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)
  • Immunology (AREA)
  • Pulmonology (AREA)
  • Oncology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Diabetes (AREA)
  • Vascular Medicine (AREA)
  • Communicable Diseases (AREA)
  • Urology & Nephrology (AREA)
  • Transplantation (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 (https=)
EP (3) EP2194049B1 (https=)
JP (2) JP4213595B2 (https=)
KR (2) KR20070058019A (https=)
CN (2) CN100467461C (https=)
AT (1) ATE380807T1 (https=)
BR (1) BR0307058A (https=)
CA (1) CA2474104C (https=)
DE (1) DE60318013T2 (https=)
ES (2) ES2503734T3 (https=)
GB (1) GB0201508D0 (https=)
IL (2) IL162979A (https=)
MX (1) MXPA04007130A (https=)
PT (2) PT1470120E (https=)
WO (1) WO2003062220A1 (https=)

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ATE454152T1 (de) * 2003-06-13 2010-01-15 Novartis Pharma Gmbh 2-aminopyrimidin-derivate als raf-kinase-hemmer
ATE428421T1 (de) * 2004-09-17 2009-05-15 Eisai R&D Man Co Ltd Medizinische zusammensetzung mit verbesserter stabilität und reduzierten gelierungseigenschaften
GB0512091D0 (en) * 2005-06-14 2005-07-20 Novartis Ag Organic compounds
WO2007015569A1 (ja) * 2005-08-01 2007-02-08 Eisai R & D Management Co., Ltd. 血管新生阻害物質の効果を予測する方法
JP4989476B2 (ja) * 2005-08-02 2012-08-01 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
GEP20105074B (en) * 2005-12-21 2010-09-10 Novartis Ag Pyrimidinyl aryl urea derivatives being fgf inhibitors
CN104706637A (zh) * 2006-05-18 2015-06-17 卫材R&D管理有限公司 针对甲状腺癌的抗肿瘤剂
WO2008027600A2 (en) * 2006-09-01 2008-03-06 Teva Pharmaceutical Industries Ltd. Imatinib compositions
EP2009008A1 (en) * 2006-10-26 2008-12-31 Sicor, Inc. Imatinib base, and imatinib mesylate and processes for preparation thereof
WO2008057291A2 (en) * 2006-10-26 2008-05-15 Sicor Inc. Crystalline and amorphous imatinib base, 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
CA2676796C (en) 2007-01-29 2016-02-23 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
TWI433677B (zh) 2007-06-04 2014-04-11 Avila Therapeutics Inc 雜環化合物及其用途
EP2166860B1 (en) 2007-06-07 2016-09-21 Intra-Cellular Therapies, Inc. Novel heterocycle 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
EP2081556A1 (en) * 2007-09-25 2009-07-29 Teva Pharmaceutical Industries Ltd. Stable imatinib compositions
US8952035B2 (en) * 2007-11-09 2015-02-10 Eisai R&D Management Co., Ltd. Combination of anti-angiogenic substance and anti-tumor platinum complex
KR101506062B1 (ko) * 2008-01-29 2015-03-25 에자이 알앤드디 매니지먼트 가부시키가이샤 혈관 저해 물질과 탁산의 병용
JP2011515685A (ja) * 2008-03-26 2011-05-19 メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツング 基質結合ビーズを長期間保存する方法
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
MY162940A (en) 2009-08-19 2017-07-31 Eisai R&D Man Co Ltd Quinoline derivative-containing pharmaceutical composition
CN102958523B (zh) 2010-06-25 2014-11-19 卫材R&D管理有限公司 使用具有激酶抑制作用的组合的抗肿瘤剂
CN103402519B (zh) 2011-04-18 2015-11-25 卫材R&D管理有限公司 肿瘤治疗剂
JP6038128B2 (ja) 2011-06-03 2016-12-07 エーザイ・アール・アンド・ディー・マネジメント株式会社 レンバチニブ化合物に対する甲状腺癌対象及び腎臓癌対象の反応性を予測及び評価するためのバイオマーカー
KR20150098605A (ko) 2012-12-21 2015-08-28 에자이 알앤드디 매니지먼트 가부시키가이샤 퀴놀린 유도체의 비정질 형태 및 그의 제조방법
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
PT3524595T (pt) 2014-08-28 2022-09-19 Eisai R&D Man Co Ltd Derivado de quinolina altamente puro e método para produção do mesmo
LT3263106T (lt) 2015-02-25 2024-01-10 Eisai R&D Management Co., Ltd. Chinolino darinių kartumo sumažinimo būdas
KR102662228B1 (ko) 2015-03-04 2024-05-02 머크 샤프 앤드 돔 코포레이션 암을 치료하기 위한 pd-1 길항제 및 vegfr/fgfr/ret 티로신 키나제 억제제의 조합
MX373231B (es) 2015-06-16 2020-05-08 Eisai R&D Man Co Ltd Agente anticancerigeno.
US12220398B2 (en) 2015-08-20 2025-02-11 Eisai R&D Management Co., Ltd. Tumor therapeutic agent
US12303505B2 (en) 2017-02-08 2025-05-20 Eisai R&D Management Co., Ltd. Tumor-treating pharmaceutical composition
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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Also Published As

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

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