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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
fludarabine phosphate
ray powder
phosphate
powder diffraction
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Pending
Application number
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
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Zhejiang Hisun Pharmaceutical Co Ltd
Original Assignee
Zhejiang Hisun Pharmaceutical Co Ltd
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
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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Classifications

    • 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
CN2015105407396 2015-08-28
CN201510540739 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
NZ588749A (en) * 2008-04-17 2012-06-29 Univ Johns Hopkins 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
EP3342778B1 (en) 2022-01-12
US20180244711A1 (en) 2018-08-30
US10669302B2 (en) 2020-06-02
WO2017036356A1 (zh) 2017-03-09
US20190112327A2 (en) 2019-04-18
EP3342778A1 (en) 2018-07-04

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Application publication date: 20180417