JP7462950B2 - 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 - Google Patents

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 Download PDF

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JP7462950B2
JP7462950B2 JP2020543388A JP2020543388A JP7462950B2 JP 7462950 B2 JP7462950 B2 JP 7462950B2 JP 2020543388 A JP2020543388 A JP 2020543388A JP 2020543388 A JP2020543388 A JP 2020543388A JP 7462950 B2 JP7462950 B2 JP 7462950B2
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gamma
methotrexate
γpmtx
cancer
liposome
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JP2021514357A5 (enExample
JP2021514357A (ja
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ニイキザ,クレト
モヨ,ヴィクター,マンドラ
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LEAF Holdings Group LLC
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D475/00Heterocyclic compounds containing pteridine ring systems
    • C07D475/06Heterocyclic compounds containing pteridine ring systems with a nitrogen atom directly attached in position 4
    • C07D475/08Heterocyclic compounds containing pteridine ring systems with a nitrogen atom directly attached in position 4 with a nitrogen atom directly attached in position 2
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    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
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    • A61K39/39533Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum against materials from animals
    • A61K39/3955Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum against materials from animals against proteinaceous materials, e.g. enzymes, hormones, lymphokines
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    • A61K47/64Drug-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
    • A61K47/645Polycationic or polyanionic oligopeptides, polypeptides or polyamino acids, e.g. polylysine, polyarginine, polyglutamic acid or peptide TAT
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    • 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
    • A61K47/62Medicinal 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
    • A61K47/64Drug-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
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    • A61K47/69Medicinal 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
    • A61K47/6905Medicinal 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
    • A61K47/6911Medicinal 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
    • A61K47/6913Medicinal 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
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    • A61K47/6911Medicinal 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
    • A61K47/6915Medicinal 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 form being a liposome with polymerisable or polymerized bilayer-forming substances, e.g. polymersomes
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K16/00Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies
    • C07K16/18Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies against material from animals or humans
    • YGENERAL 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
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    • Y02A50/30Against 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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  • Organic Chemistry (AREA)
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  • Chemical Kinetics & Catalysis (AREA)
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  • Proteomics, Peptides & Aminoacids (AREA)
  • Molecular Biology (AREA)
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  • Biochemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Endocrinology (AREA)
  • Inorganic Chemistry (AREA)
  • Genetics & Genomics (AREA)
  • Biophysics (AREA)
  • Dermatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (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)
  • Micro-Organisms Or Cultivation Processes Thereof (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
JP2020543388A 2018-02-14 2019-02-07 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 Active JP7462950B2 (ja)

Priority Applications (2)

Application Number Priority Date Filing Date Title
JP2024043740A JP7679113B2 (ja) 2018-02-14 2024-03-19 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
JP2025073080A JP2025118708A (ja) 2018-02-14 2025-04-25 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

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Application Number Priority Date Filing Date Title
US201862630713P 2018-02-14 2018-02-14
US62/630,713 2018-02-14
US201862662372P 2018-04-25 2018-04-25
US62/662,372 2018-04-25
US201862702774P 2018-07-24 2018-07-24
US62/702,774 2018-07-24
US201862764945P 2018-08-17 2018-08-17
US62/764,945 2018-08-17
PCT/US2019/016960 WO2019160733A1 (en) 2018-02-14 2019-02-07 Gamma polyglutamated methotrexate and uses thereof

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JP2021514357A5 JP2021514357A5 (enExample) 2022-02-16
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JP2025073080A Pending JP2025118708A (ja) 2018-02-14 2025-04-25 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

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EP (1) EP3752155A4 (enExample)
JP (3) JP7462950B2 (enExample)
CN (1) CN111936145A (enExample)
CA (1) CA3090989A1 (enExample)
WO (1) WO2019160733A1 (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
EP3749318A4 (en) 2018-02-07 2022-07-06 L.E.A.F Holdings Group LLC GAMMA-POLYGLUTAMATED RALTITREXED AND ITS USES
WO2019157121A1 (en) 2018-02-07 2019-08-15 L.E.A.F. Holdings Group Llc Alpha polyglutamated lometrexol and uses thereof
EP3749321A4 (en) * 2018-02-07 2022-03-09 L.E.A.F Holdings Group LLC Gamma polyglutamated antifolates 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
WO2019157129A1 (en) 2018-02-07 2019-08-15 L.E.A.F. Holdings Group Llc Alpha polyglutamated pralatrexate 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
US12310966B2 (en) 2018-02-07 2025-05-27 L.E.A.F. Holdings Group Llc Alpha polyglutamated aminopterin and uses thereof
WO2019157145A1 (en) 2018-02-07 2019-08-15 L.E.A.F. Holdings Group Llc Gamma polyglutamated pemetrexed and uses thereof
US12220431B2 (en) 2018-02-07 2025-02-11 L.E.A.F. Holdings Group Llc Gamma polyglutamated antifolates and uses thereof
EP3749319A4 (en) 2018-02-07 2022-06-22 L.E.A.F Holdings Group LLC TETRAHYDROFOLATES ALPHA POLYGLUTAMATE AND THEIR USES
EP3749314A4 (en) 2018-02-07 2022-02-23 L.E.A.F Holdings Group LLC ALPHA-POLYGLUTAMATE METHOTREXATE AND ITS USES
US12350271B2 (en) 2018-02-14 2025-07-08 L.E.A.F. Holdings Group Llc Gamma polyglutamated aminopterin and uses thereof
WO2019160735A1 (en) 2018-02-14 2019-08-22 L.E.A.F. Holdings Group Llc Gamma polyglutamated tetrahydrofolates and uses thereof
CA3090753A1 (en) 2018-02-14 2019-08-22 L.E.A.F. Holdings Group Llc Gamma polyglutamated pralatrexate 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
WO2019160734A1 (en) 2018-02-14 2019-08-22 L.E.A.F. Holdings Group Llc Gamma polyglutamated lometrexol and uses thereof
CN113041359B (zh) * 2021-03-26 2022-05-20 湖南师范大学 一种谷胱甘肽响应性抗骨肉瘤前药纳米粒子及其制备方法和用途

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2013526545A (ja) 2010-05-13 2013-06-24 パシラ ファーマシューティカルズ インコーポレーテッド 疾患修飾性抗リウマチ薬(dmard)および抗癌剤としてのメトトレキサートの持続性放出製剤
JP2017526744A (ja) 2014-08-14 2017-09-14 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L.E.A.F. Holdings Group Llc リポソームカプセル化親和性薬物
JP2019524885A (ja) 2016-08-12 2019-09-05 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L.E.A.F. Holdings Group Llc ポリグルタミン酸化抗葉酸剤およびその使用

Family Cites Families (138)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US2512572A (en) 1950-06-20 Substituted pteridines and method
US3989703A (en) 1974-03-22 1976-11-02 Institutul Oncologic Process of preparing N[p-{[(2,4-diamino-6-pteridyl)-methyl]N10 -methylamino}-benzoyl]-glutamic acid
US4106488A (en) 1974-08-20 1978-08-15 Robert Thomas Gordon Cancer treatment method
US3892801A (en) 1974-09-11 1975-07-01 American Cyanamid Co Method for preparing alkali salts of p-methylaminobenzoylglutamic acid
US4079056A (en) 1975-03-31 1978-03-14 The United States Of America As Represented By The Department Of Health, Education And Welfare Method of making pteridine compounds
US4057548A (en) 1975-11-11 1977-11-08 Jacek Wiecko Process for preparing methotrexate or an N-substituted derivative thereof and/or a di (lower) alkyl ester thereof and precursor therefor
US4067867A (en) 1976-03-30 1978-01-10 Jacek Wiecko Process for preparing pyrazine precursor of methotrexate or an N-substituted derivative thereof and/or a di(lower)alkyl ester thereof
US4080325A (en) 1976-11-17 1978-03-21 The United States Of America As Represented By The Department Of Health, Education And Welfare Synthesis of methotrexate
CH630380A5 (de) 1977-08-12 1982-06-15 Lonza Ag Verfahren zur herstellung von l-methotrexat.
US4136101A (en) 1978-02-03 1979-01-23 American Cyanamid Company Process for preparing dialkyl (p-aminobenzoyl) glutamates
US4306064A (en) 1980-03-25 1981-12-15 Ellard James A Synthesis of 2,4-diamino-6-hydroxymethylpteridine
US4421913A (en) 1980-04-23 1983-12-20 The United States Of America As Represented By The Secretary Of The Department Of Health And Human Services Separation of triphenylphosphine oxide from methotrexate ester and purification of said ester
US4374987A (en) 1980-08-14 1983-02-22 American Cyanamid Company Process for the preparation of high purity methotrexate and derivatives thereof
US4558690A (en) 1982-01-26 1985-12-17 University Of Scranton Method of administration of chemotherapy to tumors
US4662359A (en) 1983-08-12 1987-05-05 Robert T. Gordon Use of magnetic susceptibility probes in the treatment of cancer
FR2564319A1 (fr) 1984-05-21 1985-11-22 Inst Nat Sante Rech Med Nouvelles compositions de liposomes dotees d'une action specifique vis-a-vis de la proliferation de cellules donnees
US4584375A (en) 1984-08-21 1986-04-22 Rensselaer Polytechnic Institute Fluorine-containing antifolates incapable of polyglutamate formation
FR2590255B1 (fr) 1985-11-19 1987-12-24 Rhone Poulenc Sante Procede de preparation de derives de la pteridine
US5225539A (en) 1986-03-27 1993-07-06 Medical Research Council Recombinant altered antibodies and methods of making altered antibodies
CA2057635A1 (en) 1990-12-14 1992-06-15 Hiroshi Akimoto Condensed heterocyclic compounds, their production and use
US5646253A (en) 1994-03-08 1997-07-08 Memorial Sloan-Kettering Cancer Center Recombinant human anti-LK26 antibodies
US5639641A (en) 1992-09-09 1997-06-17 Immunogen Inc. Resurfacing of rodent antibodies
US6569432B1 (en) * 1995-02-24 2003-05-27 Sloan-Kettering Institute For Cancer Research Prostate-specific membrane antigen and uses thereof
US5795587A (en) 1995-01-23 1998-08-18 University Of Pittsburgh Stable lipid-comprising drug delivery complexes and methods for their production
WO1997027764A1 (en) 1996-01-31 1997-08-07 South Alabama Medical Science Foundation Food and vitamin preparations containing the natural isomer of reduced folates
US20020168761A1 (en) 2000-01-24 2002-11-14 Gour Barbara J. Peptidomimetic modulators of cell adhesion
US20030073640A1 (en) 1997-07-23 2003-04-17 Ribozyme Pharmaceuticals, Inc. Novel compositions for the delivery of negatively charged molecules
US5912251A (en) 1998-01-17 1999-06-15 Nair; Madhavan G. Metabolically inert anti-inflammatory and anti-tumor antifolates
US20050031679A1 (en) 1998-03-27 2005-02-10 Clemens Unger Method for producing liposomal formulations of active ingredients
CN1239545C (zh) 1998-07-09 2006-02-01 罗狄亚化学公司 水溶性或水可分散性接枝共聚物
WO2001005405A1 (en) 1999-07-16 2001-01-25 The General Hospital Corporation Folylpolyglutamyl synthetase gene transfer to enhance antifolate drug sensitivity
CN1095472C (zh) 2000-04-17 2002-12-04 上海复康医药科技发展有限公司 叶酸-多聚糖复合物,其制备方法和以该复合物为活性成分的药物组合物
EP1286661A2 (en) 2000-06-09 2003-03-05 OSI Pharmaceuticals, Inc. Liposomal benzoquinazoline thymidylate synthase inhibitor formulations
JP5102928B2 (ja) 2000-06-30 2012-12-19 イーライ リリー アンド カンパニー 新規な葉酸代謝拮抗薬の組み合わせ療法
JP2004501955A (ja) 2000-06-30 2004-01-22 アイネックス ファーマシューティカルズ コーポレイション リポソーム抗新生物薬剤およびその使用
US20050048512A1 (en) 2001-04-26 2005-03-03 Avidia Research Institute Combinatorial libraries of monomer domains
US20050053973A1 (en) 2001-04-26 2005-03-10 Avidia Research Institute Novel proteins with targeted binding
US20040175756A1 (en) 2001-04-26 2004-09-09 Avidia Research Institute Methods for using combinatorial libraries of monomer domains
AU2003211103A1 (en) * 2002-02-13 2003-09-04 Northeastern University Intracellular delivery of therapeutic agents
CH696628A5 (de) 2002-02-26 2007-08-31 Eprova Ag Verwendung von Folaten zur Herstellung einer Zubereitung geeignet zur Vorbeugung und Behandlung von Entzündungen und entzündungsassoziierter Krankheiten, im Speziellen zur Beeinflussung der
US7563590B2 (en) 2002-08-30 2009-07-21 Cypress Bioscience Inc. Methods of quantifying methotrexate metabolites
DK1587907T3 (da) 2003-01-07 2011-04-04 Dyax Corp Kunitz-domænebibliotek
US6921667B2 (en) 2003-03-07 2005-07-26 Prometheus Laboratories, Inc. Methods for direct detection of individual methotrexate metabolites
US20040265368A1 (en) 2003-04-02 2004-12-30 Lawrence Mayer Combination compositions of camptothecins and fluoropyrimidines
AU2005206163B2 (en) 2004-01-14 2011-06-30 Gilead Sciences, Inc. Lipid-based dispersions useful for drug delivery
EP3101034A1 (en) 2004-02-12 2016-12-07 Morphotek, Inc. Monoclonal antibodies that specifically bind to folate receptor alpha
US7612071B2 (en) 2004-03-12 2009-11-03 Syntrix Biosystems, Inc. Compositions and methods employing aminopterin
US20080260812A1 (en) 2004-04-26 2008-10-23 Takami Matsuyama C/O Kagoshima University Therapeutic Medicine Containing Monoclonal Antibody Against Folate Receptor Beta (Fr-Beta)
LT3173073T (lt) * 2004-05-03 2025-01-10 Ipsen Biopharm Ltd. Liposomos, skirtos vaistų pristatymui
US7695908B2 (en) 2004-06-15 2010-04-13 Prometheus Laboratories Inc. Methods for predicting methotrexate polyglutamate levels using pharmacogenetics
US20060008844A1 (en) 2004-06-17 2006-01-12 Avidia Research Institute c-Met kinase binding proteins
JP2008512490A (ja) 2004-09-08 2008-04-24 チェルシー・セラピューティクス,インコーポレイテッド 異常細胞増殖および炎症の障害を治療するための代謝的に不活性な葉酸拮抗剤
JPWO2006035876A1 (ja) 2004-09-29 2008-05-15 興和株式会社 関節リウマチの予防及び/又は治療薬
US8126089B2 (en) 2004-09-30 2012-02-28 Alcatel Lucent Method and apparatus for providing frame synchronization in a digital communication system that supports multiple modulation formats
US20100266709A1 (en) 2004-12-16 2010-10-21 Hicks Terry Lee Compositions and Methods for Treating Burns
WO2006074416A1 (en) * 2005-01-07 2006-07-13 Health Research Inc. 5-amino-4-imidazolecarboxamide riboside and its nucleobase as potentiators of antifolate transport and metabolism
WO2007086881A2 (en) 2005-02-14 2007-08-02 Sirna Therapeutics, Inc. Cationic lipids and formulated molecular compositions containing them
US7404969B2 (en) 2005-02-14 2008-07-29 Sirna Therapeutics, Inc. Lipid nanoparticle based compositions and methods for the delivery of biologically active molecules
JP2006248978A (ja) 2005-03-10 2006-09-21 Mebiopharm Co Ltd 新規なリポソーム製剤
GB2424837B (en) 2005-04-06 2010-10-06 Cilag Ag Int Injection device
AU2005335876A1 (en) 2005-08-24 2007-03-01 Protherics Medicines Development Limited Cleavage of antifolate compounds
EP1962796A2 (en) 2005-12-08 2008-09-03 Yissum Research Development Company Of The Hebrew University Of Jerusalem Methods for affecting liposome composition by ultrasound irradiation
WO2007098089A2 (en) 2006-02-17 2007-08-30 Novacea, Inc. Treatment of hyperproliferative diseases with methotrexate n-oxide and analogs
US9265746B2 (en) 2006-05-31 2016-02-23 Merck & Cie Method for cell-specific targeting
WO2008030818A2 (en) 2006-09-05 2008-03-13 Mebiopharm Co., Ltd. Novel liposome compositions
EP1900752A1 (en) 2006-09-15 2008-03-19 DOMPE' pha.r.ma s.p.a. Human anti-folate receptor alpha antibodies and antibody fragments for the radioimmunotherapy of ovarian carcinoma
GB2453011B (en) 2006-12-29 2010-06-23 Tracon Pharmaceuticals Inc Antifolate agent compositions in the treatment of cancer
RU2423114C2 (ru) 2006-12-29 2011-07-10 Тракон Фармасьютикалз, Инк. Комбинации антифолатного агента в лечении рака
JP2010516694A (ja) 2007-01-19 2010-05-20 チェルシー・セラピューティクス,インコーポレイテッド 新規な伝統的葉酸拮抗剤
CA2689042A1 (en) 2007-02-16 2008-08-28 Merck & Co., Inc. Compositions and methods for potentiated activity of biologicaly active molecules
CN101977620B (zh) 2008-03-18 2014-05-07 英国技术集团国际有限公司 用于治疗类风湿性关节炎或急性骨髓性白血病的环戊二烯并[g]喹唑啉衍生物
GB0811360D0 (en) 2008-06-20 2008-07-30 Imp Innovations Ltd Methods
WO2010021865A1 (en) 2008-08-18 2010-02-25 Merck Sharp & Dohme Corp. Novel lipid nanoparticles and novel components for delivery of nucleic acids
WO2010080724A1 (en) 2009-01-12 2010-07-15 Merck Sharp & Dohme Corp. Novel lipid nanoparticles and novel components for delivery of nucleic acids
EP2437596B1 (en) 2009-06-03 2017-05-03 Ex-Tek, LLC Skin treatment compositions
US8569256B2 (en) 2009-07-01 2013-10-29 Protiva Biotherapeutics, Inc. Cationic lipids and methods for the delivery of therapeutic agents
WO2011000107A1 (en) 2009-07-01 2011-01-06 Protiva Biotherapeutics, Inc. Novel lipid formulations for delivery of therapeutic agents to solid tumors
TW201118098A (en) 2009-08-13 2011-06-01 Reddy S Lab Liimited Dr Processes for preparing pemetrexed
ES2579936T3 (es) 2009-08-20 2016-08-17 Sirna Therapeutics, Inc. Nuevos lípidos catiónicos con diversos grupos de cabeza para el suministro oligonucleotídico
EP2485770A4 (en) 2009-10-08 2013-04-10 Merck Sharp & Dohme Novel cationic lipids with short lipid chains for oligonucleotide delivery
EP2525781A1 (en) 2010-01-22 2012-11-28 Schering Corporation Novel cationic lipids for oligonucleotide delivery
TWI622402B (zh) 2010-02-24 2018-05-01 免疫遺傳股份有限公司 葉酸受體1抗體類和免疫共軛物類及彼等之用途
CN102917690B (zh) 2010-03-19 2016-08-24 麻省理工学院 脂质囊泡组合物和使用方法
EP2394640A1 (en) 2010-05-21 2011-12-14 MediGene AG Improved liposomal formulations of lipophilic compounds
US8802863B2 (en) 2010-05-24 2014-08-12 Sirna Therapeutics, Inc. Amino alcohol cationic lipids for oligonucleotide delivery
CA2800693A1 (en) 2010-05-28 2011-12-01 Purdue Research Foundation Delivery of therapeutic agents to inflamed tissues using folate-targeted agents
DK2575767T3 (en) 2010-06-04 2017-03-13 Sirna Therapeutics Inc HOWEVER UNKNOWN LOW MOLECULAR CATIONIC LIPIDS TO PROCESS OIGONUCLEOTIDES
KR101761388B1 (ko) 2010-07-30 2017-07-25 큐어백 아게 트랜스펙션 및 면역 자극을 위한 이황화-크로스링크된 양이온 성분 및 핵산의 복합체
WO2012033987A2 (en) 2010-09-09 2012-03-15 Purdue Research Foundation Anti-human folate receptor beta antibodies and methods of use
WO2012037068A1 (en) 2010-09-13 2012-03-22 De Novo Diagnostics, Inc. Methods for monitoring methotrexate therapy
CA2809858C (en) 2010-09-20 2019-11-12 Sirna Therapeutics, Inc. Novel low molecular weight cationic lipids for oligonucleotide delivery
CA2811430A1 (en) 2010-09-30 2012-04-05 Merck Sharp & Dohme Corp. Low molecular weight cationic lipids for oligonucleotide delivery
EP3485913A1 (en) 2010-10-21 2019-05-22 Sirna Therapeutics, Inc. Low molecular weight cationic lipids for oligonucleotide delivery
WO2012061469A2 (en) 2010-11-02 2012-05-10 Sicor Inc. Crystalline forms of pralatrexate
WO2012061259A2 (en) 2010-11-05 2012-05-10 Merck Sharp & Dohme Corp. Novel low molecular weight cyclic amine containing cationic lipids for oligonucleotide delivery
MX343607B (es) 2010-11-05 2016-11-11 Morphotek Inc Receptor alfa de folato como marcador de diagnóstico y pronóstico para cánceres que expresan receptor alfa de folato.
WO2012078708A1 (en) 2010-12-07 2012-06-14 Chelsea Therapeutics, Inc. Combination comprising methotrexate and an antifolate compound
WO2012118806A2 (en) 2011-02-28 2012-09-07 The Regents Of The University Of California Compositions and methods for detecting and treating cancer
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
WO2012121682A2 (en) 2011-03-10 2012-09-13 National Science And Technology Development Agency Anti-folate antimalarials with dual-binding modes and their preparation
US8673914B2 (en) 2011-03-28 2014-03-18 St. John's University Use of phosphodiesterase inhibitors for treating multidrug resistance
EP2508894A1 (en) 2011-04-05 2012-10-10 Receptomon LLC Method for monitoring gene expression of translation and Integral/Secretory protein synthesis by magnetic resonance spectroscopy (MRS)
ES2795110T3 (es) 2011-06-08 2020-11-20 Translate Bio Inc Lípidos escindibles
US8183227B1 (en) 2011-07-07 2012-05-22 Chemo S. A. France Compositions, kits and methods for nutrition supplementation
RS61235B1 (sr) 2011-07-13 2021-01-29 Yissum Res Dev Co Of Hebrew Univ Jerusalem Ltd Lipozomi koji ko-inkapsuliraju bisfosfonat i amfipatički agens
SI2731972T1 (en) 2011-07-15 2018-04-30 Eisai R&D Management Co., Ltd. Anti-folate receptor alpha antibodies and uses thereof
US20130122096A1 (en) 2011-11-14 2013-05-16 Silenseed Ltd. Compositions for drug delivery and methods of manufacturing and using same
JPWO2014003137A1 (ja) 2012-06-27 2016-06-02 旭化成メディカル株式会社 高アフィニティー抗体、及びその製造方法
WO2014016740A2 (en) 2012-07-23 2014-01-30 Fresenius Kabi Oncology Ltd. Improved process for the preparation of pralatrexate
US20140120157A1 (en) 2012-09-19 2014-05-01 Georgetown University Targeted liposomes
WO2014046630A1 (en) 2012-09-19 2014-03-27 Keskin, Dilek Tumor targeted liposomal drug delivery system
US9207238B2 (en) 2012-12-07 2015-12-08 Kyowa Hakko Kirin Co., Ltd. Anti-FOLR1 antibody
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
US9192609B2 (en) 2013-04-17 2015-11-24 Hedgepath Pharmaceuticals, Inc. Treatment and prognostic monitoring of proliferation disorders using hedgehog pathway inhibitors
SG11201509043RA (en) 2013-05-14 2015-12-30 Immunogen Inc Anti-folr1 immunoconjugate dosing regimens
RS61907B1 (sr) 2015-04-06 2021-06-30 Subdomain Llc Polipeptidi koji sadrže de novo vezujući domen i njihova primena
JOP20170004B1 (ar) 2016-01-15 2022-09-15 Lilly Co Eli الأجسام المضادة لببتيد بيتا النشوي مضاد N3pGlu واستخداماته
WO2017189961A1 (en) 2016-04-29 2017-11-02 Memorial Sloan Kettering Cancer Center Compositions and methods for targeted particle penetration, distribution, and response in malignant brain tumors
WO2018031968A1 (en) 2016-08-12 2018-02-15 L.E.A.F. Holdings Group Llc Alpha and gamma-d polyglutamated antifolates and uses thereof
WO2018031980A1 (en) * 2016-08-12 2018-02-15 L.E.A.F. Holdings Group Llc Polyglutamated antifolates and uses thereof
ES3062820T3 (en) * 2017-11-08 2026-04-14 L E A F Holdings Group Llc Platinum complexes 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
EP3749314A4 (en) 2018-02-07 2022-02-23 L.E.A.F Holdings Group LLC ALPHA-POLYGLUTAMATE METHOTREXATE AND ITS USES
WO2019157145A1 (en) 2018-02-07 2019-08-15 L.E.A.F. Holdings Group Llc Gamma polyglutamated pemetrexed and uses thereof
EP3749318A4 (en) 2018-02-07 2022-07-06 L.E.A.F Holdings Group LLC GAMMA-POLYGLUTAMATED RALTITREXED AND ITS USES
EP3749321A4 (en) * 2018-02-07 2022-03-09 L.E.A.F Holdings Group LLC Gamma 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
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
US12310966B2 (en) 2018-02-07 2025-05-27 L.E.A.F. Holdings Group Llc Alpha 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
US12350271B2 (en) 2018-02-14 2025-07-08 L.E.A.F. Holdings Group Llc Gamma polyglutamated aminopterin and uses thereof
CA3090753A1 (en) 2018-02-14 2019-08-22 L.E.A.F. Holdings Group Llc Gamma polyglutamated pralatrexate and uses thereof
WO2019160735A1 (en) 2018-02-14 2019-08-22 L.E.A.F. Holdings Group Llc Gamma polyglutamated tetrahydrofolates and uses thereof
US20230000997A1 (en) 2019-08-06 2023-01-05 L.E.A.F. Holdings Group Llc Processes of preparing polyglutamated antifolates and uses of their compositions

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2013526545A (ja) 2010-05-13 2013-06-24 パシラ ファーマシューティカルズ インコーポレーテッド 疾患修飾性抗リウマチ薬(dmard)および抗癌剤としてのメトトレキサートの持続性放出製剤
JP2017526744A (ja) 2014-08-14 2017-09-14 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L.E.A.F. Holdings Group Llc リポソームカプセル化親和性薬物
JP2019524885A (ja) 2016-08-12 2019-09-05 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L.E.A.F. Holdings Group Llc ポリグルタミン酸化抗葉酸剤およびその使用

Non-Patent Citations (5)

* Cited by examiner, † Cited by third party
Title
Drug Resistance Updates,2012年,15,183-210
Journal of Controlled Release,2015年,220,29-36
Journal of Medicinal Chemistry,1990年,33(2),711-717
Molecular Pharmaceutics,2014年,11,2631-2639
The Journal of Clinical Investigation,1985年,Vol.76,pp.907-912

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WO2019160733A1 (en) 2019-08-22

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