ES2524548T3 - N-óxido de 3-(2,6-dicloro-3,5-dimetoxi-fenil)-1-{6-[4-(4-etil-piperacin-1-il)-fenilamino]-pirimidin-4-il}-1-metil-urea - Google Patents

N-óxido de 3-(2,6-dicloro-3,5-dimetoxi-fenil)-1-{6-[4-(4-etil-piperacin-1-il)-fenilamino]-pirimidin-4-il}-1-metil-urea Download PDF

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Publication number
ES2524548T3
ES2524548T3 ES10771744.9T ES10771744T ES2524548T3 ES 2524548 T3 ES2524548 T3 ES 2524548T3 ES 10771744 T ES10771744 T ES 10771744T ES 2524548 T3 ES2524548 T3 ES 2524548T3
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Prior art keywords
acid
compound
cancer
pharmaceutically acceptable
salts
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ES10771744.9T
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English (en)
Spanish (es)
Inventor
Reiner Aichholz
Francesca Blasco
Vincent Bordas
Diana Graus Porta
Vito Guagnano
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Novartis AG
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Novartis AG
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/46Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/48Two nitrogen atoms
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/4965Non-condensed pyrazines
    • A61K31/497Non-condensed pyrazines containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/10Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing aromatic rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
ES10771744.9T 2009-10-30 2010-10-29 N-óxido de 3-(2,6-dicloro-3,5-dimetoxi-fenil)-1-{6-[4-(4-etil-piperacin-1-il)-fenilamino]-pirimidin-4-il}-1-metil-urea Active ES2524548T3 (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP09174619 2009-10-30
EP09174619 2009-10-30
PCT/EP2010/066435 WO2011051425A1 (en) 2009-10-30 2010-10-29 N-oxide of 3-(2,6-dichloro-3,5-dimethoxy-phenyl)-1-{6-[4-(4-ethyl-piperazin-1-yl)-phenylamino]-pyrimidin-4-yl}-1-methyl-urea

Publications (1)

Publication Number Publication Date
ES2524548T3 true ES2524548T3 (es) 2014-12-10

Family

ID=41396002

Family Applications (1)

Application Number Title Priority Date Filing Date
ES10771744.9T Active ES2524548T3 (es) 2009-10-30 2010-10-29 N-óxido de 3-(2,6-dicloro-3,5-dimetoxi-fenil)-1-{6-[4-(4-etil-piperacin-1-il)-fenilamino]-pirimidin-4-il}-1-metil-urea

Country Status (7)

Country Link
US (3) US20120220600A1 (enExample)
EP (1) EP2493864B1 (enExample)
KR (1) KR20120101367A (enExample)
CN (1) CN102596916B (enExample)
ES (1) ES2524548T3 (enExample)
IN (1) IN2012DN03180A (enExample)
WO (1) WO2011051425A1 (enExample)

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GB0512324D0 (en) * 2005-06-16 2005-07-27 Novartis Ag Organic compounds
WO2012088266A2 (en) 2010-12-22 2012-06-28 Incyte Corporation Substituted imidazopyridazines and benzimidazoles as inhibitors of fgfr3
AU2013241664B2 (en) * 2012-03-30 2016-05-19 Novartis Ag FGFR inhibitor for use in the treatment of hypophosphatemic disorders
US9611267B2 (en) 2012-06-13 2017-04-04 Incyte Holdings Corporation Substituted tricyclic compounds as FGFR inhibitors
US9388185B2 (en) 2012-08-10 2016-07-12 Incyte Holdings Corporation Substituted pyrrolo[2,3-b]pyrazines as FGFR inhibitors
US9266892B2 (en) 2012-12-19 2016-02-23 Incyte Holdings Corporation Fused pyrazoles as FGFR inhibitors
AR094812A1 (es) 2013-02-20 2015-08-26 Eisai R&D Man Co Ltd Derivado de piridina monocíclico como inhibidor del fgfr
TWI649318B (zh) 2013-04-19 2019-02-01 英塞特控股公司 作為fgfr抑制劑之雙環雜環
PE20160546A1 (es) 2013-10-25 2016-05-26 Novartis Ag Compuestos derivados de piridilo biciclicos fusionados a anillo como inhibidores de fgfr4
BR112017002268B1 (pt) 2014-08-18 2022-11-08 Eisai R&D Management Co., Ltd Sal de derivado de piridina monocíclica e cristal do mesmo
JP6585167B2 (ja) 2014-10-03 2019-10-02 ノバルティス アーゲー Fgfr4阻害剤としての縮環二環式ピリジル誘導体の使用
US10851105B2 (en) 2014-10-22 2020-12-01 Incyte Corporation Bicyclic heterocycles as FGFR4 inhibitors
WO2016134294A1 (en) 2015-02-20 2016-08-25 Incyte Corporation Bicyclic heterocycles as fgfr4 inhibitors
AU2016219822B2 (en) 2015-02-20 2020-07-09 Incyte Holdings Corporation Bicyclic heterocycles as FGFR inhibitors
MA41551A (fr) 2015-02-20 2017-12-26 Incyte Corp Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4
US9802917B2 (en) 2015-03-25 2017-10-31 Novartis Ag Particles of N-(5-cyano-4-((2-methoxyethyl)amino)pyridin-2-yl)-7-formyl-6-((4-methyl-2-oxopiperazin-1-yl)methyl)-3,4-dihydro-1,8-naphthyridine-1(2H)-carboxamide
RU2712222C2 (ru) 2015-03-25 2020-01-27 Нэшнл Кэнсер Сентер Терапевтическое средство против рака желчных протоков
US10189813B2 (en) * 2015-03-25 2019-01-29 Novartis Ag Formylated N-heterocyclic derivatives as FGFR4 inhibitors
WO2017104739A1 (ja) 2015-12-17 2017-06-22 エーザイ・アール・アンド・ディー・マネジメント株式会社 乳がん治療剤
AR111960A1 (es) 2017-05-26 2019-09-04 Incyte Corp Formas cristalinas de un inhibidor de fgfr y procesos para su preparación
BR112020017922A2 (pt) 2018-03-28 2020-12-22 Eisai R&D Management Co., Ltd. Agente terapêutico para carcinoma hepatocelular
TW201946630A (zh) 2018-05-04 2019-12-16 美商英塞特公司 Fgfr抑制劑之鹽
ES2991427T3 (es) 2018-05-04 2024-12-03 Incyte Corp Formas sólidas de un inhibidor de FGFR y procedimientos para preparar las mismas
US11628162B2 (en) 2019-03-08 2023-04-18 Incyte Corporation Methods of treating cancer with an FGFR inhibitor
WO2021007269A1 (en) 2019-07-09 2021-01-14 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
WO2021067374A1 (en) 2019-10-01 2021-04-08 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
GEAP202415945A (en) 2019-10-14 2024-04-25 Incyte Corp Bicyclic heterocycles as fgfr inhibitors
WO2021076728A1 (en) 2019-10-16 2021-04-22 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
CA3163875A1 (en) 2019-12-04 2021-06-10 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
AU2020395185A1 (en) 2019-12-04 2022-06-02 Incyte Corporation Derivatives of an FGFR inhibitor
WO2021146424A1 (en) 2020-01-15 2021-07-22 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
CN114539258B (zh) * 2020-11-27 2025-12-30 首药控股(北京)股份有限公司 一种fgfr4蛋白激酶抑制剂的多晶型物及其制备方法
EP4323405A1 (en) 2021-04-12 2024-02-21 Incyte Corporation Combination therapy comprising an fgfr inhibitor and a nectin-4 targeting agent
CN113185510B (zh) * 2021-04-12 2022-05-13 南京海纳医药科技股份有限公司 一种阿伐曲泊帕杂质的制备方法
AR126101A1 (es) 2021-06-09 2023-09-13 Incyte Corp Heterociclos tricíclicos como inhibidores de fgfr
CA3220274A1 (en) 2021-06-09 2022-12-15 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ATE396978T1 (de) * 1999-10-07 2008-06-15 Amgen Inc Triazin-kinase-hemmer
GB0512324D0 (en) 2005-06-16 2005-07-27 Novartis Ag Organic compounds
MEP3808A (xx) * 2005-12-21 2010-02-10 Novartis Ag Derivati pirimidinil aril uree kao fgf inhibitori

Also Published As

Publication number Publication date
US20140378468A1 (en) 2014-12-25
EP2493864A1 (en) 2012-09-05
US20120220600A1 (en) 2012-08-30
KR20120101367A (ko) 2012-09-13
CN102596916A (zh) 2012-07-18
WO2011051425A1 (en) 2011-05-05
CN102596916B (zh) 2015-06-17
EP2493864B1 (en) 2014-10-01
IN2012DN03180A (enExample) 2015-09-25
US20160102062A1 (en) 2016-04-14

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