EA201692422A1 - Состав, содержащий пролекарство гемцитабина - Google Patents

Состав, содержащий пролекарство гемцитабина

Info

Publication number
EA201692422A1
EA201692422A1 EA201692422A EA201692422A EA201692422A1 EA 201692422 A1 EA201692422 A1 EA 201692422A1 EA 201692422 A EA201692422 A EA 201692422A EA 201692422 A EA201692422 A EA 201692422A EA 201692422 A1 EA201692422 A1 EA 201692422A1
Authority
EA
Eurasian Patent Office
Prior art keywords
gemcitabine
relates
hemcitabin
preservation
composition containing
Prior art date
Application number
EA201692422A
Other languages
English (en)
Other versions
EA033046B1 (ru
Inventor
Хью Гриффит
Гордон Кенновин
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
Priority claimed from GBGB1411253.6A external-priority patent/GB201411253D0/en
Priority claimed from GBGB1417646.5A external-priority patent/GB201417646D0/en
Application filed by Нукана Байомед Лимитед filed Critical Нукана Байомед Лимитед
Publication of EA201692422A1 publication Critical patent/EA201692422A1/ru
Publication of EA033046B1 publication Critical patent/EA033046B1/ru

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Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/70Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7042Compounds having saccharide radicals and heterocyclic rings
    • A61K31/7052Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
    • A61K31/706Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
    • A61K31/7064Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines
    • A61K31/7068Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/16Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing nitrogen, e.g. nitro-, nitroso-, azo-compounds, nitriles, cyanates
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/16Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing nitrogen, e.g. nitro-, nitroso-, azo-compounds, nitriles, cyanates
    • A61K47/18Amines; Amides; Ureas; Quaternary ammonium compounds; Amino acids; Oligopeptides having up to five amino acids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/20Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing sulfur, e.g. dimethyl sulfoxide [DMSO], docusate, sodium lauryl sulfate or aminosulfonic acids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/22Heterocyclic compounds, e.g. ascorbic acid, tocopherol or pyrrolidones
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/26Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/44Oils, fats or waxes according to two or more groups of A61K47/02-A61K47/42; Natural or modified natural oils, fats or waxes, e.g. castor oil, polyethoxylated castor oil, montan wax, lignite, shellac, rosin, beeswax or lanolin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/54Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
    • A61K47/548Phosphates or phosphonates, e.g. bone-seeking
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0019Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/08Solutions
    • 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
    • C07HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H19/00Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
    • C07H19/02Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
    • C07H19/04Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
    • C07H19/06Pyrimidine radicals
    • C07H19/10Pyrimidine radicals with the saccharide radical esterified by phosphoric or polyphosphoric acids

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (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)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Molecular Biology (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Dermatology (AREA)
  • Biochemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Biophysics (AREA)
  • Biotechnology (AREA)
  • Genetics & Genomics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)

Abstract

Настоящее изобретение относится к фармацевтическим составам гемцитабин-[фенилбензокси-L-аланинил)]фосфата, монофосфатного производного хорошо известного противоопухолевого лекарственного средства гемцитабина. В частности, изобретение относится к составам, которые содержат полярный апротонный растворитель, предпочтительно диметилацетамид (ДМА). Составы, содержащие указанный растворитель, оказывают терапевтически эффективное лечение гемцитабин-[фенилбензокси-L-аланинил)]фосфатом. Изобретение также относится к способам применения указанных составов и наборов, содержащих указанные составы.
EA201692422A 2014-06-25 2015-06-25 Состав, содержащий пролекарство гемцитабина EA033046B1 (ru)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
IN2050MU2014 2014-06-25
GBGB1411253.6A GB201411253D0 (en) 2014-06-25 2014-06-25 Prodrug
GBGB1417646.5A GB201417646D0 (en) 2014-10-06 2014-10-06 Formulations of phosphate derivatives
PCT/GB2015/051858 WO2015198059A1 (en) 2014-06-25 2015-06-25 Formulation comprising a gemcitabine-prodrug

Publications (2)

Publication Number Publication Date
EA201692422A1 true EA201692422A1 (ru) 2017-04-28
EA033046B1 EA033046B1 (ru) 2019-08-30

Family

ID=53499028

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201692422A EA033046B1 (ru) 2014-06-25 2015-06-25 Состав, содержащий пролекарство гемцитабина

Country Status (29)

Country Link
US (4) US10117888B2 (ru)
EP (2) EP3269391A1 (ru)
JP (3) JP6855248B2 (ru)
KR (2) KR20220104270A (ru)
CN (2) CN106470672B (ru)
AU (2) AU2015278900B2 (ru)
BR (1) BR112016025787B1 (ru)
CA (1) CA2944966C (ru)
CL (1) CL2016003261A1 (ru)
CY (1) CY1119772T1 (ru)
DK (1) DK3119794T3 (ru)
EA (1) EA033046B1 (ru)
ES (1) ES2655820T3 (ru)
HK (1) HK1244437A1 (ru)
HR (1) HRP20180007T1 (ru)
HU (1) HUE036011T2 (ru)
IL (2) IL248345B (ru)
LT (1) LT3119794T (ru)
MX (2) MX2020004054A (ru)
MY (1) MY186584A (ru)
NO (1) NO3119794T3 (ru)
PH (1) PH12016502552A1 (ru)
PL (1) PL3119794T3 (ru)
PT (1) PT3119794T (ru)
RS (1) RS56752B1 (ru)
SG (1) SG11201608809RA (ru)
SI (1) SI3119794T1 (ru)
TW (2) TWI765176B (ru)
WO (1) WO2015198059A1 (ru)

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MY196772A (en) 2015-12-11 2023-05-03 NuCana plc 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
GB201522764D0 (en) 2015-12-23 2016-02-03 Nucana Biomed Ltd Formulations of phosphate derivatives
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GB201709471D0 (en) 2017-06-14 2017-07-26 Nucana Biomed Ltd Diastereoselective synthesis of hosphate derivatives

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Publication number Publication date
CN106470672A (zh) 2017-03-01
AU2019204557A1 (en) 2019-07-18
US11040051B2 (en) 2021-06-22
BR112016025787A2 (pt) 2017-08-15
NZ725009A (en) 2021-02-26
PT3119794T (pt) 2018-01-15
CN110882268A (zh) 2020-03-17
JP2017519022A (ja) 2017-07-13
RS56752B1 (sr) 2018-04-30
TW201945007A (zh) 2019-12-01
EA033046B1 (ru) 2019-08-30
KR102421929B1 (ko) 2022-07-15
JP2022031659A (ja) 2022-02-22
US20170095498A1 (en) 2017-04-06
DK3119794T3 (en) 2018-01-22
MX2016015629A (es) 2017-08-02
HRP20180007T1 (hr) 2018-02-23
IL276199B (en) 2022-04-01
US10117888B2 (en) 2018-11-06
US20190022118A1 (en) 2019-01-24
CL2016003261A1 (es) 2017-10-06
NO3119794T3 (ru) 2018-03-10
BR112016025787B1 (pt) 2022-12-13
CY1119772T1 (el) 2018-06-27
IL276199A (en) 2020-09-30
US20220031727A1 (en) 2022-02-03
TW201613611A (en) 2016-04-16
HK1244437A1 (zh) 2018-08-10
CA2944966C (en) 2022-10-25
TWI674097B (zh) 2019-10-11
MX2020004054A (es) 2021-11-30
SI3119794T1 (en) 2018-02-28
AU2015278900B2 (en) 2019-04-04
EP3119794B1 (en) 2017-10-11
JP6855248B2 (ja) 2021-04-07
CN106470672B (zh) 2019-11-05
CA2944966A1 (en) 2015-12-30
JP2020079255A (ja) 2020-05-28
IL248345B (en) 2020-10-29
TWI765176B (zh) 2022-05-21
US20200397810A1 (en) 2020-12-24
KR20170042501A (ko) 2017-04-19
AU2015278900A1 (en) 2016-10-27
JP7329025B2 (ja) 2023-08-17
JP6970221B2 (ja) 2021-11-24
SG11201608809RA (en) 2016-11-29
KR20220104270A (ko) 2022-07-26
WO2015198059A1 (en) 2015-12-30
EP3119794A1 (en) 2017-01-25
PH12016502552A1 (en) 2017-04-10
LT3119794T (lt) 2018-02-12
IL248345A0 (en) 2016-11-30
PL3119794T3 (pl) 2018-04-30
AU2019204557B2 (en) 2020-08-27
ES2655820T3 (es) 2018-02-21
EP3269391A1 (en) 2018-01-17
US10786523B2 (en) 2020-09-29
US11707477B2 (en) 2023-07-25
HUE036011T2 (hu) 2018-06-28
MY186584A (en) 2021-07-28

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