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

Info

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
Authority
CN
China
Prior art keywords
alpha
composition
pemetrexed
cancer
glutamyl
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
CN201980024908.7A
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 CN111954531A publication Critical patent/CN111954531A/zh
Pending legal-status Critical Current

Links

Images

Classifications

    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Immunology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Organic Chemistry (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Molecular Biology (AREA)
  • Biophysics (AREA)
  • Biochemistry (AREA)
  • Genetics & Genomics (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
US62/627,741 2018-02-07
US62/627,703 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
US62/702,732 2018-07-24
US62/702,561 2018-07-24
US201862764943P 2018-08-17 2018-08-17
US201862764955P 2018-08-17 2018-08-17
US62/764,955 2018-08-17
US62/764,943 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

Family

ID=67549083

Family Applications (1)

Application Number Title Priority Date Filing Date
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

Country Status (5)

Country Link
US (2) US11779584B2 (https=)
EP (1) EP3749317A4 (https=)
JP (3) JP7491572B2 (https=)
CN (1) CN111954531A (https=)
WO (1) WO2019157138A1 (https=)

Families Citing this family (25)

* 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
EP3749319A4 (en) 2018-02-07 2022-06-22 L.E.A.F Holdings Group LLC TETRAHYDROFOLATES ALPHA POLYGLUTAMATE AND THEIR USES
US12246015B2 (en) 2018-02-07 2025-03-11 L.E.A.F. Holdings Group Llc Alpha 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
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
CA3090500A1 (en) * 2018-02-07 2019-08-15 L.E.A.F. Holdings Group Llc Alpha polyglutamated antifolates and uses thereof
US12239734B2 (en) 2018-02-07 2025-03-04 L.E.A.F. Holdings Group Llc Gamma polyglutamated raltitrexed 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
US12220431B2 (en) 2018-02-07 2025-02-11 L.E.A.F. Holdings Group Llc Gamma polyglutamated antifolates 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
WO2019157129A1 (en) 2018-02-07 2019-08-15 L.E.A.F. Holdings Group Llc Alpha polyglutamated pralatrexate 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
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
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
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
KR102821508B1 (ko) 2018-04-10 2025-06-16 셀렉타 바이오사이언시스, 인코퍼레이티드 인지질-플라베글린 접합체 및 표적화된 암 치료를 위해 이를 사용하는 방법
CA3154192A1 (en) 2019-10-10 2021-04-15 Cellectar Biosciences, Inc. Phospholipid-flavagline conjugates and methods of using the same for targeted cancer therapy
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

Citations (6)

* 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
WO2006029385A2 (en) * 2004-09-08 2006-03-16 Chelsea Therapeutics, Inc. Quinazoline derivatives as metabolically inert antifolate compounds.
US20110262948A1 (en) * 2002-08-30 2011-10-27 Exagen Diagnostics, Inc. Methods of Quantifying Methotrexate Metabolites
US20120142692A1 (en) * 2010-12-07 2012-06-07 Chelsea Therapeutics, Inc. Antifolate combinations
WO2016025882A2 (en) * 2014-08-14 2016-02-18 L.E.A.F Holdings Group Llc. Liposome encapsulated affinity drug
CN109689104A (zh) * 2016-08-12 2019-04-26 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

Family Cites Families (124)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
KR0162654B1 (ko) 1989-12-11 1998-11-16 알렌 제이. 시니스갤리 N-(피롤로[2,3-d]피리미딘-3-일아크릴)-글루타민산 유도체
EP0492316A1 (en) 1990-12-14 1992-07-01 Takeda Chemical Industries, Ltd. Condensed heterocyclic oligoglutamate derivatives, their production and pharmaceutical compositions containing them
JP3202999B2 (ja) 1991-01-31 2001-08-27 協和醗酵工業株式会社 肝移行性リポソーム製剤
US5646253A (en) 1994-03-08 1997-07-08 Memorial Sloan-Kettering Cancer Center Recombinant human anti-LK26 antibodies
US5416211A (en) 1992-09-25 1995-05-16 Eli Lilly And Company Process for preparing 5-substituted pyrrolo-[2,3-d]pyrimidines
US5795587A (en) 1995-01-23 1998-08-18 University Of Pittsburgh Stable lipid-comprising drug delivery complexes and methods for their production
CN1122456C (zh) 1996-01-31 2003-10-01 南亚拉巴马医学科学基金会 含有天然的还原叶酸盐异构体的食品和维生素制品
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
ZA987550B (en) 1997-09-26 2000-02-21 Lilly Co Eli Processes and intermediates useful to make antifolates.
US6262262B1 (en) 1997-09-26 2001-07-17 Eli Lilly And Company Processes and intermediates useful to make antifolates
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
AU5283099A (en) 1998-07-09 2000-02-01 Rhodia Chimie Water-soluble or water-dispersible grafted copolymers
US6066732A (en) 1998-08-21 2000-05-23 The Trustees Of Princeton University Process for the preparation of pyrrolo[2,3-d]pyrimidines
US7244448B2 (en) 2000-06-30 2007-07-17 Tekmira Pharmaceuticals Corporation Liposomal antineoplastic drugs and uses thereof
WO2001005405A1 (en) 1999-07-16 2001-01-25 The General Hospital Corporation Folylpolyglutamyl synthetase gene transfer to enhance antifolate drug sensitivity
EP1212325A2 (en) 1999-08-23 2002-06-12 Eli Lilly And Company A novel crystalline form of disodium n-[4-[2-(2-amino-4,7-dihydro-4-oxo-3h-pyrrolo[2,3-d]-pyrimidin-5-yl)ethyl]benzoyl]-l-glutamic acid salt and processes therefor
PT1259513E (pt) 2000-02-25 2004-02-27 Lilly Co Eli Nova forma cristalina de acido n-¬4- ¬2-amino-4,7-dihidro -4-oxo-3h-pirrolo¬2,3-d|pirimidin-5-il)etil| - benzoil|-l-glutamico e processo para a sua obtencao
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
AU7526901A (en) 2000-06-09 2001-12-24 Gilead Sciences Inc Liposomal benzoquinazoline thymidylate synthase inhibitor formulations
EP1313508B1 (en) 2000-06-30 2007-04-18 Eli Lilly And Company Combination containing an antifolate and methylmalonic acid lowering agent
US20050163832A1 (en) 2002-02-13 2005-07-28 Vladimir Torchilin 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
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
NZ548195A (en) 2004-01-14 2011-01-28 Gilead Sciences Inc Lipid-based dispersions useful for drug delivery
CA2556027C (en) 2004-02-12 2015-11-24 Morphotek, Inc. Monoclonal antibodies that specifically block biological activity of a tumor antigen
US7612071B2 (en) 2004-03-12 2009-11-03 Syntrix Biosystems, Inc. Compositions and methods employing aminopterin
WO2005103250A1 (ja) 2004-04-26 2005-11-03 Takami Matsuyama 葉酸リセプターベータ（FR-β）に対する単クローン抗体を含有する治療薬
CA2928387A1 (en) 2004-05-03 2005-11-17 Merrimack Pharmaceuticals, Inc. Drug delivery liposomes containing anionic polyols or anionic sugars
US7695908B2 (en) 2004-06-15 2010-04-13 Prometheus Laboratories Inc. Methods for predicting methotrexate polyglutamate levels using pharmacogenetics
WO2006035876A1 (ja) 2004-09-29 2006-04-06 Kowa Co., Ltd. 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
JP5042863B2 (ja) 2005-02-14 2012-10-03 サーナ・セラピューティクス・インコーポレイテッド 生物学的に活性な分子をデリバリーするための脂質ナノ粒子系組成物および方法
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
CA2619992A1 (en) * 2005-08-24 2007-03-01 Protherics Medicines Development Limited Cleavage of antifolate compounds
US20090155345A1 (en) 2005-12-08 2009-06-18 Ben Gurion University Of The Negev Research And Development Authority Methods for affecting liposome composition 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
EP1957497B1 (en) 2006-08-14 2015-09-30 Sicor, Inc. Processes for preparing intermediates of pemetrexed
KR20090052355A (ko) 2006-08-14 2009-05-25 시코르, 인크. 순도가 높은 페메트렉세드 이산 및 이의 제조 방법
WO2008030818A2 (en) 2006-09-05 2008-03-13 Mebiopharm Co., Ltd. Novel liposome compositions
RU2423114C2 (ru) 2006-12-29 2011-07-10 Тракон Фармасьютикалз, Инк. Комбинации антифолатного агента в лечении рака
KR101195366B1 (ko) 2006-12-29 2012-11-21 트라콘 파마수티칼즈, 인코포레이티드 암치료에서의 항엽산제 조합물
BRPI0806632A2 (pt) 2007-01-19 2011-09-06 Chelsea Therapeutics Inc composto, composição farmacêutica, método para o tratamento de uma condição selecionada a partir do grupo constituìdo de proliferação celular anormal, inflamação, asma e artrite
US20100015218A1 (en) 2007-02-16 2010-01-21 Vasant Jadhav Compositions and methods for potentiated activity of biologically active molecules
BRPI0807939A2 (pt) 2007-04-03 2014-07-01 Reddys Lab Ltd Dr Formas sólidas de pemetrexed
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
US20110224447A1 (en) 2008-08-18 2011-09-15 Bowman Keith A 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
WO2010141711A1 (en) 2009-06-03 2010-12-09 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
ES2613498T3 (es) 2009-07-01 2017-05-24 Protiva Biotherapeutics Inc. Nuevas formulaciones de lípidos para el suministro de agentes terapéuticos a tumores sólidos
TW201118098A (en) 2009-08-13 2011-06-01 Reddy S Lab Liimited Dr Processes for preparing pemetrexed
EP2467357B1 (en) 2009-08-20 2016-03-30 Sirna Therapeutics, Inc. Novel cationic lipids with various head groups for oligonucleotide delivery
US20120253032A1 (en) 2009-10-08 2012-10-04 Merck Sharp & Dohme Corporation Novel cationic lipids with short lipid chains for oligonucleotide delivery
US20130116419A1 (en) 2010-01-22 2013-05-09 Daniel Zewge Post-synthetic chemical modification of rna at the 2'-position of the ribose ring via "click" chemistry
CN103037900B (zh) 2010-02-24 2016-04-06 伊缪诺金公司 叶酸受体1抗体与免疫缀合物以及其用途
JP5686886B2 (ja) 2010-03-19 2015-03-18 マサチューセッツ インスチテュート オブ テクノロジーＭａｓｓａｃｈｕｓｅｔｔｓ Ｉｎｓｔｉｔｕｔｅ Ｏｆ Ｔｅｃｈｎｏｌｏｇｙ 脂質小胞組成物及び使用方法
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
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
US8748667B2 (en) 2010-06-04 2014-06-10 Sirna Therapeutics, Inc. Low molecular weight cationic lipids for oligonucleotide delivery
IT1401677B1 (it) 2010-07-22 2013-08-02 Chemi Spa Nuovo processo per la sintesi di pemetrexed sale disodico
CA2801523C (en) 2010-07-30 2021-08-03 Curevac Gmbh Complexation of nucleic acids with disulfide-crosslinked cationic components for transfection and immunostimulation
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
ES2888231T3 (es) 2010-09-20 2022-01-03 Sirna Therapeutics Inc Lípidos catiónicos de bajo peso molecular para el suministro de oligonucleótidos
EP2621480B1 (en) 2010-09-30 2018-08-15 Sirna Therapeutics, Inc. Low molecular weight cationic lipids for oligonucleotide delivery
JP2013545727A (ja) 2010-10-21 2013-12-26 メルク・シャープ・アンド・ドーム・コーポレーション オリゴヌクレオチド送達用の新規低分子量カチオン性脂質
WO2012056285A1 (en) 2010-10-25 2012-05-03 Fresenius Kabi Oncology Ltd. An improved process for the preparation of pemetrexed
WO2012061469A2 (en) 2010-11-02 2012-05-10 Sicor Inc. Crystalline forms of pralatrexate
EP2635265B1 (en) 2010-11-05 2018-04-04 Sirna Therapeutics, Inc. Novel low molecular weight cyclic amine containing cationic lipids for oligonucleotide delivery
AU2011323124C1 (en) 2010-11-05 2016-09-22 Eisai Inc. Folate receptor alpha as a diagnostic and prognostic marker for folate receptor alpha-expressing cancers
US20140086939A1 (en) 2011-02-28 2014-03-27 Michael Karin 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)
EP3354644A1 (en) 2011-06-08 2018-08-01 Translate Bio, Inc. Cleavable lipids
US8183227B1 (en) 2011-07-07 2012-05-22 Chemo S. A. France Compositions, kits and methods for nutrition supplementation
PT2731591T (pt) 2011-07-13 2020-09-18 Yissum Res Dev Co Of Hebrew Univ Jerusalem Ltd Lipossomas que coencapsulam um bisfosfonato e um agente anfipático
PL2731972T3 (pl) 2011-07-15 2018-06-29 Eisai R&D Management Co., Ltd. Przeciwciała skierowane przeciwko receptorowi folianowemu alfa i ich zastosowania
EP2591770B1 (en) 2011-11-14 2016-03-16 Silenseed Ltd Compositions for siRNA delivery and methods of manufacturing and using same
US20150239956A1 (en) 2012-06-27 2015-08-27 Asahi Kasei Medical Co., Ltd. High-affinity antibody and method for manufacturing the same
WO2014016740A2 (en) 2012-07-23 2014-01-30 Fresenius Kabi Oncology Ltd. Improved process for the preparation of pralatrexate
ITRM20120398A1 (it) 2012-08-08 2014-02-09 Berlin Chemie Ag Procedimento di sintesi pemetrexed e suo sale di lisina.
WO2014046630A1 (en) 2012-09-19 2014-03-27 Keskin, Dilek Tumor targeted liposomal drug delivery system
US20140120157A1 (en) 2012-09-19 2014-05-01 Georgetown University Targeted liposomes
JP6224619B2 (ja) 2012-12-07 2017-11-01 協和発酵キリン株式会社 抗ｆｏｌｒ１抗体
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
CA2911499A1 (en) 2013-05-14 2014-11-20 Immunogen, Inc. Anti-folr1 immunoconjugate dosing regimens
JOP20170004B1 (ar) 2016-01-15 2022-09-15 Lilly Co Eli الأجسام المضادة لببتيد بيتا النشوي مضاد N3pGlu واستخداماته
CN109069666B (zh) 2016-04-29 2023-04-04 纪念斯隆凯特琳癌症中心 使靶向颗粒穿透、分布和响应于恶性脑肿瘤中的组合物和方法
WO2018031979A1 (en) * 2016-08-12 2018-02-15 L.E.A.F. Holdings Group Llc Alpha and gamma-d polyglutamated antifolates and uses thereof
WO2018031968A1 (en) 2016-08-12 2018-02-15 L.E.A.F. Holdings Group Llc Alpha and gamma-d polyglutamated antifolates and uses thereof
US20190231690A1 (en) 2017-11-08 2019-08-01 L.E.A.F. Holdings Group Llc Platinum complexes 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
CA3090500A1 (en) 2018-02-07 2019-08-15 L.E.A.F. Holdings Group Llc Alpha polyglutamated antifolates 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
EP3749319A4 (en) 2018-02-07 2022-06-22 L.E.A.F Holdings Group LLC TETRAHYDROFOLATES ALPHA POLYGLUTAMATE AND THEIR USES
WO2019157129A1 (en) 2018-02-07 2019-08-15 L.E.A.F. Holdings Group Llc Alpha polyglutamated pralatrexate 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
US12239734B2 (en) 2018-02-07 2025-03-04 L.E.A.F. Holdings Group Llc Gamma polyglutamated raltitrexed and uses thereof
US12246015B2 (en) 2018-02-07 2025-03-11 L.E.A.F. Holdings Group Llc Alpha polyglutamated raltitrexed 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
WO2019157123A1 (en) 2018-02-07 2019-08-15 L.E.A.F. Holdings Group Llc Alpha polyglutamated aminopterin and uses thereof
EP3752157A4 (en) 2018-02-14 2022-07-06 L.E.A.F Holdings Group LLC GAMMA-POLYGLUTAMATED LOMETREXOLE 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
EP3752156A4 (en) 2018-02-14 2021-10-27 L.E.A.F Holdings Group LLC GAMMA-POLYGLUTAMIZED PRALATREXATE AND USES THEREOF
US12048766B2 (en) 2018-02-14 2024-07-30 L.E.A.F. Holdings Group Llc Gamma polyglutamated tetrahydrofolates and uses thereof
CA3149914A1 (en) 2019-08-06 2021-02-11 L.E.A.F. Holdings Group Llc Processes of preparing polyglutamated antifolates and uses of their compositions

Patent Citations (8)

* 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
US20110262948A1 (en) * 2002-08-30 2011-10-27 Exagen Diagnostics, Inc. Methods of Quantifying Methotrexate Metabolites
WO2006029385A2 (en) * 2004-09-08 2006-03-16 Chelsea Therapeutics, Inc. Quinazoline derivatives as metabolically inert antifolate compounds.
US20120142692A1 (en) * 2010-12-07 2012-06-07 Chelsea Therapeutics, Inc. Antifolate combinations
WO2016025882A2 (en) * 2014-08-14 2016-02-18 L.E.A.F Holdings Group Llc. Liposome encapsulated affinity drug
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
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
CN109689104A (zh) * 2016-08-12 2019-04-26 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

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
CHUAN SHIH ET AL.: ""LY231514，a pyrrolo[2,3-d]pyrimidine-based antifolate that inhibits multiple folate-requiring enzymes"" *
邱丽颖等, 中国医药科技出版社 *

Also Published As

Publication number Publication date
JP7491572B2 (ja) 2024-05-28
CA3090494A1 (en) 2019-08-15
US20240173321A1 (en) 2024-05-30
EP3749317A1 (en) 2020-12-16
JP7678625B2 (ja) 2025-05-16
JP2021512895A (ja) 2021-05-20
EP3749317A4 (en) 2022-06-22
US12433893B2 (en) 2025-10-07
JP2024099050A (ja) 2024-07-24
US20200360388A1 (en) 2020-11-19
US11779584B2 (en) 2023-10-10
JP2025105820A (ja) 2025-07-10
WO2019157138A1 (en) 2019-08-15

Similar Documents

Publication Publication Date Title
JP7674773B2 (ja) ガンマポリグルタミン酸化ペメトレキセドおよびその使用
JP7678625B2 (ja) 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
US12213981B2 (en) Alpha polyglutamated pralatrexate and uses thereof
US20250213577A1 (en) Alpha polyglutamated lometrexol and uses thereof
US20250213476A1 (en) Gamma polyglutamated raltitrexed and uses thereof
US20240252498A1 (en) Gamma polyglutamated lometrexol and uses thereof
US20260053807A1 (en) Alpha polyglutamated aminopterin and uses thereof
US20250082575A1 (en) Gamma polyglutamated pralatrexate and uses thereof
US20250213567A1 (en) Alpha polyglutamated raltitrexed and uses thereof
US12128046B2 (en) Alpha polyglutamated methotrexate and uses thereof
JP2024056882A (ja) γポリグルタミン酸化テトラヒドロ葉酸およびその使用
CN111936145A (zh) γ聚谷氨酸化氨甲蝶呤及其用途
CN111867593A (zh) α聚谷氨酸化抗叶酸剂及其用途
CN111936147A (zh) γ聚谷氨酸化抗叶酸剂及其用途
CN111936146A (zh) α聚谷氨酸化四氢叶酸及其用途
US20250198442A1 (en) Gamma polyglutamated pemetrexed 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