AU2012325768B2 - Process for preparing quinoline derivatives - Google Patents
Process for preparing quinoline derivatives Download PDFInfo
- Publication number
- AU2012325768B2 AU2012325768B2 AU2012325768A AU2012325768A AU2012325768B2 AU 2012325768 B2 AU2012325768 B2 AU 2012325768B2 AU 2012325768 A AU2012325768 A AU 2012325768A AU 2012325768 A AU2012325768 A AU 2012325768A AU 2012325768 B2 AU2012325768 B2 AU 2012325768B2
- Authority
- AU
- Australia
- Prior art keywords
- mixture
- compound
- approximately
- acid
- isopropyl acetate
- 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.)
- Active
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)
- Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
- Plural Heterocyclic Compounds (AREA)
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| AU2017254982A AU2017254982A1 (en) | 2011-10-20 | 2017-11-06 | Process for preparing quinoline derivatives |
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 |
|---|---|---|---|
| AU2017254982A Division AU2017254982A1 (en) | 2011-10-20 | 2017-11-06 | Process for preparing quinoline derivatives |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| AU2012325768A1 AU2012325768A1 (en) | 2014-05-22 |
| AU2012325768B2 true AU2012325768B2 (en) | 2017-08-10 |
Family
ID=47146705
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| AU2012325768A Active AU2012325768B2 (en) | 2011-10-20 | 2012-10-22 | Process for preparing quinoline derivatives |
| AU2017254982A Abandoned AU2017254982A1 (en) | 2011-10-20 | 2017-11-06 | Process for preparing quinoline derivatives |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| AU2017254982A Abandoned AU2017254982A1 (en) | 2011-10-20 | 2017-11-06 | Process for preparing quinoline derivatives |
Country Status (23)
Families Citing this family (25)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| NZ607118A (en) | 2010-07-16 | 2015-05-29 | Exelixis Inc | C-met modulator pharmaceutical compositions |
| CA2812750C (en) | 2010-09-27 | 2020-10-06 | Exelixis, Inc. | Dual inhibitors of met and vegf for the treatment of castration-resistant prostate cancer and osteoblastic bone metastases |
| 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 |
| UA115527C2 (uk) | 2011-05-02 | 2017-11-27 | Екселіксіс, Інк. | Застосування n-(4-{[6,7-бic(мeтилoкcи)xiнoлiн-4-iл]oкcи}фeнiл)-n'-(4-фтopфeнiл)циклoпpoпaн-1,1-дикapбoкcaмiду для лікування нирково-клітинної карциноми (варіанти) |
| UA115866C2 (uk) | 2011-09-22 | 2018-01-10 | Екселіксіс, Інк. | Спосіб лікування остеопорозу |
| PT2768796T (pt) * | 2011-10-20 | 2020-02-21 | Exelixis Inc | Processo para a preparação de derivados de quinolina |
| WO2013166296A1 (en) | 2012-05-02 | 2013-11-07 | Exelixis, Inc. | A dual met - vegf modulator for treating osteolytic bone metastases |
| NZ712330A (en) | 2013-03-15 | 2020-04-24 | 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 |
| MX384828B (es) | 2014-02-14 | 2025-03-14 | Exelixis Inc | Formas solidas cristalinas de n-{4-[(6,7-dimetoxiquinolin-4-il)oxi]fenil}-n'-(4-fluorofenil)ciclopropan-1,1-dicarboxamida, procesos para elaboracion y metodos de uso. |
| MA39735A (fr) | 2014-03-17 | 2017-01-25 | Exelixis Inc | Dosage de préparations de cabozantinib |
| 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 |
| EP3177311B1 (en) | 2014-08-05 | 2024-10-30 | Exelixis, Inc. | Drug combinations of cabozantinib with proteasome inhibitor to treat multiple myeloma |
| US10745346B2 (en) * | 2015-09-02 | 2020-08-18 | Kuen-Feng Chen | Agonists of protein tyrosine phosphatase SHP-1 |
| RU2748549C2 (ru) | 2016-04-15 | 2021-05-26 | Экселиксис, Инк. | Способ лечения почечно-клеточного рака с использованием n-(4-(6,7-диметоксихинолин-4-илокси)фенил)-n'-(4-фторфенил)циклопропан-1,1-дикарбоксамида, (2s)-гидроксибутандиоата |
| 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 |
| BR112020015201A2 (pt) | 2018-01-26 | 2020-12-29 | Exelixis, Inc. | Compostos para tratamento contra distúrbios dependentes de quinase |
| TWI815137B (zh) | 2018-06-15 | 2023-09-11 | 漢達生技醫藥股份有限公司 | 尼洛替尼十二烷基硫酸鹽之結晶 |
| 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 |
| 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 |
| WO2024163400A1 (en) | 2023-01-31 | 2024-08-08 | Handa Oncology, Llc | Improved cabozantinib compositions and methods of use |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2010056960A1 (en) * | 2008-11-13 | 2010-05-20 | Exelixis Inc. | Methods of preparing quinoline derivatives |
| WO2010083414A1 (en) * | 2009-01-16 | 2010-07-22 | Exelixis, Inc. | Malate salt of n- (4- { [ 6, 7-bis (methyloxy) quin0lin-4-yl] oxy}phenyl-n' - (4 -fluorophenyl) cyclopropane-1-dicarboxamide, and crystalline forms therof for the treatment of cancer |
Family Cites Families (27)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PT2210607E (pt) | 2003-09-26 | 2012-01-31 | Exelixis Inc | N-[3-fluoro-4-({6-(metiloxi)-7-[(3-morfolina-4-ilpropil)oxi]quinolina-4-il}oxi)fenil]-n'-(4-fluorofenil)ciclopropano-1,1-dicarboxamida para o tratamento do cancro |
| WO2006014325A2 (en) * | 2004-07-02 | 2006-02-09 | Exelixis, Inc. | C-met modulators and method of use |
| US20080161305A1 (en) | 2005-04-06 | 2008-07-03 | Exelixis, Inc. | C-Met Modulators and Methods of Use |
| CN105106199A (zh) | 2006-12-14 | 2015-12-02 | 埃克塞利希斯股份有限公司 | 使用mek抑制剂的方法 |
| 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 |
| WO2009136663A1 (en) * | 2008-05-08 | 2009-11-12 | Takeda Pharmaceutical Company Limited | Fused heterocyclic derivatives and use thereof |
| UY32142A (es) | 2008-09-26 | 2010-05-31 | Smithkline Beckman Corp | Preparación de una quinoliniloxidifenilciclopropanodicarboxamida |
| JP2012511017A (ja) | 2008-12-04 | 2012-05-17 | エグゼリクシス， インコーポレイテッド | キノリン誘導体の調製方法 |
| JP2012533570A (ja) | 2009-07-17 | 2012-12-27 | エグゼリクシス， インコーポレイテッド | Ｎ−［３−フルオロ−４−（｛６−（メチルオキシ）−７−［（３−モルホリン−４−イルプロピル）オキシ］−キノリン−４−イル｝オキシ）フェニル］−ｎ’−（４−フルオロフェニル）シクロプロパン−１，１−ジカルボキサミドの結晶形 |
| UA108618C2 (uk) | 2009-08-07 | 2015-05-25 | Застосування c-met-модуляторів в комбінації з темозоломідом та/або променевою терапією для лікування раку | |
| JP2013522232A (ja) | 2010-03-12 | 2013-06-13 | エグゼリクシス， インコーポレイテッド | Ｎ−［３−フルオロ−４−（｛６−（メチロキシ）−７−［（３−モルホリン−４−イルプロピル）オキシ］−キノリン−４−イル｝オキシ）フェニル］−ｎ’−（４−フルオロフェニル）シクロプロパン−１，１−ジカルボサミドの水和結晶性形状 |
| US20120070368A1 (en) | 2010-04-16 | 2012-03-22 | Exelixis, Inc. | Methods of Using C-Met Modulators |
| NZ607118A (en) | 2010-07-16 | 2015-05-29 | Exelixis Inc | C-met modulator pharmaceutical compositions |
| WO2012009723A1 (en) | 2010-07-16 | 2012-01-19 | Exelixis, Inc. | C-met modulator pharmaceutical compositions |
| CN103391772A (zh) | 2010-09-27 | 2013-11-13 | 埃克塞里艾克西斯公司 | 用于治疗去势抵抗性前列腺癌和成骨性骨转移的met和vegf的双重抑制剂 |
| CA2812750C (en) | 2010-09-27 | 2020-10-06 | Exelixis, Inc. | Dual inhibitors of met and vegf for the treatment of castration-resistant prostate cancer and osteoblastic bone metastases |
| US20140057908A1 (en) | 2010-09-27 | 2014-02-27 | Exelixis, Inc. | Method of Treating Cancer |
| EP2643001A4 (en) | 2010-11-22 | 2014-02-19 | Glaxosmithkline Ip Dev Ltd | METHOD OF TREATING CANCER |
| 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 |
| UA115527C2 (uk) | 2011-05-02 | 2017-11-27 | Екселіксіс, Інк. | Застосування n-(4-{[6,7-бic(мeтилoкcи)xiнoлiн-4-iл]oкcи}фeнiл)-n'-(4-фтopфeнiл)циклoпpoпaн-1,1-дикapбoкcaмiду для лікування нирково-клітинної карциноми (варіанти) |
| 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 |
| UA115866C2 (uk) | 2011-09-22 | 2018-01-10 | Екселіксіс, Інк. | Спосіб лікування остеопорозу |
| PT2768796T (pt) | 2011-10-20 | 2020-02-21 | Exelixis Inc | Processo para a preparação de derivados de quinolina |
| TW201818937A (zh) | 2011-11-08 | 2018-06-01 | 美商艾克塞里克斯公司 | 治療癌症之方法 |
| WO2013166296A1 (en) | 2012-05-02 | 2013-11-07 | Exelixis, Inc. | A dual met - vegf modulator for treating osteolytic bone metastases |
| CN104703600A (zh) | 2012-09-07 | 2015-06-10 | 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 |
-
2012
- 2012-10-22 PT PT127837631T patent/PT2768796T/pt unknown
- 2012-10-22 TW TW101139005A patent/TWI619694B/zh active
- 2012-10-22 BR BR112014009302A patent/BR112014009302B1/pt active IP Right Grant
- 2012-10-22 GE GEAP201213471A patent/GEP20207110B/en unknown
- 2012-10-22 EA EA201490831A patent/EA031485B1/ru unknown
- 2012-10-22 IN IN2971CHN2014 patent/IN2014CN02971A/en unknown
- 2012-10-22 UA UAA201405355A patent/UA116876C2/uk unknown
- 2012-10-22 DK DK12783763.1T patent/DK2768796T3/da active
- 2012-10-22 CN CN201910783833.2A patent/CN110511158A/zh active Pending
- 2012-10-22 AU AU2012325768A patent/AU2012325768B2/en active Active
- 2012-10-22 ES ES12783763T patent/ES2765013T3/es active Active
- 2012-10-22 KR KR1020147012435A patent/KR102075371B1/ko active Active
- 2012-10-22 WO PCT/US2012/061320 patent/WO2013059788A1/en active Application Filing
- 2012-10-22 PL PL12783763T patent/PL2768796T3/pl unknown
- 2012-10-22 CN CN201280054241.3A patent/CN104395284A/zh active Pending
- 2012-10-22 AR ARP120103944 patent/AR088483A1/es not_active Application Discontinuation
- 2012-10-22 JP JP2014537359A patent/JP6208140B2/ja active Active
- 2012-10-22 CA CA2852771A patent/CA2852771C/en active Active
- 2012-10-22 EP EP12783763.1A patent/EP2768796B1/en active Active
- 2012-10-22 US US14/353,251 patent/US9365516B2/en active Active
- 2012-10-22 HU HUE12783763A patent/HUE048023T2/hu unknown
- 2012-10-22 TW TW106121791A patent/TWI642650B/zh active
- 2012-10-22 MX MX2014004583A patent/MX343288B/es active IP Right Grant
-
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
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2010056960A1 (en) * | 2008-11-13 | 2010-05-20 | Exelixis Inc. | Methods of preparing quinoline derivatives |
| WO2010083414A1 (en) * | 2009-01-16 | 2010-07-22 | Exelixis, Inc. | Malate salt of n- (4- { [ 6, 7-bis (methyloxy) quin0lin-4-yl] oxy}phenyl-n' - (4 -fluorophenyl) cyclopropane-1-dicarboxamide, and crystalline forms therof for the treatment of cancer |
Non-Patent Citations (1)
| Title |
|---|
| SAAVEDRA, O. ET. AL. Bioorganic & Medicinal Chemistry Letters, 2009, 19, 6836-6839 * |
Also Published As
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| AU2012325768B2 (en) | Process for preparing quinoline derivatives | |
| JP6513598B2 (ja) | 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 | |
| AU2011307306A1 (en) | Dual inhibitors of MET and VEGF for the treatment of castration resistant prostate cancer and osteoblastic bone metastases | |
| US20100273808A1 (en) | Lactate salt of 4-[6-methoxy-7-(3-piperidin-1-yl-propoxy)quinazolin-4-yl]piperazine-1-carboxylic acid(4-isopropoxyphenyl)-amide and pharmaceutical compositions thereof for the treatment of cancer and other diseases or disorders | |
| KR20180111797A (ko) | 퀴놀론 유사체의 결정형 및 그것의 염 | |
| WO2016101867A1 (zh) | 萘普替尼对甲苯磺酸盐的α晶型及制备方法和含有其的药物组合物 | |
| US20150133460A1 (en) | Lactate salt of 4-[6-methoxy-7-(3-piperidin-1-yl-propoxy)quinazolin-4-yl]piperazine-1-carboxylic acid(4-isopropoxyphenyl)-amide and pharmaceutical compositions thereof for the treatment of cancer and other diseases or disorders | |
| NZ723880B2 (en) | Process for preparing quinoline derivatives | |
| NZ624328B2 (en) | Process for preparing quinoline derivatives | |
| HK1201517B (en) | Process for preparing quinoline derivatives |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FGA | Letters patent sealed or granted (standard patent) |