ZA201506842B - Metabolites of n-(4-{[6,7-bis(methyloxy)quinolin-4-yl]oxy}phenyl)-n'-(4-flourophenyl)cyclopropane-1,1-dicarboxamide - Google Patents
Metabolites of n-(4-{[6,7-bis(methyloxy)quinolin-4-yl]oxy}phenyl)-n'-(4-flourophenyl)cyclopropane-1,1-dicarboxamideInfo
- Publication number
- ZA201506842B ZA201506842B ZA2015/06842A ZA201506842A ZA201506842B ZA 201506842 B ZA201506842 B ZA 201506842B ZA 2015/06842 A ZA2015/06842 A ZA 2015/06842A ZA 201506842 A ZA201506842 A ZA 201506842A ZA 201506842 B ZA201506842 B ZA 201506842B
- Authority
- ZA
- South Africa
- Prior art keywords
- flourophenyl
- dicarboxamide
- methyloxy
- quinolin
- cyclopropane
- Prior art date
Links
- FEHLGOYZDFFMND-UHFFFAOYSA-N cyclopropane-1,1-dicarboxamide Chemical compound NC(=O)C1(C(N)=O)CC1 FEHLGOYZDFFMND-UHFFFAOYSA-N 0.000 title 1
- 239000002207 metabolite Substances 0.000 title 1
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)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (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)
- Pain & Pain Management (AREA)
- Quinoline Compounds (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201361792413P | 2013-03-15 | 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 (1)
| Publication Number | Publication Date |
|---|---|
| ZA201506842B true ZA201506842B (en) | 2017-08-30 |
Family
ID=50631091
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ZA2015/06842A ZA201506842B (en) | 2013-03-15 | 2015-09-15 | Metabolites of n-(4-{[6,7-bis(methyloxy)quinolin-4-yl]oxy}phenyl)-n'-(4-flourophenyl)cyclopropane-1,1-dicarboxamide |
Country Status (17)
| Country | Link |
|---|---|
| US (4) | US10273211B2 (OSRAM) |
| EP (1) | EP2970126B1 (OSRAM) |
| JP (1) | JP6389238B2 (OSRAM) |
| KR (1) | KR102276348B1 (OSRAM) |
| CN (1) | CN105121412B (OSRAM) |
| AU (2) | AU2014232714B2 (OSRAM) |
| BR (1) | BR112015023109A2 (OSRAM) |
| CA (1) | CA2907334C (OSRAM) |
| EA (1) | EA033786B1 (OSRAM) |
| ES (1) | ES2729626T3 (OSRAM) |
| GE (1) | GEP20196995B (OSRAM) |
| IL (1) | IL241577B (OSRAM) |
| MX (1) | MX366003B (OSRAM) |
| NZ (1) | NZ712330A (OSRAM) |
| UA (1) | UA119321C2 (OSRAM) |
| WO (1) | WO2014145715A1 (OSRAM) |
| ZA (1) | ZA201506842B (OSRAM) |
Families Citing this family (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| GEP20247677B (en) | 2011-02-10 | 2024-10-10 | Exelixis Inc | Processes for preparing quinoline compounds and pharmaceutical compositions containing such compounds |
| JP2015515988A (ja) | 2012-05-02 | 2015-06-04 | エクセリクシス， インク． | 溶骨性骨転移を治療するためのｍｅｔ−ｖｅｇｆ二重調節剤 |
| KR102276348B1 (ko) | 2013-03-15 | 2021-07-12 | 엑셀리시스, 인코포레이티드 | Ｎ（４〔［６,７비스（메틸옥시）퀴놀린４일］옥시〕페닐）ｎ′（４플루오로페닐）시클로프로판１,１디카복사미드의 대사물 |
| US11564915B2 (en) | 2013-04-04 | 2023-01-31 | Exelixis, Inc. | Cabozantinib dosage form and use in the treatment of cancer |
| 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 |
| EA201691850A1 (ru) * | 2014-03-17 | 2016-12-30 | Экселиксис, Инк. | Дозирование составов, содержащих кабозантиниб |
| MA40386A (fr) * | 2014-07-31 | 2016-02-04 | Exelixis Inc | Procédé de préparation de cabozantinib marqué au fluor-18 et d'analogues de celui-ci |
| EA034992B1 (ru) | 2014-08-05 | 2020-04-15 | Экселиксис, Инк. | Комбинации лекарственных средств для лечения множественной миеломы |
| 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 |
| 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 |
| CN117624045A (zh) | 2018-01-26 | 2024-03-01 | 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 |
| CN113292537B (zh) | 2018-06-15 | 2024-04-05 | 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 |
| AU2024215796A1 (en) | 2023-01-31 | 2025-05-15 | Handa Oncology, Llc | Improved cabozantinib compositions and methods of use |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2744997A1 (en) | 2003-09-26 | 2005-04-07 | Exelixis, Inc. | C-met modulators and method of use |
| AU2005270068B2 (en) | 2004-07-02 | 2012-04-19 | Exelixis, Inc. | C-Met modulators and method of use |
| AU2006231646A1 (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 |
| AU2007334402B2 (en) | 2006-12-14 | 2014-02-13 | 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 |
| UY32142A (es) | 2008-09-26 | 2010-05-31 | Smithkline Beckman Corp | Preparación de una quinoliniloxidifenilciclopropanodicarboxamida |
| JP5486606B2 (ja) | 2008-11-13 | 2014-05-07 | エクセリクシス， インク． | キノリン誘導体の調製方法 |
| 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 |
| KR101733773B1 (ko) | 2009-01-16 | 2017-05-10 | 엑셀리시스, 인코포레이티드 | Ｎ-（４-｛〔６，７-비스（메틸옥시）퀴놀린-4-일〕옥시｝페닐）-ｎ＇-（４-플루오로페닐）사이클로프로판-1,1-디카르복사미드의 말산염 및 그 결정형 |
| AU2010274012A1 (en) | 2009-07-17 | 2012-02-09 | 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 | |
| SG184040A1 (en) | 2010-03-12 | 2012-10-30 | Exelixis Inc | Hydrated 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 |
| 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 |
| SG10201609324UA (en) | 2010-07-16 | 2017-01-27 | Exelixis Inc | C-met modulator pharmaceutical compositions |
| US20140057908A1 (en) | 2010-09-27 | 2014-02-27 | Exelixis, Inc. | Method of Treating Cancer |
| AU2011307306A1 (en) | 2010-09-27 | 2013-05-02 | Exelixis, Inc. | Dual inhibitors of MET and VEGF for the treatment of castration resistant prostate cancer and osteoblastic bone metastases |
| 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 |
| JP2013543011A (ja) | 2010-11-22 | 2013-11-28 | グラクソスミスクライン、インテレクチュアル、プロパティー、ナンバー２、リミテッド | 癌の治療法 |
| WO2012088337A1 (en) * | 2010-12-23 | 2012-06-28 | Prometheus Laboratories Inc. | Drug selection for malignant cancer therapy using antibody-based arrays |
| 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 |
| GEP20247677B (en) | 2011-02-10 | 2024-10-10 | Exelixis Inc | Processes for preparing quinoline compounds and pharmaceutical compositions containing such compounds |
| US20120252840A1 (en) | 2011-04-04 | 2012-10-04 | Exelixis, Inc. | Method of Treating Cancer |
| JP2014513129A (ja) | 2011-05-02 | 2014-05-29 | エクセリクシス， インク． | 癌および骨癌疼痛の治療方法 |
| 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 |
| AU2012312364B2 (en) | 2011-09-22 | 2017-11-09 | 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 |
| BR112014011009A2 (pt) | 2011-11-08 | 2017-06-06 | Exelixis Inc | inibidor duplo de met e vegf para tratar câncer |
| JP2015515988A (ja) | 2012-05-02 | 2015-06-04 | エクセリクシス， インク． | 溶骨性骨転移を治療するためのｍｅｔ−ｖｅｇｆ二重調節剤 |
| 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 |
| 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 |
| 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 |
| KR102276348B1 (ko) | 2013-03-15 | 2021-07-12 | 엑셀리시스, 인코포레이티드 | Ｎ（４〔［６,７비스（메틸옥시）퀴놀린４일］옥시〕페닐）ｎ′（４플루오로페닐）시클로프로판１,１디카복사미드의 대사물 |
| BR112015025408A8 (pt) | 2013-04-04 | 2018-07-10 | Exelixis Inc | combinações de drogas para tratar câncer |
| US11564915B2 (en) | 2013-04-04 | 2023-01-31 | Exelixis, Inc. | Cabozantinib dosage form and use in the treatment of cancer |
| 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 |
| EA201691850A1 (ru) * | 2014-03-17 | 2016-12-30 | Экселиксис, Инк. | Дозирование составов, содержащих кабозантиниб |
| MA40386A (fr) * | 2014-07-31 | 2016-02-04 | Exelixis Inc | Procédé de préparation de cabozantinib marqué au fluor-18 et d'analogues de celui-ci |
-
2014
- 2014-03-17 KR KR1020157027712A patent/KR102276348B1/ko active Active
- 2014-03-17 MX MX2015012490A patent/MX366003B/es active IP Right Grant
- 2014-03-17 EA EA201591756A patent/EA033786B1/ru not_active IP Right Cessation
- 2014-03-17 BR BR112015023109A patent/BR112015023109A2/pt not_active Application Discontinuation
- 2014-03-17 WO PCT/US2014/030524 patent/WO2014145715A1/en not_active Ceased
- 2014-03-17 EP EP14721149.4A patent/EP2970126B1/en active Active
- 2014-03-17 US US14/776,337 patent/US10273211B2/en active Active
- 2014-03-17 ES ES14721149T patent/ES2729626T3/es active Active
- 2014-03-17 JP JP2016503412A patent/JP6389238B2/ja active Active
- 2014-03-17 UA UAA201510088A patent/UA119321C2/uk unknown
- 2014-03-17 NZ NZ712330A patent/NZ712330A/en unknown
- 2014-03-17 CN CN201480021215.XA patent/CN105121412B/zh active Active
- 2014-03-17 AU AU2014232714A patent/AU2014232714B2/en active Active
- 2014-03-17 GE GEAP201413960A patent/GEP20196995B/en unknown
- 2014-03-17 CA CA2907334A patent/CA2907334C/en active Active
-
2015
- 2015-09-10 IL IL24157715A patent/IL241577B/en active IP Right Grant
- 2015-09-15 ZA ZA2015/06842A patent/ZA201506842B/en unknown
-
2018
- 2018-06-27 AU AU2018204666A patent/AU2018204666A1/en not_active Abandoned
-
2019
- 2019-03-25 US US16/362,863 patent/US20190218182A1/en not_active Abandoned
-
2020
- 2020-09-24 US US17/031,196 patent/US20210002228A1/en not_active Abandoned
-
2024
- 2024-04-22 US US18/641,587 patent/US20240287002A1/en not_active Abandoned
Also Published As
| Publication number | Publication date |
|---|---|
| HK1220447A1 (en) | 2017-05-05 |
| IL241577B (en) | 2019-11-28 |
| CN105121412A (zh) | 2015-12-02 |
| NZ712330A (en) | 2020-04-24 |
| AU2014232714B2 (en) | 2018-07-19 |
| GEP20196995B (en) | 2019-07-25 |
| EP2970126A1 (en) | 2016-01-20 |
| WO2014145715A1 (en) | 2014-09-18 |
| UA119321C2 (uk) | 2019-06-10 |
| US20190218182A1 (en) | 2019-07-18 |
| JP2016516074A (ja) | 2016-06-02 |
| AU2018204666A1 (en) | 2018-07-19 |
| KR20150130376A (ko) | 2015-11-23 |
| ES2729626T3 (es) | 2019-11-05 |
| JP6389238B2 (ja) | 2018-09-12 |
| CA2907334A1 (en) | 2014-09-18 |
| EA033786B1 (ru) | 2019-11-26 |
| EA201591756A1 (ru) | 2016-02-29 |
| US20160031818A1 (en) | 2016-02-04 |
| US20240287002A1 (en) | 2024-08-29 |
| MX366003B (es) | 2019-06-24 |
| US20210002228A1 (en) | 2021-01-07 |
| CN105121412B (zh) | 2019-07-12 |
| MX2015012490A (es) | 2016-05-24 |
| AU2014232714A1 (en) | 2015-10-08 |
| BR112015023109A2 (pt) | 2018-05-15 |
| KR102276348B1 (ko) | 2021-07-12 |
| US10273211B2 (en) | 2019-04-30 |
| EP2970126B1 (en) | 2019-03-06 |
| CA2907334C (en) | 2021-12-07 |
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