RU2406503C2 - Дигидроптеридиноны, предназначенные для лечения раковых заболеваний - Google Patents

Дигидроптеридиноны, предназначенные для лечения раковых заболеваний Download PDF

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RU2406503C2
RU2406503C2 RU2007109109/15A RU2007109109A RU2406503C2 RU 2406503 C2 RU2406503 C2 RU 2406503C2 RU 2007109109/15 A RU2007109109/15 A RU 2007109109/15A RU 2007109109 A RU2007109109 A RU 2007109109A RU 2406503 C2 RU2406503 C2 RU 2406503C2
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Герд МУНЦЕРТ (DE)
Герд Мунцерт
Мартин ШТЕГМАЙЕР (DE)
Мартин Штегмайер
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Abstract

Изобретение относится к области фармакологии и медицины и касается применения соединений общей формулы (1) для лечения заболеваний, характеризующихся аномальной пролиферацией клеток в организме человека или млекопитающего, не являющегося человеком, путем ингибирования polo-подобных киназ, как регуляторов митоза. Изобретение предоставляет высокоактивные противоопухолевые средства. 7 з.п. ф-лы, 2 табл.

Description

Текст описания приведен в факсимильном виде.
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Claims (7)

1. Применение соединения формулы (I)
Figure 00000102

в котором соединение выбрано из группы соединений, приведенных в представленной ниже таблице
Figure 00000103
     Пример R1 R2 Конфигурация R1 или R2 R3 R4 Ln-R5 m

27 Н
Figure 00000104
 R
Figure 00000105
Figure 00000106
Figure 00000107
 44 Н
Figure 00000104
 R
Figure 00000108
 Н
Figure 00000109
 46 Н
Figure 00000104
 R
Figure 00000108
Figure 00000110
Figure 00000109
 55 Н
Figure 00000104
 R
Figure 00000108
Figure 00000111
Figure 00000112
 58 Н
Figure 00000104
 R
Figure 00000108
Figure 00000111
Figure 00000113
 102 Н
Figure 00000104
 R
Figure 00000105
Figure 00000111
Figure 00000114
 103 Н
Figure 00000115
 R
Figure 00000108
Figure 00000111
Figure 00000114
 105 Н
Figure 00000115
 R
Figure 00000108
Figure 00000106
Figure 00000116

110 Н
Figure 00000104
 R
Figure 00000105
Figure 00000106
Figure 00000116
 115 Н
Figure 00000115
 R
Figure 00000117
Figure 00000111
Figure 00000118
 133 Н
Figure 00000104
 R
Figure 00000108
Figure 00000106
Figure 00000107
 134 Н
Figure 00000104
 R
Figure 00000108
Figure 00000106
Figure 00000119
 234 Н
Figure 00000120
 R
Figure 00000105
Figure 00000106
Figure 00000121
 240 Н
Figure 00000122
 R
Figure 00000117
Figure 00000111
Figure 00000123

где обозначения X1, X2, Х3, Х4 и Х5, использованные в таблице, в каждом случае обозначают связывание в положении в общей формуле, приведенной в таблице, а не соответствующие группы R1, R2, R3, R4 и L-R5, необязательно в форме его рацематов и необязательно в форме его фармакологически приемлемых солей присоединения с кислотами, сольватов или гидратов, для приготовления фармацевтической композиции, предназначенной для лечения заболеваний, характеризующихся аномальной пролиферацией клеток в организме человека или млекопитающего, не являющегося человеком, путем ингибирования polo-подобных киназ, как регуляторов митоза.
2. Применение по п.1, в котором polo-подобной киназой является ППК-1.
3. Применение по п.1 или 2, характеризующееся тем, что заболевание характеризуется неприемлемой пролиферацией, миграцией, апоптозом или ангиогенезом клеток.
4. Применение по любому из пп.1-3, характеризующееся тем, что заболеванием является рак, выбранный из группы, включающей карциномы, саркомы, меланомы, миелому, опухоли кроветворной системы, лимфомы и раковые заболевания детей.
5. Применение по п.4, характеризующееся тем, что раком является лейкоз.
6. Применение по любому из пп.1-5, характеризующееся тем, что заболеванием является рак, выбранный из группы, включающей смешанные опухоли, недифференцированные опухоли и их метастазы.
7. Применение по любому из пп.1-6, в котором активный ингредиент вводят перорально, энтерально, чрескожно, внутривенно, внутрибрюшинно или путем инъекции.
RU2007109109/15A 2004-08-14 2005-08-09 Дигидроптеридиноны, предназначенные для лечения раковых заболеваний RU2406503C2 (ru)

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