EA202091857A1 - Новые низкомолекулярные лекарственные коньюгаты производных гемцитабина - Google Patents

Новые низкомолекулярные лекарственные коньюгаты производных гемцитабина

Info

Publication number
EA202091857A1
EA202091857A1 EA202091857A EA202091857A EA202091857A1 EA 202091857 A1 EA202091857 A1 EA 202091857A1 EA 202091857 A EA202091857 A EA 202091857A EA 202091857 A EA202091857 A EA 202091857A EA 202091857 A1 EA202091857 A1 EA 202091857A1
Authority
EA
Eurasian Patent Office
Prior art keywords
hemcitabin
derivatives
drug conjugates
new low
molecular drug
Prior art date
Application number
EA202091857A
Other languages
English (en)
Inventor
Стивен Альберт Эверетт
Крейг Алан Коберн
Original Assignee
Маверикс Онколоджи, Инк.
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
Application filed by Маверикс Онколоджи, Инк. filed Critical Маверикс Онколоджи, Инк.
Publication of EA202091857A1 publication Critical patent/EA202091857A1/ru

Links

Classifications

    • 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
    • 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
    • A61K49/00Preparations for testing in vivo
    • A61K49/0004Screening or testing of compounds for diagnosis of disorders, assessment of conditions, e.g. renal clearance, gastric emptying, testing for diabetes, allergy, rheuma, pancreas functions
    • 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
    • G01N33/574Immunoassay; Biospecific binding assay; Materials therefor for cancer
    • G01N33/57484Immunoassay; Biospecific binding assay; Materials therefor for cancer involving compounds serving as markers for tumor, cancer, neoplasia, e.g. cellular determinants, receptors, heat shock/stress proteins, A-protein, oligosaccharides, 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

Abstract

Раскрыты соединения формулы (I)или их фармацевтически приемлемая соль, сложный эфир, амид, сольват или стереоизомер, где каждый L, Y1, Y2, Y3, Y4, Y5, Z1, Z2, Z3, Z4, Z5, Z6 и эффектор являются такими, как определено в описании; их композиции, их применения и способы их применения.
EA202091857A 2018-02-02 2019-02-04 Новые низкомолекулярные лекарственные коньюгаты производных гемцитабина EA202091857A1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201862625779P 2018-02-02 2018-02-02
PCT/US2019/016477 WO2019152911A1 (en) 2018-02-02 2019-02-04 Novel small molecule drug conjugates of gemcitabine derivatives

Publications (1)

Publication Number Publication Date
EA202091857A1 true EA202091857A1 (ru) 2020-12-04

Family

ID=65494546

Family Applications (1)

Application Number Title Priority Date Filing Date
EA202091857A EA202091857A1 (ru) 2018-02-02 2019-02-04 Новые низкомолекулярные лекарственные коньюгаты производных гемцитабина

Country Status (13)

Country Link
US (1) US20210380626A1 (ru)
EP (1) EP3746133A1 (ru)
JP (1) JP2021512951A (ru)
KR (1) KR20200118828A (ru)
CN (1) CN112135635A (ru)
AU (1) AU2019216514A1 (ru)
BR (1) BR112020015747A2 (ru)
CA (1) CA3090272A1 (ru)
EA (1) EA202091857A1 (ru)
IL (1) IL276442A (ru)
PH (1) PH12020551178A1 (ru)
SG (1) SG11202007381YA (ru)
WO (1) WO2019152911A1 (ru)

Families Citing this family (2)

* Cited by examiner, † Cited by third party
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
CN114349816A (zh) * 2021-11-30 2022-04-15 青岛博创生物科学研究院 一种基于氨肽酶n/cd13的小分子偶联分子及其制备方法和应用

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2319837C (en) 1998-02-12 2009-10-27 De Montfort University Hydroxylation activated drug release
US7148226B2 (en) 2003-02-21 2006-12-12 Agouron Pharmaceuticals, Inc. Inhibitors of hepatitis C virus RNA-dependent RNA polymerase, and compositions and treatments using the same
GB0317009D0 (en) * 2003-07-21 2003-08-27 Univ Cardiff Chemical compounds
GB0907551D0 (en) * 2009-05-01 2009-06-10 Univ Dundee Treatment or prophylaxis of proliferative conditions
JP6212831B2 (ja) * 2013-12-04 2017-10-18 杭州源昶医薬科技有限公司 ゲムシタビン誘導体、該誘導体を含む組成物及び該誘導体の製薬用途
EP3119795A4 (en) * 2014-03-03 2018-03-14 Nucorion Pharmaceuticals, Inc. Gemcitabine analogs
CN105001291B (zh) * 2014-04-15 2018-12-04 上海知萌生物医药科技有限公司 吉西他滨化学传递前药及其制备方法和应用
CN107295800A (zh) * 2015-02-25 2017-10-24 配体药物公司 吉西他滨衍生物

Also Published As

Publication number Publication date
BR112020015747A2 (pt) 2020-12-08
JP2021512951A (ja) 2021-05-20
EP3746133A1 (en) 2020-12-09
CA3090272A1 (en) 2019-08-08
CN112135635A (zh) 2020-12-25
KR20200118828A (ko) 2020-10-16
IL276442A (en) 2020-09-30
PH12020551178A1 (en) 2021-06-07
SG11202007381YA (en) 2020-08-28
WO2019152911A1 (en) 2019-08-08
US20210380626A1 (en) 2021-12-09
AU2019216514A1 (en) 2020-09-24

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