EA201591756A1 - Метаболиты n-(4-{[6,7-бис-(метилокси)хинолин-4-ил]окси}фенил)-n'-(4-фторфенил)циклопропан-1,1-дикарбоксамида - Google Patents

Метаболиты n-(4-{[6,7-бис-(метилокси)хинолин-4-ил]окси}фенил)-n'-(4-фторфенил)циклопропан-1,1-дикарбоксамида

Info

Publication number
EA201591756A1
EA201591756A1 EA201591756A EA201591756A EA201591756A1 EA 201591756 A1 EA201591756 A1 EA 201591756A1 EA 201591756 A EA201591756 A EA 201591756A EA 201591756 A EA201591756 A EA 201591756A EA 201591756 A1 EA201591756 A1 EA 201591756A1
Authority
EA
Eurasian Patent Office
Prior art keywords
metabolites
ftorphenyl
cyclopropan
dicarboxamide
methyloxy
Prior art date
Application number
EA201591756A
Other languages
English (en)
Other versions
EA033786B1 (ru
Inventor
Дана Т. Афтаб
Срирам Наганатхан
Вей Сюй
Стивен Лэйси
Линь Нгуйен
Original Assignee
Экселиксис, Инк.
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Экселиксис, Инк. filed Critical Экселиксис, Инк.
Publication of EA201591756A1 publication Critical patent/EA201591756A1/ru
Publication of EA033786B1 publication Critical patent/EA033786B1/ru

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C233/00—Carboxylic acid amides
    • C07C233/57—Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of rings other than six-membered aromatic rings
    • C07C233/60—Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of rings other than six-membered aromatic rings having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by singly-bound oxygen atoms
    • 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
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C305/00—Esters of sulfuric acids
    • C07C305/22—Esters of sulfuric acids having oxygen atoms of sulfate groups bound to carbon atoms of six-membered aromatic rings
    • C07C305/24—Esters of sulfuric acids having oxygen atoms of sulfate groups bound to carbon atoms of six-membered aromatic rings of non-condensed six-membered aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms 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
    • C07D215/20—Oxygen atoms
    • C07D215/22—Oxygen atoms attached in position 2 or 4
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/58—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems with hetero atoms directly attached to the ring nitrogen atom
    • C07D215/60—N-oxides
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N33/00—Investigating or analysing materials by specific methods not covered by groups G01N1/00 - G01N31/00
    • G01N33/48—Biological material, e.g. blood, urine; Haemocytometers
    • G01N33/483—Physical analysis of biological material
    • G01N33/487—Physical analysis of biological material of liquid biological material
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2601/00—Systems containing only non-condensed rings
    • C07C2601/02—Systems containing only non-condensed rings with a three-membered ring
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N2570/00—Omics, e.g. proteomics, glycomics or lipidomics; Methods of analysis focusing on the entire complement of classes of biological molecules or subsets thereof, i.e. focusing on proteomes, glycomes or lipidomes

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Biomedical Technology (AREA)
  • Physics & Mathematics (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Biophysics (AREA)
  • Pathology (AREA)
  • Immunology (AREA)
  • General Physics & Mathematics (AREA)
  • Biochemistry (AREA)
  • Analytical Chemistry (AREA)
  • Food Science & Technology (AREA)
  • Urology & Nephrology (AREA)
  • Hematology (AREA)
  • Molecular Biology (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Epidemiology (AREA)
  • Pain & Pain Management (AREA)
  • Saccharide Compounds (AREA)
  • Quinoline Compounds (AREA)

Abstract

Изобретение относится к метаболитам кабозантиниба (I), а также к их применению.
EA201591756A 2013-03-15 2014-03-17 Метаболиты n-(4-{[6,7-бис-(метилокси)хинолин-4-ил]окси}фенил)-n'-(4-фторфенил)циклопропан-1,1-дикарбоксамида EA033786B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201361792413P 2013-03-15 2013-03-15
PCT/US2014/030524 WO2014145715A1 (en) 2013-03-15 2014-03-17 Metabolites of n-(4-{[6,7-bis(methyloxy)quinolin-4-yl]oxy}phenyl)-n'-(4-fluorophenyl) cyclopropane-1,1-dicarboxamide

Publications (2)

Publication Number Publication Date
EA201591756A1 true EA201591756A1 (ru) 2016-02-29
EA033786B1 EA033786B1 (ru) 2019-11-26

Family

ID=50631091

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201591756A EA033786B1 (ru) 2013-03-15 2014-03-17 Метаболиты n-(4-{[6,7-бис-(метилокси)хинолин-4-ил]окси}фенил)-n'-(4-фторфенил)циклопропан-1,1-дикарбоксамида

Country Status (18)

Country Link
US (3) US10273211B2 (ru)
EP (1) EP2970126B1 (ru)
JP (1) JP6389238B2 (ru)
KR (1) KR102276348B1 (ru)
CN (1) CN105121412B (ru)
AU (2) AU2014232714B2 (ru)
BR (1) BR112015023109A2 (ru)
CA (1) CA2907334C (ru)
EA (1) EA033786B1 (ru)
ES (1) ES2729626T3 (ru)
GE (1) GEP20196995B (ru)
HK (1) HK1220447A1 (ru)
IL (1) IL241577B (ru)
MX (1) MX366003B (ru)
NZ (1) NZ712330A (ru)
UA (1) UA119321C2 (ru)
WO (1) WO2014145715A1 (ru)
ZA (1) ZA201506842B (ru)

Families Citing this family (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DK2621481T4 (da) 2010-09-27 2023-01-09 Exelixis Inc Dobbelte inhibitorer af MET og VEGF til behandling af kastrationsresistent prostatacancer og osteoblastiske knoglemetastaser
TW201309650A (zh) 2011-02-10 2013-03-01 Exelixis Inc 製造喹啉化合物之方法及包含該化合物之醫藥組合物
JP2015515988A (ja) 2012-05-02 2015-06-04 エクセリクシス， インク． 溶骨性骨転移を治療するためのｍｅｔ−ｖｅｇｆ二重調節剤
NZ712330A (en) 2013-03-15 2020-04-24 Exelixis Inc Metabolites of n-(4-{ [6,7-bis(methyloxy)quinolin-4-yl]oxy} phenyl)-n’-(4-fluorophenyl) cyclopropane-1,1-dicarboxamide
US11564915B2 (en) 2013-04-04 2023-01-31 Exelixis, Inc. Cabozantinib dosage form and use in the treatment of cancer
BR112016018450A2 (pt) 2014-02-14 2018-09-18 Exelixis Inc formas sólidas cristalinas de n-{4-[(6,7-dimetoxiquinolin-4-il)oxi]fenil}-n'-(4-fluorofenil)ciclopropano-1,1-dicarboxamida, processos de preparo e métodos de uso
EP3119476A1 (en) 2014-03-17 2017-01-25 Exelixis, Inc. Dosing of cabozantinib formulations
ES2929888T3 (es) * 2014-07-31 2022-12-02 Exelixis Inc Procedimiento para preparar cabozantinib marcado con flúor 18 y sus análogos
BR112017002318A2 (pt) 2014-08-05 2018-07-17 Exelixis, Inc. combinações de fármacos para tratar mieloma múltiplo.
WO2017181187A1 (en) 2016-04-15 2017-10-19 Exelixis, Inc. Method of treating renal cell carcinoma using n-(4-(6,7-dimethoxyquinolin-4-yloxy) phenyl)-n'-(4-fluoropheny)cyclopropane-1,1-dicarboxamide, (2s)-hydroxybutanedioate
CN107556238A (zh) * 2016-06-30 2018-01-09 深圳万乐药业有限公司 一种卡博替尼的合成方法
CN111757735B (zh) 2018-01-26 2023-09-22 埃克塞里艾克西斯公司 用于治疗激酶依赖性病症的化合物
CN110423218A (zh) * 2019-08-09 2019-11-08 新乡双鹭药业有限公司 一种苹果酸卡博替尼合成中杂质的制备方法
WO2024114710A1 (zh) * 2022-12-01 2024-06-06 江苏奥赛康药业有限公司 一种制备卡博替尼及其中间体的方法

Family Cites Families (40)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2537812C (en) 2003-09-26 2013-01-22 Exelixis, Inc. C-met modulators and method of use
WO2006014325A2 (en) 2004-07-02 2006-02-09 Exelixis, Inc. C-met modulators and method of use
WO2006108059A1 (en) 2005-04-06 2006-10-12 Exelixis, Inc. C-met modulators and methods of use
UY30183A1 (es) 2006-03-02 2007-10-31 Astrazeneca Ab Derivados de quinolina
WO2008076415A1 (en) 2006-12-14 2008-06-26 Exelixis, Inc. Methods of using mek inhibitors
UY31800A (es) 2008-05-05 2009-11-10 Smithkline Beckman Corp Metodo de tratamiento de cancer usando un inhibidor de cmet y axl y un inhibidor de erbb
UY32142A (es) 2008-09-26 2010-05-31 Smithkline Beckman Corp Preparación de una quinoliniloxidifenilciclopropanodicarboxamida
CN102282134B (zh) 2008-11-13 2015-04-01 埃克塞里艾克西斯公司 喹啉衍生物制备方法
TW201028383A (en) 2008-12-04 2010-08-01 Exelixis Inc Methods of preparing quinoline derivatives
CA2995880C (en) 2009-01-16 2021-01-05 Exelixis, Inc. Processes for preparing n-(4-{[6,7-bis(methyloxy)quinolin-4-yl]oxy}phenyl)-n'-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide
KR20120051702A (ko) 2009-07-17 2012-05-22 엑셀리시스, 인코포레이티드 Ｎ-〔３-플루오로-４-(｛６-(메틸옥시)-７-〔(３-모르폴린-４-일프로필)옥시〕퀴놀린-４-일｝옥시)페닐〕-ｎ''-(４-플루오로페닐)시클로프로판-１,１-디카르복사미드의 결정형
UA108618C2 (uk) 2009-08-07 2015-05-25 Застосування c-met-модуляторів в комбінації з темозоломідом та/або променевою терапією для лікування раку
KR20130038206A (ko) 2010-03-12 2013-04-17 엑셀리시스, 인코포레이티드 Ｎ-〔3-플루오로-4-(｛6-（메틸옥시）-7-〔（3-모폴린-4-일프로필）옥시〕-퀴놀린-4-일｝옥시）페닐〕-ｎ’-（4-플루오로페닐）사이클로프로판-1,1-디카복사미드의 수화된 결정형 형태
US20120070368A1 (en) 2010-04-16 2012-03-22 Exelixis, Inc. Methods of Using C-Met Modulators
EP2593091A1 (en) 2010-07-16 2013-05-22 Exelixis, Inc. C-met modulator pharmaceutical compositions
ES2904646T3 (es) 2010-07-16 2022-04-05 Exelixis Inc Composiciones farmacéuticas moduladoras de c-Met
DK2621481T4 (da) 2010-09-27 2023-01-09 Exelixis Inc Dobbelte inhibitorer af MET og VEGF til behandling af kastrationsresistent prostatacancer og osteoblastiske knoglemetastaser
US20140066444A1 (en) 2010-09-27 2014-03-06 Exelixis, Inc. Method of Treating Cancer
EP2621483A1 (en) 2010-09-27 2013-08-07 Exelixis, Inc. Dual inhibitors of met and vegf for the treatment of castration resistant prostate cancer and osteoblastic bone metastases
JP2013543011A (ja) 2010-11-22 2013-11-28 グラクソスミスクライン、インテレクチュアル、プロパティー、ナンバー２、リミテッド 癌の治療法
KR20140002711A (ko) * 2010-12-23 2014-01-08 네스텍 소시에테아노님 항체-기반 어레이를 사용한 악성 암 치료를 위한 약물 선별법
CN102093421B (zh) 2011-01-28 2014-07-02 北京康辰药业有限公司 一种含磷取代基的喹啉类化合物及其制备方法、以及含有该化合物的药物组合物及其应用
TW201309650A (zh) 2011-02-10 2013-03-01 Exelixis Inc 製造喹啉化合物之方法及包含該化合物之醫藥組合物
US20120252840A1 (en) 2011-04-04 2012-10-04 Exelixis, Inc. Method of Treating Cancer
BR212013028314U2 (pt) 2011-05-02 2015-11-03 Exelixis Inc método para tratar câncer e dor de câncer de osso
TW201306842A (zh) 2011-06-15 2013-02-16 Exelixis Inc 使用ｐｉ３ｋ／ｍｔｏｒ吡啶並嘧啶酮抑制劑及苯達莫司汀及／或利妥昔單抗治療惡性血液疾病之組合療法
UA115866C2 (uk) 2011-09-22 2018-01-10 Екселіксіс, Інк. Спосіб лікування остеопорозу
HUE048023T2 (hu) 2011-10-20 2020-05-28 Exelixis Inc Eljárás kinolin-származékok elõállítására
WO2013070890A1 (en) 2011-11-08 2013-05-16 Exelixis, Inc. Dual inhibitor of met and vegf for treating cancer
JP2015515988A (ja) 2012-05-02 2015-06-04 エクセリクシス， インク． 溶骨性骨転移を治療するためのｍｅｔ−ｖｅｇｆ二重調節剤
ES2726605T3 (es) 2012-09-07 2019-10-08 Exelixis Inc Inhibidores de MET, VEGFR y RET para usar en el tratamiento del adenocarcinoma de pulmón
CN103664776B (zh) * 2012-09-26 2016-05-04 正大天晴药业集团股份有限公司 一种酪氨酸激酶抑制剂及其中间体的制备方法
US20140221372A1 (en) 2013-02-06 2014-08-07 GlaxoSmithKline Intellectual Property (NO 2.) Limited Method of administration and treatment
WO2014145693A1 (en) 2013-03-15 2014-09-18 Exelixis, Inc. Metabolites of n-[3-fluoro-4-({ 6-(methyloxy)-7-[(3-morpholin-4-ylpropyl)oxy]quinolin-4-yl}oxy)phenyl]-n'-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide
NZ712330A (en) 2013-03-15 2020-04-24 Exelixis Inc Metabolites of n-(4-{ [6,7-bis(methyloxy)quinolin-4-yl]oxy} phenyl)-n’-(4-fluorophenyl) cyclopropane-1,1-dicarboxamide
US11564915B2 (en) 2013-04-04 2023-01-31 Exelixis, Inc. Cabozantinib dosage form and use in the treatment of cancer
MX2015014046A (es) 2013-04-04 2016-05-16 Exelixis Inc Combinaciones de farmacos para tratar cancer.
BR112016018450A2 (pt) 2014-02-14 2018-09-18 Exelixis Inc formas sólidas cristalinas de n-{4-[(6,7-dimetoxiquinolin-4-il)oxi]fenil}-n'-(4-fluorofenil)ciclopropano-1,1-dicarboxamida, processos de preparo e métodos de uso
EP3119476A1 (en) 2014-03-17 2017-01-25 Exelixis, Inc. Dosing of cabozantinib formulations
ES2929888T3 (es) 2014-07-31 2022-12-02 Exelixis Inc Procedimiento para preparar cabozantinib marcado con flúor 18 y sus análogos

Also Published As

Publication number Publication date
MX366003B (es) 2019-06-24
ES2729626T3 (es) 2019-11-05
CA2907334A1 (en) 2014-09-18
KR102276348B1 (ko) 2021-07-12
US20210002228A1 (en) 2021-01-07
GEP20196995B (en) 2019-07-25
WO2014145715A1 (en) 2014-09-18
MX2015012490A (es) 2016-05-24
AU2018204666A1 (en) 2018-07-19
ZA201506842B (en) 2017-08-30
KR20150130376A (ko) 2015-11-23
JP2016516074A (ja) 2016-06-02
UA119321C2 (uk) 2019-06-10
BR112015023109A2 (pt) 2018-05-15
NZ712330A (en) 2020-04-24
HK1220447A1 (zh) 2017-05-05
IL241577B (en) 2019-11-28
CN105121412B (zh) 2019-07-12
US20190218182A1 (en) 2019-07-18
AU2014232714B2 (en) 2018-07-19
JP6389238B2 (ja) 2018-09-12
EA033786B1 (ru) 2019-11-26
AU2014232714A1 (en) 2015-10-08
US20160031818A1 (en) 2016-02-04
CA2907334C (en) 2021-12-07
US10273211B2 (en) 2019-04-30
EP2970126B1 (en) 2019-03-06
CN105121412A (zh) 2015-12-02
EP2970126A1 (en) 2016-01-20

Similar Documents

Publication Publication Date Title
EA201591756A1 (ru) Метаболиты n-(4-{[6,7-бис-(метилокси)хинолин-4-ил]окси}фенил)-n'-(4-фторфенил)циклопропан-1,1-дикарбоксамида
CR20150500A (es) Derivados de 3-acetilamino-1 (fenil-heteroaril- aminocarbonil o fenil-heteroaril-carbonilamino) benceno para el tratamiento de desordenes hiperproliferativos
UA110880C2 (uk) Заміщені амідином бета-лактами, їх одержання та застосування як антибактеріальних засобів
EA201690598A1 (ru) Аминогетероарил бензамиды в качестве ингибиторов киназы
BR112015022191A8 (pt) compostos heteroarila e usos dos mesmos
EA201490676A1 (ru) Способ лечения остеопороза
EA201400412A1 (ru) ЗАМЕЩЕННЫЕ БЕНЗИЛИНДАЗОЛЫ ДЛЯ ПРИМЕНЕНИЯ В КАЧЕСТВЕ ИНГИБИТОРОВ Bub1 КИНАЗЫ ДЛЯ ЛЕЧЕНИЯ ГИПЕРПРОЛИФЕРАТИВНЫХ ЗАБОЛЕВАНИЙ
RS54873B1 (sr) Policiklična-karbamoilpiridonska jedinjenja i njihova farmaceutska upotreba
EA201691259A1 (ru) РЕГУЛЯТОРЫ Nrf2
EA201591003A1 (ru) Производные бороновой кислоты и их терапевтическое применение
CY1119151T1 (el) Ν-(4-(αζαϊνδαζολ-6-υλ)-φαινυλ)-σουλφοναμιδiα και η χρηση τους ως φαρμακα
EA201501142A1 (ru) Гетероциклические соединения в качестве средств для борьбы с вредителями
EA201591624A1 (ru) Новые производные пиразола
EA201591728A1 (ru) Гетероциклические соединения и способы их применения
EA201600506A1 (ru) КРИСТАЛЛИЧЕСКИЙ КОМПЛЕКС 1-ЦИАНО-2-(4-ЦИКЛОПРОПИЛБЕНЗИЛ)-4-(β-D-ГЛЮКОПИРАНОЗ-1-ИЛ)БЕНЗОЛА, СПОСОБЫ ЕГО ПОЛУЧЕНИЯ И ЕГО ПРИМЕНЕНИЕ ДЛЯ ПРИГОТОВЛЕНИЯ ЛЕКАРСТВЕННЫХ СРЕДСТВ
EA201591064A1 (ru) Новые производные пиридина
EA201590854A1 (ru) Пиридин-2-амиды, пригодные в качестве агонистов каннабиноидного рецептора 2
EA201591451A1 (ru) Модуляторы flap
EA201590552A1 (ru) Аминохинолины в качестве ингибиторов киназы
EA201591567A1 (ru) Новые производные пиридина
EA201600434A1 (ru) Применение производных бензимидазолпролина
EA201592183A1 (ru) Ингибиторы bace
EA201591380A1 (ru) АНТАГОНИСТЫ Kv1.3 И СПОСОБЫ ИХ ПРИМЕНЕНИЯ
EA201890532A1 (ru) Новые аннелированные бензамиды
EA201891804A1 (ru) Тетрациклиновые соединения

Legal Events

Date Code Title Description
MM4A Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s)

Designated state(s): AM AZ KG TJ TM