JP4854850B2 - 代謝的に不活性な抗炎症性および抗腫瘍性葉酸拮抗剤 - Google Patents

代謝的に不活性な抗炎症性および抗腫瘍性葉酸拮抗剤 Download PDF

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JP4854850B2
JP4854850B2 JP2000540125A JP2000540125A JP4854850B2 JP 4854850 B2 JP4854850 B2 JP 4854850B2 JP 2000540125 A JP2000540125 A JP 2000540125A JP 2000540125 A JP2000540125 A JP 2000540125A JP 4854850 B2 JP4854850 B2 JP 4854850B2
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pharmaceutically acceptable
deoxy
amino
acceptable salt
pharmaceutical composition
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JP2002509139A5 (https=
JP2002509139A (ja
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ネア，マドヘイヴァン，ジー
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72—Quinazolines; Hydrogenated quinazolines
    • C07D239/95—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in positions 2 and 4
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

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  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pulmonology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
JP2000540125A 1998-01-17 1999-01-13 代謝的に不活性な抗炎症性および抗腫瘍性葉酸拮抗剤 Expired - Lifetime JP4854850B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US09/008,613 US5912251A (en) 1998-01-17 1998-01-17 Metabolically inert anti-inflammatory and anti-tumor antifolates
US09/008,613 1998-01-17
PCT/US1999/000948 WO1999036409A1 (en) 1998-01-17 1999-01-13 Metabolically inert anti-inflammatory and anti-tumor antifolates

Publications (3)

Publication Number Publication Date
JP2002509139A JP2002509139A (ja) 2002-03-26
JP2002509139A5 JP2002509139A5 (https=) 2007-01-11
JP4854850B2 true JP4854850B2 (ja) 2012-01-18

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JP2000540125A Expired - Lifetime JP4854850B2 (ja) 1998-01-17 1999-01-13 代謝的に不活性な抗炎症性および抗腫瘍性葉酸拮抗剤

Country Status (5)

Country Link
US (1) US5912251A (https=)
EP (2) EP1062209B1 (https=)
JP (1) JP4854850B2 (https=)
DE (1) DE69940881D1 (https=)
WO (1) WO1999036409A1 (https=)

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AU2002306824B2 (en) * 2001-04-04 2007-10-25 Bionumerik Pharmaceuticals, Inc. Process for coupling amino acids to an antifolate scaffold
GB0219897D0 (en) * 2002-08-27 2002-10-02 Melacure Therapeutics Ab Pharmaceutically active compounds
US7563590B2 (en) * 2002-08-30 2009-07-21 Cypress Bioscience Inc. Methods of quantifying methotrexate metabolites
US20040092739A1 (en) * 2002-11-13 2004-05-13 Zejun Xiao Process for synthesizing antifolates
US7060825B2 (en) * 2003-07-25 2006-06-13 Bionumerik Pharmaceuticals, Inc. Process for synthesizing 6-quinazolinyl-ethyl-benzoyl and related antifolates
US20050032807A1 (en) * 2003-08-06 2005-02-10 Rosenwald Lindsay A. Methods of treating inflammatory diseases with ammonium salts of ornitihine derivatives
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
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
KR20100132061A (ko) * 2008-04-07 2010-12-16 첼시 쎄라퓨틱스, 인코포레이티드 항엽산제 화합물의 결정 염 형태 및 이의 제조 방법
US20100260825A1 (en) * 2009-04-13 2010-10-14 Nair Madhavan G Antifolates for the treatment of cardiovascular, inflammatory, neoplastic, autoimmune and related diseases in sublingual dosage units, film strips, or skin patches
MX2012000437A (es) * 2009-07-08 2012-02-21 Chelsea Therapeutics Inc Polimorfos cristalinos estables de la sal dipotasica de acido (s)-2-{2,4-diamono-quizolin-6-il)-etil]-benzoilamino}-4-metilen-p entanodioico.
AU2010315152A1 (en) 2009-11-06 2012-06-14 Chelsea Therapeutics, Inc. Enzyme inhibiting compounds
US20110237609A1 (en) * 2010-03-29 2011-09-29 Chelsea Therapeutics, Inc. Antifolate compositions
WO2012078708A1 (en) 2010-12-07 2012-06-14 Chelsea Therapeutics, Inc. Combination comprising methotrexate and an antifolate compound
WO2018031968A1 (en) 2016-08-12 2018-02-15 L.E.A.F. Holdings Group Llc Alpha and gamma-d polyglutamated antifolates and uses thereof
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
EP3749318A4 (en) 2018-02-07 2022-07-06 L.E.A.F Holdings Group LLC GAMMA-POLYGLUTAMATED RALTITREXED AND ITS USES
US12310966B2 (en) 2018-02-07 2025-05-27 L.E.A.F. Holdings Group Llc Alpha polyglutamated aminopterin 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
WO2019157121A1 (en) 2018-02-07 2019-08-15 L.E.A.F. Holdings Group Llc Alpha polyglutamated lometrexol and uses thereof
WO2019157145A1 (en) 2018-02-07 2019-08-15 L.E.A.F. Holdings Group Llc Gamma polyglutamated pemetrexed and uses thereof
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
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
WO2019160735A1 (en) 2018-02-14 2019-08-22 L.E.A.F. Holdings Group Llc Gamma polyglutamated tetrahydrofolates and uses thereof
WO2019160734A1 (en) 2018-02-14 2019-08-22 L.E.A.F. Holdings Group Llc Gamma polyglutamated lometrexol 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
US12350271B2 (en) 2018-02-14 2025-07-08 L.E.A.F. Holdings Group Llc Gamma polyglutamated aminopterin and uses thereof

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPH0228162A (ja) * 1988-04-01 1990-01-30 Takeda Chem Ind Ltd 縮合ピリミジン誘導体
US5073554A (en) * 1990-01-18 1991-12-17 Nair Madhavan G Two non-polyglutamatable antifolates
US5550128A (en) * 1994-09-09 1996-08-27 Nair; Madhavan G. Enantiomers of gamma methylene 10-deaza aminopterin and process for preparing the same

Family Cites Families (4)

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GB8607683D0 (en) * 1986-03-27 1986-04-30 Ici Plc Anti-tumor agents
US4818753A (en) * 1987-09-18 1989-04-04 Sri International Synthesis and method of use for 2, 4 diaminoquinazoline
US4996207A (en) * 1990-01-18 1991-02-26 Nair Madhavan G Three new non-polyglutamatable deazaaminopterins
US5593999A (en) * 1995-06-07 1997-01-14 Nair; Madhavan G. Non-classical folate analogue inhibitors of glycinamide ribonucleotide formyltransferase (GARFT)

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPH0228162A (ja) * 1988-04-01 1990-01-30 Takeda Chem Ind Ltd 縮合ピリミジン誘導体
US5073554A (en) * 1990-01-18 1991-12-17 Nair Madhavan G Two non-polyglutamatable antifolates
US5550128A (en) * 1994-09-09 1996-08-27 Nair; Madhavan G. Enantiomers of gamma methylene 10-deaza aminopterin and process for preparing the same

Also Published As

Publication number Publication date
WO1999036409A1 (en) 1999-07-22
DE69940881D1 (de) 2009-06-25
EP1062209B1 (en) 2009-05-13
EP1062209A4 (en) 2002-02-27
JP2002509139A (ja) 2002-03-26
EP1062209A1 (en) 2000-12-27
US5912251A (en) 1999-06-15
EP1535911A1 (en) 2005-06-01

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