JP5438680B2 - Rafキナーゼ阻害剤の製造方法及び該方法に使用する中間体 - Google Patents

Rafキナーゼ阻害剤の製造方法及び該方法に使用する中間体 Download PDF

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JP5438680B2
JP5438680B2 JP2010523590A JP2010523590A JP5438680B2 JP 5438680 B2 JP5438680 B2 JP 5438680B2 JP 2010523590 A JP2010523590 A JP 2010523590A JP 2010523590 A JP2010523590 A JP 2010523590A JP 5438680 B2 JP5438680 B2 JP 5438680B2
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sorafenib
derivative
formula
trifluoromethyl
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JP2010539076A5 (OSRAM
JP2010539076A (ja
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ラマチャンドラ ラオ ドハルマラジェ
ナラヤンラオ カンカン ラジェンドラ
グハガレ マルトイ
チクハリカル サンドイプ
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シプラ・リミテッド
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C271/00Derivatives of carbamic acids, i.e. compounds containing any of the groups, the nitrogen atom not being part of nitro or nitroso groups
    • C07C271/06Esters of carbamic acids
    • C07C271/40Esters of carbamic acids having oxygen atoms of carbamate groups bound to carbon atoms of six-membered aromatic rings
    • C07C271/58Esters of carbamic acids having oxygen atoms of carbamate groups bound to carbon atoms of six-membered aromatic rings with the nitrogen atom of at least one of the carbamate groups bound to a carbon atom of a six-membered aromatic ring
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C233/00Carboxylic acid amides
    • C07C233/01Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
    • C07C233/12Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by halogen atoms or by nitro or nitroso groups
    • C07C233/15Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by halogen atoms or by nitro or nitroso groups with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by a carbon atom of a six-membered aromatic ring
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C275/00Derivatives of urea, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups
    • C07C275/28Derivatives of urea, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of urea groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
    • C07C275/30Derivatives of urea, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of urea groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton being further substituted by halogen atoms, or by nitro or nitroso groups
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C275/00Derivatives of urea, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups
    • C07C275/28Derivatives of urea, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of urea groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
    • C07C275/32Derivatives of urea, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of urea groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton being further substituted by singly-bound oxygen atoms
    • C07C275/34Derivatives of urea, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of urea groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton being further substituted by singly-bound oxygen atoms having nitrogen atoms of urea groups and singly-bound oxygen atoms bound to carbon atoms of the same non-condensed six-membered aromatic ring
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C275/00Derivatives of urea, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups
    • C07C275/64Derivatives of urea, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of urea groups singly-bound to oxygen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D213/00Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/78Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/81Amides; Imides

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Pyridine Compounds (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
JP2010523590A 2007-09-10 2008-09-10 Rafキナーゼ阻害剤の製造方法及び該方法に使用する中間体 Expired - Fee Related JP5438680B2 (ja)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
IN1734/MUM/2007 2007-09-10
IN1733MU2007 2007-09-10
IN1734MU2007 2007-09-10
IN1733/MUM/2007 2007-09-10
PCT/GB2008/003048 WO2009034308A2 (en) 2007-09-10 2008-09-10 Process for the preparation of a raf kinase inhibitor and intermediates for use in the process

Publications (3)

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JP2010539076A JP2010539076A (ja) 2010-12-16
JP2010539076A5 JP2010539076A5 (OSRAM) 2011-10-27
JP5438680B2 true JP5438680B2 (ja) 2014-03-12

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JP2010523590A Expired - Fee Related JP5438680B2 (ja) 2007-09-10 2008-09-10 Rafキナーゼ阻害剤の製造方法及び該方法に使用する中間体

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Country Link
US (1) US8445687B2 (OSRAM)
EP (1) EP2195286A2 (OSRAM)
JP (1) JP5438680B2 (OSRAM)
KR (1) KR101553211B1 (OSRAM)
AU (1) AU2008299703C1 (OSRAM)
CA (1) CA2698795C (OSRAM)
NZ (1) NZ583790A (OSRAM)
WO (1) WO2009034308A2 (OSRAM)
ZA (1) ZA201001935B (OSRAM)

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US8124630B2 (en) 1999-01-13 2012-02-28 Bayer Healthcare Llc ω-carboxyaryl substituted diphenyl ureas as raf kinase inhibitors
EP1158985B1 (en) 1999-01-13 2011-12-28 Bayer HealthCare LLC OMEGA-CARBOXY ARYL SUBSTITUTED DIPHENYL UREAS AS p38 KINASE INHIBITORS
ES2425739T3 (es) 2002-02-11 2013-10-17 Bayer Healthcare Llc Sorafenib-tosilato para el tratamiento de enfermedades caracterizadas por angiogénesis anormal
DE602004011340T2 (de) 2003-05-20 2008-11-06 Bayer Healthcare Llc Diaryl-harnstoffe mit kinasehemmender wirkung
US8445687B2 (en) 2007-09-10 2013-05-21 Cipla Limited Process for the preparation of a RAF kinase inhibitor and intermediates for use in the process
PE20110298A1 (es) 2008-09-02 2011-05-21 Novartis Ag Derivados de picolinamida como inhibidores de cinasa
US8609854B2 (en) 2009-09-24 2013-12-17 Ranbaxy Laboratories Limited Process for the preparation of sorafenib tosylate
WO2011036648A1 (en) 2009-09-24 2011-03-31 Ranbaxy Laboratories Limited Polymorphs of sorafenib acid addition salts
US8552197B2 (en) 2009-11-12 2013-10-08 Ranbaxy Laboratories Limited Sorafenib ethylsulfonate salt, process for preparation and use
WO2011092663A2 (en) 2010-01-29 2011-08-04 Ranbaxy Laboratories Limited 4-(4-{3-[4-chloro-3-(trifluoromethyl)phenyl]ureido}phenoxy)-n2-methylpyridine-2-carboxamide dimethyl sulphoxide solvate
CN102190616B (zh) * 2010-03-18 2015-07-29 苏州泽璟生物制药有限公司 一种氘代的ω-二苯基脲的合成及生产的方法和工艺
JP2014510714A (ja) * 2011-01-18 2014-05-01 グラクソ グループ リミテッド レチガビンの製造方法
CN102485714B (zh) * 2011-10-09 2013-07-24 连云港盛和生物科技有限公司 一种羰基化合成索拉菲尼的方法
US8987457B2 (en) 2012-05-21 2015-03-24 Novartis Ag Ring-substituted N-pyridinyl amides as kinase inhibitors
CN103508961B (zh) * 2012-06-26 2015-07-22 中美冠科生物技术(太仓)有限公司 抗肿瘤药物
CN103408488A (zh) * 2013-08-13 2013-11-27 张家港威胜生物医药有限公司 一种索拉非尼的优化合成方法
PT3039424T (pt) 2013-08-28 2020-09-03 Crown Bioscience Inc Taicang Assinaturas de expressão genética que permitem prever a resposta de um sujeito a um inibidor multiquinase e métodos de utilização do mesmo
CN104761492A (zh) * 2014-01-03 2015-07-08 正大天晴药业集团股份有限公司 对甲苯磺酸索拉非尼的晶型及其制备方法
CN105481764A (zh) * 2014-09-16 2016-04-13 重庆圣华曦药业股份有限公司 一种索拉非尼对甲苯磺酸盐的制备方法
CN105399668B (zh) * 2015-12-29 2018-11-16 开封制药(集团)有限公司 一种“一锅法”制备索拉菲尼的方法
CN105801475B (zh) * 2016-04-25 2018-01-12 华润双鹤利民药业(济南)有限公司 一种甲苯磺酸索拉非尼的制备方法
CN109796400B (zh) * 2017-11-16 2022-07-29 四川科伦药物研究院有限公司 一种甲苯磺酸索拉菲尼晶型及其制备方法
CN108623521B (zh) * 2018-03-22 2020-09-04 盐城师范学院 一种乐伐替尼的制备方法
CN108558747A (zh) * 2018-03-31 2018-09-21 山东罗欣药业集团恒欣药业有限公司 一种瑞戈非尼的制备方法
CN108440403A (zh) * 2018-03-31 2018-08-24 山东罗欣药业集团恒欣药业有限公司 一种瑞戈非尼的制备方法
CN108341770A (zh) * 2018-03-31 2018-07-31 山东罗欣药业集团恒欣药业有限公司 一种索拉非尼化合物的制备方法
CN108586329A (zh) * 2018-03-31 2018-09-28 山东罗欣药业集团恒欣药业有限公司 一种索拉非尼的合成方法
CN108276328A (zh) * 2018-03-31 2018-07-13 山东罗欣药业集团恒欣药业有限公司 一种索拉非尼的制备方法
CN108276327A (zh) * 2018-03-31 2018-07-13 山东罗欣药业集团恒欣药业有限公司 一种索拉非尼的制备方法
CN108586330A (zh) * 2018-04-18 2018-09-28 日照市普达医药科技有限公司 一种治疗肿瘤药物的制备方法及其应用
CN114144410A (zh) 2019-07-19 2022-03-04 阿纳格纳斯生物技术股份有限公司 多芳基脲衍生物及其在治疗肌肉疾病中的用途
EP4029501A1 (en) 2021-01-19 2022-07-20 Anagenesis Biotechnologies Combination of polyaromatic urea derivatives and glucocorticoid or hdac inhibitor for the treatment of diseases or conditions associated with muscle cells and/or satellite cells

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Also Published As

Publication number Publication date
AU2008299703B2 (en) 2013-06-20
ZA201001935B (en) 2010-11-24
WO2009034308A3 (en) 2009-07-16
AU2008299703C1 (en) 2013-09-05
KR101553211B1 (ko) 2015-09-15
CA2698795A1 (en) 2009-03-19
AU2008299703A1 (en) 2009-03-19
CA2698795C (en) 2016-04-19
KR20100074175A (ko) 2010-07-01
NZ583790A (en) 2012-04-27
US20100311980A1 (en) 2010-12-09
JP2010539076A (ja) 2010-12-16
EP2195286A2 (en) 2010-06-16
WO2009034308A2 (en) 2009-03-19
US8445687B2 (en) 2013-05-21

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