RU2004133811A - Новые соединения - Google Patents

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RU2004133811A
RU2004133811A RU2004133811/04A RU2004133811A RU2004133811A RU 2004133811 A RU2004133811 A RU 2004133811A RU 2004133811/04 A RU2004133811/04 A RU 2004133811/04A RU 2004133811 A RU2004133811 A RU 2004133811A RU 2004133811 A RU2004133811 A RU 2004133811A
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difluorophenyl
pyrido
pyrimidin
methylsulfanylpyrimidine
carbaldehyde
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RU2004133811/04A
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Джеффри К БОЭМ (US)
Джеффри К БОЭМ
Кэтрин Л ВИДДОУСОН (US)
Кэтрин Л ВИДДОУСОН
Джеймс Ф КАЛЛАХАН (US)
Джеймс Ф КАЛЛАХАН
Цзэхун ВАНЬ (US)
Цзэхун ВАНЬ
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Смитклайн Бичам Корпорейшн (US)
Смитклайн Бичам Корпорейшн
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Publication of RU2004133811A publication Critical patent/RU2004133811A/ru

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    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
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    • AHUMAN NECESSITIES
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Claims (7)

1. Соединение, которое представляет собой
8-(2,4,6-трифторфенил)-4-(2,4-дифторфенил)-2-(2-гидрокси-1-гидроксиметилэтиламино)-8Н-пиридо[2,3-d]пиримидин-7-он;
4,8-бис(2,4-дифторфенил)-2-(2-гидрокси-1-гидроксиметилэтиламино)-8Н-пиридо[2,3-d]пиримидин-7-он;
8-(2,4,6-трифторфенил)-4-(2-фторфенил)-2-(2-гидрокси-1-гидроксиметилэтиламино)-8Н-пиридо[2,3-d]пиримидин-7-он;
8-(2,4,6-трифторфенил)-4-(4-фторфенил)-2-(2-гидрокси-1-гидроксиметилэтиламино)-8Н-пиридо[2,3-d]пиримидин-7-он;
4-(2-фторфенил)-8-(2,4-дифторфенил)-2-((S)-2-гидрокси-1-метилэтиламино)-8Н-пиридо[2,3-d]пиримидин-7-он;
4-(2,4-дифторфенил)-8-(4-фторфенил)-2-((S)-2-гидрокси-1-метилэтиламино)-8Н-пиридо[2,3-d]пиримидин-7-он;
4,8-бис(2,4-дифторфенил)-2-(2-гидрокси-1-метилэтиламино)-8Н-пиридо[2,3-d]пиримидин-7-он;
8-(2,4-дифторфенил)-4-(2-хлор-4-фторфенил)-2-(2-гидрокси-1-гидроксиметилэтиламино)-8Н-пиридо[2,3-d]пиримидин-7-он; или
8-(2,3-дифторфенил)-4-(2,4-дифторфенил)-2-(2-гидрокси-1-гидроксиметилэтиламино)-8Н-пиридо[2,3-d]пиримидин-7-он; или его фармацевтически приемлемая соль.
2. Фармацевтическая композиция, включающая эффективное количество соединения по п.1 и фармацевтически приемлемый носитель или разбавитель.
3. Способ лечения заболевания, опосредованного CSBP/RK/p38-киназой, у нуждающегося в этом млекопитающего, включающий введение указанному млекопитающему эффективного количества соединения по п.1.
4. Способ по п.3, где заболеванием, опосредованным CSBP/RK/p38-киназой, является псориатический артрит, синдром Рейтера, подагра, травматический артрит, коревый артрит, острый синовиит, ревматоидный артрит, ревматоидный спондилит, остеоартрит, подагрический артрит и другие связанные с артритом состояния, сепсис, септический шок, эндотоксический шок, грамотрицательный сепсис, синдром токсического шока, церебральная малярия, менингит, ишемический и геморрагический приступ, нейротравма/закрытая рана головы, астма, респираторный дистресс-синдром у взрослых, хронические воспалительные заболевания легких, хронические заболевания, связанные с закупоркой легких, силикоз, легочный саркоидоз, болезни, вызванные резорбцией костей, остеопороз, рестеноз, вызванное реперфузией поражение сердца, мозга и почек, застойная сердечная недостаточность, хирургия шунтированием коронарных артерий (CABG), тромбоз, атеросклероз, гломерулонефрит, хроническая почечная недостаточность, диабет, диабетическая ретинопатия, макулодистрофия, реакция “трансплантат против хозяина”, отторжение аллотрансплантата, воспаление кишечника, болезнь Крона, язвенный колит, нейродегенеративные заболевания, дистрофия мышц, диабетическая ретинопатия, макулодистрофия, рост и метастазирование опухолей, болезнь, связанная с ангиогенезом, вызываемое гриппом воспаление легких, экзема, контактный дерматит, псориаз, солнечный ожог или конъюнктивит.
5. Способ лечения простуды или респираторной вирусной инфекции, вызываемой риновирусом человека (HRV), другими энтеровирусами, коронавирусом, вирусом гриппа, вирусом парагриппа, респираторным синцитиальным вирусом или аденовирусом у нуждающегося в таком лечении человека, включающий введение указанному человеку эффективного количества соединения по п. 1.
6. Способ по п.5, где респираторная вирусная инфекция обостряет астму, обостряет хронический бронхит, обостряет хроническое заболевание, связанное с закупоркой легких, обостряет средний отит, обостряет синусит, или где респираторная вирусная инфекция связана с вторичной бактериальной инфекцией, средним отитом, синуситом или воспалением легких.
7. Соединение, которое представляет собой
4-(2,4-дифторфениламино)-6-(2,4,6-трифторфениламино)-2-метилсульфанилпиримидин-5-карбальдегид;
4-(2,4-дифторфенил)-6-(2,4-дифторфениламино)-2-метилсульфанилпиримидин-5-карбальдегид;
4-(2-фторфенил)-6-(2,4,6-трифторфениламино)-2-метилсульфанилпиримидин-5-карбальдегид;
4-(4-фторфенил)-6-(2,4,6-трифторфениламино)-2-метилсульфанилпиримидин-5-карбальдегид;
4-(2-фторфенил)-6-(2,4-дифторфениламино)-2-метилсульфанилпиримидин-5-карбальдегид;
4-(2,4-дифторфенил)-6-(4-фторфениламино)-2-метилсульфанилпиримидин-5-карбальдегид;
4-(2,4-дифторфенил)-6-(2,4-дифторфениламино)-2-метилсульфанилпиримидин-5-карбальдегид;
4-(2-хлор-4-фторфенил)-6-(2,4-дифторфениламино)-2-метилсульфанилпиримидин-5-карбальдегид; или
4-(2,4-дифторфенил)-6-(2,3-дифторфениламино)-2-метилсульфанилпиримидин-5-карбальдегид.
RU2004133811/04A 2002-04-19 2003-04-18 Новые соединения RU2004133811A (ru)

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US60/374,219 2002-04-19
US38855702P 2002-06-13 2002-06-13
US60/388,557 2002-06-13

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ATE370952T1 (de) 2007-09-15
DE60315826T2 (de) 2008-05-21
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US20060293348A1 (en) 2006-12-28
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EP1499320A1 (en) 2005-01-26
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