KR102611445B1 - N-{4-[(6,7-디메톡시퀴놀린-4-일)옥시]페닐}-n′-(4-플루오로페닐) 시클로프로판-1,1-디카르복스아미드의 염의 결정성 고체 형태, 이들을 만들기 위한 제법, 그리고 이들의 이용 방법 - Google Patents
N-{4-[(6,7-디메톡시퀴놀린-4-일)옥시]페닐}-n′-(4-플루오로페닐) 시클로프로판-1,1-디카르복스아미드의 염의 결정성 고체 형태, 이들을 만들기 위한 제법, 그리고 이들의 이용 방법 Download PDFInfo
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- KR102611445B1 KR102611445B1 KR1020197031409A KR20197031409A KR102611445B1 KR 102611445 B1 KR102611445 B1 KR 102611445B1 KR 1020197031409 A KR1020197031409 A KR 1020197031409A KR 20197031409 A KR20197031409 A KR 20197031409A KR 102611445 B1 KR102611445 B1 KR 102611445B1
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Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/47—Quinolines; Isoquinolines
-
- 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
- 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
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/13—Crystalline forms, e.g. polymorphs
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Quinoline Compounds (AREA)
- Medicinal Preparation (AREA)
- Other In-Based Heterocyclic Compounds (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201762511714P | 2017-05-26 | 2017-05-26 | |
| US62/511,714 | 2017-05-26 | ||
| PCT/US2018/034784 WO2018218233A1 (en) | 2017-05-26 | 2018-05-26 | Crystalline solid forms of salts of n-{4-[(6,7-dimethoxyquinolin-4-yl) oxy]phenyl}-n'-(4-fluorphenyl) cyclopropane-1,1-dicarboxamide, processes for making, and methods of use |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| KR20200010205A KR20200010205A (ko) | 2020-01-30 |
| KR102611445B1 true KR102611445B1 (ko) | 2023-12-06 |
Family
ID=62683441
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| KR1020197031409A Active KR102611445B1 (ko) | 2017-05-26 | 2018-05-26 | N-{4-[(6,7-디메톡시퀴놀린-4-일)옥시]페닐}-n′-(4-플루오로페닐) 시클로프로판-1,1-디카르복스아미드의 염의 결정성 고체 형태, 이들을 만들기 위한 제법, 그리고 이들의 이용 방법 |
Country Status (20)
| Country | Link |
|---|---|
| US (3) | US11279675B2 (https=) |
| EP (1) | EP3630726B1 (https=) |
| JP (3) | JP7166292B2 (https=) |
| KR (1) | KR102611445B1 (https=) |
| CN (1) | CN110621662B (https=) |
| AU (1) | AU2018272088C1 (https=) |
| CA (1) | CA3060370A1 (https=) |
| DK (1) | DK3630726T3 (https=) |
| EA (1) | EA039654B1 (https=) |
| ES (1) | ES2909390T3 (https=) |
| HU (1) | HUE058196T2 (https=) |
| IL (1) | IL270780B2 (https=) |
| MA (1) | MA48776A (https=) |
| MX (1) | MX2019012505A (https=) |
| PL (1) | PL3630726T3 (https=) |
| PT (1) | PT3630726T (https=) |
| SG (1) | SG11201909161PA (https=) |
| UA (1) | UA127760C2 (https=) |
| WO (1) | WO2018218233A1 (https=) |
| ZA (1) | ZA201906127B (https=) |
Families Citing this family (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| MA48776A (fr) * | 2017-05-26 | 2020-04-08 | Exelixis Inc | Formes solides cristallines de sels de n-{4-[(6,7-diméthoxyquinolin-4-yl) oxy]phényl}-n'-(4-fluorphényl) cyclopropane-1,1-dicarboxamide, procédés de préparation et d'utilisation |
| CN117402114A (zh) | 2018-01-26 | 2024-01-16 | 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 |
| TWI831259B (zh) | 2018-06-15 | 2024-02-01 | 漢達生技醫藥股份有限公司 | 包含達沙替尼十二烷基硫酸鹽組合物的膠囊 |
| KR102828472B1 (ko) | 2018-12-13 | 2025-07-03 | 엑셀리시스, 인코포레이티드 | 키나아제 억제제의 결정질 형태 및 염 형태 |
| MX2021014773A (es) * | 2019-06-03 | 2022-01-18 | Exelixis Inc | Formas de sales cristalinas de un inhibidor de cinasas. |
| EP4486725A1 (en) | 2022-03-01 | 2025-01-08 | Synthon B.V. | Cabozantinib salt with l-(+)-tartaric acid and solid forms thereof |
| WO2024163400A1 (en) | 2023-01-31 | 2024-08-08 | Handa Oncology, Llc | Improved cabozantinib compositions and methods of use |
| US11814356B1 (en) | 2023-03-29 | 2023-11-14 | Apotex Inc. | Salt of cabozantinib |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 (23)
| 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 |
| UA108618C2 (uk) | 2009-08-07 | 2015-05-25 | Застосування c-met-модуляторів в комбінації з темозоломідом та/або променевою терапією для лікування раку | |
| US20120070368A1 (en) | 2010-04-16 | 2012-03-22 | Exelixis, Inc. | Methods of Using C-Met Modulators |
| EA030435B1 (ru) | 2010-07-16 | 2018-08-31 | Экселиксис, Инк. | ТАБЛЕТКА, СОДЕРЖАЩАЯ МОДУЛЯТОР c-MET В ФОРМЕ КРИСТАЛЛИЧЕСКОЙ L-МАЛАТНОЙ СОЛИ (ВАРИАНТЫ), СПОСОБ ЕЕ ПРОИЗВОДСТВА И СПОСОБ ЛЕЧЕНИЯ ОНКОЛОГИЧЕСКОГО ЗАБОЛЕВАНИЯ С ЕЕ ИСПОЛЬЗОВАНИЕМ |
| US20140057908A1 (en) | 2010-09-27 | 2014-02-27 | Exelixis, Inc. | Method of Treating Cancer |
| MX352926B (es) | 2010-09-27 | 2017-12-14 | Exelixis Inc | Inhibidores dobles de met y factor de crecimiento endotelial vascular (vegf) para el tratamiento de cancer de prostata resistente a la castracion y metastasis osteoblasticas en los huesos. |
| BR112013020362A2 (pt) | 2011-02-10 | 2018-05-29 | Exelixis Inc | processos para a preparação de compostos de quinolina, compostos e combinações farmacêuticas que os contem |
| US20120252840A1 (en) | 2011-04-04 | 2012-10-04 | Exelixis, Inc. | Method of Treating Cancer |
| MX2013012695A (es) | 2011-05-02 | 2014-03-27 | Exelixis Inc | Metodo para el tratamiento del cancer y el dolor por cancer de hueso. |
| EP2758057B1 (en) | 2011-09-22 | 2017-05-31 | Exelixis, Inc. | Method for treating osteoporosis |
| US9535315B2 (en) | 2011-10-31 | 2017-01-03 | Applied Materials, Inc. | Method of fabricating a color filter array using a multilevel structure |
| IN2014CN04067A (https=) | 2011-11-08 | 2015-10-23 | Exelixis Inc | |
| TW201323864A (zh) | 2011-11-08 | 2013-06-16 | Exelixis Inc | 定量癌症治療之方法 |
| 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 |
| 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 |
| WO2015177758A1 (en) * | 2014-05-23 | 2015-11-26 | Mylan Laboratories Ltd | Novel polymorphs of cabozantinib (s)-malate and cabozantinib free base |
| CN104961680B (zh) | 2014-11-07 | 2017-09-12 | 苏州晶云药物科技有限公司 | N‑(4‑{[6,7‑双(甲基氧基)喹啉‑4‑基]氧基}苯基)‑n’‑(4‑氟苯基)环丙烷‑1,1‑二甲酰胺的盐酸盐及其多晶型 |
| CN104961681B (zh) | 2014-11-13 | 2017-06-13 | 苏州晶云药物科技有限公司 | 卡博替尼的粘酸盐及其晶型 |
| EP3274333B1 (en) * | 2015-03-25 | 2019-04-24 | Sandoz AG | Cabozantinib salts and their use as anti-cancer agents |
| EP3274332B1 (en) | 2015-03-25 | 2018-12-19 | Sandoz AG | Crystalline forms of cabozantinib phosphate and cabozantinib hydrochloride |
| US10980792B2 (en) * | 2016-09-12 | 2021-04-20 | Zhuhai Beihai Biotech Co., Ltd. | Formulations of Cabozantinib |
| WO2018104954A1 (en) * | 2016-12-07 | 2018-06-14 | Msn Laboratories Private Limited, R&D Center | Process for the preparation of n-(4-(6,7-dimethoxyquinolin-4-yloxy) phenyl)-n'-(4-fluorophenyl)cyclopropane-1, 1-dicarboxamide, (2s)-hydroxybutanedioate and its polymorphs thereof |
| MA48776A (fr) * | 2017-05-26 | 2020-04-08 | Exelixis Inc | Formes solides cristallines de sels de n-{4-[(6,7-diméthoxyquinolin-4-yl) oxy]phényl}-n'-(4-fluorphényl) cyclopropane-1,1-dicarboxamide, procédés de préparation et d'utilisation |
-
2018
- 2018-05-26 MA MA048776A patent/MA48776A/fr unknown
- 2018-05-26 PT PT187325485T patent/PT3630726T/pt unknown
- 2018-05-26 KR KR1020197031409A patent/KR102611445B1/ko active Active
- 2018-05-26 CN CN201880027861.5A patent/CN110621662B/zh active Active
- 2018-05-26 PL PL18732548T patent/PL3630726T3/pl unknown
- 2018-05-26 SG SG11201909161P patent/SG11201909161PA/en unknown
- 2018-05-26 AU AU2018272088A patent/AU2018272088C1/en active Active
- 2018-05-26 DK DK18732548.5T patent/DK3630726T3/da active
- 2018-05-26 EA EA201992803A patent/EA039654B1/ru unknown
- 2018-05-26 US US16/617,352 patent/US11279675B2/en active Active
- 2018-05-26 IL IL270780A patent/IL270780B2/en unknown
- 2018-05-26 WO PCT/US2018/034784 patent/WO2018218233A1/en not_active Ceased
- 2018-05-26 JP JP2019562380A patent/JP7166292B2/ja active Active
- 2018-05-26 CA CA3060370A patent/CA3060370A1/en active Pending
- 2018-05-26 MX MX2019012505A patent/MX2019012505A/es unknown
- 2018-05-26 HU HUE18732548A patent/HUE058196T2/hu unknown
- 2018-05-26 UA UAA201912198A patent/UA127760C2/uk unknown
- 2018-05-26 ES ES18732548T patent/ES2909390T3/es active Active
- 2018-05-26 EP EP18732548.5A patent/EP3630726B1/en active Active
-
2019
- 2019-09-17 ZA ZA2019/06127A patent/ZA201906127B/en unknown
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2022
- 2022-02-09 US US17/668,098 patent/US11731941B2/en active Active
- 2022-08-09 JP JP2022127094A patent/JP7437460B2/ja active Active
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2023
- 2023-06-29 US US18/344,267 patent/US12227481B2/en active Active
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2024
- 2024-02-09 JP JP2024018527A patent/JP7659097B2/ja active Active
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
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Legal Events
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| PA0105 | International application |
Patent event date: 20191024 Patent event code: PA01051R01D Comment text: International Patent Application |
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Patent event code: PA02012R01D Patent event date: 20210525 Comment text: Request for Examination of Application |
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Comment text: Notification of reason for refusal Patent event date: 20230412 Patent event code: PE09021S01D |
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Patent event code: PE07011S01D Comment text: Decision to Grant Registration Patent event date: 20230921 |
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| PR0701 | Registration of establishment |
Comment text: Registration of Establishment Patent event date: 20231204 Patent event code: PR07011E01D |
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| PR1002 | Payment of registration fee |
Payment date: 20231204 End annual number: 3 Start annual number: 1 |
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