CA2474104C - N-oxides of n-phenyl-2-pyrimidine-amine derivatives - Google Patents

N-oxides of n-phenyl-2-pyrimidine-amine derivatives Download PDF

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Publication number
CA2474104C
CA2474104C CA2474104A CA2474104A CA2474104C CA 2474104 C CA2474104 C CA 2474104C CA 2474104 A CA2474104 A CA 2474104A CA 2474104 A CA2474104 A CA 2474104A CA 2474104 C CA2474104 C CA 2474104C
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CA
Canada
Prior art keywords
compound
formula
methyl
cells
compounds
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 - Fee Related
Application number
CA2474104A
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English (en)
French (fr)
Other versions
CA2474104A1 (en
Inventor
Klaus Olaf Boernsen
Peter End
Gerhard Gross
Ulrike Pfaar
Paul William Manley
Juerg Zimmermann
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Novartis AG
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Novartis AG
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Application filed by Novartis AG filed Critical Novartis AG
Publication of CA2474104A1 publication Critical patent/CA2474104A1/en
Application granted granted Critical
Publication of CA2474104C publication Critical patent/CA2474104C/en
Anticipated expiration legal-status Critical
Expired - Fee Related legal-status Critical Current

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • 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
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
    • 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
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • 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
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • 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
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • 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
    • A61P9/10Drugs 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Hematology (AREA)
  • Pulmonology (AREA)
  • Immunology (AREA)
  • Oncology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Diabetes (AREA)
  • Transplantation (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Communicable Diseases (AREA)
  • Dermatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Liquid Crystal Substances (AREA)
CA2474104A 2002-01-23 2003-01-22 N-oxides of n-phenyl-2-pyrimidine-amine derivatives Expired - Fee Related CA2474104C (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
GB0201508.9 2002-01-23
GBGB0201508.9A GB0201508D0 (en) 2002-01-23 2002-01-23 Organic compounds
PCT/EP2003/000613 WO2003062220A1 (en) 2002-01-23 2003-01-22 N-oxyde of n-phenyl-2-pyrimidine-amine derivatives

Publications (2)

Publication Number Publication Date
CA2474104A1 CA2474104A1 (en) 2003-07-31
CA2474104C true CA2474104C (en) 2012-04-17

Family

ID=9929594

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2474104A Expired - Fee Related CA2474104C (en) 2002-01-23 2003-01-22 N-oxides of n-phenyl-2-pyrimidine-amine derivatives

Country Status (15)

Country Link
US (5) US7557105B2 (OSRAM)
EP (3) EP2194049B1 (OSRAM)
JP (2) JP4213595B2 (OSRAM)
KR (2) KR100778163B1 (OSRAM)
CN (2) CN100467461C (OSRAM)
AT (1) ATE380807T1 (OSRAM)
BR (1) BR0307058A (OSRAM)
CA (1) CA2474104C (OSRAM)
DE (1) DE60318013T2 (OSRAM)
ES (2) ES2294293T3 (OSRAM)
GB (1) GB0201508D0 (OSRAM)
IL (2) IL162979A (OSRAM)
MX (1) MXPA04007130A (OSRAM)
PT (2) PT2194049E (OSRAM)
WO (1) WO2003062220A1 (OSRAM)

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EP1506962B1 (en) * 2000-10-20 2008-07-02 Eisai R&D Management Co., Ltd. Nitrogen-containing aromatic heterocycles
GB0201508D0 (en) * 2002-01-23 2002-03-13 Novartis Ag Organic compounds
PT1635835E (pt) * 2003-06-13 2010-03-17 Novartis Ag Derivados de 2-aminopiridina como inibidores da raf-quinase
US8969379B2 (en) * 2004-09-17 2015-03-03 Eisai R&D Management Co., Ltd. Pharmaceutical compositions of 4-(3-chloro-4-(cyclopropylaminocarbonyl)aminophenoxy)-7=methoxy-6-quinolinecarboxide
GB0512091D0 (en) * 2005-06-14 2005-07-20 Novartis Ag Organic compounds
JP5066446B2 (ja) * 2005-08-01 2012-11-07 エーザイ・アール・アンド・ディー・マネジメント株式会社 血管新生阻害物質の効果を予測する方法
WO2007015578A1 (ja) 2005-08-02 2007-02-08 Eisai R & D Management Co., Ltd. 血管新生阻害物質の効果を検定する方法
US20090053236A1 (en) * 2005-11-07 2009-02-26 Eisai R & D Management Co., Ltd. USE OF COMBINATION OF ANTI-ANGIOGENIC SUBSTANCE AND c-kit KINASE INHIBITOR
WO2007071752A2 (en) * 2005-12-21 2007-06-28 Novartis Ag Pyrimidinyl aryl urea derivatives being fgf inhibitors
CA2652442C (en) * 2006-05-18 2014-12-09 Eisai R & D Management Co., Ltd. Antitumor agent for thyroid cancer
WO2008027600A2 (en) * 2006-09-01 2008-03-06 Teva Pharmaceutical Industries Ltd. Imatinib compositions
MX2008008447A (es) * 2006-10-26 2008-09-15 Sicor Inc Proceso para la preparacion de imatinib.
EP2009008A1 (en) * 2006-10-26 2008-12-31 Sicor, Inc. Imatinib base, and imatinib mesylate and processes for preparation thereof
CN101225085B (zh) * 2007-01-17 2011-09-21 天津天士力集团有限公司 苯基呋咱氮类一氧化氮供体型2-苯胺嘧啶衍生物、其制备方法、含有该化合物的组合物及其用途
US8962655B2 (en) 2007-01-29 2015-02-24 Eisai R&D Management Co., Ltd. Composition for treatment of undifferentiated gastric cancer
CN101245061B (zh) * 2007-02-13 2012-09-19 天津天士力集团有限公司 N-(5-氨基-2-甲基苯基)-4-(3-吡啶基)-2-嘧啶胺类一氧化氮供体型衍生物,制备方法及其用途
US7550591B2 (en) * 2007-05-02 2009-06-23 Chemagis Ltd. Imatinib production process
EP2152079A4 (en) * 2007-06-04 2011-03-09 Avila Therapeutics Inc HETEROCYCLIC COMPOUNDS AND USES THEREOF
US9062023B2 (en) 2007-06-07 2015-06-23 Intra-Cellular Therapies, Inc. Heterocycle compounds and uses thereof
US8367686B2 (en) 2007-06-07 2013-02-05 Intra-Cellular Therapies, Inc. Heterocycle compounds and uses thereof
US8414918B2 (en) * 2007-09-25 2013-04-09 Teva Pharmaceutical Industries Ltd. Stable imatinib compositions
CN101848895B (zh) * 2007-11-09 2013-10-23 卫材R&D管理有限公司 血管新生抑制物质和抗肿瘤性铂络合物的组合使用
BRPI0906576A2 (pt) * 2008-01-29 2015-07-07 Eisai R&D Man Co Ltd Composição farmacêutica, kit, uso de um composto, e, agente terapêutico para câncer
WO2009118108A1 (en) * 2008-03-26 2009-10-01 Merck Patent Gmbh Method of long term storage of substrate-coupled beads
CN101417995B (zh) * 2008-11-21 2012-06-06 陈依军 苯氧基嘧啶衍生物及其制备方法和用途
ES2573515T3 (es) 2010-06-25 2016-06-08 Eisai R&D Management Co., Ltd. Agente antitumoral que emplea compuestos con efecto inhibitorio de cinasas combinados
MX2013009931A (es) 2011-04-18 2013-10-01 Eisai R&D Man Co Ltd Agentes terapeuticos contra tumores.
EP2714937B1 (en) 2011-06-03 2018-11-14 Eisai R&D Management Co., Ltd. Biomarkers for predicting and assessing responsiveness of thyroid and kidney cancer subjects to lenvatinib compounds
MX2015004979A (es) 2012-12-21 2015-07-17 Eisai R&D Man Co Ltd Forma amorfa de derivado de quinolina y metodo para su produccion.
NZ714049A (en) 2013-05-14 2020-05-29 Eisai R&D Man Co Ltd Biomarkers for predicting and assessing responsiveness of endometrial cancer subjects to lenvatinib compounds
CN103588754B (zh) * 2013-11-04 2015-05-27 遵义医学院 伊马替尼的制备方法
CN113683564A (zh) 2014-08-28 2021-11-23 卫材R&D管理有限公司 高纯度喹啉衍生物及其生产方法
LT3263106T (lt) 2015-02-25 2024-01-10 Eisai R&D Management Co., Ltd. Chinolino darinių kartumo sumažinimo būdas
CA2978226C (en) 2015-03-04 2025-02-18 Eisai R&D Management Co., Ltd. COMBINATION OF A PD-1 ANTAGONIST AND A VEGFR/FGFR/RET TYROSINE KINASE INHIBITOR TO TREAT CANCER
CN107801379B (zh) 2015-06-16 2021-05-25 卫材R&D管理有限公司 抗癌剂
RU2718048C2 (ru) 2015-08-20 2020-03-30 Эйсай Ар Энд Ди Менеджмент Ко., Лтд. Противоопухолевое терапевтическое средство
WO2018147275A1 (ja) 2017-02-08 2018-08-16 エーザイ・アール・アンド・ディー・マネジメント株式会社 腫瘍治療用医薬組成物
RU2019134940A (ru) 2017-05-16 2021-06-16 Эйсай Ар Энд Ди Менеджмент Ко., Лтд. Лечение гепатоцеллюлярной карциномы
CN107573322A (zh) * 2017-09-06 2018-01-12 南京优科生物医药研究有限公司 伊马替尼双氮氧化物、其制备方法和用途
CN109761970B (zh) * 2019-01-26 2020-06-09 中国药科大学 一种蛋白靶向降解嵌合分子、制备方法及应用

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US5521184A (en) * 1992-04-03 1996-05-28 Ciba-Geigy Corporation Pyrimidine derivatives and processes for the preparation thereof
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Also Published As

Publication number Publication date
KR100778163B1 (ko) 2007-11-28
JP4213595B2 (ja) 2009-01-21
PT1470120E (pt) 2008-03-03
US20110294820A1 (en) 2011-12-01
IL208399A0 (en) 2010-12-30
DE60318013T2 (de) 2008-11-13
US20050209452A1 (en) 2005-09-22
JP2009051837A (ja) 2009-03-12
MXPA04007130A (es) 2004-10-29
JP2005519908A (ja) 2005-07-07
CN1646519A (zh) 2005-07-27
US7557105B2 (en) 2009-07-07
KR20040081467A (ko) 2004-09-21
US20100222362A1 (en) 2010-09-02
EP1783126A2 (en) 2007-05-09
EP1470120A1 (en) 2004-10-27
EP1783126A3 (en) 2008-11-26
CN100467461C (zh) 2009-03-11
IL162979A (en) 2010-12-30
ES2294293T3 (es) 2008-04-01
EP2194049A1 (en) 2010-06-09
PT2194049E (pt) 2014-11-10
DE60318013D1 (de) 2008-01-24
EP1470120B1 (en) 2007-12-12
US20090239879A1 (en) 2009-09-24
JP5027076B2 (ja) 2012-09-19
CA2474104A1 (en) 2003-07-31
IL208399A (en) 2013-02-28
ES2503734T3 (es) 2014-10-07
ATE380807T1 (de) 2007-12-15
GB0201508D0 (en) 2002-03-13
WO2003062220A1 (en) 2003-07-31
US20140323494A1 (en) 2014-10-30
EP2194049B1 (en) 2014-08-13
KR20070058019A (ko) 2007-06-07
CN101468984A (zh) 2009-07-01
BR0307058A (pt) 2004-12-28

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Effective date: 20180122