CN112135634A - 单磷酸吉西他滨的小分子药物偶联物 - Google Patents

单磷酸吉西他滨的小分子药物偶联物 Download PDF

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Publication number
CN112135634A
CN112135634A CN201980024079.2A CN201980024079A CN112135634A CN 112135634 A CN112135634 A CN 112135634A CN 201980024079 A CN201980024079 A CN 201980024079A CN 112135634 A CN112135634 A CN 112135634A
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compound
pharmaceutically acceptable
ester
alkoxy
amide
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Chinese (zh)
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S·A·艾弗雷特
C·A·科伯恩
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Marfurix Oncology Co ltd
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Marfurix Oncology Co ltd
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    • 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
    • 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
    • A61K47/50Medicinal 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
    • A61K47/545Heterocyclic compounds
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • GPHYSICS
    • G01MEASURING; TESTING
    • G01NINVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N33/00Investigating or analysing materials by specific methods not covered by groups G01N1/00 - G01N31/00
    • G01N33/48Biological material, e.g. blood, urine; Haemocytometers
    • G01N33/50Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
    • G01N33/53Immunoassay; Biospecific binding assay; Materials therefor
    • G01N33/575Immunoassay; Biospecific binding assay; Materials therefor for cancer
    • G01N33/5758Immunoassay; Biospecific binding assay; Materials therefor for cancer involving compounds serving as markers for tumours, cancers or neoplasias, e.g. cellular determinants, receptors, heat shock/stress proteins, A-protein, oligosaccharides or metabolites
    • GPHYSICS
    • G01MEASURING; TESTING
    • G01NINVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N2333/00Assays involving biological materials from specific organisms or of a specific nature
    • G01N2333/90Enzymes; Proenzymes
    • G01N2333/902Oxidoreductases (1.)
    • G01N2333/90245Oxidoreductases (1.) acting on paired donors with incorporation of molecular oxygen (1.14)
    • GPHYSICS
    • G01MEASURING; TESTING
    • G01NINVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N2440/00Post-translational modifications [PTMs] in chemical analysis of biological material
    • G01N2440/24Post-translational modifications [PTMs] in chemical analysis of biological material hydroxylation

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Medicinal Chemistry (AREA)
  • Molecular Biology (AREA)
  • Organic Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Immunology (AREA)
  • Epidemiology (AREA)
  • Biochemistry (AREA)
  • Biotechnology (AREA)
  • Urology & Nephrology (AREA)
  • Biomedical Technology (AREA)
  • Hematology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Genetics & Genomics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Cell Biology (AREA)
  • Food Science & Technology (AREA)
  • Pathology (AREA)
  • Physics & Mathematics (AREA)
  • Microbiology (AREA)
  • Analytical Chemistry (AREA)
  • General Physics & Mathematics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Saccharide Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Investigating Or Analysing Biological Materials (AREA)
CN201980024079.2A 2018-02-02 2019-02-04 单磷酸吉西他滨的小分子药物偶联物 Pending CN112135634A (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201862625820P 2018-02-02 2018-02-02
US62/625,820 2018-02-02
PCT/US2019/016557 WO2019152955A1 (en) 2018-02-02 2019-02-04 Small molecule drug conjugates of gemcitabine monophosphate

Publications (1)

Publication Number Publication Date
CN112135634A true CN112135634A (zh) 2020-12-25

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CN201980024079.2A Pending CN112135634A (zh) 2018-02-02 2019-02-04 单磷酸吉西他滨的小分子药物偶联物

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Country Link
US (1) US11760773B2 (https=)
EP (1) EP3746134A1 (https=)
JP (2) JP2021512953A (https=)
KR (1) KR20200118827A (https=)
CN (1) CN112135634A (https=)
AU (1) AU2019216531A1 (https=)
BR (1) BR112020015745A2 (https=)
CA (1) CA3091027A1 (https=)
CL (1) CL2020002022A1 (https=)
CO (1) CO2020010970A2 (https=)
EA (1) EA202091856A1 (https=)
IL (1) IL276436A (https=)
MX (1) MX2020008188A (https=)
PE (1) PE20210367A1 (https=)
PH (1) PH12020551182A1 (https=)
SG (1) SG11202007386RA (https=)
WO (1) WO2019152955A1 (https=)

Families Citing this family (1)

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Publication number Priority date Publication date Assignee Title
PE20210367A1 (es) * 2018-02-02 2021-02-26 Maverix Oncology Inc Conjugados de farmacos de molecula pequena de monofosfato de gemcitabina

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CN105792830A (zh) * 2013-03-15 2016-07-20 Z·索 取代的吉西他滨双环酰胺类似物和使用其的治疗方法
CN106459130A (zh) * 2014-03-03 2017-02-22 纽科利制药公司 吉西他滨类似物

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KR20200118827A (ko) 2020-10-16
PH12020551182A1 (en) 2021-05-10
US11760773B2 (en) 2023-09-19
MX2020008188A (es) 2020-11-18
US20210040136A1 (en) 2021-02-11
IL276436A (en) 2020-09-30
SG11202007386RA (en) 2020-08-28
WO2019152955A9 (en) 2020-08-13
EA202091856A1 (ru) 2020-12-07
BR112020015745A2 (pt) 2020-12-08
AU2019216531A1 (en) 2020-09-24
CA3091027A1 (en) 2019-08-08
PE20210367A1 (es) 2021-02-26
CO2020010970A2 (es) 2020-11-20
JP2024054873A (ja) 2024-04-17
WO2019152955A1 (en) 2019-08-08
EP3746134A1 (en) 2020-12-09
CL2020002022A1 (es) 2021-02-12
JP2021512953A (ja) 2021-05-20

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