EA031106B1 - Диоксолановые аналоги уридина для лечения рака - Google Patents

Диоксолановые аналоги уридина для лечения рака Download PDF

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Publication number
EA031106B1
EA031106B1 EA201790328A EA201790328A EA031106B1 EA 031106 B1 EA031106 B1 EA 031106B1 EA 201790328 A EA201790328 A EA 201790328A EA 201790328 A EA201790328 A EA 201790328A EA 031106 B1 EA031106 B1 EA 031106B1
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EA
Eurasian Patent Office
Prior art keywords
mmol
alkyl
dia
mixture
compound
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EA201790328A
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English (en)
Russian (ru)
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EA201790328A1 (ru
Inventor
Рикард Бетель
Андеш Энерот
Бьерн Классон
Фредрик Эберг
Original Assignee
Медивир Аб
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Application filed by Медивир Аб filed Critical Медивир Аб
Publication of EA201790328A1 publication Critical patent/EA201790328A1/ru
Publication of EA031106B1 publication Critical patent/EA031106B1/ru

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02Phosphorus compounds
    • C07F9/547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6558Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system
    • C07F9/65586Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system at least one of the hetero rings does not contain nitrogen as ring hetero atom
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/04Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/66Phosphorus compounds
    • A61K31/665Phosphorus compounds having oxygen as a ring hetero atom, e.g. fosfomycin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/66Phosphorus compounds
    • A61K31/675Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02Phosphorus compounds
    • C07F9/06Phosphorus compounds without P—C bonds
    • C07F9/22Amides of acids of phosphorus
    • C07F9/24Esteramides

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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)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Biochemistry (AREA)
  • Molecular Biology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Plural Heterocyclic Compounds (AREA)
EA201790328A 2014-08-25 2015-08-24 Диоксолановые аналоги уридина для лечения рака EA031106B1 (ru)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
SE1450983 2014-08-25
SE1550858 2015-06-22
PCT/EP2015/069370 WO2016030335A1 (en) 2014-08-25 2015-08-24 Dioxolane analogues of uridine for the treatment of cancer

Publications (2)

Publication Number Publication Date
EA201790328A1 EA201790328A1 (ru) 2017-08-31
EA031106B1 true EA031106B1 (ru) 2018-11-30

Family

ID=54014804

Family Applications (2)

Application Number Title Priority Date Filing Date
EA201790328A EA031106B1 (ru) 2014-08-25 2015-08-24 Диоксолановые аналоги уридина для лечения рака
EA201890648A EA033300B1 (ru) 2014-08-25 2015-08-24 Диоксолановые аналоги уридина для лечения рака

Family Applications After (1)

Application Number Title Priority Date Filing Date
EA201890648A EA033300B1 (ru) 2014-08-25 2015-08-24 Диоксолановые аналоги уридина для лечения рака

Country Status (24)

Country Link
US (7) US10144750B2 (2)
EP (2) EP3186244B1 (2)
JP (2) JP6663424B2 (2)
KR (2) KR102396905B1 (2)
CN (4) CN110790789B (2)
AU (2) AU2015308988C1 (2)
BR (1) BR112017003898B1 (2)
CA (2) CA2956251C (2)
CY (1) CY1122945T1 (2)
DK (2) DK3572410T3 (2)
EA (2) EA031106B1 (2)
ES (2) ES2927212T3 (2)
HR (1) HRP20201023T1 (2)
HU (2) HUE050705T2 (2)
IL (2) IL250344B (2)
MX (1) MX369649B (2)
MY (2) MY188089A (2)
NZ (2) NZ729118A (2)
PH (2) PH12017500184A1 (2)
PL (2) PL3572410T3 (2)
PT (2) PT3186244T (2)
SG (3) SG11201701172SA (2)
WO (1) WO2016030335A1 (2)
ZA (1) ZA201802864B (2)

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NZ729118A (en) * 2014-08-25 2022-02-25 Medivir Ab Dioxolane analogues of uridine for the treatment of cancer
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
RS62593B1 (sr) * 2015-12-11 2021-12-31 NuCana plc Dijastereoselektivna sinteza derivata fosfata i proleka gemcitabina nuc-1031
CA3014769C (en) * 2016-03-02 2024-01-09 Medivir Aktiebolag Combination therapy with sorafenib or regorafenib and a phosphoramidate prodrug of troxacitabine
CN106432328B (zh) * 2016-09-14 2019-03-22 江苏福瑞生物医药有限公司 一种索非布韦中间体的制备方法
CA3043437A1 (en) * 2016-11-18 2018-05-24 Neurovive Pharmaceutical Ab Liver prodrugs of mitochondrial proton ionophores
GB201709471D0 (en) * 2017-06-14 2017-07-26 Nucana Biomed Ltd Diastereoselective synthesis of hosphate derivatives
WO2019245444A1 (en) 2018-06-21 2019-12-26 Medivir Ab Base-modified cytidine nucleotides for leukemia therapy
JP7337539B2 (ja) * 2018-06-21 2023-09-04 メディヴィル・アクチエボラーグ 白血病療法のための塩基修飾シチジンヌクレオチド
CN113453685A (zh) * 2019-02-18 2021-09-28 美迪维尔公司 使用口服给药的二氧戊环核苷酸与抗pd1或抗pdl1单克隆抗体的组合治疗肝癌的方法
CN110964057B (zh) * 2019-12-25 2022-05-06 东南大学 一种利用微流体反应装置制备索非布韦中间体的方法
CN113402546A (zh) * 2020-03-17 2021-09-17 浙江四维医药科技有限公司 一种瑞德西韦磷酸中间体尾链动态动力学拆分方法
HUE071473T2 (hu) * 2020-04-15 2025-09-28 Medivir Ab MIV-818/lenvatinib kombinációs terápia májrák kezelésére
CN113754692B (zh) * 2020-06-03 2022-06-10 上海交通大学 瑞德西韦中间体(s,s)-氨基磷酸酯的不对称催化合成方法
CN114380860A (zh) * 2020-10-22 2022-04-22 广东东阳光药业有限公司 一种含磷化合物的制备方法
CN114685558A (zh) * 2020-12-28 2022-07-01 尚科生物医药(上海)有限公司 一种瑞德西韦中间体的制备方法
CN114249764A (zh) * 2021-11-10 2022-03-29 宁波大学 一种磷酰胺酯类前药的中间体及其制备方法与应用
WO2025155547A1 (en) * 2024-01-17 2025-07-24 University Of Georgia Research Foundation, Inc. An efficient synthesis of beta-l-5-[(e)-2-bromovinyl)-1-((2s,4s)-2-(hydroxymethyl)-1,3-(dioxolane-4-yl) uracil)] (l-bhdu) via chiral pure l-dioxolane
CN119240898A (zh) * 2024-11-21 2025-01-03 中冶赛迪工程技术股份有限公司 适用于连续流污水处理的精准调酸系统

Citations (2)

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WO2002030922A2 (en) * 2000-10-13 2002-04-18 Shire Biochem Inc. Dioxolane analogs for improved inter-cellular delivery
WO2005012327A2 (en) * 2003-07-21 2005-02-10 University College Cardiff Consultants Limited Nucleotide phosphoramidates as anticancer agents

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US5444063A (en) * 1990-12-05 1995-08-22 Emory University Enantiomerically pure β-D-dioxolane nucleosides with selective anti-Hepatitis B virus activity
US6022876A (en) 1996-11-15 2000-02-08 Yale University L-β-dioxolane uridine analogs and methods for treating and preventing Epstein-Barr virus infections
WO2007106450A2 (en) * 2006-03-10 2007-09-20 University Of Georgia Research Foundation, Inc. Diketo acids with nucleobase scaffolds: anti-hiv replication inhibitors targeted at hiv integrase in combination therapy
KR20090057050A (ko) 2006-09-01 2009-06-03 유니버시티 오브 조지아 리서치 파운데이션, 인코포레이티드 암치료를 위한 트록사시타빈 전구약물
PL216525B1 (pl) * 2006-10-17 2014-04-30 Ct Badań Molekularnych I Makromolekularnych Polskiej Akademii Nauk 5'-O-[(N-acylo)amidoditiofosforano] nukleozydy oraz sposób wytwarzania 5'-O-[(N-acylo)amidofosforano]-,5'-O-[(N-acylo)amidotiofosforano]-, 5'-O-[(N-acylo)amidoditiofosforano]nukleozydów
US20130143835A1 (en) * 2011-12-05 2013-06-06 Medivir Ab HCV Polymerase Inhibitors
CN105934438A (zh) * 2013-11-27 2016-09-07 艾登尼克斯药业有限公司 用于治疗肝癌的核苷酸
NZ729118A (en) * 2014-08-25 2022-02-25 Medivir Ab Dioxolane analogues of uridine for the treatment of cancer

Patent Citations (2)

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Publication number Priority date Publication date Assignee Title
WO2002030922A2 (en) * 2000-10-13 2002-04-18 Shire Biochem Inc. Dioxolane analogs for improved inter-cellular delivery
WO2005012327A2 (en) * 2003-07-21 2005-02-10 University College Cardiff Consultants Limited Nucleotide phosphoramidates as anticancer agents

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Publication number Publication date
JP6905609B2 (ja) 2021-07-21
NZ762628A (en) 2023-04-28
AU2018201980A1 (en) 2018-04-12
US10336780B2 (en) 2019-07-02
EP3186244B1 (en) 2020-04-22
JP2020090535A (ja) 2020-06-11
AU2018201980B2 (en) 2019-05-16
AU2015308988A1 (en) 2017-02-23
CN107074826B (zh) 2020-05-22
US20200239502A1 (en) 2020-07-30
MX369649B (es) 2019-11-15
BR112017003898A2 (pt) 2017-12-05
CA2956251C (en) 2022-10-25
PH12017500184B1 (en) 2017-06-28
US10822360B2 (en) 2020-11-03
CA3128645A1 (en) 2016-03-03
EA033300B1 (ru) 2019-09-30
SG11201701172SA (en) 2017-03-30
ES2927212T3 (es) 2022-11-03
SG10202001117YA (en) 2020-04-29
CN107074826A (zh) 2017-08-18
US20210054008A1 (en) 2021-02-25
ZA201802864B (en) 2019-07-31
SG10201911558UA (en) 2020-01-30
US20170267705A1 (en) 2017-09-21
EP3572410B1 (en) 2022-07-20
KR20200035482A (ko) 2020-04-03
AU2015308988C1 (en) 2018-09-06
HUE050705T2 (hu) 2020-12-28
CN110804072A (zh) 2020-02-18
EP3186244A1 (en) 2017-07-05
MY188089A (en) 2021-11-17
NZ729118A (en) 2022-02-25
MX2017002328A (es) 2017-05-22
US20230382931A1 (en) 2023-11-30
DK3186244T3 (da) 2020-07-13
MY198325A (en) 2023-08-24
US20230117570A1 (en) 2023-04-20
KR20170046736A (ko) 2017-05-02
PL3572410T3 (pl) 2022-10-03
HRP20201023T1 (hr) 2020-10-16
JP6663424B2 (ja) 2020-03-11
IL266766A (en) 2019-07-31
IL250344A0 (en) 2017-03-30
CN111269264A (zh) 2020-06-12
WO2016030335A1 (en) 2016-03-03
EA201790328A1 (ru) 2017-08-31
EA201890648A2 (ru) 2018-08-31
US10144750B2 (en) 2018-12-04
EA201890648A3 (ru) 2019-02-28
PL3186244T3 (pl) 2020-11-16
US20190389890A1 (en) 2019-12-26
CY1122945T1 (el) 2021-10-29
US20190100541A1 (en) 2019-04-04
IL266766B (en) 2020-05-31
EP3572410A1 (en) 2019-11-27
HUE059640T2 (hu) 2022-12-28
IL250344B (en) 2020-01-30
JP2017526677A (ja) 2017-09-14
BR112017003898B1 (pt) 2022-10-18
DK3572410T3 (da) 2022-08-29
PH12017500184A1 (en) 2017-06-28
KR102398714B1 (ko) 2022-05-17
US10654877B2 (en) 2020-05-19
ES2796089T3 (es) 2020-11-25
US11447511B2 (en) 2022-09-20
AU2015308988B2 (en) 2018-04-26
PT3572410T (pt) 2022-09-15
CN110790789B (zh) 2023-05-12
PH12019501919A1 (en) 2020-09-14
CN110790789A (zh) 2020-02-14
CN110804072B (zh) 2023-05-12
CA3128645C (en) 2023-06-27
PT3186244T (pt) 2020-05-29
CA2956251A1 (en) 2016-03-03
KR102396905B1 (ko) 2022-05-13

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