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RU2015115397A - Аморфная форма производного хинолина и способ его получения - Google Patents

Аморфная форма производного хинолина и способ его получения Download PDF

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Publication number
RU2015115397A
RU2015115397A RU2015115397A RU2015115397A RU2015115397A RU 2015115397 A RU2015115397 A RU 2015115397A RU 2015115397 A RU2015115397 A RU 2015115397A RU 2015115397 A RU2015115397 A RU 2015115397A RU 2015115397 A RU2015115397 A RU 2015115397A
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RU
Russia
Prior art keywords
cancer
compound according
cyclopropylaminocarbonyl
aminophenoxy
chloro
Prior art date
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RU2015115397A
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English (en)
Inventor
Масахару ГОТОДА
Кенши ЙОСИДА
Нао СИБУГУТИ
Original Assignee
Эйсай Ар Энд Ди Менеджмент Ко., Лтд.
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
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Application filed by Эйсай Ар Энд Ди Менеджмент Ко., Лтд. filed Critical Эйсай Ар Энд Ди Менеджмент Ко., Лтд.
Publication of RU2015115397A publication Critical patent/RU2015115397A/ru

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Classifications

    • 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
    • C07D215/48—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
    • 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)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Oncology (AREA)
  • Hematology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Epidemiology (AREA)
  • Quinoline Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)

Claims (11)

1. Аморфный 4-(3-хлор-4-(циклопропиламинокарбонил)аминофенокси)-7-метокси-6-хинолинкарбоксамид.
2. Аморфное соединение по п. 1, имеющее диффузное гало без отчетливого пика в картине порошковой рентгеновской дифракции.
3. Аморфное соединение по п. 1 или 2, имеющее химические сдвиги пимов 13С, равные 158,1 м.д., 107,4 м.д., 56,3 м.д. и 6,8 м.д., в спектре ядерного магнитного резонанса твердого тела.
4. Способ получения аморфного 4-(3-хлор-4-(циклопропиламинокарбонил)аминофенокси)-7-метокси-6-хинолинкарбоксамида, включающий стадию растворения кристаллов 4-(3-хлор-4-(циклопропиламинокарбонил)аминофенокси)-7-метокси-6-хинолинкарбоксамида в растворителе.
5. Способ по п. 4, дополнительно включающий стадию сублимационной сушки раствора 4-(3-хлор-4-(циклопропиламинокарбонил)аминофенокси)-7-метокси-6-хинолинкарбоксамида.
6. Способ по п. 4 или 5, отличающийся тем, что растворитель выбирают из группы, состоящей из воды, спирта, простого эфира и ацетонитрила и их комбинации.
7. Способ по п. 4 или 5, отличающийся тем, что растворитель выбирают из группы, состоящей из воды, С1-6 спирта и их комбинации.
8. Фармацевтическая композиция, содержащая аморфное соединение по любому одному из пп. 1-3.
9. Противоопухолевое средство, содержащее аморфное соединение по любому одному из пп. 1-3.
10. Противоопухолевое средство по. 9, отличающееся тем, что злокачественная опухоль представляет собой рак щитовидной железы, рак матки, рак яичника, почечно-клеточный рак, рак легкого, глиому, меланому, рак печени, рак желудка, колоректальный рак, рак молочной железы, рак простаты, злокачественную опухоль головного мозга или злокачественное новообразование крови.
11. Ингибитор метастазирования злокачественной опухоли, содержащий аморфное соединение по любому одному из пп. 1-3.
RU2015115397A 2012-12-21 2013-12-19 Аморфная форма производного хинолина и способ его получения RU2015115397A (ru)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
JP2012-279158 2012-12-21
JP2012279158 2012-12-21
PCT/JP2013/084052 WO2014098176A1 (ja) 2012-12-21 2013-12-19 キノリン誘導体のアモルファス及びその製造方法

Publications (1)

Publication Number Publication Date
RU2015115397A true RU2015115397A (ru) 2017-01-25

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RU2015115397A RU2015115397A (ru) 2012-12-21 2013-12-19 Аморфная форма производного хинолина и способ его получения

Country Status (12)

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US (1) US9334239B2 (ru)
EP (1) EP2937337A4 (ru)
JP (1) JPWO2014098176A1 (ru)
KR (1) KR20150098605A (ru)
CN (1) CN104755463A (ru)
AU (1) AU2013364953A1 (ru)
BR (1) BR112015009004A8 (ru)
CA (1) CA2889866A1 (ru)
IL (1) IL238463A0 (ru)
MX (1) MX2015004979A (ru)
RU (1) RU2015115397A (ru)
WO (1) WO2014098176A1 (ru)

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EP3293177B1 (en) * 2015-04-07 2024-11-27 Guangdong Raynovent Biotech Co., Ltd. Tyrosine kinase inhibitor and pharmaceutical composition comprising same
CN104876864B (zh) * 2015-06-05 2017-03-08 北京康立生医药技术开发有限公司 一种乐伐替尼的制备方法
CZ2016240A3 (cs) 2016-04-27 2017-11-08 Zentiva, K.S. Soli lenvatinibu
WO2017218365A1 (en) * 2016-06-16 2017-12-21 Sunshine Lake Pharma Co., Ltd. Crystalline form of a substituted quinoline compound and pharmaceutical compositions thereof
WO2021226738A1 (zh) * 2020-05-09 2021-11-18 北京睿创康泰医药研究院有限公司 包含仑伐替尼的分子水平的药物组合物及其制备方法和应用
CN113831283B (zh) * 2021-11-04 2024-04-19 南京科默生物医药有限公司 一种仑伐替尼盐无定形物的制备方法
CN116354880A (zh) * 2021-12-27 2023-06-30 南京科默生物医药有限公司 一种甲磺酸仑伐替尼晶型c的制备工艺

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AU2013364953A1 (en) 2015-04-30
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