AU2005282241B2 - Quinazoline derivatives as metabolically inert antifolate compounds. - Google Patents

Quinazoline derivatives as metabolically inert antifolate compounds. Download PDF

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Publication number
AU2005282241B2
AU2005282241B2 AU2005282241A AU2005282241A AU2005282241B2 AU 2005282241 B2 AU2005282241 B2 AU 2005282241B2 AU 2005282241 A AU2005282241 A AU 2005282241A AU 2005282241 A AU2005282241 A AU 2005282241A AU 2005282241 B2 AU2005282241 B2 AU 2005282241B2
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Prior art keywords
disease
agents
alkyl
alkynyl
independently
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AU2005282241A
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AU2005282241A1 (en
Inventor
Simon Pedder
Michael J. Roberts
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Lundbeck NA Ltd
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Chelsea Therapeutics Inc
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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
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • 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
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    • 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
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    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A—HUMAN NECESSITIES
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    • A61P15/02—Drugs for genital or sexual disorders; Contraceptives for disorders of the vagina
    • A—HUMAN NECESSITIES
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    • A—HUMAN NECESSITIES
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    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/12—Antihypertensives

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Diabetes (AREA)
  • Pulmonology (AREA)
  • Immunology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Dermatology (AREA)
  • Urology & Nephrology (AREA)
  • Hematology (AREA)
  • Endocrinology (AREA)
  • Psychiatry (AREA)
  • Obesity (AREA)
  • Rheumatology (AREA)
  • Reproductive Health (AREA)
  • Ophthalmology & Optometry (AREA)
  • Emergency Medicine (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychology (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Gynecology & Obstetrics (AREA)
  • Vascular Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
AU2005282241A 2004-09-08 2005-09-08 Quinazoline derivatives as metabolically inert antifolate compounds. Ceased AU2005282241B2 (en)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US60788304P 2004-09-08 2004-09-08
US60/607,883 2004-09-08
US61148204P 2004-09-20 2004-09-20
US60/611,482 2004-09-20
PCT/US2005/032352 WO2006029385A2 (en) 2004-09-08 2005-09-08 Quinazoline derivatives as metabolically inert antifolate compounds.

Related Child Applications (1)

Application Number Title Priority Date Filing Date
AU2011202657A Division AU2011202657A1 (en) 2004-09-08 2011-06-03 Quinazoline derivatives as metabolically inert antifolate compounds

Publications (2)

Publication Number Publication Date
AU2005282241A1 AU2005282241A1 (en) 2006-03-16
AU2005282241B2 true AU2005282241B2 (en) 2011-03-03

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Application Number Title Priority Date Filing Date
AU2005282241A Ceased AU2005282241B2 (en) 2004-09-08 2005-09-08 Quinazoline derivatives as metabolically inert antifolate compounds.

Country Status (6)

Country Link
US (3) US7829708B2 (enExample)
EP (1) EP1791544A4 (enExample)
JP (1) JP2008512490A (enExample)
AU (1) AU2005282241B2 (enExample)
CA (1) CA2579096C (enExample)
WO (1) WO2006029385A2 (enExample)

Families Citing this family (83)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6702949B2 (en) 1997-10-24 2004-03-09 Microdiffusion, Inc. Diffuser/emulsifier for aquaculture applications
CN100522989C (zh) 2002-09-11 2009-08-05 中外制药株式会社 纯化蛋白质的方法
WO2006014293A2 (en) * 2004-07-02 2006-02-09 Aqualizer, Llc Moisture condensation control system
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
US20070135380A1 (en) 2005-08-12 2007-06-14 Radiorx, Inc. O-nitro compounds, pharmaceutical compositions thereof and uses thereof
US7507842B2 (en) 2005-08-12 2009-03-24 Radiorx, Inc. Cyclic nitro compounds, pharmaceutical compositions thereof and uses thereof
US7745587B2 (en) * 2005-12-30 2010-06-29 Dyax Corp. Antibodies that bind MMP-14
WO2007081981A2 (en) * 2006-01-11 2007-07-19 Attune Foods Probiotic food, process for its preparation and dietary regimen
EP1880723A1 (en) * 2006-07-14 2008-01-23 Novartis AG Combination of mTOR inhibitor and antifolate compound
JP2009523149A (ja) * 2006-01-12 2009-06-18 ノバルティス アクチエンゲゼルシャフト mTOR阻害剤および抗葉酸化合物の組み合わせ
GB0608821D0 (en) * 2006-05-04 2006-06-14 Chroma Therapeutics Ltd DHFR enzyme inhibitors
CA2655933C (en) 2006-06-23 2014-09-09 Alethia Biotherapeutics Inc. Polynucleotides and polypeptide sequences involved in cancer
US7820689B2 (en) * 2006-08-10 2010-10-26 Hua-Lin Wu Methods and compositions for preventing or treating cardiovascular disease
AU2007308840C1 (en) 2006-10-25 2014-09-25 Revalesio Corporation Methods of therapeutic treatment of eyes and other human tissues using an oxygen-enriched solution
US8445546B2 (en) 2006-10-25 2013-05-21 Revalesio Corporation Electrokinetically-altered fluids comprising charge-stabilized gas-containing nanostructures
EP2086668B1 (en) 2006-10-25 2016-11-16 Revalesio Corporation Mixing device and method
AU2008206161A1 (en) * 2007-01-19 2008-07-24 Chelsea Therapeutics, Inc. New classical antifolates
US9523090B2 (en) 2007-10-25 2016-12-20 Revalesio Corporation Compositions and methods for treating inflammation
US9745567B2 (en) 2008-04-28 2017-08-29 Revalesio Corporation Compositions and methods for treating multiple sclerosis
US20090227018A1 (en) * 2007-10-25 2009-09-10 Revalesio Corporation Compositions and methods for modulating cellular membrane-mediated intracellular signal transduction
US10125359B2 (en) 2007-10-25 2018-11-13 Revalesio Corporation Compositions and methods for treating inflammation
CA2707637A1 (en) 2007-12-17 2009-06-25 Dyax Corp. Compositions and methods for treating osteolytic disorders comprising mmp-14 binding proteins
CA2718330A1 (en) * 2008-04-07 2009-10-15 Chelsea Therapeutics, Inc. Antifolate compositions
EP2285347A4 (en) 2008-05-01 2011-09-21 Revalesio Corp COMPOSITIONS AND METHODS OF TREATING DISORDERS OF THE DIGESTION SYSTEM
WO2010048432A1 (en) * 2008-10-22 2010-04-29 Dyax Corp. Combination treatments comprising protease binding proteins for inflammatory disorders
CN104829714A (zh) 2008-11-03 2015-08-12 阿莱斯亚生物疗法股份有限公司 特异性地阻滞肿瘤抗原的生物活性的抗体
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
US8815292B2 (en) 2009-04-27 2014-08-26 Revalesio Corporation Compositions and methods for treating insulin resistance and diabetes mellitus
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.
US9364507B2 (en) 2009-08-11 2016-06-14 Imagilin Technology, Llc Probiotic enhancement of steroid and immune suppressor activity in mammals with chronic diseases
WO2011031676A2 (en) * 2009-09-10 2011-03-17 Mayo Foundation For Medical Education And Research Depleting immunosuppressive monocytes within a mammal
WO2011056957A2 (en) * 2009-11-06 2011-05-12 Chelsea Therapeutics, Inc. Enzyme inhibiting compounds
MX2012005711A (es) * 2009-11-17 2012-10-05 Cipla Ltd Soluciones de inhalacion.
EP2505188A1 (en) * 2009-12-02 2012-10-03 Bettina Heil Suppository for rectal, vaginal or urethral administration
US8471041B2 (en) * 2010-02-09 2013-06-25 Alliant Techsystems Inc. Methods of synthesizing and isolating N-(bromoacetyl)-3,3-dinitroazetidine and a composition including the same
US20110237609A1 (en) * 2010-03-29 2011-09-29 Chelsea Therapeutics, Inc. Antifolate compositions
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
AU2011289172B2 (en) 2010-08-12 2015-09-24 Revalesio Corporation Compositions and methods for treatment of taupathy
US8658652B2 (en) * 2010-12-07 2014-02-25 Chelsea Therapeutics, Inc. Antifolate combinations
US20120149678A1 (en) * 2010-12-09 2012-06-14 Oronsky Bryan T Organonitro Compounds for Use in Treating Non-Hodgkin's Lymphoma and Leukemia, and Methods Relating Thereto
CA2893376A1 (en) 2011-03-31 2012-10-04 Alethia Biotherapeutics Inc. Antibodies against kidney associated antigen 1 and antigen binding fragemnts thereof
US8664247B2 (en) 2011-08-26 2014-03-04 Radiorx, Inc. Acyclic organonitro compounds for use in treating cancer
US20140308260A1 (en) 2011-10-07 2014-10-16 Radiorx, Inc. Methods and compositions comprising a nitrite-reductase promoter for treatment of medical disorders and preservation of blood products
WO2013052164A1 (en) 2011-10-07 2013-04-11 Radiorx, Inc. Organonitro thioether compounds and medical uses thereof
US10314909B2 (en) 2011-10-21 2019-06-11 Dyax Corp. Combination therapy comprising an MMP-14 binding protein
CN107050457A (zh) 2012-01-06 2017-08-18 翁特拉制药公司 游离酸形式的ω‑3多不饱和脂肪酸的富含dpa组合物
AU2013209234B2 (en) 2012-01-09 2017-11-09 Adc Therapeutics Sa Method for treating breast cancer
US9091868B2 (en) 2012-08-08 2015-07-28 Kinestral Technologies, Inc. Electrochromic multi-layer devices with composite current modulating structure
US9091895B2 (en) * 2012-08-08 2015-07-28 Kinestral Technologies, Inc. Electrochromic multi-layer devices with composite electrically conductive layers
WO2014025921A1 (en) 2012-08-08 2014-02-13 Kinestral Technologies, Inc. Electrochromic multi-layer devices with current modulating structure
AU2015209133B2 (en) 2014-01-24 2019-10-03 AI Therapeutics, Inc. Apilimod compositions and methods for using same
CN107249638B (zh) 2014-11-07 2021-05-14 人工智能治疗公司 阿匹莫德用于治疗肾癌
ES2734081T3 (es) 2014-11-07 2019-12-04 Ai Therapeutics Inc Apilimod para el uso en el tratamiento de melanoma
US9822190B2 (en) * 2015-01-29 2017-11-21 Shaker A. Mousa Compositions and method for anti-sickling of red blood cells in sickle cell disease
US10342778B1 (en) 2015-10-20 2019-07-09 Epicentrx, Inc. Treatment of brain metastases using organonitro compound combination therapy
US9987270B1 (en) 2015-10-29 2018-06-05 Epicentrix, Inc. Treatment of gliomas using organonitro compound combination therapy
DK3402480T3 (da) 2016-01-11 2021-06-28 Epicentrx Inc Sammensætninger og fremgangsmåder til intravenøs administration af 2-brom-1-(3,3-dinitroazetidin-1-yl)ethanon
KR102584446B1 (ko) 2016-08-12 2023-10-04 엘.이.에이.에프. 홀딩스 그룹 엘엘씨. 알파 및 감마-d 폴리글루타메이트화 항엽산 및 이의 용도
US20180236098A1 (en) 2016-08-12 2018-08-23 L.E.A.F. Holdings Group Llc Alpha and gamma-d polyglutamated antifolates and uses thereof
WO2018071741A1 (en) 2016-10-14 2018-04-19 Epicentrix, Inc. Sulfoxyalkyl organonitro and related compounds and pharmaceutical compositions for use in medicine
US10016425B2 (en) 2016-11-03 2018-07-10 King Saud University Anti-ulcerative colitis compound
MX2020000265A (es) 2017-07-07 2020-07-22 Epicentrx Inc Composiciones para la administración parenteral de agentes terapéuticos.
WO2019164593A2 (en) 2018-01-08 2019-08-29 Epicentrx, Inc. Methods and compositions utilizing rrx-001 combination therapy for radioprotection
US12246019B2 (en) 2018-02-07 2025-03-11 L.E.A.F. Holdings Group Llc Alpha polyglutamated lometrexol and uses thereof
WO2019157129A1 (en) 2018-02-07 2019-08-15 L.E.A.F. Holdings Group Llc Alpha polyglutamated pralatrexate and uses thereof
WO2019157133A1 (en) 2018-02-07 2019-08-15 L.E.A.F. Holdings Group Llc Alpha polyglutamated raltitrexed and uses thereof
CA3090384A1 (en) 2018-02-07 2019-08-15 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
CA3090391A1 (en) 2018-02-07 2019-08-15 L.E.A.F. Holdings Group Llc Gamma polyglutamated raltitrexed and uses thereof
EP3749317A4 (en) * 2018-02-07 2022-06-22 L.E.A.F Holdings Group LLC PEMETREXED ALPHA-POLYGLUTAMATE AND ASSOCIATED USES
US12246018B2 (en) 2018-02-07 2025-03-11 L.E.A.F. Holdings Group Llc Gamma polyglutamated pemetrexed and uses thereof
WO2019157146A1 (en) 2018-02-07 2019-08-15 L.E.A.F. Holdings Group Llc Alpha polyglutamated antifolates and uses thereof
WO2019157148A1 (en) * 2018-02-07 2019-08-15 L.E.A.F. Holdings Group Llc Gamma polyglutamated antifolates 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
JP7514533B2 (ja) 2018-02-07 2024-07-11 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テトラヒドロ葉酸およびその使用
CA3090943A1 (en) 2018-02-14 2019-08-22 L.E.A.F. Holdings Group Llc Gamma polyglutamated aminopterin and uses thereof
US12048767B2 (en) 2018-02-14 2024-07-30 L.E.A.F. Holdings Group Llc Gamma polyglutamated pralatrexate and uses thereof
US12290518B2 (en) 2018-02-14 2025-05-06 L.E.A.F. Holdings Group Llc Gamma polyglutamated methotrexate and uses thereof
CA3090875A1 (en) 2018-02-14 2019-08-22 L.E.A.F. Holdings Group Llc Gamma polyglutamated lometrexol and uses thereof
JP7442822B2 (ja) 2018-02-14 2024-03-05 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 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
US10751345B2 (en) 2018-02-21 2020-08-25 AI Therapeutics, Inc. Combination therapy with apilimod and glutamatergic agents
US12589097B2 (en) 2018-02-21 2026-03-31 OrphAl Therapeutics Inc. Apilimod compositions and methods of use
CN112058287B (zh) * 2020-08-25 2023-04-18 浙江工业大学 一种二维金属硒化物@MXene复合电催化剂的原位制备方法

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5912251A (en) * 1998-01-17 1999-06-15 Nair; Madhavan G. Metabolically inert anti-inflammatory and anti-tumor antifolates

Family Cites Families (25)

* 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
US5028554A (en) * 1986-07-03 1991-07-02 Oki Electric Industry Co., Ltd. Process of fabricating an MIS FET
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
US5248775A (en) 1989-12-11 1993-09-28 The Trustees Of Princeton University Pyrrolo(2,3-d)pyrimidines
US5028608A (en) 1989-12-11 1991-07-02 The Trustees Of Princeton University N-(6-Amino-(pyrrolo(2,3-d)pyrimidin-3-ylacyl) )-glutamic acid derivatives
KR0162654B1 (ko) 1989-12-11 1998-11-16 알렌 제이. 시니스갤리 N-(피롤로[2,3-d]피리미딘-3-일아크릴)-글루타민산 유도체
US5073554A (en) 1990-01-18 1991-12-17 Nair Madhavan G Two non-polyglutamatable antifolates
US4996207A (en) 1990-01-18 1991-02-26 Nair Madhavan G Three new non-polyglutamatable deazaaminopterins
US5508281A (en) * 1991-04-08 1996-04-16 Duquesne University Of The Holy Ghost Derivatives of pyrido [2,3-d] and [3,2-d] pyrimidine and methods of using these derivatives
WO1993013079A1 (en) 1991-12-20 1993-07-08 Agouron Pharmaceuticals, Inc. Antifolate quinazolines
IL108630A0 (en) * 1993-02-18 1994-05-30 Fmc Corp Insecticidal substituted 2,4-diaminoquinazolines
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)
AU7904998A (en) * 1997-07-07 1999-02-08 Peptichemio Ag Pharmaceutical composition containing peptichemio
US6048736A (en) * 1998-04-29 2000-04-11 Kosak; Kenneth M. Cyclodextrin polymers for carrying and releasing drugs
DE60136926D1 (de) * 2000-05-02 2009-01-22 Theravance Inc Zusammensetzung die eine zyklodextrin und ein glykopeptid-antibiotikum enthält
IL155683A0 (en) 2000-11-28 2003-11-23 Genentech Inc Lfa-1 antagonist compounds
DE60211670T2 (de) 2001-04-04 2006-10-26 Bionumerik Pharmaceuticals, Inc., San Antonio Verfahren zur kupplung von aminosäuren an das gerüst eines folsäureantagonisten
US20030181635A1 (en) 2002-03-22 2003-09-25 Harry Kochat Process for coupling amino acids to an antifolate scaffold
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
US7612071B2 (en) * 2004-03-12 2009-11-03 Syntrix Biosystems, Inc. Compositions and methods employing aminopterin
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
US7687473B2 (en) 2005-01-07 2010-03-30 Health Research, Inc. 5-amino-4-imidazolecarboxamide riboside and its nucleobase as potentiators of antifolate transport and metabolism

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5912251A (en) * 1998-01-17 1999-06-15 Nair; Madhavan G. Metabolically inert anti-inflammatory and anti-tumor antifolates

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