DE69940881D1 - Metabolisch inerte antifolate mit entzündungshemmender und anti-tumor wirkung - Google Patents

Metabolisch inerte antifolate mit entzündungshemmender und anti-tumor wirkung

Info

Publication number
DE69940881D1
DE69940881D1 DE69940881T DE69940881T DE69940881D1 DE 69940881 D1 DE69940881 D1 DE 69940881D1 DE 69940881 T DE69940881 T DE 69940881T DE 69940881 T DE69940881 T DE 69940881T DE 69940881 D1 DE69940881 D1 DE 69940881D1
Authority
DE
Germany
Prior art keywords
inflammatory
tumor effect
metabolic
antifolate
inert antifolate
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.)
Expired - Lifetime
Application number
DE69940881T
Other languages
German (de)
English (en)
Inventor
Madhavan G Nair
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.)
Individual
Original Assignee
Individual
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 Individual filed Critical Individual
Application granted granted Critical
Publication of DE69940881D1 publication Critical patent/DE69940881D1/de
Anticipated expiration legal-status Critical
Expired - Lifetime legal-status Critical Current

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72Quinazolines; Hydrogenated quinazolines
    • C07D239/95Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in positions 2 and 4
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

Landscapes

  • 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)
DE69940881T 1998-01-17 1999-01-13 Metabolisch inerte antifolate mit entzündungshemmender und anti-tumor wirkung Expired - Lifetime DE69940881D1 (de)

Applications Claiming Priority (2)

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
PCT/US1999/000948 WO1999036409A1 (en) 1998-01-17 1999-01-13 Metabolically inert anti-inflammatory and anti-tumor antifolates

Publications (1)

Publication Number Publication Date
DE69940881D1 true DE69940881D1 (de) 2009-06-25

Family

ID=21732611

Family Applications (1)

Application Number Title Priority Date Filing Date
DE69940881T Expired - Lifetime DE69940881D1 (de) 1998-01-17 1999-01-13 Metabolisch inerte antifolate mit entzündungshemmender und anti-tumor wirkung

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
Publication number Priority date Publication date Assignee Title
JP5079969B2 (ja) * 2001-04-04 2012-11-21 バイオニューメリック・ファーマスーティカルズ・インコーポレイテッド 葉酸拮抗剤骨格へのアミノ酸のカップリング方法
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
CA2579096C (en) * 2004-09-08 2012-11-13 Chelsea Therapeutics, Inc. Quinazoline derivatives as metabolically inert antifolate compounds
WO2008089390A1 (en) * 2007-01-19 2008-07-24 Chelsea Therapeutics, Inc. New classical antifolates
WO2009126637A1 (en) * 2008-04-07 2009-10-15 Chelsea Therapeutics, Inc. Antifolate compositions
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
JP2013510163A (ja) * 2009-11-06 2013-03-21 チェルシー・セラピューティクス,インコーポレイテッド 酵素阻害化合物
WO2012064377A1 (en) 2010-03-29 2012-05-18 Chelsea Therapeutics, Inc. Antifolate compositions
US8658652B2 (en) 2010-12-07 2014-02-25 Chelsea Therapeutics, Inc. Antifolate combinations
WO2018031968A1 (en) 2016-08-12 2018-02-15 L.E.A.F. Holdings Group Llc Alpha and gamma-d polyglutamated antifolates and uses thereof
EP4052729A1 (en) 2016-08-12 2022-09-07 L.E.A.F Holdings Group LLC Alpha and gamma-d polyglutamated antifolates and uses thereof
CA3090384A1 (en) 2018-02-07 2019-08-15 L.E.A.F. Holdings Group Llc Alpha polyglutamated aminopterin and uses thereof
WO2019157125A1 (en) 2018-02-07 2019-08-15 L.E.A.F. Holdings Group Llc Alpha polyglutamated methotrexate and uses thereof
WO2019157138A1 (en) 2018-02-07 2019-08-15 L.E.A.F. Holdings Group Llc Alpha polyglutamated pemetrexed and uses thereof
CN111936146A (zh) 2018-02-07 2020-11-13 L.E.A.F.控股集团公司 α聚谷氨酸化四氢叶酸及其用途
WO2019157133A1 (en) 2018-02-07 2019-08-15 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
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
WO2019157129A1 (en) 2018-02-07 2019-08-15 L.E.A.F. Holdings Group Llc Alpha polyglutamated pralatrexate and uses thereof
EP3749318A4 (en) 2018-02-07 2022-07-06 L.E.A.F Holdings Group LLC GAMMA-POLYGLUTAMATED RALTITREXED AND ITS USES
EP3749312A4 (en) 2018-02-07 2022-02-23 L.E.A.F Holdings Group LLC ALPHA-POLYGLUTAMATED LOMETREXOLE AND USES THEREOF
JP7490239B2 (ja) 2018-02-07 2024-05-27 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ペメトレキセドおよびその使用
US12048767B2 (en) 2018-02-14 2024-07-30 L.E.A.F. Holdings Group Llc Gamma polyglutamated pralatrexate and uses thereof
EP3752157A4 (en) 2018-02-14 2022-07-06 L.E.A.F Holdings Group LLC GAMMA-POLYGLUTAMATED LOMETREXOLE AND USES THEREOF
EP3755335A4 (en) 2018-02-14 2022-06-22 L.E.A.F Holdings Group LLC GAMMA POLYGLUTAMIC TETRAHYDROFOLATES AND THEIR USES
US12350271B2 (en) 2018-02-14 2025-07-08 L.E.A.F. Holdings Group Llc Gamma polyglutamated aminopterin 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

Family Cites Families (7)

* Cited by examiner, † Cited by third party
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
JP2830008B2 (ja) * 1988-04-01 1998-12-02 武田薬品工業株式会社 縮合ピリミジン誘導体
US4996207A (en) * 1990-01-18 1991-02-26 Nair Madhavan G Three new non-polyglutamatable deazaaminopterins
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
US5593999A (en) * 1995-06-07 1997-01-14 Nair; Madhavan G. Non-classical folate analogue inhibitors of glycinamide ribonucleotide formyltransferase (GARFT)

Also Published As

Publication number Publication date
US5912251A (en) 1999-06-15
EP1062209B1 (en) 2009-05-13
WO1999036409A1 (en) 1999-07-22
EP1062209A4 (en) 2002-02-27
JP4854850B2 (ja) 2012-01-18
JP2002509139A (ja) 2002-03-26
EP1062209A1 (en) 2000-12-27
EP1535911A1 (en) 2005-06-01

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