RU2448096C2 - Диарилгидантоины - Google Patents

Диарилгидантоины Download PDF

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RU2448096C2
RU2448096C2 RU2007146462/04A RU2007146462A RU2448096C2 RU 2448096 C2 RU2448096 C2 RU 2448096C2 RU 2007146462/04 A RU2007146462/04 A RU 2007146462/04A RU 2007146462 A RU2007146462 A RU 2007146462A RU 2448096 C2 RU2448096 C2 RU 2448096C2
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pharmaceutical composition
hyperproliferative disorder
composition according
pharmaceutically acceptable
treating
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RU2007146462A (ru
RU2448096C3 (ru
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Чарлз Л. СОЙЕРС (US)
Чарлз Л. СОЙЕРС
Майкл Э. ЮНГ (US)
Майкл Э. ЮНГ
Чарли Д. ЧЭН (US)
Чарли Д. ЧЭН
Самеди ОУК (US)
Самеди Оук
Дерек УЭЛСБИ (US)
Дерек УЭЛСБИ
Крис ТРАН (US)
Крис ТРАН
Джон ВОНГВАЙПАТ (US)
Джон ВОНГВАЙПАТ
Донгвон УО (US)
Донгвон УО
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Abstract

Настоящее изобретение относится к новым производным диарилгидантоина, а именно к соединениям формул [RD162], [RD162′] [RD162′′]. Также изобретение относится к фармацевтической композиции на основе указанных соединений, к способу лечения гиперпролиферативного заболевания, основанному на использовании указанных соединений. Технический результат: получены новые производные диарилтиогидантоина, обладающие полезной биологической активностью. 6 н. и 18 з.п. ф-лы, 29 ил., 11 табл., 60 пр.
Figure 00000114
Figure 00000115

Description

Текст описания приведен в факсимильном виде.
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Claims (24)

1. Соединение, выбранное из группы, включающей
Figure 00000111

[RD162]
Figure 00000112

[RD162′] и
Figure 00000113

[RD162′′]
2. Соединение по п.1 формулы
Figure 00000111

[RD162]
3. Соединение по п.1 формулы
Figure 00000112

[RD162′]
4. Соединение по п.1 формулы
Figure 00000113

[RD162′′]
5. Фармацевтическая композиция для лечения гиперпролиферативного нарушения, содержащая терапевтически эффективное количество соединения по любому из пп.1-4 или его фармацевтически приемлемой соли и фармацевтически приемлемые носитель или разбавитель.
6. Фармацевтическая композиция по п.5, которая имеет форму, выбранную из группы, состоящей из раствора, дисперсии, суспензии, порошка, капсулы, таблетки, пилюли, капсулы с замедленным выделением, таблетки с замедленным выделением, пилюли с замедленным выделением.
7. Фармацевтическая композиция по п.5, в которой соединение растворено.
8. Фармацевтическая композиция по п.5, дополнительно содержащая растворитель.
9. Фармацевтическая композиция по п.5, содержащая один или более диметилсульфоксид (ДМСО), полиэтиленгликоль (ПЕГ) и воду.
10. Фармацевтическая композиция по п.5, содержащая диметилсульфоксид (ДМСО), полиэтиленгликоль (ПЕГ) и воду.
11. Способ лечения гиперпролиферативного нарушения, включающий назначение фармацевтической композиции по п.5 субъекту, нуждающемуся в указанном лечении, осуществляя таким образом лечение гиперпролиферативного нарушения.
12. Способ по п.11, в котором композиция назначается с дозой соединения в диапазоне:
(a) около 0,001-100 мг на кг веса тела в день;
(b) около 0,01-100 мг на кг веса тела в день;
(c) около 0,1-10 мг на кг веса тела в день;
(d) около 1 мг на кг веса тела в день.
13. Способ по п.11, в котором композицию вводят внутривенной инъекцией, инъекцией в ткань, внутрибрюшинно, перорально или через нос.
14. Способ по п.11, в котором гиперпролиферативным нарушением является рак простаты.
15. Способ по п.14, в котором гиперпролиферативным нарушением является резистентный к гормонам рак простаты.
16. Фармацевтическая композиция для лечения гиперпролиферативного нарушения, содержащая терапевтически эффективное количество соединения по п.2 или его фармацевтически приемлемой соли, и фармацевтически приемлемый носитель или разбавитель.
17. Фармацевтическая композиция для лечения гиперпролиферативного нарушения, содержащая терапевтически эффективное количество соединения по п.3 или его фармацевтически приемлемой соли, и фармацевтически приемлемый носитель или разбавитель.
18. Фармацевтическая композиция для лечения гиперпролиферативного нарушения, содержащая терапевтически эффективное количество соединения по п.4 или его фармацевтически приемлемой соли, и фармацевтически приемлемый носитель или разбавитель.
19. Фармацевтическая композиция по п.5, в которой гиперпролиферативное нарушение представляет собой рак простаты.
20. Фармацевтическая композиция по п.5, в которой гиперпролиферативное нарушение представляет собой резистентный к гормонам рак простаты.
21. Фармацевтическая композиция по п.5, в которой гиперпролиферативное нарушение представляет собой чувствительный к гормонам рак простаты.
22. Фармацевтическая композиция по п.5, в которой гиперпролиферативное нарушение представляет собой доброкачественную гиперплазию простаты.
23. Фармацевтическая композиция по п.5, в которой гиперпролиферативное нарушение представляет собой рак молочной железы.
24. Фармацевтическая композиция по п.5, в которой гиперпролиферативное нарушение представляет собой рак яичников.
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