RU2013145556A - Применение 3-(5-амино-2-метил-4-оксохиназолин-3(4н)-ил)пиперидин-2,6-диона в лечении иммунных и воспалительных заболеваний - Google Patents
Применение 3-(5-амино-2-метил-4-оксохиназолин-3(4н)-ил)пиперидин-2,6-диона в лечении иммунных и воспалительных заболеваний Download PDFInfo
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Abstract
1. Способ лечения, предотвращения или менеджмента иммунного заболевания или воспалительного заболевания, включающий введение пациенту, нуждающемуся в этом, эффективного количества 3-(5-амино-2-метил-4-оксохиназолин-3(4H)-ил)пиперидин-2,6-диона, или его фармацевтически приемлемой соли, сольвата, гидрата, стереоизомера, таутомера, рацемической смеси, со-кристалла, клатрата или полиморфа.2. Способ по п. 1, где заболевание представляет собой системную красную волчанку, склеродермию, синдром Шегрена, ANCA-индуцированный васкулит, антифосфолипидный синдром или миастению.3. Способ по п. 1 или 2, где заболевание представляет собой системную красную волчанку.4. Способ по п. 1 или 2, где заболевание представляет собой системную красную волчанку в тяжелой форме.5. Способ по п. 1 или 2, где заболевание представляет собой склеродермию.6. Способ по п. 5, где склеродермия представляет собой локализованную, системную, ограниченную или диффузную склеродермию.7. Способ по п. 6, где системная склеродермия включает синдром CREST.8. Способ уменьшения, ингибирования или предотвращения симптома системной красной волчанки, включающий введение эффективного количества 3-(5-амино-2-метил-4-оксохиназолин-3(4H)-ил)пиперидин-2,6-диона или его фармацевтически приемлемой соли, сольвата, гидрата, стереоизомера, таутомера или рацемической смеси пациенту с симптомом системной красной волчанки, где симптом выбирают из группы, состоящей из боли в суставах, опухания суставов, артрита, боли в груди при глубоком вдохе, усталости, лихорадки без видимых причин, общего дискомфорта, беспокойства, выпадения волос, язв в полости рта, увеличения лимфатических узлов, повышенной чувст
Claims (14)
1. Способ лечения, предотвращения или менеджмента иммунного заболевания или воспалительного заболевания, включающий введение пациенту, нуждающемуся в этом, эффективного количества 3-(5-амино-2-метил-4-оксохиназолин-3(4H)-ил)пиперидин-2,6-диона, или его фармацевтически приемлемой соли, сольвата, гидрата, стереоизомера, таутомера, рацемической смеси, со-кристалла, клатрата или полиморфа.
2. Способ по п. 1, где заболевание представляет собой системную красную волчанку, склеродермию, синдром Шегрена, ANCA-индуцированный васкулит, антифосфолипидный синдром или миастению.
3. Способ по п. 1 или 2, где заболевание представляет собой системную красную волчанку.
4. Способ по п. 1 или 2, где заболевание представляет собой системную красную волчанку в тяжелой форме.
5. Способ по п. 1 или 2, где заболевание представляет собой склеродермию.
6. Способ по п. 5, где склеродермия представляет собой локализованную, системную, ограниченную или диффузную склеродермию.
7. Способ по п. 6, где системная склеродермия включает синдром CREST.
8. Способ уменьшения, ингибирования или предотвращения симптома системной красной волчанки, включающий введение эффективного количества 3-(5-амино-2-метил-4-оксохиназолин-3(4H)-ил)пиперидин-2,6-диона или его фармацевтически приемлемой соли, сольвата, гидрата, стереоизомера, таутомера или рацемической смеси пациенту с симптомом системной красной волчанки, где симптом выбирают из группы, состоящей из боли в суставах, опухания суставов, артрита, боли в груди при глубоком вдохе, усталости, лихорадки без видимых причин, общего дискомфорта, беспокойства, выпадения волос, язв в полости рта, увеличения лимфатических узлов, повышенной чувствительности к солнечному свету, сыпи на коже, головной боли, онемения, покалывания, судорог, проблем со зрением, изменений личности, боли в животе, тошноты, рвоты, аномальных сердечных ритмов, кашля с кровью и затрудненного дыхания, неоднородного цвета кожи и синдрома Рейно.
9. Способ уменьшения, ингибирования или предотвращения симптома склеродермии, включающий введение пациенту, имеющему симптом склеродермии, эффективного количества 3-(5-амино-2-метил-4-оксохиназолин-3(4H)-ил)пиперидин-2,6-диона или его фармацевтически приемлемой соли, сольвата, гидрата, стереоизомера, таутомера, рацемической смеси, со-кристалла, клатрата или полиморфа, где симптом выбирают из группы, состоящей из (i) постепенного затвердевания, утолщения и уплотнения кожи; (ii) изменения цвета кожи; (III), онемения конечностей; (iv) блестящей кожи; (v) небольших белых узелков под поверхностью кожи, при разрыве которых вытекает белая как мел жидкость; (vi) дисфункции пищевода Рейно; (vii) телеангиэктазии; (viii) боли и/или ригидности в суставах; (ix) отека рук и ног; (x) кожного зуда; (xi) одеревенения и скручивания пальцев; (xii) язв на внешней стороне некоторых суставов, таких как межфаланговые суставы пальцев и локти; (xiii) проблем с пищеварением, таких как изжога, трудности при глотании, диарея, раздраженный кишечник и запор; (xiv) усталости и слабости; (xv) одышки; (xvi) артрита; (xvii) выпадения волос; (xviii) проблем с внутренними органами; (xix) язв на пальцах или (xx) аутоампутации пальцев.
10. Способ улучшения показателей модифицированной оценки состояния кожи по Роднану, улучшения состояния или уменьшения толщины кожи, улучшения состояния или уменьшения уплотнения кожи, улучшения функции легких, улучшения дерматологического индекса качества жизни, улучшения диффузионной способности для окиси углерода, улучшения индекса одышки по Малеру, улучшения показателя в баллах анкеты больницы святого Георгия при патологии органов дыхания, улучшения показателей оценки состояния желудочно-кишечного тракта согласно консорциуму по клиническим испытаниям склеродермии на базе Калифорнийского университета, улучшения поток-опосредованной дилатации или улучшения или увеличения расстояния в тесте шестиминутной ходьбы для пациента, страдающего склеродермией, включающий введение пациенту эффективного количества 3-(5-амино-2-метил-4-оксохиназолин-3(4H)-ил)пиперидин-2,6-диона или его фармацевтически приемлемой соли, сольвата, гидрата, стереоизомера, таутомера, рацемической смеси, со-кристалла, клатрата или полиморфа.
11. Способ по любому из пп. 1, 8-10, дополнительно включающий введение второго активного вещества, представляющего собой противовоспалительное или иммуномодулирующее соединение.
12. Способ по любому из пп. 1, 8-10, где эффективное количество составляет от примерно 0,005 мг/кг до примерно 10 мг/кг массы тела пациента.
13. Способ модулирования активности B-клетки, включающий создание контакта клетки с эффективным количеством 3-(5-амино-2-метил-4-оксохиназолин-3(4H)-ил)пиперидин-2,6-диона или его фармацевтически приемлемой соли, сольвата, гидрата, стереоизомера, таутомера, рацемической смеси, со-кристалла, клатрата или полиморфа.
14. Способ модулирования активности T-клетки, включающий создание контакта клетки с эффективным количеством 3-(5-амино-2-метил-4-оксохиназолин-3(4H)-ил)пиперидин-2,6-диона или его фармацевтически приемлемой соли, сольвата, гидрата, стереоизомера, таутомера, рацемической смеси, со-кристалла, клатрата или полиморфа.
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| PCT/US2012/028538 WO2012125475A1 (en) | 2011-03-11 | 2012-03-09 | Use of 3-(5-amino-2-methyl-4-oxoquinazolin-3(4h)-yl)piperidine-2-6-dione in treatment of immune-related and inflammatory diseases |
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