CN111936147A - γ聚谷氨酸化抗叶酸剂及其用途 - Google Patents

γ聚谷氨酸化抗叶酸剂及其用途 Download PDF

Info

Publication number
CN111936147A
CN111936147A CN201980024669.5A CN201980024669A CN111936147A CN 111936147 A CN111936147 A CN 111936147A CN 201980024669 A CN201980024669 A CN 201980024669A CN 111936147 A CN111936147 A CN 111936147A
Authority
CN
China
Prior art keywords
gamma
antifolate
composition
γpantifol
cancer
Prior art date
Legal status (The legal status 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 status listed.)
Pending
Application number
CN201980024669.5A
Other languages
English (en)
Chinese (zh)
Inventor
C·尼基萨
V·M·莫约
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
LEAF Holdings Group LLC
Original Assignee
LEAF Holdings Group LLC
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 LEAF Holdings Group LLC filed Critical LEAF Holdings Group LLC
Publication of CN111936147A publication Critical patent/CN111936147A/zh
Pending legal-status Critical Current

Links

Images

Classifications

    • 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
    • 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
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/555—Heterocyclic compounds containing heavy metals, e.g. hemin, hematin, melarsoprol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K33/00—Medicinal preparations containing inorganic active ingredients
    • A61K33/24—Heavy metals; Compounds thereof
    • A61K33/243—Platinum; Compounds thereof
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • A61K47/55—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 the modifying agent being also a pharmacologically or therapeutically active agent, i.e. the entire conjugate being a codrug
    • A61K47/551—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 the modifying agent being also a pharmacologically or therapeutically active agent, i.e. the entire conjugate being a codrug one of the codrug's components being a vitamin, e.g. niacinamide, vitamin B3, cobalamin, vitamin B12, folate, vitamin A or retinoic 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
    • A61K47/50—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
    • A61K47/56—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 macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule
    • A61K47/59—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 macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes
    • 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
    • A61K47/69—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 conjugate being characterised by physical or galenical forms, e.g. emulsion, particle, inclusion complex, stent or kit
    • A61K47/6905—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 conjugate being characterised by physical or galenical forms, e.g. emulsion, particle, inclusion complex, stent or kit the form being a colloid or an emulsion
    • A61K47/6911—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 conjugate being characterised by physical or galenical forms, e.g. emulsion, particle, inclusion complex, stent or kit the form being a colloid or an emulsion the form being a liposome
    • A61K47/6913—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 conjugate being characterised by physical or galenical forms, e.g. emulsion, particle, inclusion complex, stent or kit the form being a colloid or an emulsion the form being a liposome the liposome being modified on its surface by an antibody
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D475/00—Heterocyclic compounds containing pteridine ring systems
    • C07D475/06—Heterocyclic compounds containing pteridine ring systems with a nitrogen atom directly attached in position 4
    • C07D475/08—Heterocyclic compounds containing pteridine ring systems with a nitrogen atom directly attached in position 4 with a nitrogen atom directly attached in position 2
    • 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
    • C07K2317/00—Immunoglobulins specific features
    • C07K2317/90—Immunoglobulins specific features characterized by (pharmaco)kinetic aspects or by stability of the immunoglobulin
    • C07K2317/92—Affinity (KD), association rate (Ka), dissociation rate (Kd) or EC50 value
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Dispersion Chemistry (AREA)
  • Biophysics (AREA)
  • Oncology (AREA)
  • Molecular Biology (AREA)
  • Genetics & Genomics (AREA)
  • Biochemistry (AREA)
  • Inorganic Chemistry (AREA)
  • Communicable Diseases (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicinal Preparation (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)
CN201980024669.5A 2018-02-07 2019-02-07 γ聚谷氨酸化抗叶酸剂及其用途 Pending CN111936147A (zh)

Applications Claiming Priority (29)

Application Number Priority Date Filing Date Title
US201862627733P 2018-02-07 2018-02-07
US201862627732P 2018-02-07 2018-02-07
US62/627,733 2018-02-07
US62/627,732 2018-02-07
US201862630620P 2018-02-14 2018-02-14
US201862630751P 2018-02-14 2018-02-14
US201862630652P 2018-02-14 2018-02-14
US201862630625P 2018-02-14 2018-02-14
US201862630613P 2018-02-14 2018-02-14
US201862630824P 2018-02-14 2018-02-14
US62/630,751 2018-02-14
US62/630,824 2018-02-14
US62/630,652 2018-02-14
US62/630,625 2018-02-14
US62/630,620 2018-02-14
US62/630,613 2018-02-14
US201862636289P 2018-02-28 2018-02-28
US62/636,289 2018-02-28
US201862662372P 2018-04-25 2018-04-25
US62/662,372 2018-04-25
US201862702774P 2018-07-24 2018-07-24
US201862702779P 2018-07-24 2018-07-24
US62/702,774 2018-07-24
US62/702,779 2018-07-24
US201862764951P 2018-08-17 2018-08-17
US201862764945P 2018-08-17 2018-08-17
US62/764,945 2018-08-17
US62/764,951 2018-08-17
PCT/US2019/017004 WO2019157148A1 (en) 2018-02-07 2019-02-07 Gamma polyglutamated antifolates and uses thereof

Publications (1)

Publication Number Publication Date
CN111936147A true CN111936147A (zh) 2020-11-13

Family

ID=67548055

Family Applications (1)

Application Number Title Priority Date Filing Date
CN201980024669.5A Pending CN111936147A (zh) 2018-02-07 2019-02-07 γ聚谷氨酸化抗叶酸剂及其用途

Country Status (5)

Country Link
EP (1) EP3749321A4 (https=)
JP (3) JP7490240B2 (https=)
CN (1) CN111936147A (https=)
CA (1) CA3090505A1 (https=)
WO (1) WO2019157148A1 (https=)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN114555127A (zh) * 2019-08-06 2022-05-27 L.E.A.F.控股集团公司 制备聚谷氨酸化抗叶酸剂的方法以及它们的组合物的用途

Families Citing this family (18)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN120939250A (zh) 2016-08-12 2025-11-14 L.E.A.F.控股集团公司 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
WO2019157123A1 (en) 2018-02-07 2019-08-15 L.E.A.F. Holdings Group Llc Alpha polyglutamated aminopterin and uses thereof
CA3090500A1 (en) 2018-02-07 2019-08-15 L.E.A.F. Holdings Group Llc Alpha 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
EP3749319A4 (en) 2018-02-07 2022-06-22 L.E.A.F Holdings Group LLC TETRAHYDROFOLATES ALPHA POLYGLUTAMATE AND THEIR USES
WO2019157121A1 (en) 2018-02-07 2019-08-15 L.E.A.F. Holdings Group Llc Alpha polyglutamated lometrexol and uses thereof
CN111954531A (zh) 2018-02-07 2020-11-17 L.E.A.F.控股集团公司 α聚谷氨酸化培美曲塞及其用途
US12239734B2 (en) 2018-02-07 2025-03-04 L.E.A.F. Holdings Group Llc Gamma polyglutamated raltitrexed and uses thereof
EP3749311A4 (en) 2018-02-07 2022-07-06 L.E.A.F Holdings Group LLC PEMETREXED POLYGLUTAMATE GAMMA COMPOSITIONS AND THEIR USES
JP7491573B2 (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メトトレキセートおよびその使用
US12246015B2 (en) 2018-02-07 2025-03-11 L.E.A.F. Holdings Group Llc Alpha polyglutamated raltitrexed and uses thereof
US12220431B2 (en) 2018-02-07 2025-02-11 L.E.A.F. Holdings Group Llc Gamma polyglutamated antifolates and uses thereof
EP3752157A4 (en) 2018-02-14 2022-07-06 L.E.A.F Holdings Group LLC GAMMA-POLYGLUTAMATED LOMETREXOLE AND USES THEREOF
CN111936145A (zh) 2018-02-14 2020-11-13 L.E.A.F.控股集团公司 γ聚谷氨酸化氨甲蝶呤及其用途
EP3752156A4 (en) 2018-02-14 2021-10-27 L.E.A.F Holdings Group LLC GAMMA-POLYGLUTAMIZED PRALATREXATE AND USES THEREOF
WO2019160732A1 (en) * 2018-02-14 2019-08-22 L.E.A.F. Holdings Group Llc Gamma polyglutamated aminopterin and uses thereof
US12048766B2 (en) 2018-02-14 2024-07-30 L.E.A.F. Holdings Group Llc Gamma polyglutamated tetrahydrofolates and uses thereof

Citations (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20050209239A1 (en) * 2004-03-12 2005-09-22 Barton Kamen Compositions and methods employing aminopterin
US20060160751A1 (en) * 2005-01-07 2006-07-20 Mcguire John J 5-Amino-4-imidazolecarboxamide riboside and its nucleobase as potentiators of antifolate transport and metabolism
US20080214585A1 (en) * 2007-01-19 2008-09-04 Chelsea Therapeutics, Inc. New classical antifolates
US20080234298A1 (en) * 2006-12-29 2008-09-25 Tracon Pharmaceuticals, Inc. Antifolate agent combinations in the treatment of cancer
US20080288177A1 (en) * 2006-08-30 2008-11-20 Hendrik Jan Guchelaar Pharacogenetic method for prediction of the efficacy of methotrexate monotherapy in recent-onset arthritis
CN106794164A (zh) * 2014-08-14 2017-05-31 L.E.A.F.控股集团公司 脂质体包封的亲和性药物
US20180236098A1 (en) * 2016-08-12 2018-08-23 L.E.A.F. Holdings Group Llc Alpha and gamma-d polyglutamated antifolates and uses thereof

Family Cites Families (25)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6569432B1 (en) * 1995-02-24 2003-05-27 Sloan-Kettering Institute For Cancer Research Prostate-specific membrane antigen and uses thereof
US20020168761A1 (en) * 2000-01-24 2002-11-14 Gour Barbara J. Peptidomimetic modulators of cell adhesion
EP1791544A4 (en) * 2004-09-08 2007-09-12 Chelsea Therapeutics Inc CHINAZOLINE DERIVATIVES AS METABOLIC INERT ANTIFOLATE
WO2010141711A1 (en) * 2009-06-03 2010-12-09 Ex-Tek, Llc Skin treatment compositions
US9770414B2 (en) 2010-05-13 2017-09-26 Pacira Pharmaceuticals, Inc. Sustained release formulation of methotrexate as a disease-modifying antirheumatic drug (DMARD) and an anti-cancer agent
PL226015B1 (pl) 2011-03-03 2017-06-30 Wrocławskie Centrum Badań Eit + Spółka Z Ograniczoną Liposomowy preparat zawierajacy przeciwnowotworowa substancje aktywna, sposob jego wytwarzania i zawierajaca go kompozycja farmaceutyczna
CN103040748B (zh) 2012-12-18 2014-07-02 海南圣欣医药科技有限公司 一种培美曲塞二钠脂质体注射剂
WO2018031979A1 (en) * 2016-08-12 2018-02-15 L.E.A.F. Holdings Group Llc Alpha and gamma-d polyglutamated antifolates and uses thereof
CN120939250A (zh) 2016-08-12 2025-11-14 L.E.A.F.控股集团公司 聚谷氨酸化抗叶酸剂及其用途
US20190231690A1 (en) * 2017-11-08 2019-08-01 L.E.A.F. Holdings Group Llc Platinum complexes and uses thereof
US12239734B2 (en) * 2018-02-07 2025-03-04 L.E.A.F. Holdings Group Llc Gamma polyglutamated raltitrexed and uses thereof
WO2019157123A1 (en) * 2018-02-07 2019-08-15 L.E.A.F. Holdings Group Llc Alpha polyglutamated aminopterin and uses thereof
US12246015B2 (en) * 2018-02-07 2025-03-11 L.E.A.F. Holdings Group Llc Alpha polyglutamated raltitrexed and uses thereof
EP3749311A4 (en) * 2018-02-07 2022-07-06 L.E.A.F Holdings Group LLC PEMETREXED POLYGLUTAMATE GAMMA COMPOSITIONS AND THEIR USES
WO2019157121A1 (en) * 2018-02-07 2019-08-15 L.E.A.F. Holdings Group Llc Alpha polyglutamated lometrexol and uses thereof
CA3090500A1 (en) * 2018-02-07 2019-08-15 L.E.A.F. Holdings Group Llc Alpha polyglutamated antifolates and uses thereof
JP7491573B2 (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メトトレキセートおよびその使用
CN111954531A (zh) * 2018-02-07 2020-11-17 L.E.A.F.控股集团公司 α聚谷氨酸化培美曲塞及其用途
WO2019157129A1 (en) * 2018-02-07 2019-08-15 L.E.A.F. Holdings Group Llc Alpha polyglutamated pralatrexate and uses thereof
EP3749319A4 (en) * 2018-02-07 2022-06-22 L.E.A.F Holdings Group LLC TETRAHYDROFOLATES ALPHA POLYGLUTAMATE AND THEIR USES
EP3752157A4 (en) * 2018-02-14 2022-07-06 L.E.A.F Holdings Group LLC GAMMA-POLYGLUTAMATED LOMETREXOLE AND USES THEREOF
EP3752156A4 (en) * 2018-02-14 2021-10-27 L.E.A.F Holdings Group LLC GAMMA-POLYGLUTAMIZED PRALATREXATE AND USES THEREOF
WO2019160732A1 (en) * 2018-02-14 2019-08-22 L.E.A.F. Holdings Group Llc Gamma polyglutamated aminopterin and uses thereof
CN111936145A (zh) * 2018-02-14 2020-11-13 L.E.A.F.控股集团公司 γ聚谷氨酸化氨甲蝶呤及其用途
US12048766B2 (en) * 2018-02-14 2024-07-30 L.E.A.F. Holdings Group Llc Gamma polyglutamated tetrahydrofolates and uses thereof

Patent Citations (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20050209239A1 (en) * 2004-03-12 2005-09-22 Barton Kamen Compositions and methods employing aminopterin
US20060160751A1 (en) * 2005-01-07 2006-07-20 Mcguire John J 5-Amino-4-imidazolecarboxamide riboside and its nucleobase as potentiators of antifolate transport and metabolism
US20080288177A1 (en) * 2006-08-30 2008-11-20 Hendrik Jan Guchelaar Pharacogenetic method for prediction of the efficacy of methotrexate monotherapy in recent-onset arthritis
US20080234298A1 (en) * 2006-12-29 2008-09-25 Tracon Pharmaceuticals, Inc. Antifolate agent combinations in the treatment of cancer
US20080214585A1 (en) * 2007-01-19 2008-09-04 Chelsea Therapeutics, Inc. New classical antifolates
CN106794164A (zh) * 2014-08-14 2017-05-31 L.E.A.F.控股集团公司 脂质体包封的亲和性药物
US20180236098A1 (en) * 2016-08-12 2018-08-23 L.E.A.F. Holdings Group Llc Alpha and gamma-d polyglutamated antifolates and uses thereof

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
D S DUCH，等: "Biochemical and cellular pharmacology of 1843U89, a novel benzoquinazoline inhibitor of thymidylate synthase" *
曹胜利，等: "抗叶酸剂类抗肿瘤药物的研究进展" *

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN114555127A (zh) * 2019-08-06 2022-05-27 L.E.A.F.控股集团公司 制备聚谷氨酸化抗叶酸剂的方法以及它们的组合物的用途

Also Published As

Publication number Publication date
JP7490240B2 (ja) 2024-05-27
JP7676063B2 (ja) 2025-05-14
WO2019157148A1 (en) 2019-08-15
EP3749321A4 (en) 2022-03-09
CA3090505A1 (en) 2019-08-15
JP2025105775A (ja) 2025-07-10
EP3749321A1 (en) 2020-12-16
JP2021513533A (ja) 2021-05-27
JP2024097894A (ja) 2024-07-19

Similar Documents

Publication Publication Date Title
JP7679114B2 (ja) アルファポリグルタミン酸化葉酸代謝拮抗薬およびその使用
JP7676063B2 (ja) ガンマポリグルタミン酸化葉酸代謝拮抗薬およびその使用
JP7674775B2 (ja) アルファポリグルタミン酸化テトラヒドロ葉酸およびその使用
US20260053806A1 (en) Gamma polyglutamated methotrexate and uses thereof
US20260053807A1 (en) Alpha polyglutamated aminopterin and uses thereof
US12246018B2 (en) Gamma polyglutamated pemetrexed and uses thereof
US12128046B2 (en) Alpha polyglutamated methotrexate and uses thereof
CN111954531A (zh) α聚谷氨酸化培美曲塞及其用途
CN111971047A (zh) γ聚谷氨酸化四氢叶酸及其用途
CA3090943A1 (en) Gamma polyglutamated aminopterin and uses thereof
US20250198442A1 (en) Gamma polyglutamated pemetrexed and uses thereof
US20250319123A1 (en) Gamma polyglutamated antifolates and uses thereof
US20250319188A1 (en) Alpha polyglutamated antifolates and uses thereof
US12220431B2 (en) Gamma polyglutamated antifolates and uses thereof

Legal Events

Date Code Title Description
PB01 Publication
PB01 Publication
SE01 Entry into force of request for substantive examination
SE01 Entry into force of request for substantive examination