GEP20196995B - 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-dicarboxamideInfo
- Publication number
- GEP20196995B GEP20196995B GEAP201413960A GEAP2014013960A GEP20196995B GE P20196995 B GEP20196995 B GE P20196995B GE AP201413960 A GEAP201413960 A GE AP201413960A GE AP2014013960 A GEAP2014013960 A GE AP2014013960A GE P20196995 B GEP20196995 B GE P20196995B
- Authority
- GE
- Georgia
- Prior art keywords
- metabolites
- dicarboxamide
- methyloxy
- quinolin
- cyclopropane
- Prior art date
Links
- 239000002207 metabolite Substances 0.000 title abstract 2
- ONIQOQHATWINJY-UHFFFAOYSA-N cabozantinib Chemical class C=12C=C(OC)C(OC)=CC2=NC=CC=1OC(C=C1)=CC=C1NC(=O)C1(C(=O)NC=2C=CC(F)=CC=2)CC1 ONIQOQHATWINJY-UHFFFAOYSA-N 0.000 title 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 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)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Epidemiology (AREA)
- Saccharide Compounds (AREA)
- Quinoline Compounds (AREA)
- Pain & Pain Management (AREA)
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201361792413P | 2013-03-15 | 2013-03-15 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| GEP20196995B true GEP20196995B (en) | 2019-07-25 |
Family
ID=50631091
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| GEAP201413960A GEP20196995B (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 (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 |
|---|---|---|---|---|
| FI2621481T4 (fi) | 2010-09-27 | 2023-01-13 | Met- ja vegf-kaksoisestäjiä kastraatioresistentin eturauhassyövän ja osteoblastisten luun etäispesäkkeiden hoitamiseen | |
| EA033513B1 (ru) | 2011-02-10 | 2019-10-31 | Exelixis Inc | Способы получения хинолиновых соединений и фармацевтических композиций, содержащих такие соединения |
| EP2844254A1 (en) | 2012-05-02 | 2015-03-11 | Exelixis, Inc. | A dual met - vegf modulator for treating osteolytic bone metastases |
| JP6389238B2 (ja) | 2013-03-15 | 2018-09-12 | エグゼリクシス， インコーポレイテッド | Ｎ−（４−｛［６，７−ビス（メンチルオキシ）キノリン−４−イル］オキシ｝フェニル）−ｎ’−（４−フルオロフェニル）サイクロプロペイン−１，１−ジカルボキシアミドのメタボライト |
| US11564915B2 (en) | 2013-04-04 | 2023-01-31 | Exelixis, Inc. | Cabozantinib dosage form and use in the treatment of cancer |
| 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. |
| WO2015142928A1 (en) * | 2014-03-17 | 2015-09-24 | Exelixis, Inc. | Dosing of cabozantinib formulations |
| EP3174854B1 (en) * | 2014-07-31 | 2022-08-24 | Exelixis, Inc. | Method of preparing fluorine-18 labeled cabozantinib and its analogs |
| MA40457A (fr) | 2014-08-05 | 2017-06-14 | Exelixis Inc | Combinaison de médicaments pour traiter le myélome multiple |
| CA3020749A1 (en) | 2016-04-15 | 2017-10-19 | Exelixis, Inc. | Method of treating renal cell carcinoma using n-(4-(6,7-dimethoxyquinolin-4-yloxy) phenyl)-n'-(4-fluoropheny)cyclopropane-1,1-dicarboxamide, (2s)-hydroxybutanedioate |
| 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 |
| SG11202006921PA (en) | 2018-01-26 | 2020-08-28 | Exelixis Inc | Compounds for the treatment of kinase-dependent disorders |
| 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 |
| CN120417903A (zh) | 2023-01-31 | 2025-08-01 | 汉达癌症医药责任有限公司 | 改良的卡博替尼组合物及其使用方法 |
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| CA2744997A1 (en) | 2003-09-26 | 2005-04-07 | Exelixis, Inc. | C-met modulators and method of use |
| CA2572331A1 (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 |
| UY30183A1 (es) | 2006-03-02 | 2007-10-31 | Astrazeneca Ab | Derivados de quinolina |
| 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 |
| TW201035017A (en) | 2008-09-26 | 2010-10-01 | Smithkline Beecham Corp | Preparation of a quinolinyloxydiphenylcyclopropanedicarboxamide |
| 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 |
| US20130030172A1 (en) | 2008-12-04 | 2013-01-31 | Exelixis, Inc. | Methods of Preparing Quinoline Derivatives |
| DK2387563T4 (da) | 2009-01-16 | 2022-07-18 | Exelixis Inc | Malatsalt af n-(4-{ [ 6, 7-bis(methyloxy)quinolin-4-yl]oxy}phenyl-n'-(4-fluorphenyl)cyclopropan-1,1-dicarboxamid, og krystallinske former deraf til behandling af cancer |
| KR20120051702A (ko) | 2009-07-17 | 2012-05-22 | 엑셀리시스, 인코포레이티드 | Ｎ-〔３-플루오로-４-(｛６-(메틸옥시)-７-〔(３-모르폴린-４-일프로필)옥시〕퀴놀린-４-일｝옥시)페닐〕-ｎ''-(４-플루오로페닐)시클로프로판-１,１-디카르복사미드의 결정형 |
| UA108618C2 (uk) | 2009-08-07 | 2015-05-25 | Застосування c-met-модуляторів в комбінації з темозоломідом та/або променевою терапією для лікування раку | |
| CN102933551A (zh) | 2010-03-12 | 2013-02-13 | 埃克塞里艾克西斯公司 | N-[3-氟-4-({6-(甲氧基)-7-[(3-吗啉-4-基丙基)氧基]-喹啉-4-基}氧基)苯基]-n’-(4-氟苯基)环丙烷-1,1-二甲酰胺的水合结晶形式 |
| US20120070368A1 (en) | 2010-04-16 | 2012-03-22 | Exelixis, Inc. | Methods of Using C-Met Modulators |
| EP2593090B1 (en) | 2010-07-16 | 2021-10-13 | Exelixis, Inc. | C-met modulator pharmaceutical compositions |
| EP2593091A1 (en) | 2010-07-16 | 2013-05-22 | Exelixis, Inc. | C-met modulator pharmaceutical compositions |
| JP2013540759A (ja) | 2010-09-27 | 2013-11-07 | 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 |
| JP2013537918A (ja) | 2010-09-27 | 2013-10-07 | エクセリクシス， インク． | 去勢抵抗性前立腺癌および骨芽細胞骨転移の治療のためのｍｅｔおよびｖｅｇｆの二元阻害薬 |
| FI2621481T4 (fi) | 2010-09-27 | 2023-01-13 | Met- ja vegf-kaksoisestäjiä kastraatioresistentin eturauhassyövän ja osteoblastisten luun etäispesäkkeiden hoitamiseen | |
| CN103327979A (zh) | 2010-11-22 | 2013-09-25 | 葛兰素史密斯克莱知识产权（第2号）有限公司 | 治疗癌症的方法 |
| SG10201510086VA (en) | 2010-12-23 | 2016-01-28 | Nestec Sa | 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 |
| EA033513B1 (ru) | 2011-02-10 | 2019-10-31 | Exelixis Inc | Способы получения хинолиновых соединений и фармацевтических композиций, содержащих такие соединения |
| US20120252840A1 (en) | 2011-04-04 | 2012-10-04 | Exelixis, Inc. | Method of Treating Cancer |
| BR212013028314U2 (pt) | 2011-05-02 | 2015-11-03 | Exelixis Inc | método para tratar câncer e dor de câncer de osso |
| 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 |
| EP2758057B1 (en) | 2011-09-22 | 2017-05-31 | Exelixis, Inc. | Method for treating osteoporosis |
| PT2768796T (pt) | 2011-10-20 | 2020-02-21 | Exelixis Inc | Processo para a preparação de derivados de quinolina |
| IN2014CN04067A (OSRAM) | 2011-11-08 | 2015-10-23 | Exelixis Inc | |
| EP2844254A1 (en) | 2012-05-02 | 2015-03-11 | Exelixis, Inc. | A dual met - vegf modulator for treating osteolytic bone metastases |
| US20150238477A1 (en) | 2012-09-07 | 2015-08-27 | Exelixis, Inc. | Method of Treating Lung Adenocarcinoma |
| 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 |
| JP6389238B2 (ja) | 2013-03-15 | 2018-09-12 | エグゼリクシス， インコーポレイテッド | Ｎ−（４−｛［６，７−ビス（メンチルオキシ）キノリン−４−イル］オキシ｝フェニル）−ｎ’−（４−フルオロフェニル）サイクロプロペイン−１，１−ジカルボキシアミドのメタボライト |
| 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 |
| 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. |
| WO2015142928A1 (en) | 2014-03-17 | 2015-09-24 | Exelixis, Inc. | Dosing of cabozantinib formulations |
| EP3174854B1 (en) | 2014-07-31 | 2022-08-24 | Exelixis, Inc. | Method of preparing fluorine-18 labeled cabozantinib and its analogs |
-
2014
- 2014-03-17 JP JP2016503412A patent/JP6389238B2/ja active Active
- 2014-03-17 CN CN201480021215.XA patent/CN105121412B/zh active Active
- 2014-03-17 MX MX2015012490A patent/MX366003B/es active IP Right Grant
- 2014-03-17 AU AU2014232714A patent/AU2014232714B2/en active Active
- 2014-03-17 US US14/776,337 patent/US10273211B2/en active Active
- 2014-03-17 NZ NZ712330A patent/NZ712330A/en unknown
- 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 EA EA201591756A patent/EA033786B1/ru not_active IP Right Cessation
- 2014-03-17 ES ES14721149T patent/ES2729626T3/es active Active
- 2014-03-17 KR KR1020157027712A patent/KR102276348B1/ko active Active
- 2014-03-17 GE GEAP201413960A patent/GEP20196995B/en unknown
- 2014-03-17 UA UAA201510088A patent/UA119321C2/uk unknown
- 2014-03-17 CA CA2907334A patent/CA2907334C/en active Active
- 2014-03-17 BR BR112015023109A patent/BR112015023109A2/pt not_active Application Discontinuation
-
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 |
|---|---|
| AU2014232714B2 (en) | 2018-07-19 |
| EA201591756A1 (ru) | 2016-02-29 |
| CA2907334C (en) | 2021-12-07 |
| US20160031818A1 (en) | 2016-02-04 |
| UA119321C2 (uk) | 2019-06-10 |
| ES2729626T3 (es) | 2019-11-05 |
| KR102276348B1 (ko) | 2021-07-12 |
| AU2018204666A1 (en) | 2018-07-19 |
| US20190218182A1 (en) | 2019-07-18 |
| CA2907334A1 (en) | 2014-09-18 |
| CN105121412B (zh) | 2019-07-12 |
| CN105121412A (zh) | 2015-12-02 |
| US20210002228A1 (en) | 2021-01-07 |
| MX366003B (es) | 2019-06-24 |
| JP6389238B2 (ja) | 2018-09-12 |
| MX2015012490A (es) | 2016-05-24 |
| EP2970126B1 (en) | 2019-03-06 |
| WO2014145715A1 (en) | 2014-09-18 |
| NZ712330A (en) | 2020-04-24 |
| ZA201506842B (en) | 2017-08-30 |
| JP2016516074A (ja) | 2016-06-02 |
| EA033786B1 (ru) | 2019-11-26 |
| BR112015023109A2 (pt) | 2018-05-15 |
| EP2970126A1 (en) | 2016-01-20 |
| AU2014232714A1 (en) | 2015-10-08 |
| HK1220447A1 (en) | 2017-05-05 |
| IL241577B (en) | 2019-11-28 |
| KR20150130376A (ko) | 2015-11-23 |
| US10273211B2 (en) | 2019-04-30 |
| US20240287002A1 (en) | 2024-08-29 |
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