EA201790794A1 - Способы разделения диастереоизомеров фосфата гемцитабина - Google Patents

Способы разделения диастереоизомеров фосфата гемцитабина

Info

Publication number
EA201790794A1
EA201790794A1 EA201790794A EA201790794A EA201790794A1 EA 201790794 A1 EA201790794 A1 EA 201790794A1 EA 201790794 A EA201790794 A EA 201790794A EA 201790794 A EA201790794 A EA 201790794A EA 201790794 A1 EA201790794 A1 EA 201790794A1
Authority
EA
Eurasian Patent Office
Prior art keywords
phosphate
separation
diastereoisomers
hemcitabin
methods
Prior art date
Application number
EA201790794A
Other languages
English (en)
Other versions
EA033118B1 (ru
Inventor
Хью Гриффит
Original Assignee
Нукана Байомед Лимитед
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 Нукана Байомед Лимитед filed Critical Нукана Байомед Лимитед
Publication of EA201790794A1 publication Critical patent/EA201790794A1/ru
Publication of EA033118B1 publication Critical patent/EA033118B1/ru

Links

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
    • C07H19/06—Pyrimidine radicals
    • C07H19/10—Pyrimidine 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
    • 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
    • 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

Landscapes

  • 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)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Saccharide Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Preparation Of Compounds By Using Micro-Organisms (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Abstract

Настоящая заявка относится к способу разделения фосфатных диастереоизомеров гемцитабин[фенилбензокси-L-аланинил)]фосфата (NUC-1031) с использованием кристаллизации. В частности, путем кристаллизации из изопропилового спирта получается гемцитабин[фенилбензокси-L-аланинил)]-(S)-фосфат в диастереоизомерно высокочистой форме. Настоящая заявка также относится к кристаллической форме гемцитабин[фенилбензокси-L-аланинил)]-(S)-фосфата.
EA201790794A 2014-10-06 2015-09-29 Способы разделения диастереоизомеров фосфата гемцитабина EA033118B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
GBGB1417644.0A GB201417644D0 (en) 2014-10-06 2014-10-06 Method of separating phosphate diastereoisomers
PCT/GB2015/052839 WO2016055769A1 (en) 2014-10-06 2015-09-29 Methods of separating gemcitabine-phosphate diastereoisomers

Publications (2)

Publication Number Publication Date
EA201790794A1 true EA201790794A1 (ru) 2017-07-31
EA033118B1 EA033118B1 (ru) 2019-08-30

Family

ID=51946917

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201790794A EA033118B1 (ru) 2014-10-06 2015-09-29 Способы разделения диастереоизомеров фосфата гемцитабина

Country Status (29)

Country Link
US (1) US10669300B2 (ru)
EP (2) EP3204398B1 (ru)
JP (2) JP6893172B2 (ru)
KR (1) KR102532498B1 (ru)
CN (2) CN107108682B (ru)
AU (2) AU2015329767B2 (ru)
CA (1) CA2959977C (ru)
CL (1) CL2017000819A1 (ru)
CY (1) CY1123061T1 (ru)
DK (1) DK3204398T3 (ru)
EA (1) EA033118B1 (ru)
ES (1) ES2793957T3 (ru)
GB (1) GB201417644D0 (ru)
HR (1) HRP20200849T1 (ru)
HU (1) HUE050882T2 (ru)
IL (1) IL251125B (ru)
LT (1) LT3204398T (ru)
MA (1) MA41039B1 (ru)
ME (1) ME03730B (ru)
MX (2) MX2017004446A (ru)
MY (1) MY183302A (ru)
PH (1) PH12017500586A1 (ru)
PL (1) PL3204398T3 (ru)
PT (1) PT3204398T (ru)
RS (1) RS60634B1 (ru)
SG (2) SG10201902952SA (ru)
SI (1) SI3204398T1 (ru)
WO (1) WO2016055769A1 (ru)
ZA (1) ZA201701723B (ru)

Families Citing this family (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB0317009D0 (en) * 2003-07-21 2003-08-27 Univ Cardiff Chemical compounds
PT3150616T (pt) 2012-11-16 2017-06-09 Univ College Cardiff Consultants Ltd Mistura de rp/sp gencitabina-[fenil-(benziloxi-l-alaninil)]-fosfato
WO2015198058A1 (en) 2014-06-25 2015-12-30 Nucana Biomed Limited Gemcitabine prodrugs
ES2655820T3 (es) 2014-06-25 2018-02-21 NuCana plc Formulación que comprende un profármaco de gemcitabina
GB201417644D0 (en) 2014-10-06 2014-11-19 Nucana Biomed Ltd Method of separating phosphate diastereoisomers
CN106543220A (zh) * 2015-09-16 2017-03-29 博瑞生物医药（苏州）股份有限公司 氨基磷酸酯化合物及其制备方法和晶体
CN106478753A (zh) * 2015-09-16 2017-03-08 博瑞生物医药（苏州）股份有限公司 一种nuc‑1031单一异构体的制备方法和用途
CN106543252A (zh) * 2015-09-16 2017-03-29 博瑞生物医药（苏州）股份有限公司 核苷氨基磷酸酯类前药的制备方法及其中间体
WO2017060661A1 (en) 2015-10-05 2017-04-13 Nucana Biomed Limited Combination therapy
WO2017098252A1 (en) 2015-12-11 2017-06-15 Nucana Biomed Limited Diastereoselective synthesis of phosphate derivatives and of the gemcitabine prodrug nuc-1031
GB201522771D0 (en) 2015-12-23 2016-02-03 Nucana Biomed Ltd Crystalline form of a phosphate derivative
WO2018019188A1 (zh) * 2016-07-23 2018-02-01 博瑞生物医药（苏州）股份有限公司 核苷氨基磷酸酯类前药的多晶型及其制备方法
GB201709471D0 (en) 2017-06-14 2017-07-26 Nucana Biomed Ltd Diastereoselective synthesis of hosphate derivatives
CN107400156B (zh) * 2017-09-19 2020-01-31 北京大学 一种分离麦角甾烷型三萜25r-与25s-差向异构体的方法
CN115028594A (zh) * 2020-06-03 2022-09-09 吴卫东 恩替他滨药用前体化合物及其制备方法和医学用途

Family Cites Families (16)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1254092B1 (en) * 2000-02-11 2004-01-21 Degussa AG Resolution of dl-racemic mixtures
GB0317009D0 (en) * 2003-07-21 2003-08-27 Univ Cardiff Chemical compounds
FR2954310B1 (fr) * 2009-12-18 2014-07-25 Univ Rouen Procede de dedoublement d'enantiomeres par evapocristallisation preferentielle
PT3150616T (pt) * 2012-11-16 2017-06-09 Univ College Cardiff Consultants Ltd Mistura de rp/sp gencitabina-[fenil-(benziloxi-l-alaninil)]-fosfato
WO2014204856A1 (en) 2013-06-17 2014-12-24 Catabasis Pharmaceuticals, Inc. Fatty acid anticancer derivatives and their uses
MX2016006919A (es) * 2013-11-27 2016-08-17 Idenix Pharmaceuticals Llc Nucleotidos para el tratamiento de cancer de higado.
ES2655820T3 (es) * 2014-06-25 2018-02-21 NuCana plc Formulación que comprende un profármaco de gemcitabina
WO2015198058A1 (en) 2014-06-25 2015-12-30 Nucana Biomed Limited Gemcitabine prodrugs
ES2830784T3 (es) 2014-07-22 2021-06-04 NuCana plc Proceso para la preparación de gemcitabina-[fenil(benzoxi-L-alanil)]fosfato
GB201417644D0 (en) 2014-10-06 2014-11-19 Nucana Biomed Ltd Method of separating phosphate diastereoisomers
KR20180021697A (ko) 2015-05-14 2018-03-05 뉴카나 피엘씨 암 치료
WO2017060661A1 (en) 2015-10-05 2017-04-13 Nucana Biomed Limited Combination therapy
WO2017098252A1 (en) 2015-12-11 2017-06-15 Nucana Biomed Limited Diastereoselective synthesis of phosphate derivatives and of the gemcitabine prodrug nuc-1031
RS60211B1 (sr) 2015-12-23 2020-06-30 NuCana plc Kombinovana terapija
CA3008769A1 (en) 2015-12-23 2017-06-29 NuCana plc Combination therapy comprising nuc-1031 and cisplatin
GB201522771D0 (en) 2015-12-23 2016-02-03 Nucana Biomed Ltd Crystalline form of a phosphate derivative

Also Published As

Publication number Publication date
CN107108682A (zh) 2017-08-29
SG11201701885UA (en) 2017-04-27
ES2793957T3 (es) 2020-11-17
IL251125A0 (en) 2017-04-30
PL3204398T3 (pl) 2020-11-16
BR112017006855A2 (pt) 2017-12-12
LT3204398T (lt) 2020-09-10
MY183302A (en) 2021-02-18
CY1123061T1 (el) 2021-10-29
WO2016055769A1 (en) 2016-04-14
US20170226147A1 (en) 2017-08-10
DK3204398T3 (da) 2020-06-02
US10669300B2 (en) 2020-06-02
SG10201902952SA (en) 2019-05-30
HRP20200849T1 (hr) 2020-10-30
AU2015329767B2 (en) 2020-03-12
CN107108682B (zh) 2020-12-18
IL251125B (en) 2020-07-30
KR102532498B1 (ko) 2023-05-12
GB201417644D0 (en) 2014-11-19
CA2959977A1 (en) 2016-04-14
AU2015329767A1 (en) 2017-04-13
SI3204398T1 (sl) 2020-09-30
EA033118B1 (ru) 2019-08-30
MA41039B1 (fr) 2020-08-31
ME03730B (me) 2021-01-20
AU2020203714A1 (en) 2020-06-25
CL2017000819A1 (es) 2017-11-03
MX2017004446A (es) 2017-06-19
EP3204398B1 (en) 2020-05-13
JP2020128392A (ja) 2020-08-27
PT3204398T (pt) 2020-05-28
ZA201701723B (en) 2023-11-29
JP2017530172A (ja) 2017-10-12
EP3725794A1 (en) 2020-10-21
JP6967625B2 (ja) 2021-11-17
EP3204398A1 (en) 2017-08-16
JP6893172B2 (ja) 2021-06-23
MX2020003758A (es) 2021-10-26
PH12017500586A1 (en) 2017-08-30
HUE050882T2 (hu) 2021-01-28
CN112552362A (zh) 2021-03-26
CA2959977C (en) 2024-01-02
AU2020203714B2 (en) 2021-07-22
RS60634B1 (sr) 2020-09-30
KR20170090413A (ko) 2017-08-07

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