EA201891391A1 - Диастереоселективный синтез фосфатных производных и пролекарства гемцитабина nuc-1031 - Google Patents

Диастереоселективный синтез фосфатных производных и пролекарства гемцитабина nuc-1031

Info

Publication number
EA201891391A1
EA201891391A1 EA201891391A EA201891391A EA201891391A1 EA 201891391 A1 EA201891391 A1 EA 201891391A1 EA 201891391 A EA201891391 A EA 201891391A EA 201891391 A EA201891391 A EA 201891391A EA 201891391 A1 EA201891391 A1 EA 201891391A1
Authority
EA
Eurasian Patent Office
Prior art keywords
synthesis
hemicitabin
diastereocelective
nuc
protection
Prior art date
Application number
EA201891391A
Other languages
English (en)
Other versions
EA038658B1 (ru
Inventor
Мани Бушан Котала
Венката Лакшми Нарасимха Рао Даммалапати
Original Assignee
НУКАНА ПиЭлСи
Лаурус Лэбз Прайвет Лтд
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
Priority claimed from GBGB1602185.9A external-priority patent/GB201602185D0/en
Application filed by НУКАНА ПиЭлСи, Лаурус Лэбз Прайвет Лтд filed Critical НУКАНА ПиЭлСи
Publication of EA201891391A1 publication Critical patent/EA201891391A1/ru
Publication of EA038658B1 publication Critical patent/EA038658B1/ru

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H1/00—Processes for the preparation of sugar derivatives
    • C07H1/02—Phosphorylation
    • 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
    • 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
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/06—Phosphorus compounds without P—C bonds
    • C07F9/22—Amides of acids of phosphorus
    • C07F9/222—Amides of phosphoric acids
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/06—Phosphorus compounds without P—C bonds
    • C07F9/22—Amides of acids of phosphorus
    • C07F9/24—Esteramides
    • 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
    • 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
    • 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
    • C07B2200/07—Optical isomers
    • 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
    • Y02P20/55—Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Biochemistry (AREA)
  • Molecular Biology (AREA)
  • Engineering & Computer Science (AREA)
  • Biotechnology (AREA)
  • Genetics & Genomics (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)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Saccharide Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Preparation Of Compounds By Using Micro-Organisms (AREA)

Abstract

Настоящее изобретение предоставляет способ получения промежуточных соединений, полезных при синтезе гемцитабин[фенил(бензокси-L-аланинил)]фосфата. Также предоставлен способ получения гемцитабин[фенил(бензокси-L-аланинил)]фосфата.
EA201891391A 2015-12-11 2016-12-09 Способ получения пролекарства гемцитабина nuc-1031 с использованием диастереоселективного обогащения промежуточных фосфатных производных EA038658B1 (ru)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
IN6635CH2015 2015-12-11
GBGB1602185.9A GB201602185D0 (en) 2016-02-08 2016-02-08 Diastereoselective synthesis of phosphate derivatives
PCT/GB2016/053875 WO2017098252A1 (en) 2015-12-11 2016-12-09 Diastereoselective synthesis of phosphate derivatives and of the gemcitabine prodrug nuc-1031

Publications (2)

Publication Number Publication Date
EA201891391A1 true EA201891391A1 (ru) 2019-02-28
EA038658B1 EA038658B1 (ru) 2021-09-30

Family

ID=57570086

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201891391A EA038658B1 (ru) 2015-12-11 2016-12-09 Способ получения пролекарства гемцитабина nuc-1031 с использованием диастереоселективного обогащения промежуточных фосфатных производных

Country Status (28)

Country Link
US (2) US10774104B2 (ru)
EP (2) EP3386998B1 (ru)
JP (1) JP6889180B2 (ru)
KR (1) KR20180101370A (ru)
CN (2) CN108779136B (ru)
AU (1) AU2016367237B2 (ru)
BR (1) BR112018011695A2 (ru)
CA (1) CA3007347C (ru)
CL (1) CL2018001541A1 (ru)
CY (1) CY1124809T1 (ru)
EA (1) EA038658B1 (ru)
ES (1) ES2898890T3 (ru)
HR (1) HRP20211812T1 (ru)
HU (1) HUE059026T2 (ru)
IL (1) IL259887B (ru)
LT (1) LT3386998T (ru)
MA (1) MA43405B1 (ru)
MD (1) MD3386998T2 (ru)
MX (1) MX2018007083A (ru)
MY (1) MY196772A (ru)
PH (1) PH12018501224A1 (ru)
PL (1) PL3386998T3 (ru)
PT (1) PT3386998T (ru)
RS (1) RS62593B1 (ru)
SA (1) SA518391776B1 (ru)
SG (1) SG11201804774YA (ru)
SI (1) SI3386998T1 (ru)
WO (1) WO2017098252A1 (ru)

Families Citing this family (10)

* 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
NZ708177A (en) 2012-11-16 2017-08-25 Univ College Cardiff Consultants Ltd Process for preparing nucleoside prodrugs
KR102421929B1 (ko) 2014-06-25 2022-07-15 뉴카나 피엘씨 젬시타빈-전구 약물 함유 제제
SG11201608808TA (en) 2014-06-25 2016-11-29 Nucana Biomed Ltd Gemcitabine prodrugs
GB201417644D0 (en) 2014-10-06 2014-11-19 Nucana Biomed Ltd Method of separating phosphate diastereoisomers
JP7038653B2 (ja) 2015-10-05 2022-03-18 ニューカナ パブリック リミテッド カンパニー 併用療法
BR112018011695A2 (pt) 2015-12-11 2018-11-27 Laurus Labs Private Ltd síntese diastereosseletiva de derivados fosfato e do pró-fármaco de gencitabina nuc-1031
GB201522771D0 (en) 2015-12-23 2016-02-03 Nucana Biomed Ltd Crystalline form of a phosphate derivative
GB201709471D0 (en) * 2017-06-14 2017-07-26 Nucana Biomed Ltd Diastereoselective synthesis of hosphate derivatives
CN114644651A (zh) * 2022-04-13 2022-06-21 中国人民解放军军事科学院军事医学研究院 芳氧基磷酰化氨基酸酯化合物的制备方法

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US4526988A (en) 1983-03-10 1985-07-02 Eli Lilly And Company Difluoro antivirals and intermediate therefor
GB0317009D0 (en) * 2003-07-21 2003-08-27 Univ Cardiff Chemical compounds
TWI576352B (zh) * 2009-05-20 2017-04-01 基利法瑪席特有限責任公司 核苷磷醯胺
US8618076B2 (en) * 2009-05-20 2013-12-31 Gilead Pharmasset Llc Nucleoside phosphoramidates
JP2013527145A (ja) * 2010-03-31 2013-06-27 ギリード・ファーマセット・エルエルシー リン含有活性化剤の立体選択的合成
KR101995598B1 (ko) 2010-07-19 2019-07-02 길리애드 사이언시즈, 인코포레이티드 부분입체 이성질성으로 순수한 포스포라미데이트 전구약물의 제조 방법
AR084044A1 (es) 2010-11-30 2013-04-17 Pharmasset Inc Compuestos 2’-espiro-nucleosidos
US20130143835A1 (en) * 2011-12-05 2013-06-06 Medivir Ab HCV Polymerase Inhibitors
WO2013187978A1 (en) 2012-06-16 2013-12-19 Nanjing Molecular Research, Inc. Double-liver-targeting phosphoramidate and phosphonoamidate prodrugs
NZ708177A (en) 2012-11-16 2017-08-25 Univ College Cardiff Consultants Ltd Process for preparing nucleoside prodrugs
SG11201608808TA (en) 2014-06-25 2016-11-29 Nucana Biomed Ltd Gemcitabine prodrugs
KR102421929B1 (ko) 2014-06-25 2022-07-15 뉴카나 피엘씨 젬시타빈-전구 약물 함유 제제
ES2830784T3 (es) 2014-07-22 2021-06-04 NuCana plc Proceso para la preparación de gemcitabina-[fenil(benzoxi-L-alanil)]fosfato
MX369649B (es) * 2014-08-25 2019-11-15 Medivir Ab Analogos de dioxolano de uridina para el tratamiento del cancer.
GB201417644D0 (en) 2014-10-06 2014-11-19 Nucana Biomed Ltd Method of separating phosphate diastereoisomers
HUE038541T2 (hu) 2015-05-14 2018-10-29 NuCana plc Rák kezelési módszerek
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
CN106539810B (zh) 2015-09-16 2021-03-09 济南高合医疗科技有限公司 一种富集了nuc-1031单一异构体的组合物及其制备方法和用途
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
JP7038653B2 (ja) 2015-10-05 2022-03-18 ニューカナ パブリック リミテッド カンパニー 併用療法
BR112018011695A2 (pt) 2015-12-11 2018-11-27 Laurus Labs Private Ltd síntese diastereosseletiva de derivados fosfato e do pró-fármaco de gencitabina nuc-1031
CA3008769A1 (en) 2015-12-23 2017-06-29 NuCana plc Combination therapy comprising nuc-1031 and cisplatin
SI3393478T1 (sl) 2015-12-23 2020-07-31 NuCana plc Kombinacijska terapija
GB201522771D0 (en) 2015-12-23 2016-02-03 Nucana Biomed Ltd Crystalline form of a phosphate derivative
GB201709471D0 (en) 2017-06-14 2017-07-26 Nucana Biomed Ltd Diastereoselective synthesis of hosphate derivatives

Also Published As

Publication number Publication date
BR112018011695A2 (pt) 2018-11-27
MX2018007083A (es) 2019-02-20
CA3007347C (en) 2020-08-04
AU2016367237A1 (en) 2018-07-05
CN115746073A (zh) 2023-03-07
CA3007347A1 (en) 2017-06-15
US20180362571A1 (en) 2018-12-20
JP6889180B2 (ja) 2021-06-18
PT3386998T (pt) 2021-11-30
IL259887B (en) 2020-09-30
SG11201804774YA (en) 2018-07-30
SI3386998T1 (sl) 2022-02-28
CN108779136A (zh) 2018-11-09
EP3386998B1 (en) 2021-11-10
CY1124809T1 (el) 2022-11-25
MD3386998T2 (ro) 2022-03-31
ES2898890T3 (es) 2022-03-09
AU2016367237B2 (en) 2020-12-24
CL2018001541A1 (es) 2019-02-01
KR20180101370A (ko) 2018-09-12
CN108779136B (zh) 2022-07-08
US10774104B2 (en) 2020-09-15
HRP20211812T1 (hr) 2022-03-04
LT3386998T (lt) 2022-01-25
US11603382B2 (en) 2023-03-14
EP4011896A1 (en) 2022-06-15
EP3386998A1 (en) 2018-10-17
MY196772A (en) 2023-05-03
PH12018501224A1 (en) 2019-01-28
MA43405A (fr) 2021-03-17
PL3386998T3 (pl) 2022-02-07
RS62593B1 (sr) 2021-12-31
JP2019500420A (ja) 2019-01-10
EA038658B1 (ru) 2021-09-30
SA518391776B1 (ar) 2022-01-13
IL259887A (en) 2018-07-31
MA43405B1 (fr) 2021-11-30
WO2017098252A1 (en) 2017-06-15
HUE059026T2 (hu) 2022-10-28
US20210009625A1 (en) 2021-01-14

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