EA033046B1 - Состав, содержащий пролекарство гемцитабина - Google Patents

Состав, содержащий пролекарство гемцитабина

Info

Publication number
EA033046B1
EA033046B1 EA201692422A EA201692422A EA033046B1 EA 033046 B1 EA033046 B1 EA 033046B1 EA 201692422 A EA201692422 A EA 201692422A EA 201692422 A EA201692422 A EA 201692422A EA 033046 B1 EA033046 B1 EA 033046B1
Authority
EA
Eurasian Patent Office
Prior art keywords
formulations
gemcitabine
relates
alaninyl
benzoxy
Prior art date
Application number
EA201692422A
Other languages
English (en)
Other versions
EA201692422A1 (ru
Inventor
Хью Гриффит
Гордон Кенновин
Original Assignee
НУКАНА ПиЭлСи
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 ПиЭлСи filed Critical НУКАНА ПиЭлСи
Publication of EA201692422A1 publication Critical patent/EA201692422A1/ru
Publication of EA033046B1 publication Critical patent/EA033046B1/ru

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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
    • A61K31/7052—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
    • A61K31/706—Compounds 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
    • A61K31/7064—Compounds 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
    • A61K31/7068—Compounds 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/16—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing nitrogen, e.g. nitro-, nitroso-, azo-compounds, nitriles, cyanates
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/16—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing nitrogen, e.g. nitro-, nitroso-, azo-compounds, nitriles, cyanates
    • A61K47/18—Amines; Amides; Ureas; Quaternary ammonium compounds; Amino acids; Oligopeptides having up to five amino acids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/20—Organic 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/22—Heterocyclic compounds, e.g. ascorbic acid, tocopherol or pyrrolidones
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/26—Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/44—Oils, 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal 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
    • A61K47/51—Medicinal 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
    • A61K47/54—Medicinal 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
    • A61K47/548—Phosphates or phosphonates, e.g. bone-seeking
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/08—Solutions
    • 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
    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (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

Изобретение относится к фармацевтическим составам гемцитабин[фенил(бензокси-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[фенил(бензокси-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
GBGB1411253.6A GB201411253D0 (en) 2014-06-25 2014-06-25 Prodrug
IN2050MU2014 2014-06-25
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 EA201692422A1 (ru) 2017-04-28
EA033046B1 true EA033046B1 (ru) 2019-08-30

Family

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EA201692422A EA033046B1 (ru) 2014-06-25 2015-06-25 Состав, содержащий пролекарство гемцитабина

Country Status (29)

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US (4) US10117888B2 (ru)
EP (2) EP3119794B1 (ru)
JP (3) JP6855248B2 (ru)
KR (2) KR20220104270A (ru)
CN (2) CN110882268A (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) TWI674097B (ru)
WO (1) WO2015198059A1 (ru)

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CY1119772T1 (el) 2018-06-27
KR102421929B1 (ko) 2022-07-15
US11707477B2 (en) 2023-07-25
EP3269391A1 (en) 2018-01-17
JP2020079255A (ja) 2020-05-28
CL2016003261A1 (es) 2017-10-06
MX2020004054A (es) 2021-11-30
RS56752B1 (sr) 2018-04-30
HK1244437A1 (zh) 2018-08-10
US10117888B2 (en) 2018-11-06
CA2944966A1 (en) 2015-12-30
CA2944966C (en) 2022-10-25
PH12016502552A1 (en) 2017-04-10
US10786523B2 (en) 2020-09-29
MX2016015629A (es) 2017-08-02
US11040051B2 (en) 2021-06-22
TWI674097B (zh) 2019-10-11
CN106470672B (zh) 2019-11-05
US20220031727A1 (en) 2022-02-03
IL248345B (en) 2020-10-29
BR112016025787A2 (pt) 2017-08-15
PT3119794T (pt) 2018-01-15
HRP20180007T1 (hr) 2018-02-23
EP3119794B1 (en) 2017-10-11
ES2655820T3 (es) 2018-02-21
NO3119794T3 (ru) 2018-03-10
BR112016025787B1 (pt) 2022-12-13
AU2019204557B2 (en) 2020-08-27
CN106470672A (zh) 2017-03-01
TWI765176B (zh) 2022-05-21
HUE036011T2 (hu) 2018-06-28
JP2017519022A (ja) 2017-07-13
JP2022031659A (ja) 2022-02-22
MY186584A (en) 2021-07-28
TW201945007A (zh) 2019-12-01
EP3119794A1 (en) 2017-01-25
TW201613611A (en) 2016-04-16
CN110882268A (zh) 2020-03-17
JP7329025B2 (ja) 2023-08-17
SG11201608809RA (en) 2016-11-29
AU2019204557A1 (en) 2019-07-18
US20200397810A1 (en) 2020-12-24
JP6855248B2 (ja) 2021-04-07
AU2015278900A1 (en) 2016-10-27
DK3119794T3 (en) 2018-01-22
AU2015278900B2 (en) 2019-04-04
IL276199B (en) 2022-04-01
IL248345A0 (en) 2016-11-30
JP6970221B2 (ja) 2021-11-24
US20190022118A1 (en) 2019-01-24
LT3119794T (lt) 2018-02-12
SI3119794T1 (en) 2018-02-28
KR20220104270A (ko) 2022-07-26
US20170095498A1 (en) 2017-04-06
EA201692422A1 (ru) 2017-04-28
PL3119794T3 (pl) 2018-04-30
KR20170042501A (ko) 2017-04-19
WO2015198059A1 (en) 2015-12-30
IL276199A (en) 2020-09-30
NZ725009A (en) 2021-02-26

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