RU2017128583A - Способ ослабления горечи хинолинового производного - Google Patents

Способ ослабления горечи хинолинового производного Download PDF

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RU2017128583A
RU2017128583A RU2017128583A RU2017128583A RU2017128583A RU 2017128583 A RU2017128583 A RU 2017128583A RU 2017128583 A RU2017128583 A RU 2017128583A RU 2017128583 A RU2017128583 A RU 2017128583A RU 2017128583 A RU2017128583 A RU 2017128583A
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pharmaceutically acceptable
acceptable salt
cyclopropylaminocarbonyl
aminophenoxy
chloro
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RU2017128583A
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Кентаро НАГАНЕ
Йосуке УЕКИ
Сюсуке САНО
Такахиса САКАГУТИ
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Эйсай Ар Энд Ди Менеджмент Ко., Лтд.
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/02—Inorganic compounds
    • 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
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
    • A61K9/0056—Mouth soluble or dispersible forms; Suckable, eatable, chewable coherent forms; Forms rapidly disintegrating in the mouth; Lozenges; Lollipops; Bite capsules; Baked products; Baits or other oral forms for animals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0087—Galenical forms not covered by A61K9/02 - A61K9/7023
    • A61K9/0095—Drinks; Beverages; Syrups; Compositions for reconstitution thereof, e.g. powders or tablets to be dispersed in a glass of water; Veterinary drenches
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/10—Dispersions; Emulsions
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

Claims (41)

1. Способ ослабления горечи 4-(3-хлор-4-(циклопропиламинокарбонил)аминофенокси)-7-метокси-6-хинолинкарбоксамида, включающий смешивание 4-(3-хлор-4-(циклопропиламинокарбонил)аминофенокси)-7-метокси-6-хинолинкарбоксамида или его фармацевтически приемлемой соли и основного вещества.
2. Способ по п. 1, где смешивают 0,01-50 весовых частей основного вещества на 1 весовую часть 4-(3-хлор-4-(циклопропиламинокарбонил)аминофенокси)-7-метокси-6-хинолинкарбоксамида или его фармацевтически приемлемой соли.
3. Способ по п. 1, где смешивают 0,16-80 моль основного вещества на 1 моль 4-(3-хлор-4-(циклопропиламинокарбонил)аминофенокси)-7-метокси-6-хинолинкарбоксамида или его фармацевтически приемлемой соли.
4. Способ по любому из пп. 1-3, где основное вещество представляет собой основный оксид, основный карбонат или основный гидроксид.
5. Способ по любому из пп. 1-3, где основное вещество представляет собой карбонат кальция или оксид магния.
6. Способ по любому из пп. 1-3, где основное вещество представляет собой карбонат кальция.
7. Способ по любому из пп. 1-6, где фармацевтически приемлемая соль представляет собой мезилат.
8. Фармацевтическая композиция, содержащая 4-(3-хлор-4-(циклопропиламинокарбонил)аминофенокси)-7-метокси-6-хинолинкарбоксамид или его фармацевтически приемлемую соль и основное вещество в количестве, эффективном для ослабления горечи.
9. Фармацевтическая композиция, содержащая 4-(3-хлор-4-(циклопропиламинокарбонил)аминофенокси)-7-метокси-6-хинолинкарбоксамид или его фармацевтически приемлемую соль, при этом фармацевтическая композиция содержит средство для смешивания с основным веществом для ослабления горечи.
10. Фармацевтическая композиция, содержащая 4-(3-хлор-4-(циклопропиламинокарбонил)аминофенокси)-7-метокси-6-хинолинкарбоксамид или его фармацевтически приемлемую соль и основное вещество, при этом фармацевтическая композиция характеризуется ослабленной горечью.
11. Фармацевтическая композиция по любому из пп. 8-10, содержащая 0,01-50 весовых частей основного вещества на 1 весовую часть 4-(3-хлор-4-(циклопропиламинокарбонил)аминофенокси)-7-метокси-6-хинолинкарбоксамида или его фармацевтически приемлемой соли.
12. Фармацевтическая композиция по любому из пп. 8-10, где смешивают 0,16-80 моль основного вещества на 1 моль 4-(3-хлор-4-(циклопропиламинокарбонил)аминофенокси)-7-метокси-6-хинолинкарбоксамида или его фармацевтически приемлемой соли.
13. Фармацевтическая композиция по любому из пп. 8-12, где основное вещество представляет собой основный оксид, основный карбонат или основный гидроксид.
14. Фармацевтическая композиция по любому из пп. 8-12, где основное вещество представляет собой карбонат кальция или оксид магния.
15. Фармацевтическая композиция по любому из пп. 8-12, где основное вещество представляет собой карбонат кальция.
16. Фармацевтическая композиция по любому из пп. 8-15, где фармацевтически приемлемая соль представляет собой мезилат.
17. Фармацевтическая композиция по любому из пп. 8-16 в виде лекарственной формы, представляющей собой таблетку, распадающуюся в полости рта, препарат в жевательной форме, шипучую таблетку, диспергируемую таблетку, растворимую таблетку, сироп, препарат для получения сиропа, пастилку или жидкий препарат для перорального применения.
18. Фармацевтическая композиция по любому из пп. 8-16, представляющая собой препарат, который при введении может быть суспендирован в водном растворителе с получением суспензии.
19. Средство для ослабления горечи 4-(3-хлор-4-(циклопропиламинокарбонил)аминофенокси)-7-метокси-6-хинолинкарбоксамида или его фармацевтически приемлемой соли, содержащее основное вещество.
20. Средство для ослабления горечи по п. 19, где добавляемое основное вещество содержится в количестве 0,01-50 весовых частей на 1 весовую часть 4-(3-хлор-4-(циклопропиламинокарбонил)аминофенокси)-7-метокси-6-хинолинкарбоксамида или его фармацевтически приемлемой соли.
21. Средство для ослабления горечи по п. 19, где добавляемое основное вещество содержится в количестве 0,16-80 моль на 1 моль 4-(3-хлор-4-(циклопропиламинокарбонил)аминофенокси)-7-метокси-6-хинолинкарбоксамида или его фармацевтически приемлемой соли.
22. Средство для ослабления горечи по любому из пп. 19-21, где основное вещество представляет собой основный оксид, основный карбонат или основный гидроксид.
23. Средство для ослабления горечи по любому из пп. 19-21, где основное вещество представляет собой карбонат кальция или оксид магния.
24. Средство для ослабления горечи по любому из пп. 19-21, где основное вещество представляет собой карбонат кальция.
25. Средство для ослабления горечи по любому из пп. 19-24, где фармацевтически приемлемая соль представляет собой мезилат.
26. Способ введения суспензии, содержащей 4-(3-хлор-4-(циклопропиламинокарбонил)аминофенокси)-7-метокси-6-хинолинкарбоксамид или его фармацевтически приемлемую соль и основное вещество, при этом способ включает:
суспендирование в водном растворителе в сосуде фармацевтической композиции, содержащей 1-24 мг 4-(3-хлор-4-(циклопропиламинокарбонил)аминофенокси)-7-метокси-6-хинолинкарбоксамида или его фармацевтически приемлемой соли и основное вещество;
введение пациенту суспензии, полученной на 1), из сосуда;
ополаскивание сосуда водным растворителем; и
введение пациенту раствора после ополаскивания, полученного на 3).
27. Способ по п. 26, где 1) включает i) выливание водного растворителя в сосуд, ii) обеспечение возможности отстаивания содержимого сосуда и iii) встряхивание сосуда.
28. Способ по п. 26 или 27, где на 1) фармацевтическую композицию суспендируют в 1-10 мл водного растворителя.
29. Способ по п. 28, где на 1) фармацевтическую композицию суспендируют в приблизительно 3 мл водного растворителя.
30. Способ по п. 26, где на 3) сосуд ополаскивают 1-10 мл водного растворителя.
31. Способ по п. 30, где на 3) сосуд ополаскивают приблизительно 2 мл водного растворителя.
32. Способ лечения рака, включающий введение суспензии, содержащей 1-24 мг 4-(3-хлор-4-(циклопропиламинокарбонил)аминофенокси)-7-метокси-6-хинолинкарбоксамида или его фармацевтически приемлемой соли и основное вещество.
33. Способ лечения рака, включающий введение суспензии, содержащей 4-(3-хлор-4-(циклопропиламинокарбонил)аминофенокси)-7-метокси-6-хинолинкарбоксамид или его фармацевтически приемлемую соль и основное вещество, при этом способ включает:
суспендирование в водном растворителе в сосуде фармацевтической композиции, содержащей 1-24 мг 4-(3-хлор-4-(циклопропиламинокарбонил)аминофенокси)-7-метокси-6-хинолинкарбоксамида или его фармацевтически приемлемой соли и основное вещество;
введение пациенту суспензии, полученной на 1), из сосуда;
ополаскивание сосуда водным растворителем; и
введение пациенту раствора после ополаскивания, полученного на 3).
RU2017128583A 2015-02-25 2016-02-23 Способ ослабления горечи хинолинового производного RU2017128583A (ru)

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US201562120561P 2015-02-25 2015-02-25
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PCT/JP2016/055268 WO2016136745A1 (ja) 2015-02-25 2016-02-23 キノリン誘導体の苦味抑制方法

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