DK2768796T3 - Fremgangsmåde til fremstilling af quinolin-derivater - Google Patents

Fremgangsmåde til fremstilling af quinolin-derivater Download PDF

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Publication number
DK2768796T3
DK2768796T3 DK12783763.1T DK12783763T DK2768796T3 DK 2768796 T3 DK2768796 T3 DK 2768796T3 DK 12783763 T DK12783763 T DK 12783763T DK 2768796 T3 DK2768796 T3 DK 2768796T3
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DK
Denmark
Prior art keywords
preparation
quinoline derivatives
quinoline
derivatives
Prior art date
Application number
DK12783763.1T
Other languages
English (en)
Inventor
Jo Ann Wilson
Sriram Naganathan
Neil G Andersen
Matthew Pfeiffer
Original Assignee
Exelixis Inc
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 Exelixis Inc filed Critical Exelixis Inc
Application granted granted Critical
Publication of DK2768796T3 publication Critical patent/DK2768796T3/da

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D215/00Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02Heterocyclic 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
    • C07D215/16Heterocyclic 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
    • C07D215/20Oxygen atoms
    • C07D215/22Oxygen atoms attached in position 2 or 4
    • C07D215/233Oxygen atoms attached in position 2 or 4 only one oxygen atom which is attached in position 4
    • 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
    • C07C231/00Preparation of carboxylic acid amides
    • C07C231/02Preparation of carboxylic acid amides from carboxylic acids or from esters, anhydrides, or halides thereof by reaction with ammonia or amines
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C233/00Carboxylic acid amides
    • C07C233/57Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of rings other than six-membered aromatic rings
    • C07C233/58Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of rings other than six-membered aromatic rings having the nitrogen atoms of the carboxamide groups bound to hydrogen atoms or to carbon atoms of unsubstituted hydrocarbon radicals
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C233/00Carboxylic acid amides
    • C07C233/57Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of rings other than six-membered aromatic rings
    • C07C233/59Carboxylic 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 halogen atoms or by nitro or nitroso groups
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D215/00Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72Quinazolines; Hydrogenated quinazolines
    • C07D239/86Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 4
    • C07D239/88Oxygen atoms
    • C07D239/90Oxygen atoms with acyclic radicals attached in position 2 or 3
DK12783763.1T 2011-10-20 2012-10-22 Fremgangsmåde til fremstilling af quinolin-derivater DK2768796T3 (da)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201161549312P 2011-10-20 2011-10-20
PCT/US2012/061320 WO2013059788A1 (en) 2011-10-20 2012-10-22 Process for preparing quinoline derivatives

Publications (1)

Publication Number Publication Date
DK2768796T3 true DK2768796T3 (da) 2020-02-24

Family

ID=47146705

Family Applications (1)

Application Number Title Priority Date Filing Date
DK12783763.1T DK2768796T3 (da) 2011-10-20 2012-10-22 Fremgangsmåde til fremstilling af quinolin-derivater

Country Status (24)

Country Link
US (3) US9365516B2 (da)
EP (1) EP2768796B1 (da)
JP (2) JP6208140B2 (da)
KR (1) KR102075371B1 (da)
CN (2) CN104395284A (da)
AR (1) AR088483A1 (da)
AU (2) AU2012325768B2 (da)
BR (1) BR112014009302B1 (da)
CA (1) CA2852771C (da)
DK (1) DK2768796T3 (da)
EA (1) EA031485B1 (da)
ES (1) ES2765013T3 (da)
GE (1) GEP20207110B (da)
HK (1) HK1201517A1 (da)
HU (1) HUE048023T2 (da)
IL (1) IL232139A (da)
IN (1) IN2014CN02971A (da)
MX (1) MX343288B (da)
PL (1) PL2768796T3 (da)
PT (1) PT2768796T (da)
TW (2) TWI619694B (da)
UA (1) UA116876C2 (da)
WO (1) WO2013059788A1 (da)
ZA (1) ZA201402579B (da)

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BR112013000980B1 (pt) 2010-07-16 2022-08-16 Exelixis, Inc Composições farmacêuticas 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
JP2014505109A (ja) 2011-02-10 2014-02-27 エクセリクシス, インク. キノリン化合物およびそのような化合物を含有する医薬組成物の調製方法
US20120252840A1 (en) 2011-04-04 2012-10-04 Exelixis, Inc. Method of Treating Cancer
TW201806598A (zh) 2011-05-02 2018-03-01 艾克塞里克斯公司 治療癌症及骨癌疼痛之方法
BR112014006702A2 (pt) 2011-09-22 2017-06-13 Exelixis Inc método para tratar osteoporose
DK2768796T3 (da) * 2011-10-20 2020-02-24 Exelixis Inc Fremgangsmåde til fremstilling af quinolin-derivater
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
US10273211B2 (en) 2013-03-15 2019-04-30 Exelixis, Inc. Metabolites of N-{4-([6,7-bis(methyloxy)quinolin-4-yl]oxy}phenyl)-N′-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide
ES2927651T3 (es) 2013-04-04 2022-11-10 Exelixis Inc Forma de dosificación de cabozantinib y uso en el tratamiento del cáncer
CN104649969B (zh) * 2013-11-22 2019-02-12 广东东阳光药业有限公司 一种替尼类药物的盐及其制备方法
KR102354963B1 (ko) 2014-02-14 2022-01-21 엑셀리시스, 인코포레이티드 N-{4-[(6,7-다이메톡시퀴놀린-4-일)옥시]페닐}-n'-(4-플루오로페닐) 사이클로프로판-1,1-다이카복스아마이드의 결정질 고체 형태, 제조 방법 및 사용 방법
JP6666849B2 (ja) 2014-03-17 2020-03-18 エグゼリクシス, インコーポレイテッド カボザンチニブ製剤の投与
CN104788372B (zh) * 2014-07-25 2018-01-30 上海圣考医药科技有限公司 一种氘代卡博替尼衍生物、其制备方法、应用及其中间体
ES2929888T3 (es) 2014-07-31 2022-12-02 Exelixis Inc Procedimiento para preparar cabozantinib marcado con flúor 18 y sus análogos
CN106573042A (zh) 2014-08-05 2017-04-19 埃克塞里艾克西斯公司 治疗多发性骨髓瘤的药物组合
WO2017036405A1 (zh) * 2015-09-02 2017-03-09 陈昆锋 具有蛋白酪氨酸磷酸酶shp-1激动剂活性的化合物
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
CN109836382B (zh) * 2017-11-29 2021-11-05 江苏豪森药业集团有限公司 苹果酸卡博替尼及其中间体的制备方法
KR20200115582A (ko) 2018-01-26 2020-10-07 엑셀리시스, 인코포레이티드 키나제-의존성 장애의 치료용 화합물
CN112142619B (zh) * 2020-10-20 2023-01-10 浙江工业大学 一种1,1-环丙烷二羧酸酰胺类化合物及其制备方法和应用

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EP1673085B1 (en) 2003-09-26 2011-11-09 Exelixis, Inc. C-met modulators and methods of use
JP5368701B2 (ja) * 2004-07-02 2013-12-18 エクセリクシス、インコーポレイテッド c−Metモジュレーター及び使用方法
WO2006108059A1 (en) 2005-04-06 2006-10-12 Exelixis, Inc. C-met modulators and methods of use
EP2101759B1 (en) 2006-12-14 2018-10-10 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
US8445509B2 (en) * 2008-05-08 2013-05-21 Takeda Pharmaceutical Company Limited Fused heterocyclic derivatives and use thereof
AR075084A1 (es) * 2008-09-26 2011-03-09 Smithkline Beecham Corp Metodo de preparacion de quinolinil -oxidifenil - ciclopropanodicarboxamidas e intermediarios correspondientes
CA2743416A1 (en) * 2008-11-13 2010-05-20 Exelixis Inc. Methods of preparing quinoline derivatives
TW201028383A (en) 2008-12-04 2010-08-01 Exelixis Inc Methods of preparing quinoline derivatives
KR101733773B1 (ko) 2009-01-16 2017-05-10 엑셀리시스, 인코포레이티드 N-(4-{〔6,7-비스(메틸옥시)퀴놀린-4-일〕옥시}페닐)-n'-(4-플루오로페닐)사이클로프로판-1,1-디카르복사미드의 말산염 및 그 결정형
BR112012001118A2 (pt) 2009-07-17 2016-02-23 Exelixis Inc formas cristalinas de n-[3-flúor-4-({6-(metilóxi)-7-[(3-morfolin-4-ilpropil)óxi]-quinolin-4-il}óxi)fenil]-n'-(4-fluorfenil)ciclopropano-1,1-dicarboxamida, composição farmacêutica com as mesmas, métodos de preparação das mesmas e tratamento de câncer
UA108618C2 (uk) 2009-08-07 2015-05-25 Застосування c-met-модуляторів в комбінації з темозоломідом та/або променевою терапією для лікування раку
WO2011112896A1 (en) 2010-03-12 2011-09-15 Exelixis, Inc Hydrated crystalline forms 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
US20120070368A1 (en) 2010-04-16 2012-03-22 Exelixis, Inc. Methods of Using C-Met Modulators
BR112013000980B1 (pt) 2010-07-16 2022-08-16 Exelixis, Inc Composições farmacêuticas moduladoras de c-met
EP2593091A1 (en) 2010-07-16 2013-05-22 Exelixis, Inc. C-met modulator pharmaceutical compositions
DK2621481T4 (da) 2010-09-27 2023-01-09 Exelixis Inc Dobbelte inhibitorer af MET og VEGF til behandling af kastrationsresistent prostatacancer og osteoblastiske knoglemetastaser
CA2812744A1 (en) 2010-09-27 2012-04-05 Exelixis, Inc. Dual inhibitors of met and vegf for the treatment of castration resistant prostate cancer and osteoblastic bone metastases
JP2013540759A (ja) 2010-09-27 2013-11-07 エクセリクシス, インク. 去勢抵抗性前立腺癌および造骨性転移の治療のためのmetおよびvegfの二元阻害薬
CN103327979A (zh) 2010-11-22 2013-09-25 葛兰素史密斯克莱知识产权(第2号)有限公司 治疗癌症的方法
JP2014505109A (ja) 2011-02-10 2014-02-27 エクセリクシス, インク. キノリン化合物およびそのような化合物を含有する医薬組成物の調製方法
US20120252840A1 (en) 2011-04-04 2012-10-04 Exelixis, Inc. Method of Treating Cancer
TW201806598A (zh) 2011-05-02 2018-03-01 艾克塞里克斯公司 治療癌症及骨癌疼痛之方法
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
BR112014006702A2 (pt) 2011-09-22 2017-06-13 Exelixis Inc método para tratar osteoporose
DK2768796T3 (da) 2011-10-20 2020-02-24 Exelixis Inc Fremgangsmåde til fremstilling af quinolin-derivater
US20140323522A1 (en) 2011-11-08 2014-10-30 Exelixis, Inc. Method of 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
CN114129566A (zh) 2012-09-07 2022-03-04 埃克塞里艾克西斯公司 用于治疗肺腺癌的met、vegfr和ret的抑制剂

Also Published As

Publication number Publication date
BR112014009302A2 (pt) 2017-05-23
WO2013059788A1 (en) 2013-04-25
CA2852771A1 (en) 2013-04-25
JP6208140B2 (ja) 2017-10-04
GEAP201913471A (en) 2019-10-25
PL2768796T3 (pl) 2020-05-18
AU2012325768B2 (en) 2017-08-10
NZ723880A (en) 2018-03-23
IL232139A (en) 2017-11-30
BR112014009302B1 (pt) 2020-04-28
HUE048023T2 (hu) 2020-05-28
AU2012325768A1 (en) 2014-05-22
TW201321342A (zh) 2013-06-01
US20140256938A1 (en) 2014-09-11
CA2852771C (en) 2019-11-26
US9969692B2 (en) 2018-05-15
KR20140088874A (ko) 2014-07-11
IL232139A0 (en) 2014-05-28
PT2768796T (pt) 2020-02-21
TW201731812A (zh) 2017-09-16
AR088483A1 (es) 2014-06-11
JP2017222648A (ja) 2017-12-21
MX343288B (es) 2016-11-01
EP2768796A1 (en) 2014-08-27
ES2765013T3 (es) 2020-06-05
EP2768796B1 (en) 2019-11-20
US20180230100A1 (en) 2018-08-16
UA116876C2 (uk) 2018-05-25
TWI642650B (zh) 2018-12-01
IN2014CN02971A (da) 2015-07-03
CN110511158A (zh) 2019-11-29
EA201490831A1 (ru) 2014-09-30
JP2014530880A (ja) 2014-11-20
MX2014004583A (es) 2014-10-06
AU2017254982A1 (en) 2017-11-23
GEP20207110B (en) 2020-05-25
CN104395284A (zh) 2015-03-04
ZA201402579B (en) 2015-03-25
HK1201517A1 (en) 2015-09-04
US9365516B2 (en) 2016-06-14
US20160229805A1 (en) 2016-08-11
EA031485B1 (ru) 2019-01-31
NZ624328A (en) 2016-10-28
TWI619694B (zh) 2018-04-01
KR102075371B1 (ko) 2020-02-10

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