CN102596916B - 3-(2,6-二氯-3,5-二甲氧基-苯基)-1-{6-[4-(4-乙基-哌嗪-1-基)-苯基氨基]-嘧啶-4-基}-1-甲基-脲的n-氧化物 - Google Patents

3-(2,6-二氯-3,5-二甲氧基-苯基)-1-{6-[4-(4-乙基-哌嗪-1-基)-苯基氨基]-嘧啶-4-基}-1-甲基-脲的n-氧化物 Download PDF

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Publication number
CN102596916B
CN102596916B CN201080048756.3A CN201080048756A CN102596916B CN 102596916 B CN102596916 B CN 102596916B CN 201080048756 A CN201080048756 A CN 201080048756A CN 102596916 B CN102596916 B CN 102596916B
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acid
compound
pharmaceutically acceptable
compounds
ethyl
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CN102596916A (zh
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R·艾希霍尔茨
F·布拉斯科
V·博尔达斯
D·格劳斯波塔
V·瓜格纳诺
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Novartis AG
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Novartis AG
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic 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
    • C07D239/28—Heterocyclic 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
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/48—Two nitrogen atoms
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic 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
    • A61K31/4965—Non-condensed pyrazines
    • A61K31/497—Non-condensed pyrazines containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic 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
    • C07D403/10—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic 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
    • C07D403/12—Heterocyclic 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00—Mixtures 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)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (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)
CN201080048756.3A 2009-10-30 2010-10-29 3-(2,6-二氯-3,5-二甲氧基-苯基)-1-{6-[4-(4-乙基-哌嗪-1-基)-苯基氨基]-嘧啶-4-基}-1-甲基-脲的n-氧化物 Expired - Fee Related CN102596916B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP09174619 2009-10-30
EP09174619.8 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

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CN102596916A CN102596916A (zh) 2012-07-18
CN102596916B true CN102596916B (zh) 2015-06-17

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CN201080048756.3A Expired - Fee Related CN102596916B (zh) 2009-10-30 2010-10-29 3-(2,6-二氯-3,5-二甲氧基-苯基)-1-{6-[4-(4-乙基-哌嗪-1-基)-苯基氨基]-嘧啶-4-基}-1-甲基-脲的n-氧化物

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US (3) US20120220600A1 (https=)
EP (1) EP2493864B1 (https=)
KR (1) KR20120101367A (https=)
CN (1) CN102596916B (https=)
ES (1) ES2524548T3 (https=)
IN (1) IN2012DN03180A (https=)
WO (1) WO2011051425A1 (https=)

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US8754114B2 (en) 2010-12-22 2014-06-17 Incyte Corporation Substituted imidazopyridazines and benzimidazoles as inhibitors of FGFR3
US20150072019A1 (en) * 2012-03-30 2015-03-12 Novartis Ag Fgfr inhibitor for use in the treatment of hypophosphatemic disorders
RS58514B1 (sr) 2012-06-13 2019-04-30 Incyte Holdings Corp Supstituisana triciklična jedinjenja kao inhibitori fgfr
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
PH12015502383B1 (en) 2013-04-19 2023-02-03 Incyte Holdings Corp Bicyclic heterocycles as fgfr inhibitors
TN2016000115A1 (en) 2013-10-25 2017-07-05 Novartis Ag Ring-fused bicyclic pyridyl derivatives as fgfr4 inhibitors.
KR102344105B1 (ko) 2014-08-18 2021-12-29 에자이 알앤드디 매니지먼트 가부시키가이샤 모노시클릭 피리딘 유도체의 염 및 이의 결정
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
TWI712601B (zh) 2015-02-20 2020-12-11 美商英塞特公司 作為fgfr抑制劑之雙環雜環
MA41551A (fr) 2015-02-20 2017-12-26 Incyte Corp Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4
US9580423B2 (en) 2015-02-20 2017-02-28 Incyte Corporation Bicyclic heterocycles as FGFR4 inhibitors
EP3275442B1 (en) 2015-03-25 2021-07-28 National Cancer Center Therapeutic agent for bile duct cancer
AU2016238436A1 (en) * 2015-03-25 2017-08-17 Novartis Ag Formylated N-heterocyclic derivatives as FGFR4 inhibitors
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
CN108367000A (zh) 2015-12-17 2018-08-03 卫材R&D管理有限公司 用于乳腺癌的治疗剂
AR111960A1 (es) 2017-05-26 2019-09-04 Incyte Corp Formas cristalinas de un inhibidor de fgfr y procesos para su preparación
US11219619B2 (en) 2018-03-28 2022-01-11 Eisai R&D Management Co., Ltd. Therapeutic agent for hepatocellular carcinoma
HRP20241288T1 (hr) 2018-05-04 2024-12-06 Incyte Corporation Čvrsti oblici fgfr inhibitora i postupci za njihovu proizvodnju
AU2019262579B2 (en) 2018-05-04 2024-09-12 Incyte Corporation Salts of an FGFR inhibitor
US11628162B2 (en) 2019-03-08 2023-04-18 Incyte Corporation Methods of treating cancer with an FGFR inhibitor
US11591329B2 (en) 2019-07-09 2023-02-28 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
WO2021067374A1 (en) 2019-10-01 2021-04-08 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
CA3157361A1 (en) 2019-10-14 2021-04-22 Incyte Corporation 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
JP7832891B2 (ja) 2019-12-04 2026-03-18 インサイト・コーポレイション Ｆｇｆｒ阻害剤の誘導体
US12012409B2 (en) 2020-01-15 2024-06-18 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
WO2022221170A1 (en) 2021-04-12 2022-10-20 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
US11939331B2 (en) 2021-06-09 2024-03-26 Incyte Corporation Tricyclic heterocycles as FGFR inhibitors
CA3220155A1 (en) 2021-06-09 2022-12-15 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors

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CN101336237A (zh) * 2005-12-21 2008-12-31 诺瓦提斯公司 作为fgf抑制剂的嘧啶基芳基脲衍生物

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GB0512324D0 (en) 2005-06-16 2005-07-27 Novartis Ag Organic compounds

Patent Citations (2)

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Publication number Priority date Publication date Assignee Title
WO2001025220A1 (en) * 1999-10-07 2001-04-12 Amgen Inc. Triazine kinase inhibitors
CN101336237A (zh) * 2005-12-21 2008-12-31 诺瓦提斯公司 作为fgf抑制剂的嘧啶基芳基脲衍生物

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US20160102062A1 (en) 2016-04-14
EP2493864B1 (en) 2014-10-01
WO2011051425A1 (en) 2011-05-05
IN2012DN03180A (https=) 2015-09-25
ES2524548T3 (es) 2014-12-10
US20140378468A1 (en) 2014-12-25
CN102596916A (zh) 2012-07-18
US20120220600A1 (en) 2012-08-30
KR20120101367A (ko) 2012-09-13
EP2493864A1 (en) 2012-09-05

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