CN111954531A - α聚谷氨酸化培美曲塞及其用途 - Google Patents

α聚谷氨酸化培美曲塞及其用途 Download PDF

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Publication number
CN111954531A
CN111954531A CN201980024908.7A CN201980024908A CN111954531A CN 111954531 A CN111954531 A CN 111954531A CN 201980024908 A CN201980024908 A CN 201980024908A CN 111954531 A CN111954531 A CN 111954531A
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Prior art keywords
alpha
composition
pemetrexed
cancer
glutamyl
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Pending
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CN201980024908.7A
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English (en)
Chinese (zh)
Inventor
C·尼基萨
V·M·莫约
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LEAF Holdings Group LLC
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LEAF Holdings Group LLC
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Publication of CN111954531A publication Critical patent/CN111954531A/zh
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    • 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
    • A61K47/62—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 a protein, peptide or polyamino acid
    • A61K47/64—Drug-peptide, drug-protein or drug-polyamino acid conjugates, i.e. the modifying agent being a peptide, protein or polyamino acid which is covalently bonded or complexed to a therapeutically active agent
    • A61K47/645—Polycationic or polyanionic oligopeptides, polypeptides or polyamino acids, e.g. polylysine, polyarginine, polyglutamic acid or peptide TAT
    • 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
    • A61K31/28—Compounds containing heavy metals
    • A61K31/282—Platinum compounds
    • 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
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • 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
    • A61K9/10—Dispersions; Emulsions
    • A61K9/127—Synthetic bilayered vehicles, e.g. liposomes or liposomes with cholesterol as the only non-phosphatidyl surfactant
    • A61K9/1271—Non-conventional liposomes, e.g. PEGylated liposomes or liposomes coated or grafted with polymers
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K16/00—Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies
    • C07K16/18—Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies against material from animals or humans
    • C07K16/28—Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K16/00—Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies
    • C07K16/18—Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies against material from animals or humans
    • C07K16/28—Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
    • C07K16/2803—Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants against the immunoglobulin superfamily
    • C07K16/2818—Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants against the immunoglobulin superfamily against CD28 or CD152
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Immunology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Organic Chemistry (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Molecular Biology (AREA)
  • Biophysics (AREA)
  • Genetics & Genomics (AREA)
  • Biochemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Dispersion Chemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
CN201980024908.7A 2018-02-07 2019-02-07 α聚谷氨酸化培美曲塞及其用途 Pending CN111954531A (zh)

Applications Claiming Priority (17)

Application Number Priority Date Filing Date Title
US201862627703P 2018-02-07 2018-02-07
US201862627741P 2018-02-07 2018-02-07
US62/627,703 2018-02-07
US62/627,741 2018-02-07
US201862630629P 2018-02-14 2018-02-14
US62/630,629 2018-02-14
US201862662374P 2018-04-25 2018-04-25
US62/662,374 2018-04-25
US201862702732P 2018-07-24 2018-07-24
US201862702561P 2018-07-24 2018-07-24
US62/702,561 2018-07-24
US62/702,732 2018-07-24
US201862764943P 2018-08-17 2018-08-17
US201862764955P 2018-08-17 2018-08-17
US62/764,943 2018-08-17
US62/764,955 2018-08-17
PCT/US2019/016989 WO2019157138A1 (en) 2018-02-07 2019-02-07 Alpha polyglutamated pemetrexed and uses thereof

Publications (1)

Publication Number Publication Date
CN111954531A true CN111954531A (zh) 2020-11-17

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CN201980024908.7A Pending CN111954531A (zh) 2018-02-07 2019-02-07 α聚谷氨酸化培美曲塞及其用途

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US (2) US11779584B2 (enExample)
EP (1) EP3749317A4 (enExample)
JP (3) JP7491572B2 (enExample)
CN (1) CN111954531A (enExample)
WO (1) WO2019157138A1 (enExample)

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CN121177507A (zh) 2016-08-12 2025-12-23 L.E.A.F.控股集团公司 α和γ-D聚谷氨酸化抗叶酸剂及其用途
WO2018031968A1 (en) 2016-08-12 2018-02-15 L.E.A.F. Holdings Group Llc Alpha and gamma-d polyglutamated antifolates and uses thereof
WO2019157129A1 (en) 2018-02-07 2019-08-15 L.E.A.F. Holdings Group Llc Alpha polyglutamated pralatrexate and uses thereof
EP3749314A4 (en) 2018-02-07 2022-02-23 L.E.A.F Holdings Group LLC ALPHA-POLYGLUTAMATE METHOTREXATE AND ITS USES
US12310966B2 (en) 2018-02-07 2025-05-27 L.E.A.F. Holdings Group Llc Alpha polyglutamated aminopterin and uses thereof
EP3749321A4 (en) * 2018-02-07 2022-03-09 L.E.A.F Holdings Group LLC Gamma polyglutamated antifolates and uses thereof
WO2019157121A1 (en) 2018-02-07 2019-08-15 L.E.A.F. Holdings Group Llc Alpha polyglutamated lometrexol and uses thereof
JP7491572B2 (ja) 2018-02-07 2024-05-28 エル．イー．エー．エフ． ホールディングス グループ エルエルシー アルファポリグルタミン酸化ペメトレキセドおよびその使用
CA3090389A1 (en) 2018-02-07 2019-08-15 L.E.A.F. Holdings Group Llc Alpha polyglutamated raltitrexed and uses thereof
WO2019157145A1 (en) 2018-02-07 2019-08-15 L.E.A.F. Holdings Group Llc Gamma polyglutamated pemetrexed and uses thereof
CN111867593A (zh) * 2018-02-07 2020-10-30 L.E.A.F.控股集团公司 α聚谷氨酸化抗叶酸剂及其用途
EP3749319A4 (en) 2018-02-07 2022-06-22 L.E.A.F Holdings Group LLC TETRAHYDROFOLATES ALPHA POLYGLUTAMATE AND THEIR USES
EP3749318A4 (en) 2018-02-07 2022-07-06 L.E.A.F Holdings Group LLC GAMMA-POLYGLUTAMATED RALTITREXED AND ITS USES
US12220431B2 (en) 2018-02-07 2025-02-11 L.E.A.F. Holdings Group Llc Gamma polyglutamated antifolates and uses thereof
CA3090753A1 (en) 2018-02-14 2019-08-22 L.E.A.F. Holdings Group Llc Gamma polyglutamated pralatrexate and uses thereof
US12350271B2 (en) 2018-02-14 2025-07-08 L.E.A.F. Holdings Group Llc Gamma polyglutamated aminopterin and uses thereof
WO2019160734A1 (en) 2018-02-14 2019-08-22 L.E.A.F. Holdings Group Llc Gamma polyglutamated lometrexol and uses thereof
JP7462950B2 (ja) 2018-02-14 2024-04-08 エル．イー．エー．エフ． ホールディングス グループ エルエルシー ガンマポリグルタミン酸化メトトレキセートおよびその使用
WO2019160735A1 (en) 2018-02-14 2019-08-22 L.E.A.F. Holdings Group Llc Gamma polyglutamated tetrahydrofolates and uses thereof
CA3095515A1 (en) 2018-04-10 2019-10-17 Cellectar Biosciences, Inc. Phospholipid-flavagline conjugates and methods of using the same for targeted cancer therapy
BR112022006739B1 (pt) 2019-10-10 2024-01-23 Cellectar Biosciences, Inc Conjugados fosfolipídio-flavagina e métodos de uso do mesmo para terapia direcionada a câncer
KR102557016B1 (ko) * 2020-09-22 2023-07-20 비피진 주식회사 암 치료를 위한 cd47 바인더 및 리포좀 복합체
KR102579284B1 (ko) * 2020-09-22 2023-09-18 비피진 주식회사 신규의 cd47 바인더와 폴리뉴클레오티드를 포함하는 암 치료를 위한 리포좀 복합체
CN114539353B (zh) * 2020-11-26 2024-08-30 南京碳硅人工智能生物医药技术研究院有限公司 培美曲塞多谷氨酸化代谢物及其制备方法
WO2022119531A1 (en) * 2020-12-01 2022-06-09 Ege Üni̇versi̇tesi̇ Investigation of the potential of pemetrexed-loaded liposome system in cancer treatment

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