KR102075371B1 - 퀴놀린 유도체 제조 방법 - Google Patents

퀴놀린 유도체 제조 방법 Download PDF

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KR102075371B1
KR102075371B1 KR1020147012435A KR20147012435A KR102075371B1 KR 102075371 B1 KR102075371 B1 KR 102075371B1 KR 1020147012435 A KR1020147012435 A KR 1020147012435A KR 20147012435 A KR20147012435 A KR 20147012435A KR 102075371 B1 KR102075371 B1 KR 102075371B1
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compound
mixture
formula
acid
polar aprotic
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KR20140088874A (ko
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조 안 윌슨
스리람 나가나탄
매튜 파이퍼
네일 쥐. 앤더슨
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엑셀리시스, 인코포레이티드
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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

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Quinoline Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
KR1020147012435A 2011-10-20 2012-10-22 퀴놀린 유도체 제조 방법 Active KR102075371B1 (ko)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201161549312P 2011-10-20 2011-10-20
US61/549,312 2011-10-20
PCT/US2012/061320 WO2013059788A1 (en) 2011-10-20 2012-10-22 Process for preparing quinoline derivatives

Publications (2)

Publication Number Publication Date
KR20140088874A KR20140088874A (ko) 2014-07-11
KR102075371B1 true KR102075371B1 (ko) 2020-02-10

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

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MX352926B (es) 2010-09-27 2017-12-14 Exelixis Inc Inhibidores dobles de met y factor de crecimiento endotelial vascular (vegf) para el tratamiento de cancer de prostata resistente a la castracion y metastasis osteoblasticas en los huesos.
BR112013020362A2 (pt) 2011-02-10 2018-05-29 Exelixis Inc processos para a preparação de compostos de quinolina, compostos e combinações farmacêuticas que os contem
US20120252840A1 (en) 2011-04-04 2012-10-04 Exelixis, Inc. Method of Treating Cancer
MX2013012695A (es) 2011-05-02 2014-03-27 Exelixis Inc Metodo para el tratamiento del cancer y el dolor por cancer de hueso.
EP2758057B1 (en) 2011-09-22 2017-05-31 Exelixis, Inc. Method for treating osteoporosis
CN104395284A (zh) * 2011-10-20 2015-03-04 埃克塞里艾克西斯公司 制备喹啉衍生物的方法
WO2013166296A1 (en) 2012-05-02 2013-11-07 Exelixis, Inc. A dual met - vegf modulator for treating osteolytic bone metastases
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US11564915B2 (en) 2013-04-04 2023-01-31 Exelixis, Inc. Cabozantinib dosage form and use in the treatment of cancer
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
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
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
EP3174854B1 (en) 2014-07-31 2022-08-24 Exelixis, Inc. Method of preparing fluorine-18 labeled cabozantinib and its analogs
MX382904B (es) 2014-08-05 2025-03-13 Exelixis Inc Combinaciones de fármacos para tratar mieloma múltiple.
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
EP3442531A1 (en) 2016-04-15 2019-02-20 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
CN117402114A (zh) 2018-01-26 2024-01-16 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
TWI831259B (zh) 2018-06-15 2024-02-01 漢達生技醫藥股份有限公司 包含達沙替尼十二烷基硫酸鹽組合物的膠囊
CN115461328B (zh) 2020-04-30 2025-11-07 埃克塞里艾克西斯公司 用于制备激酶抑制剂的方法
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
CA3213086A1 (en) * 2021-03-24 2022-09-29 Ramakrishna Parameshwar Bhat Process for preparation of cabozantinib
WO2024111001A1 (en) * 2022-11-25 2024-05-30 Msn Laboratories Private Limited, R&D Center Crystalline forms of n-(4-(6,7-dimethoxyquinolin-4-yloxy)phenyl)-n'-(4-fluorophenyl) cyclopropane-1,1-dicarboxamide fumarate and process for its preparation
WO2024163400A1 (en) 2023-01-31 2024-08-08 Handa Oncology, Llc Improved cabozantinib compositions and methods of use

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Also Published As

Publication number Publication date
CN104395284A (zh) 2015-03-04
BR112014009302A2 (pt) 2017-05-23
CN110511158A (zh) 2019-11-29
AU2012325768B2 (en) 2017-08-10
JP2017222648A (ja) 2017-12-21
JP2014530880A (ja) 2014-11-20
GEAP201913471A (en) 2019-10-25
DK2768796T3 (da) 2020-02-24
HUE048023T2 (hu) 2020-05-28
IL232139A (en) 2017-11-30
WO2013059788A1 (en) 2013-04-25
PL2768796T3 (pl) 2020-05-18
US20180230100A1 (en) 2018-08-16
AU2017254982A1 (en) 2017-11-23
IL232139A0 (en) 2014-05-28
US20160229805A1 (en) 2016-08-11
MX343288B (es) 2016-11-01
HK1201517A1 (en) 2015-09-04
NZ723880A (en) 2018-03-23
MX2014004583A (es) 2014-10-06
US9365516B2 (en) 2016-06-14
AU2012325768A1 (en) 2014-05-22
CA2852771A1 (en) 2013-04-25
NZ624328A (en) 2016-10-28
JP6208140B2 (ja) 2017-10-04
EA201490831A1 (ru) 2014-09-30
UA116876C2 (uk) 2018-05-25
ES2765013T3 (es) 2020-06-05
US9969692B2 (en) 2018-05-15
US20140256938A1 (en) 2014-09-11
KR20140088874A (ko) 2014-07-11
CA2852771C (en) 2019-11-26
TWI642650B (zh) 2018-12-01
TW201731812A (zh) 2017-09-16
BR112014009302B1 (pt) 2020-04-28
EP2768796A1 (en) 2014-08-27
ZA201402579B (en) 2015-03-25
TW201321342A (zh) 2013-06-01
IN2014CN02971A (https=) 2015-07-03
EA031485B1 (ru) 2019-01-31
TWI619694B (zh) 2018-04-01
PT2768796T (pt) 2020-02-21
GEP20207110B (en) 2020-05-25
EP2768796B1 (en) 2019-11-20
AR088483A1 (es) 2014-06-11

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