CN106068255A - 结晶固体形式的n‑{4‑[(6,7‑二甲氧基喹啉‑4‑基)氧基]苯基}‑n′‑(4‑氟苯基)环丙烷‑1,1‑二甲酰胺、制备方法以及使用方法 - Google Patents
结晶固体形式的n‑{4‑[(6,7‑二甲氧基喹啉‑4‑基)氧基]苯基}‑n′‑(4‑氟苯基)环丙烷‑1,1‑二甲酰胺、制备方法以及使用方法 Download PDFInfo
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- CN106068255A CN106068255A CN201580012614.4A CN201580012614A CN106068255A CN 106068255 A CN106068255 A CN 106068255A CN 201580012614 A CN201580012614 A CN 201580012614A CN 106068255 A CN106068255 A CN 106068255A
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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
- C07D215/233—Oxygen atoms attached in position 2 or 4 only one oxygen atom which is attached in position 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
- 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
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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)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (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 |
|---|---|---|---|
| US201461939985P | 2014-02-14 | 2014-02-14 | |
| US61/939,985 | 2014-02-14 | ||
| PCT/US2015/016052 WO2015123639A1 (en) | 2014-02-14 | 2015-02-16 | 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 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN106068255A true CN106068255A (zh) | 2016-11-02 |
Family
ID=52684662
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201580012614.4A Pending CN106068255A (zh) | 2014-02-14 | 2015-02-16 | 结晶固体形式的n‑{4‑[(6,7‑二甲氧基喹啉‑4‑基)氧基]苯基}‑n′‑(4‑氟苯基)环丙烷‑1,1‑二甲酰胺、制备方法以及使用方法 |
Country Status (14)
| Country | Link |
|---|---|
| US (5) | US10501418B2 (enExample) |
| EP (2) | EP3738952A1 (enExample) |
| JP (2) | JP6756617B2 (enExample) |
| KR (1) | KR102354963B1 (enExample) |
| CN (1) | CN106068255A (enExample) |
| AU (3) | AU2015218236B2 (enExample) |
| BR (1) | BR112016018450A2 (enExample) |
| CA (2) | CA3181899A1 (enExample) |
| EA (1) | EA032757B1 (enExample) |
| IL (1) | IL247035B2 (enExample) |
| MX (2) | MX384828B (enExample) |
| UA (1) | UA123534C2 (enExample) |
| WO (1) | WO2015123639A1 (enExample) |
| ZA (1) | ZA201605424B (enExample) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN107951850A (zh) * | 2017-12-20 | 2018-04-24 | 深圳万乐药业有限公司 | 一种苹果酸卡博替尼片的制备方法 |
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| 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 |
| RS61485B1 (sr) | 2015-07-16 | 2021-03-31 | Array Biopharma Inc | Supstituisana pirazolo [1,5-a] piridinska jedinjenja kao inhibitori ret kinaze |
| 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 |
| TWI704148B (zh) | 2016-10-10 | 2020-09-11 | 美商亞雷生物製藥股份有限公司 | 作為ret激酶抑制劑之經取代吡唑并[1,5-a]吡啶化合物 |
| JOP20190077A1 (ar) | 2016-10-10 | 2019-04-09 | Array Biopharma Inc | مركبات بيرازولو [1، 5-a]بيريدين بها استبدال كمثبطات كيناز ret |
| 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 |
| EP3571203B1 (en) | 2017-01-18 | 2023-06-07 | Array BioPharma Inc. | Substituted pyrazolo[1,5-a]pyrazine compounds as ret kinase inhibitors |
| WO2018136663A1 (en) | 2017-01-18 | 2018-07-26 | Array Biopharma, Inc. | Ret inhibitors |
| WO2018136796A1 (en) * | 2017-01-20 | 2018-07-26 | Exelixis, Inc. | Combinations of cabozantinib and atezolizumab to treat cancer |
| JOP20190213A1 (ar) | 2017-03-16 | 2019-09-16 | Array Biopharma Inc | مركبات حلقية ضخمة كمثبطات لكيناز ros1 |
| PL3630726T3 (pl) * | 2017-05-26 | 2022-05-09 | Exelixis, Inc. | Krystaliczne stałe sole N-{4-[(6,7-dimetoksychinolin-4-ylo)oksy]fenylo}-N'-(4-fluorofenylo)cyklopropano-1,1-dikarboksyamidu, sposoby ich wytwarzanie oraz ich zastosowania |
| CN110678180A (zh) | 2017-06-09 | 2020-01-10 | 埃克塞里艾克西斯公司 | 治疗癌症的液体剂型 |
| TWI876442B (zh) | 2017-10-10 | 2025-03-11 | 美商絡速藥業公司 | 6-(2-羥基-2-甲基丙氧基)-4-(6-(6-((6-甲氧基吡啶-3-基)甲基)-3,6-二氮雜雙環[3.1.1]庚-3-基)吡啶-3-基)吡唑并[1,5-a]吡啶-3-甲腈之調配物 |
| TWI791053B (zh) | 2017-10-10 | 2023-02-01 | 美商亞雷生物製藥股份有限公司 | 6-(2-羥基-2-甲基丙氧基)-4-(6-(6-((6-甲氧基吡啶-3-基)甲基)-3,6-二氮雜雙環[3.1.1]庚-3-基)吡啶-3-基)吡唑并[1,5-a]吡啶-3-甲腈之結晶形式及其醫藥組合物 |
| CA3087578C (en) | 2018-01-18 | 2023-08-08 | Array Biopharma Inc. | Substituted pyrazolo[3,4-d]pyrimidine compounds as ret kinase inhibitors |
| CN111615514B (zh) | 2018-01-18 | 2022-10-11 | 奥瑞生物药品公司 | 作为ret激酶抑制剂的取代的吡唑并[4,3-c]吡啶化合物 |
| EP3740491A1 (en) | 2018-01-18 | 2020-11-25 | Array Biopharma, Inc. | Substituted pyrrolo[2,3-d]pyrimidines compounds as ret kinase inhibitors |
| 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 |
| JP2022500383A (ja) | 2018-09-10 | 2022-01-04 | アレイ バイオファーマ インコーポレイテッド | Retキナーゼ阻害剤としての縮合複素環式化合物 |
| CR20210375A (es) | 2018-12-13 | 2021-08-18 | Exelixis Inc | Formas cristalinas y formas de sal de un inhibidor de cinasa |
| CA3202761A1 (en) | 2020-11-25 | 2022-06-02 | Nanocopoeia, Llc | Amorphous cabozantinib particles and uses thereof |
| US11590122B2 (en) * | 2021-02-19 | 2023-02-28 | Slayback Pharma Llc | Pharmaceutical compositions of cabozantinib |
| 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 |
| US11814356B1 (en) | 2023-03-29 | 2023-11-14 | Apotex Inc. | Salt of cabozantinib |
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2015
- 2015-02-16 MX MX2016010266A patent/MX384828B/es unknown
- 2015-02-16 BR BR112016018450A patent/BR112016018450A2/pt not_active Application Discontinuation
- 2015-02-16 WO PCT/US2015/016052 patent/WO2015123639A1/en not_active Ceased
- 2015-02-16 JP JP2016551712A patent/JP6756617B2/ja active Active
- 2015-02-16 KR KR1020167024184A patent/KR102354963B1/ko active Active
- 2015-02-16 CA CA3181899A patent/CA3181899A1/en active Pending
- 2015-02-16 EP EP19190844.1A patent/EP3738952A1/en active Pending
- 2015-02-16 UA UAA201609472A patent/UA123534C2/uk unknown
- 2015-02-16 US US15/118,738 patent/US10501418B2/en active Active
- 2015-02-16 EA EA201691629A patent/EA032757B1/ru not_active IP Right Cessation
- 2015-02-16 CA CA2939546A patent/CA2939546C/en active Active
- 2015-02-16 IL IL247035A patent/IL247035B2/en unknown
- 2015-02-16 AU AU2015218236A patent/AU2015218236B2/en active Active
- 2015-02-16 CN CN201580012614.4A patent/CN106068255A/zh active Pending
- 2015-02-16 EP EP15710315.1A patent/EP3105204A1/en not_active Withdrawn
- 2015-02-16 MX MX2021001583A patent/MX2021001583A/es unknown
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2016
- 2016-08-02 ZA ZA2016/05424A patent/ZA201605424B/en unknown
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2019
- 2019-07-04 JP JP2019125128A patent/JP2019163337A/ja active Pending
- 2019-09-10 AU AU2019226302A patent/AU2019226302B2/en active Active
- 2019-11-01 US US16/671,834 patent/US10851061B2/en active Active
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2020
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