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

Quinazoline derivatives as metabolically inert antifolate compounds. Download PDF

Info

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
Authority
AU
Australia
Prior art keywords
disease
agents
alkyl
alkynyl
independently
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.)
Ceased
Application number
AU2005282241A
Other languages
English (en)
Other versions
AU2005282241A1 (en
Inventor
Simon Pedder
Michael J. Roberts
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.)
Lundbeck NA Ltd
Original Assignee
Chelsea Therapeutics Inc
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 Chelsea Therapeutics Inc filed Critical Chelsea Therapeutics Inc
Publication of AU2005282241A1 publication Critical patent/AU2005282241A1/en
Application granted granted Critical
Publication of AU2005282241B2 publication Critical patent/AU2005282241B2/en
Anticipated expiration legal-status Critical
Ceased 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
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • 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
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/16Central respiratory analeptics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • A61P15/02Drugs for genital or sexual disorders; Contraceptives for disorders of the vagina
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/02Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/18Antioxidants, e.g. antiradicals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16Anti-Parkinson drugs
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • 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
    • A61P3/00Drugs for disorders of the metabolism
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04Antibacterial agents
    • 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
    • A61P37/00Drugs for immunological or allergic disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/08Antiallergic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/08Vasodilators for multiple indications
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/12Antihypertensives

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Pulmonology (AREA)
  • Immunology (AREA)
  • Diabetes (AREA)
  • Dermatology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Urology & Nephrology (AREA)
  • Endocrinology (AREA)
  • Hematology (AREA)
  • Reproductive Health (AREA)
  • Obesity (AREA)
  • Rheumatology (AREA)
  • Psychiatry (AREA)
  • Ophthalmology & Optometry (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Vascular Medicine (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychology (AREA)
  • Pain & Pain Management (AREA)
  • Physical Education & Sports Medicine (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

Family

ID=36037042

Family Applications (1)

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 (OSRAM)
EP (1) EP1791544A4 (OSRAM)
JP (1) JP2008512490A (OSRAM)
AU (1) AU2005282241B2 (OSRAM)
CA (1) CA2579096C (OSRAM)
WO (1) WO2006029385A2 (OSRAM)

Families Citing this family (82)

* 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
ES2558303T3 (es) 2002-09-11 2016-02-03 Chugai Seiyaku Kabushiki Kaisha Método de purificación de proteínas
WO2006014293A2 (en) * 2004-07-02 2006-02-09 Aqualizer, Llc Moisture condensation control system
CA2579096C (en) 2004-09-08 2012-11-13 Chelsea Therapeutics, Inc. Quinazoline derivatives as metabolically inert antifolate compounds
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
ES2524015T3 (es) 2005-12-30 2014-12-03 Dyax Corporation Proteínas de enlazamiento a la metaloproteinasa
WO2007081981A2 (en) * 2006-01-11 2007-07-19 Attune Foods Probiotic food, process for its preparation and dietary regimen
AU2007204410A1 (en) * 2006-01-12 2007-07-19 Novartis Ag Combination of mTOR inhibitor and antipolate compound
EP1880723A1 (en) * 2006-07-14 2008-01-23 Novartis AG Combination of mTOR inhibitor and antifolate compound
GB0608821D0 (en) * 2006-05-04 2006-06-14 Chroma Therapeutics Ltd DHFR enzyme inhibitors
EP3231442B1 (en) 2006-06-23 2019-12-25 ADC Therapeutics SA 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
US8445546B2 (en) 2006-10-25 2013-05-21 Revalesio Corporation Electrokinetically-altered fluids comprising charge-stabilized gas-containing nanostructures
EP2097107B1 (en) 2006-10-25 2016-05-04 Revalesio Corporation Therapeutic treatment of eyes using an oxygen-enriched solution
JP5306214B2 (ja) 2006-10-25 2013-10-02 リバルシオ コーポレイション 混合装置
WO2008089390A1 (en) * 2007-01-19 2008-07-24 Chelsea Therapeutics, Inc. New classical antifolates
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
US9523090B2 (en) 2007-10-25 2016-12-20 Revalesio Corporation Compositions and methods for treating inflammation
US10125359B2 (en) 2007-10-25 2018-11-13 Revalesio Corporation Compositions and methods for treating inflammation
US8147836B2 (en) 2007-12-17 2012-04-03 Dyax Corp. Compositions and methods for treating osteolytic disorders comprising MMP-14 binding proteins
WO2009126637A1 (en) * 2008-04-07 2009-10-15 Chelsea Therapeutics, Inc. Antifolate compositions
CN102076327B (zh) 2008-05-01 2014-04-16 利发利希奥公司 治疗消化功能紊乱的组合物和方法
WO2010048432A1 (en) * 2008-10-22 2010-04-29 Dyax Corp. Combination treatments comprising protease binding proteins for inflammatory disorders
WO2010060186A1 (en) 2008-11-03 2010-06-03 Alethia Biotherapeutics Inc. Antibodies that specifically block the biological activity of a tumor antigen
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
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
US9364507B2 (en) 2009-08-11 2016-06-14 Imagilin Technology, Llc Probiotic enhancement of steroid and immune suppressor activity in mammals with chronic diseases
US9289469B2 (en) * 2009-09-10 2016-03-22 Mayo Foundation For Medical Education And Research Depleting immunosuppressive monocytes within a mammal
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
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
WO2012064377A1 (en) * 2010-03-29 2012-05-18 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
MX2013001636A (es) 2010-08-12 2013-05-01 Revalesio Corp Composiciones y metodos para el tratamiento de taupatias
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
PL3173427T3 (pl) 2011-03-31 2019-11-29 Adc Therapeutics Sa Przeciwciała przeciwko antygenowi związanemu z nerkami 1 i ich fragmenty wiążące antygen
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
EP2763667B1 (en) 2011-10-07 2022-10-26 EpicentRx, Inc. Organonitro thioether compounds and medical uses thereof
WO2013059439A2 (en) 2011-10-21 2013-04-25 Dyax Corp. Combination therapy comprising an mmp-14 binding protein
JP6399655B2 (ja) 2012-01-06 2018-10-03 オムセラ・ファーマシューティカルズ・インコーポレイテッド 遊離酸型のオメガ−3多価不飽和脂肪酸のdpa濃縮組成物
AU2013209234B2 (en) 2012-01-09 2017-11-09 Adc Therapeutics Sa Method for treating breast cancer
WO2014025913A1 (en) 2012-08-08 2014-02-13 Kinestral Technologies, Inc. Electrochromic multi-layer devices with composite current modulating structure
US9507233B2 (en) 2012-08-08 2016-11-29 Kinestral Technologies, Inc. Electrochromic multi-layer devices with current modulating structure
US9091895B2 (en) 2012-08-08 2015-07-28 Kinestral Technologies, Inc. Electrochromic multi-layer devices with composite electrically conductive layers
JP6855243B2 (ja) * 2014-01-24 2021-04-07 エイアイ・セラピューティクス・インコーポレーテッド 癌治療のためのアピリモド(apilimod)組成物
ES2741399T3 (es) 2014-11-07 2020-02-10 Ai Therapeutics Inc Apilimod para el uso en el tratamiento de cáncer renal
WO2016073884A1 (en) 2014-11-07 2016-05-12 Lam Therapeutics, Inc. Apilimod for use in the treatment of colorectal cancer
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
EA201891606A1 (ru) 2016-01-11 2019-02-28 Эписентарикс, Инк. Композиции и способы для внутривенного введения 2-бром-1-(3,3-динитроазетидин-1-ил)этанона
EP4052729A1 (en) 2016-08-12 2022-09-07 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
JP7332469B2 (ja) 2016-10-14 2023-08-23 エピセントアールエックス,インコーポレイテッド スルホキシアルキル有機窒素および関連のある化合物ならびに医学における使用のための医薬組成物
US10016425B2 (en) 2016-11-03 2018-07-10 King Saud University Anti-ulcerative colitis compound
WO2019010447A1 (en) 2017-07-07 2019-01-10 Epicentrx, Inc. COMPOSITIONS FOR PARENTERAL ADMINISTRATION OF THERAPEUTIC AGENTS
WO2019164593A2 (en) 2018-01-08 2019-08-29 Epicentrx, Inc. Methods and compositions utilizing rrx-001 combination therapy for radioprotection
WO2019157133A1 (en) 2018-02-07 2019-08-15 L.E.A.F. Holdings Group Llc Alpha polyglutamated raltitrexed 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
WO2019157148A1 (en) * 2018-02-07 2019-08-15 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
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
US12220431B2 (en) 2018-02-07 2025-02-11 L.E.A.F. Holdings Group Llc Gamma polyglutamated antifolates and uses thereof
EP3749312A4 (en) 2018-02-07 2022-02-23 L.E.A.F Holdings Group LLC ALPHA-POLYGLUTAMATED LOMETREXOLE AND USES THEREOF
WO2019157125A1 (en) 2018-02-07 2019-08-15 L.E.A.F. Holdings Group Llc Alpha polyglutamated methotrexate and uses thereof
EP3749318A4 (en) 2018-02-07 2022-07-06 L.E.A.F Holdings Group LLC GAMMA-POLYGLUTAMATED RALTITREXED AND ITS USES
CA3090384A1 (en) 2018-02-07 2019-08-15 L.E.A.F. Holdings Group Llc Alpha 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
EP3755335A4 (en) 2018-02-14 2022-06-22 L.E.A.F Holdings Group LLC GAMMA POLYGLUTAMIC TETRAHYDROFOLATES AND THEIR USES
EP3752157A4 (en) 2018-02-14 2022-07-06 L.E.A.F Holdings Group LLC GAMMA-POLYGLUTAMATED LOMETREXOLE AND USES THEREOF
US12350271B2 (en) 2018-02-14 2025-07-08 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
EP3755332A1 (en) 2018-02-21 2020-12-30 AI Therapeutics, Inc. Combination therapy with apilimod and glutamatergic agents
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
KR0162654B1 (ko) 1989-12-11 1998-11-16 알렌 제이. 시니스갤리 N-(피롤로[2,3-d]피리미딘-3-일아크릴)-글루타민산 유도체
US4996206A (en) 1989-12-11 1991-02-26 The Trustees Of Princeton University N-(pyrrolo[2,3-d]pyrimidin-3-ylacyl)-glutamic acid derivatives
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
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)
EP1001799B1 (de) * 1997-07-07 2001-10-31 PTC Pharma AG Pharmazeutische zusammensetzung enthaltend peptichemio
US6048736A (en) * 1998-04-29 2000-04-11 Kosak; Kenneth M. Cyclodextrin polymers for carrying and releasing drugs
ATE416791T1 (de) * 2000-05-02 2008-12-15 Theravance Inc Zusammensetzung die eine zyklodextrin und ein glykopeptid-antibiotikum enthält
CA2429353A1 (en) 2000-11-28 2002-08-01 Genentech, Inc. Lfa-1 antagonist compounds
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
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
CA2579096C (en) 2004-09-08 2012-11-13 Chelsea Therapeutics, Inc. Quinazoline derivatives as metabolically inert antifolate compounds
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

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

Also Published As

Publication number Publication date
WO2006029385A3 (en) 2006-05-11
WO2006029385A2 (en) 2006-03-16
EP1791544A4 (en) 2007-09-12
US7829708B2 (en) 2010-11-09
US20110082149A1 (en) 2011-04-07
US20060111272A1 (en) 2006-05-25
JP2008512490A (ja) 2008-04-24
US20110081338A1 (en) 2011-04-07
CA2579096A1 (en) 2006-03-16
CA2579096C (en) 2012-11-13
AU2005282241A1 (en) 2006-03-16
EP1791544A2 (en) 2007-06-06

Similar Documents

Publication Publication Date Title
AU2005282241B2 (en) Quinazoline derivatives as metabolically inert antifolate compounds.
US7951812B2 (en) Substituted pyrrolo[2,3-d]pyrimidines as antifolates
US20090253720A1 (en) Antifolate compositions
BRPI0818006B1 (pt) compostos de piperidino-di-hidrotienopirimidinas substituídas, uso dos mesmos e formulações farmacêuticas
CN100554264C (zh) 吡唑基与咪唑基嘧啶
MX2014012009A (es) 1H-PIRAZOLO [3,4-ß] PIRIDINAS Y USOS TERAPEUTICOS DE LAS MISMAS.
TW201106951A (en) 3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]octane-or heptane-nitrile as JAK inhibitors
HUE032273T2 (en) 3-Imidazolyl-pyrazolo [3,4-b] pyridines
JP6155026B2 (ja) プロテインキナーゼ阻害のための新規化合物及びその治療的使用
US8530653B2 (en) Enzyme inhibiting compounds
AU2011202657A1 (en) Quinazoline derivatives as metabolically inert antifolate compounds
US20110124650A1 (en) Stable crystalline salts of antifolate compounds
DE10217799A1 (de) Stents
CN101208329A (zh) 嘧啶衍生物及其在治疗癌症中的应用

Legal Events

Date Code Title Description
FGA Letters patent sealed or granted (standard patent)
MK14 Patent ceased section 143(a) (annual fees not paid) or expired