RU2018127873A - Получение и составление композиции, содержащей ингибитор mek - Google Patents

Получение и составление композиции, содержащей ингибитор mek Download PDF

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RU2018127873A
RU2018127873A RU2018127873A RU2018127873A RU2018127873A RU 2018127873 A RU2018127873 A RU 2018127873A RU 2018127873 A RU2018127873 A RU 2018127873A RU 2018127873 A RU2018127873 A RU 2018127873A RU 2018127873 A RU2018127873 A RU 2018127873A
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pharmaceutical composition
cancer
methyl
cellulose
fluorophenylamino
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RU2018127873A
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Кристоф Макс КРЕЛЛ
Мариан МИСУН
Даниэль Андреас НЬЕДЕРЕЕР
Вернер Хейнц ПАХИНГЕР
Мари-Кристин ВОЛЬФ
Даниэль ЦИММЕРМАНН
Вэйдун ЛЮ
Питер Дж. СТЕНДЖЕЛ
Пол НИКОЛС
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Новартис Аг
Эррэй Биофарма Инк.
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Application filed by Новартис Аг, Эррэй Биофарма Инк. filed Critical Новартис Аг
Publication of RU2018127873A publication Critical patent/RU2018127873A/ru

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    • AHUMAN NECESSITIES
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    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/41641,3-Diazoles
    • A61K31/41841,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
    • AHUMAN NECESSITIES
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    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
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    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
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    • A61K47/06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
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    • A61K47/06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/26Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
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    • A61K47/30Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/36Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
    • A61K47/38Cellulose; Derivatives thereof
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    • A61K9/0053Mouth and digestive tract, i.e. intraoral and peroral administration
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    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2009Inorganic compounds
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2013Organic compounds, e.g. phospholipids, fats
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    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2013Organic compounds, e.g. phospholipids, fats
    • A61K9/2018Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
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    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2022Organic macromolecular compounds
    • A61K9/205Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2054Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • C07D235/00Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04Benzimidazoles; Hydrogenated benzimidazoles
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    • C07D235/04Benzimidazoles; Hydrogenated benzimidazoles
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    • C30B7/00Single-crystal growth from solutions using solvents which are liquid at normal temperature, e.g. aqueous solutions
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Claims (18)

1. Фармацевтическая композиция, содержащая кристаллический (2-гидроксиэтокси)амид 6-(4-бром-2-фторфениламино)-7-фтор-3-метил-3H-бензимидазол-5-карбоновой кислоты, по меньшей мере один сахар и по меньшей мере одно целлюлозное вспомогательное вещество.
2. Фармацевтическая композиция по п. 1, где по меньшей мере один сахар представляет собой моногидрат лактозы.
3. Фармацевтическая композиция по п. 1, где по меньшей мере одно целлюлозное вспомогательное вещество представляет собой микрокристаллическую целлюлозу, сверхтонкую целлюлозу, порошкообразную целлюлозу, метилцеллюлозу, гидроксиэтилцеллюлозу, гидроксиметилцеллюлозу, гидроксипропилцеллюлозу или гидроксипропилметилцеллюлозу.
4. Фармацевтическая композиция по п. 3, где по меньшей мере одно целлюлозное вспомогательное вещество представляет собой микрокристаллическую целлюлозу.
5. Фармацевтическая композиция по любому из пп. 1-4, дополнительно содержащая одно или более из кроскармеллозы натрия, стеарата магния и диоксида кремния.
6. Фармацевтическая композиция по любому из пп. 1-5, содержащая 5-35 массовых процентов кристаллического (2-гидроксиэтокси)амида 6-(4-бром-2-фторфениламино)-7-фтор-3-метил-3H-бензимидазол-5-карбоновой кислоты.
7. Фармацевтическая композиция по любому из пп. 1-5, содержащая приблизительно 15 мг кристаллического (2-гидроксиэтокси)амида 6-(4-бром-2-фторфениламино)-7-фтор-3-метил-3H-бензимидазол-5-карбоновой кислоты.
8. Фармацевтическая композиция по любому из пп. 1-5, содержащая приблизительно 45 мг кристаллического (2-гидроксиэтокси)амида 6-(4-бром-2-фторфениламино)-7-фтор-3-метил-3H-бензимидазол-5-карбоновой кислоты.
9. Фармацевтическая композиция, содержащая около 5-11% кристаллического (2-гидроксиэтокси)амида 6-(4-бром-2-фторфениламино)-7-фтор-3-метил-3H-бензимидазол-5-карбоновой кислоты, около 55-56% моногидрата лактозы и около 30-36% микрокристаллической целлюлозы относительно массы композиции.
10. Фармацевтическая композиция по п. 9, дополнительно содержащая около 1,5-2,5% кроскармеллозы натрия, около 0,5-0,9% стеарата магния и около 0,1-1% коллоидного диоксида кремния/коллоидного безводного диоксида кремния относительно массы композиции.
11. Фармацевтическая композиция по любому из пп. 1-10, которая представлена в форме таблетки.
12. Фармацевтическая композиция для лечения пролиферативного заболевания у субъекта, содержащая кристаллический (2-гидроксиэтокси)амид 6-(4-бром-2-фторфениламино)-7-фтор-3-метил-3H-бензимидазол-5-карбоновой кислоты, по меньшей мере один сахар и по меньшей мере одно целлюлозное вспомогательное вещество, отличающаяся тем, что композицию вводят нуждающемуся в том субъекту.
13. Фармацевтическая композиция по п. 12, где пролиферативное заболевание представляет собой рак.
14. Фармацевтическая композиция по п. 13, где рак представляет собой солидную опухоль или лимфому.
15. Фармацевтическая композиция по п. 13, где рак представляет собой меланому, рак поджелудочной железы, рак яичников, рак фаллопиевых труб, перитонеальный рак, рак желчных протоков, рак толстой кишки или рак прямой кишки.
16. Фармацевтическая композиция по п. 13, где рак представляет собой меланому.
17. Фармацевтическая композиция по п. 13, где рак представляет собой рак толстой кишки.
18. Фармацевтическая композиция по п. 13, где рак представляет собой рак яичников.
RU2018127873A 2012-10-19 2013-10-18 Получение и составление композиции, содержащей ингибитор mek RU2018127873A (ru)

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BR112015008623A2 (pt) 2017-07-04
EP3702351B1 (en) 2023-11-22
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RU2669391C2 (ru) 2018-10-11
DK3702351T3 (da) 2024-01-29
AR099630A1 (es) 2016-08-10
PT2909182T (pt) 2020-03-02
JP2018135399A (ja) 2018-08-30
WO2014063024A1 (en) 2014-04-24
EP2909182A4 (en) 2016-07-06
US20160168104A1 (en) 2016-06-16
US20160168103A1 (en) 2016-06-16
CA2888474C (en) 2021-03-02
JP2016503391A (ja) 2016-02-04
TWI650316B (zh) 2019-02-11
HK1214254A1 (zh) 2016-07-22
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US9562016B2 (en) 2017-02-07
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