RU2004135069A - Приготовление смеси флавоноидов со свободным в-кольцом и флаванов как терапевтического агента - Google Patents

Приготовление смеси флавоноидов со свободным в-кольцом и флаванов как терапевтического агента Download PDF

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RU2004135069A
RU2004135069A RU2004135069/15A RU2004135069A RU2004135069A RU 2004135069 A RU2004135069 A RU 2004135069A RU 2004135069/15 A RU2004135069/15 A RU 2004135069/15A RU 2004135069 A RU2004135069 A RU 2004135069A RU 2004135069 A RU2004135069 A RU 2004135069A
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flavonoids
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Ци ДЗЯ (US)
Ци ДЗЯ
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Юниджен Фармасьютиклз, Инк. (Us)
Юниджен Фармасьютиклз, Инк.
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Claims (39)

1. Композиция, содержащая смесь по меньшей мере одного флавоноида со свободным В-кольцом и по меньшей мере одного флаван.
2. Композиция по п.1, в которой соотношение флавоноидов со свободным В-кольцом к флаванам выбрано из диапазона от 99:1 флавоноидов со свободным В-кольцом к флаванам до 1:99 флавоноидов со свободным В-кольцом к флаванам.
3. Композиция по п.2, в которой соотношение флавоноидов со свободным В-кольцом к флаванам в составе композиции примерно равно 85:15.
4. Композиция по п.1, в которой указанные флавоноиды со свободным В-кольцом выбраны из группы веществ формулы
Figure 00000001
где R1, R2, R3, R4 и R5 независимо выбраны из группы, включающей -Н, -ОН, -SH, OR, -SR, -NH2, -NHR, -NR2, -NR3+X-, углерод, кислород, азот или серу, гликозид простого сахара или комбинацию сложных Сахаров, включая альдопентозы, метилальдопентозу, альдогексозы, кетогексозу и их химические производные;
где R означает алкильную группу, имеющую от 1 до 10 атомов углерода; и
Х выбран из группы фармацевтически приемлемых противоанионов, включая гидроксил, хлорид, иодид, сульфат, фосфат, ацетат, фторид и карбонат.
5. Композиция по п.1, в которой указанный флаван выбран из группы веществ, имеющих следующую структуру:
Figure 00000002
где R1, R2, R3, R4 и R5 независимо выбраны из группы, содержащей Н, -ОН, -SH, -ОСН3, -SCH3, -OR, -SR, -NH2, -NRH, -NR2, -NR3+X-, сложные эфиры замещающих групп, независимо выбранные из группы, содержащей галлат, ацетат, циннамоил и сложные эфиры гидроксилциннамоила, сложные эфиры тригидроксибензоила и сложные эфиры каффеоила; углерод, кислород, азот или серу; гликозид протого сахара или комбинацию сложных Сахаров, включая альдопентозы, метилальдопентозу, альдогексозы, котогексозу и их химические производные; димеры, тримеры или другие полимеризованные флаваны;
где R означает алкильную группу из 1-10 атомов углерода; и
Х выбран из группы фармацевтически приемлемых противоанионов, включая, но не ограничиваясь ими, гидроксил, хлорид, иодид, сульфат, фосфат, ацетат, фторид, карбонат.
6. Композиция по п.1, в которой указанный флавоноид со свободным В-кольцом и указанный флаван получены органическим синтезом или выделены из растения.
7. Композиция по п.6, в которой указанный флавоноид со свободным В-кольцом и указанный флаван выделены из частей растений, выбранных из группы, содержащей стебли, кору стеблей, стволы, кору стволов, ветки, клубни, корни, кору корней, молодые побеги, семена, корневища, цветы и другие репродуктивные органы, листья и другие надземные части растений.
8. Композиция по п.6, в которой указанный флавоноид со свободным В-кольцом выделен из семейства растений, выбранного из группы, включающей семейства Annonaceae, Asteraceae, Bignoniaceae, Combretaceae, Compositae, Euphorbiaceae, Labiatae, Lauranceae, Leguminosae, Moraceae, Pinaceae, Pteridaceae, Sinopteridaceae, Ulmaceae и Zingiberacea.
9. Композиция по п.6, в которой указанный флавоноид со свободным В-кольцом выделен из рода растений, выбранного из группы, включающей роды растений Desmos, Achyrocline, Oroxylum, Buchenavia, Anaphalis, Cotula, Gnaphalium, Helichrysum, Centaurea, Eupatorium, Baccharis, Sapium, Scutellaria, Molsa, Colebrookea, Stachys, Origanum, Ziziphora, Lindera, Actinodaphne, Acacia, Derris, Glycyrrhiza, Millettia, Pongamia, Tephrosia, Artocarpus, Ficus, Pityrogramma, Notholaena, Pinus, Ulmus и Alpinia.
10. Композиция по п.6, в которой указанный флаван выделен из растения, относящегося к виду, выбранному из группы, включающей виды растений Acacia catechu, A. concinna, A. farnesiana, A. Senegal, A. speciosa, A. arabica, A. caesia, A. pennata, A. sinuata. A. mearnsii, A. picnantha, A. dealbata, A. auriculiformis, A. holoserecia и A. mangium.
11. Композиция по п.6, в которой указанный флавоноид со свободным В-кольцом выделен из растения или растений рода Scutellaria и указанный флавон выделен из растения или растений рода Acacia.
12. Способ облегчения суставной боли и тугоподвижности и улучшения подвижности и физической функции, заключающийся во введении субъекту, нуждающемуся в этом, эффективного количества композиции, содержащей смесь флавоноидов со свободным В-кольцом и флаванов.
13. Способ по п.12, в котором композиция применяется в дозе, выбранной от 0,01 до 200 мг/кг веса тела.
14. Способ по п.12, в котором путь введения выбран из группы, включающей пероральный, местный, суппозитарный, внутрикожный, внутрижелудочный, внутримышечный, внутрибрюшинный и внутривенный.
15. Способ предупреждения и лечения патологических состояний, связанных с остеоартритом и ревматоидным артритом, который заключается во введении субъекту, нуждающемуся в этом, эффективного количества композиции, содержащей смесь флавоноидов со свободным В-кольцом и флаванов вместе с фармацевтически приемлемым носителем.
16. Способ по п.15, в котором композиция вводится в дозе, выбранной от 0,01 до 200 мг/кг веса тела.
17. Способ по п.15, в котором путь введения выбран из группы, включающей пероральный, местный, суппозитарный, внутрикожный, внутрижелудочный, внутримышечный, внутрибрюшинный и внутривенный.
18. Способ ингибирования ферментной активности фермента циклооксигеназы ЦО-2, заключающийся во введении субъекту, нуждающемуся в этом, эффективного количества композиции, содержащей смесь флавоноидов со свободным В-кольцом и флаванов.
19. Способ по п.18, в котором композиция вводится в дозе, выбранной от 0,01 до 200 мг/кг веса тела.
20. Способ по п.18, в котором путь введения выбран из группы, включающей пероральный, местный, суппозитарный, внутрикожный, внутрижелудочный, внутримышечный, внутрибрюшинный и внутривенный.
21. Способ ингибирования ферментной активности фермента 5-липоксигеназы (5-ЛО), заключающийся во введении субъекту, нуждающемуся в этом, эффективного количества композиции, содержащей смесь флавоноидов со свободным В-кольцом и флаванов.
22. Способ по п.21, в котором композиция вводится в дозе, выбранной от 0,01 до 200 мг/кг веса тела.
23. Способ по п.21, в котором путь введения выбран из группы, включающей пероральный, местный, суппозитарный, внутрикожный, внутрижелудочный, внутримышечный, внутрибрюшинный и внутривенный.
24. Способ одновременного ингибирования ферментной активности фермента ЦО-2 и фермента 5-ЛО, заключающийся во введении субъекту, нуждающемуся в этом, эффективного количества композиции, содержащей смесь флавоноидов со свободным В-кольцом и флаванов.
25. Способ по п.24, в котором композиция вводится в дозе, выбранной от 0,01 до 200 мг/кг веса тела.
26. Способ по п.24, в котором путь введения выбран из группы, включающей пероральный, местный, суппозитарный, внутрикожный, внутрижелудочный, внутримышечный, внутрибрюшинный и внутривенный.
27. Способ ингибирования образования сох-2 и РНК, заключающийся во введении субъекту, нуждающемуся в этом, эффективного количества композиции, содержащей смесь флавоноидов со свободным В-кольцом и флаванов.
28. Способ по п.27, в котором композиция вводится в дозе, выбранной от 0,01 до 200 мг/кг веса тела.
29. Способ по п.27, в котором путь введения выбран из группы, включающей пероральный, местный, суппозитарный, внутрикожный, внутрижелудочный, внутримышечный, внутрибрюшинный и внутривенный.
30. Способ предупреждения и лечения заболеваний и болезненных состояний, связанных с метаболическими путями ЦО-2 и 5-ЛО, заключающийся во введении субъекту, нуждающемуся в этом, эффективного количества композиции, содержащей смесь флавоноидов со свободным В-кольцом и флаванов.
31. Способ по п.30, в котором композиция вводится в дозе, выбранной от 0,01 до 200 мг/кг веса тела.
32. Способ по п.30, в котором путь введения выбран из группы, включающей пероральный, местный, суппозитарный, внутрикожный, внутрижелудочный, внутримышечный, внутрибрюшинный и внутривенный.
33. Способ по п.30, в котором физиологические и патологические состояния, связанные в метаболическими путями ЦО-2 и 5-ЛО, выбраны из группы, включающей менструальные спазмы, артериосклероз, сердечный приступ, ожирение, диабет, синдром X, болезнь Альцгеймера, респираторную аллергическую реакцию, хроническую венозную недостаточность, геморрой, системную красную волчанку, псориаз, хронической синдром головной боли, мигрень, воспаление кишечника; местные инфекции, вызванные вирусами, бактериями, грибами, солнечную эритему, термические ожоги, контактный дерматит, меланому и карциному.
34. Способ снижения содержания глюкозы в крови, заключающийся во введении субъекту, нуждающемуся в этом, эффективного количества композиции, содержащей смесь флавоноидов со свободным В-кольцом и флаванов.
35. Способ по п.34, в котором композиция вводится в дозе, выбранной от 0,01 до 200 мг/кг веса тела.
36. Способ по п.34, в котором путь введения выбран из группы, включающей пероральный, местный, суппозитарный, внутрикожный, внутрижелудочный, внутримышечный, внутрибрюшинный и внутривенный.
37. Способ снижения индекса массы тела и вызывающий потерю веса, заключающийся во введении субъекту, нуждающемуся в этом, эффективного количества композиции, содержащей смесь флавоноидов со свободным В-кольцом и флаванов.
38. Способ по п.37, в котором композиция вводится в дозе, выбранной от 0,01 до 200 мг/кг веса тела.
39. Способ по п.37, в котором пути введения выбран из группы, включающей пероральный, местный, суппозитарный, внутрикожный, внутрижелудочный, внутримышечный, внутрибрюшинный и внутривенный.
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