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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JP2002509139A (ja
JP2002509139A5 (enExample
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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 (enExample) 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 (enExample)
EP (2) EP1062209B1 (enExample)
JP (1) JP4854850B2 (enExample)
DE (1) DE69940881D1 (enExample)
WO (1) WO1999036409A1 (enExample)

Families Citing this family (32)

* Cited by examiner, † Cited by third party
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WO2002081455A1 (en) * 2001-04-04 2002-10-17 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
US7829708B2 (en) * 2004-09-08 2010-11-09 Chelsea Therapeutics, Inc. Metabolically inert antifolates for treating disorders of abnormal cellular proliferation and inflammation
US7951812B2 (en) * 2007-01-19 2011-05-31 Chelsea Therapeutics, Inc. Substituted pyrrolo[2,3-d]pyrimidines as antifolates
CA2718544A1 (en) * 2008-04-07 2009-10-15 Chelsea Therapeutics, Inc. Crystalline salt forms of antifolate compounds and methods of manufacturing thereof
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
CA2767257A1 (en) * 2009-07-08 2011-01-13 Chelsea Therapeutics, Inc. Stable crystalline polymorphs of the dipotassium salt of (s)-2-{4-[2-(2,4-diamino-quinazolin-6-yl)-ethyl]-benzoylamino}-4-methylene-penta nedioic acid
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
CA3177187A1 (en) 2016-08-12 2018-02-15 L.E.A.F Holdings Group Llc Alpha and gamma-d polyglutamated antifolates and uses thereof
WO2018031967A1 (en) 2016-08-12 2018-02-15 L.E.A.F. Holdings Group Llc Polyglutamated antifolates and uses thereof
EP3749320A4 (en) 2018-02-07 2022-03-09 L.E.A.F Holdings Group LLC ALPHA-POLYGLUTAMATED AMINOPTERIN AND ITS USES
EP3749317A4 (en) 2018-02-07 2022-06-22 L.E.A.F Holdings Group LLC PEMETREXED ALPHA-POLYGLUTAMATE AND ASSOCIATED USES
US12220431B2 (en) 2018-02-07 2025-02-11 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
CA3090391A1 (en) 2018-02-07 2019-08-15 L.E.A.F. Holdings Group Llc Gamma polyglutamated raltitrexed and uses thereof
WO2019157145A1 (en) 2018-02-07 2019-08-15 L.E.A.F. Holdings Group Llc Gamma polyglutamated pemetrexed and uses thereof
US12076402B2 (en) 2018-02-07 2024-09-03 L.E.A.F. Holdings Group Llc Alpha polyglutamated antifolates and uses thereof
CA3090381A1 (en) 2018-02-07 2019-08-15 L.E.A.F. Holdings Group Llc Alpha polyglutamated lometrexol and uses thereof
US12128046B2 (en) 2018-02-07 2024-10-29 L.E.A.F. Holdings Group Llc Alpha polyglutamated methotrexate and uses thereof
CA3090506A1 (en) 2018-02-07 2019-08-15 L.E.A.F. Holdings Group Llc Alpha polyglutamated tetrahydrofolates and uses thereof
WO2019157133A1 (en) 2018-02-07 2019-08-15 L.E.A.F. Holdings Group Llc Alpha polyglutamated raltitrexed 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
EP3752156A4 (en) 2018-02-14 2021-10-27 L.E.A.F Holdings Group LLC GAMMA-POLYGLUTAMIZED PRALATREXATE AND USES THEREOF
CA3090992A1 (en) 2018-02-14 2019-08-22 L.E.A.F. Holdings Group Llc Gamma polyglutamated tetrahydrofolates and uses thereof
EP3752157A4 (en) 2018-02-14 2022-07-06 L.E.A.F Holdings Group LLC GAMMA-POLYGLUTAMATED LOMETREXOLE 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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Publication number Priority date Publication date Assignee Title
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
JP2002509139A (ja) 2002-03-26
DE69940881D1 (de) 2009-06-25
EP1062209A1 (en) 2000-12-27
EP1062209B1 (en) 2009-05-13
EP1535911A1 (en) 2005-06-01
US5912251A (en) 1999-06-15
WO1999036409A1 (en) 1999-07-22
EP1062209A4 (en) 2002-02-27

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