ON01910.Na enhances chemotherapeutic agent activity in drug-resistant tumors

Patent Citations (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5296589A (en) * 1989-12-04 1994-03-22 Ash Stevens, Inc. Hydrogenation of 2-fluoro-9-(2,3,5-tri-o-benzyl-beta-D-arabinofuranosyl)adenine
US6046322A (en) * 1997-12-11 2000-04-04 Schering Aktiengesellschaft Process for the production of fludarabine-phosphate lithium, sodium, potassium, calcium and magnesium salts and purification process for the production of fludarabine-phosphate and fludarabine-phosphate with a purity of at least 99.5%
WO2004087939A1 (en) * 2003-04-03 2004-10-14 Pro.Bio.Sint. S.P.A. A process for the preparation of fludarabine phosphate from 2-fluoroadenine and fludarabine phosphate salts with amines or ammonia
CN1867575A (zh) * 2003-10-15 2006-11-22 阿多凯姆技术有限公司 氟达拉滨磷酸酯的制备方法
WO2007144168A1 (en) * 2006-06-15 2007-12-21 Adorkem Technology Spa Enzymatic process for preparation of 5'-monophosphate-nucleotides
CN103040855A (zh) * 2012-12-28 2013-04-17 海南锦瑞制药股份有限公司 一种磷酸氟达拉滨的药物组合物及其制备方法
CN104592337A (zh) * 2013-10-31 2015-05-06 山东新时代药业有限公司 一种9-β-D-阿拉伯呋喃糖基-2-氟代腺嘌呤-5’-磷酸酯的制备方法

Also Published As

Publication number Publication date
EP3342778A4 (en) 2019-05-29
US20190112327A2 (en) 2019-04-18
US10669302B2 (en) 2020-06-02
EP3342778B1 (en) 2022-01-12
EP3342778A1 (en) 2018-07-04
US20180244711A1 (en) 2018-08-30
WO2017036356A1 (zh) 2017-03-09

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