CA2907334C - Metabolites of n-(4-{[6,7-bis(methyloxy)quinolin-4-yl]oxy}phenyl)-n'-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide - Google Patents
Metabolites of n-(4-{[6,7-bis(methyloxy)quinolin-4-yl]oxy}phenyl)-n'-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide Download PDFInfo
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- CA2907334C CA2907334C CA2907334A CA2907334A CA2907334C CA 2907334 C CA2907334 C CA 2907334C CA 2907334 A CA2907334 A CA 2907334A CA 2907334 A CA2907334 A CA 2907334A CA 2907334 C CA2907334 C CA 2907334C
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- metabolite
- pharmaceutically acceptable
- acceptable salt
- cabozantinib
- lel
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- 229940116362 tragacanth Drugs 0.000 description 1
- 230000009466 transformation Effects 0.000 description 1
- 238000000844 transformation Methods 0.000 description 1
- 206010044412 transitional cell carcinoma Diseases 0.000 description 1
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Classifications
-
- 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
- C07C233/60—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 singly-bound oxygen atoms
-
- 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
- C07C305/00—Esters of sulfuric acids
- C07C305/22—Esters of sulfuric acids having oxygen atoms of sulfate groups bound to carbon atoms of six-membered aromatic rings
- C07C305/24—Esters of sulfuric acids having oxygen atoms of sulfate groups bound to carbon atoms of six-membered aromatic rings of non-condensed six-membered aromatic rings
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
- C07D215/58—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems with hetero atoms directly attached to the ring nitrogen atom
- C07D215/60—N-oxides
-
- G—PHYSICS
- G01—MEASURING; TESTING
- G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
- G01N33/00—Investigating or analysing materials by specific methods not covered by groups G01N1/00 - G01N31/00
- G01N33/48—Biological material, e.g. blood, urine; Haemocytometers
- G01N33/483—Physical analysis of biological material
- G01N33/487—Physical analysis of biological material of liquid biological material
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C2601/00—Systems containing only non-condensed rings
- C07C2601/02—Systems containing only non-condensed rings with a three-membered ring
-
- G—PHYSICS
- G01—MEASURING; TESTING
- G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
- G01N2570/00—Omics, e.g. proteomics, glycomics or lipidomics; Methods of analysis focusing on the entire complement of classes of biological molecules or subsets thereof, i.e. focusing on proteomes, glycomes or lipidomes
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Engineering & Computer Science (AREA)
- Biomedical Technology (AREA)
- Physics & Mathematics (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Biophysics (AREA)
- Pathology (AREA)
- Immunology (AREA)
- General Physics & Mathematics (AREA)
- Biochemistry (AREA)
- Analytical Chemistry (AREA)
- Food Science & Technology (AREA)
- Urology & Nephrology (AREA)
- Hematology (AREA)
- Molecular Biology (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Epidemiology (AREA)
- Saccharide Compounds (AREA)
- Quinoline Compounds (AREA)
- Pain & Pain Management (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201361792413P | 2013-03-15 | 2013-03-15 | |
| US61/792,413 | 2013-03-15 | ||
| PCT/US2014/030524 WO2014145715A1 (en) | 2013-03-15 | 2014-03-17 | Metabolites of n-(4-{[6,7-bis(methyloxy)quinolin-4-yl]oxy}phenyl)-n'-(4-fluorophenyl) cyclopropane-1,1-dicarboxamide |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CA2907334A1 CA2907334A1 (en) | 2014-09-18 |
| CA2907334C true CA2907334C (en) | 2021-12-07 |
Family
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CA2907334A Active CA2907334C (en) | 2013-03-15 | 2014-03-17 | Metabolites of n-(4-{[6,7-bis(methyloxy)quinolin-4-yl]oxy}phenyl)-n'-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide |
Country Status (17)
| Country | Link |
|---|---|
| US (4) | US10273211B2 (enExample) |
| EP (1) | EP2970126B1 (enExample) |
| JP (1) | JP6389238B2 (enExample) |
| KR (1) | KR102276348B1 (enExample) |
| CN (1) | CN105121412B (enExample) |
| AU (2) | AU2014232714B2 (enExample) |
| BR (1) | BR112015023109A2 (enExample) |
| CA (1) | CA2907334C (enExample) |
| EA (1) | EA033786B1 (enExample) |
| ES (1) | ES2729626T3 (enExample) |
| GE (1) | GEP20196995B (enExample) |
| IL (1) | IL241577B (enExample) |
| MX (1) | MX366003B (enExample) |
| NZ (1) | NZ712330A (enExample) |
| UA (1) | UA119321C2 (enExample) |
| WO (1) | WO2014145715A1 (enExample) |
| ZA (1) | ZA201506842B (enExample) |
Families Citing this family (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP6158705B2 (ja) | 2010-09-27 | 2017-07-05 | エクセリクシス， インク． | 去勢抵抗性前立腺癌および造骨性転移の治療のためのｍｅｔおよびｖｅｇｆの二元阻害薬 |
| KR20210147117A (ko) | 2011-02-10 | 2021-12-06 | 엑셀리시스, 인코포레이티드 | 퀴놀린 화합물들의 제조 방법들 및 상기 화합물들을 함유하는 약학 조성물들 |
| EP2844254A1 (en) | 2012-05-02 | 2015-03-11 | Exelixis, Inc. | A dual met - vegf modulator for treating osteolytic bone metastases |
| BR112015023109A2 (pt) | 2013-03-15 | 2018-05-15 | Exelixis Inc | Metabolitos de n-(4-{[6,7-bis(metiloxi)quinoloin-4-il] oxi}fenil)-n -(4-fluorofenil)ciclopropano-1, 1- dicarboxamida |
| ES2927651T3 (es) | 2013-04-04 | 2022-11-10 | Exelixis Inc | Forma de dosificación de cabozantinib y uso en el tratamiento del cáncer |
| UA123534C2 (uk) | 2014-02-14 | 2021-04-21 | Екселіксис, Інк. | Кристалічні тверді форми n-{4-[(6,7-диметоксихінолін-4-іл)окси]феніл}-n'-(4-флуорофеніл)циклопропан-1,1-дикарбоксаміду, способи отримання і способи застосування |
| JP6666849B2 (ja) * | 2014-03-17 | 2020-03-18 | エグゼリクシス， インコーポレイテッド | カボザンチニブ製剤の投与 |
| 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 |
| AU2015301097B2 (en) | 2014-08-05 | 2021-03-04 | Exelixis, Inc. | Drug combinations to treat multiple myeloma |
| 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 |
| CN107556238A (zh) * | 2016-06-30 | 2018-01-09 | 深圳万乐药业有限公司 | 一种卡博替尼的合成方法 |
| US11542259B2 (en) | 2018-01-26 | 2023-01-03 | Exelixis, Inc. | Compounds for the treatment of kinase-dependent disorders |
| CN116808044A (zh) | 2018-06-15 | 2023-09-29 | 汉达癌症医药责任有限公司 | 激酶抑制剂的盐类及其组合物 |
| CN110423218A (zh) * | 2019-08-09 | 2019-11-08 | 新乡双鹭药业有限公司 | 一种苹果酸卡博替尼合成中杂质的制备方法 |
| CN120239695A (zh) * | 2022-12-01 | 2025-07-01 | 江苏奥赛康药业有限公司 | 一种制备卡博替尼及其中间体的方法 |
| KR20250136810A (ko) | 2023-01-31 | 2025-09-16 | 한다 온콜로지, 엘엘씨 | 개선된 카보잔티닙 조성물 및 사용 방법 |
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| ES2436888T3 (es) | 2003-09-26 | 2014-01-07 | Exelixis, Inc | Moduladores c-Met y métodos de uso |
| EP1773826A4 (en) | 2004-07-02 | 2009-06-03 | Exelixis Inc | MODULATORS OF C-MET AND THEIR METHOD OF USE |
| CA2603748A1 (en) | 2005-04-06 | 2006-10-12 | Exelixis, Inc. | C-met modulators and methods of use |
| UY30183A1 (es) | 2006-03-02 | 2007-10-31 | Astrazeneca Ab | Derivados de quinolina |
| JP5311673B2 (ja) | 2006-12-14 | 2013-10-09 | エグゼリクシス， インコーポレイテッド | Ｍｅｋ阻害剤の使用方法 |
| 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 |
| AR075084A1 (es) | 2008-09-26 | 2011-03-09 | Smithkline Beecham Corp | Metodo de preparacion de quinolinil -oxidifenil - ciclopropanodicarboxamidas e intermediarios correspondientes |
| MX2011005038A (es) | 2008-11-13 | 2011-06-16 | Exelisis Inc | Metodo de preparacion de derivados de quinolina. |
| EP2367795A1 (en) | 2008-12-04 | 2011-09-28 | Exelixis, Inc. | Methods of preparing quinoline derivatives |
| CA2995880C (en) | 2009-01-16 | 2021-01-05 | Exelixis, Inc. | Processes for preparing n-(4-{[6,7-bis(methyloxy)quinolin-4-yl]oxy}phenyl)-n'-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide |
| TW201118072A (en) | 2009-07-17 | 2011-06-01 | Exelixis Inc | Crystalline forms of N-[3-fluoro-4-({6-(methyloxy)-7-[(3-morpholin-4-ylpropyl)oxy]-quinolin-4-yl}oxy)phenyl]-N'-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide |
| 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 |
| IL224189A (en) | 2010-07-16 | 2017-07-31 | Exelixis Inc | C-met modulator pharmaceutical compositions |
| US20140186407A9 (en) | 2010-07-16 | 2014-07-03 | Exelixis Inc. | C-Met Modulator Pharmaceutical Compositions |
| JP6158705B2 (ja) | 2010-09-27 | 2017-07-05 | エクセリクシス， インク． | 去勢抵抗性前立腺癌および造骨性転移の治療のためのｍｅｔおよびｖｅｇｆの二元阻害薬 |
| CA2812744A1 (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 |
| 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 |
| EP2643001A4 (en) | 2010-11-22 | 2014-02-19 | Glaxosmithkline Ip Dev Ltd | METHOD OF TREATING CANCER |
| JP2014503821A (ja) * | 2010-12-23 | 2014-02-13 | ネステク ソシエテ アノニム | 抗体ベースのアレイを用いる悪性がんの療法のための薬剤選択 |
| CN102093421B (zh) | 2011-01-28 | 2014-07-02 | 北京康辰药业有限公司 | 一种含磷取代基的喹啉类化合物及其制备方法、以及含有该化合物的药物组合物及其应用 |
| KR20210147117A (ko) | 2011-02-10 | 2021-12-06 | 엑셀리시스, 인코포레이티드 | 퀴놀린 화합물들의 제조 방법들 및 상기 화합물들을 함유하는 약학 조성물들 |
| US20120252840A1 (en) | 2011-04-04 | 2012-10-04 | Exelixis, Inc. | Method of Treating Cancer |
| GEP201706678B (en) | 2011-05-02 | 2017-06-12 | Exelixis Inc | Method of treating cancer and bone cancer |
| 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 |
| CA2848512A1 (en) | 2011-09-22 | 2013-03-28 | Exelixis, Inc. | Method for treating osteoporosis |
| MX343288B (es) | 2011-10-20 | 2016-11-01 | Exelixis Inc | Proceso para la preparación de derivados de quinolina. |
| US20140323522A1 (en) | 2011-11-08 | 2014-10-30 | Exelixis, Inc. | Method of Treating Cancer |
| EP2844254A1 (en) | 2012-05-02 | 2015-03-11 | Exelixis, Inc. | A dual met - vegf modulator for treating osteolytic bone metastases |
| ES2726605T3 (es) | 2012-09-07 | 2019-10-08 | Exelixis Inc | Inhibidores de MET, VEGFR y RET para usar en el tratamiento del adenocarcinoma de pulmón |
| CN103664776B (zh) * | 2012-09-26 | 2016-05-04 | 正大天晴药业集团股份有限公司 | 一种酪氨酸激酶抑制剂及其中间体的制备方法 |
| US20140221372A1 (en) | 2013-02-06 | 2014-08-07 | GlaxoSmithKline Intellectual Property (NO 2.) Limited | Method of administration and treatment |
| BR112015023109A2 (pt) | 2013-03-15 | 2018-05-15 | Exelixis Inc | Metabolitos de n-(4-{[6,7-bis(metiloxi)quinoloin-4-il] oxi}fenil)-n -(4-fluorofenil)ciclopropano-1, 1- dicarboxamida |
| WO2014145693A1 (en) | 2013-03-15 | 2014-09-18 | Exelixis, Inc. | Metabolites of n-[3-fluoro-4-({ 6-(methyloxy)-7-[(3-morpholin-4-ylpropyl)oxy]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 |
| CN108472242A (zh) | 2013-04-04 | 2018-08-31 | 埃克塞里艾克西斯公司 | 治疗癌症的药物组合 |
| UA123534C2 (uk) | 2014-02-14 | 2021-04-21 | Екселіксис, Інк. | Кристалічні тверді форми n-{4-[(6,7-диметоксихінолін-4-іл)окси]феніл}-n'-(4-флуорофеніл)циклопропан-1,1-дикарбоксаміду, способи отримання і способи застосування |
| JP6666849B2 (ja) | 2014-03-17 | 2020-03-18 | エグゼリクシス， インコーポレイテッド | カボザンチニブ製剤の投与 |
| 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 |
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2014
- 2014-03-17 BR BR112015023109A patent/BR112015023109A2/pt not_active Application Discontinuation
- 2014-03-17 CA CA2907334A patent/CA2907334C/en active Active
- 2014-03-17 JP JP2016503412A patent/JP6389238B2/ja active Active
- 2014-03-17 NZ NZ712330A patent/NZ712330A/en unknown
- 2014-03-17 CN CN201480021215.XA patent/CN105121412B/zh active Active
- 2014-03-17 KR KR1020157027712A patent/KR102276348B1/ko active Active
- 2014-03-17 US US14/776,337 patent/US10273211B2/en active Active
- 2014-03-17 EP EP14721149.4A patent/EP2970126B1/en active Active
- 2014-03-17 UA UAA201510088A patent/UA119321C2/uk unknown
- 2014-03-17 MX MX2015012490A patent/MX366003B/es active IP Right Grant
- 2014-03-17 ES ES14721149T patent/ES2729626T3/es active Active
- 2014-03-17 WO PCT/US2014/030524 patent/WO2014145715A1/en not_active Ceased
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- 2014-03-17 EA EA201591756A patent/EA033786B1/ru not_active IP Right Cessation
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2019
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2024
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| US20190218182A1 (en) | 2019-07-18 |
| ZA201506842B (en) | 2017-08-30 |
| IL241577B (en) | 2019-11-28 |
| EP2970126B1 (en) | 2019-03-06 |
| MX366003B (es) | 2019-06-24 |
| US10273211B2 (en) | 2019-04-30 |
| WO2014145715A1 (en) | 2014-09-18 |
| US20240287002A1 (en) | 2024-08-29 |
| UA119321C2 (uk) | 2019-06-10 |
| HK1220447A1 (en) | 2017-05-05 |
| MX2015012490A (es) | 2016-05-24 |
| EA033786B1 (ru) | 2019-11-26 |
| NZ712330A (en) | 2020-04-24 |
| GEP20196995B (en) | 2019-07-25 |
| ES2729626T3 (es) | 2019-11-05 |
| US20210002228A1 (en) | 2021-01-07 |
| BR112015023109A2 (pt) | 2018-05-15 |
| CN105121412B (zh) | 2019-07-12 |
| EA201591756A1 (ru) | 2016-02-29 |
| AU2014232714B2 (en) | 2018-07-19 |
| KR20150130376A (ko) | 2015-11-23 |
| CN105121412A (zh) | 2015-12-02 |
| AU2014232714A1 (en) | 2015-10-08 |
| JP2016516074A (ja) | 2016-06-02 |
| JP6389238B2 (ja) | 2018-09-12 |
| EP2970126A1 (en) | 2016-01-20 |
| AU2018204666A1 (en) | 2018-07-19 |
| CA2907334A1 (en) | 2014-09-18 |
| US20160031818A1 (en) | 2016-02-04 |
| KR102276348B1 (ko) | 2021-07-12 |
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