JP6208140B2 - キノリン誘導体の調製プロセス - Google Patents
キノリン誘導体の調製プロセス Download PDFInfo
- Publication number
- JP6208140B2 JP6208140B2 JP2014537359A JP2014537359A JP6208140B2 JP 6208140 B2 JP6208140 B2 JP 6208140B2 JP 2014537359 A JP2014537359 A JP 2014537359A JP 2014537359 A JP2014537359 A JP 2014537359A JP 6208140 B2 JP6208140 B2 JP 6208140B2
- Authority
- JP
- Japan
- Prior art keywords
- mixture
- compound
- acid
- formula
- polar aprotic
- Prior art date
- Legal status (The legal status 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 status listed.)
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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)
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 |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017112355A Division JP2017222648A (ja) | 2011-10-20 | 2017-06-07 | キノリン誘導体の調製プロセス |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2014530880A JP2014530880A (ja) | 2014-11-20 |
| JP6208140B2 true JP6208140B2 (ja) | 2017-10-04 |
Family
ID=47146705
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014537359A Active JP6208140B2 (ja) | 2011-10-20 | 2012-10-22 | キノリン誘導体の調製プロセス |
| JP2017112355A Pending JP2017222648A (ja) | 2011-10-20 | 2017-06-07 | キノリン誘導体の調製プロセス |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017112355A Pending JP2017222648A (ja) | 2011-10-20 | 2017-06-07 | キノリン誘導体の調製プロセス |
Country Status (23)
| Country | Link |
|---|---|
| US (3) | US9365516B2 (enExample) |
| EP (1) | EP2768796B1 (enExample) |
| JP (2) | JP6208140B2 (enExample) |
| KR (1) | KR102075371B1 (enExample) |
| CN (2) | CN104395284A (enExample) |
| AR (1) | AR088483A1 (enExample) |
| AU (2) | AU2012325768B2 (enExample) |
| BR (1) | BR112014009302B1 (enExample) |
| CA (1) | CA2852771C (enExample) |
| DK (1) | DK2768796T3 (enExample) |
| EA (1) | EA031485B1 (enExample) |
| ES (1) | ES2765013T3 (enExample) |
| GE (1) | GEP20207110B (enExample) |
| HU (1) | HUE048023T2 (enExample) |
| IL (1) | IL232139A (enExample) |
| IN (1) | IN2014CN02971A (enExample) |
| MX (1) | MX343288B (enExample) |
| PL (1) | PL2768796T3 (enExample) |
| PT (1) | PT2768796T (enExample) |
| TW (2) | TWI619694B (enExample) |
| UA (1) | UA116876C2 (enExample) |
| WO (1) | WO2013059788A1 (enExample) |
| ZA (1) | ZA201402579B (enExample) |
Families Citing this family (27)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2012009722A1 (en) | 2010-07-16 | 2012-01-19 | Exelixis, Inc. | C-met modulator pharmaceutical compositions |
| HUE045810T2 (hu) | 2010-09-27 | 2020-01-28 | Exelixis Inc | MET és VEGF kettõs inhibitorai kasztrációrezisztens prosztatarák és oszteoblasztos csontáttétek kezelésére |
| TW201309650A (zh) | 2011-02-10 | 2013-03-01 | 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 |
| EP2704717A1 (en) | 2011-05-02 | 2014-03-12 | Exelixis, Inc. | Method of treating cancer and bone cancer pain |
| GEP201606523B (en) | 2011-09-22 | 2016-08-10 | Exelixis Inc | Method for treating osteoporosis |
| PL2768796T3 (pl) * | 2011-10-20 | 2020-05-18 | Exelixis, Inc. | Sposób wytwarzania pochodnych chinoliny |
| HK1207587A1 (en) | 2012-05-02 | 2016-02-05 | Exelixis, Inc. | A dual met - vegf modulator for treating osteolytic bone metastases |
| GEP20196995B (en) | 2013-03-15 | 2019-07-25 | Inc Exelixis | 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 |
| EA032757B1 (ru) | 2014-02-14 | 2019-07-31 | Экселиксис, Инк. | Кристаллические твердые формы n-{4-[(6,7-диметоксихинолин-4-ил)окси]фенил}-n'-(4-фторфенил)циклопропан-1,1-дикарбоксамида, способы получения и способы применения |
| CN106255499A (zh) | 2014-03-17 | 2016-12-21 | 埃克塞里艾克西斯公司 | 卡博替尼制剂的给药 |
| 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 |
| EA033834B1 (ru) | 2014-07-31 | 2019-11-29 | Exelixis Inc | Способ получения кабозантиниба, меченного фтором-18, и его аналогов |
| MA40457A (fr) | 2014-08-05 | 2017-06-14 | Exelixis Inc | Combinaison de médicaments pour traiter le myélome multiple |
| CN108026035B (zh) * | 2015-09-02 | 2021-03-30 | 陈昆锋 | 具有蛋白酪氨酸磷酸酶shp-1激动剂活性的化合物 |
| US11141413B2 (en) | 2016-04-15 | 2021-10-12 | Exelixis, Inc. | Method of treating renal cell carcinoma using N-(4-(6,7-dimethoxyquinolin-4-yloxy)phenyl)-N′-(4-fluorophenyl)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 |
| HRP20251184T1 (hr) | 2018-01-26 | 2025-12-05 | Exelixis, Inc. | Spojevi za liječenje poremećaja ovisnih o kinazi |
| TWI787523B (zh) | 2018-06-15 | 2022-12-21 | 漢達生技醫藥股份有限公司 | 達沙替尼十二烷基硫酸鹽之結晶 |
| FI4143169T3 (fi) | 2020-04-30 | 2026-06-08 | Exelixis Inc | Kinaasi-inhibiittorin valmistusmenetelmät |
| 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 |
| CA3202761A1 (en) | 2020-11-25 | 2022-06-02 | Nanocopoeia, Llc | Amorphous cabozantinib particles and uses thereof |
| US20240190825A1 (en) * | 2021-03-24 | 2024-06-13 | Biocon Limited | Process for preparation of cabozantinib |
| 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 |
| KR20250136810A (ko) | 2023-01-31 | 2025-09-16 | 한다 온콜로지, 엘엘씨 | 개선된 카보잔티닙 조성물 및 사용 방법 |
Family Cites Families (29)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2210607B1 (en) | 2003-09-26 | 2011-08-17 | Exelixis Inc. | N-[3-fluoro-4-({6-(methyloxy)-7-[(3-morpholin-4-ylpropyl)oxy]quinolin-4-yl}oxy)phenyl]-N'-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide for the treatment of cancer |
| CA2572331A1 (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 |
| 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 |
| 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 |
| US20130030172A1 (en) | 2008-12-04 | 2013-01-31 | Exelixis, Inc. | Methods of Preparing Quinoline Derivatives |
| TW201920110A (zh) | 2009-01-16 | 2019-06-01 | 美商艾克塞里克斯公司 | 包含n-(4-{[6,7-雙(甲氧基)喹啉-4-基]氧基}苯基)-n'-(4-氟苯基)環丙烷-1,1-二甲醯胺之蘋果酸鹽之醫藥組合物及其用途 |
| 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 | |
| EA201290906A1 (ru) | 2010-03-12 | 2013-03-29 | Экселиксис, Инк. | Кристаллогидратные формы n-[3-фтор-4-({6-(метилокси)-7-[(3-морфолин-4-илпропил)окси]хинолин-4-ил}окси)фенил]-n'-(4-фторфенил)циклопропан-1,1-дикарбоксамида |
| 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 |
| WO2012009722A1 (en) | 2010-07-16 | 2012-01-19 | Exelixis, Inc. | C-met modulator pharmaceutical compositions |
| EP2621482A1 (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 |
| WO2012044577A1 (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 |
| HUE045810T2 (hu) | 2010-09-27 | 2020-01-28 | Exelixis Inc | MET és VEGF kettõs inhibitorai kasztrációrezisztens prosztatarák és oszteoblasztos csontáttétek kezelésére |
| US20130252956A1 (en) | 2010-11-22 | 2013-09-26 | Howard Kallender | Methods of treating cancer |
| TW201309650A (zh) | 2011-02-10 | 2013-03-01 | 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 |
| EP2704717A1 (en) | 2011-05-02 | 2014-03-12 | Exelixis, Inc. | Method of treating cancer and bone cancer pain |
| 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 |
| PL2768796T3 (pl) | 2011-10-20 | 2020-05-18 | Exelixis, Inc. | Sposób wytwarzania pochodnych chinoliny |
| MX2014005458A (es) | 2011-11-08 | 2015-04-16 | Exelixis Inc | Inhibidor doble de met y del factor de crecimiento endotelial vascular (vegf) para el tratamiento del cáncer. |
| HK1207587A1 (en) | 2012-05-02 | 2016-02-05 | Exelixis, Inc. | A dual met - vegf modulator for treating osteolytic bone metastases |
| JP6513567B2 (ja) | 2012-09-07 | 2019-05-15 | エクセリクシス, インク. | 肺腺癌の治療で使用するためのmet、vegfr、およびretの阻害剤 |
-
2012
- 2012-10-22 PL PL12783763T patent/PL2768796T3/pl unknown
- 2012-10-22 CN CN201280054241.3A patent/CN104395284A/zh active Pending
- 2012-10-22 TW TW101139005A patent/TWI619694B/zh active
- 2012-10-22 DK DK12783763.1T patent/DK2768796T3/da active
- 2012-10-22 MX MX2014004583A patent/MX343288B/es active IP Right Grant
- 2012-10-22 CA CA2852771A patent/CA2852771C/en active Active
- 2012-10-22 TW TW106121791A patent/TWI642650B/zh active
- 2012-10-22 GE GEAP201213471A patent/GEP20207110B/en unknown
- 2012-10-22 EP EP12783763.1A patent/EP2768796B1/en active Active
- 2012-10-22 AR ARP120103944 patent/AR088483A1/es not_active Application Discontinuation
- 2012-10-22 UA UAA201405355A patent/UA116876C2/uk unknown
- 2012-10-22 PT PT127837631T patent/PT2768796T/pt unknown
- 2012-10-22 EA EA201490831A patent/EA031485B1/ru unknown
- 2012-10-22 US US14/353,251 patent/US9365516B2/en active Active
- 2012-10-22 BR BR112014009302A patent/BR112014009302B1/pt active IP Right Grant
- 2012-10-22 WO PCT/US2012/061320 patent/WO2013059788A1/en not_active Ceased
- 2012-10-22 AU AU2012325768A patent/AU2012325768B2/en active Active
- 2012-10-22 ES ES12783763T patent/ES2765013T3/es active Active
- 2012-10-22 IN IN2971CHN2014 patent/IN2014CN02971A/en unknown
- 2012-10-22 CN CN201910783833.2A patent/CN110511158A/zh active Pending
- 2012-10-22 KR KR1020147012435A patent/KR102075371B1/ko active Active
- 2012-10-22 HU HUE12783763A patent/HUE048023T2/hu unknown
- 2012-10-22 JP JP2014537359A patent/JP6208140B2/ja active Active
-
2014
- 2014-04-09 ZA ZA2014/02579A patent/ZA201402579B/en unknown
- 2014-04-22 IL IL232139A patent/IL232139A/en active IP Right Grant
-
2016
- 2016-04-20 US US15/133,708 patent/US9969692B2/en active Active
-
2017
- 2017-06-07 JP JP2017112355A patent/JP2017222648A/ja active Pending
- 2017-11-06 AU AU2017254982A patent/AU2017254982A1/en not_active Abandoned
-
2018
- 2018-04-17 US US15/955,246 patent/US20180230100A1/en not_active Abandoned
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