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 (enExample) | 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 (enExample) |
| EP (1) | EP3630726B1 (enExample) |
| JP (3) | JP7166292B2 (enExample) |
| KR (1) | KR102611445B1 (enExample) |
| CN (1) | CN110621662B (enExample) |
| AU (1) | AU2018272088C1 (enExample) |
| CA (1) | CA3060370A1 (enExample) |
| DK (1) | DK3630726T3 (enExample) |
| EA (1) | EA039654B1 (enExample) |
| ES (1) | ES2909390T3 (enExample) |
| HU (1) | HUE058196T2 (enExample) |
| IL (1) | IL270780B2 (enExample) |
| MA (1) | MA48776A (enExample) |
| MX (1) | MX2019012505A (enExample) |
| PL (1) | PL3630726T3 (enExample) |
| PT (1) | PT3630726T (enExample) |
| SG (1) | SG11201909161PA (enExample) |
| UA (1) | UA127760C2 (enExample) |
| WO (1) | WO2018218233A1 (enExample) |
| ZA (1) | ZA201906127B (enExample) |
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 |
|---|---|---|---|---|
| CA2939546C (en) * | 2014-02-14 | 2023-01-17 | Exelixis, Inc. | Crystalline solid forms of n-{4-[(6,7-dimethoxyquinolin-4-yl)oxy]phenyl}-n'-(4-fluorophenyl) cyclopropane-1,1-dicarboxamide, processes for making, and methods of use |
| CA3088200A1 (en) | 2018-01-26 | 2019-08-01 | Exelixis, Inc. | Compounds for the treatment of kinase-dependent disorders |
| TWI770624B (zh) | 2018-06-15 | 2022-07-11 | 漢達生技醫藥股份有限公司 | 尼洛替尼十二烷基硫酸鹽在製備用於治療慢性骨髓性白血病之劑型的用途 |
| JP7509779B2 (ja) | 2018-12-13 | 2024-07-02 | エグゼリクシス, インコーポレイテッド | キナーゼ阻害剤の結晶性形態及び塩形態 |
| CA3139148A1 (en) * | 2019-06-03 | 2020-12-10 | Exelixis, Inc. | Crystalline salt forms of a kinase inhibitor |
| CA3245315A1 (en) | 2022-03-01 | 2023-09-07 | Synthon B.V. | L(+) TARTARIC ACID CABOZANTINIB SALT AND ITS SOLID FORMS |
| AU2024215796A1 (en) | 2023-01-31 | 2025-05-15 | Handa Oncology, Llc | Improved cabozantinib compositions and methods of use |
| 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 |
|---|---|---|---|---|
| ES2651730T3 (es) | 2003-09-26 | 2018-01-29 | Exelixis, Inc. | Moduladores c-Met y 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 |
| TWI619495B (zh) | 2010-07-16 | 2018-04-01 | 艾克塞里克斯公司 | C-met調節劑醫藥組合物 |
| US20140057908A1 (en) | 2010-09-27 | 2014-02-27 | Exelixis, Inc. | Method of Treating Cancer |
| EP2621481B2 (en) | 2010-09-27 | 2022-10-19 | Exelixis, Inc. | Dual inhibitors of met and vegf for the treatment of castration-resistant prostate cancer and osteoblastic bone metastases |
| CA2826751C (en) * | 2011-02-10 | 2021-05-18 | 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 |
| MX2013012695A (es) | 2011-05-02 | 2014-03-27 | Exelixis Inc | Metodo para el tratamiento del cancer y el dolor por cancer de hueso. |
| KR20140069133A (ko) | 2011-09-22 | 2014-06-09 | 엑셀리시스, 인코포레이티드 | 골다공증의 치료방법 |
| US9535315B2 (en) | 2011-10-31 | 2017-01-03 | Applied Materials, Inc. | Method of fabricating a color filter array using a multilevel structure |
| JP2015505360A (ja) | 2011-11-08 | 2015-02-19 | エクセリクシス, インク. | 癌治療を定量化する方法 |
| MX2014005458A (es) | 2011-11-08 | 2015-04-16 | Exelixis Inc | Inhibidor doble de met y del factor de crecimiento endotelial vascular (vegf) para el tratamiento del cáncer. |
| 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 |
| CA2939546C (en) * | 2014-02-14 | 2023-01-17 | Exelixis, Inc. | Crystalline solid forms of n-{4-[(6,7-dimethoxyquinolin-4-yl)oxy]phenyl}-n'-(4-fluorophenyl) cyclopropane-1,1-dicarboxamide, processes for making, and methods of use |
| 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 |
| ES2716633T3 (es) | 2015-03-25 | 2019-06-13 | Sandoz Ag | Formas cristalinas de fosfato de cabozantinib e hidrocloruro de cabozantinib |
| US10980792B2 (en) * | 2016-09-12 | 2021-04-20 | Zhuhai Beihai Biotech Co., Ltd. | Formulations of Cabozantinib |
| EP3551612A4 (en) * | 2016-12-07 | 2020-08-12 | 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) -HYDROXYBUTANYEDIOOR AND ITS POLYDROXYBUTANYMATE |
| EA039654B1 (ru) * | 2017-05-26 | 2022-02-22 | Экселиксис, Инк. | Кристаллические твердые формы солей n-{4-[(6,7-диметоксихинолин-4-ил)окси]фенил}-n'-(4-фторфенил)циклопропан-1,1-дикарбоксамида, способы получения и методы использования |
-
2018
- 2018-05-26 EA EA201992803A patent/EA039654B1/ru unknown
- 2018-05-26 AU AU2018272088A patent/AU2018272088C1/en active Active
- 2018-05-26 JP JP2019562380A patent/JP7166292B2/ja active Active
- 2018-05-26 CA CA3060370A patent/CA3060370A1/en active Pending
- 2018-05-26 PL PL18732548T patent/PL3630726T3/pl unknown
- 2018-05-26 UA UAA201912198A patent/UA127760C2/uk unknown
- 2018-05-26 PT PT187325485T patent/PT3630726T/pt unknown
- 2018-05-26 DK DK18732548.5T patent/DK3630726T3/da active
- 2018-05-26 MX MX2019012505A patent/MX2019012505A/es unknown
- 2018-05-26 IL IL270780A patent/IL270780B2/en unknown
- 2018-05-26 KR KR1020197031409A patent/KR102611445B1/ko active Active
- 2018-05-26 SG SG11201909161P patent/SG11201909161PA/en unknown
- 2018-05-26 ES ES18732548T patent/ES2909390T3/es active Active
- 2018-05-26 HU HUE18732548A patent/HUE058196T2/hu 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 US US16/617,352 patent/US11279675B2/en active Active
- 2018-05-26 EP EP18732548.5A patent/EP3630726B1/en active Active
- 2018-05-26 MA MA048776A patent/MA48776A/fr unknown
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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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