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 |
|---|---|---|---|---|
| AU2015218236B2 (en) * | 2014-02-14 | 2019-06-13 | 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 |
| GEAP202415420A (en) | 2018-01-26 | 2024-12-25 | Exelixis Inc | Compounds for the treatment of kinase-dependent disorders |
| CN120305263A (zh) | 2018-06-15 | 2025-07-15 | 汉达癌症医药责任有限公司 | 卡博替尼的盐类于制备治疗癌症的剂型的用途 |
| EP4631505A3 (en) * | 2018-12-13 | 2025-12-10 | Exelixis, Inc. | Crystalline forms and salt forms of a kinase inhibitor |
| SG11202111978VA (en) * | 2019-06-03 | 2021-11-29 | Exelixis Inc | Crystalline salt forms of a kinase inhibitor |
| WO2023165948A1 (en) | 2022-03-01 | 2023-09-07 | Synthon B.V. | Cabozantinib salt with l-(+)-tartaric acid and solid forms thereof |
| 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 |
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| Publication number | Priority date | Publication date | Assignee | Title |
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| CA2744997A1 (en) | 2003-09-26 | 2005-04-07 | Exelixis, Inc. | C-met modulators and method of use |
| 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 |
| WO2012009722A1 (en) | 2010-07-16 | 2012-01-19 | Exelixis, Inc. | C-met modulator pharmaceutical compositions |
| CN103391773A (zh) | 2010-09-27 | 2013-11-13 | 埃克塞里艾克西斯公司 | 用于治疗去势抵抗性前列腺癌和成骨性骨转移的met和vegf的双重抑制剂 |
| DK2621481T4 (da) | 2010-09-27 | 2023-01-09 | Exelixis Inc | Dobbelte inhibitorer af MET og VEGF til behandling af kastrationsresistent prostatacancer og osteoblastiske knoglemetastaser |
| TWI640509B (zh) | 2011-02-10 | 2018-11-11 | 艾克塞里克斯公司 | 製造喹啉化合物之方法及包含該化合物之醫藥組合物 |
| US20120252840A1 (en) | 2011-04-04 | 2012-10-04 | Exelixis, Inc. | Method of Treating Cancer |
| TWI610918B (zh) | 2011-05-02 | 2018-01-11 | 艾克塞里克斯公司 | 治療癌症及骨癌疼痛之方法 |
| GEP201606523B (en) | 2011-09-22 | 2016-08-10 | Exelixis Inc | Method for treating osteoporosis |
| WO2013066296A1 (en) | 2011-10-31 | 2013-05-10 | Hewlett-Packard Development Company, L.P. | Method of fabricating a color filter array using a multilevel structure |
| EP2776033A1 (en) | 2011-11-08 | 2014-09-17 | Exelixis, Inc. | Dual inhibitor of met and vegf for treating cancer |
| 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 |
| AU2015218236B2 (en) * | 2014-02-14 | 2019-06-13 | 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 |
| 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 |
| WO2016150966A1 (en) | 2015-03-25 | 2016-09-29 | 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 |
| IL270780B2 (en) * | 2017-05-26 | 2025-04-01 | Exelixis Inc | Crystalline solid forms of salts of N–{4–[(7,6–dimethoxyquinolin–4–yl)oxy]phenyl}–N'–(4–fluorophenyl)cyclopropane–1,1–dicarboxamide, processes for preparation and methods of use |
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2018
- 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 MA MA048776A patent/MA48776A/fr unknown
- 2018-05-26 ES ES18732548T patent/ES2909390T3/es active Active
- 2018-05-26 MX MX2019012505A patent/MX2019012505A/es unknown
- 2018-05-26 EA EA201992803A patent/EA039654B1/ru unknown
- 2018-05-26 CN CN201880027861.5A patent/CN110621662B/zh active Active
- 2018-05-26 DK DK18732548.5T patent/DK3630726T3/da active
- 2018-05-26 PL PL18732548T patent/PL3630726T3/pl unknown
- 2018-05-26 PT PT187325485T patent/PT3630726T/pt unknown
- 2018-05-26 EP EP18732548.5A patent/EP3630726B1/en active Active
- 2018-05-26 HU HUE18732548A patent/HUE058196T2/hu unknown
- 2018-05-26 AU AU2018272088A patent/AU2018272088C1/en active Active
- 2018-05-26 CA CA3060370A patent/CA3060370A1/en active Pending
- 2018-05-26 US US16/617,352 patent/US11279675B2/en active Active
- 2018-05-26 SG SG11201909161P patent/SG11201909161PA/en unknown
- 2018-05-26 KR KR1020197031409A patent/KR102611445B1/ko active Active
- 2018-05-26 UA UAA201912198A patent/UA127760C2/uk unknown
- 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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