CN104395284A - 制备喹啉衍生物的方法 - Google Patents

制备喹啉衍生物的方法 Download PDF

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Publication number
CN104395284A
CN104395284A CN201280054241.3A CN201280054241A CN104395284A CN 104395284 A CN104395284 A CN 104395284A CN 201280054241 A CN201280054241 A CN 201280054241A CN 104395284 A CN104395284 A CN 104395284A
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China
Prior art keywords
mixture
compound
formula
acid
dicarboxylic acid
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Pending
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CN201280054241.3A
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English (en)
Chinese (zh)
Inventor
乔·安·威尔逊
斯里拉姆·纳加纳坦
马修·普法伊弗
尼尔·G·安德森
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Exelixis Inc
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Exelixis Inc
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Publication date
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Priority to CN201910783833.2A priority Critical patent/CN110511158A/zh
Publication of CN104395284A publication Critical patent/CN104395284A/zh
Pending legal-status Critical Current

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    • 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
    • C07D215/233—Oxygen atoms attached in position 2 or 4 only one oxygen atom which is attached in position 4
    • 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
    • C07C231/00—Preparation of carboxylic acid amides
    • C07C231/02—Preparation of carboxylic acid amides from carboxylic acids or from esters, anhydrides, or halides thereof by reaction with ammonia or amines
    • 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
    • C07C233/58—Carboxylic 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
    • 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
    • C07C233/59—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 halogen atoms or by nitro or nitroso groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72—Quinazolines; Hydrogenated quinazolines
    • C07D239/86—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 4
    • C07D239/88—Oxygen atoms
    • C07D239/90—Oxygen 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)
CN201280054241.3A 2011-10-20 2012-10-22 制备喹啉衍生物的方法 Pending CN104395284A (zh)

Priority Applications (1)

Application Number Priority Date Filing Date Title
CN201910783833.2A CN110511158A (zh) 2011-10-20 2012-10-22 制备喹啉衍生物的方法

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201161549312P 2011-10-20 2011-10-20
US61/549312 2011-10-20
PCT/US2012/061320 WO2013059788A1 (en) 2011-10-20 2012-10-22 Process for preparing quinoline derivatives

Related Child Applications (1)

Application Number Title Priority Date Filing Date
CN201910783833.2A Division CN110511158A (zh) 2011-10-20 2012-10-22 制备喹啉衍生物的方法

Publications (1)

Publication Number Publication Date
CN104395284A true CN104395284A (zh) 2015-03-04

Family

ID=47146705

Family Applications (2)

Application Number Title Priority Date Filing Date
CN201280054241.3A Pending CN104395284A (zh) 2011-10-20 2012-10-22 制备喹啉衍生物的方法
CN201910783833.2A Pending CN110511158A (zh) 2011-10-20 2012-10-22 制备喹啉衍生物的方法

Family Applications After (1)

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CN201910783833.2A Pending CN110511158A (zh) 2011-10-20 2012-10-22 制备喹啉衍生物的方法

Country Status (23)

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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=)

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN109836382A (zh) * 2017-11-29 2019-06-04 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
CN112142619A (zh) * 2020-10-20 2020-12-29 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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EA030435B1 (ru) 2010-07-16 2018-08-31 Экселиксис, Инк. ТАБЛЕТКА, СОДЕРЖАЩАЯ МОДУЛЯТОР c-MET В ФОРМЕ КРИСТАЛЛИЧЕСКОЙ L-МАЛАТНОЙ СОЛИ (ВАРИАНТЫ), СПОСОБ ЕЕ ПРОИЗВОДСТВА И СПОСОБ ЛЕЧЕНИЯ ОНКОЛОГИЧЕСКОГО ЗАБОЛЕВАНИЯ С ЕЕ ИСПОЛЬЗОВАНИЕМ
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
CA2907334C (en) 2013-03-15 2021-12-07 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
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
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
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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Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN109836382A (zh) * 2017-11-29 2019-06-04 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
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CN112142619A (zh) * 2020-10-20 2020-12-29 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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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
KR102075371B1 (ko) 2020-02-10
AR088483A1 (es) 2014-06-11

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