UA116876C2 - Спосіб одержання хінолінових похідних - Google Patents

Спосіб одержання хінолінових похідних

Info

Publication number
UA116876C2
UA116876C2 UAA201405355A UAA201405355A UA116876C2 UA 116876 C2 UA116876 C2 UA 116876C2 UA A201405355 A UAA201405355 A UA A201405355A UA A201405355 A UAA201405355 A UA A201405355A UA 116876 C2 UA116876 C2 UA 116876C2
Authority
UA
Ukraine
Prior art keywords
formula
compound
embed isisserver
quinoline derivatives
аlкуl
Prior art date
Application number
UAA201405355A
Other languages
English (en)
Inventor
Джо Енн Уілсон
Срірам Наганатхан
Меттью Пфайффер
Ніл Г. Андерсен
Original Assignee
Екселіксіс, Інк.
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 Екселіксіс, Інк. filed Critical Екселіксіс, Інк.
Publication of UA116876C2 publication Critical patent/UA116876C2/uk

Links

Classifications

    • 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

Landscapes

  • 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)

Abstract

Винахід стосується способу одержання сполуки Формули І, де: R1 є галогеном; R2 є галогеном; R3 є (С1-С6)алкілом або (С1-С6)алкілом, необов'язково заміщеним гетероціклоалкілом; R4 є (С1-С6)алкілом; і Q є СН або N, що включає: (а) взаємодію 1,1-циклопропандикарбонової кислоти з тіонілхлоридом у полярному апротонному розчиннику при температурі навколишнього середовища; (b) додавання третинної амінної основи до суміші стадії (а) з утворенням сполуки Формули А; і (с) зв'язування сполуки Формули А з аміном Формули В з утворенням сполуки Формули І. EMBED ISISServer EMBED ISISServer EMBED ISISServer EMBED ISISServer
UAA201405355A 2011-10-20 2012-10-22 Спосіб одержання хінолінових похідних UA116876C2 (uk)

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
UA116876C2 true UA116876C2 (uk) 2018-05-25

Family

ID=47146705

Family Applications (1)

Application Number Title Priority Date Filing Date
UAA201405355A UA116876C2 (uk) 2011-10-20 2012-10-22 Спосіб одержання хінолінових похідних

Country Status (23)

Country Link
US (3) US9365516B2 (uk)
EP (1) EP2768796B1 (uk)
JP (2) JP6208140B2 (uk)
KR (1) KR102075371B1 (uk)
CN (2) CN110511158A (uk)
AR (1) AR088483A1 (uk)
AU (2) AU2012325768B2 (uk)
BR (1) BR112014009302B1 (uk)
CA (1) CA2852771C (uk)
DK (1) DK2768796T3 (uk)
EA (1) EA031485B1 (uk)
ES (1) ES2765013T3 (uk)
GE (1) GEP20207110B (uk)
HU (1) HUE048023T2 (uk)
IL (1) IL232139A (uk)
IN (1) IN2014CN02971A (uk)
MX (1) MX343288B (uk)
PL (1) PL2768796T3 (uk)
PT (1) PT2768796T (uk)
TW (2) TWI642650B (uk)
UA (1) UA116876C2 (uk)
WO (1) WO2013059788A1 (uk)
ZA (1) ZA201402579B (uk)

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DK2621481T4 (da) 2010-09-27 2023-01-09 Exelixis Inc Dobbelte inhibitorer af MET og VEGF til behandling af kastrationsresistent prostatacancer og osteoblastiske knoglemetastaser
TWI640509B (zh) 2011-02-10 2018-11-11 艾克塞里克斯公司 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
TWI610918B (zh) 2011-05-02 2018-01-11 艾克塞里克斯公司 治療癌症及骨癌疼痛之方法
GEP201606523B (en) 2011-09-22 2016-08-10 Exelixis Inc Method for treating osteoporosis
EP2768796B1 (en) * 2011-10-20 2019-11-20 Exelixis, Inc. Process for preparing quinoline derivatives
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
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AU2015218236B2 (en) 2014-02-14 2019-06-13 Exelixis, Inc. Crystalline solid forms of N-{4-[(6,7-dimethoxyquinolin-4-yl)oxy]phenyl}-N'-(4-fluorophenyl) cyclopropane-1, 1-dicarboxamide, processes for making, and methods of use
US10159666B2 (en) 2014-03-17 2018-12-25 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
CN106715397B (zh) 2014-07-31 2021-07-23 埃克塞里艾克西斯公司 制备氟-18标记的卡博替尼及其类似物的方法
BR112017002318A2 (pt) 2014-08-05 2018-07-17 Exelixis, Inc. combinações de fármacos para tratar mieloma múltiplo.
US10745346B2 (en) * 2015-09-02 2020-08-18 Kuen-Feng Chen Agonists of protein tyrosine phosphatase SHP-1
CN109069499A (zh) 2016-04-15 2018-12-21 埃克塞里艾克西斯公司 使用 n-(4-(6,7-二甲氧基喹啉-4-基氧基)苯基)-n’-(4-氟苯基)环丙烷-1,1-二甲酰胺,(2s)-羟基丁二酸盐治疗肾细胞癌的方法
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
GEAP202415420A (en) 2018-01-26 2024-12-25 Exelixis Inc Compounds for the treatment of kinase-dependent disorders
CN120305263A (zh) 2018-06-15 2025-07-15 汉达癌症医药责任有限公司 卡博替尼的盐类于制备治疗癌症的剂型的用途
PE20230110A1 (es) 2020-04-30 2023-01-25 Exelixis Inc Procesos para la preparacion de un inhibidor de cinasa
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
KR20240006021A (ko) * 2021-03-24 2024-01-12 바이오콘 리미티드 카보잔티닙의 제조방법
AU2023384196A1 (en) * 2022-11-25 2025-06-12 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
AU2024215796A1 (en) 2023-01-31 2025-05-15 Handa Oncology, Llc Improved cabozantinib compositions and methods of use

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TWI640509B (zh) 2011-02-10 2018-11-11 艾克塞里克斯公司 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
TWI610918B (zh) 2011-05-02 2018-01-11 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
GEP201606523B (en) 2011-09-22 2016-08-10 Exelixis Inc Method for treating osteoporosis
EP2768796B1 (en) 2011-10-20 2019-11-20 Exelixis, Inc. Process for preparing quinoline derivatives
EP2776033A1 (en) 2011-11-08 2014-09-17 Exelixis, Inc. Dual inhibitor of met and vegf for treating cancer
WO2013166296A1 (en) 2012-05-02 2013-11-07 Exelixis, Inc. A dual met - vegf modulator for treating osteolytic bone metastases
EP2892532B1 (en) 2012-09-07 2019-02-13 Exelixis, Inc. Inhibitors of met, vegfr and ret for use in the treatment of lung adenocarcinoma

Also Published As

Publication number Publication date
IL232139A (en) 2017-11-30
EP2768796A1 (en) 2014-08-27
JP6208140B2 (ja) 2017-10-04
BR112014009302A2 (pt) 2017-05-23
ZA201402579B (en) 2015-03-25
CN110511158A (zh) 2019-11-29
TWI619694B (zh) 2018-04-01
JP2017222648A (ja) 2017-12-21
US20160229805A1 (en) 2016-08-11
AU2012325768B2 (en) 2017-08-10
EA031485B1 (ru) 2019-01-31
GEP20207110B (en) 2020-05-25
AU2017254982A1 (en) 2017-11-23
MX343288B (es) 2016-11-01
KR102075371B1 (ko) 2020-02-10
MX2014004583A (es) 2014-10-06
US9365516B2 (en) 2016-06-14
CA2852771A1 (en) 2013-04-25
ES2765013T3 (es) 2020-06-05
PL2768796T3 (pl) 2020-05-18
PT2768796T (pt) 2020-02-21
HK1201517A1 (en) 2015-09-04
IL232139A0 (en) 2014-05-28
AR088483A1 (es) 2014-06-11
AU2012325768A1 (en) 2014-05-22
WO2013059788A1 (en) 2013-04-25
TW201731812A (zh) 2017-09-16
BR112014009302B1 (pt) 2020-04-28
TW201321342A (zh) 2013-06-01
EP2768796B1 (en) 2019-11-20
JP2014530880A (ja) 2014-11-20
DK2768796T3 (da) 2020-02-24
US20180230100A1 (en) 2018-08-16
HUE048023T2 (hu) 2020-05-28
GEAP201913471A (en) 2019-10-25
EA201490831A1 (ru) 2014-09-30
TWI642650B (zh) 2018-12-01
US9969692B2 (en) 2018-05-15
IN2014CN02971A (uk) 2015-07-03
NZ624328A (en) 2016-10-28
CN104395284A (zh) 2015-03-04
NZ723880A (en) 2018-03-23
CA2852771C (en) 2019-11-26
US20140256938A1 (en) 2014-09-11
KR20140088874A (ko) 2014-07-11

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