JP7166292B2 - N-{4-[(6,7-ジメトキシキノリン-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塩の結晶性固体形態、製造プロセス、及び使用方法 - Google Patents
N-{4-[(6,7-ジメトキシキノリン-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塩の結晶性固体形態、製造プロセス、及び使用方法 Download PDFInfo
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- JP7166292B2 JP7166292B2 JP2019562380A JP2019562380A JP7166292B2 JP 7166292 B2 JP7166292 B2 JP 7166292B2 JP 2019562380 A JP2019562380 A JP 2019562380A JP 2019562380 A JP2019562380 A JP 2019562380A JP 7166292 B2 JP7166292 B2 JP 7166292B2
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- 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
-
- 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
- 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
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- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Quinoline Compounds (AREA)
- Medicinal Preparation (AREA)
- Other In-Based Heterocyclic Compounds (AREA)
Priority Applications (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2022127094A JP7437460B2 (ja) | 2017-05-26 | 2022-08-09 | N-{4-[(6,7-ジメトキシキノリン-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塩の結晶性固体形態、製造プロセス、及び使用方法 |
| JP2024018527A JP7659097B2 (ja) | 2017-05-26 | 2024-02-09 | N-{4-[(6,7-ジメトキシキノリン-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塩の結晶性固体形態、製造プロセス、及び使用方法 |
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 |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2022127094A Division JP7437460B2 (ja) | 2017-05-26 | 2022-08-09 | N-{4-[(6,7-ジメトキシキノリン-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塩の結晶性固体形態、製造プロセス、及び使用方法 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2020521732A JP2020521732A (ja) | 2020-07-27 |
| JP2020521732A5 JP2020521732A5 (https=) | 2021-07-26 |
| JP7166292B2 true JP7166292B2 (ja) | 2022-11-07 |
Family
ID=62683441
Family Applications (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019562380A Active JP7166292B2 (ja) | 2017-05-26 | 2018-05-26 | N-{4-[(6,7-ジメトキシキノリン-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塩の結晶性固体形態、製造プロセス、及び使用方法 |
| JP2022127094A Active JP7437460B2 (ja) | 2017-05-26 | 2022-08-09 | N-{4-[(6,7-ジメトキシキノリン-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塩の結晶性固体形態、製造プロセス、及び使用方法 |
| JP2024018527A Active JP7659097B2 (ja) | 2017-05-26 | 2024-02-09 | N-{4-[(6,7-ジメトキシキノリン-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塩の結晶性固体形態、製造プロセス、及び使用方法 |
Family Applications After (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2022127094A Active JP7437460B2 (ja) | 2017-05-26 | 2022-08-09 | N-{4-[(6,7-ジメトキシキノリン-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塩の結晶性固体形態、製造プロセス、及び使用方法 |
| JP2024018527A Active JP7659097B2 (ja) | 2017-05-26 | 2024-02-09 | N-{4-[(6,7-ジメトキシキノリン-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塩の結晶性固体形態、製造プロセス、及び使用方法 |
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=) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2022145852A (ja) * | 2017-05-26 | 2022-10-04 | エグゼリクシス, インコーポレイテッド | N-{4-[(6,7-ジメトキシキノリン-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塩の結晶性固体形態、製造プロセス、及び使用方法 |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR102354963B1 (ko) * | 2014-02-14 | 2022-01-21 | 엑셀리시스, 인코포레이티드 | N-{4-[(6,7-다이메톡시퀴놀린-4-일)옥시]페닐}-n'-(4-플루오로페닐) 사이클로프로판-1,1-다이카복스아마이드의 결정질 고체 형태, 제조 방법 및 사용 방법 |
| UA128476C2 (uk) | 2018-01-26 | 2024-07-24 | Екселіксіс, Інк. | Сполуки для лікування кіназозалежних розладів |
| 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 |
| PL3894012T4 (pl) * | 2018-12-13 | 2026-01-05 | Exelixis, Inc. | Postacie krystaliczne i postacie soli inhibitora kinazy |
| CA3139148A1 (en) * | 2019-06-03 | 2020-12-10 | Exelixis, Inc. | Crystalline salt forms of a kinase inhibitor |
| CN118974017A (zh) | 2022-03-01 | 2024-11-15 | 斯索恩有限公司 | 卡博替尼的l-(+)-酒石酸盐及其固体形式 |
| TW202444365A (zh) | 2023-01-31 | 2024-11-16 | 漢達生技醫藥股份有限公司 | 改良之卡博替尼組合物及其使用方法 |
| US11814356B1 (en) | 2023-03-29 | 2023-11-14 | Apotex Inc. | Salt of cabozantinib |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2012515220A (ja) | 2009-01-16 | 2012-07-05 | エクセリクシス, インク. | N−(4−{[6,7−ビス(メチルオキシ)キノリン−4−イル]オキシ}フェニル)−n’−(4−フルオロフェニル)シクロプロパン−1,1−ジカルボキサミドのリンゴ酸塩およびその結晶質形態 |
| WO2016150963A1 (en) | 2015-03-25 | 2016-09-29 | Sandoz Ag | Cabozantinib salts and their use as anti-cancer agents |
Family Cites Families (22)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PT2213661E (pt) | 2003-09-26 | 2011-12-15 | Exelixis Inc | Moduladores de c-met e métodos de uso |
| 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 |
| EP2593090B1 (en) | 2010-07-16 | 2021-10-13 | Exelixis, Inc. | C-met modulator pharmaceutical compositions |
| EP2621483A1 (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 |
| 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 |
| JP2014505109A (ja) | 2011-02-10 | 2014-02-27 | エクセリクシス, インク. | 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 |
| US20120252840A1 (en) | 2011-04-04 | 2012-10-04 | Exelixis, Inc. | Method of Treating Cancer |
| KR20140025496A (ko) | 2011-05-02 | 2014-03-04 | 엑셀리시스, 인코포레이티드 | 암 및 뼈 암 통증의 치료방법 |
| GEP201606523B (en) | 2011-09-22 | 2016-08-10 | 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 |
| JP2014532766A (ja) | 2011-11-08 | 2014-12-08 | エクセリクシス, インク. | 癌を治療する、met及びvegfの二重阻害剤 |
| EP2775921A1 (en) | 2011-11-08 | 2014-09-17 | Exelixis, Inc. | Method of quantifying cancer treatment |
| 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 |
| KR102354963B1 (ko) * | 2014-02-14 | 2022-01-21 | 엑셀리시스, 인코포레이티드 | N-{4-[(6,7-다이메톡시퀴놀린-4-일)옥시]페닐}-n'-(4-플루오로페닐) 사이클로프로판-1,1-다이카복스아마이드의 결정질 고체 형태, 제조 방법 및 사용 방법 |
| EP3145913A1 (en) * | 2014-05-23 | 2017-03-29 | 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 |
| 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 |
| US11261160B2 (en) * | 2016-12-07 | 2022-03-01 | 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 |
| AU2018272088C1 (en) | 2017-05-26 | 2022-09-22 | Exelixis, Inc. | 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 |
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2018
- 2018-05-26 AU AU2018272088A patent/AU2018272088C1/en active Active
- 2018-05-26 KR KR1020197031409A patent/KR102611445B1/ko active Active
- 2018-05-26 UA UAA201912198A patent/UA127760C2/uk unknown
- 2018-05-26 MX MX2019012505A patent/MX2019012505A/es unknown
- 2018-05-26 CA CA3060370A patent/CA3060370A1/en active Pending
- 2018-05-26 EA EA201992803A patent/EA039654B1/ru unknown
- 2018-05-26 PT PT187325485T patent/PT3630726T/pt unknown
- 2018-05-26 PL PL18732548T patent/PL3630726T3/pl unknown
- 2018-05-26 ES ES18732548T patent/ES2909390T3/es active Active
- 2018-05-26 EP EP18732548.5A patent/EP3630726B1/en active Active
- 2018-05-26 IL IL270780A patent/IL270780B2/en unknown
- 2018-05-26 HU HUE18732548A patent/HUE058196T2/hu unknown
- 2018-05-26 US US16/617,352 patent/US11279675B2/en active Active
- 2018-05-26 MA MA048776A patent/MA48776A/fr unknown
- 2018-05-26 DK DK18732548.5T patent/DK3630726T3/da active
- 2018-05-26 SG SG11201909161P patent/SG11201909161PA/en unknown
- 2018-05-26 CN CN201880027861.5A patent/CN110621662B/zh active Active
- 2018-05-26 WO PCT/US2018/034784 patent/WO2018218233A1/en not_active Ceased
- 2018-05-26 JP JP2019562380A patent/JP7166292B2/ja active Active
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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 (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2012515220A (ja) | 2009-01-16 | 2012-07-05 | エクセリクシス, インク. | N−(4−{[6,7−ビス(メチルオキシ)キノリン−4−イル]オキシ}フェニル)−n’−(4−フルオロフェニル)シクロプロパン−1,1−ジカルボキサミドのリンゴ酸塩およびその結晶質形態 |
| WO2016150963A1 (en) | 2015-03-25 | 2016-09-29 | Sandoz Ag | Cabozantinib salts and their use as anti-cancer agents |
Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2022145852A (ja) * | 2017-05-26 | 2022-10-04 | エグゼリクシス, インコーポレイテッド | N-{4-[(6,7-ジメトキシキノリン-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塩の結晶性固体形態、製造プロセス、及び使用方法 |
| JP7437460B2 (ja) | 2017-05-26 | 2024-02-22 | エグゼリクシス, インコーポレイテッド | N-{4-[(6,7-ジメトキシキノリン-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塩の結晶性固体形態、製造プロセス、及び使用方法 |
| JP2024036690A (ja) * | 2017-05-26 | 2024-03-15 | エグゼリクシス, インコーポレイテッド | N-{4-[(6,7-ジメトキシキノリン-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塩の結晶性固体形態、製造プロセス、及び使用方法 |
| JP7659097B2 (ja) | 2017-05-26 | 2025-04-08 | エグゼリクシス, インコーポレイテッド | N-{4-[(6,7-ジメトキシキノリン-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塩の結晶性固体形態、製造プロセス、及び使用方法 |
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