RU2011133741A - Модифицированные 2'- и 3'-нуклеозиды и их применение для получения лекарственного средства для лечения инфекций flaviviridae - Google Patents
Модифицированные 2'- и 3'-нуклеозиды и их применение для получения лекарственного средства для лечения инфекций flaviviridae Download PDFInfo
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Abstract
1. Соединение формулы (IVa):или его фармацевтически приемлемая соль,где основание представляет собой пуриновое или пиримидиновое основание;Rи Rвместе образуют циклический 3',5'-фосфатный эфир;Rпредставляет собой галоген;Yнезависимо представляет собой Н, F, Cl, Br или I.2. Соединение по п.1, где Rпредставляет собой F.3. Фармацевтическая композиция, содержащая эффективное для лечения инфекции Flaviviridae количество соединения или его фармацевтически приемлемой соли по п.1 или 2 в фармацевтически приемлемом носителе.4. Фармацевтическая композиция по п.3, где носитель является подходящим для пероральной доставки.5. Фармацевтическая композиция по п.3, содержащая эффективное для лечения хозяина, инфицированного вирусом Западного Нила, вирусом желтой лихорадки, вирусом денге или BVDV, количество соединения или его фармацевтически приемлемой соли.6. Композиция по п.3, где вирусом Flaviviridae является вирус гепатита С.7. Фармацевтическая композиция по п.3, где соединение или его фармацевтически приемлемая соль представлены в виде стандартной лекарственной формы.8. Композиция по п.7, где стандартная лекарственная форма содержит 0,1-50 мг или 50-1000 мг соединения или его фармацевтически приемлемой соли.9. Композиция по п.7, где указанная стандартная лекарственная форма является таблеткой или капсулой.10. Фармацевтическая композиция по п.3, дополнительно содержащая второй антивирусный агент.11. Фармацевтическая композиция по п.10, где второй антивирусный агент выбран из группы, включающей интерферон, рибавирин, интерлейкин, ингибитор протеазы NS3, ингибитор цистеинпротеазы, фенантренхинон, производный тиазолидин, тиазолидин, бензанилид, ингибитор геликаз
Claims (22)
2. Соединение по п.1, где R7 представляет собой F.
3. Фармацевтическая композиция, содержащая эффективное для лечения инфекции Flaviviridae количество соединения или его фармацевтически приемлемой соли по п.1 или 2 в фармацевтически приемлемом носителе.
4. Фармацевтическая композиция по п.3, где носитель является подходящим для пероральной доставки.
5. Фармацевтическая композиция по п.3, содержащая эффективное для лечения хозяина, инфицированного вирусом Западного Нила, вирусом желтой лихорадки, вирусом денге или BVDV, количество соединения или его фармацевтически приемлемой соли.
6. Композиция по п.3, где вирусом Flaviviridae является вирус гепатита С.
7. Фармацевтическая композиция по п.3, где соединение или его фармацевтически приемлемая соль представлены в виде стандартной лекарственной формы.
8. Композиция по п.7, где стандартная лекарственная форма содержит 0,1-50 мг или 50-1000 мг соединения или его фармацевтически приемлемой соли.
9. Композиция по п.7, где указанная стандартная лекарственная форма является таблеткой или капсулой.
10. Фармацевтическая композиция по п.3, дополнительно содержащая второй антивирусный агент.
11. Фармацевтическая композиция по п.10, где второй антивирусный агент выбран из группы, включающей интерферон, рибавирин, интерлейкин, ингибитор протеазы NS3, ингибитор цистеинпротеазы, фенантренхинон, производный тиазолидин, тиазолидин, бензанилид, ингибитор геликазы, ингибитор полимеразы, аналог нуклеотида, глиотоксин, церуленин, антисмысловой фосфоротиоатный олигодеоксинуклеотид, ингибитор IRES-зависимой трансляции и рибозима.
12. Фармацевтическая композиция по п.11, где вторым антивирусным агентом является интерферон.
13. Фармацевтическая композиция по п.12, где второй антивирусный агент выбран из группы, включающей пэгилированный интерферон 2а, интерферон альфакон-1, природный интерферон, албуферон, интерферон бета-1а, омега-интерферон, интерферон альфа, интерферон гамма, интерферон тау, интерферон дельта и интерферон гамма-1b.
14. Фармацевтическая композиция по п.3, где соединение или его фармацевтически приемлемая соль находится по существу в чистой форме.
15. Фармацевтическая композиция по п.3, где соединение или его фармацевтически приемлемая соль содержит, по меньшей мере, 90 мас.% β-D-изомера.
16. Фармацевтическая композиция по п.3, где соединение или его фармацевтически приемлемая соль содержит, по меньшей мере, 95 мас.% β-D-изомера.
17. Фармацевтическая композиция по п.3, дополнительно содержащая фармацевтически приемлемый носитель, пригодный для пероральной, парентеральной, ингаляционной или внутривенной доставки.
18. Фармацевтическая композиция по п.3, где фармацевтически приемлемая соль выбрана из группы, включающей тозилат, метансульфонат, ацетат, цитрат, малонат, тартрат, сукцинат, бензоат, аскорбат, α-кетоглутарат, α-глицерофосфат, формиат, фумарат, пропионат, гликолят, лактат, пируват, оксалат, малеат, силицилат, сульфат, нитрат, бикарбонат, карбонат, гидробромат, гидрохлорид, дигидрохлорид и соль фосфорной кислоты.
19. Фармацевтическая композиция по п.18, где фармацевтически приемлемой солью является гидрохлоридная соль.
20. Применение соединения или его фармацевтически приемлемой соли по п.1 при получении лекарственного средства для лечения хозяина, инфицированного вирусом Flaviviridae.
21. Применение по п.20, где вирусом является вирус гепатита С.
22. Применение по п.20, где хозяином является человек.
Applications Claiming Priority (8)
Application Number | Priority Date | Filing Date | Title |
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US39235002P | 2002-06-28 | 2002-06-28 | |
US39235102P | 2002-06-28 | 2002-06-28 | |
US60/392,351 | 2002-06-28 | ||
US60/392,350 | 2002-06-28 | ||
US46619403P | 2003-04-28 | 2003-04-28 | |
US60/466,194 | 2003-04-28 | ||
US47094903P | 2003-05-14 | 2003-05-14 | |
US60/470,949 | 2003-05-14 |
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RU2009117156/04A Division RU2437892C2 (ru) | 2002-06-28 | 2003-06-27 | Модифицированные 2- и 3-нуклеозиды и их применение для получения лекарственного средства, обладающего ингибирующей активностью в отношении вируса гепатита с |
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RU2011133741A true RU2011133741A (ru) | 2013-02-20 |
RU2483075C2 RU2483075C2 (ru) | 2013-05-27 |
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