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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First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=9929594&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=CA2474104(C) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
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)
  • Public Health (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Hematology (AREA)
  • Pulmonology (AREA)
  • Immunology (AREA)
  • Cardiology (AREA)
  • Diabetes (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Oncology (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Transplantation (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
GBGB0201508.9A GB0201508D0 (en) 2002-01-23 2002-01-23 Organic compounds
GB0201508.9 2002-01-23
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 (enExample)
EP (3) EP1783126A3 (enExample)
JP (2) JP4213595B2 (enExample)
KR (2) KR20070058019A (enExample)
CN (2) CN101468984A (enExample)
AT (1) ATE380807T1 (enExample)
BR (1) BR0307058A (enExample)
CA (1) CA2474104C (enExample)
DE (1) DE60318013T2 (enExample)
ES (2) ES2503734T3 (enExample)
GB (1) GB0201508D0 (enExample)
IL (2) IL162979A (enExample)
MX (1) MXPA04007130A (enExample)
PT (2) PT2194049E (enExample)
WO (1) WO2003062220A1 (enExample)

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GB0201508D0 (en) * 2002-01-23 2002-03-13 Novartis Ag Organic compounds
ATE454152T1 (de) * 2003-06-13 2010-01-15 Novartis Pharma Gmbh 2-aminopyrimidin-derivate als raf-kinase-hemmer
EP1797881B1 (en) 2004-09-17 2009-04-15 Eisai R&D Management Co., Ltd. Medicinal composition with improved stability and reduced gelation properties
GB0512091D0 (en) * 2005-06-14 2005-07-20 Novartis Ag Organic compounds
EP1925941B1 (en) * 2005-08-01 2012-11-28 Eisai R&D Management Co., Ltd. Method for prediction of the efficacy of vascularization inhibitor
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
AU2006309551B2 (en) * 2005-11-07 2012-04-19 Eisai R & D Management Co., Ltd. Use of combination of anti-angiogenic substance and c-kit kinase inhibitor
ME00011A (me) * 2005-12-21 2009-02-10 Novartis Ag Derivati pirimidinilaril uree kao fgf inhibitori
ES2556173T3 (es) * 2006-05-18 2016-01-13 Eisai R&D Management Co., Ltd. Agente antitumoral para un cáncer de tiroides
EP2068835A2 (en) * 2006-09-01 2009-06-17 Teva Pharmaceutical Industries Ltd. Imatinib compositions
US20080207904A1 (en) * 2006-10-26 2008-08-28 Macdonald Peter Imatinib base, and imatinib mesylate and processes for preparation thereof
EP1988089A1 (en) * 2006-10-26 2008-11-05 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
KR101445892B1 (ko) 2007-01-29 2014-09-29 에자이 알앤드디 매니지먼트 가부시키가이샤 미분화형 위암 치료용 조성물
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
CA2689989A1 (en) 2007-06-04 2008-12-11 Avila Therapeutics, Inc. Heterocyclic compounds and uses thereof
JP5710251B2 (ja) 2007-06-07 2015-04-30 イントラ−セルラー・セラピーズ・インコーポレイテッドIntra−Cellular Therapies, Inc. 新規ヘテロ環化合物およびその使用
EP2166860B1 (en) 2007-06-07 2016-09-21 Intra-Cellular Therapies, Inc. Novel heterocycle compounds and uses thereof
EP2086520A1 (en) * 2007-09-25 2009-08-12 Teva Pharmaceutical Industries Ltd. 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
JP5399926B2 (ja) * 2008-01-29 2014-01-29 エーザイ・アール・アンド・ディー・マネジメント株式会社 血管阻害物質とタキサンとの併用
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
CA2802644C (en) 2010-06-25 2017-02-21 Eisai R & D Management Co., Ltd. Antitumor agent using compounds having kinase inhibitory effect in combination
RU2580609C2 (ru) 2011-04-18 2016-04-10 Эйсай Ар Энд Ди Менеджмент Ко., Лтд. Противоопухолевое терапевтическое средство
EP3444363B1 (en) 2011-06-03 2020-11-25 Eisai R&D Management Co., Ltd. Biomarkers for prediciting and assessing responsiveness of thyroid and kidney cancer subjects to lenvatinib compounds
AU2013364953A1 (en) 2012-12-21 2015-04-30 Eisai R&D Management Co., Ltd. Amorphous form of quinoline derivative, and method for producing same
WO2014185540A1 (en) 2013-05-14 2014-11-20 Eisai R&D Management 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
KR102329681B1 (ko) 2014-08-28 2021-11-23 에자이 알앤드디 매니지먼트 가부시키가이샤 고순도의 퀴놀린 유도체 및 이를 제조하는 방법
KR20250024102A (ko) 2015-02-25 2025-02-18 에자이 알앤드디 매니지먼트 가부시키가이샤 퀴놀린 유도체의 고미 억제 방법
AU2015384801B2 (en) 2015-03-04 2022-01-06 Eisai R&D Management Co., Ltd. Combination of a PD-1 antagonist and a VEGFR/FGFR/RET tyrosine kinase inhibitor for treating cancer
ES2886107T3 (es) 2015-06-16 2021-12-16 Prism Biolab Co Ltd Antineoplásico
SG11201801083UA (en) 2015-08-20 2018-03-28 Eisai R&D Man Co Ltd Tumor therapeutic agent
US12303505B2 (en) 2017-02-08 2025-05-20 Eisai R&D Management Co., Ltd. Tumor-treating pharmaceutical composition
US20200197384A1 (en) 2017-05-16 2020-06-25 Eisai R&D Management Co., Ltd. Treatment of hepatocellular carcinoma
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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Also Published As

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

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Effective date: 20180122