RU2017128583A - Способ ослабления горечи хинолинового производного - Google Patents
Способ ослабления горечи хинолинового производного Download PDFInfo
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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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- 238000000034 method Methods 0.000 title claims 18
- SMWDFEZZVXVKRB-UHFFFAOYSA-N Quinoline Chemical class N1=CC=CC2=CC=CC=C21 SMWDFEZZVXVKRB-UHFFFAOYSA-N 0.000 title 1
- 239000000126 substance Substances 0.000 claims 22
- 150000003839 salts Chemical class 0.000 claims 19
- WOSKHXYHFSIKNG-UHFFFAOYSA-N lenvatinib Chemical compound C=12C=C(C(N)=O)C(OC)=CC2=NC=CC=1OC(C=C1Cl)=CC=C1NC(=O)NC1CC1 WOSKHXYHFSIKNG-UHFFFAOYSA-N 0.000 claims 17
- 239000008194 pharmaceutical composition Substances 0.000 claims 17
- VTYYLEPIZMXCLO-UHFFFAOYSA-L Calcium carbonate Chemical group [Ca+2].[O-]C([O-])=O VTYYLEPIZMXCLO-UHFFFAOYSA-L 0.000 claims 12
- 235000019658 bitter taste Nutrition 0.000 claims 11
- 239000003125 aqueous solvent Substances 0.000 claims 10
- 239000000725 suspension Substances 0.000 claims 8
- 229910000019 calcium carbonate Inorganic materials 0.000 claims 6
- 238000002360 preparation method Methods 0.000 claims 4
- BVKZGUZCCUSVTD-UHFFFAOYSA-L Carbonate Chemical compound [O-]C([O-])=O BVKZGUZCCUSVTD-UHFFFAOYSA-L 0.000 claims 3
- AFVFQIVMOAPDHO-UHFFFAOYSA-N Methanesulfonic acid Chemical group CS(O)(=O)=O AFVFQIVMOAPDHO-UHFFFAOYSA-N 0.000 claims 3
- XLYOFNOQVPJJNP-UHFFFAOYSA-M hydroxide Chemical compound [OH-] XLYOFNOQVPJJNP-UHFFFAOYSA-M 0.000 claims 3
- 239000000395 magnesium oxide Substances 0.000 claims 3
- CPLXHLVBOLITMK-UHFFFAOYSA-N magnesium oxide Inorganic materials [Mg]=O CPLXHLVBOLITMK-UHFFFAOYSA-N 0.000 claims 3
- AXZKOIWUVFPNLO-UHFFFAOYSA-N magnesium;oxygen(2-) Chemical compound [O-2].[Mg+2] AXZKOIWUVFPNLO-UHFFFAOYSA-N 0.000 claims 3
- 239000000463 material Substances 0.000 claims 3
- 206010028980 Neoplasm Diseases 0.000 claims 2
- 201000011510 cancer Diseases 0.000 claims 2
- 239000003795 chemical substances by application Substances 0.000 claims 2
- 239000006188 syrup Substances 0.000 claims 2
- 235000020357 syrup Nutrition 0.000 claims 2
- 239000007919 dispersible tablet Substances 0.000 claims 1
- 239000002552 dosage form Substances 0.000 claims 1
- 239000007938 effervescent tablet Substances 0.000 claims 1
- 239000007788 liquid Substances 0.000 claims 1
- 239000007937 lozenge Substances 0.000 claims 1
- 210000000214 mouth Anatomy 0.000 claims 1
- 239000007944 soluble tablet Substances 0.000 claims 1
- 239000003826 tablet Substances 0.000 claims 1
Classifications
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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
- A61K9/0087—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
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- General Chemical & Material Sciences (AREA)
- Inorganic Chemistry (AREA)
- Dispersion Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nutrition Science (AREA)
- Physiology (AREA)
- Plural Heterocyclic Compounds (AREA)
- Zoology (AREA)
- Quinoline Compounds (AREA)
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).
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201562120561P | 2015-02-25 | 2015-02-25 | |
| US62/120561 | 2015-02-25 | ||
| 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 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| RU2017128583A true RU2017128583A (ru) | 2019-03-25 |
| RU2017128583A3 RU2017128583A3 (ru) | 2019-03-25 |
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| Application Number | Title | Priority Date | Filing Date |
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| RU2017128583A RU2017128583A (ru) | 2015-02-25 | 2016-02-23 | Способ ослабления горечи хинолинового производного |
Country Status (24)
| Country | Link |
|---|---|
| US (2) | US20180028662A1 (ru) |
| EP (1) | EP3263106B1 (ru) |
| JP (1) | JP6792546B2 (ru) |
| KR (2) | KR20250024102A (ru) |
| CN (1) | CN107427505A (ru) |
| AU (1) | AU2016224583B2 (ru) |
| BR (1) | BR112017017428A2 (ru) |
| CA (1) | CA2976325C (ru) |
| DK (1) | DK3263106T3 (ru) |
| ES (1) | ES2967362T3 (ru) |
| FI (1) | FI3263106T3 (ru) |
| HR (1) | HRP20231692T1 (ru) |
| HU (1) | HUE064614T2 (ru) |
| IL (2) | IL253946B1 (ru) |
| LT (1) | LT3263106T (ru) |
| MX (1) | MX385403B (ru) |
| PL (1) | PL3263106T3 (ru) |
| PT (1) | PT3263106T (ru) |
| RS (1) | RS65049B1 (ru) |
| RU (1) | RU2017128583A (ru) |
| SG (1) | SG11201706630UA (ru) |
| SI (1) | SI3263106T1 (ru) |
| SM (1) | SMT202400005T1 (ru) |
| WO (1) | WO2016136745A1 (ru) |
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| Publication number | Priority date | Publication date | Assignee | Title |
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| US20200345637A1 (en) * | 2018-01-19 | 2020-11-05 | Aiviva Biopharma, Inc. | Suspension compositions of multi-target inhibitors |
| CN112190583B (zh) * | 2019-07-08 | 2021-10-29 | 成都苑东生物制药股份有限公司 | 一种乐伐替尼药物组合物及其制备方法 |
| EP4153140A4 (en) * | 2020-05-23 | 2024-07-17 | Shilpa Medicare Limited | Oral liquid formulations of lenvatinib |
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